Abstract

Formulation and in-vitro evaluation of mucoadhesive buccal patches containing zolmitriptan using gel forming polymers

The zolmitriptan is a serotonin (5-HT1) agonist used for the treatment of migraine with or without aura. The absolute oral bioavailability is about 40 to 50%. The half-life of zolmitriptan is 2.5 to 3 hrs and it undergoes hepatic metabolism. So, in order to improve the bioavailability and efficacy, we have prepared buccal patches of zolmitriptan. In the present research work, buccal patches were prepared using hydroxy propyl methyl cellulose (HPMC). HPMC is one the polymers which is having good mucoadhesive property so therefore various formulations were developed by using release rate controlling and gel forming polymers like HPMC (K4M), carbopol, poly vinyl pyrrolidone and Eudragit RL-100 by Solvent Casting technique. In addition to this propylene glycol and tween 80 was used as plasticizer and permeation enhancer respectively. Buccal patches were characterized for number of parameters like physical appearance and surface texture, weight uniformity, thickness, folding endurance, swelling index, surface pH, drug content uniformity, in-vitro residence time, bursting strength, drug-excipients interaction study, and in-vitro drug release study. All the prepared patches were smooth surface and elegant texture. From among all the developed formations, the formulation F8 containing HPMC K4M and carbopol 934 retarded the drug release in a controlled manner for prolonged period of more than 8 hrs, gave satisfactory in-vitro resident time maximum duration of 7.46 hrs, so it was selected as the best formulation. Swelling studies indicated significant water uptake and contributed in drug release. Stability studies were as per ICH guidelines, suggesting that there was no significant change in surface pH, drug content, bioadhesion property, swelling behavior of the patches. FTIR studies revealed that, there was no incompatibility of the drug with the excipients used.


Author(s): N. G. Raghavendra Rao, Sunil Firangi, Keyur Patel

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