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Design, Development and Evaluation of Selegiline Hydrochloride Transdermal Patch

机译:盐酸司来吉兰透皮贴剂的设计,开发与评价

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Many monoamine oxidase inhibitors (MAOIs) have been used to treat major depressive disorder (MDD). However, the prescription of MAOIs has decreased considerably as a result of side effects such as tyramine-induced hypertensive crisis, known as “Cheese Effect”. The drug delivery system itself can affect the effi cacy and bioavailability of certain drugs when medications are given by oral, intravesical and intravaginal routes. Therefore there is a need for advanced drug delivery techniques that can avoid toxic effects and improve the bioavailability at the same time. In this context, the transdermal patches of selegiline hydrochloride (SH) were prepared by the solvent casting method using hydroxy propyl methyl cellulose (HPMC), polyvinyl alcohol (PVA) and methyl cellulose (MC) as reservoir polymers in different ratios (1:1, 1:2 and 1:3). Rate controlling membrane was caste by using 2% ethyl cellulose (EC) membrane. The prepared patches possessed satisfactory physicochemical characteristics. The formulation exhibited fl exibility, uniform weight, thickness, smoothness, drug content (93 to 97 %), little moisture loss and moisture absorption. The in-vitro permeation studies in phosphate buffer (pH 7.4) revealed formulations released drug in the range of 86.77 to 96.79% and followed diffusion mechanism. Formulations with 1:1 and 1:2 ratio released drug up to 10 to 20 h only. The optimized formulation F6 containing PVA (1:3) showed good release rate of 90.08% for 24 h. The patches were seemingly free of potential hazardous skin irritation. FT-IR and DSC studies revealed no interaction between the drug and polymers used.
机译:许多单胺氧化酶抑制剂(MAOIs)已用于治疗重度抑郁症(MDD)。然而,由于诸如酪胺引起的高血压危机之类的副作用,即所谓的“乳酪效应”,MAOI的处方已大大减少。当通过口服,膀胱内和阴道内途径给药时,药物输送系统本身会影响某些药物的功效和生物利用度。因此,需要能够避免毒性作用并同时提高生物利用度的先进的药物递送技术。在这种情况下,盐酸司来吉兰(SH)的透皮贴剂是通过溶剂浇铸法制备的,使用羟丙基甲基纤维素(HPMC),聚乙烯醇(PVA)和甲基纤维素(MC)作为储藏聚合物以不同的比例(1:1) ,1:2和1:3)。通过使用2%乙基纤维素(EC)膜来铸造速率控制膜。制备的贴剂具有令人满意的理化特性。该制剂表现出柔韧性,均匀的重量,厚度,光滑度,药物含量(93%至97%),极少的水分损失和水分吸收。在磷酸盐缓冲液(pH 7.4)中的体外渗透研究表明,制剂释放的药物范围为86.77%至96.79%,并遵循扩散机制。比例为1:1和1:2的制剂最多只能释放10至20小时。含有PVA(1:3)的优化配方F6在24小时内显示90.08%的良好释放率。贴剂似乎没有潜在的有害皮肤刺激性。 FT-IR和DSC研究表明,药物与所用聚合物之间没有相互作用。

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