33 factorial design-based optimization of the formulation of nitrofurantoin microcapsules

A microcapsule form of nitrofurantoin was prepared by a simple coacervation method with carboxymethylcellulose and aluminium sulfate. 3³ factorial design was performed for three independent variables, namely, the particle size of the drug, the size of the microcapsules and the pH of the dissolution medium. The dissolution tests with the formulated microcapsules were carried out according to the United States Pharmacopeia XXII rotating basket method at pH 1.2, 5 and 7.5, which represent the pH of gastrointestinal fluids. Release data were examined kinetically and the ideal kinetic models were estimated and t _63.2 values obtained from RRSBW distribution were used in the factorial design experiment. The influence of the independent variables on the dissolution of nitrofurantoin microcapsules could be expressed as the pH of the dissolution medium > particle size of the microcapsule > particle size of nitrofurantoin. The other aim of this study was to evaluate microcapsule formulation in terms of the United States Pharmacopeia criteria with a minimum of experiments. Our findings suggest that dosage forms which comply with the pharmacopoeia criteria for dissolution can be prepared and selected by factorial design.     

应用威布尔分布函数研究红霉素微囊的溶出度

本文测定了红霉素微囊在人工肠液中的溶出度，并用威布尔分布函数求出了溶出百分率与时间的关系。     

Preparation and evaluation of sodium diclofenac controlled-release tablets

The dissolution behaviour of a direct compression compact prepared with sodium diclofenac and dibasic calcium phosphate (DCP) in different weight ratios with or without Biosoluble polymer^® (acrylic-based resin) was investigated in distilled water and in a medium with changing pH. The results indicate that the amount of sodium diclofenac released from the compact was dependent on the amount of drug and DCP used in the compact, and was also controlled by the amount of Biosoluble polymer^® added. A chemical reaction forming diclofenac acid might occur on the surface of the sodium diclofenac compact during exposure to the acidic medium, which was confirmed by diffuse-reflectance spectroscopy. The tablet with a 12 weight ratio of sodium diclofenac to DCP exhibited a sustained-release behaviour, similar to commercial sustained-release products (Voltaren SR-100^® and Grofenac Retard^®), but a lower release rate was found as compared to the commercial products. The dissolution behaviour of the study tablet and the commercial products was found to be dependent on the dissolution medium and the rotating speeds. Glass beads were added to the dissolution assembly to simulate the influence of food, and the enhanced friction between tablet and glass beads might result in a higher dissolution rate of the tablet and the commercial products.     

酮康唑微囊的体外溶出度研究

目的 研究酮康唑微囊的体外溶出特点。方法 按中国药典所载转蓝法进行体外溶出度测定。结果 酮康唑微囊在人工胃液中90min内可达到最大溶出，其最高累积溶出百分率接近90％，其溶出行为符合Weibull概率函数分布，相关参数为：药物溶出50％的t1/2=25min，特征数td=42min，形态参数m=0．6min。结论 酮康唑微囊在人工胃液中溶出较理想。     

微粉化工艺对羊血提取物中氯高铁血红素溶出度的影响

目的研究微粉化工艺对羊血提取物中氯高铁血红素溶出度的影响。方法采用溶出度参数T50值对比了原药粉和3种原料药与乳糖的混合工艺(包括微粉化处理、高速粉碎机粉碎、简单混合)对氯高铁血红素溶出度的影响。结果原料药与乳糖混合后3种不同的处理方法对氯高铁血红素溶出度均有不同程度的改善,它们的T50值依次为2.36,3.79和10.29min,而原料药为28.03min。其中经过微粉化的样品溶出最快,比原料药加快了近12倍。结论将氯高铁血红素与乳糖一起微粉化是改善溶出度行之有效的方法。     

利巴韦林分散片的制备及稳定性评价

目的研究利巴韦林分散片的处方和制备工艺。方法对按笔者自我设计配方制备的4种利巴韦林分散片,采用高效液相色谱法测定溶出度及进行稳定性评价。结果以处方3工艺制成的片剂,质量可控,稳定性较好。结论处方3工艺成熟,质量稳定,是一种易于服用、奏效快的新制剂。     

复方解热凝胶溶出度方法研究

目的：建立复方解热凝胶的溶出度标准。方法：采用《中华人民国和国药典》(2000年版)二部附录X溶出度测定第二法，以0.062 mol·L 1盐酸为溶剂，测定复方解热凝胶溶出度。结果：复方解热凝胶溶出度均一性好，累积溶出百分率在30 min内达89.8%；经后差检验，C＝0.000 98，P＝1。结论：该剂型溶出度标准30 min内确定为标示量的85.0%。     

三种市售甲巯咪唑片的质量比较

目的:比较甲巯咪唑片的质量.方法:用<中国药典>2000年版和参考文献的方法对甲巯咪唑片的含量均匀度、溶出度、含量进行考察.结果:3个厂家中,B药含量均匀度较好,溶出度参数m,Td,T50差异小,含量稳定.结论:不同厂家产品的内在质量存在差异,临床用药时应加以注意.     

维甲酸自乳化制剂的含量测定及体外溶出评价

目的:研究维甲酸RA自乳化制剂的含量测定方法及体外溶出行为.方法:采用HPLC法测定维甲酸RA自乳化制剂的药物含量,与市售胶囊比较,考察RA自乳化制剂体外溶出行为.结果:与市售胶囊剂相比,以水为溶出介质,维甲酸RA自乳化制剂15min可以溶出80%以上,而市售胶囊只溶出不到5%.自乳化制剂可以显著提高药物的体外溶出.     

蝙蝠葛酚性碱片溶出度方法考察

目的:探讨中药制剂蝙蝠葛酚性碱片的溶出度,为临床用药提供参考。方法:采用紫外分光光度法,分别对其溶出介质、转速进行考察,对累积溶出百分率进行测定,并对3批样品进行均一性试验。结果:蝙蝠葛酚性碱片在45 m in内即溶出70%以上,相对标准偏差在3.0%以内。结论:中药固体制剂蝙蝠葛酚性碱片按照《中国药典》(二部)有关溶出度测定方法控制其内在质量是可行的,可保证临床用药安全、有效。