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Sci. Pharm. 2014, 82(2), 423-440; doi:10.3797/scipharm.1301-27

Development of Press-Coated, Floating-Pulsatile Drug Delivery of Lisinopril

1
Department of Pharmaceutics, MAEER’s Maharashtra Institute of Pharmacy, Kothrud, Pune, 411 038, Maharashtra, India
2
Quality Assurance, Nulife Pharmaceuticals, Pimpri, 411 018 Pune, Maharashtra, India
3
Department of Pharmaceutical Chemistry, MAEER’s Maharashtra Institute of Pharmacy, Kothrud, Pune, 411 038, Maharashtra, India
*
Author to whom correspondence should be addressed.
Received: 30 January 2013 / Accepted: 14 April 2014 / Published: 14 April 2014
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Abstract

Lisinopril is an angiotensin-converting enzyme (ACE) inhibitor, primarily used for the treatment of hypertension, congestive heart failure, and heart attack. It belongs to BCS class III having a half-life of 12 hrs and 25% bioavailability. The purpose of the present work was to develop a press-coated, floating-pulsatile drug delivery system. The core tablet was formulated using the super-disintegrants crosprovidone and croscarmellose sodium. A press-coated tablet (barrier layer) contained the polymer carrageenan, xanthan gum, HPMC K4M, and HPMC K15M. The buoyant layer was optimized with HPMC K100M, sodium bicarbonate, and citric acid. The tablets were evaluated for physical characteristics, floating lag time, swelling index, FTIR, DSC, and in vitro and in vivo behavior. The 5% superdisintgrant showed good results. The FTIR and DSC study predicted no chemical interactions between the drug and excipients. The formulation containing xanthan gum showed drug retaining abilities, but failed to float. The tablet containing HPMC K15M showed a high swelling index. The lag time for the tablet coated with 200 mg carrageenan was 3±0.1 hrs with 99.99±1.5% drug release; with 140 mg HPMC K4M, the lag time was 3±0.1 hrs with 99.71±1.2% drug release; and with 120 mg HPMC K15M, the lag time was 3±0.2 hrs with 99.98±1.7% drug release. The release mechanism of the tablet followed the Korsmeyer-Peppas equation and a first-order release pattern. Floating and lag time behavior have shown good in vitro and in vivo correlations.
Keywords: Floating; Press-coated; Carrageenan; Xanthan; Pulsatile; Delivery Floating; Press-coated; Carrageenan; Xanthan; Pulsatile; Delivery
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

JAGDALE, S.C.; SURYAWANSHI, V.M.; PANDYA, S.V.; KUCHEKAR, B.S.; CHABUKSWAR, A.R. Development of Press-Coated, Floating-Pulsatile Drug Delivery of Lisinopril. Sci. Pharm. 2014, 82, 423-440.

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