Hoffmann-la Roche Inc.

Joel Unowsky

Navnit Hargovindas Shah

Charanjit R Behl

Martin Howard Infeld

Jacques L Tossounian

Maria Oksana Bachynsky

George Beskid

The oral absorption of antibiotics given of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of Laureth-12 together with a second component salts of capric acid and caprylic acids. The antibiotic containing two component enhancer system includes Miglyol-812 for optimum absorption.

Absorption enhancement of antibiotics

The absorption of antibiotics given through oral and rectal routes of administration is significantly enhanced by use of the antibiotic in conjunction with a two-component absorption enhancing system made up of an ether of a C.sub.6 to C.sub.18 alcohol and a polyoxyethylene glycol together with a second component selected from among polyoxyethylene glycol C.sub.6 to C.sub.18 glyceride esters, C.sub.6 to C.sub.18 carboxylic acids or salts thereof, and esters of two or more C.sub.6 to C.sub.18 carboxylic acids, glycerol and a polyoxyethylene glycol. A carrier and adjuvants are usually included. These compositions can be administered in any convenient oral or rectal dosage form, including tablets, capsules, beadlets and suppositories.

The rectal absorption of the beta-lactam antibiotic ceftriaxone in a solid dosage form is enhanced with chenodeoxycholic acid or its sodium salt, in the presence of a carrier consisting of a mixture of two or more glycerides of C.sub.12 to C.sub.18 fatty acids.

Rectal dosage form

There is presented a method, in the form of a dosage formulation, for transforming substantially orally inactive .beta.-lactam antibiotics or their pharmaceutically acceptable salts or the esters, ethers, or hydrates of said antibiotics or their salts into orally active compounds by combination of the chosen .beta.-lactam antibiotic with an enhancer comprising an aliphatic, preferably a C.sub.2 to C.sub.18, straight- or branched-chain, saturated or unsaturated, fatty acid or an aliphatic, preferably a C.sub.2 to C.sub.12, straight- or branched-chain, saturated or unsaturated, fatty acid mono-, di- or triglyceride or mixtures thereof, partial or total esters of propylene glycol, polyethylene glycol and carbohydrates of C.sub.2 to C.sub.12 fatty acids, as well as the pharmaceutically acceptable esters and ethers of said glycerides. The antibiotic and enhancer mixture may be administered orally as a solid dosage form with the .beta.-lactam antibiotic above or, optionally, with the enhancer protected by an enteric coating.

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Livingston, NJ, United States of America

Joel Unowsky