琥乙红霉素缓释片释放度研究

目的建立琥乙红霉素缓释片体外释放研究分析的硫酸显色法。方法以900 mL经脱气处理的0.1 mol/L盐酸溶液为释放介质,转速为75 r/min,75%的硫酸溶液为显色剂,采用紫外-可见分光光度法于482 nm波长处对琥乙红霉素缓释片的释放度进行测定。结果琥乙红霉素显色后质量浓度在40～72μg/mL范围内与吸收度呈良好线性关系(r=0.999 9);平均回收率为99.75%,RSD为0.76%;12 h内3批样品的释放量均在标示量的90%以上。结论该方法操作简便、准确可靠,可用于琥乙红霉素缓释片释放度的测定,为质量标准的制订提供了依据。     

阿司匹林肠溶片释放度测定方法的改进

目的对阿司匹林肠溶片释放度的测定方法进行改进。方法建立新的释放度测定方法。结果新法比原法更真实更准确地反映出阿司匹林肠溶片的释放度。结论建立的新测定方法,结果满意。     

双氯芬酸钠肠溶片释放度的测定

目的建立双氯芬酸钠肠溶片释放度测定方法。方法采用UV法测定双氯芬酸钠肠溶片释放度，测定波长为276nm。结果双氯芬酸钠线性范围为6．0～20．0μg／ml，r=0．9998；平均回收率为99．8％，RSD=0．3％(n=9)。结论本法简便、准确，可作为双氯芬酸钠肠溶片释放度测定方法。     

双氯芬酸钠肠溶片释放度的测定

目的建立双氯芬酸钠肠溶片释放度测定方法.方法采用UV法测定双氯芬酸钠肠溶片释放度,测定波长为276 nm.结果双氯芬酸钠线性范围为6.0～20.0 μg/ml,r=0.9998;平均回收率为99.8%,RSD=0.3%(n=9).结论本法简便、准确,可作为双氯芬酸钠肠溶片释放度测定方法.     

双氯芬酸钠肠溶片释放度的测定

目的　建立双氯芬酸钠肠溶片释放度测定方法。方法　采用UV法测定双氯芬酸钠肠溶片释放度 ,测定波长为 2 76nm。结果　双氯芬酸钠线性范围为 6 .0～ 2 0 .0 μg/ml,r =0 .9998;平均回收率为 99.8% ,RSD =0 .3% (n =9)。 结论　本法简便、准确 ,可作为双氯芬酸钠肠溶片释放度测定方法。     

红霉素肠溶片释放度测定实验条件的改进

目的优化红霉素肠溶片释放度测定条件,减少吸收度测量误差.方法以实验溶剂代替原规定溶剂,按中国药典2000年版二部收载标准实验. 结果红霉素肠溶片在实验溶剂中测得的吸收值约为0.5左右,测量误差小,峰形单纯尖锐,显色稳定,比色液浓度20～34μg.mL-1范围线性良好,r=0.9993.结论实验溶剂提高了释放度测定值的准确度、精密度,更适用于该制剂的质量分析检验.     

红霉素肠溶片质量分析

目的:对国内不同厂家生产的红霉素肠溶片的质量进行对比研究。方法:采用释放曲线测定、有关物质、含量测定等检测方法,综合评价不同工艺的制剂产品。结果:释放曲线测定结果显示目前国内的红霉素肠溶片厂家间质量差异较大,同一厂家不同批次的质量均一性不好。数据同时还显示存在低限投料和用不合格原料投料的情况。结论:结果表明国内红霉素肠溶片质量参差不齐,应引导企业进行制剂工艺改进,提高质量。     

蒽酮硫酸法与苯酚硫酸法测定竹节参多糖含量的比较研究

目的 考察蒽酮硫酸法与苯酚硫酸法测定竹节参多糖(Panax japonicus polysaccharides,PJPS)含量的可行性并比较其差异,建立竹节参多糖含量测定方法.方法 对蒽酮硫酸法和苯酚硫酸法测定竹节参多糖含量的显色条件和方法学进行研究,比较2种方法测定结果的差异.结果 蒽酮硫酸法含量测定结果高于苯酚硫酸法,其差异有统计学意义,蒽酮硫酸法的线性、重现性和稳定性都优于苯酚硫酸法.结论 蒽酮硫酸法比苯酚硫酸法更适合测定竹节参中多糖的含量.     

