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PST Level 5 Semester 2

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05210 Basic Pharmacognosy

Introduction to Volatile Oils and Resins – PST05210 Basic Pharmacognosy

NTA Level 5 • Semester 2 • PST05210 Introduction to Volatile Oils and Resins Basic Pharmacognosy • Source Session/Topic 30 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 30: Introduction to Volatile Oils and Resins Total Session Time: 120 minutes Prerequisites None Learning Tasks By the end of this session students are expected to be able to: • List characteristics of volatile oils • Describe the composition of volatile oils • Classify volatile oils • Describe extraction of volatile oils • List therapeutic uses of volatile oils Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board and chalk/whiteboard markers • LCD Projector and Laptop SESSION OVERVIEW |Step |Time |Activity/ |Content | | | |Method | | |1 |05 minutes |Presentation |Introduction, Learning Tasks | |2 |25 minutes |Presentation |Characteristics of Volatile Oils | | | | |and Resins | |3 |20 minutes |Presentation |Composition of Volatile Oils | | | |Brainstorm | | |4 |15 minutes |Presentation |Classification of Volatile Oils | |5 |30 minutes |Presentation |Extraction of Volatile Oils | |6 |15 minutes |Presentation |Therapeutic Uses of Volatile Oils | | | |Small group | | |7 |05 minutes |Presentation |Key Points | | 8|05 minutes |Presentation |Evaluation | SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Characteristics of Volatile Oils (25 minutes) • Volatile oils, also known as essential oils, are concentrated, odoriferous liquids that entirely or almost entirely volatile in steam • Volatile oils are referred to as "essential" in the sense that they carry a distinctive scent, or essence of the plant • Essential oils do not as a group need to have any specific chemical properties in common, beyond conveying characteristic fragrances (Essential oils should not be confused with essential fatty acids) • Volatile oil originates from plants, possess a unique odour or flavour, mainly used in perfumes and flavourings • Essential oils have the following general characteristics o They evaporate under atmospheric pressure at room temperature o They are soluble in alcohol and other organic solvents o They are insoluble in water o They have high refractive index o They are optically active o Most of them are colourless or pale yellow o They are odoriferous o They are sensitive to air (resinify on exposure to air) o Most of them are terpenoid in nature • Resins o Resins are hydrocarbon secretions of many plants, more or less solid amorphous products of complex chemical nature o Resin produced by most plants is a viscous liquid o Resins may be associated with volatile oils or gum or may be found in irregular masses which are insoluble in water but soluble in alcohol o Resins, oleoresins (resins associated with oils) and gum resins (resins associated with gums) are usually secreted into secretory cavities or ducts STEP 3: Composition of Volatile Oils (20 minutes) |Activity: Brainstorming (10 minutes) | | | |DIVIDE students into small manageable groups | | | |ASK students to discuss on the following question | | | |What is composition of volatile oils? | | | |ALLOW students to discuss for 15 minutes | | | |ALLOW few groups to present and the rest to add points not | |mentioned | | | |CLARIFY and SUMMARIZE by using the contents below | • Volatile oils are chemically derived from terpenes (mainly from mono and sesqui terpenes) o Terpenoids are hydroxycarbons of plant origin with general formula (C5H8) n i.e. isoprene units o Terpenoids are naturally occurring and give plants and flowers their fragrance • Many oils are terpenoid in origin, some oils such as cinnamon and clove contain principally aromatic (benzene) derivatives mixed with terpenes • With the exception of oils derived from glycosides (e.g. bitter almond oil and mustard oil), volatile oils are mixtures of hydrocarbons and oxygenated compounds derived from these hydrocarbons • Some oils are acyclic, aromatic or contain sulphur or nitrogen • In some oils (e.g. Oil of turpentine) the hydrocarbons predominate and only limited amount of oxygenated constituents are present, other volatile oils (e.g. Oil of cloves) the bulk of the oil consists of oxygenated compounds STEP 4: Classification of Volatile Oils (15 minutes) • Volatile oils can be classified based on extraction method into; o Concretes ▪ Uses solvent e.g. hexane and waxes or resins to contact the plant materials and then the solvent removed by gent heating e.g. jasmine oil o Pomades ▪ Obtained by enfleurage (hot or cold) e.g. oils from flowers o Resinoids ▪ Extraction with resinous materials i.e. to prolong effect of fragrance o Absolutes ▪ Remains after alcoholic extraction from pomades or concretes • Volatile can be classified on the basis of their functional groups into; o Hydrocarbon volatile oils e.g. turpentine o Alcoholic volatile oils e.g. peppermint, cardamom and coriander oils o Aldehydic volatile oils e.g. lemon oil, orange oil, cinnamon o Ketonic volatile oils e.g. camphor, spearmint oils o Phenolic volatile oils e.g. clove, anise, nutmeg oils o Phenolic ether volatile oils e.g. fennel oil o Oxide volatile oils e.g. rosemary oil STEP 5: Extraction of Volatile Oils (30 minutes) • The following methods are used as general extractions for volatile oils; o Distillation ▪ Water (Simple) distillation (for dry plant materials, materials not destroyed by boiling e.g. turpentine oil) ▪ Water and steam distillation (for dry plant materials not destroyed by direct heating e.g. clove and cinnamon oils) ▪ Steam distillation (for fresh plant materials e.g. peppermint and spearmint oils) • Simple steam distillation • Saturated steam distillation • Hydrodifusion o Scarification ▪ Sponge extraction ▪ Ecuelle method ▪ Enzymatic hydrolysis o Soxhlet extraction o Solvent extraction ▪ Extraction by non-volatile solvents • Enfleurage (hot or cold) • Maceration • Spraying or pneumatic method o Extraction by

