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用于化疗呕吐管理的盐酸昂丹司琼黏膜黏附微球的制备及体外评价

Fabrication and in vitro evaluation of mucoadhesive ondansetron hydrochloride beads for the management of emesis in chemotherapy.

作者信息

Malik Raj Kaur, Malik Prashant, Gulati Neha, Nagaich Upendra

机构信息

Department of Pharmaceutics, School of Pharmacy, Bharat Institute of Technology, Meerut, Uttar Pradesh, India.

出版信息

Int J Pharm Investig. 2013 Jan;3(1):42-6. doi: 10.4103/2230-973X.108962.

Abstract

BACKGROUND

Mucoadhesive beads were fabricated and evaluated for controlled release of an antiemetic drug 'Ondansetron Hydrochloride'. Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist mainly used for the treatment of emesis, which occurs as a side effect of chemotherapy.

MATERIALS AND METHODS

The present work was to fabricate and evaluate ondansetron-loaded microbeads by using chitosan as mucoadhesive and sustained release polymer. Sodium tripolyphosphate (Na-TPP) was used as a cross-linking agent. The microbeads were successfully prepared by ionotropic gelation technique. The particle size, entrapment efficiency, and mucoadhesive strength of drug-loaded formulations was measured by an optical microscope, direct crushing method, and in vitro wash-off method, respectively.

RESULTS

Particle size, entrapment efficiency, mucoadhesive strength, and in vitro drug release of optimized formulation was found to be 760.11 ± 1.02 μm, 75.09 ± 2.40%, 95.14 ± 0.27% and 87.45 ± 1.21%, respectively. The data was fitted to different kinetic models to illustrate its anomalous (non-Fickian) diffusion.

CONCLUSIONS

The results revealed that ondansetron HCl loaded microbeads are most suitable mode of drug delivery for promising therapeutic action. Ondansetron HCl-loaded microbeads can prove to be potential pharmaceutical dosage forms for sustaining the drug release and reducing the dose frequency.

摘要

背景

制备了用于控制释放抗呕吐药物“盐酸昂丹司琼”的粘膜粘附微球并进行了评估。盐酸昂丹司琼是一种5-羟色胺5-HT3受体拮抗剂,主要用于治疗作为化疗副作用出现的呕吐。

材料与方法

本研究工作是使用壳聚糖作为粘膜粘附和缓释聚合物来制备和评估载有昂丹司琼的微球。三聚磷酸钠(Na-TPP)用作交联剂。通过离子凝胶化技术成功制备了微球。分别通过光学显微镜、直接压碎法和体外冲洗法测量了载药制剂的粒径、包封率和粘膜粘附强度。

结果

优化制剂的粒径、包封率、粘膜粘附强度和体外药物释放分别为760.11±1.02μm、75.09±2.40%、95.14±0.27%和87.45±1.21%。将数据拟合到不同动力学模型以说明其非菲克扩散。

结论

结果表明,载有盐酸昂丹司琼的微球是具有良好治疗作用的最适合药物递送方式。载有盐酸昂丹司琼的微球可被证明是维持药物释放和减少给药频率的潜在药物剂型。

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