红霉素肠溶片包衣处方工艺

目的：解决红霉素肠溶片贮存过程中释放度易下降导致不合格的问题。方法：通过改进肠溶包衣材料处方及包衣工艺，采用聚丙烯酸Ⅱ、Ⅲ混合树脂作包衣材料，粉衣层中用羟丙甲纤维素代替明胶，包衣工艺采用在肠衣层表面喷上一层保护液。结果：红霉素肠溶片在贮存3年后，释放度高于标示量的85％。结论：此包衣处方及包衣工艺能够保证红霉素肠溶片在有效期3年内释放度符合中国药典规定。     

盐酸二甲双胍缓释片体外释放度研究

目的对盐酸二甲双胍缓释片体外释放度相关因素进行研究。方法对溶出介质、转速、测定波长及辅料等因素进行考察,确定盐酸二甲双胍缓释片体外释放度的测定方法,对测定方法进行回收试验,并对三批样品及参比制剂进行测定。结果采用转篮法,以1000ml水为溶出介质,转速为100rpm/min,采用UV法,测定波长为233nm,将溶出液稀释至1～12.5μg/ml进行测定。结论本释放度方法简单,快速,可用于盐酸二甲双胍缓释片体外释放度测定。     

对柳氮磺吡啶肠溶片释放行为及其限度标准的探讨

目的：考察《中国药典》2010年版柳氮磺吡啶肠溶片中薄膜衣片和糖衣片处方工艺对释放度的影响,探讨其释放度限度标准的科学性与合理性。方法：采用转篮法（转速为100 r·min^-1）,考察国内7家生产企业样品在pH 6.0,pH 6.8,pH 7.5磷酸盐缓冲液中的体外释放行为。结果：在pH 7.5磷酸盐缓冲液中,不同企业的肠溶薄膜衣片释放曲线一致;薄膜衣片和糖衣片的释放曲线存在差异;在pH 6.0和pH 6.8磷酸盐缓冲液中,国内原研企业的薄膜衣片释放行为最符合该品种的药剂学特性。结论：通过对比国内外药典关于该品种的释放度限度规定及国内样品在3种释放介质中的释放行为研究,认为《中国药典》2010年版柳氮磺吡啶肠溶片释放度限度标准有待完善,肠溶糖衣片的处方工艺有待优化。     

Preparation and in vitro evaluation of enteric-coated tablets of rosiglitazone sodium

The aim of this study was to prepare the rosiglitazone sodium enteric-coated tablets and investigate its release rate. The rosiglitazone sodium enteric-coated tablet was prepared by single punch tablet press using substituted hydroxypropyl cellulose and polyvinylpyrrolidone (PVP). The release rate from the enteric-coated tablet of rosiglitazone sodium was evaluated. The release rate study showed that few rosiglitazone sodium was released from enteric coated formulation within 2 h in simulated gastric juice, while it released more than 80% of the labeled amount in 30 min in simulated intestinal juice. The preparing method of rosiglitazone sodium enteric-coated tablets was simple and had a good reproducibility. The release condition and determined methods could be used for the routine determinations of rosiglitazone sodium enteric-coated tablets.     

埃索美拉唑镁肠溶片的制备

目的：制备埃索美拉唑镁肠溶片并对自制片进行质量分析。方法：采用流化床包衣法制备埃索美拉唑镁肠溶微丸,然后选用适宜辅料采用直接压片法对微丸压片,并将自制片与市售片进行药物体外药物释放度、耐酸力及稳定性的比较。结果：自制的埃索美拉唑镁肠溶片的各项指标均符合质量标准的要求。结论：优选的埃索美拉唑镁肠溶片的处方工艺合理,重现性好,有效地解决了埃索美拉唑镁的稳定性问题。     

右旋酮洛芬肠溶微丸的研制及其体外释放研究

目的：制备右旋酮洛芬肠溶微丸,并考察其在0.1 mol·L-1盐酸溶液和pH 6.8磷酸缓冲液（PBS）中的释放情况。方法：采用流化床包衣技术,在空白糖丸芯上依次包主药层、隔离层和肠溶衣层,制备成肠溶衣微丸;以上药率为指标,考察HPMC浓度和主药上药浓度;观察是否粘连、颗粒大小均一度和表面色泽均匀与否等综合指标,采用正交试验优选包衣工艺条件;与普通肠溶片比较在PBS中的释放情况。结果：制得的微丸上药均匀、上药率高、外观圆整有光泽;确定HPMC浓度和主药上药浓度分别为5%和15%,优选出最佳包衣工艺条件为物料温度为36℃、雾化压力为1.0 bar及喷枪速度为0.8 ml·min-1;在盐酸溶液中2 h的释放量小于10%,在PBS中的释放度高于普通肠溶片。结论：所制右旋酮洛芬肠溶微丸工艺可行,具有良好的耐酸性和体外释放度。     

