Solidified Reverse Micellar Solution (SRMS)-Based Indomethacin Sustained-Release Tablets: Formulation and In vitro Evaluation

Purpose: To formulate and evaluate sustained-release indomethacin tablets based on solidified reverse micellar solution (SRMS). Methods: SRMS consisting of mixtures of phospholipid (Phospholipon ® 90H) and triglyceride (Softisan ® 154) were prepared in the ratios of 1:1, 2:1 and 1:2, respectively. SRMS-based tablets containing 75 mg of indomethacin each were prepared using a validated plastic mould. The physicochemical properties of the tablet formulations were studied. In vitro release study was carried out in simulated intestinal fluid (SIF, pH 7.5). Results: The results showed that the physicochemical properties of the tablet formulations were significantly affected by the composition/ratio of the lipid matrix used (p < 0.05). Tablet hardness ranged from 5.00 ± 0.39 to 5.60 ± 0.36 kgf for tablets formulated with SRMS 1:2 and 2:1 (N3 and N2), respectively. The tablets exhibited friability of < 1 % (p < 0.05). Erosion time in SIF ranged from 124.0 ± 0.5 to 180.0 ± 1.1 min while drug release from the tablets reached a maximum in 8 – 11 h for all the batches. Conclusion: Indomethacin tablets based on SRMS exhibited good sustained-release properties and can be further developed to achieve once daily administration for improved patient adherence to therapy.

[1]  A. Attama,et al.  Preparation of novel solid lipid microparticles loaded with gentamicin and its evaluation in vitro and in vivo , 2012, Journal of microencapsulation.

[2]  J. Singh,et al.  Prediction of in vitro Drug Release Mechanisms from Extended Release Matrix Tablets using SSR/R2 Technique , 2011 .

[3]  D. Singh,et al.  Influence of Selected Formulation Variables on the Preparation of Peptide Loaded Lipospheres , 2011 .

[4]  V. Dixit,et al.  Formulation Optimization of Metronidazole Loaded Chitosan Microspheres for Wound Management by 3-Factor, 3-Level Box-Behnken Design , 2010 .

[5]  V. Dixit,et al.  Optimization and Characterization of Gentamicin Loaded Chitosan Microspheres for Effective Wound Healing , 2010 .

[6]  A. Attama,et al.  Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium , 2009, Drug delivery.

[7]  P. Owlia,et al.  Evaluation of Ceftriaxone Releasing from Microspheres Based on Starch Against Salmonella spp. , 2007 .

[8]  F. Cui,et al.  A novel formulation design about water-insoluble oily drug: preparation of zedoary turmeric oil microspheres with self-emulsifying ability and evaluation in rabbits. , 2005, International journal of pharmaceutics.

[9]  Ping Gao,et al.  Enhanced Oral Bioavailability of a Poorly Water Soluble Drug PNU‐91325 by Supersaturatable Formulations , 2004, Drug development and industrial pharmacy.

[10]  C. Müller-Goymann,et al.  Characterization of solidified reverse micellar solutions (SRMS) and production development of SRMS-based nanosuspensions. , 2003, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[11]  C. Xie,et al.  The production and characteristics of solid lipid nanoparticles (SLNs). , 2003, Biomaterials.

[12]  N. Sarkar Mifepristone: bioavailability, pharmacokinetics and use-effectiveness. , 2002, European journal of obstetrics, gynecology, and reproductive biology.

[13]  A. Göpferich,et al.  Development and characterization of lipid microparticles as a drug carrier for somatostatin. , 2001, International journal of pharmaceutics.

[14]  Ravi Kumar M.N.V. Nano and microparticles as controlled drug delivery devices. , 2000 .

[15]  C. Müller-Goymann,et al.  Controlled release of solid-reversed-micellar-solution (SRMS) suppositories containing metoclopramide-HCl. , 2000, International journal of pharmaceutics.

[16]  F. Oehme Goodman and Gilman 's: The pharmacological basis of therapeutics , 1996 .