PST05208 Pharmaceutics Theory and Compounding

NTA Level 5 • Semester 2 • PST05208 Semi Solid Preparations Pharmaceutics Theory and Compounding • Source Session/Topic 5 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 5: Semi Solid Preparations Total Session Time: 120 Minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to:  Define semi – solid pharmaceutical preparations  List ideal properties of semi – solid preparations  Explain rational approaches to topical formulation  List treatment target for semisolid preparations  Explain components of semi – solid pharmaceutical preparations 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 10 Minutes Presentation Definition of Semi- Solid Pharmaceutical 2 Buzzing Preparations 3 15 Minutes Presentation Ideal Properties of Semi – Solid Preparations 4 15 Minutes Presentation Rational Approaches to Topical formulation 35 Minutes Presentation 5 Treatment Target for Semisolid Preparations Brainstorming 30 Minutes Presentation Components of Semi – Solid Pharmaceutical 6 Preparations 7 05 Minutes Presentation Key Points 8 05 Minutes Presentation Evaluation 27 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 Semi – Solid Preparations (10 minutes) Activity: Buzzing (5 minutes) ASK students to pair up and buzz on the following question for 2 minutes • What are semi – solid pharmaceutical preparations? 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 • Pharmaceutical semisolid preparations: Are the topical products intended for application on the skin or accessible mucous membranes to provide localized and sometimes systemic effects at the site of application, it is a preparations designed to exert local activity when applied to the skin or mucous membranes • The main medicinal applications of semi-solids pharmaceutical preparations are as protective, emollient, and therapeutic agents, these semi-solid pharmaceutical preparations for external application are: ointments, pastes, creams, poultices/cataplasms and gels. STEP 3: Ideal Properties of Semi – Solid Preparations (15 minutes) • Physical properties: o Smooth texture o Elegant in appearance o Non dehydrating o Non gritty o Non greasy and non-staining o Non hygroscopic 28 • Physiological properties: o Non irritating o Do not alter membrane / skin functioning o Miscible with skin secretion o Have low sensitization index • Application properties: o Easily applicable with efficient drug release. o High aqueous washability. • Storage properties: o Should be stored at temperatures not exceeding 25°c unless otherwise authorized. o They should not be allowed to freeze and must be stored in a well-closed container or, if the preparation contains water or other volatile ingredients, store in an airtight container. o The containers are preferably collapsible metal tubes from which the preparation may be readily extruded. o If the preparation is sterile, store in a sterile, airtight, tamper-proof container. STEP 4: Rational Approaches to Topical Formulation (15 minutes) • There are three main methods for a successful formulation of topical dosage form o By manipulating barrier function of skin;  Topical antibiotics and antibacterials help damaged barrier to avoid infections  Sunscreen and the horny layer protect viable tissues from u.v. radiations  Emollients restore pliability to desiccated horny layer o By directing drugs to the viable skin tissues without using oral, systemic or other routes of therapy o By using skin delivery for systemic treatment  e.g. transdermal therapeutic systems provide systemic therapy for motion sickness, angina and hypertension 29 STEP 5: Treatment Target for Semi – Solid Preparations (35 minutes) Activity: Brainstorming (15 minutes) Ask students to brainstorm on the following question: • What are treatment target for semi – solid preparations? ALLOW few students to respond WRITE their responses on the flip chart/ board CLARIFY and SUMMARISE by using the content below • Five main target regions: o Skin surface, horny layer, viable epidermis and upper dermis, skin glands, and systemic circulation. • Surface treatment o Care for skin surface is mainly by cosmetic application, that form protective layer, or attack bacteria and fungi o Sunscreens, barriers that hinder moisture loss, antimicrobials and insect repellants) • Stratum corneum treatment o Main therapies aimed at the horny layer improve emolliency by raising water content or stimulating sloughing o E.g. keratosis, exfolients such as salicylic acid • Skin appendage treatment o Antiperspirants (aluminium) reduce hyperhidrosis of sweat glands o Exfolients (e.g. salicylic acid, tretinoin (retinoic acid), benzoyl peroxide) for acne o Topical antimicrobials, depilatories etc. • Viable epidermis and dermis treatment o Diseases can be treated provided that the preparation efficiently delivers drug to the receptor o E.g. anti-inflammatory drugs (steroids & non steroids), antitumor (e.g. methotrexate, 5- fluorouracil) anesthetics (e.g. benzocaine), antihistamines 30 • Systemic treatment via percutaneous absorption o In recent years considerable scientific work has led to the skin route being used to treat several conditions by means of transdermal patches o E.g. motion sickness (hyoscine), angina (nitroglycerin) STEP 6: Components of Semi – Solid Pharmaceutical Preparations (30 minutes) • Antioxidant o Prevents or slows oxidation of other components o Examples: Tocopherol, butylated hydroxy toluene, or a reducing agent such as ascorbic acid. • Base o Major classes or types of formulation compositions based on composition and physical properties. o Examples: Please refer to bases chapter. • Buffer o Acid-conjugate base mixture employed to control pH and therefore control ionization state of drug and impart stability o Examples: Citrate, phosphate, tartarate • Chelating agent o Have the ability to bind metal ions; prevents auto-oxidation phenomena frequently catalyzed by metal ions and enhances action of preservatives by binding iron and copper ions essential to microbial growth. o

