Course Objectives

To impart knowledge and skills necessary to train the students on par with the routine of Industrial activities in R&D and F&D

Learning Outcomes

On completion of this course it is expected that students will be able to understand-

• The scheduled activities in a Pharmaceutical firm.
• The pre formulation studies of pilot batches of pharmaceutical industry.
• The significance of dissolution and product stability.
• How to apply the knowledge and skills on drug development

Course Syllabus

Module-1: 

Preformulation Studies: Molecular optimization of APIs (drug substances), crystal morphology and variations, powder flow, structure modification, drug-excipient compatibility studies, methods of determination.

Module-2:

Formulation Additives: Study of different formulation additives, factors influencing their incorporation, role of formulation development and processing, new developments in excipient science. Design of experiments – factorial design for product and process development.

Module-3:

Solubility: Importance, experimental determination, phase- solubility analysis, pH-solubility profile, solubility techniques to improve solubility and utilization of analytical methods – cosolvency, salt formation, complexation, solid dispersion, micellar solubilization and hydrotropy.

Module-4:

Dissolution: Theories, mechanisms of dissolution, in-vitro dissolution testing models– sink and non-sink. Factors influencing dissolution and intrinsic dissolution studies. Dissolution test apparatus – designs, dissolution testing for conventional and controlled release products. Data handling and correction factor. Biorelevant media, in-vitro and in-vivo correlations, levels of correlations.

Module-5:

Product Stability: Degradation kinetics, mechanisms, stability testing of drugs and pharmaceuticals, factors influencing-media effects and pH effects, accelerated stability studies, interpretation of kinetic data (API & tablets). Solid state stability and shelf life assignment. Stability protocols, reports and ICH guidelines.

Session Plan

Session 1

Preformulation Studies-Introduction

Pharmaceuticals Preformulation

Session 2

Molecular optimization of APIs (drug substances), crystal morphology and variations

Molecular optimization of APIs ( DRUG SUBSTANCES)

Session 3

Powder flow, structure modification

Session 4

Drug-excipient compatibility studies, methods of determination

Drug-Excipient Compatibility Studies in Formulation Development_

Session 5

Study of different formulation additives

FORMULATION ADDITIVES

Session 6

Factors influencing their incorporation, role of formulation development and processing, new developments in excipient science

FORMULATION ADDITIVES

Session 7

Design of experiments – factorial design for product and process development

Design of experiments – factorial design for product and process development

Session 8

Importance of Solubility, experimental determination

Importance of Solubility

Session 9

Phase- solubility analysis, pH-solubility profile

Session 10

Solubility techniques to improve solubility and utilization of analytical methods

Session 11

Cosolvency, salt formation, complexation, solid dispersion, micellar solubilization and hydrotropy

Session 12

Dissolution-Theories

Dissolution

Session 13

Mechanisms of dissolution

Mechanism of Dissolution

Session 14

In-vitro dissolution testing models– sink and non-sink

Session 15

Factors influencing dissolution and intrinsic dissolution studies

Session 16

Dissolution test apparatus – designs

DissolutionandDissolutionApparatusAReview

Session 17

Dissolution testing for conventional and controlled release products

Session 18

Data handling and correction factor Biorelevant media

Session 19

in-vitro and in-vivo correlations, levels of correlations.

Session 20

Product Stability-Degradation kinetics

Session 21

Mechanisms, stability testing of drugs and pharmaceuticals

Session 22

Factors influencing-media effects and pH effects, accelerated stability studies, interpretation of kinetic data (API & tablets)

Session 23

Solid state stability and shelf life assignment. Stability protocols, reports and ICH guidelines.

References

1. Lachman L, Lieberman HA, Kanig JL. The Theory and Practice Of Industrial Pharmacy, 3^rd ed., Varghese Publishers, Mumbai 1991.
2. Sinko PJ. Martin's physical pharmacy and pharmaceutical sciences, 5^th ed., B.I. Publications Pvt. Ltd, Noida, 2006.

3. Lieberman HA, Lachman L, Schwartz JB. Pharmaceutical dosage forms: tablets Vol. I-III, 2^nd, CBS Publishers & distributors, New Delhi, 2005.
4. Conners KA. A Text book of pharmaceutical analysi Wells JI. Pharmaceutical preformulation: Thephysicochemical properties of drug substances. Ellis Horwood Ltd., England, 1998.
5. Yalkowsky SH. Techniques of solubilization of drugs. Vol-12. Marcel Dekker Inc., New York, 1981
6. Dressman J, Kramer J. Pharmaceutical dissolution testing. Saurah printer pvt. Ltd., New Delhi,2005.
7. Sethi PD. Quantitative analysis of drugs in pharmaceutical formulations, 3^rd, CBS publications, New Delhi, 2008.
8. Carstensen JT, Rhodes CT. Drug stability principles and practices, 3^rd,CBS Publishers & distributors, New Delhi, 2005.
9. Yoshioka S, Stella VJ. Stability of drugs and dosage forms, Springer (India) Pvt. Ltd., New Delhi, 2006.
10. Banker GS, Rhodes CT. Modern Pharmaceutics, 4^th , Marcel Dekker Inc, New York, 2005.
11. Grimm - Stability testing of drug products.
12. Mazzo DJ. International stability testing. Eastern Press Pvt. Ltd., Bangalore, 1999. 13. Beckett AH, Stenlake JB. Practical pharmaceutical chemistry, Part I & II., 4^th ,CBS Publishers & distributors, New Delhi, 2004.
13. Indian Pharmacopoeia. Controller of Publication. Delhi, 1996.
14. British Pharmacopoeia. British Pharmacopoeia Commission Office, London, 2008.
15. United States Pharmacopoeia. United States Pharmacopeial Convention, Inc, USA, 2003.
16. Encyclopaedia of Pharm. Technology, Vol I – III.
17. Wells J. I. Pharmaceutical Preformulation : The physicochemical properties of drug substances, Ellis Horwood Ltd. England, 1988.