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Formulation of unidirectional release buccal patches of carbamazepine and study of permeation through porcine buccal mucosa

机译:卡马西平单向释药口腔贴剂的制备及对猪口腔黏膜渗透的研究

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Objective:To achieve transbuccal release of carbamazepine by loading in unidirectional release mucoadhesive buccal patches. Methods:Buccal patches of carbamazepine with unidirectional drug release were prepared using hydroxypropyl methyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone and ethyl cellulose by solvent casting method. Water impermeable backing layer (Pidilite® Biaxially-oriented polypropylene film) of patches provided unidirectional drug release. They were evaluated for thickness, mass uniformity, surface pH and folding endurance. Six formulations FA2, FA8, FA10, FB1, FB14 and FB16 (folding endurance above 250) were evaluated further for swelling studies, ex vivo mucoadhesive strength, ex vivo mucoadhesion time, in vitro drug release, ex vivo permeation, accelerated stability studies and FTIR and XRD spectral studies. Results: The ex vivo mucoadhesion time of patches ranged between 109 min (FA10) to 126 min (FB14). The ex vivo mucoadhesive force was in the range of 0.278 to 0.479 kg/m/s. The in vitro drug release studies revealed that formulation FA8 released 84%and FB16 released 99.01%of drug in 140 min. Conclusions: The prepared unidirectional buccal patches of carbamazepine provided a maximum drug release within specified mucoadhesion period and it indicates a potential alternative drug delivery system for systemic delivery of carbamazepine.
机译:目的:通过负载单向释放粘膜粘附性颊黏膜片实现卡马西平经颊释药。 方法:采用羟丙基甲基纤维素,聚乙烯醇,聚乙烯吡咯烷酮和乙基纤维素,通过溶剂浇铸法制备卡马西平单向释放的颊贴剂。贴剂的不透水背衬层(Pidilite®双轴取向聚丙烯薄膜)可单向释放药物。对它们的厚度,质量均匀性,表面pH和耐折性进行了评估。进一步评估了六种配方FA2,FA8,FA10,FB1,FB14和FB16(耐折性超过250)以进行溶胀研究,离体粘膜粘附强度,离体粘膜粘附时间,离体药物释放,离体渗透,加速稳定性研究和FTIR和XRD光谱研究。 结果:贴剂的离体粘膜粘附时间介于109分钟(FA10)至126分钟(FB14)之间。离体粘膜粘附力在0.278至0.479kg / m / s的范围内。体外药物释放研究表明,制剂FA8在140分钟内释放了84%,FB16释放了99.01%。 结论:制备的卡马西平单向颊面贴片在指定的粘膜粘附期内可提供最大的药物释放,这表明系统性输送卡马西平的潜在替代药物输送系统。

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