氧氟沙星胶囊剂溶出度的测定

目的　采用转篮法测定氧氟沙星 (OFL X)胶囊的体外溶出度 ,以建立其溶出度的测定法。方法　按《中国药典》2 0 0 0年版溶出度的测定法测定 OFL X胶囊的溶出度。结果　实验数据根据威布尔分布模型计算出 T50 、Td 及 m。结论　方差分析表明 :不同厂家产品溶出度呈显著性差异 (P <0 .0 1)。 15 min时的累积溶出量之间无显著性差异 (P >0 .0 5 ) ,且符合《中国药典》2 0 0 0年版规定。     

国产麦迪霉素胶囊的溶出度研究

目的研究国产麦迪霉素胶囊的溶出度。方法通过稳定性试验考察处方组成、制粒工艺及不同包装材料对麦迪霉素胶囊溶出度的影响。结果表明不同处方、工艺所制备的国产麦迪霉素胶囊的初始溶出度,在20m in时几乎都达100%,但经加速试验30d或长期试验90d后,其溶出度急剧下降,在60m in时仍低于50%。而用日本进口的麦迪霉素原料制备的胶囊,其溶出度及稳定性均很好,经加速试验30d或长期试验90d后,经时20m in的溶出量均大于90%。结论在同样的处方工艺条件下,国产麦迪霉素胶囊放置后溶出度下降较快,而日本进口原料制备的麦迪霉素胶囊稳定性良好。     

异十五烷酸胶囊溶出度测定方法研究

目的 建立异十五烷酸胶囊溶出度测定方法 .方法 依照<中国药典>(2005年版)附录溶出度项下第二法,以十二烷基硫酸钠为溶出介质,转速为75r·min-1,高效液相色谱法测定,检测波长:210nm.结果 在4.44～22.2μg范围内(r=0.9998),浓度与峰面积呈良好的线性关系,平均回收率为99.69%,RSD为0.74%(n=9).结论 该方法 操作简便,准确可靠.     

Correlation between dissolution rate and bioavailability of different commercial mefenamic acid capsules

A dissolution test was performed with five brands of 250 mg mefenamic acid capsule products available on the market. Three of them, the fast dissolving A and the slow dissolving D and E were subjected to a bioavailability study using a commercially available suspension as the reference. The products were administered orally in a cross-over design to 6 healthy men, and then parameters for the bioavailability were calculated from the plasma concentration-time curve. Analysis of variance indicated several significant differences among the products with respect to C_max, T_max and AUC. The relative availabilities of A, D and E were 86, 81 and 28%, respectively, with the AUC value (0-7 h) for the suspension as 100%.No correlation was observed between the in vitro dissolution rate of the drug from the capsules and the in vivo data, because the dispersing behavior of the capsule exerted a marked influence on its in vitro dissolution rate. To eliminate the influence of the capsule disintegrating process, a dissolution test was done on the contents of the capsules. A good correlation was found between the bioavailability and the dissolution rate of the drug from the capsule contents.Product E with the lowest bioavailability was passed through a 200-mesh sieve, placed in a new capsule, and tested for its bioavailabilky in humans. The AUC value was greater than that of the original product and the bioavailability was about equal to that of the suspension. The in vitro dissolution rate of the drug from the pulverized product E was also markedly increased.     

Effects of various formulation factors on dissolution stability of aztreonam, hydrochlorothiazide, and sorivudine capsules

A split-split-plot 3² × 2² factorial design was used to study the effects of capsule filling machine and formulation factors such as lactose type, lubricant concentration, and capsule shell size on the dissolution stability of 50 mg potency hydrochlorothiazide (HCTZ), sorivudine (BV-araU), and aztreonam capsules packaged in HDPE bottles and stored under different conditions. It was observed that neither magnesium stearate concentration nor the type of capsule machine used to fill the capsule shells had any effect on dissolution stability of capsules of all three drugs for up to 6 months of storage at 50°C. For aztreonam, neither capsule shell size nor the type of lactose had any effect on dissolution stability. On the other hand, HCTZ size no. 1 capsules demonstrated better dissolution stability than size no. 2 capsules. Moreover, dissolution stability of capsules of sorivudine and HCTZ on storage at 50°C, 40°C/75% RH, and 40°C was dependent on the type of lactose used. HCTZ capsules containing Fast-Flo^® lactose, hydrous lactose, or anhydrous lactose showed up to 45, 25, and 10% decrease in dissolution, respectively, compared to initial values, at the 20 min dissolution time point after 6 months storage at 50°C. The extent of decrease in the dissolution rate was less under the conditions of storage at 40°C/75% RH and 40°C. Similar effects of decrease in the dissolution rate with the different types of lactose were observed with sorivudine, although to a much lesser degree compared to HCTZ capsules. No decrease in dissolution rate was observed for any drug after 20 months storage at 30°C. It was hypothesized that the slight decrease in dissolution rate of sorivudine capsules was due to significant caking of the capsule contents in the presence of the moisture liberated from the excipients and the capsule shells. For aztreonam capsules, the caking of their contents was without any discernable effect on dissolution because of the high aqueous solubility. In contrast, for HCTZ capsules, changes in dissolution rate were far too pronounced to be attributed to caking only.     

