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Factors Affecting
Bioavailability of drug
Ashutosh Gupta
M. Pharm (pharmaceutics)
From BIT Mesra Ranchi
Assistant Professor
at
Department of Pharmaceutics
College of Pharmacy
TMU Moradabad
1
CONTENTS
 Introduction of Bioavailability
 Objective of bioavailability studies
 Types of bioavailability
 Factors Affecting Bioavailability
 Pharmaceutical factors
 Pharmacological factors
 Route of administration
 Bibliography
2
Introduction of bioavailability
 The rate and extent at which the active concentration of a drug is available
at the desired site of action.
Bioavailability=
𝑨𝑼𝑪 𝒐𝒇 𝒐𝒓𝒂𝒍
𝑨𝑼𝑪 𝒐𝒇 𝑰𝑽
*
𝑰𝑽 𝒅𝒐𝒔𝒆
𝑶𝒓𝒂𝒍 𝒅𝒐𝒔𝒆
 In such cases, the dose available to the patient, called as bioavailable
dose. It often less than the administered dose.
 The amount of drug that reaches the systemic circulation is called as
systemic availability.
 The term bioavailable fraction F refers to the fraction of administered
dose that enters the systemic circulation.
𝐅 =
𝐁𝐢𝐨𝐚𝐯𝐚𝐢𝐥𝐚𝐛𝐥𝐞
𝐀𝐝𝐦𝐢𝐧𝐢𝐬𝐭𝐞𝐫𝐞𝐝 𝐝𝐨𝐬𝐞
3
 Primary stages of development of a suitable dosage foam for a new drug
entity to obtain evidence of its therapeutic utility.
Objective of bioavailability studies
Bioavailability studies are important in the-
 Determination of influence of excipients, patient-related factors and
possible interaction with other drug on the efficiency of absorption.
 Development of new formulations of the existing drugs.
4
 Control of quality of a drug product during the early stages of factors,
storages and stability on the drug absorption.
 Comparison of availability of a drug substance from different dosage
forms or from the same dosage from produced by different manufactures.
5
Types of bioavailability
There are two types of bioavailability
- Relative bioavailability
- Absolute bioavailability
 Relative bioavailability
The relative bioavailability is the systemic availability of a drug after oral
administration is compared with that of oral standard of the same drug.
𝐅𝐫 =
𝐎𝐫𝐚𝐥 𝐝𝐨𝐬𝐞 (𝐝𝐫𝐮𝐠)
𝐎𝐫𝐚𝐥 𝐝𝐨𝐬𝐞 (𝐬𝐭𝐚𝐧𝐝𝐚𝐫𝐝)
6
 Absolute bioavailability
when the systemic availability of a drug administered orally is comparison
to its intravenous administration, is called as absolute bioavailability .
𝐅 =
𝑶𝒓𝒂𝒍 𝒅𝒐𝒔𝒆
𝐈. 𝐕 𝐝𝐨𝐬𝐞
7
Factors affecting Bioavailability
There are various factors which affect the bioavailability of drug-
 Pharmaceutical factors
 Pharmacological factors
 Route of administration
8
Pharmaceutical Factors:
 It is expected that, bioavailability of drugs to be in this decreasing
order-
Solutions > Suspension > Capsule > Tablet > Coated Tablet
9
The Pharmaceutical factors include:
 Particle Size
 Salt Form
 Crystal Forms
 Nature of Excipients
 Degree of Ionisation
 Partition coefficient
 The method of manufacturing
10
Pharmacological Factors 11
The Pharmacological factors include:
 Gastric Emptying and Gastrointestinal Motility
 Gastrointestinal Diseases
 Food and Other Substances
 First Pass Metabolism
 Drug-Drug Interactions
12
Route of administration
 Parenteral
 Oral
 Topical
 Rectal
 Inhalation
Parenteral > Oral > rectal > Topical
13
Bibliography:
 Brahmankar D.M, biopharmaceutics and pharmacokinetics, New Delhi,
Vallabh Publications, 2012.
 Goodman L. S, Goodman & Gilman’s Pharmacological Basis of
Therapeutics, 13th Edition, New York; New Delhi, TataMcGraw-Hill
Education, 2017.
 Katzung B. G, Basic and Clinical Pharmacology, 14th Edition, New York;
New Delhi, TataMcGraw-Hill Education, 2017.
 Tripathi K.D, Essentials of Medical Pharmacology, 7th Edition, New
Delhi, Jaypee Brothers Publications, 2013.
14
ThankYou!

