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首页> 美国卫生研究院文献>AAPS PharmSciTech >Formulation and Development of Extended-Release Micro Particulate Drug Delivery System of Solubilized Rifaximin
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Formulation and Development of Extended-Release Micro Particulate Drug Delivery System of Solubilized Rifaximin

机译：溶解性利福昔明延长释放微颗粒药物递送系统的研制与开发

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摘要

Rifaximin (RFX), a semi-synthetic antibiotic belonging to BCS class IV category, has been used in the treatment of traveler’s diarrhea. An attempt has been made to improve aqueous solubility of RFX in the presence of β-cyclodextrin (β-CD) and hydroxy propyl β-cyclodextrin (HP-β-CD) and control its release in the gut by enteric coating. The stoichiometric proportion of RFX and complexing agent’s β-CD and HP-β-CD were determined by phase solubility studies. RFX–β-CD and RFX–HP-β-CD were prepared in 1:2 ratio by solvent evaporation technique using rota-evaporator with yield of 78% and 84% respectively followed by their evaluation using different techniques such as saturation solubility, Fourier transform infrared, differential scanning calorimeter, powder X-ray diffractometer, in vitro antimicrobial activity. The saturation solubility of RFX had improved from 0.0736 mg/ml to 0.2354 mg/ml and 0.5681 mg/ml in presence of β-CD and HP-β-CD respectively resulting in an increased zone of inhibition in the later complex during antimicrobial studies. The RFX–HP-β-CD complex particles were coated with eudragit L 100 (EL 100) by spray drying technique. The 32 factorial design was applied to formulate the micro particles. All formulations exhibited pH dependant drug release. The % EE was 69% and the release of RFX was retarded by enteric coating in the optimized batch FB2. Therefore, it can be concluded that solubility of some BCS class IV drugs can be improved by β-CD complexation and release of such inclusion complexes can be retarded to increase the residence time of RFX in the gastrointestinal tract.
机译：利福昔明（RFX）是BCS IV类的半合成抗生素，已用于治疗旅行者的腹泻。已经尝试在存在β-环糊精（β-CD）和羟丙基β-环糊精（HP-β-CD）的情况下改善RFX的水溶性并通过肠溶衣控制其在肠中的释放。通过相溶解度研究确定了RFX和络合剂的β-CD和HP-β-CD的化学计量比。使用旋转蒸发仪通过溶剂蒸发技术以1：2的比例制备RFX-β-CD和RFX-HP-β-CD，产率分别为78％和84％，然后使用饱和溶解度，傅立叶等不同技术进行评估变换红外，差示扫描量热仪，粉末X射线衍射仪，体外抗菌活性。在存在β-CD和HP-β-CD的情况下，RFX的饱和溶解度分别从0.0736 mg / ml提高至0.2354 mg / ml和0.5681 mg / ml，从而在抗菌研究期间增加了对后者复合物的抑制范围。 RFX-HP-β-CD复合颗粒通过喷雾干燥技术涂有eudragit L 100（EL 100）。采用3 2 析因设计来制备微粒。所有制剂均表现出pH依赖性药物释放。 EE的百分比为69％，并且在优化的批FB2中肠溶衣抑制了RFX的释放。因此，可以得出结论，某些BCS IV类药物的溶解度可以通过β-CD络合得到改善，并且可以抑制此类包合物的释放，从而延长RFX在胃肠道中的停留时间。

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