Development of theophylline floating microballoons using cellulose acetate butyrate and/or Eudragit RL 100 polymers with different permeability characteristics
Development of theophylline floating microballoons using cellulose acetate butyrate and/or Eudragit RL 100 polymers with different permeability characteristics
复制标题
使用具有不同渗透特性的醋酸丁酸纤维素和/或 Eudragit RL 100 聚合物开发茶碱漂浮微球
DOI：
--
复制
发表时间：
2010
影响因子：
2.1
通讯作者：
H. Nemati
中科院分区：
文献类型：
--
作者：
M. Jelvehgari;M. Maghsoodi;H. Nemati
本研究的目的是设计一种缓释漂浮微囊茶碱使用两种聚合物的不同渗透特性; Eudragit RL 100（Eu RL）和醋酸丁酸纤维素（CAB）使用油包油乳液溶剂蒸发法。聚合物单独使用和组合使用以制备不同的微胶囊。研究了每种聚合物及其组合的药物-聚合物相互作用的影响。对微球的包封率、产率、粒径、漂浮性、形貌、粉末X射线衍射分析（XRD）和差示扫描量热法（DSC）进行了评价。在PH 1.2和7.4下进行体外释放研究。EuRL和CAB的最佳药物与聚合物的比例分别为4：1（F2）和0.75：1（F '2）。混合制剂中药物与聚合物的最佳比例为4：1：1（茶碱：Eu RL：CAB比例）。发现F2和F '2的产率、装载效率和粒度分别为59.14%和45.39%、73.93%和95.87%、372和273微米。CAB法制备的微球在0.1M盐酸中的漂浮能力最好，可达80.3 ± 4.02%。XRD和DSC结果表明，载药微球中茶碱稳定，呈结晶状。使用Eu RL和CAB聚合物的共混物制备的微粒显示比商业片剂更持久的模式（P<0.05）。结果表明，Eu RL与CAB以1：1的比例混合制备的载药漂浮微球，其聚合物含量较低，是一种适合茶碱缓释的载药系统。
The objective of the present investigation was to design a sustained release floating microcapsules of theophylline using two polymers of different permeability characteristics; Eudragit RL 100 (Eu RL) and cellulose acetate butyrate (CAB) using the oil-in-oil emulsion solvent evaporation method. Polymers were used separately and in combination to prepare different microcapsules. The effect of drug-polymer interaction was studied for each of the polymers and for their combination. Encapsulation efficiency, the yield, particle size, floating capability, morphology of microspheres, powder X-ray diffraction analysis (XRD), and differential scanning calorimetry (DSC) were evaluated. The in vitro release studies were performed in PH 1.2 and 7.4. The optimized drug to polymer ratios was found to be 4:1 (F2) and 0.75:1 (F'2) with Eu RL and CAB, respectively. The best drug to polymer ratio in mix formulation was 4:1:1 (theophylline: Eu RL: CAB ratio). Production yield, loading efficiencies, and particle size of F2 and F’2 were found to be 59.14% and 45.39%, 73.93% and 95.87%, 372 and 273 micron, respectively. Microsphere prepared with CAB showed the best floating ability (80.3 ± 4.02% buoyancy) in 0.1 M HCl for over 12 h. The XRD and DSC showed that theophylline in the drug loaded microspheres was stable and in crystaline form. Microparticles prepared using blend of Eu RL and CAB polymers indicated more sustained pattern than the commercial tablet (P<0.05). Drug loaded floating microballoons prepared of combination of Eu RL and CAB with 1:1 ratio were found to be a suitable delivery system for sustained release delivery of theophylline which contained lower amount of polymer contents in the microspheres.