萘普生微囊的制备及其质量考察

目的:制备萘普生微囊并考察其制剂质量。方法:以明胶和阿拉伯胶为囊材,采用复凝聚法将萘普生制成微囊;以阿拉伯胶浓度(A)、萘普生与阿拉伯胶的质量比例(B)和成囊温度(C)为考察因素,包封率为指标设计正交试验优化成囊的最佳制备工艺,并对优化工艺所制得微囊的粒径、包封率、载药量、体外释放性进行考察。结果:最佳工艺条件为A2%、B1:1、C50℃;所制微囊的平均囊径48.92μm,包封率(77.03±1.43)%,载药量(35.31±1.02)%,微囊在48h时体外累积溶出百分率达到91.32%。结论:所制萘普生微囊工艺重现性好、稳定,并具有良好的缓释作用。     

大蒜素肠溶微囊的制备及其性质研究

目的 以肠溶材料聚丙烯酸树脂Ⅱ为囊材制备大蒜素微囊.方法 采用单凝聚法制备大蒜素肠溶微囊并研究其粒径、载药量、包封率、体外释药等性质.结果 经优化制得的大蒜素肠溶微囊为类圆球形颗粒,平均粒径为52.2μm,平均载药量28.97%,包封率80.74%,体外释放符合肠溶制剂的标准,对大鼠的胃黏膜几乎无刺激.在4.5×103 lx照射,60°C高温及相对湿度90%条件下放置10 d,微囊的粒径分布和剩余药量无显著变化.结论 制备工艺简单,所制得的大蒜素微囊具有肠溶特性.     

甲硝唑微囊的制备及质量评价

目的制备甲硝唑微囊并对其质量进行评价。方法以明胶和阿拉伯胶为囊材,采用复凝聚法制备甲硝唑微囊,并对微囊的包封率、载药量和体外释药性进行考察。结果所制微囊包封率在72%以上,载药量大于40%,8h时累积释药量达85%。结论该制剂制备方法简便易行,质量评价合格。     

双嘧达莫缓释微囊的制备与体外评价

目的:研究以明胶和阿拉伯胶为囊材,将双嘧达莫微囊化的制备工艺。方法:以微囊的药物包封率为制备工艺优化指标,利用复凝聚法,通过正交实验得出微囊的最佳制备工艺条件。结果:囊材与囊心物的质量比2∶1,搅拌转速140r·min-1,固化时间3h、成囊pH4.0、成囊温度为50℃为最佳工艺条件。结论:以最佳制备工艺条件制备含药微囊,重复性好,工艺稳定,同时体外溶出实验表明,该微囊具有较好的缓释作用。     

左旋多巴微囊制备工艺的研究

目的以乙基纤维素为囊材,优选左旋多巴微囊的制备工艺。方法以微囊的包封率及载药量为评价指标,采用正交实验优选左旋多巴微囊液中干燥法制备工艺条件,并对制备的微囊进行质量检查。结果优选出的制备工艺为:囊材与药量比例为0.6∶1.4,油水相比例为105∶30,PVP量为0.2g,验证实验表明,优化工艺所制左旋多巴微囊的平均载药量为54.94%,平均包封率为89.2%。质量检查结果表明,微囊外观圆整且无粘连现象,大部分微囊的粒径分布在300～600μm范围内。优选出的左旋多巴微囊在体外具有明显的缓释效果。结论采用液中干燥法制备左旋多巴微囊,工艺稳定可靠,操作简便,工艺条件合理、可行。     

星点设计-效应面法优化流化床制备盐酸普萘洛尔微囊工艺

目的优化盐酸普萘洛尔微囊的制备工艺。方法采用流化床制备普萘洛尔微囊,以平均粒径,包封率、载药量及总评归一值为评价指标,并运用星点设计考察囊材液流速、喷雾压力对制备工艺的影响,对结果进行多元线性和二项式拟合,效应面法选取最佳工艺条件进行预测分析。结果从复相关系数上看,各指标二项式拟合方程均优于多元线性回归方程,最佳工艺参数:囊材液流速1.00 mL·min-1,喷雾压力0.65 bar,在此工艺条件下得到微囊粒径为300μm,载药量为20.54%,包封率达89.63%。结论优选普萘洛尔微囊的流化床制备工艺稳定可行,包封率高,有利于工业化生产。     

