Enteric coated capsules of eprosartan mesylate with pH-modifier for augmenting the dissolution

Damodaram Atmakuri, Zenab Attari, Girish Pai, K. B. Koteshwara

Research output: Contribution to journalArticle

Abstract

Eprosartan mesylate, an antihypertensive, exhibits low oral bioavailability due to its ionization at alkaline pH. An attempt has been made to prepare enteric coated capsule containing drug and maleic acid, as dosage form. Male-ic acid acts as pH-modifier, facilitates the absorption of drug by reducing the pH of intestinal environment (prefer-ably duodenum) so as to reduce the ionization of eprosartan, once the capsule reaches the duodenum. The capsules were coated with eudragit L100-55 (enteric coating agent) by dip method and evaluated for % weight gain to ensure coating. The capsules coated with 300 mg eudragit L100-55 in 5 ml acetone showed 9-10% weight gain and maximum drug release at the end of the 180 min. This was considered optimized formulation. The coated capsules were filled with drug and maleic acid and evaluated for drug release in the acid (pH 1.2) and alkaline (pH 6.2) media. The optimized capsules exhibited optimum dissolution profile with the maximum release of drug in the alkaline medium.

Original languageEnglish
Pages (from-to)34-38
Number of pages5
JournalInternational Journal of Research in Pharmaceutical Sciences
Volume7
Issue number1
Publication statusPublished - 2016

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Mesylates
Capsules
Duodenum
Weight Gain
Pharmaceutical Preparations
Acids
Dosage Forms
Acetone
Antihypertensive Agents
Biological Availability
eprosartan
Drug Liberation

All Science Journal Classification (ASJC) codes

  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

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abstract = "Eprosartan mesylate, an antihypertensive, exhibits low oral bioavailability due to its ionization at alkaline pH. An attempt has been made to prepare enteric coated capsule containing drug and maleic acid, as dosage form. Male-ic acid acts as pH-modifier, facilitates the absorption of drug by reducing the pH of intestinal environment (prefer-ably duodenum) so as to reduce the ionization of eprosartan, once the capsule reaches the duodenum. The capsules were coated with eudragit L100-55 (enteric coating agent) by dip method and evaluated for {\%} weight gain to ensure coating. The capsules coated with 300 mg eudragit L100-55 in 5 ml acetone showed 9-10{\%} weight gain and maximum drug release at the end of the 180 min. This was considered optimized formulation. The coated capsules were filled with drug and maleic acid and evaluated for drug release in the acid (pH 1.2) and alkaline (pH 6.2) media. The optimized capsules exhibited optimum dissolution profile with the maximum release of drug in the alkaline medium.",
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Enteric coated capsules of eprosartan mesylate with pH-modifier for augmenting the dissolution. / Atmakuri, Damodaram; Attari, Zenab; Pai, Girish; Koteshwara, K. B.

In: International Journal of Research in Pharmaceutical Sciences, Vol. 7, No. 1, 2016, p. 34-38.

Research output: Contribution to journalArticle

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