NTA Level 5 • Semester 2 • PST05208 Percutaneous Absorption Pharmaceutics Theory and Compounding • Source Session/Topic 4 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 4: Percutaneous Absorption Total Session Time: 120 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to:  Explain percutaneous Absorption  Explain factors affecting percutaneous absorption 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 50 Minutes Presentation 2 Percutaneous Absorption Brainstorming 55 Minutes Presentation 3 Factors Affecting Percutaneous Absorption Buzzing 4 05 Minutes Presentation Key Points 5 05 Minutes Presentation Evaluation 19 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: Percutaneous Absorption (50 minutes) Activity: Buzzing (5 minutes) ASK students to pair up and buzz on the following question for 2 minutes • What is percutaneous absorption? 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 • Percutaneous absorption is the term used to describe the penetration of a substance through the skin and subsequent movement into the systemic circulation. • For drugs applied topically for therapeutic purpose, its necessary that: o The medicament is released from the base o Adequate amount of drug penetrate the skin o Sufficient concentration of the drug is maintained at the site of action. • In some instance, skin penetration of medicament is not necessary for a topical applied medicament • A surface film of the active medicament is necessary for this instance. e.g. for medicament applied topically purposely for: o Skin protection (against sunlight or moisture loss o For emollient effect o For antimicrobial activities in skin disinfection 20 • When skin penetration for local activity is the aim, the active substance should be retained for as longer as possible in the viable epidermis and dermis with minimal elimination by systemic circulation. • Therefore, by regarding skin as the route of drug administration, it‟s important to know the mechanism by which medicaments penetrates the skin barrier. • Structure of skin o The skin is divided into three layers:  epidermis  dermis  hypodermis (subcutaneous fat layer) • Epidermis o Is about 110µm thick o Is pierced by hair follicles & sebaceous gland o It is non vascular o The outer layer of the epidermis is called stratum corneum o The stratum corneum is transparent, tough coherent & viscoelastic properties. o The stratum corneum is composed of dead cells each packed with keratin. o Resistance to the diffusion of chemicals is greater in stratum corneum (sc) than in the underlying living skin tissue. o SC is the rate-limiting barrier to movement of materials & responsible tissue for impenetrability of the skin. o However the is not an absolute barriers and trace amount of penetrants can be detected; eg nickel, chromium ions, parathion & toxic gases. o The thickness of sc varies. It is thick on the plantar & palmar areas and thin behind the ear and on the eyelid. o Cells are formed through mitosis at the basale layer o The daughter cells move up the strata changing shape and composition as they die due to isolation from their blood source o The cytoplasm is released and the protein keratin is inserted. o They eventually reach the corneum and slough off (desquamation). o This process is called keratinization and takes place within about 27 days. o This keratinized layer of skin is responsible for keeping water in the body and keeping other harmful chemicals and pathogens out, making skin a natural barrier to infection. • Dermis o The dermis is the layer of skin beneath the epidermis that consists of connective tissue and cushions the body from stress and strain. 21 o The dermis is tightly connected to the epidermis by a basement membrane. o It also harbours many Mechanoreceptor/nerve endings that provide the sense of touch and heat. o It contains the hair follicles, sweat glands, sebaceous glands, apocrine glands, lymphatic vessels and blood vessels. o The blood vessels in the dermis provide nourishment and waste removal from its own cells as well as from the Stratum basale of the epidermis. 22 • Hypodermis o The hypodermis lies below the dermis o Its purpose is to attach the skin to underlying bone and muscle as well as supplying it with blood vessels and nerves. o The main cell types are fibroblasts, macrophages and adipocytes (the hypodermis contains 50% of body fat). Fat serves as padding and insulation for the body. Figure: 1.4. Structure of skin Source: Human Anatomy by Matthew Hoffman, MD (2014) STEP 3:Factors Affecting Percutaneous Absorption (55 minutes) Activity: Brainstorming (20 minutes) Ask students to brainstorm on the following question: • What are factors affecting percutaneous absorption? ALLOW few students to respond? WRITE their responses on the flip chart/ board CLARIFY and SUMMARISE by using the content below 23 • Factors affecting percutaneous absorption can be considered under three main heading o Condition of the skin o Physicochemical characteristics of the active substance o Effect due to the vehicle. • Condition of the skin. o Damage and disease.  Intact skin presents a barrier to absorption that can be reduced considerably when the skin is damaged or is in a disease state.  Skin can be damaged by: • Dryness • Irritation • Allergic reaction • abrasion o Injured skin has increased percutaneous than intact skin. • Age o Percutaneous absorption of infants is higher than in adult to a given medicament due to  large surface

