四种茶碱缓释制剂释放度比较

茶碱是一种临床上使用多年的有效平喘药,国内外已有多种茶碱缓释制剂上市。由于茶碱治疗窗较窄,严格控制缓释制剂释放度显得十分重要。国内外茶碱缓释制剂产品多达数十种,其质量标准各异,如何估价这些产品的优劣自然也成为临床医药工作者关心的问题。为此,国际药学会OLMCS(Officil Laboratory and Medicines Control Services Sections)于1996年组织了茶碱缓释制剂质量国际协作研究,我国由中国药品生物制品检定所选送时尔平等茶碱缓释制剂产品参加此项协作研究。协作研究的主要内容是:制订统一的的测定方法,对选送的各产品含量、含量均匀度和释放度进行测定,然后对测定结果进行综合评价。其中释放度是评价的重点。 本实验对国内临床上使用的四种茶碱缓释制剂进行了释放度测定,并对它们的释药特性作出估价,供临床上使用茶碱缓释制剂产品参考。 1 实验材料和方法 1.1 样品:时尔平(茶碱控释胶囊,0.1g/粒,批号960631,杭州民生药厂);舒弗美(茶碱缓释片,0.1g/片,批号960501,广州兴华制药厂);埃斯玛隆(茶碱控释小     

口服缓释、控释制剂体外释放度的研究进展

口服缓释、控释制剂能降低血浆药物浓度波动,减少给药次数,提高药物疗效,降低不良反应,而且能改善病人的顺应性,使用方便,因而越来越引起人们的关注。体外释放度实验是筛选缓释、控释制剂处方和控制其质量的重要手段。由于口服缓释、控释制剂的长效作用是通过延缓吸收而达到,所     

双氯芬酸钠缓释制剂的释放度比较

目的：考察不同药厂双氯芬酸钠制剂的释放度，评价其内在质量。方法：按《中国药典》2000版释放度测定法，以磷酸缓冲液为释放介质，采用转篮法，用反相高效液相色谱法测定释放涟含量，进而计算其累积释放百分率并提取释放参数。结果：普通肠溶片释放最快，24．5min即释放85％以上，双释放控释片及双释放胶囊12h累积释放百分率均为80％以上。结论：三个厂家的双氯芬酸钠制剂均符合《中国药典》2000版规定。     

缓释控释制剂的释放度测定方法的研究进展

目的 介绍缓、控释制剂的体外释放度测定方法，使其能更好地模拟体内状态。方法 综述最近的中外文献中有关缓释、控释制剂的体外释放度测定实验方法，实验条件的选择及影响因素。结果 体外释放度实验条件如释放介质的pH值、高于强度、增溶剂、表面活性剂和释放仪器等可影响缓、控释制剂的体外释放度。结论 根据不同药物选择尽可能接近体内状态的方法。     

两种双氯芬酸钠缓释制剂体外释放度考察

双氯芬酸钠 (Diclofenac Sodium,DS)为第三代灭酸类强效、非甾体抗炎药 (NSAIDS) ,临床广泛用于消炎、镇痛、解热及治疗风湿性或类风湿性关节炎 [1 ] ,其优点是临床剂量小 ,用药后个体差异较少。但由于其生物半衰期短 [2 ] ,欲维持其有效血药浓度 ,需频繁给药 ,因而不少厂家将该药制成缓释剂型。本文对市售国产双氯芬酸钠缓释制剂与进口的双氯芬酸钠缓释制剂释放度进行了测定和比较。1　仪器与试药1.1　仪器岛津 UV16 0 1PC紫外分光光度计 ;ZRS- 8智能溶出仪 (天津大学无线电厂 )。1.2　药品与试剂双氯芬酸钠缓释片 (加拿大 ) ;自制…     

2种双氯芬酸钠缓释制剂的体外释放度比较

双氯芬酸钠为邻氨基苯甲酸非甾体类抗炎药物，是一种强效消炎镇痛药。其镇痛消炎及解热作用比吲哚美辛强2．0～2．5倍，该药剂量低，副作用小，疗效显著，目前广泛用于临床。现国内已有多家药厂研究生产，但不同厂家因处方，工艺和剂型的不同，使得释放度存在不同差异。因此，我们考察了2种缓释制剂的溶出度，并对其进行比较，以评价其内在质量。     

缓释控释制剂的释放度测定方法的研究进展

目的　介绍缓、控释制剂的体外释放度测定方法 ,使其能更好地模拟体内状态。方法　综述最近的中外文献中有关缓释、控释制剂的体外释放度测定实验方法 ,实验条件的选择及影响因素。结果　体外释放度实验条件如释放介质的 pH值、离子强度、增溶剂、表面活性剂和释放仪器等可影响缓、控释制剂的体外释放度。结论　根据不同药物选择尽可能接近体内状态的方法     

缓释控释制剂的释放度测定方法的研究进展

目的介绍缓、控释制剂的体外释放度测定方法,使其能更好地模拟体内状态.方法综述最近的中外文献中有关缓释、控释制剂的体外释放度测定实验方法,实验条件的选择及影响因素.结果体外释放度实验条件如释放介质的pH值、离子强度、增溶剂、表面活性剂和释放仪器等可影响缓、控释制剂的体外释放度.结论根据不同药物选择尽可能接近体内状态的方法.     

