<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>Bearing in mind the present scenario of the increasing biological tolerance of bacteria against antibiotics, a time controlled two pulse dosage form of amoxicillin was developed. The compression coating inlay tablet approach was used to deliver the drug in two pulses to different parts of the GIT after a well defined lag time between the two releases. This was made possible by formulating a core containing one of the two drug fractions (intended to be delivered as the second pulse), which was spray coated with a suspension of ethyl cellulose and a hydrophilic but water insoluble agent as a pore former (microcrystalline cellulose). Coating of up to 5 % (<italic>m/m</italic>) was applied over the core tablet, giving a corresponding lag of 3, 5, 7 and 12 h. Increasing the level of coating led to retardation of the water uptake capacity of the core, leading to prolongation of the lag time. Microcrystalline cellulose was used as a hydrophilic but water insoluble porosity modifier in the barrier layer, varying the concentration of which had a significant effect on shortening or prolongation of the lag time. This coated system was further partially compression coated with the remaining drug fraction (to be released as the first immediate release pulse) with a disintegrant, giving a final tablet. The core tablet and the final two pulse inlay tablet were further investigated for their <italic>in vitro</italic> performance.</p></abstract>

Bearing in mind the present scenario of the increasing biological tolerance of bacteria against antibiotics, a time controlled two pulse dosage form of amoxicillin was developed. The compression coating inlay tablet approach was used to deliver the drug in two pulses to different parts of the GIT after a well defined lag time between the two releases. This was made possible by formulating a core containing one of the two drug fractions (intended to be delivered as the second pulse), which was spray coated with a suspension of ethyl cellulose and a hydrophilic but water insoluble agent as a pore former (microcrystalline cellulose). Coating of up to 5 % (m/m) was applied over the core tablet, giving a corresponding lag of 3, 5, 7 and 12 h. Increasing the level of coating led to retardation of the water uptake capacity of the core, leading to prolongation of the lag time. Microcrystalline cellulose was used as a hydrophilic but water insoluble porosity modifier in the barrier layer, varying the concentration of which had a significant effect on shortening or prolongation of the lag time. This coated system was further partially compression coated with the remaining drug fraction (to be released as the first immediate release pulse) with a disintegrant, giving a final tablet. The core tablet and the final two pulse inlay tablet were further investigated for their in vitro performance.

A two pulse drug delivery system for amoxicillin: An attempt to counter the scourge of bacterial resistance against antibiotics

Alwar Pharmacy College, Alwar-301030, Rajasthan, India

Dr. Reddy Laboratories Ltd., Hyderabad-500034, India

Jamia Hamdard, Hamdard Nagar New Delhi-110062, India

Acta Pharmaceutica

Bearing in mind the present scenario of the increasing biological tolerance of bacteria against antibiotics, a time controlled two pulse dosage form of...

A two pulse drug delivery system for amoxicillin: An attempt to counter the scourge of bacterial resistance against antibiotics

Publié en ligne: 26 sept. 2011

Pages: 313 - 322

DOI: https://doi.org/10.2478/v10007-011-0026-2

Mots clés
amoksicilin, pulsativno oslobađanje lijeka, dva pulsa, vremenski odmak, etilceluloza, mikrokristalinična celuloza

This content is open access.

A two pulse drug delivery system for amoxicillin: An attempt to counter the scourge of bacterial resistance against antibiotics

Publié en ligne: 26 sept. 2011

Pages: 313 - 322

DOI: https://doi.org/10.2478/v10007-011-0026-2

Mots clésamoksicilin, pulsativno oslobađanje lijeka, dva pulsa, vremenski odmak, etilceluloza, mikrokristalinična celuloza

This content is open access.

Mots clés
amoksicilin, pulsativno oslobađanje lijeka, dva pulsa, vremenski odmak, etilceluloza, mikrokristalinična celuloza