托吡酯负载小体治疗癫痫的处方、开发和评价

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摘要

托吡酯(TPM)是一种用于治疗癫痫和癫痫发作的抗癫痫药物。这项研究有三个目的。一是提高BCS III类药物TPM的溶解度和生物利用度;第二,减轻癫痫患者在发作期间对制剂的管理,第三,减少持久治疗所需的药物剂量。采用响应面设计法,通过改变Tween、Labrafil和胆固醇的浓度,对TPM小体的配方进行优化。进一步采用醚注射法制备了TPM膜体。然后对该制剂进行囊泡大小、包封效率和体外释药研究。对纯药和优化批进行FTIR和DSC研究。结果表明,优化后的微泡大小为0。35 nm。优化批的包封率和释药率分别为94.64%和92.027%。从目前的研究可以看出,TPM小体的发育在治疗癫痫方面具有很大的潜力。
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Formulation, Development and Evaluation of Topiramate Loaded Niosomes for the Treatment of Epilepsy
Topiramate (TPM) is an anti-epileptic drug used in the treatment of epilepsy and seizures. The study was designed with three aims. First, to enhance the solubility and bioavailability of BCS class III drug TPM; second, to ease administration of the formulation to the epileptic patient, during an attack, and third, to decrease the dose of drug for enduring treatment. Formulation of TPM niosomes was optimized by changing the concentration of Tween, Labrafil and cholesterol using response surface design. Further the TPM niosomes were prepared by using ether injection method. The formulation was then evaluated for vesicle size, entrapment efficiency and in-vitro drug release study. FTIR and DSC studies were performed for pure drug and optimized batch. The vesicle size of the optimized batch was found to be 0. 35 nm. The %entrapment efficiency and %drug release of optimized batch was found to be 94.64% and 92.027% respectively. From the present study it can be concluded that the developed niosomes of TPM has shown great potential in treatment of epilepsy.
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