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05210 Basic Pharmacognosy

Anthraquinone Glycosides – PST05210 Basic Pharmacognosy

NTA Level 5 • Semester 2 • PST05210 Anthraquinone Glycosides Basic Pharmacognosy • Source Session/Topic 29 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 29: Anthraquinone Glycosides Total Session Time: 120 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Define anthraquinone glycosides • Explain natural sources and uses of Senna • Explain natural sources and uses of Cascara • Explain natural sources and uses of Aloe • Explain natural sources and uses of Rhubarb Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board and chalk/whiteboard markers • LCD Projector and Laptop SESSION OVERVIEW |Step |Time |Activity/ |Content | | | |Method | | |1 |5 minutes |Presentation |Introduction, Learning Tasks | |2 |20 minutes |Presentation |Introduction to Anthraquinone | | | | |Glycosides | |3 |20 minutes |Presentation |Natural Sources and Uses of Senna | |4 |20 minutes |Presentation |Natural Sources and Uses of | | | | |Cascara | |5 |25 minutes |Buzzing |Natural Sources and Uses of Aloe | | | |Presentation | | |6 |20 minutes |Presentation |Natural Sources and Uses of | | | | |Rhubarb | |7 |5 minutes |Presentation |Key Points | |8 |5 minutes |Presentation |Evaluation | SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Introduction to Anthraquinone Glycosides (20 minutes) • Are glycosides in which the aglycone portion contains an anthracene ring structure and attached to glycone portion • They are found in drugs such as cascara, rhubarb, senna, aloes • They are used as cathartics or stimulant laxative • They act by increasing the tone of the smooth muscle in the walls of the colon and stimulate the secretion of water and electrolytes STEP 3: Natural Sources and Uses of Senna (20 minutes) • Definition o Senna consists of the dried leaflets of Casssia senna (Alexandrian senna) and Cassia angustifolia (Tinnevelly senna), family Fabaceae (Leguminosae) o Cassia senna is indigenous to tropical Africa and is cultivated in Sudan o Cassia angustifolia is indigenous to Somaliland, Arabia, Pujab and is cultivated in South India • Constituents o The basic constituents of senna are the anthraquinone glycosides; ▪ Sennoside A ▪ Sennoside B o Other constituents include; ▪ Aloe-emodin ▪ Rhein • Uses o Laxative ▪ Senna is a useful purgative either for habitual constipation or on occasional use ▪ Senna increases the peristaltic movements of the colon by its local action upon the intestinal wall STEP 4: Natural Sources and Uses of Cascara (20 minutes) • Definition o Cascara consists of the dried bark of Rhamnus purshianus, family Rhamnaceae o Requires long storage to destroy compounds called anthrones in the fresh bark, which cause vomiting • Constituents o Cascaroside A o Cascaroside B o Cascaroside C o Cascaroside D o Tannins o Volatile oils • Uses o Purgative ▪ Used in the form of liquid extract/elixir/as tablets prepared from dry extract STEP 5: Natural Sources and Uses of Aloe (25 minutes) |Activity: Buzzing (5 minutes) | | | |ASK students to pair up and buzz on the following question for 2 | |minutes | | | |What are Aloes? | | | |ALLOW few pairs to respond and let other pairs to add on points not| |mentioned | | | |WRITE their response on the flip chart/board | | | |CLARIFY and SUMMARIZE by using the content below | • Definition o Aloes consists of a solid residue obtained by evaporating the liquid which drains from the transversely cut leaves of various species of aloe, family Liliaceae o The species that yield aloe are: ▪ Aloe barbadensis ▪ Aloe ferox ▪ Aloe perryi ▪ Aloe vera • Constituents o The most important constituents of Aloes are the two Aloins: ▪ Barbaloin ▪ Isobarbaloin • Barbaloin is the major constituent of the plant o Other constituents are resins and Aloe-emodin • Uses o Stimulant purgative o Anthelminthic STEP 6: Natural Sources and Uses of Rhubarb (20 minutes) • Definition o Rhubarb consists of the dried underground parts of Rheum palmatum or R. officinale, family Polygonaceae • Constituents o Rhubarb contains free anthraquinone ▪ Rhein ▪ Emodin ▪ Aloe-emodine ▪ Emodin monomethylether • Uses o Rhubarb can be used as a strong laxative o Rhubarb has an astringent effect on the mucous membranes of the mouth and the nasal cavity STEP 7: Key Points (5 minutes) • Anthraquinones are glycosides in which the aglycone portion contains an anthracene ring structure and attached to glycone portion • Anthraquinone glycosides are obtained from sources including cascara, rhubarb, senna, aloes • Anthraquinone glycosides are generally used as cathartics or laxatives STEP 8: Evaluation (5 minutes) • What are the therapeutic uses of Rhubarb? • What are the constituents of Senna leaf? • Mention the uses of aloe vera? References Trease, G. E., Evans, W. C., & Evans, D. (2009). Trease and Evans pharmacognosy. London: Saunders. Joanne Barnes et al (2002), Herbal medicines 3rd Edition: Pharmaceutical Press Wallis, T. E. (2005). Textbook of pharmacognosy. New Delhi: CBS. Robbers, J. E., Speedie, M. K., Tyler, V. E., & Tyler, V. E. (1996). Pharmacognosy and pharmacobiotechnology. Baltimore: Williams & Wilkins. Heinrich, M., Kinghorn, A. D., Maizels, D., Gibbons, S., & Phillipson, J. D. (2012). Fundamentals of pharmacognosy and phytotherapy. Edinburgh: Churchill Livingstone/Elsevier. ← Previous TopicNext Topic →View all Basic Pharmacognosy topicsOpen Complete Full Notes PDF / OFFLINE NOTES Unataka kutumiwa notes hizi kupitia WhatsApp?Kwa notes zilizopangiliwa vizuri kwa kusoma offline au PDF, bonyeza kitufe hapa chini. Ujumbe wenye Level, Semester, Module na Topic utaandaliwa moja kwa moja.TUMIWA NOTES WHATSAPP WhatsApp: 255620339260

