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Introduction of

Biopharmaceutics &

Pharmacokinetics

So what is this course about ??

So what is this course about ?? pharmaceutics Bio- Pharmacokinetics Here we will study factors affecting

pharmaceutics

So what is this course about ?? pharmaceutics Bio- Pharmacokinetics Here we will study factors affecting
  • Bio- Pharmacokinetics

So what is this course about ?? pharmaceutics Bio- Pharmacokinetics Here we will study factors affecting

Here we will study factors

affecting the entry of drugs

Here we will study kinetic’s of drug movement (both entry &

exit out of body)

So how is the course organized??

Factors affecting Drug Entry Drug Drug Distribution Elimination Mathematical Concepts in PK
Factors
affecting
Drug Entry
Drug
Drug
Distribution
Elimination
Mathematical
Concepts in PK

Concepts in Bioavailability/ BE

Biopharmaceutics

Drug response depends on several variables

Route of administration

Different dosage forms Physico-chem properties Excipients

Biopharmaceutics

Definition:

Biopharmaceutics is a study of factors affecting rate/amount of drug reaching systemic circulation

Route of administration Different dosage forms Physico-chem properties Excipients

Optimize drug efficacy

Important role of Biopharmaceutics in Drug

discovery & development

Solubility
Solubility
Pro--Drugs
Pro--Drugs

Particle Size

Stereo-Chem

Factors

Discovery
Discovery

Salt Formation

Crystalline state

Dissolution Rate

Formulations

Manufacturing process Development Stability
Manufacturing
process
Development
Stability

Permeability

Important role of Biopharmaceutics in Drug

discovery & development

Brivanib (BMS-540215) had shown excellent anti-cancer activity in animals & in-vitro

models, however the solubility was very poor. Poor solubility is known to affect the overall amount of drug entering body.

Solution:

Design a salt form of drug that has a better solubility. The discovery scientist developed

an alaninate salt that had much better solubility & better bioavailability

Important role of Biopharmaceutics in Drug

discovery & development

Vemurafenib, a blockbuster anti-cancer drug was hitting dose limiting solubility in clinical trials ( increase of drug did not lead to increase in drug conc due to poor solubility)

Solution:

Particle size of drug is known to affect solubility, can we reduce particle size to increase solubility, YES, That’s what the company did. They developed a micro-particle formulation that increased overall solubility

Important role of Biopharmaceutics in Drug

discovery & development

AIKTC therapeutics has a pain medicine already on market in tablet form, it wants to develop a sustained release formulation. What information will it need to develop this new formulation

Solution:

Understand the rate of drug absorption by tablet form, evaluate how sustain release will

affect absorption & ultimately the drug effect

Pharmacokinetics (PK)

For a better, safe use of drugs we need to know

Absorption Distribution

Metabolism

Excretion

Rate & Mechanism of ADME

Pharmacokinetics

Definition of Pharmacokinetics:

Study of time course of ADME and their relationship with therapeutic and toxic effects of drug

Role of PK in drug discovery

AIKTC-123 has a good anti-cancer activity in animals. we need to know what’s an effective dose in humans ??

Understand Metabolism/Excretion in animals

Understand overall

PK in animals

Predict what is PK in humans

Role of PK in drug discovery • AIKTC-123 has a good anti-cancer activity in animals. we

We know effective drug from animal studies

We know PK in humans

We know then calculate dose needed to get effect

Role of PK in drug development

Role of PK in drug development • Sunitinib is a anti-cancer drug that is metabolized by

Sunitinib is a anti-cancer drug that is metabolized by enzyme CYP3A4.

Doctor wants to know if he can give it with another drug ketoconazole which is CYP3A4 inhibitor

Ketoconazole will inhibit CYP3A4 sunitinib will not be metabolized

increase in concentration of sunitinib, might lead to toxicity

Role of PK in drug development

Brivanib is a anti-cancer drug that is developed to treat liver cancer

During the clinical trials, the doctor wants to know if he can give it to patients with liver impairment

Evaluate PK of brivanib in liver impaired patients See how different the exposure is compared to normal liver patients Accordingly advise doctors if the dose needs to be changed

THANK YOU -PHARMA STREET