Dissolution Testing as a Prognostic Tool for Oral Drug Absorption: Immediate Release Dosage Forms

Dissolution tests are used for many purposes in the pharmaceutical industry: in the development of new products, for quality control and, to assist with the determination of bioequivalence. Recent regulatory developments such as the Biopharmaceutics Classification Scheme have highlighted the importance of dissolution in the regulation of post-approval changes and introduced the possibility of substituting dissolution tests for clinical studies in some cases. Therefore, there is a need to develop dissolution tests that better predict the in vivo performance of drug products. This could be achieved if the conditions in the gastrointestinal tract were successfully reconstructed in vitro. The aims of this article are, first, to clarify under which circumstances dissolution testing can be prognostic for in vivo performance, and second, to present physiological data relevant to the design of dissolution tests, particularly with respect to the composition, volume, flow rates and mixing patterns of the fluids in the gastrointestinal tract. Finally, brief comments are made in regard to the composition of in vitro dissolution media as well as the hydrodynamics and duration of the test.     

Evaluation of Different Metrics as Indirect Measures of Rate of Drug Absorption from Extended Release Dosage Forms at Steady-State

Bioequivalence assessment of extended release (ER) dosage forms is usually carried out at steady-state, using area under the curve (AUC) to evaluate extent of absorption and maximum concentration (C_max) and % peak trough fluctuation ratio (%PTF) to evaluate rate of absorption. Other metrics such as C_max/AUC and partial AUCs have recently been proposed as alternatives for assessing the absorption rate of drugs from immediate release (IR) dosage forms under single dose conditions. The performances of these metrics were assessed using the results of two sets of simulated experiments of ER dosage forms at steady-state and 2 actual pharmacokinetic studies involving ER dosage forms of a Glaxo drug. In the first set of simulations there was no difference in bioavailability between the two formulations; in the second set of simulations the test formulation had a 50% greater absorption rate-constant (ka) than the reference formulation. The following conclusions were reached: 1. For ER dosage forms at steady-state, all the metrics, with the exception of %PTF, resulted in much smaller increases than the underlying 50% increase in ka. Although, %PTF gave the largest effect it was also the most imprecisely estimated. 2. In our studies, none of the metrics tested provided reliable information about changes in the underlying rate of absorption from ER dosage forms under steady-state conditions. 3. The current practice of comparing rate of absorption from ER dosage forms using steady-state C_max is inappropriate due to lack of sensitivity. The use of %PTF may require a widening in the currently accepted 80-125% permissible range set for C_max and AUC.     

Effect of Destruction Force on Drug Release from Multiple Unit Controlled Release Dosage Forms in Humans

Purpose. This study examined the effects of mechanical destructive forces on drug release from controlled release (CR) multiple unit dosage forms in vitro and in vivo and their colonic release, using two CR granules of acetaminophen, AG and BG, which differed in hardness (AG was hard and BG was soft), but which did not depend on agitation speed or pH for their release. Methods. In vitro release rates were determined using several official methods and the rotating dialysis cell method. Granules were administered to healthy volunteers under fasting and fed conditions. Results. Both granules showed similar release rates under mild destructive conditions in official dissolution tests, but BG showed a faster release rate in the rotating dialysis cell method. In the fasting state, the drug absorption-time profiles of AG and BG were almost equal. In the fed state, the drug release rate of BG increases whereas that of AG is almost equal to the fasted state. The food effect on BG could be caused by an increase in the mechanical stress of the GI tract due to food intake judging from the findings in vitro and in dogs. The colonic release from multiple unit CR products was larger than that from single unit ones. Conclusions. In vivo release of drug from a multiple unit CR product that is structurally weak is affected by mechanical stresses, which differ among human subjects but are increased by food ingestion. Colonic release from multiple unit CR products is larger than that from single unit products.     

对乙酰氨基酚缓释片的生产工艺研究

目的：研究制备对乙酰氨基酚缓释片最佳工艺。方法：通过测定颗粒的可压性和片剂释放度来评价并确定制备工艺。结果与结论：实验表明,分层制粒为较理想的制备工艺。采用该工艺所制样品的体外释放度和体内生物利用度与美国麦克尼尔公司进口的对乙酰氨基酚控释片基本一致,达到国外同品种的技术要求。     

In Vitro-In Vivo Relationship of Oral Extended-Release Dosage Forms

Purpose. A method to establish the in vitro-in vivo relationship of oral extended-release products is proposed. Methods. The approach utilizes incremental amounts of drug released and absorbed within defined time intervals, to construct a ² distributed variable for testing in vitro-in vivo similarity. Results. A case study is used to demonstrate that the similarities between incremental values of in vivo absorbed and in vitro dissolved fractions are distinguishable for different dissolution profiles despite naturally significant linear correlations between cumulative in vivo absorbed and in vitro dissolved fractions (with different dissolution tests) of an oral extended-release product. Conclusions. The method enables investigators to compare different in vitro dissolution profiles of an oral extended-release product to find an optimized dissolution profile to be the surrogate of the in vivo release process of the product.     

口服固体速释制剂及其制备技术

介绍了固体分散滴丸,膜剂,口服冻干制剂,分散片,自乳化／自微乳化释药系统（ＳＥＤＤＳ／ＳＭＥＤＤＳ）,干凝胶和干酏剂等口服固体速释制剂的研究与开发。     

Scaleup of Immediate Release Oral Solid Dosage Forms

Pharmaceutical Research -     

布洛芬缓释微丸的制备

目的制备布洛芬缓释微丸。方法以药用糖丸为母核，欧巴代为粘合剂和包衣材料，采用包衣造粒机撒粉上药及流化床包衣的工艺制备布洛芬缓释微丸。结果制得的微丸均匀圆整，体外释放度测定结果表明，该微丸符合2005年版《中国药典（二部）》布洛芬缓释胶囊的质量要求。结论采用药用糖丸撒粉上药及流化床包衣的工艺可制备布洛芬缓释微丸。