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05210 Basic Pharmacognosy

Cardiac Glycosides – PST05210 Basic Pharmacognosy

NTA Level 5 • Semester 2 • PST05210 Cardiac Glycosides Basic Pharmacognosy • Source Session/Topic 28 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 28: Cardiac Glycosides Total Session Time: 120 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Define cardiac glycosides • List properties of cardiac glycosides • Mention natural sources of cardiac glycosides • Explain mechanisms of action • Differentiate types of cardiac glycosides • Explain chemical tests for cardiac glycosides • Mention general uses of cardiac glycoside Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board and chalk/whiteboard markers • LCD Projector and Lapatop SESSION OVERVIEW |Step |Time |Activity/ |Content | | | |Method | | |1 |5 minutes |Presentation |Introduction, Learning Objectives | |2 |30 minutes |Presentation |Properties of Cardiac Glycosides | |3 |60 minutes |Presentation |Sources, Constituents and Uses of | | | | |Selected Cardiac Glycosides | |4 |15 minutes |Presentation |Mechanism of Action for Cardiac | | | | |Glycosides | |5 |5 minutes |Presentation |Key Points | |6 |5 minutes |Presentation |Evaluation | SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Properties of Cardiac Glycosides (30 minutes) • Cardiac glycosides are a group of glycosides with powerful action on cardiac muscles (positive ionotropic effect on the heart) • Cardiac glycosides are also made up of aglycone and glycone moities • The Glycone part o consists of one or more monosaccharide units o contains a steroid nucleus and a lactone ring • The Aglycone part o has steroidal nucleus o is always attached at C-3 position of aglycone part • There are two groups of cardiac glycosides; o Cardenolides ▪ The cardenolides have an unsaturated butyrolactone ring –a five membered-ring e.g. strophanthus o Bufadienolides ▪ In this group the lactone ring is a 6 membered (pyrrone) ring ▪ These are obtained from animal sources e.g. Bufadieonolides from toads • Characteristics of Cardiac Glycosides; o Amorphous o Odorless o Bitter tasting o Soluble in water o Insoluble in organic solvents o Very toxic compounds • Chemical tests for cardiac glycosides o Keller Kilian test ▪ Cardiac glycoside + CH3COOH + H2SO4 + FeCl3, produces brown colour o Legal test ▪ Cardiac glycoside + pyridine Sodium Nitroprusside, produces red to pink colour STEP 3: Sources, Constituents and Uses of Selected Cardiac Glycosides (60 minutes) • Digitalis o Definition ▪ Digitalis consists of dried leaves of Digitalis lanata or Digitalis purpurea (common name purple fox glove), family Scrophulariaceae ▪ Digitalis – finger-like corolla ▪ Purpurea – purple colour o Constituents ▪ D. purpurea produces primary glycosides • Purpurea glycoside A • Purpurea glycoside B • Glucogitaloxin ▪ On drying, enzyme degradation taken place with the loss of the terminal glucose to produce; • Digitoxin from purpurea glycoside A • Gitoxin from purpurea glycoside B • Gitaloxin o D. lanata produces ▪ Digoxin ▪ Lanatosides A, B and C • During drying: acetyl terminal sugar can be lost • Deacetylation produces primary glycosides as those produced by Digitalis purpurea • Lanatoside A produces Purpurea glycoside A • Lanatoside B produces Purpurea glycoside B • Lanatoside C produces Deslanoside C/ Deacetyllanatoside o Uses of digitalis ▪ Digitalis glycosides are used for the treatment of; • Congestive Heart Failure (CHF) • Arrhythmias • Atrial fibrillations • Squill o Definition ▪ Squill consists of the dried sliced bulbs of Urgenea maritima, from which the membrenous outer scales have been removed (family Liliaceae) ▪ The common name for squill is “sea onion” ▪ There are two types of squill; red squill and white squill o Constituents ▪ Squill contains the glycosides; • Scillaren A o Which is crystalline in form • Scillaren B o An amorphous mixture of glycosides • The red squill contains Scillirosides in addition to the other glycosides o Uses ▪ White squill • As cardiotonic drugs • As diuretics agents • In small dose –as expectorant agents • In large dose –as emetic agents ▪ Red squill • Used as a rodenticide (due to Scillirosides) • Strophanthus o Definition ▪ Consist of the dried ripe seed of Strophanthus kombe/strophanthus hispidus, family apocynaceae o Constituents ▪ Mixture of glycosides • K-strophanithin, erysimoside, K strophanthoside and cymarin • Fixed oils, resins and mucilage are also present • K-strophanthosides; o Composed of the genin strophanthidin o Coupled to a trissaccharide with cymarose, β-glucose and α-glucose o Are short-acting cardiac glycosides STEP 4: Mechanism of Action for Cardiac Glycosides (15 minutes) • Cardiac glycosides act by; o Inhibition of Na+/K+ ATPase of the cardiac cells, which increases the intracellular Na+ ions levels o The increased Na+ ion levels within the cardiac cells inhibits the Na+/Ca2+ exchanger, this in turn, results in increased concentrations of Ca2+ within the cardiac cells o The increased intracellular Ca2+ increases contractile force of the cardiac muscles [pic] STEP 5: Key Points (5 minutes) • Cardiac glycosides are glycosides with powerful positive inotropic action on cardiac muscles • Digitalis consists of dried leaves of Digitalis lanata or Digitalis purpurea • Digoxin is obtained from Digitalis lanata • Digitalis glycosides are used for the treatment of heart conditions including congestive heart failure (CHF), arrhythmias and atrial fibrillations STEP 10: Evaluation (5 minutes) • What is the source of digoxin? • What is the main use of digoxin? • What is strophanthus? References Trease, G. E., Evans, W. C., & Evans, D. (2009). Trease and Evans pharmacognosy. London: Saunders. Joanne Barnes et al (2002), Herbal medicines 3rd Edition: Pharmaceutical Press Wallis, T. E. (2005). Textbook of pharmacognosy. New Delhi: CBS. Robbers, J. E., Speedie, M. K., Tyler, V. E., & Tyler, V. E. (1996). Pharmacognosy and pharmacobiotechnology. Baltimore: Williams & Wilkins. Heinrich, M., Kinghorn, A.

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05210 Basic Pharmacognosy

Introduction of Glycosides – PST05210 Basic Pharmacognosy

NTA Level 5 • Semester 2 • PST05210 Introduction of Glycosides Basic Pharmacognosy • Source Session/Topic 27 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 27: Introduction of Glycosides Total Session Time: 60 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Explain the meaning of glycosides • List the characteristics of glycosides • Classify glycosides • List functions of glycosides in the plants Resources Needed • Flip charts, marker pens, and masking tape • Black/white board and chalk/whiteboard markers • LCD projector and Laptop SESSION OVERVIEW |Step |Time |Activity/ |Content | | | |Method | | |1 |05 Minutes |Presentation |Introduction, Learning Tasks | |2 |15 Minutes |Presentation |Meaning and Characteristics of | | | | |Glycosides | |3 |30 Minutes |Presentation |Classification of Glycosides | |4 |05 Minutes |Presentation |Key Points | | 5|05 Minutes |Presentation |Evaluation | SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Meaning and Characteristics of Glycosides (15 minutes) |Activity: Brainstorming (5 minutes) | | | |Ask students to brainstorm on the following question: | | | |What is a glycoside? | | | |ALLOW few students to respond | | | |WRITE their responses on the flip chart/ board | | | |CLARIFY and SUMMARIZE by using the content below | ← Glycosides are molecules in which a sugar part (sugar moiety called the glycone) is bound to a non-sugar part (non-sugar moiety called the aglycone) joined together by glycosidic bond ← Glycosides play numerous important roles in living organisms ← Many plants store important chemicals in the form of inactive glycosides ← Many such plant glycosides are used as medications ← Characteristics of glycosides include; o Glycosides are soluble in water but insoluble in organic solvents ▪ The glycone part is water soluble but insoluble in the organic solvents ▪ The aglycone part is water insoluble but soluble in the organic solvents ▪ Some glycosides are soluble in alcohol o Glycosides are ccolorless (except flavonoid- yellow, anthraquinone-red or orange) o They are solid, amorphous and nonvolatile o They give a positive reaction with Molisch's and Fehling's solution test (after hydrolysis). o Most glycosides have bitter taste o They are oodorless except saponin (glycyrrhizin). o Glycosides with lots of sugars have increased solubility in water o Glycosides hydrolyzed by using mineral acids and temperature or by using enzymes STEP 3: Classification of Glycosides (30 minutes) ← Glycosides can be classified base on the following basis: o Based on therapeutic effects ▪ Cardiac glycosides, Laxative glycosides etc. o Based on glycone moiety ▪ Rhamnosides, glucorhamnosides, rhamnoglucosides etc. o Based on glycosidic linkage/bond ▪ O-glycosides, s-glycosides, N-glycosides, C-glycosides o Based on chemical nature of the aglycone ▪ Alcoholic and phenolic glycosides ▪ Anthraquinone glycosides ▪ Coumarin glycosides ▪ Cyanogenic glycosides ▪ Flavanoidal glycosides ▪ Steroidal glycosides ▪ Thioglycosides STEP 4: Key Points (5 minutes) ← Glycosides are made up of a glycone and aglycone moieties ← Glycosides are water soluble ← Glycosides are hydrolysed by acids, bases and acids into their components STEP 5: Evaluation (5 minutes) ← What is a glycoside? ← What are characteristics of glycosides ← What are the classes of glycosides References: Gleadow, RM; Møller, BL (2014). "Cyanogenic glycosides: synthesis, physiology, and phenotypic plasticity". Annual Review of Plant Biology. 65: 155–85. doi:10.1146/annurev-arplant-050213- 040027. PMID 24579992. Sun, Hong-Xiang; Xie, Yong; Ye, Yi-Ping (2009). "Advances in saponin-based adjuvants". Vaccine. 27 (12): 1787–1796. doi:10.1016/j.vaccine.01.091. Trease, G. E., Evans, W. C., & Evans, D. (2009). Trease and Evans pharmacognosy. London: Saunders. Joanne Barnes et al (2002), Herbal medicines 3rd Edition: Pharmaceutical Press Wallis, T. E. (2005). Textbook of pharmacognosy. New Delhi: CBS. Robbers, J. E., Speedie, M. K., Tyler, V. E., & Tyler, V. E. (1996). Pharmacognosy and pharmacobiotechnology. Baltimore: Williams & Wilkins. Heinrich, M., Kinghorn, A. D., Maizels, D., Gibbons, S., & Phillipson, J. D. (2012). Fundamentals of pharmacognosy and phytotherapy. Edinburgh: Churchill Livingstone/Elsevier. ← Previous TopicNext Topic →View all Basic Pharmacognosy topicsOpen Complete Full Notes PDF / OFFLINE NOTES Unataka kutumiwa notes hizi kupitia WhatsApp?Kwa notes zilizopangiliwa vizuri kwa kusoma offline au PDF, bonyeza kitufe hapa chini. Ujumbe wenye Level, Semester, Module na Topic utaandaliwa moja kwa moja.TUMIWA NOTES WHATSAPP WhatsApp: 255620339260