生姜油微囊的制备及其质量评价

目的:制备生姜油微囊并对其进行质量评价。方法:以辛烯基琥珀酸淀粉钠为囊材,采用喷雾干燥法制备生姜油微囊。以囊材与囊芯的混合温度、囊材与囊芯质量比、搅拌速度为考察因素,包封率为评价指标,采用正交试验优化生姜油微囊的制备工艺,并对其载药量、包封率、外观、粒径分布及光、热、湿稳定性(以碘价、过氧化值为指标)进行评价。结果:生姜油微囊的最优制备工艺为囊材与囊芯的混合温度60℃、囊材与囊芯质量比10∶1、搅拌速度12 000 r/min。最优工艺所制生姜油微囊的平均载药量为17.97%(n=3)、平均包封率为73.57%(n=3),生姜油微囊形态圆整光滑、无粘连、粒径分布均匀,平均粒径为(6.30±0.27)μm,在光、热、湿条件下生姜油微囊碘价、过氧化值变化较小。结论:优化后的生姜油微囊制备工艺简单、重复性好,生姜油微囊的包封率及载药量高,且稳定性较好。     

萘普生缓释微囊的制备及其体外释药研究

目的 对以壳聚糖和海藻酸钠为囊材,通过复凝聚法将萘普生微囊化的制备工艺和体外释药进行研究.方法 以微囊的药物包封率为制备工艺优化指标,得出成囊的最佳制备工艺条件.结果 最佳工艺条件为:搅拌速度500 r·min-1,pH4.0,壳聚糖浓度3%,反应温度50℃.结论 以最佳制备工艺条件制备了可生物相容,自然降解无毒的载药微囊,重现性好,工艺稳定,同时体外溶出实验表明,该微囊具有较好的缓释作用.     

甲硝唑微囊口服结肠定位给药系统的制备

目的 :考察甲硝唑微囊口服结肠定位给药系统的制备工艺。方法 :采用液中干燥法制备微囊 ,应用均匀试验设计 ,考察各因素水平对微囊包封率、载药量的影响。按优化后的结果选择实验条件 ,进行重复实验 ,用体外溶出实验考察其结肠定位释放效果。结果 :制备的甲硝唑微囊包封率为 ( 62 .3± 1.3 ) % ,载药量为 ( 5 9.8± 2 .0 ) % ,所制备的片剂在 0 .1mol·L- 1 盐酸溶液和 pH6.8磷酸盐缓冲液中几乎不释放 ,而在 pH7.5磷酸盐缓冲液中 3 0min的平均累积释放量为 82 .13 %。结论 :优化后的制备工艺对甲硝唑微囊口服结肠定位给药系统的研究和应用具有一定的参考价值。     

盐酸小檗碱微囊的制备及其体外释放研究

目的:为改善口感、减小对胃黏膜的刺激,制备盐酸小檗碱微囊,并考察其体外释药特性。方法:以阿拉伯胶、明胶为囊材,采用复凝聚法制备盐酸小檗碱微囊,以包封率、载药量、外形为指标,采用正交设计试验对囊心(盐酸小檗碱)-囊材质量比、囊材质量分数、搅拌速度进行优化,并进行验证。考察所制制剂的粒径分布及在人工肠液中5 h内的体外释药率。结果:最优处方为囊心-囊材质量比为1∶3,阿拉伯胶和明胶的质量分数均为2.50%,搅拌速度为200 r/min,成囊温度为53℃。所制盐酸小檗碱微囊的包封率为38%,载药量为41.71%;微囊圆整光滑,无粘连,粒径均匀,外形评分50.6;80%以上分布在3~9μm;3 h的累积释药率即达90%。结论:成功制得盐酸小檗碱微囊。     

Preparation and in vitro evaluation of slow release ketoprofen microcapsules formulated into tablets and capsules.

