Formulation and Evaluation of Solid Dispersion of an AntiEpileptic Drug Carbamazepine
Journal Title: IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS) - Year 2016, Vol 11, Issue 5
Abstract
Carbamazepine (CBZ), relatively water insoluble anti epileptic candidate was selected as a model drug for the study, which is BCS class II drug (low soluble and high permeable). Solid dispersions were formulated with an aim of improving aqueous solubility, oral bioavailability and the rate of dissolution of Carbamazepine using different hydrophyllic polymer like Polyethylene Glycol (PEG) 6000, Polyethylene Glycol (PEG) 4000, Polyethylene Glycol (PEG) 1500, kollidon 30, HPMC 6 cps, poloxamer 407 and povidone k 30. Binary and ternary solid dispersions were prepared by physical misxing as well as fusion method with different drug-to-polymer weight ratio. The effects of different polymers on the solubility and in-vitro dissolution behavior were investigated spectrophotometrically at 288 nm. These formulations were characterized in the solid state by Fourier Transform Infrared (FTIR) spectroscopy and Scanning Electron Microscopy (SEM). SEM study indicated CBZ was present as fine particles and entrapped in carrier matrix of PEG 6000 and poloxamer 407 solid dispersions. Fourier Transform Infrared (FTIR) spectroscopic studies showed the stability of CBZ and absence of well-defined drug-polymer interactions. It was found that only 27.06% was released within 60 minutes from active carbamazepine on the other hand the release of carbamazepine from the solid dispersion containing combined PEG 6000 and poloxamer 407 at the ratio of 1:1:1 showed the best result which was 100.12% within the same period of time. Even physical mixtures of CBZ prepared with both carriers also showed better dissolution profiles than those of pure CBZ. This can be attributed to increased wettability and dispersibility, as well as decreased crystallinity and increase in amorphous fraction of drug when they remain dispersed in polymer. In conclusions, solid dispersions could be a promising delivery of CBZ with improved oral bioavailability and immediate release profiles.
Authors and Affiliations
Sharmin Akhter, Md. Salahuddin, A. K. M. Saif Uddin2,, Marufa Marium5, Md. Bodrudoza Alam6, Saikat Barua, Prakrety Chakrabarty, Mohammad Fahim Kadir
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