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3 results on '"drug partition"'

1. Drug Permeation through Membranes I: Effect of Various Substances on Amobarbital Permeation through Polydimethylsiloxane

Author

Lovering, Edward G. and Black, Donald B.

Abstract

The effect of some excipients, nutrients, surfactants, and adsorbents on the permeation of amobarbital through polydimethylsiloxane was measured. At a pH of 5, the permeability coefficient, P, of amobarbital is (7.70 ± 0.34) × 10−8cm.2sec.−1. The rate of drug transfer across the membrane depends on pH because only the unionized species is eligible for transfer. If Pis calculated from the actual concentration of unionized drug, then transfer is not a function of pH. Excipients typical of those used in Canadian formulations of amobarbital or its sodium salt have no significant effect on the coefficient of permeability. Bovine albumin has no effect, but the coefficient is depressed by skim milk, perhaps due to binding of the drug. The drug is strongly adsorbed by charcoal. The permeation coefficient is reduced by anionic, cationic, and nonionic surfactants in a way that is consistent with the concept of drug partition between the aqueous and surfactant phases present when surfactant micelles form in water. After dissolution, the permeability coefficients of all Canadian amobarbital preparations tested were found to be identical.

Published
1973
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2. Drug permeation through membranes. I. Effect of various substances on amobarbital permeation through polydimethylsiloxane

Author

Donald B. Black and Edward G Lovering

Subjects
Amobarbital, Pharmaceutical Science, In Vitro Techniques, Micelle, Permeability, Biopharmaceutics, Surface-Active Agents, Pulmonary surfactant, medicine, Pharmaceutic Aids, Animals, Dissolution, Chromatography, Aqueous solution, Chemistry, Sodium Dodecyl Sulfate, Membranes, Artificial, Serum Albumin, Bovine, Permeation, Hydrogen-Ion Concentration, Models, Theoretical, Rats, Membrane, Milk, Intestinal Absorption, Pharmaceutical Preparations, Permeability (electromagnetism), Charcoal, Silicone Elastomers, Spectrophotometry, Ultraviolet, medicine.drug
Abstract

The effect of some excipients, nutrients, surfactants, and adsorbents on the permeation of amobarbital through polydimethylsiloxane was measured. At a pH of 5, the permeability coefficient, P, of amobarbital is (7.70 ± 0.34) × 10−8 cm.2 sec.−1. The rate of drug transfer across the membrane depends on pH because only the unionized species is eligible for transfer. If P is calculated from the actual concentration of unionized drug, then transfer is not a function of pH. Excipients typical of those used in Canadian formulations of amobarbital or its sodium salt have no significant effect on the coefficient of permeability. Bovine albumin has no effect, but the coefficient is depressed by skim milk, perhaps due to binding of the drug. The drug is strongly adsorbed by charcoal. The permeation coefficient is reduced by anionic, cationic, and nonionic surfactants in a way that is consistent with the concept of drug partition between the aqueous and surfactant phases present when surfactant micelles form in water. After dissolution, the permeability coefficients of all Canadian amobarbital preparations tested were found to be identical.

Published
1973

3. Drug Design : Medicinal Chemistry: A Series of Monographs, Vol. 4

Author

E. J. Ariëns and E. J. Ariëns

Subjects
Pharmaceutical chemistry--Juvenile literature, Pharmacology--Juvenile literature
Abstract

Drug Design, Volume IV covers the pharmaceutical phase of drug action, with emphasis on those aspects that are of importance in the design of optimally effective drug products. The book discusses biopharmaceutics as a basis for the design of drug products; the types and pharmacokinetics of peroral prolonged action dosage forms and parenteral prolonged action forms; and the design of topical drug products. The text also describes physical-chemical parameters which affect the bioavailability of topical drug products; the design of sunscreen preparations; as well as the clinical application of litholytic agents, which are preventive and curative drugs for nephrolithiasis. The design of biologically active nucleosides and of insecticidal chlorohydrocarbon derivatives is also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design will find the book invaluable.

Published
1973

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