Course

Unit 1

Preformulation-

· Drug Excipient interactions – Types and different methods to determine interactions

· Solid State properties : Crystalline state, polymorphism and pharmaceuticals, Solvates Cocyrstal and salts, crystal structure prediction, Solubility.

· Stability testing: Kinetics of stability, ICH Guidelines for accelerated and real time studies . Preparation and stability of large and small volume Parenterals.

· Theories of disperse systems: Particle size analysis, rheological measurements, temperature and gravitational stress test of pharmaceutical dispersion systems like SMEDDS.

Unit 2

Protein Pharmaceuticals and Stability:

· Physicochemical characterization of protein molecules

· Physical and chemical Stability Challenges Strategies for OvercomingStability Challenges

· Role of Excipients in Protein Formulations

· Formulation Design and Development

· Freeze-Drying and Lyophilization Techniques

· Stability testing of protein pharmaceuticals and RegulatoryConcerns

Unit 3

· Validation:

Introduction to Pharmaceutical Validation, Scope & merits of Validation, Types of validation. Validation of Tablets.

· Good manufacturing practices

Objectives and policies of current good manufacturing practices, layout of buildings, services, equipments and their maintenance. Layout of buildings. (3hrs)

Unit 4

· Physics of Tablet Compression, Consolidation, Effect of friction, distribution of forces

· Compaction profiles, Heckel Plots

Unit 5

· Definitions, Fundamentals and applications of diffusion and dissolution in Pharmacy, Diffusion and Dissolution parameters, USP III and IV Apparatus with applications .

· Similarity factors – f2 and f1, Higuchi and Peppas plot.

· Official and non official methods for dissolution testing, Method Development and Validation.

Assignments

1. Comaparative Analysis of Predictive dissolution Methodologies: Biorelevant Dissolution vs. Quality Control Dissolution .

2. Current Good Manufacturing Practices (cGMP) in Dissolution Testing: Role of cGMP in ensuring the reliability and consistency of dissolution testing.

3. Mini tablets and multiparticulate systemsfor enhancing drug delivery in paediatrics and geriatrics.Technical Challeges in formulation, scalability, uniformity, and stability.

4. Case studies involving preformulation of pharmaceutical products like amorphous solid dispersion and lipid based drug delivery system.

5. Overview of the pharmaceutical industry: Size, scope. Significance in drug discovery, biotechnology advancements and personalized medicine.

6. Challenges faced in developing stable protein formulations . Examples of successful protein formulations and their impact on therapeutic outcomes.

This course is designed to impart advanced knowledge and skills required to learn various aspects of formulation and concepts in pharmaceutical industries. It deals with the study of physical and chemical properties of the drug substance for effective dosage form development. It also emphasizes the study of compatibility between excipients and drugs in designing a stable dosage form. The need and significance of protein stability and formulation is also highlighted. It discusses the scope of pharmaceutical validation which involves activities aim at developing products with predetermined specifications and standards.

The subject focuses the importance of solid state pharmaceuticals in stability, formulation development and bioavailability as well as the scope of disperse systems and its characterisation. It imparts knowledge on the physics behind the process of tablets that helps formulation scientists to optimize the manufacturing process. It also explores the importance of dissolution and diffusion mechanisms and its role in drug formulation and bioavailability.

COURSE LEARNING OUTCOMES

Upon successful completion of the course, the student shall be able to;

KNOWLEDGE

K1: Outline the concept and elements of preformulation

K2: Illustrate the types and methods to determine the drug-excipient interaction.

K3: Examine pharmaceutical validation of tablets

K4: Discuss the stability testing methods of pharmaceuticals

K5: Describe the properties and characterisation of disperse systems

K6: Compare the methods for diffusion and dissolution

SKILL

S1: Determine the preformulation parameters of selected drugs

S2: Perform the stability studies of formulation

S3: Determine the solubility of different drugs

S4: Interpret the particle size of dispersion systems

S5: Demonstrate the drug –excipient compatibility studies

S6: Assess the dissolution mechanism of formulation.

ATTITUDE

A1: Foster a sense of responsibility

A2: Promote group discussions

A3: Build empathy and compassion

A4.Appreciate innovations

A5: Cultivate adaptability

A6: Embrace proactive learning attitude

References:

1. Gilbert Banker, Christopher T. Rhodes, Modern Pharmaceutics 4th edition, 2009

2. Alexander Florence Modern Pharmaceutics Volume 1,2 5th edition, NewYork; Marcl Dekker; 2009

3. Leon Lachman, A. Lieberman, Joseph.l.Kanig. The theory of practice of Industrial Pharmacy, 4th edition. CBS Publisher’s and distributer’s, 2013

4. Patrick J Sinko,Martins Physical Pharmacy and Pharmaceutical Science, 4th edition 2004

Journals:

1. Journal of Pharmaceutical Sciences-Elsevier
2. Pharmaceutical Research-Springer
3. Molecular Pharmaceutics- ACS
4. Drug Development and Industrial Pharmacy-Taylor & Francis
5. Pharmaceutical Development and Technology – Taylor & Francis
6. European Journal of Pharmaceutical Sciences-Elsevier
7. The AAPS Journal-Springer