NTA Level 5 • Semester 2 • PST05208 Requirements for Preparation of Sterile Pharmaceutics Theory and Compounding • Source Session/Topic 3 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 3: Requirements for Preparation of Sterile Pharmaceutical Products Total Session Time: 120 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to:  Explain premise requirements for sterile production.  Explain personnel requirements for sterile production.  Explain raw materials requirements for sterile production.  Explain documentation requirements for sterile production.  Explain equipment requirements for sterile production. 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 30 Minutes Presentation 2 Buzzing Premise Requirements for Sterile Production. 30 Minutes Presentation 3 Brainstorming Personnel Requirements for Sterile Production. 15 Minutes Presentation 4 Raw Materials Requirements for Sterile Production. Buzzing 15Minutes Presentation 5 Documentation Requirements for Sterile Production. Brainstorming 15 Minutes Presentation Equipment Requirements for Sterile Production. 6 Brainstorming 7 05 Minutes Presentation Key Points 13 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: Premise Requirements for Sterile Production (30 minutes) • The quality of infusions produced will depends very much on the degree of care taken during its preparation. • Each step in the production process is a possible source of contamination to the manufactured product. • Hence, Manufacture of sterile preparations (e.g. infusions) needs special requirements to minimise the risks of particulate, microbial and pyrogens contamination. • Therefore, production of sterile preparations needs environmental control of particulate and microbial contamination, so as to reduce the introduction, generation, and retention of contaminants during preparation. • Well maintained premises: o The facilities for the manufacture of sterile products should be designed for near to perfect level of cleanliness. o The maximum degree of cleanliness must be achieved in the aseptic filling rooms. o The surrounding areas should provide a buffer area in which standards of cleanliness are only slightly lower than the aseptic rooms. o The prevention of contamination must be the primary objective in the design of these facilities. o Well-maintained premise is a good indicator that production of infusions is done in clean environment that reduces risks of contamination to the product. • Methods of cleansing: o All equipment and surrounding work area must be cleaned thoroughly at the end of the working day. o After thorough cleaning, all surfaces should be disinfected, at least in the aseptic area. o An effective liquid disinfectant should be sprayed or wiped on all surface. 14 o Irradiation from UV lamps properly located will further reduce the viable microorganisms on surfaces and in the air. • Production Flow pattern: o The facility should be designed in such a way that it provides a continuous flow of production activities. o A change area has to be available before entering the facilities to allow change of street clothes into the appropriate production garments and gear. o There should then be a continuous process from supply storage to compounding of product, filling, sealing, sterilisation, labelling/packaging and finally to storage of the finished product. STEP 3: Personnel Requirements for Sterile Production (30 minutes) Activity: Brainstorming (5 minutes) Ask students to brainstorm on the following question: • What are the personnel requirements for sterile production ALLOW few students to respond? WRITE their responses on the flip chart/ board CLARIFY and SUMMARISE by using the content below • Should be adequately trained and motivated e.g. Equipped with basic understanding of pharmaceutical technology, microbiology and hygiene. • They should be aware of the role that every movement has, in determining the quality of the final product. e.g. Aware of the sources of contamination. • Appropriate protective clothing should be worn. e.g. Boots, coats, caps, gloves, hats, and mask. • Personnel working in aseptic areas should be required to follow laid down preparatory procedures. o These include removing outside street clothing, scrubbing the hands and arms thoroughly with disinfectant soap, and wearing of prescribed uniforms. o Uniforms usually consist of sterile overalls, hats, facemasks and shoe covers. Sterile rubber gloves also may be required. o Uniforms are worn to control emission of particulate matter, which is continually shedding from body surfaces. o Aware of the hazards, which can be caused by using products of poor standards. 15 o Behaviour like smoking, eating, drinking, chewing, attending phone calls, in- and out- movements and any other activity that influence the product quality while in production processes are restricted STEP 4: Raw Materials Requirements for Sterile Production (15 minutes) • All materials purchased for use in compounding and dispensing o Should be of suitable quality and obtained from a licensed or reliable source. o „In house‟ check of quality may be made on starting materials. o Materials should be fully identifiable and carry a clear batch identification and expiry date. o Appropriate storage conditions should be maintained and out-of-date stock safely disposed o Should be pyrogens free STEP 5: Documentation Requirements for Sterile Production (15 minutes) • All compounding procedures should be fully documented and the record should include the following details: o The name of the product. o A written master formula & the working formula of the batch being prepared. o The method of preparation o The names, quantities and identification of each starting material (Supplier, batch number and date received) o The date of manufacture. o The appropriate container and closure. o The required storage conditions. o A copy of the label. STEP 6: Equipment Requirements for Sterile Production.(15 minutes) Activity: Buzzing (5 minutes) Ask students to brainstorm on the following question: •

