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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Preparation and in vitro evaluation of propylthiouracil microspheres made of Eudragit RL 100 and cellulose acetate butyrate polymers using the emulsion-solvent evaporation method
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Preparation and in vitro evaluation of propylthiouracil microspheres made of Eudragit RL 100 and cellulose acetate butyrate polymers using the emulsion-solvent evaporation method

机译:用乳液-溶剂蒸发法制备Eudragit RL 100和醋酸丁酸纤维素聚合物制成的丙基硫氧嘧啶微球并进行体外评估

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摘要

The objectives of this investigation are to evaluate the encapsulation efficiency of the anti-thyroid agent 6-n-propyl-2-thiouracil using two polymers of different characteristics (cellulose acetate butyrate polymer,(CAB-551-0.01) and ammonio methacrylate copolymer (Eudragit RL 100) and to study the effect of this encapsulation on the drug release properties.Polymers were used separately and in combination to prepare different microspheres.Also,the effect of polymer solution phase viscosity was studied for each of the polymers and for their combinations.An Ostwald viscometer was used to evaluate the relative viscosities of polymer solution phases and their combinations.Microspheres with 25% theoretical drug loading of 6-n-propyl-2-thiouracil core material were prepared by the emulsion solvent evaporation method.Microspheres prepared from CAB-551-0.01,which has higher relative polymer phase viscosity than Eudragit RL 100,showed significantly lower drug release rates and a noticeable lag time.Polymer combinations of CAB-551-0.01 and Eudragit RL 100 (1:1) showed an interesting synergistic increase in relative polymer solution viscosities at all concentrations.Unlike microspheres prepared from the two polymers separately which follow Higuchi spherical matrix release kinetics,microspheres prepared using a combination (1:1) of the two polymers showed near zero order with faster rates compared to those prepared using CAB-551-0.01 equivalent polymer concentrations.The results of this study suggest that 6-n-propyl-2-thiouracil was successfully and efficiently encapsulated and release rates of matrix microspheres are related to polymer solution phase viscosity,but when polymer combinations were used other factors such as structural effects must be considered.
机译:这项研究的目的是使用两种不同特性的聚合物(醋酸丁酸纤维素聚合物,(CAB-551-0.01)和甲基丙烯酸铵共聚物(),评估抗甲状腺药6-正丙基-2-硫尿嘧啶的包封效率。 Eudragit RL 100),并研究这种封装对药物释放特性的影响。分别单独或组合使用聚合物制备不同的微球。此外,还研究了每种聚合物及其组合的聚合物溶液相粘度的影响。用奥斯特瓦尔德粘度计评估聚合物溶液相及其组合的相对粘度。通过乳液溶剂蒸发法制备理论药物载量为25%的6-正丙基-2-硫尿嘧啶核心材料的微球。 CAB-551-0.01的相对聚合物相粘度比Eudragit RL 100高,显示出较低的药物释放速率和明显的滞后CAB-551-0.01和Eudragit RL 100(1:1)的聚合物组合在所有浓度下均表现出令人感兴趣的协同增高的相对聚合物溶液粘度。与分别由两种聚合物制得的遵循Higuchi球形基质释放动力学的微球不同,微球与使用CAB-551-0.01等效聚合物浓度制备的聚合物相比,使用两种聚合物的组合(1:1)制备的聚合物显示出接近零级的速率更快。聚合物被成功有效地包封,基质微球的释放速率与聚合物溶液相的粘度有关,但是当使用聚合物组合时,必须考虑其他因素,例如结构效应。

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