布洛芬液体胶囊的处方筛选及体外溶出的评价

目的筛选布洛芬液体胶囊处方,并采用高效液相色谱法对其进行溶出度考察。方法以液体胶囊的稳定性、崩解时限、体外溶出度为指标进行正交试验。结果最佳工艺处方为：甘油50mg,聚乙二醇100mg,吐温8010mg,氢氧化钠14mg。所制得的液体胶囊稳定,药物溶出快。结论布洛芬液体胶囊处方主要与氢氧化钠的用量有关。布洛芬液体胶囊与市售片剂相比,其溶出速率有明显提高。     

布洛芬软胶囊的溶出度测定

目的建立布洛芬软胶囊溶出度的测定方法,方法以磷酸盐缓冲液（pH 7.2）900 ml为溶出介质,采用转篮法（120 r.min^-1）45 min取样,运用HPLC法对其溶出度进行测定,并考察了溶出曲线。结果样品溶出均一性良好,溶出度均〉90%。布洛芬软胶囊与市售片剂相比,其溶出速率有明显提高。结论本法能考察和控制布洛芬软胶囊的质量。     

国产氟苯水杨酸胶囊剂与进口片剂溶出度的比较

目的：对国产氟苯水杨酸胶囊剂与进口片剂进行溶出度的比较。方法：参照ＵＳＰ２３ 版氟苯水杨酸片剂的溶出度测定方法,用紫外分光光度仪测定其含量。结果：测定方法的平均回收率为１００－２７％ ,ＲＳＤ为０－６２％ ,溶出度的重现性与均一性都较好。胶囊剂与片剂溶出８０％ 所需的时间分别为１２－８０ｍｉｎ 与１３－０４ｍｉｎ。结论：胶囊剂与片剂均符合质量标准中所规定的溶出限度,Ｔ８０ 两者无显著性差异。     

二氟尼柳胶囊溶出度的研究

目的：通过对二氟尼柳胶溶出速率的评价,以期得到一个有较好溶出特性的胶囊剂。方法：参照ＵＳＰ２３版二氟尼柳片剂的溶出度测定方法,用紫外分光光度仪测定溶出度。结果：二氟尼柳胶囊溶出度的方法回收率为１００．２７％,ＲＳＤ为０．６２％,重现性与均一性都较好。     

罗红霉素胶囊溶出度考察

目的:对不同厂家的罗红霉素胶囊进行溶出度比较。方法:采用2000年药典规定的方法测定溶出度,并对其溶出参数(Td、T50、m)进行统计处理。结果:不同厂家之间溶出速率相差很大(P<0.01),B厂最快,C厂最慢。结论:不同厂家的产品内在质量有显著差别。     

石杉碱甲胶囊剂与片剂的溶出度研究

目的：测定石杉碱甲胶囊和片剂的体外溶出速率。方法：用中国药典９５年版溶出度测定法第三法测定石杉碱甲胶囊与片剂的溶出度，在Ｗｅｉｂｕｌｌ概率纸上求出参数，用ｔ检验法进行比较；采用ＨＰＬＣ测定溶出液中用碱甲的含量。结果：片剂刚开始释放较快，胶囊有一滞后时间，胶囊与片剂的Ｔ５０分别为５．５和４．４ｍｉｎ，两者在１０ｍｉｎ后溶出百分数无显著性差异，２０ｍｉｎ时均达到９０％以上。     

Permeability and stability of chitosan-based capsules: effect of preparation

Capsules were obtained by interpolymer complexation between chitosan (polycation) and sodium hexametaphosphate (oligoanion). The effect of preparation variables such as the pH, ionic strength as well as the reagent and porogen concentration on the capsule characteristics was evaluated. By decreasing the chitosan/SMP ratio, adding mannitol up to 1% or maintaining the salt concentrations below 0.15 w/v%, the diffusion characteristics can be modulated without disturbing the capsule mechanical stability. Higher concentrations of the cross-linking agent (2.25 w/v%) produced stable capsules only in the absence of electrolyte and low polyol amounts. Furthermore, by increasing the ionic strength, or the pH of the initial chitosan solution, the membrane exclusion limit shifted to higher values concomitant with a significant loss in the membrane compression resistance. The results obtained showed that the capsule characteristics could be independently controlled by manipulating the coacervation conditions.     

