Semi Solid Preparations – 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

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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

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• 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

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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

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• 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 Example: EDTA, citric acid

• Emulsifying agent: Reduces surface tension of two phases in an emulsion, preventing coalescence

of individual phases.

o Example: Detergent, emulsifying wax (detergent treated wax), cetostearyl alcohol,

polysorbate 20.

• Humectant: Promotes retention of water in a mixture Glycerin, propylene glycol, polyethylene

glycols (low MW).

• Permeation enhancer: Facilitates diffusion process of active ingredient across the stratum

corneum by chemical modification.

o Example: Ethanol, oleic acid, propylene glycol, polyethylene glycol (400)

• Preservative:

o Prevents or slows microbial growth; may be one of 4 major compound types: acid, alcohol,

quaternary ammonium compounds, or organic mercurial.

o Example: Acid: benzoic acid; alcohol: phenylethyl alcohol; quaternary ammonium: stearyl

dimethyl benzyl ammonium chloride; organic mercurial: thimerosal.

• Thickening agent: Increase viscosity; may be natural, semi-synthetic, or synthetic.

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o Example: Natural: cellulose, pectin; semi-synthetic: methylcellulose, (sodium)

carboxymethylcellulose; synthetic: Carbopol

STEP 7: Key Points (5 minutes)

• Pharmaceutical semisolid preparations: Is 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

• Ideal properties of semi – solid preparations include, physical properties, physiological properties,

application properties and storage properties

STEP 8: Evaluation (5 minutes)

• What are treatment target for semi – solid preparations?
• What are semis – solid pharmaceutical preparations?

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References

Britain, R. P. S. o. G. (1994). The Pharmaceutical Codex (12 ed.). London: London Pharmaceutical

Press.

Winfield, J. A. R., I. Smith. (2009). Pharmaceutical Practice (4th ed.)British

Wolverton, SE. Comprehensive Dermatologic Drug Therapy. WB Saunders. 2001. pp 563-572.New

York

Singh Malik, D; Mital, N; Kaur, G (2016). "Topical drug delivery systems: a patent review". Expert

opinion on therapeutic patents. 26 (2): 213–28. Sudan

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.

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