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05210 Basic Pharmacognosy

Proto alkaloids – PST05210 Basic Pharmacognosy

NTA Level 5 • Semester 2 • PST05210 Proto alkaloids Basic Pharmacognosy • Source Session/Topic 26 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 26: Proto alkaloids Total Session Time: 60 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Define proto-alkaloids • Explain natural source and uses of proto-alkaloids Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board and chalk/whiteboard markers • LCD Projector and Laptop SESSION OVERVIEW |Step |Time |Activity/ |Content | | | |Method | | |1 |05 minutes |Presentation |Introduction, Learning Objectives | |2 |10 minutes |Brainstorming |Introduction to Proto-alkaloids | | | |Presentation | | |3 |35 minutes |Presentation |Natural Sources of Proto-alkaloids| |4 |05 minutes |Presentation |Key Points | |5 |05 minutes |Presentation |Evaluation | SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Introduction to Proto-alkaloids (10 minutes) |Activity: Brainstorming (3 minutes) | | | |Ask students to brainstorm on the following question: | | | |What are the characteristics of proto-alkaloids? | | | |ALLOW few students to respond | | | |WRITE their responses on the flip chart/ board | | | |CLARIFY and SUMMARIZE by using the content below | • Proto-alkaloids do not have nitrogen as part of the heterocyclic ring • Proto-alkaloids include ephedrine adrenaline, • Both cause dilation of the bronchi, increase heart rate and peripheral vasoconstriction STEP 3: Natural Sources of Proto-alkaloids (35 minutes) • Ephedra o Ephedra is a protoalkaloid obtained from dried young stems of Ephedra gerardiana and Ephedra nebrodensis, family Ephedraceeae o Its synonym is Ma-Huang o Constituents ▪ Ephedrine ▪ Nor-ephedrine ▪ Pseudoephidrine ▪ N-methylephedrine o Uses ▪ Included in asthma, colds, flu and Hayfever medications • It is a bronchodilator • Action is more prolonged than adrenaline • Need not be given by injection, but can be administered orally • Allopathic: Sinumed (dries a runny nose) • Used as an anti-inflammatory. • Used for weight loss • Increases metabolism • Decreases appetite • CNS stimulant – acts on adrenergic receptors • Colchicum o Colchicum is the dried ripe seeds of Colchicum luteum and Colchicum autumnale. o Family: Liliaceae o Constituents ▪ Colchicine (main constituent) ▪ Demecolcine o Uses ▪ Relieves gout (used with caution – professional supervision) ▪ Also used in biological experiments to produce polyploidy (multiplication of the chromosomes in a cell nucleus) in horticulture and cultivation of medicinal plants STEP 4: Key Points (5 minutes) • Proto-alkaloids do not have nitrogen as part of the heterocyclic ring • Ephedra is a protoalkaloid obtained from dried young stems of Ephedra gerardiana and Ephedra nebrodensis • Ephedrine is a bronchodilator which is included in asthma, colds, flu and hay fever medications STEP 5: Evaluation (5 minutes) • What is the natural source of Ephedra? • What are the uses of ephedrine? References Trease, G. E., Evans, W. C., & Evans, D. (2009). Trease and Evans pharmacognosy. London: Saunders. Joanne Barnes et al (2002), Herbal medicines 3rd Edition: Pharmaceutical Press Wallis, T. E. (2005). Textbook of pharmacognosy. New Delhi: CBS. Robbers, J. E., Speedie, M. K., Tyler, V. E., & Tyler, V. E. (1996). Pharmacognosy and pharmacobiotechnology. Baltimore: Williams & Wilkins. Heinrich, M., Kinghorn, A. D., Maizels, D., Gibbons, S., & Phillipson, J. D. (2012). Fundamentals of pharmacognosy and phytotherapy. Edinburgh: Churchill Livingstone/Elsevier. ← Previous TopicNext Topic →View all Basic Pharmacognosy topicsOpen Complete Full Notes PDF / OFFLINE NOTES Unataka kutumiwa notes hizi kupitia WhatsApp?Kwa notes zilizopangiliwa vizuri kwa kusoma offline au PDF, bonyeza kitufe hapa chini. Ujumbe wenye Level, Semester, Module na Topic utaandaliwa moja kwa moja.TUMIWA NOTES WHATSAPP WhatsApp: 255620339260

