Development, Characterization & Statistical Optimization of Matrix Type Transdermal Patches of Almotriptan Malate for The Treatment of Migraine

Akila Rm, Naseem Ak
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Abstract

The present work is focused on the development, evaluation and statistical optimization of almotriptan malate transdermal patches. Almotriptan malate is used as anti-migraine drug and reported to have the best-sustained pain free rate and the lowest adverse events rate of all the triptans and thus making interest in the development of new route for the therapeutic administration of the drug, So, the present research work was aimed to develop matrix type transdermal patches using polymers HPMC K15M, ERS100 and EC and plasticizers DBP and PEG400 by solvent casting method. This formulation would help to avoid non-compliance of the tablet dosage form The IR spectra of the drug and physical mixtures of drug-polymer confirmed the absence of incompatibility between drug and polymers. The in-vitro drug release studies revealed that patches made of HPMC K15M-ERS 100 with DBP as plasticizer was considered as the best formulation and incorporated in 2 factorial design and evaluated for further studies. The concentration of HPMC K 15M and ERS 100 are chosen as the independent variables. Drug content, %moisture absorption %, moisture loss, and cumulative % drug released at 12h are chosen as dependent variables. The drug release from transdermal patches followed zero order kinetics. Various physicochemical parameters of the patches were investigated. The current research work of transdermal patches of almotriptan malate may provide sustained delivery for prolonged periods in the management of migraine, which can be a good way to bypass the extensive hepatic first-pass metabolism.
基质型苹果酸阿莫曲坦透皮贴剂治疗偏头痛的研制、表征及统计优化
本文主要对苹果酸阿莫曲坦透皮贴剂的研制、评价和统计优化进行了综述。苹果酸阿莫曲坦作为抗偏头痛药物,在所有曲坦类药物中具有最佳的持续无痛率和最低的不良事件发生率,因此对开发新的给药途径产生了兴趣,因此,本研究旨在采用溶剂铸造法,以聚合物HPMC K15M、ERS100和EC以及增塑剂DBP和PEG400为材料,开发基质型透皮贴剂。该制剂有助于避免片剂剂型的不符合。药物和药物-聚合物物理混合物的红外光谱证实了药物与聚合物之间不存在不相容性。体外释药研究结果表明,以DBP为增塑剂的HPMC K15M-ERS 100为贴片的最佳配方,并采用2因子设计进行评价,以供进一步研究。选取HPMC k15m和er100浓度作为自变量。因变量为药物含量、吸湿率%、失湿率、12h药物累计释放率%。透皮贴剂的药物释放遵循零级动力学。研究了贴片的各种理化参数。目前研究的苹果酸阿莫曲坦透皮贴剂可能为偏头痛的治疗提供长时间的持续给药,这可能是一种绕过肝脏广泛的首过代谢的好方法。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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