盐酸甲氧氯普胺口腔片用于儿童术后护理:体外和体内评价

Amal M. Abd El Razek, Azza A. Hasan, Shereen A Sabry, M. Mahdy, Eslam E. Hamed
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引用次数: 0

摘要

本研究将盐酸甲氧氯普胺(metoclopramide HCl, MET HCl)负载口服硅片(OWs)作为快速溶解剂型,无需饮用水即可迅速改善呕吐。以羟丙基甲基纤维素(HPMC)为成膜剂,丙二醇(PG)、聚乙二醇(PEG) 400和聚乙二醇600为增塑剂,采用浇铸法制备了OWs。对制备的制剂进行目测、厚度、重量变化、药物含量、折叠耐力、表面pH、抗拉强度、黏附性、吸湿率、失湿率、体外释放等评价参数研究。选择G3批进行进一步的研究,如DSC、FTIR和体内评价。通过测定各组家兔血浆中MET - HCl浓度,评价MET - HCl负载OWs的生物利用度。所有硅片透明、光滑、均匀、柔韧。G3批次(300 mg HPMC, 20% PEG 400)的抗拉强度、伸长率、黏附性和释药速度最高。代药动力学数据显示,MET HCl负载OWs制剂(G3批)的Cmax、AUC0-24和Tmax均显著高于口服普通MET HCl溶液(p<0.001)。由此可见,载MET HCl的OWs是一种很有前景的快速释放制剂,其药物吸收速度和程度都有所提高,因此对儿科特别是术后呕吐和恶心有较高的治疗效果。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Metoclopramide Hydrochloride Loaded Oral Wafers for Postoperative Care of Children: In Vitro and In Vivo Evaluation
The present study focused on the formulation of metoclopramide HCl (MET HCl) loaded oral wafers (OWs) as a fast dissolving dosage form without drinking water to produce a prompt improvement of emesis. OWs were prepared by casting technique using Hydroxypropyl Methylcellulose (HPMC) as a film forming agent and plasticizers like propylene glycol (PG), polyethylene glycol (PEG) 400 and polyethylene glycol 600. The prepared formulations were visually inspected and subjected to evaluation parameters such as thickness, weight variation, drug content, folding endurance, surface pH, tensile strength, mucoadhesiveness, percentage of moisture absorption, percentage of moisture loss and in vitro release study. G3 batch was selected for further investigations e.g. DSC, FTIR and in vivo evaluation. The bioavailability of MET HCl loaded OWs was assessed by measuring the plasma concentrations of MET HCl in different studied rabbit's groups' .All wafers were transparent, smooth, uniform and flexible. G3 batch (300 mg HPMC, 20% PEG 400) showed the highest tensile strength, percent elongation, mucoadhesiveness and faster drug release. The pharmacokinetic data of MET HCl loaded OWs preparation (G3 batch) showed a significant higher Cmax, AUC0-24 and lower Tmax (p<0.001) than oral plain MET HCl solution. It could be concluded that MET HCl loaded OWs is a promising fast-release preparation with enhanced rate and extent of drug absorption hence, higher therapeutic efficiency against vomiting and nausea in pediatrics, especially postoperatively can be expected.
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