15

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Bioavailability and Factors Affecting Bioavailability of drug

  • 1. Factors Affecting Bioavailability of drug Ashutosh Gupta M. Pharm (pharmaceutics) From BIT Mesra Ranchi Assistant Professor at Department of Pharmaceutics College of Pharmacy TMU Moradabad 1
  • 2. CONTENTS  Introduction of Bioavailability  Objective of bioavailability studies  Types of bioavailability  Factors Affecting Bioavailability  Pharmaceutical factors  Pharmacological factors  Route of administration  Bibliography 2
  • 3. Introduction of bioavailability  The rate and extent at which the active concentration of a drug is available at the desired site of action. Bioavailability= 𝑨𝑼𝑪 𝒐𝒇 𝒐𝒓𝒂𝒍 𝑨𝑼𝑪 𝒐𝒇 𝑰𝑽 * 𝑰𝑽 𝒅𝒐𝒔𝒆 𝑶𝒓𝒂𝒍 𝒅𝒐𝒔𝒆  In such cases, the dose available to the patient, called as bioavailable dose. It often less than the administered dose.  The amount of drug that reaches the systemic circulation is called as systemic availability.  The term bioavailable fraction F refers to the fraction of administered dose that enters the systemic circulation. 𝐅 = 𝐁𝐢𝐨𝐚𝐯𝐚𝐢𝐥𝐚𝐛𝐥𝐞 𝐀𝐝𝐦𝐢𝐧𝐢𝐬𝐭𝐞𝐫𝐞𝐝 𝐝𝐨𝐬𝐞 3
  • 4.  Primary stages of development of a suitable dosage foam for a new drug entity to obtain evidence of its therapeutic utility. Objective of bioavailability studies Bioavailability studies are important in the-  Determination of influence of excipients, patient-related factors and possible interaction with other drug on the efficiency of absorption.  Development of new formulations of the existing drugs. 4
  • 5.  Control of quality of a drug product during the early stages of factors, storages and stability on the drug absorption.  Comparison of availability of a drug substance from different dosage forms or from the same dosage from produced by different manufactures. 5
  • 6. Types of bioavailability There are two types of bioavailability - Relative bioavailability - Absolute bioavailability  Relative bioavailability The relative bioavailability is the systemic availability of a drug after oral administration is compared with that of oral standard of the same drug. 𝐅𝐫 = 𝐎𝐫𝐚𝐥 𝐝𝐨𝐬𝐞 (𝐝𝐫𝐮𝐠) 𝐎𝐫𝐚𝐥 𝐝𝐨𝐬𝐞 (𝐬𝐭𝐚𝐧𝐝𝐚𝐫𝐝) 6
  • 7.  Absolute bioavailability when the systemic availability of a drug administered orally is comparison to its intravenous administration, is called as absolute bioavailability . 𝐅 = 𝑶𝒓𝒂𝒍 𝒅𝒐𝒔𝒆 𝐈. 𝐕 𝐝𝐨𝐬𝐞 7
  • 8. Factors affecting Bioavailability There are various factors which affect the bioavailability of drug-  Pharmaceutical factors  Pharmacological factors  Route of administration 8
  • 9. Pharmaceutical Factors:  It is expected that, bioavailability of drugs to be in this decreasing order- Solutions > Suspension > Capsule > Tablet > Coated Tablet 9
  • 10. The Pharmaceutical factors include:  Particle Size  Salt Form  Crystal Forms  Nature of Excipients  Degree of Ionisation  Partition coefficient  The method of manufacturing 10
  • 12. The Pharmacological factors include:  Gastric Emptying and Gastrointestinal Motility  Gastrointestinal Diseases  Food and Other Substances  First Pass Metabolism  Drug-Drug Interactions 12
  • 13. Route of administration  Parenteral  Oral  Topical  Rectal  Inhalation Parenteral > Oral > rectal > Topical 13
  • 14. Bibliography:  Brahmankar D.M, biopharmaceutics and pharmacokinetics, New Delhi, Vallabh Publications, 2012.  Goodman L. S, Goodman & Gilman’s Pharmacological Basis of Therapeutics, 13th Edition, New York; New Delhi, TataMcGraw-Hill Education, 2017.  Katzung B. G, Basic and Clinical Pharmacology, 14th Edition, New York; New Delhi, TataMcGraw-Hill Education, 2017.  Tripathi K.D, Essentials of Medical Pharmacology, 7th Edition, New Delhi, Jaypee Brothers Publications, 2013. 14