NDLI: Canine Intestinal Contents vs. Simulated Media for the Assessment of Solubility of Two Weak Bases in the Human Small Intestinal Contents

Content Provider	Springer Nature Link
Author	Kalantzi, Lida Persson, Eva Polentarutti, Britta Abrahamsson, Bertil Goumas, Konstantis Dressman, Jennifer B. Reppas, Christos
Copyright Year	2006
Abstract	This study was conducted to assess the relative usefulness of canine intestinal contents and simulated media in the prediction of solubility of two weak bases (dipyridamole and ketoconazole) in fasted and fed human intestinal aspirates that were collected under conditions simulating those in bioavailability/bioequivalence studies.After administration of 250 mL of water or 500 mL of Ensure plus® [both containing 10 mg/mL polyethylene glycol (PEG) 4000 as nonabsorbable marker], intestinal aspirates were collected from the fourth part of the duodenum of 12 healthy adults and from the mid-jejunum of four Labradors. Pooled samples were analyzed for PEG, pH, buffer capacity, osmolality, surface tension, pepsin, total carbohydrates, total protein content, bile salts, phospholipids, and neutral lipids. The shake-flask method was used to measure the solubility of dipyridamole and ketoconazole in pooled human and canine intestinal contents and in fasted-state-simulating intestinal fluid (FaSSIF) and fed-state-simulating intestinal fluid (FeSSIF) containing various bile salts and pH-buffering agents.For both compounds, solubility in canine contents may be predictive of human intralumenal solubility in the fasting state but not in the fed state. The poor agreement of results in canine and human aspirates can be attributed to the higher bile salt content in canine bile. Solubility in FaSSIF containing a mixture of bile salts from crude bile predicted satisfactorily the intralumenal solubility of both drugs in the fasted state in humans. Solubility in FeSSIF, regardless of the identity of bile salts or of the buffering species, deviated from intralumenal values in the fed human aspirates by up to 40%. This was attributed to the lack of lipolytic products in FeSSIF, the higher bile salt content of FeSSIF, and the lower pH of FeSSIF.FaSSIF containing a mixture of bile salts from crude bile, and FeSSIF containing lipolytic products and, perhaps, having lower bile salt content but slightly higher pH, should be more useful than canine intestinal aspirates for predicting intralumenal solubilities in humans.
Starting Page	1373
Ending Page	1381
Page Count	9
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	23
Issue Number	6
e-ISSN	1573904X
Language	English
Publisher	Springer-Verlag
Publisher Date	2006-05-25
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	canine intestinal fluid dipyridamole FaSSIF FeSSIF human intestinal fluid ketoconazole solubility Pharmacology/Toxicology Pharmacy Biochemistry Medical Law Biomedical Engineering
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

Estimation of Intragastric Solubility of Drugs: In What Medium?

Computational Prediction of Drug Solubility in Fasted Simulated and Aspirated Human Intestinal Fluid

Computational Prediction of Drug Solubility in Fasted Simulated and Aspirated Human Intestinal Fluid

Forecasting the Oral Absorption Behavior of Poorly Soluble Weak Bases Using Solubility and Dissolution Studies in Biorelevant Media

Dissolution of Hydrocortisone in Human and Simulated Intestinal Fluids

Precipitation in and Supersaturation of Contents of the Upper Small Intestine After Administration of Two Weak Bases to Fasted Adults

P-Glycoprotein Attenuating Effect of Human Intestinal Fluid

Postprandial Changes in Solubilizing Capacity of Human Intestinal Fluids for BCS Class II Drugs

Intestine, fasted-state simulated intestinal fluid (fassif) and fed-state simulated intestinal fluid (fessif), were (2009).

Canine Intestinal Contents vs. Simulated Media for the Assessment of Solubility of Two Weak Bases in the Human Small Intestinal Contents

Similar Documents

Estimation of Intragastric Solubility of Drugs: In What Medium?

Computational Prediction of Drug Solubility in Fasted Simulated and Aspirated Human Intestinal Fluid

Computational Prediction of Drug Solubility in Fasted Simulated and Aspirated Human Intestinal Fluid

Forecasting the Oral Absorption Behavior of Poorly Soluble Weak Bases Using Solubility and Dissolution Studies in Biorelevant Media

Dissolution of Hydrocortisone in Human and Simulated Intestinal Fluids

Precipitation in and Supersaturation of Contents of the Upper Small Intestine After Administration of Two Weak Bases to Fasted Adults

P-Glycoprotein Attenuating Effect of Human Intestinal Fluid

Postprandial Changes in Solubilizing Capacity of Human Intestinal Fluids for BCS Class II Drugs

Intestine, fasted-state simulated intestinal fluid (fassif) and fed-state simulated intestinal fluid (fessif), were (2009).

Canine Intestinal Contents vs. Simulated Media for the Assessment of Solubility of Two Weak Bases in the Human Small Intestinal Contents