It is a course intended to give the students an insight into the
problems of making dosage forms of drugs. It brings together the various sciences that are involved in the development of formulae of pharmaceutical products and in evaluation of their qualities. The laboratory component involves some fundamental exercises in the evolution of formulae of products such as tablets, ointments, solutions, parenteral products, sustained action medications etc. It also imparts knowledge of newer dosage forms.
Text Book:
Mithal B.M., Text Book of Pharmaceutical Formulation, Vallabh
Prakashan, 6th edn., Delhi, 1997. Lect. Topics to be Learning Objectives Reference No. covered Books Formulation – an Basic principles of formulation 1 Ch.1 introduction The Drug Understanding different dosage 2 delivery systems forms and their characteristics Ch.2 & classification Components of a Understanding formulation 3 Ch.2 dosage form ingredients and their effect Design of dosage How a dosage form is formulated and 4 Ref 2 (i) forms how to modify it for better action Physical Understanding how physical properties of characteristics of a drug and 5 Ch.3 drugs & formulation component affect formulation formulation Chemical Understanding how chemical properties of characteristics of a drug and 6 Ch.4 drugs & formulation component affect formulation formulation Understanding how physicochemical Biopharmaceutica characteristics of a drug and 7-8 l characters of Ch.5 formulation component affect drugs bioactivity Understanding of formulation Tablets and 9-13 aspects, manufacture of Ch.13 pellets tablets and pellets Formulation design and 14-16 Capsules Ch.14 manufacture capsules Types of Parenterals and their formulation aspects Parenteral Understanding of design and 17-19 Ch.21 products requirements of manufacturing facilities for sterile dosage forms Ocular Formulation and quality 20 dosage control of ophthalmic Ch. 22 forms products. How to make drug release Sustained release 21-23 from a formulation slow and Ch.23 dosage forms controllable. Process of coating of a Coating & formulation; Process for 24-26 Ch.32 Microencapsulation making microencapsulated dosage form. How to formulate a Transdermal drug 27 transdermal drug delivery Ch.24 delivery systems system Targeted Drug Designing targeted drug 28-30 Ch. 25 Delivery Systems delivery systems Other novel drug Designing of various novel Ch. 26 31-32 delivery systems drug delivery systems & 29 Quality control of Quality control of dosage 33 Ch.32 dosage forms forms CGMP and Process CGMP and Process Validation 34 Ref. Validation Component Duration Weightage Date & Remarks (%) Time Surprise Tests* 10 min 15 During CB semester Mid-Term Test 90 minutes 30 To be CB announced Laboratory 20 Lab hours Components$ Comprehensive 3 hrs 35 To be OB/CB Exam announced
* Surprise tests will be conducted during class/tutorials on the basis
of topics covered in class $ Lab component will consists: Day to day work 10 %; Lab viva + quiz 5%; Lab compre. 5% Formulation – an introduction Drug ? • Active drug substance (active pharmaceutical ingredient - API) •Chemical compound with pharmacological (or other direct effect ) intended for used in diagnosis, treatment or prevention of diseases Direct clinical use of the active drug substances is rare: Why?? •API handling and Accurate dosing can be difficult or impossible (e.g., potent drugs: low mg and μg doses) •API administration can be impractical/unfeasible because of smell, taste and low activity. •Some API are chemically unstable in light, moisture, O2 •API can be degraded at the site of administration (e.g., low pH in stomach). •API may cause local irritations or injury when they are present at high concentrations at the site of administration. •Administration of active substance would mean to have no chance for modification (improvement) of its PK profile. Dosage Forms
Definition: Dosage forms are the means by
which drug molecules / APIs are delivered to sites of action within the body to produce optimum desired effects and minimum adverese effect. Need of dosage forms: overcoming the difficulties 1. To provide for the safe and convenient delivery of accurate dosage. Examples: Tablets, Capsules, syrups 2. Reduction is frequency of doasing (sustained and prolonged release delivery) 3. For the protection of a drug substance from the destructive influence of atmospheric oxygen or moisture and gastric acid (after oral administration). Example: enteric coated tablets 4. To conceal the bitter taste, salty obnoxious or odor of a drug substance. Examples: Capsules, coated tablets, flavored syrups Need of dosage forms: overcoming the difficulties 5. To provide liquid preparations of substances that are either insoluble or unstable in the desired vehicle. Example: suspension 6. To provide extended drug action through controlled release mechanisms Examples: controlled release tablets, capsules, suspensions 7. To provide optimal drug action from topical administration sites Examples: ointments, creams, ophthalmic, ear and nasal preparations 8. To improve bioavailability of drug with narrow absorption window (gastro-retentive delivery). Need of dosage forms: overcoming the difficulties 9. To provide for insertion of a drug into one of the body’s orifices Examples: rectal and vaginal suppositories 10. To provide for the placement of drugs within body tissues. Examples: Implants 12. In addition, many dosage forms permit ease of drug identification through distinctiveness of color, shape, or identifying markings Types of Dosage Forms TYPES OF DOSAGE FORMS: Physical TYPES OF DOSAGE FORMS: Route of Administration TYPES OF DOSAGE FORMS: Combined Table General Considerations in Dosage Form Design Drug substances are seldom administered in their natural or pure state, but rather as part of a formulation in combination with one or more non-medicinal agents that serve varied and specialized pharmaceutical functions Through selective use of these non-medicinal agents, referred to as excipients, pharmaceutical ingredients, or adjuncts, pharmaceutical preparations of various types result. It is the pharmaceutical excipients that serves to solubilize, suspend, thicken, dilute, emulsify, stabilize, preserve, color, flavor and fashion the many and varied medicinal agents into effective and appealing pharmaceutical preparations. The term “Pharmaceutics” which is the study that concerns itself with the physical, chemical and biological factors which influence the formulation, manufacture, stability and effectiveness of pharmaceutical dosage forms. General Considerations in Dosage Form Design 1. Drug Consideration in Dosage Form Design 1.1 Characteristics of Drug Substances 1.2 Drug Stability 1.3 Determining Drug Formulation Stability 1.4 Prevention Against Microbial Contamination 1.5 Appearance and Palatability 2. Therapeutic Considerations in Dosage Form Design 2.1 Nature of the disease or illness 2.2 Age of the Patient 3. Biopharmaceutics Considerations 3.1 Biopharmaceutics 3.2 Concept of Bioavailability Oral Dosage Form 1. Should have appropriate disintegration and dissolution time 2. Should be stable in the GI environment : Both pH and enzyme stability 3. Should be available for absorption at the appropriate location 4. Drugs which are susceptible for degradation should be coated properly 5. Drug – food interaction should be taken into account. Nature and quantity of food staffs influence gastric emptying time and alter absorption rate 6. Oral dosage forms should have appropriate organoleptic properties. Systemic Dosage Form 1. Must contain only the most needed additives in the smallest possible quantity 2. Absorption is dependent on the administration site; however, bioavailability is normally ~100% 3. By proper selection of vehicle and administration site, can be made sustained release formulation 4. Sterility is very important: product design should be done accordingly. Topical Dosage Form 1. Base must be selected based on ease of application and removal. 2. Viscosity, absorption and transfer rate into skin should be optimized 3. Evaporation rate should be optimal 4. Particle size should be proper so as to prevent gritty feeling 5. Should have good spreading and covering capacity
FORMULATION AND EVALUATION OF MICONAZOLE NITRATE LOADED NANOSPONGES FOR VAGINAL DRUG DELIVERY P.Suresh Kumar, N.Hematheerthani J.Vijaya Ratna and V.Saikishor