泮托拉唑钠肠溶微丸型片剂的制备

研究泮托拉唑钠肠溶微丸型片剂制备方法。采用流化床包衣法制备泮托拉唑钠肠溶微丸, 将肠溶微丸与适合的辅料混合采用直接压片法制备泮托拉唑钠微丸型片剂。用体外释放度法及扫描电镜法观察压片前后药物的体外累计释放量及微丸形态。结果表明, 优化处方: 衣膜增重55%, 增塑剂含量20%, Eudragit L30D-55/ NE30D为8∶2, 肠溶微丸/辅料 (MCC/PPVP/PEG 6000, 2∶1∶1) 为5∶5时, 肠溶片在0.1 mol·L⁻¹盐酸中2 h累积释放百分数<10%, pH 6.8磷酸盐缓冲液中1 h累积释放百分数>85%。制备的泮托拉唑钠肠溶微丸片的释药行为较好, 有望应用于工业生产。     

Citric acid as excipient in multiple-unit enteric-coated tablets for targeting drugs on the colon

Delivery of drugs to the large bowel has been extensively investigated during the last decade. The aim of this study was to investigate whether enteric-coated tablets could be made from enteric-coated matrix granules and drug release targeted to the colon. Whether in vitro drug release rate and in vivo absorption could be delayed by adding citric acid to the granules and/or to the tablet matrix was also studied. Ibuprofen was used as model drug because it is absorbed throughout the gastrointestinal tract. Eudragit S and Aqoat AS-HF were used as enteric polymers. Drug release rates were studied at different pH levels and drug absorption was studied in bioavailability tests. The conclusion was that citric acid retarded in vitro drug release when used in multiple-unit tablets. In vivo absorption of ibuprofen was markedly delayed when citric acid was included in both granules and tablet matrix. Further studies are needed to determine the optimal amount of citric acid in formulations.     

Drug Release from Tablets Containing Cellulose Acetate Phthalate As an Additive or Enteric-Coating Material

A formulation containing cellulose acetate phthalate for preparing enteric-coated granules was developed with the use of granulation and microencapsulation techniques. Drug release from tablets or tabletted microcapsules was measured in a disintegration apparatus and an in vitro variable-pH release simulator of the flow type. The release mechanism for the tablets or tabletted microcapsules was determined with the Higuchi matrix model, a first-order kinetic model, and the Weibull distribution function. Adding acetone directly to the mixture of sulfamethoxazole and cellulose acetate phthalate resulted in enteric-coated granules with more prolonged release than other granulation methods. Microencapsulation of the granules significantly delayed the drug release and enhanced the effectiveness of the enteric coating. Microencapsulated granules show release patterns that are sustained and can be simulated with three different release models, i.e., with square-root time plotting, diffusional first-order plotting, and Weibull distribution plotting. The enteric-coating behavior of the tablets was more clearly demonstrated with the variable-pH release simulator than with a fixed-pH dissolution method.     

Tablet Formulation Study of Spray-Dried Sodium Diclofenac Enteric-Coated Microcapsules

Sodium diclofenac enteric-coated microcapsules were prepared by a spray-drying technique with Eudragit L 30D as enteric-coating material. The spray-dried powder, mixed with neocel or flo-starch, or the mixture of neocel and flo-starch (weight ratio, 1:1) was directly compressed into a tablet. The micromeritic properties of the spray-dried powder and the mixed powder for tableting were investigated. The flowability of the spray-dried powder was poor but improved after incorporating the excipients. The release rates of sodium diclofenac from the spray-dried powder, the mixed powder before tableting, and the tablets were determined in 0.1 N HC1 solution, pH 6.8, phosphate buffer solution, distilled water, and pH-changed medium. The results indicated that the spray-dried powder, the mixed powder before tableting, and the tablets all exhibited enteric-coated release properties; these powders and tablets showed some resistance to simulated gastric acid and then released drug more rapidly in pH 6.8 buffer solution. The weight ratio of neocel to flo-starch plays an important role in controlling the release of sodium diclofenac from enteric tablets. The 1:1 weight ratio of neocel to flo-starch was more suitable for designing the microdispersed sodium diclofenac enteric-coated tablets.     

长效喘通制剂的研究

为了进一步解决喘通的前体药物——双羟荼酸喘通在体内的长效作用,制成了肠溶颗粒装入硬胶囊,及将肠溶颗粒压成片剂两种剂型。用体外溶出试验与临床平喘时间相结合得出体外溶出最低浓度,并以此比较两种制剂的缓释效果。肠溶颗粒压成片剂为比较理想的长效喘通制剂。它能较恒定地缓释药物,体外溶出最低浓度达10小时以上。并试用于临床,初步取得了予期的副作用小、平喘时间达12小时的良好效果。     

盐酸小檗碱肠溶缓释片制剂工艺研究

目的 研究盐酸小檗碱肠溶缓释片的制剂工艺。方法 采用体外释放度评价的方法,以单因素设计及正交设计筛选片芯处方及工艺,并对片芯进行肠溶包衣,制备盐酸小檗碱肠溶缓释片。结果 体外释放度实验显示,片芯及肠溶片均符合Higuchi释药模型。结论 盐酸小檗碱肠溶缓释片工艺稳定,体外释放符合设计要求。