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首页> 外文期刊>Journal of Drug Delivery and Therapeutics >Formulation and evaluation of sublingual tablet of Venlafaxine hydrochloride for the treatment of depression
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Formulation and evaluation of sublingual tablet of Venlafaxine hydrochloride for the treatment of depression

机译:盐酸文拉法辛舌下片治疗抑郁症的研制及评价

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The objective of preparing Venlafaxine hydrochloride as sublingual formulations as it is very patient friendly compared to the conventional tablets. Sublingual tablet formulation was proposed to be developed for Venlafaxine hydrochloride to enhance the bioavailability by avoiding first pass effect. Crospovidone and sodium starch glycolate used as superdisintegrants. Lactose was used as glidant and mannitol as directly compressible filler. Microcrystalline cellulose used as tablet disintegrant. Direct compression method found best and easy for preparing the sublingual tablets. Seven formulations (S1-S7) were prepared and evaluated for thickness which ranges from 1.91 to 2.21, hardness ranges from 2.6 to 3.4 kg/cmsup2/sup, friability 0.71% to 0.90%, weight variations, wetting time ranges from 32-69 seconds disintegration time ranges from 29 to 57 seconds and in vitro drug release ranges from 70.7 to 98%. Formulation F-7 containing crospovidone (15mg) emerged as best formulation based on drug release characteristics. From the present study, it can be concluded that the superdisintegrants increased the solubility and in vitro drug release of Venlafaxine hydrochloride. Sublingual formulation (tablets) increased the onset of action and bioavailability of Venlafaxine Hydrochloride and prevent them from extensive first-pass effect.
机译:制备盐酸文拉法辛舌下制剂的目的是因为与常规片剂相比,它对患者非常友好。有人建议开发盐酸文拉法辛的舌下片剂,以通过避免首过效应来提高生物利用度。交聚维酮和羟乙酸淀粉钠用作超级崩解剂。乳糖用作助流剂,甘露醇用作直接可压缩的填充剂。微晶纤维素用作片剂崩解剂。发现直接压缩法是制备舌下片剂的最佳方法。制备了七个配方(S1-S7),并评估了厚度在1.91至2.21之间,硬度在2.6至3.4 kg / cm 2 ,脆碎度0.71%至0.90%,重量变化,润湿时间方面崩解时间为32-69秒,崩解时间为29至57秒,体外药物释放范围为70.7至98%。基于药物释放特性,含有交聚维酮(15毫克)的配方F-7成为最佳配方。从本研究可以得出结论,超级崩解剂增加了盐酸文拉法辛的溶解度和体外药物释放。舌下制剂(片剂)增加了盐酸文拉法辛的作用和生物利用度,并阻止了它们的广泛首过效应。

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