文献检索文档翻译深度研究
Suppr Zotero 插件Zotero 插件
邀请有礼套餐&价格历史记录

新学期,新优惠

限时优惠:9月1日-9月22日

30天高级会员仅需29元

1天体验卡首发特惠仅需5.99元

了解详情
不再提醒
插件&应用
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
高级版
套餐订阅购买积分包
AI 工具
文献检索文档翻译深度研究
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2025

盐酸肉桂嗪胃滞留片的体外释放动力学和生物利用度。

In vitro release kinetics and bioavailability of gastroretentive cinnarizine hydrochloride tablet.

机构信息

Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi 221005, Uttar Pradesh, India.

出版信息

AAPS PharmSciTech. 2010 Mar;11(1):294-303. doi: 10.1208/s12249-010-9380-5. Epub 2010 Feb 25.


DOI:10.1208/s12249-010-9380-5
PMID:20182827
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2850455/
Abstract

An oral sustained release dosage form of cinnarizine HCl (CNZ) based on gastric floating matrix tablets was studied. The release of CNZ from different floating matrix formulations containing four viscosity grades of hydroxypropyl methylcellulose, sodium alginate or polyethylene oxide, and gas-forming agent (sodium bicarbonate or calcium carbonate) was studied in simulated gastric fluid (pH 1.2). CNZ release data from the matrix tablets were analyzed kinetically using Higuchi, Peppas, Weibull, and Vergnaud models. From water uptake, matrix erosion studies, and drug release data, the overall release mechanism can be explained as a result of rapid hydration of polymer on the surface of the floating tablet and formation of a gel layer surrounding the matrix that controls water penetration into its center. On the basis of in vitro release data, batch HP1 (CNZ, HPMC-K100LV, SBC, LTS, and MgS) was subjected to bioavailability studies in rabbits and was compared with CNZ suspension. It was concluded that the greater bioavailability of HP1 was due to its longer retention in the gastric environment of the test animal. Batch no. HP1 of floating tablet in rabbits demonstrated that the floating tablet CNZ could be a 24-h sustained release formulation.

摘要

研究了一种基于胃漂浮基质片的盐酸桂利嗪(CNZ)口服缓释剂型。在模拟胃液(pH 1.2)中,研究了含有四种粘度级别的羟丙基甲基纤维素、海藻酸钠或聚乙烯氧化物以及产气剂(碳酸氢钠或碳酸钙)的不同漂浮基质配方中 CNZ 的释放情况。使用 Higuchi、Peppas、Weibull 和 Vergnaud 模型对基质片中的 CNZ 释放数据进行了动力学分析。从水合作用、基质侵蚀研究和药物释放数据来看,整体释放机制可以解释为漂浮片表面聚合物的快速水合作用以及在基质周围形成控制水渗透到其中心的凝胶层的结果。基于体外释放数据,对批 HP1(CNZ、HPMC-K100LV、SBC、LTS 和 MgS)进行了兔体内生物利用度研究,并与 CNZ 混悬剂进行了比较。结果表明,HP1 的生物利用度更高是由于其在试验动物的胃环境中滞留时间更长。兔用漂浮片批 HP1 表明,漂浮片 CNZ 可以是一种 24 小时持续释放制剂。

相似文献

[1]
In vitro release kinetics and bioavailability of gastroretentive cinnarizine hydrochloride tablet.

AAPS PharmSciTech. 2010-2-25

[2]
Enhanced bioavailability of atorvastatin calcium from stabilized gastric resident formulation.

AAPS PharmSciTech. 2011-8-31

[3]
Gastroretentive Matrix Tablets of Boswellia Oleogum Resin: Preparation, Optimization, In Vitro Evaluation, and Cytoprotective Effect on Indomethacin-Induced Gastric Ulcer in Rabbits.

AAPS PharmSciTech. 2016-4

[4]
Preparation and evaluation of gastroretentive floating tablets of Silymarin.

Chem Pharm Bull (Tokyo). 2009-6

[5]
Formulation and in vitro, in vivo evaluation of effervescent floating sustained-release imatinib mesylate tablet.