Ketoprofen powder was encapsulated with Eudragit RL/RS polymer solutions in isopropanol-acetone 1:1, using a simple and rapid method. Microcapsules were prepared using Eudragit solutions with different RL/RS ratios. The encapsulation process produces free-flowing microcapsules with good drug content and marked decrease in dissolution rate. The retardation in release profile of ketoprofen from microcapsules was a function of the polymer ratio employed in the encapsulation process. In vitro release of ketoprofen from microcapsules either filled in gelatin capsules or compressed into tablets, using calcium sulphate as diluent, confirmed the efficiency of the encapsulation process for preparing prolonged release medication. A capsule formulation with optimum sustained-release profile was suggested.     

克拉霉素微囊的制备及其质量评价

目的:制备克拉霉素微囊并对其质量进行评价。方法:以乙基纤维素为囊材,采用乳化-溶剂挥发法制备克拉霉素微囊,并对微囊粒径、包封率和载药量、体外释药性进行考察。结果:所制微囊粒径分布均匀,粒径33.0～38.0μm,包封率在87%以上,载药量大于45%,6h时累积释药量达75%。结论:该制剂制备方法简便易行,质量评价合格。     

Preparation and in vitro evaluation of slow release ketoprofen microcapsules formulated into tablets and capsules

Abstract

Ketoprofen powder was encapsulated with Eudragit RL/RS polymer solutions in isopropanol-acetone 1:1, using a simple and rapid method. Microcapsules were prepared using Eudragit solutions with different RL/RS ratios. The encapsulation process produces free-flowing microcapsules with good drug content and marked decrease in dissolution rate. The retardation in release profile of ketoprofen from microcapsules was a function of the polymer ratio employed in the encapsulation process. In vitro release of ketoprofen from microcapsules either filled in gelatin capsules or compressed into tablets, using calcium sulphate as diluent, confirmed the efficiency of the encapsulation process for preparing prolonged release medication. A capsule formulation with optimum sustained-release profile was suggested.     

Preparation of double-encapsulated microcapsules for mitigating drug loss and extending release.

The double-encapsulated microcapsules were prepared by the non-solvent addition, phase-separation method to form core material and, encapsulated with the O/W emulsion non-solvent addition method to increase drug loading and regulate drug release rate. The drug used was theophylline, which is water-soluble. Dichloromethane and n-hexane were used as the solvent and non-solvent, respectively. This study investigated how various core material and microcapsule EC/TH ratios affect the drug loss, particle size, surface morphology and release rate. The drug loss of the double-encapsuLated microcapsules was 12.8% less than that of microcapsules prepared by the O/W emulsion non-solvent addition method alone. The particle size of these double-encapsulated microcapsules decreased as the concentration of EC polymer was increased in the second encapsulation process. The roughness of their surface was also in proportion to the concentration of polymer solution used in the second encapsulation process. The dissolution study showed that the T20 of the double-encapsulated microcapsules ranged from 2-35.4 h, while that of the O/W emulsion non-solvent addition method microcapsules was from 2.7-7.7 h. The greater the level of EC in the polymer solution, the slower the release rate of the drug from the microcapsules when the EC was not over the critical amount.     

Preparation of double-encapsulated microcapsules for mitigating drug loss and extending release

The double-encapsulated microcapsules were prepared by the non-solvent addition, phase-separation method to form core material and, encapsulated with the O/W emulsion non-solvent addition method to increase drug loading and regulate drug release rate. The drug used was theophylline, which is watersoluble. Dichloromethane and n-hexane were used as the solvent and non-solvent, respectively. This study investigated how various core material and microcapsule EC/TH ratios affect the drug loss, particle size, surface morphology and release rate. The drug loss of the double-encapsulated microcapsules was 12.8% less than that of microcapsules prepared by the O/W emulsion non-solvent addition method alone. The particle size of these double-encapsulated microcapsules decreased as the concentration of EC polymer was increased in the second encapsulation process. The roughness of their surface was also in proportion to the concentration of polymer solution used in the second encapsulation process. The dissolution study showed that the T 20 of the double-encapsulated microcapsules ranged from 2-35.4 h, while that of the O/W emulsion non-solvent addition method microcapsules was from 2.7-7.7 h. The greater the level of EC in the polymer solution, the slower the release rate of the drug from the microcapsules when the EC was not over the critical amount.     

