Shujaat Ali Khan,
Mahmood Ahmad,
Ghulam Murtaza ,
Muhammad Naeem Aamir,
Nisar ur Rehman,
Rozina Kousar,
Fatima Rasool,
Mohammad Akhtar
Faculty of Pharmacy and Alternative Medicine, The Islamia University of Bahawalpur, Bahawalpur-63100, Pakistan;
For correspondence:- Ghulam Murtaza
Email: gmdogar356@gmail.com Tel:+9203142082826
Received: 11 September 2009
Accepted: 20 April 2010
Published: 24 June 2010
Citation:
Khan SA, Ahmad M, Murtaza G, Aamir MN, Rehman Nu, Kousar R, et al.
Formulation of Nimesulide Floating Microparticles Using Low-viscosity Hydroxypropyl Methylcellulose. Trop J Pharm Res 2010; 9(3):293-299
doi:
10.4314/tjpr.v9i3.11
© 2010 The authors.
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Abstract
Purpose: To formulate prolonged-release floating microparticles that would minimise the irritant effect of weakly acidic drugs, such as nimesulide, on the stomach by avoiding direct contact with gastric mucosa.
Methods: Sustained release floating microparticles of nimesulide was prepared by a coacervation (non-solvent addition technique. Three different ratios of the coacervating polymer, low-viscosity hydroxypropyl methylcellulose (HPMC), were used, and the dissolution characteristics of the floating microparticles in simulated gastric and intestinal media were evaluated. In order to determine whether there was drug – polymer interaction, the microparticles were also assessed by infra-red (FTIR) spectroscopy and x-ray diffraction (XRD). Micromeritic properties of the microparticles were also assessed.
Results: The drug content of the floating microparticles increased with increase in the level of HPMC incorporated. All floating microparticles formulations showed good flow properties while particle size analysis revealed that the appearance and size distribution of the formulations varied with polymer concentration. FTIR and XRD data indicated the crystalline nature of the drug but there was no chemical interaction between the drug and the polymer in the microparticles. Nimesulide release was faster in simulated intestinal fluid (pH 6.8) than in simulated gastric fluid (pH 1.2) and distilled water (pH 6.5).
Conclusion: Coacervation non-solvent addition is a suitable technique for preparing floating microparticles of nimesulide using low-viscosity HPMC.
Keywords: Floating microparticles, Nimesulide, HPMC, Coacervation, Non-solvent addition, Sustained release