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05210 Basic Pharmacognosy

Purine Alkaloids – PST05210 Basic Pharmacognosy

NTA Level 5 • Semester 2 • PST05210 Purine Alkaloids Basic Pharmacognosy • Source Session/Topic 25 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 25: Purine Alkaloids Total Session Time: 60 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Define purine alkaloids • Explain natural sources and uses of alkaloids Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board and chalk/whiteboard markers • LCD Projector and laptop SESSION OVERVIEW |Step |Time |Activity/ |Content | | | |Method | | |1 |05 minutes |Presentation |Introduction, Learning Tasks | |2 |15 minutes |Presentation |Introduction to Purine Alkaloids | |3 |30 minutes |Presentation/ |Natural Sources and Uses of | | | |Brainstorming |Alkaloids | |4 |05 minutes |Presentation |Key Points | |5 |05 minutes |Presentation |Evaluation | SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Introduction to Purine Alkaloids (15 minutes) • Purine alkaloids are derivatives of Xanthines • They have amphoteric character • They exhibit peculiar solubility in warm water and in chlorinated solvents • These alkaloids include caffeine (seeds of coffee plants, kola plants, tea leaves and guarana seeds), theobromine (Theobroma cocao) and theophylline (tea leaves and cola nuts) • The stimulant action in beverages such as tea and coffee is due to the purine alkaloids • Caffeine (1, 3, 7-trimethylxanthine) stimulates CNS and has a weak diuretic action. • Theobromine (3,7-dimetylxanthine) produce opposite action to that of Caffeine • Theophylline (1,3-dimetylxanthine) relaxes involuntary muscles more effectively than caffeine or theobromine STEP 3: Natural Sources and Uses of Alkaloids (30 minutes) • Cocoa o Cocoa consists of seeds of Theobroma cacao, family sterculiaceae o Cocoa is produced in South America (Ecuador, Columbia, Venezuela), West Indies and West Africa (Nigeria, Ghana and Java) o Cocoa kernels contain 0.9 – 3% theobromine and the husk 0.19- 2.98% of this alkaloid o The seed also contains 0.05 – 0.36% caffeine, cocoa fat/butter, condensed tannins and volatile compounds o Main constituents are Theobromine and Theophyllline o Uses ▪ Theobromine is used • As base for suppositories (cocoa butter) • For heart and kidney tonic • As a drink e.g. cocoa • As flavouring agent e.g. chocolate ▪ Theophylline • Relaxes bronchial smooth muscles • Stimulates respiratory centre in the brain stem by increasing sensitivity to CO2 • Stimulates the CNS • Slightly inotropic • Diuretic activity is stronger than that of caffeine • Used for relief of cough (bronchodilator) • Smooth muscle relaxant for symptomatic relief/prevention of bronchial asthma • Treatment of reversible bronchospasm associated with chronic bronchitis and emphysema • Coffee o Coffee consists of seeds of coffea arabica and other species of coffee, family rubiaceae o Constituents: ▪ Caffeine, tannins, Nicotinic acid, fixed oils and chlorogenic acid ▪ Caffeine eenhances alertness, ffacilitates thought formation and decreases the sensation of fatigue. At high doses caffeine induces nervousness, insomnia and tremors. o Another source of caffeine is Tea, which consists of prepared leaves of Thea sinensis/Camellia sinensis |Activity: Brainstorming (5 minutes) | | | |Ask students to brainstorm on the following question: | | | |What are the uses of Caffeine? | | | |ALLOW few students to respond | | | |WRITE their responses on the flip chart/ board | | | |CLARIFY and SUMMARISE by using the content below | o Uses ▪ Coffee produce caffeine which is used in combinations with antipyretics and analgesics, cold and flu medication (increases the intestinal absorption of some of these drugs or to counteract drowsiness) ▪ Caffeine is also used as an ingredient in non-alcoholic beverages and “energizing” beverages STEP 4: Key Points (5 minutes) • Purine alkaloids are derivatives of xanthines • Purine alkaloids exhibit peculiar solubility in warm water • Main constituents of cocoa are Theobromine and Theophyllline • Cocoa butter is used a suppository base STEP 5: Evaluation (5 minutes) • Mention the cardiovascular use of caffeine • What are the pharmacological uses of Theophylline? • What are the uses of Theobromine? References Trease, G. E., Evans, W. C., & Evans, D. (2009). Trease and Evans pharmacognosy. London: Saunders. Joanne Barnes et al (2002), Herbal medicines 3rd Edition: Pharmaceutical Press Wallis, T. E. (2005). Textbook of pharmacognosy. New Delhi: CBS. Robbers, J. E., Speedie, M. K., Tyler, V. E., & Tyler, V. E. (1996). Pharmacognosy and pharmacobiotechnology. Baltimore: Williams & Wilkins. Heinrich, M., Kinghorn, A. D., Maizels, D., Gibbons, S., & Phillipson, J. D. (2012). Fundamentals of pharmacognosy and phytotherapy. Edinburgh: Churchill Livingstone/Elsevier. ← Previous TopicNext Topic →View all Basic Pharmacognosy topicsOpen Complete Full Notes PDF / OFFLINE NOTES Unataka kutumiwa notes hizi kupitia WhatsApp?Kwa notes zilizopangiliwa vizuri kwa kusoma offline au PDF, bonyeza kitufe hapa chini. Ujumbe wenye Level, Semester, Module na Topic utaandaliwa moja kwa moja.TUMIWA NOTES WHATSAPP WhatsApp: 255620339260

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05208 Pharmaceutics Theory and Compounding

Introduction to Sterile Pharmaceutical Preparations – PST05208 Pharmaceutics Theory and Compounding