对乙酰氨基酚/阿拉伯胶-壳聚糖多层微囊的制备及其体外释药研究

目的:制备对乙酰氨基酚多层微囊并考察其体外释药性能和机制。方法:以阿拉伯胶和壳聚糖为囊材,以戊二醛为交联剂,使用溶液干燥法(复合乳液法)制备载药(对乙酰氨基酚)多层(阿拉伯胶-壳聚糖-阿拉伯胶-壳聚糖)微囊。通过正交试验,以阿拉伯胶溶液-二氯甲烷体积比(A)、壳聚糖用量(B)、戊二醛-成壳材料总量比例(C)为因素,包封率为指标,优选制备工艺。通过测定其在盐酸溶液中的体外累积释药率并进行释放动力学模型拟合分析其释药机制。结果:最佳工艺条件为A4:3、B0.6g、C1:3。所制备的多层微囊球形完整、光滑,囊壁较厚;突释效果不明显,药物在12h内全部释放,其体外释药机制符合Ritger-Peppas模型。结论:所制载药多层微囊突释效应小、缓释效果较好。     

双嘧达莫中空微球的制备及评价

目的制备双嘧达莫中空微球,并对其进行初步评价。方法采用溶剂扩散-挥发法制备双嘧达莫中空微球,以外观、平均粒径、载药量及包封率为指标进行单因素考察优化处方,并对优化处方制备的中空微球进行体外漂浮及体外释放实验。结果双嘧达莫中空微球的最优处方及工艺为:乙基纤维素质量浓度为100 g.L-1、乙基纤维素与药物的质量比为5:1、乙醇与乙醚的体积比为4:l、乳化剂质量浓度为10 g.L-1、硬脂酸镁质量浓度为0.2 g.L-1,反应温度为30℃,搅拌速度为300 r.min-1。以最优处方制备的双嘧达莫中空微球,其载药量为11.57%,包封率为70.12%。该微球在人工胃液中12 h漂浮率可达94%,在人工胃液中12 h释放达80%,且无突释现象。结论双嘧达莫中空微球具有较理想的体外漂浮及缓释特性。     

双氯芬酸钠明胶微球的制备

目的：对双氯芬酸钠明胶微球的处方及制备工艺进行初步研究。方法：以生物降解材料明胶为载体,采用乳化交联法制备双氯芬酸钠明胶微球;单因素考察的基础上,利用正交实验设计筛选最佳处方和工艺;建立紫外分光光度法测定微囊中恩诺沙星的包封率和载药量的方法。结果：所制备的双氯芬酸钠明胶微球外形圆整,大小均匀,载药量为2.05%,包封率为37.67%。结论：获得较为满意的双氯芬酸钠明胶微球。     

Preparation and statistical optimization of alginate based stomach specific floating microcapsules of simvastatin

The present study involves preparation and characterization of floating microcapsules with simvastatin as model drug for prolongation of gastric residence time. The main objective is to improve solubility of simvastatin beta-CD complex (1:2) by co-precipitation method and then to deliver the same in sustained release dosage form. Sustained-release simvastatin microcapsules were prepared by the ionic gelation technique, using carbopol 941 as swellable floating polymer. A 3(3) full factorial design was used to study the effect of polymer concentration, drug complex and sodium alginate by plotting main effect plot and 3D surface plots. The formed microcapsules were subjected to various evaluation tests such as drug encapsulation efficiency, in vitro drug release and surface morphology by scanning electron microscopy. Powdered X-ray diffractometry and FTIR were used to investigate the complexation of simvastatin in the microcapsules. As the carbopol 941 is self swellable polymer, immediate floating was observed. The in vitro release studies and floating behavior were performed in HCI buffer of pH 1.2. The release profile and dissolution kinetic showed that drug release from the microcapsules follows zero order kinetics. It was concluded from the present investigation that porous carbopol 941 microcapsules are promising sustained release system as well as stomach specific carriers for delivery of simvastatin.