e-journal

Formulation and evaluation of controlled-release of telmisartan microspheres: In vitro/in vivo study

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The aim of this work was to design a controlled-release drug-delivery system for the angiotensin-II receptor antagonist drug telmisartan. Telmisartan was encapsulated with different EUDRAGIT polymers by an emulsion solvent evaporation technique and the physicochemical properties of the formulations were characterized. Using a solvent evaporation method, white spherical microspheres with particle sizes of 629.9e792.1 mm were produced. The in vitro drug release was studied in three different pH media (pH 1.2 for 2 hours, pH 6.8 for 4 hours, and pH 7.4 for 18 hours). The formulations were then evaluated for their pharmacokinetic parameters. The entrapment efficiency of these microspheres was between 58.6% and 90.56%. The obtained microspheres showed good flow properties, which were evaluated in terms of angle of repose (15.29e26.32), bulk and tapped densities (0.37e0.53 and 0.43e0.64, respectively), Carr indices and Hausner
ratio (12.94e19.14% and 1.14e1.23, respectively). No drug release was observed in the simulated gastric medium up to 2 hours; however, a change in pH from 1.2 to 6.8 increased the drug release. At pH 7.4, formulations with EUDRAGIT RS 100 showed a steady drug release. The microsphere formulation TMRS-3 (i.e., microspheres containing 2-mg telmisartan) gave the highest Cmax value (6.8641 mg/mL) at 6 hours, which was three times higher than Cmax for telmisartan oral suspension (TOS). Correspondingly,the area under the curve for TMRS-3 was 8.5 times higher than TOS. Particle size and
drug release depended on the nature and content of polymer used. The drug release mechanism of the TMRS-3 formulation can be explained using the Higuchi model. The controlled release of drug from TMRS-3 also provides for higher plasma drug content and improved bioavailability.

Keywords:
Microsphere Release kinetics Solvent evaporation Telmisartan

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Informasi Detail

Judul Seri

j o u rnal of food and drug a n a l y s i s

No. Panggil

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Penerbit

: Elsevier Taiwan., 2014

Deskripsi Fisik

j o u rnal of food and drug a n a l y s i s 2 2 ( 2 0 1 4 ) 5 4 2 e5 4 8

Bahasa

English

ISBN/ISSN

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Klasifikasi

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Tipe Isi

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Tipe Media

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Tipe Pembawa

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Edisi

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Subjek

Food And Health

Info Detail Spesifik

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Pernyataan Tanggungjawab

Wati/Agus

Versi lain/terkait

Lampiran Berkas

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