NTA Level 5 • Semester 2 • PST05208 Aseptic Processing Pharmaceutics Theory and Compounding • Source Session/Topic 2 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 2: Aseptic Processing Total Session Time: 60 minutes Prerequisites • None Learning Tasks By the end of this session students are expected to be able to: • Give introduction of aseptic processing. • Explain concept of aseptic processing • Identify basic rules for effective aseptic processing Resources Needed: • Flip charts, marker pens, and masking tape • Black/white board, chalk and whiteboard markers • LCD projector and computer • Figure.2. 1: Aseptic techniques SESSION OVERVIEW Activity/ Step Time Content Method 1 05 Minutes Presentation Introduction, Learning Tasks 15 Minutes Presentation Introduction to Aseptic Processing. 2 Brainstorming 10 Minutes Concept of Aseptic Processing Presentation 3 Buzzing 4 20 Minutes Presentation Basic Rules for Effective Aseptic Processing 6 05 Minutes Presentation Key Points 7 05 Minutes Presentation Evaluation 8 SESSION CONTENTS STEP 1: Presentation of Session Title and Learning Tasks (05 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 Aseptic Processing (15 minutes) Activity: Buzzing (5 minutes) ASK students to pair up and buzz on the following question for 2 minutes • What is aseptic processing? 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 Aseptic processing • Is the processing and packaging of a commercially sterile product into sterilized containers followed by hermetic sealing with a sterilized closure in a manners that prevents viable microbiological recontamination of the sterile product. • It require careful control of the aseptic environment, of personnel practices and procedures, sterilization of equipment and components, extensive environmental monitoring, and many other controls. • The number of controls required and the severe consequences of control failure make aseptic processing one of the highest-risk pharmaceutical processes. Quality risk management is an essential tool in ensuring product quality. 9 STEP 3: Concept of Aseptic Processing (10 minutes) Activity: Brainstorming (5 minutes) ASK students to pair up and buzz on the following question for 2 minutes • What are the concepts of aseptic processing? 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 • Suitable measures must be taken to ensure the microbiological quality of pharmaceutical preparations during manufacturing but also during packaging, storage and distribution is maintained • The requirements necessary to achieve strict asepsis include: o sterile starting materials o Sterile equipment o Controlled environment o Sterile containers o Suitable technique by trained personnel Figure.2. 1: Aseptic techniques processing operation by Ranjith Kumar kankala (2012) 10 STEP 4: Basic Rules for Effective Aseptic Processing (20 minutes) • Use a „no touch‟ technique whenever possible. o Handle small articles with sterile forceps and, when sterile apparatus must be touched, handle as distant as possible from the part which will come into contact with a sterile liquid or solid, this rule applies even though sterile gloves may be worn • Reduce air disturbances to a minimum o Standard procedures should be designed to minimize movement of personnel within the clean room. Objects should be positioned within reach under the laminar air flow cabinet. Sharp and sudden movements should be avoided. • Consider the arrangement of objects under the laminar air flow (LAF) o Clean air should not flow over dirty articles to contaminate sterile articles, the cabinet should not be loaded with unnecessary equipment, and materials required should be carefully selected and arranged before beginning the procedure. • Refuse to be distracted o No interruption should be allowed until a set procedure has been completed. STEP 4: Key Points (5 minutes • Aseptic process requires careful control of the aseptic environment, of personnel practices and procedures, sterilization of equipment and components, extensive environmental monitoring and many other controls. • The number of controls required and the severe consequences of control failure make aseptic processing one of the highest-risk pharmaceutical processes. Quality risk management is an essential tool in ensuring product quality. STEP 5: Evaluation (5 minutes) • What is aseptic processing? • What is the requirements necessary to achieve strict asepsis 11 References Nelson, Philip (1993). Principles of Aseptic Processing and Packaging (3 ed.). USA: GMA Science and Education Foundation. Retrieved 19 April 2018. Sudan D., David, Jairus R. (2013). Handbook of aseptic processing and packaging. Graves, Ralph H., Szemplenski, Thomas. Boca Raton: Taylor & Francis. Hargreaves, Paul. (2018)"Recommendation on the Validation of Aseptic Processes". Pharmaceutical Inspection Co-Operation Scheme. PIC/S. Retrieved 8 May 2018.New York 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: 12 ← Previous TopicNext Topic →View all Pharmaceutics Theory and Compounding 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