NTA Level 5 • Semester 2 • PST05208 Introduction to Sterile Pharmaceutical Preparations Pharmaceutics Theory and Compounding • Source Session/Topic 1 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 1: Introduction to Sterile Pharmaceutical Preparations Total Session Time: 120 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Define sterile pharmaceutical products. • Explain categories of sterile pharmaceutical Products. • List qualities of sterile pharmaceutical products. • Explain the role of aseptic techniques in assuring quality in pharmaceutical production Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board, chalk and whiteboard markers • LCD projector and computer • Handout 1.1: Categories of Sterile Pharmaceutical products & medical devices SESSION OVERVIEW Activity/ Step Time Content Method 1 05 Minutes Presentation Introduction, Learning Tasks 2 10 Minutes Presentation Definition of Sterile Pharmaceutical Products 25 Minutes Presentation Classification Categories of Sterile 3 Brainstorming Pharmaceutical Products 4 35 Minutes Presentation Qualities of Sterile Pharmaceutical Products 35 Minutes Presentation General Methods of Sterilizing Pharmaceutical 5 Buzzing Products 6 05 Minutes Presentation Key Points 7 05 Minutes Presentation Evaluation 1 SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Definition of Sterile Pharmaceutical Products (10 minutes) • Sterile pharmaceutical products refer to pharmaceutical products that are free from any viable microorganisms, these are pharmaceutical products from which viable micro-organisms must be totally absent. • The production of sterile products requires special care and attention in order to eliminate microbial and particulate contamination at all stages of manufacture and wherever possible also includes a terminal sterilization process. STEP 3: Categories of Sterile Pharmaceutical Products (25 minutes) Activity: Brainstorming (10 minutes) Ask students to brainstorm on the following question: • What are the classification categories of sterile pharmaceutical products? ALLOW few students to respond? WRITE their responses on the flip chart/ board CLARIFY and SUMMARISE by using the content below • Not all pharmaceutical products need to be sterile. Sterility is insisted on the following products: o Parenterally administered products e.g. injections, irrigations, ophthalmology products etc. o Pharmaceutical products that come into direct contact with broken skin/mucous membrane or internal organs e.g. certain instruments, sutures, surgical dressings etc. • These products are required to be prepared and maintained in a sterile state until used. Handout 1.1 Categories of Sterile Pharmaceutical products & medical devices 2 STEP 4: Qualities of Sterile Pharmaceutical Products (35 minutes) Activity: Buzzing (10 minutes) Ask students to brainstorm on the following question: • What are the qualities of sterile pharmaceutical products? ALLOW few students to respond? WRITE their responses on the flip chart/ board CLARIFY and SUMMARISE by using the content below • All products intended for sterilization should be manufactured under clean conditions and therefore will be of low microbial content (bio burden) prior to sterilization. • Sterile formulations must meet the following standard of quality: o Should be sterile o Free from particulate contaminants o Free from pyrogen o Should be physically and chemically stable o Should have the same pH as the blood; (isohydric means the same concentration of H+ (Hydrogen ions) or pH = 7.38 o Same Osmotic pressure as blood plasma (isotonic) 3 STEP 5: Role of Aseptic Technique in Assuring Quality in Pharmaceutical Production (40 minutes) Activity: Brainstorming (5minutes) Ask students to brainstorm on the following question: • What are the roles of aseptic techniques in assuring quality in pharmaceutical production? ALLOW few students to respond? WRITE their responses on the flip chart/ board CLARIFY and SUMMARISE by using the content below • This is a method of handling sterile materials by employing techniques, which minimize the chances of microbial contamination in order to obtain the sterile products. • The followings are the roles of aseptic techniques in assuring the quality in pharmaceutical production; o To minimize and reduce the risks of contamination o To disinfect working area, equipment and ingredients in order to attain sterility o To prevent access of viable micro-organisms and particulate contamination during preparation and testing of pharmaceutical products STEP 6: Key Points (5 minutes) • Sterile formulations must meet the following standard of quality: remained sterile, free from particulate contaminants, free from pyrogen, been physically and chemically stable, should have the same pH as the blood and same Osmotic pressure as blood plasma (isotonic) • The production of sterile products requires special care and attention in order to eliminate microbial and particulate contamination at all stages of manufacture and wherever possible also includes a terminal sterilization process. STEP 7: Evaluation (5 minutes) • What is sterile pharmaceutical products • What are the roles of aseptic techniques in assuring quality in pharmaceutical production? 4 References Senya, S. S., Mwasha, C. Y. S., Muyinga, A. M., Amiri, R. I., & Mauga, E. A. S. K. (2011). Tanzania Pharmaceutical Handbook (2nd ed.). Dar es salaam. A. J. Winfield, J. A. R., I. Smith. (2009). Pharmaceutical Practice (4th ed.) British Britain, R. P. S. o. G. (1994). The Pharmaceutical Codex (12 ed.). London: London Pharmaceutical Press. 5 Handout 1.1. Categories of Sterile Pharmaceutical products & medical devices SN Types/Categories Examples 1. Injections • Intravenous infusions • Intravenous additives • Total Parenteral nutrition (TPN) fluids • Small-volume injections • Small-volume oily injections 2. Non-injectable sterile fluids • Non-injectable water, (Sterile water for irrigation) • Urological irrigation solutions, • Peritoneal dialysis solutions, • Haemodialysis solutions, • Inhaler solutions 3. Ophthalmic preparations • Eye drops • Eye lotions • Eye ointments • Contact lens solutions • Wetting solutions • Cleaning solutions • Soaking solutions 4. Intravenous additives • Potassium chloride • Lidocaine (lignocaine) These are sterile drugs or additives • Heparin regularly added to infusions • certain vitamins immediately before administration. • Antimalarial injection, eg. Quinine injection •

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05208 Pharmaceutics Theory and Compounding

Determination of Isotonicity by Freezing Point – PST05208 Pharmaceutics Theory and Compounding

NTA Level 5 • Semester 2 • PST05208 Determination of Isotonicity by Freezing Point Pharmaceutics Theory and Compounding • Source Session/Topic 12 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 12: Determination of Isotonicity by Freezing Point Method Total Session Time: 120 minutes + 6 hours of Practices Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Define freezing point depression • Determine the isotonicity by freezing point depression Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board, chalk and whiteboard markers • LCD projector and computer SESSION OVERVIEW Activity/ Step Time Content Method 1 05 Minutes Presentation Introduction, Learning Tasks 2 45 Minutes Presentation Introduction to Freezing Point Depression Presentation Determining the Isotonicity by freezing Point 3 60 Minutes Small Group Depression Discussion 4 05 Minutes Presentation Key Points 5 05 Minutes Presentation Evaluation 92 SESSION CONTENTS STEP1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing STEP 2: Freezing Point Depression (45 minutes) • The freezing point of body fluid is at – 0.520C. • Any solution freezing at – 0.520C will have the same osmotic pressure as body fluids • Hypotonic solution will have a higher freezing-point and consequently need the addition of adjusting substance to reach a freezing point of – 0.520C • The amount of adjusting substance which is often sodium chloride, is calculated as shown in the following examples. o Solution A freezes at – 0.390C. How much sodium has to be added to obtain an isotonic solution? o The adjusting substance sodium chloride has to decrease the freezing point by 0.52 – 0.39 = 0.130C o A 1 % w/v sodium chloride solution freezes at – 0.5760C; so the amount needed is found by the proportion: o 1 == x x == 1 x 0.13 == 0.2%w/v 0.576 0.13 0.576 • Therefore, solution A will need the addition of 0.2%w/v sodium chloride in order to become isotonic with body fluids; e.g. 50mL of this solution require 0.1g sodium chloride. • From the above used proportion, the following equation has been derived: o W == 0.52 – a b o Where:  w== concentration %w/v of adjusting substance in the final solution  a == freezing point of unadjusted solution  b==freezing point of a 1%w/v solution of adjusting substance • The freezing points of 1%w/v aqueous solution of various substances are obtain from the table below; “a „ is calculated by multiplying the freezing depression of a 1%w/v solution by the concentration of unadjusted solution expressed as %w/v 93 • Example: o Adjust 1000mL of a 2%w/v solution of anhydrous dextrose isotonic with body fluids; adjusting substance is sodium chloride  Freezing point of 1%w/v anhydrous dextrose solution : – 0.1010C  Freezing point of unadjusted solution: – 0.101 x 2 == – 0 .2020C  Freezing point of 1%w/v sodium chloride solution = -0.5760C  The last two values are substituting “ a “ and “b” in the formula o W = 0.52 – 0.202 = 0.318 = 0.55%w/v 0.576 0.576 o Therefore, a 2%w/v anhydrous dextrose solution requires the addition of 0.55%w/v sodium chloride in order to become isotonic with blood serum and tears; for 1000mL solution 5.5g are needed STEP 3: Determining the Isotonicity by Freezing Point Depression (60 minutes) To determine amount of ingredients required to make isotonic solution Activity: Small Group Discussion ( 30 minutes) DIVIDE students in small manageable groups ASK students to discuss in groups on the following questions 1. Render the following solution iso – osmotic with blood and tears Ephedrine hydrochloride…………………………0.1g Chlorbutol…………………………………………0.1g Water for preparation……………………….to 20mL Adjusting substance is sodium chloride REFER Students to Pharmaceutical Calculation. 13th Edition by HOWARD C. ANSEL: Chapter 11, For reference ALLOW students to discuss for 20 minutes ALLOW each groups to present for 5 minutes CLARIFY and SUMMARIZE by using the contents below 94 • The freezing point depression of 1%w/v solution is obtained from the table below. • First the concentrations %w/v must be calculated for ephedrine hydrochloride and Chlorbutol by proportion: 0.1 = xx =0.1 x100 x = 0.5%w/v 20 100 20 • A 0.5%w/v solution of ephedrine hydrochloride has a freezing point depression of 0.165 x 0.5 = 0.08250C • A 0.5%w/v solution for Chlorbutol has a freezing point depression of 0.14 x 0.5 =0.070C • Now the equation can be used: W = 0.52 – 0.1525 ==0.3675 = 0.638%w/v =0.64%w/v 0.576 0.576 • Therefore, the unadjusted solution needs the addition of 0.64%w/v sodium chloride. The actual amount for 20mL solution is found by simple proportion 0.638 = x x = 0.638 x 20 =0.1276gm of sodium chloride 100 20 100 • So the formula for the adjusted solution becomes: Ephedrine hydrochloride…………………………0.1g Chlorbutol………………………………………..0.1g Sodium chloride………………………………….0.13g Water for preparation……………………….to 20mL STEP 4: Key Points (5 minutes) • Freezing-point depression is the decrease of the freezing point of a solvent on addition of a non- volatile solute • The formula for determining the Isotonicity by freezing point depression is w= 0.52 – a b STEP 5: Evaluation (5 minutes) • What is freezing point depression in determining isotonicity? • What is the formula for determining isotonicity by freezing point depression? 95 STEP 6: Take Home Assignment (15 minutes) Activity: Take home Assignment (15 minutes) ASK each individual student to do the following assignment • Calculate the strength of sodium chloride solution which is iso – osmotic with blood serum and tears ALLOCATE time for students to do the assignment and submit REFER students to recommended references 96 References Aulton, M. E., & Taylor, K. (2013). Aulton's pharmaceutics : the design and manufacture of medicines (4th ed.). Edinburgh: Churchill Livingstone/Elsevier. Pharmaceutical Society of Great Britain., & Pharmaceutical Society of Great Britain. Department of

