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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Formulation of venlafaxine for once daily administration using polymeric material hybrids
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Formulation of venlafaxine for once daily administration using polymeric material hybrids

机译：使用聚合物混合材料配制文拉法辛，每天给药一次

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摘要

Objective: Controlled release venlafaxine for once daily administration.Methods: Drug resin complexation followed by polymer encapsulation. A 4(1).2(1) factorial design was used to study the effect of polymer type and core: coat ratio on the release profile and kinetics. Polymer combinations were tried for optimisation adapting the desIMNCility function. The optimised formula was tested in rabbits against commercial extended release capsules.Results: Poly-epsilon-caprolactone, poly(d, l-lactide-co-glycolide) ester and poly(d, l-lactide) ester polymers were more efficient in lowering the release rate and the initial burst release than Eudragit((R))RS100. Encapsulation at 1:1 ratio ensured complete coats and drug release sustainment. Formula prepared using 50:50 PLA/Eudragit at 1:1 ratio sustained the drug release up to 24h with low burst release. This formula had higher venlafaxine absorption in rabbits compared to the commercial capsules.Conclusions: The optimised formula is superior to the available once-daily trials regarding enhanced bioavailability, dosage form versatility and ease of scaling up.
机译：目的：文拉法辛控释药物，每日一次。方法：药物树脂复合，然后进行聚合物包封。 4（1）.2（1）析因设计用于研究聚合物类型和核芯：涂层比率对释放曲线和动力学的影响。尝试对聚合物组合进行优化以适应desIMNCility函数。结果表明：聚ε-己内酯，聚（d，l-丙交酯-共-乙交酯）酯和聚（d，l-丙交酯）酯聚合物在降低降脂效果方面更有效。释放速率和初始猝发释放均高于Eudragit（R）RS100。以1：1的比例封装可确保完整的涂层和持续的药物释放。使用50:50 PLA / Eudragit以1：1比例制备的配方可将药物释放持续长达24h，且释放量低。与市售胶囊相比，该配方在兔子中具有更高的文拉法辛吸收。结论：优化的配方在提高生物利用度，剂型通用性和易于规模化方面优于每日一次的每日试验。

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