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苦参碱固体分散体的制备及体外溶出研究OA

Preparation and in vitro dissolution of matrine amorphous solid dispersion

中文摘要英文摘要

为提高苦参碱(matrine,MAT)的缓释性能,延长体外释药时间,本研究以苦参碱为目标药物,以乙基纤维素(EC)为载体,利用球磨法制备苦参碱无定形固体分散体(MAT-ASD),通过粉末X射线衍射(PXRD)、差示扫描量热(DSC)、傅里叶红外光谱(FT-IR)对其进行表征,并考察其体外释放特性.结果显示,利用该方法成功制备了MAT-ASD(药物与载体比例为1∶9),粉末X射线衍射中无苦参碱的晶体特征峰,差示扫描量热分析显示无苦参碱晶体吸热峰,傅里叶红外光谱扫描显示苦参碱与乙基纤维素之间存在相互作用,可能产生了分子间氢键.体外溶出结果显示,在0.25 h内苦参碱的累积溶出率几乎达100%,而MAT-ASD的累积溶出率仅为56.29%,在6h时MAT-ASD的累积溶出率为95.22%.结果提示,以乙基纤维素为载体,利用球磨法可成功制备MAT-ASD,并可有效延长苦参碱的体外释药性能,为苦参碱缓释制剂的开发奠定了基础.

The purpose was to improve sustained-release performance of matrine(MAT)and prolong the release time in vitro.In this study,matrine amorphous solid dispersion(MAT-ASD)was prepared by ball milling method with MAT as the target drug and ethyl cellulose(EC)as the carrier,and was characterized by powder X-ray diffraction(PXRD),differential scanning calorimetry(DSC)and Fourier transform infrared spectroscopy(FT-IR),so as to investigate its release characteristics in vitro.The results showed that MAT-ASD was successfully prepared using this method(the ratio of drug to carrier was 1∶9).There were no crystal characteristic peaks of matrine in PXRD,and no crystal endothermic peak of matrine in DSC,and FT-IR showed that there was an interaction between matrine and EC,which may have resulted in intermolecular hydrogen bonds.The results of in vitro dissolution showed that the cumulative dissolution rate of MAT reached almost 100%within 0.25 h,while the cumulative dissolution rate of MAT-ASD was only 56.29%.At 6 h,the cumulative dissolution rate of MAT-ASD was 95.22%.The results showed that MAT-ASD was successful prepared by ball milling with EC as the carrier,which could effectively prolong the in vitro release time of matrine and lay a foundation for the development of matrine sustained release preparations.

张静茹;路晨月;师鑫潮;何欣

河北农业大学中兽医学院,河北保定 071000

畜牧业

苦参碱;固体分散体;球磨法;缓释;累积溶出率

matrine;solid dispersion;ball milling;slow release;cumulative dissolution rate

《中兽医医药杂志》 2024 (003)

28-32 / 5

河北省自然科学基金资助项目(C2022204215)

10.13823/j.cnki.jtcvm.2024.040

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