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05208 Pharmaceutics Theory and Compounding

Introduction to Isotonicity – PST05208 Pharmaceutics Theory and Compounding

NTA Level 5 • Semester 2 • PST05208 Introduction to Isotonicity Pharmaceutics Theory and Compounding • Source Session/Topic 11 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 11: Introduction to Isotonicity Total Session Time: 60 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Define terms used in isotonicity • Explain the importance of isotonic solution. • Explain effects of administering paratonic solutions Resources Needed: Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board, chalk and whiteboard markers • LCD projector and computer SESSION OVERVIEW Step Time Activity/Method Content 1 05 Minutes Presentation Introduction, Learning Tasks Presentation Definition of Terms Used in Isotonicity and 2 15 Minutes Brainstorming Electrolytes. 15 Minutes Presentation Importance of isotonic solution. 3 Small group discussion 4 15 Minutes Presentation Effects of administering paratonic solutions 5 05 Minutes Presentation Key Points 05 Minutes Presentation 6 Evaluation 84 CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Definition of Terms used in Isotonicity and Electrolytes (15 minutes) Activity: Buzzing (5 minutes) ASK students to pair up and buzz on the following question for 2 minutes • What is isotonicity? ALLOW few pairs to respond and let other pairs to add on points not mentioned WRITE their response on the flip chart/board CLARIFY and SUMMARIZE by using the content below • Body fluids e.g. blood plasma have certain quantity of dissolved substances e.g. salts that determine power of the blood called osmotic pressure. • Osmotic pressure is the pressure created by solvent molecules moving from a low concentrated solution to higher concentrated solution through a semi-permeable membrane, a semi-permeable membrane allow only the solvent molecules to pass. • The characteristics of a solution is determined by the number of dissolved substances in it, aqueous solutions which exert the same osmotic pressure as blood plasma are said to be isotonic with plasma. This is equivalent to 0.9%w/v sodium chloride injection (Normal saline) • An isotonic solution is a solution in which body cells can be bathed without a net flow of water across a semipermeable membrane. E.g. 0.9% normal saline (NS). • Osmolality o A unit of measure of osmotic pressure. o Blood has 300 mOsmol per liter. (MiliOsmolality) o Both Normal Saline and Dextrose 5% solutions have a similar osmolarity. 85 • Solutions, which exert a different osmotic pressure as blood plasma, are said to be paratonic with plasma. (i.e. solutions with hypotonic or hypertonic osmotic pressure) • Those solutions with a lower osmotic pressure than blood plasma are said to be hypotonic solutions and a solution of less than normal tonicity is hypotonic, which has fewer numbers of dissolved solutes than blood cells. E.g. 0.45% Normal Saline. • Solutions with a higher osmotic pressure than blood plasma are said to be hypertonic solutions, a hypertonic solution has more number of dissolved solutes than the blood cells themselves. E.g. 50% Dextrose or 3% Sodium chloride. • Aqueous solutions intended to contact with body fluid should preferably be made isotonic with speci※c bodily ‼uid in order to minimize any possible adverse effects. • Tonicity is generally classified in three types: o Hypertonicity o Hypo tonicity o Isotonicity • Hypertonic, isotonic and hypotonic solutions are defined in reference to a cell membrane by comparing the tonicity of the solution with the tonicity within the cell. • For a solution to be termed isotonic (equal tone) it must have the same osmotic pressure as a speci※c bodily ‼uid. The easiest way to calculate the osmotic pressure of a solution is to utilize the more easily measured property of the freezing point depression, as they are proportional to one another. • In pharmacy, isotonicity calculations are most often performed for parenteral and ophthalmic solutions, which must have a freezing point depression of 0.520C for them to be isotonic with blood plasma and tears. Therefore a solution is considered to be isotonic if it has a freezing point of -0.520C • Electrolytes are substances containing free ions, thus rendering the substance electrically conductive • Electrolyte preparations are used in the treatment of disturbances of electrolyte and fluid balance in the body. In clinical practice, they are provided in the form of oral solutions, and syrup as dry granules intended to be dissolved in water or juice to make an oral solution and when necessary as intravenous infusions 86 STEP 3: Importance of Isotonicity (15 minutes) Activity: Small Group Discussion ( 10 minutes) DIVIDE students into small manageable groups ASK students to discuss on the following question • What is the importance of isotonicity? REFER Students to Tanzania Pharmaceutical Handbook pg. 33-50 ALLOW students to discuss for 10 minutes ALLOW few groups to present and the rest to add points not mentioned CLARIFY and SUMMARIZE by using the contents below • It is important for a solution to be isotonic with a bodily ‼uid to prevent irritation and cell damage, and to maximize drug efficacy. Its neutrality is not affecting the osmotic pressure of a cell • This state allows for the free movement of water across the membrane without changing the concentration of solutes on either side. • Isotonic solutions are used in Oral Rehydration Therapy (ORT), which is a treatment for dehydration associated with gastroenteritis. ORT replenishes the body's lost electrolytes and promotes the uptake of glucose and fluid by the intestinal epithelial cells. • Isotonic solutions given intravenously in case of severe dehydration and is used in the treatment of hypernatremia (a condition in which serum concentration of sodium is high) in individuals who have impaired water excretion, eg 0.9% NaCl solution • It can be used as a medium for intravenous administration of drugs like propofol, which are not