脂必泰胶囊溶出度测定的方法研究

目的 建立脂必泰胶囊溶出度的测定方法。方法 采用ZABAX-C₁₈色谱柱（250 mm×4.6 mm,5 μm）,甲醇-0.05%磷酸（80：20）为流动相;流速1.0 ml/min;检测波长238 nm。按《中华人民共和国药典》2015年版四部溶出度测定第三法（小杯法）,采用SOTAX AT7智能药物溶出仪,通过对溶出介质、转速和取样时间的优化选择,确定脂必泰胶囊中红曲的有效成分洛伐他汀溶出度测定方法。结果 本研究建立的色谱条件,专属性良好。洛伐他汀的线性范围1.63~122.2 μg/ml （r=1.000 0）。样品的溶出度均一性良好,以含1.0%十二烷基硫酸钠的磷酸盐溶液（pH 7.0）为溶出介质,取样时间为45 min,转速为100 r/min。溶出度均不低于80%。结论 本研究建立的方法可用于脂必泰胶囊溶出度的测定,能有效控制药品的质量,为提高脂必泰胶囊质量标准提供依据。     

聚维酮碘泡腾栓的稳定性

目的：考察不同条件下聚维酮碘泡腾栓的稳定性。方法：采用加速试验，经典恒温法和多元线性模型预测其有效期。结果：经典恒温法和多元线性模型预测室温贮存期分别为432d和419d。两种方法结果差异无显著性。结论：聚维酮碘泡腾栓贮存期可定为1年，且密闭，阴凉，干燥处保存。     

盐酸依匹斯汀胶囊溶出度试验方法的建立及溶出曲线的评价

目的:建立盐酸依匹斯汀胶囊溶出度试验方法,并与市售产品进行溶出曲线评价,考察其有效性。方法:采用篮法,以水为溶出介质,转速为75 r·min-1,并对其与市售产品进行溶出曲线评价。溶出液色谱条件:色谱柱为Agilent Zorbax SB-CN柱(250 mm×4.6 mm,5μm);流动相为乙腈-0.05 mol.L-1磷酸盐缓冲溶液(35∶65);流速为1.0 mL·min-1;检测波长为220 nm;柱温为30℃。结果:盐酸依匹斯汀在0.10～24.12μg.mL-1范围内呈良好线性关系,r=0.999 9,因此采用此法检测本品溶出度,能达到要求,并且与市售产品溶出曲线相似。结论:溶出度的考察更能体现药品的有效性,该方法专属、灵敏、简便,可用于测定盐酸依匹斯汀胶囊的溶出度。     

Nitrofurantoin-p-aminobenzoic acid cocrystal: hydration stability and dissolution rate studies

Nitrofurantoin (NF) drug is known to transform to a hydrate form in aqueous medium. The hydration stability and dissolution rate of a few cocrystals of NF were compared with that of its stable β polymorph and hydrate form II. Hydrogen bonding and molecular packing in the novel cocrystal structures were analyzed. Pharmaceutical cocrystals of NF with p-aminobenzoic acid (PABA) and urea showed superior physicochemical properties compared with the known L-arginine salt hydrate. All the solid-state adducts were characterized by single-crystal X-ray diffraction, X-ray powder diffraction, differential scanning calorimetry, and thermogravimetric analysis. NF-PABA cocrystal was found to be superior among the compounds studied in terms of minimal transformation to NF hydrate and comparable dissolution rate to the reference drug.     

吲达帕胺胶囊的研制及溶出度考察

目的:研制吲达帕胺胶囊并对其溶出度进行考察.方法:溶出介质选用乙醇-水(5:895)900mL,用紫外分光光度法测定其溶出度,测定波长为240nm.测定吲达帕胺胶囊在不同转速及不同时间的累积溶出量.结果:转速为75r·min-1,取样时间为45min,吲达帕胺胶囊的溶出度均大于标示量的70%.结论:所研制的吲达帕胺胶囊溶出度符合要求.