PLoS One. 2015-6-2

[6]
Formulation and evaluation of swellable and floating gastroretentive ciprofloxacin hydrochloride tablets.

AAPS PharmSciTech. 2009

[7]
Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers.

Int J Pharm. 2006-3-9

[8]
Effect of formulation parameters on the drug release and floating properties of gastric floating two-layer tablets with acetylsalicylic acid.

Acta Pharm. 2011-9-1

[9]
Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: development, optimization and in vitro-in vivo evaluation in healthy human volunteers.

Eur J Pharm Biopharm. 2009-11-22

[10]
Preparation and characterization of a gastric floating dosage form of capecitabine.

Biomed Res Int. 2013-10-29

引用本文的文献

[1]
A novel Posaconazole oral formulation using spray dried solid dispersion technology: in-vitro and in-vivo study.

Drug Deliv Transl Res. 2024-5

[2]
SeDeM expert system with I-optimal mixture design for oral multiparticulate drug delivery: An encapsulated floating minitablets of loxoprofen Na and its physiologically based pharmacokinetic modeling.

Front Pharmacol. 2023-3-3

[3]
Novel Mucoadhesive Chitosomes as a Platform for Enhanced Oral Bioavailability of Cinnarizine.

Int J Nanomedicine. 2022

[4]
Stabilization benefits of single and multi-layer self-nanoemulsifying pellets: A poorly-water soluble model drug with hydrolytic susceptibility.

PLoS One. 2018-7-19

[5]
Increasing procaspase 8 expression using repurposed drugs to induce HIV infected cell death in ex vivo patient cells.

PLoS One. 2017-6-19

[6]
Recent advances in delivery systems and therapeutics of cinnarizine: a poorly water soluble drug with absorption window in stomach.

J Drug Deliv. 2014

[7]
Development and characterization of gastroretentive sustained-release formulation by combination of swelling and mucoadhesive approach: a mechanistic study.

Drug Des Devel Ther. 2013-12-5

[8]
Preparation and characterization of a gastric floating dosage form of capecitabine.

Biomed Res Int. 2013-10-29

[9]
Natural gums as sustained release carriers: development of gastroretentive drug delivery system of ziprasidone HCl.

Daru. 2012-10-17

[10]
Development of controlled-release matrix tablet of risperidone: influence of Methocel®- and Ethocel®-based novel polymeric blend on in vitro drug release and bioavailability.

AAPS PharmSciTech. 2011-4-15

本文引用的文献

[1]
Matrices containing NaCMC and HPMC 1. Dissolution performance characterization.

Int J Pharm. 2007-3-21

[2]
Bioavailability of riboflavin from a gastric retention formulation.

Int J Pharm. 2007-2-7

[3]
Floating hot-melt extruded tablets for gastroretentive controlled drug release system.

J Control Release. 2006-10-10

[4]
Effect of added Pharmatose DCL11 on the sustained-release of metronidazole from Methocel K4M and Carbopol 971P NF floating matrices.

Drug Dev Ind Pharm. 2006-9

[5]
Floating matrix dosage form for phenoporlamine hydrochloride based on gas forming agent: in vitro and in vivo evaluation in healthy volunteers.

Int J Pharm. 2006-3-9

[6]
Assessment of a controlled release hydrophilic matrix formulation for metoclopramide HCl.

Eur J Pharm Biopharm. 2003-5

[7]
Comparative evaluation of rate of hydration and matrix erosion of HEC and HPC and study of drug release from their matrices.

Eur J Pharm Sci. 2002-8

[8]
Preparation of alginate beads for floating drug delivery system: effects of CO(2) gas-forming agents.

Int J Pharm. 2002-6-4

[9]
LC and TLC determination of cinnarizine in pharmaceutical preparations and serum.

J Pharm Biomed Anal. 2002-5-15

[10]
Microspheres as floating drug-delivery systems to increase gastric retention of drugs.

Drug Metab Rev. 2001-5

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

推荐工具

医学文档翻译智能文献检索