Pharmaceutical Sciences Notes, PST Level 5 Semester 2, PST NTA Level 5, PST05208 Pharmaceutics Theory and Compounding

Compounding of Gels/ Jellies – PST05208 Pharmaceutics Theory and Compounding

NTA Level 5 • Semester 2 • PST05208 Compounding of Gels/ Jellies Pharmaceutics Theory and Compounding • Source Session/Topic 10 Full source-text version: all educational wording from the extracted learning source is retained; only presenter/tutor metadata and web-layout noise are removed, while formatting is improved for readability. Session 10: Compounding of Gels/ Jellies Total Session Time: 120 Minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to:  Give overview of gels  Describe procedures for preparing gels  Prepare gels  Label prepared gels  Dispense prepared gels into suitable containers and closure Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board, chalk and whiteboard markers • LCD projector and computer • Figure 10.1: Gels jars and tube SESSION OVERVIEW Activity/ Step Time Content Method 1 05 Minutes Presentation Introduction, Learning Tasks Presentation 2 25 Minutes Buzzing Introduction to Gels 3 10 Minutes Presentation Procedures for Preparing Gels Presentation 4 Preparing Gels 35 Minutes Demonstration Presentation 5 25 Minutes Demonstration Labeling of Prepared Gels Presentation Dispensing of Prepared Gels into Suitable Containers 6 10 Minutes Brainstorming and Closure 7 05 Minutes Presentation Key Points 8 05 Minutes Presentation Evaluation 74 SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (5 minutes) READ or ASK students to read the learning tasks and clarify ASK students if they have any questions before continuing. STEP 2: Introduction to Gels (25 minutes) Activity: Buzzing (5 minutes) ASK students to pair up and buzz on the following question for 2 minutes • What are Gels? ALLOW few pairs to respond and let other pairs to add on points not mentioned WRITE their response on the flip chart/board CLARIFY and SUMMARIZE by using the content below • Gels are transparent (or translucent) semi-solid or solid preparations of either suspensions made up of small inorganic particles or large organic molecules interpenetrated by a liquid • Are semisolid systems consisting of dispersion of small or large molecules in an aqueous liquid vehicle rendered jelly-like through addition of a gelling agent • Movement of dispersing system is restricted by interlacing network of particles or solvated macromolecules of dispersed phase • Gels are made using substances (called gelling agents) that undergo a high degree of cross- linking or association when hydrated and dispersed in the dispersing medium or when dissolved in the dispersing medium • Cross-linking or association of dispersed phase alters the viscosity of the dispersing medium • Hence the movement of dispersing medium is restricted by the dispersed phase • Two-phase System Gel o Is when the gel contains a network of small discrete particles • One or Single-phase System Gel o When gels appear to have no discrete particles, 75 o Macromolecules are uniformly distributed throughout the liquid, usually organics o No apparent boundaries between dispersed macromolecules and the liquid o Two-phase system gels are thixotropic Gel mass consists of floccules of small distinct particles Usually involve inorganics Semisolid on standing but liquefy on shaking If the particles in the two-phase systems are large • The gel is called a Magma or Milk Composition of gels is: o Gelling agents o Water o Co-solvents o Preservatives o Stabilizers • One-phase gels are made from synthetic or natural organic macromolecules distributed uniformly throughout a liquid without any boundary between dispersed and dispersing phases (e.g. tragacanth, cellulose, methylcellulose) • If made from natural gum, single-phase gels are called Mucilages • Some Gelling Agents o Acacia, tragacanth, Methylcellulose, o Alginic acid, Bentonite, Carbopol®, o Carboxymethylcellulose (CMC), o Gelatin, Hydroxypropyl cellulose, o Magnesium Aluminium Silicate (Veegum®) etc • Characteristic Properties of gels are:often non-greasy, smooth, elegant, produce cooling effect on application and easily washable from skin STEP 3: Procedures for Preparing Gels (10 minutes) • Specific method depends on gelling agent o e.g. gelatin gels o By dispersing gelatin in hot water followed by cooling OR o By wetting gelatin with organic liquid e.g. Propylene glycol, followed by addition of hot water and cooling • Example of a gel formulation: • Methylcellulose and Carbomer Gel Base o Methylcellulose, 4000cps 1.0% o Carbomer 934 0.35% o 1N Sodium Hydroxide Solution qs to pH 7 76 o Propylene glycol 16.7% o Methyl paraben 0.015% o Purified water, qs 100 o Disperse the methylcellulose in a portion of hot (80-90°C) water o Cool to room temperature, and disperse the Carbomer 934 in the gel using a bladed stirrer. o Adjust the pH of the dispersion to 7.0 by adding sufficient 1N Sodium hydroxide solution. o Dissolve the methylparaben in the propylene glycol. Mix the methylcellulose, Carbopol 934 and propylene glycol fractions using caution to avoid incorporating air. STEP 4: Preparing of gels (35 minutes) Activity: Demonstration (45 minutes) DIVIDE students in small manageable groups. PREPARE equipment and materials needed for demonstration POSITION students so that everyone can see and hear REVIEW steps of preparing pastes with students REFER students to the official formula of preparing Ichthammol gel IP In the Tanzania Pharmaceutical Handbook DEMONSTRATE the procedure of preparing ointments according to the instruction under the official formula in the Tanzania Pharmaceutical Handbook (Mitte 50g) ALLOW one student from each group to do a return demonstration and let others comment on it CLARIFY and SUMMARIZE Using the content below INFORM the students that “every student will practice in the skills laboratory under supervision until is competent” • Official formula given for Ichthammol gel PCx Ichthammol……………………………………………………….. 1.0g Tragacanth, in powder……………………………………………… 2.5g Alcohol 90%……………………………………………………………… 5.0g 77 Glycerin……………………………………………………………… 1.0g Purified water q.s………………………………………………………… 50.0g Mitte 50.0g for Allen Mbogo • Thus, amount of official formula = 100g • Total amount required = 50g • Amount of each ingredient (x) =? • FACTOR= Required amount Official amount = 50g 100g = 0.5 Then, amount of each ingredient can be obtain as summarised in the table below: Formula Official amount Factors Required amount Ichthammol 1.0g 0.5g Tragacanth, in powder 2.5g 0.5 1.25g Alcohol 90% 5.0g 2.5g Glycerol 1.0g 0.5g Purified water q.s 50.0g 25g

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