Formulation and evaluation of intragastric floating drug delivery system of diltiazem hydrochloride

Main Article Content

Yogesh S Gattani
Durgacharan A Bhagwat
Akhil P Maske

Abstract

The present study is aimed towards formulation and evaluation of floating multiparticulate oral drug delivery system of diltiazem hydrochloride, which can provide sustained release. The work also aims to study various parameters
affecting the behavior of floating multiparticulate in oral dosage form. Floating microspheres were prepared by non-aqueous emulsification solvent evaporation technique, using ethyl cellulose and Eudragit RS-100 as the rate controlling polymer.The in vitro performance was evaluated by the usual pharmacopoeial and other tests such as drug-polymer compatibility, (%) yield, particle size analysis, drug entrapment efficiency, surface topography, in vitro floatability and release studies. Results show that the mixing ratio of components in the organic phase affected the size, size distribution (199-320 μm), drug content (59-84%), %yield (57-77%) and drug release of microsphere (45-99% after 12 h) and floating time >12 h. The best results were obtained at the ratio of drug: polymer Eudragit RS-100 (1:3). In most cases, good in vitro floating behavior was observed
and broad variety of drug release pattern could be achieved by variation of the polymer ratio, which was optimized to match target release profile. Stability studies showed no significant change in the drug content in the formulation even after 3 months.The data obtained in this study thus suggest that a micro particulate floating dosage form of diltiazem hydrochloride
can be successfully designed to give controlled delivery and improved oral bioavailability.

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How to Cite
Gattani, Y. S., Bhagwat, D. A., & Maske, A. P. (2014). Formulation and evaluation of intragastric floating drug delivery system of diltiazem hydrochloride. Asian Journal of Pharmaceutics (AJP), 2(4). https://doi.org/10.22377/ajp.v2i4.199
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References

Chawla G, Gupta P, Koradia V, Bansal AK. Gastroretention: A means to

address regional variability in intestinal drug absorption. 2003.

Yeole PG, Khan S, Patel VF. Floating drug delivery system: Need and

development. Indian J Pharm Sci 2005;67:265-72.

Singh BN, Kim KH. Floating drug delivery via gastric retention. J

Controlled Release 2000;63:235-59.

Asmussen; Bodo, Cremer; Karsten, Hoffmann; Hans-Rainer. Expandable

gastro-retentive therapeutic system with controlled active substance

release in the gastro-intestinal tract. U. S. Patent: 6,290,989 Aug

, 1999.

Indian Pharmacopoeia. Vol. 1. 1996. p. A-82.

Patel A, Ray S, Thakur RS. In-vitro evaluation and optimization of

controlled release floating drug delivery system of metformin

hydrochloride. DARU 2006;14:57-64.

Kawashima Y, Niwa T, Takeuchi H, Hino T, Itoh Y. Hollow microspheres

for use as a floating controlled drug delivery system in the stomach. J

Pharma Sci (USA) 1992;81:135-40.

Zhenqiu Yang, Baozhen Song, Qiaoxia Li, Honglei Fan, Fan Ouyang.

Preparation of Microspheres with microballoons inside for floating

drug delivery systems. J Appl Polymer Sci 2004;94:197-202.

Martin AN, Swarbrick J, Commarata A. Physical pharmacy. 3rd ed.

Philadelphia: Lea and Febiger; 1983. p. 423-5.

Kiyoyama S, Shiomori K, Kawano Y, Hatate Y. Preparation of

microcapsules and control of their morphology. J Microencapsul

;20:497-508.

Streubel A, Siepmann J, Bodmeier R. Floating microparticles based on

low density foam powder. Int J Pharma 2002;241:279-82.

El-Kamel AH, Sokar MS, Al Gamal SS, Naggar VF. Preparation and

evaluation of Ketoprofen floating oral delivery system. Int J Pharma

;220:13-21.

Soppimath KS, Kulkarni AR, Aminabhavi TM. Development of hollow

microspheres as floating controlled-release system for cardiovascular

drugs: Preparation and release characteristics. Drug Dev Industrial

Pharma 2001;27:407-515.

The United States Pharmacopoeia, 2000. United States Pharmacopeial

Convention Inc: 1941.

Diane JB, Anthony JH. Microsphere technology and application.

Encyclopedia of Pharmaceutical Technology by Mercel Dekker; 2002.

p. 1783-94.