软胶囊崩解迟缓现象影响因素研究

目的：研究储存条件以及软胶囊处方对明胶胶片稳定性的影响，探讨软胶囊崩解迟缓的原因。方法：制备明胶胶片模拟软胶囊囊壳，采用溶胀动力学法测定明胶胶片平衡溶胀量(Seq)，同时测定软胶囊内容物溶媒PEG400中甲醛含量。以上述结果为指标，考察不同储存条件与胶囊处方对明胶胶片交联程度的影响。结果：空白明胶胶片在40℃条件下Seq与对照组具有极显著性差异，PEG400中甲醛含量增加。含有甘油、山梨醇、二氧化钛等辅料的胶片浸泡在PEG400中后Seq与对照组具有极显著性差异，PEG400中甲醛含量量著增加。加速条件下含有抗氧剂的胶片Seq与PEG400中甲醛含量变化不大。结论：在考察的储存条件中，温度对软胶囊稳定性影响较大。含有一些常用辅料的明胶胶片易受PEG400中外源性醛类杂质的影响，Seq降低。低沮保存、纯化辅料以及添加抗氧剂有助于缓解软胶囊崩解迟缓现象的发生。     

麝香保心分散片的制备和人参总皂苷的体外溶出度研究

目的　制备麝香保心分散片 ,考察人参总皂苷的体外溶出度。方法　以PVPP为崩解剂、MCC为填充剂、CMC Ca为溶胀性辅料、1%HPMC水溶液为粘合剂 ,制备麝香保心分散片 ;采用比色法以人参总皂苷为测定指标 ,考察其体外溶出度。结果与结论　按最佳工艺制备的麝香保心分散片在 (2 0± 1)℃水中于 15s内可完全崩解且分散均匀 ,其指标性成分人参总皂苷的溶出速率明显高于麝香保心丸     

自乳化释药系统的体外评价

目的 探讨自乳化释药系统的体外评价方法。方法 通过测定自乳化时间、乳化后乳剂粒径的大小及模型药物的体外溶出行为对自乳化释药系统进行体外评价。结果 优选出的自乳化处方10min内已基本乳化完全，乳化后乳剂粒子大小大多数在3μm左右，以吲哚美辛和尼莫地平为模型药物制备出自乳化释药系统，体外溶出结果表明：与混悬液相比，两种药物的体外溶出显提高。结论 自乳化释药系统能够提高难溶性药物的体外溶出。     

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。     

对乙酰氨基酚栓的溶出度测定

目的：测定对乙酰氨基酚栓的溶出度，考察不同厂家栓剂的质量。方法：用pH7．4的磷酸盐缓冲液为溶剂，浆法测定，紫外分光光度法涵定溶出度。结果：不同厂家的栓剂溶出度差异很大。结论：应建立溶出度涵定法以有效控制药品的质量。     

复方利福平片溶出度测定方法的研究

目的 建立复方利福平片的溶出度测定方法。方法 采用溶出度测定法第二法，以水为溶剂，转速为50r／min，经45min取样，紫外分光光度法在474nm处测定利福平的溶出量，溶出限度为标示量的75％。结果利福平在10．3—36．1μg／ml范围内线性关系良好(r＝1．0000)，平均回收率99．8％。结论 本方法准确、快速、简便。通过测定复方利福平片的溶出度可有效检测其制剂工艺水平。     

影响甲硝唑片溶出度的因素

目的：考察影响甲硝唑片溶出度的因素。方法：压片前分别按5种不同比例加羧甲基淀粉钠(CMS—Na)及硬脂酸镁，混匀，压片，测其溶出度：分别以87℃与50’C的淀粉作粘合剂制软材，压片，测其溶出度；分别以不同大小、不同硬度的颗粒压片，测其溶出度：同批颗粒分别制成直径8，9，10mm三种规格的片剂，测其溶出度。结果：CMS—Na能显著提高甲硝唑片溶出度。