NDLI: Elucidating the Role of Dose in the Biopharmaceutics Classification of Drugs: The Concepts of Critical Dose, Effective In Vivo Solubility, and Dose-Dependent BCS

Content Provider	Springer Nature Link
Author	Charkoftaki, Georgia Dokoumetzidis, Aristides Valsami, Georgia Macheras, Pas
Copyright Year	2012
Abstract	To develop a dose dependent version of BCS and identify a critical dose after which the amount absorbed is independent from the dose.We utilized a mathematical model of drug absorption in order to produce simulations of the fraction of dose absorbed (F) and the amount absorbed as function of the dose for the various classes of BCS and the marginal cases in between classes.Simulations based on the mathematical model of F versus dose produced patterns of a constant F throughout a wide range of doses for drugs of Classes I, II and III, justifying biowaiver claim. For Classes I and III the pattern of a constant F stops at a critical dose Dose$_{cr}$ after which the amount of drug absorbed, is independent from the dose. For doses higher than Dose$_{cr}$, Class I drugs become Class II and Class III drugs become Class IV. Dose$_{cr}$ was used to define an in vivo effective solubility as S$_{eff}$ = Dose$_{cr}$/250 ml. Literature data were used to support our simulation results.A new biopharmaceutic classification of drugs is proposed, based on F, separating drugs into three regions, taking into account the dose, and Dose$_{cr}$, while the regions for claiming biowaiver are clearly defined.
Starting Page	3188
Ending Page	3198
Page Count	11
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	29
Issue Number	11
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2012-07-04
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Biochemistry Biomedical Engineering Pharmacy Medical Law Pharmacology/Toxicology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Quantitative Biopharmaceutics Classification System: The Central Role of Dose/Solubility Ratio

Does the Dose-Solubility Ratio Affect the Mean Dissolution Time of Drugs?

Powder Dissolution Method for Estimating Rotating Disk Intrinsic Dissolution Rates of Low Solubility Drugs

Biopharmaceutics Classification System: The Scientific Basis for Biowaiver Extensions

Computational Models to Assign Biopharmaceutics Drug Disposition Classification from Molecular Structure

Forecasting the In Vivo Performance of Four Low Solubility Drugs from Their In Vitro Dissolution Data

Scientific Perspectives on Extending the Provision for Waivers of In vivo Bioavailability and Bioequivalence Studies for Drug Products Containing High Solubility-Low Permeability Drugs (BCS-Class 3)

Prediction of Solubility and Permeability Class Membership: Provisional BCS Classification of the World’s Top Oral Drugs

The Mean Dissolution Time Depends on the Dose/Solubility Ratio

Elucidating the Role of Dose in the Biopharmaceutics Classification of Drugs: The Concepts of Critical Dose, Effective In Vivo Solubility, and Dose-Dependent BCS

Similar Documents

Quantitative Biopharmaceutics Classification System: The Central Role of Dose/Solubility Ratio

Does the Dose-Solubility Ratio Affect the Mean Dissolution Time of Drugs?

Powder Dissolution Method for Estimating Rotating Disk Intrinsic Dissolution Rates of Low Solubility Drugs

Biopharmaceutics Classification System: The Scientific Basis for Biowaiver Extensions

Computational Models to Assign Biopharmaceutics Drug Disposition Classification from Molecular Structure

Forecasting the In Vivo Performance of Four Low Solubility Drugs from Their In Vitro Dissolution Data

Scientific Perspectives on Extending the Provision for Waivers of In vivo Bioavailability and Bioequivalence Studies for Drug Products Containing High Solubility-Low Permeability Drugs (BCS-Class 3)

Prediction of Solubility and Permeability Class Membership: Provisional BCS Classification of the World’s Top Oral Drugs

The Mean Dissolution Time Depends on the Dose/Solubility Ratio

Elucidating the Role of Dose in the Biopharmaceutics Classification of Drugs: The Concepts of Critical Dose, Effective In Vivo Solubility, and Dose-Dependent BCS