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黄芩苷-甘草酸纳米晶的制备工艺优化及体外释放考察
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| 篇名： | 黄芩苷-甘草酸纳米晶的制备工艺优化及体外释放考察 |
| TITLE： | Optimization of preparation technology and in vitro release of baicalin-glycyrrhizic acid solid nanocrystals |
| 摘要： | 目的 优化黄芩苷（BCN）-甘草酸（GA）纳米晶（BCN-GA-SN）的制备工艺，并进行表征和体外释放考察。方法根据经典药对“黄芩-甘草”配伍比例，固定BCN和GA的配伍比例为6∶1（m/m），采用沉淀法结合高压均质法制备BCN-GA纳米混悬液。以平均粒径、多分散性指数（PDI）为评价指标，以稳定剂的种类及用量、搅拌转速和时间、高压均质压力和次数为考察因素，优化BCN-GA纳米混悬液制备工艺；再以平均粒径、PDI、再分散系数（RDI）为评价指标，以冻干保护剂种类和用量为考察因素，优化BCN-GA纳米混悬液的冻干固化工艺，进而制备BCN-GA-SN；然后对BCN-GA-SN的理化性质表征和体外释放进行考察。结果BCN-GA-SN的最优制备工艺为：先以15%十二烷基硫酸钠为稳定剂，1000r/min搅拌15min，100MPa高压均质20次制备BCN-GA纳米混悬液；再以5%甘露醇（相对于BCN的用量）冻干固化。所制得的BCN-GA-SN的平均粒径为（442.2±5.7）nm，PDI为0.225±0.015，RDI为1.055±0.013，呈不规则球形，大小较为均匀；该纳米晶中BCN的载药量为（62.5±0.7）%，GA的载药量为（9.4±0.2）%；体外释放结果表明，BCN-GA-SN的累积溶出度均高于BCN、GA的物理混合物。结论本研究成功制备了BCN-GA-SN，其粒径大小均一、分布均匀，可有效提高BCN的体外溶出度。 |
| ABSTRACT： | OBJECTIVE To optimize the preparation technology of baicalin （BCN）-glycyrrhizic acid （GA） solid nanocrystals （BCN-GA-SN）， to characterize them and investigate their in vitro release characteristics. METHODS According to the compatibility ratio of classic couplet medicinals “Scutellaria baicalensis-Glycyrrhiza uralensis”， the compatibility ratio of BCN and GA was determined as 6∶1 （m/m）； BCN-GA nanosuspension was prepared by precipitation method combined with high-pressure homogenization method. The preparation technology of BCN-GA nanosuspension was optimized by using mean particle size and polydispersity index （PDI） as indexes and with types and dosage of stabilizers， stirring speed and time， high-pressure homogenization pressure and frequency as factors. The freeze-dried consolidation process of BCN-GA nanosuspension was optimized to prepare BCN-GA-SN using average particle size， PDI and redispersibility index （RDI） as indicators， with the type and dosage of freeze-dried protective agents as factors； then， the physicochemical properties and in vitro release of BCN-GA-SN were investigated. RESULTS The optimal preparation technology of BCN-GA-SN was as follows： BCN-GA nanosuspension was prepared by using 15% sodium dodecyl sulfate as a stabilizer， stirring at 1 000 r/min for 15 minutes， and homogenizing at 100 MPa for 20 times； then， BCN-GA nanosuspension was freeze-dried and solidified with 5% mannitol （corresponding to the dosage of BCN）. The average particle size of prepared BCN-GA-SN was （442.2±5.7） nm with PDI of 0.225±0.015 and RDI of 1.055± 0.013. The prepared BCN-GA-SN presented as the irregularly spherical shape with more uniform size； the drug-loading amount of BCN in the nanocrystal was （62.5±0.7）%， and that of GA was （9.4±0.2）%； the in vitro release results showed that the cumulative dissolution of BCN-GA-SN was higher than that of the physical mixture of BCN and GA. CONCLUSIONS BCN-GA-SN is prepared successfully in this study with uniform particle size and even distribution， which can effectively improve the dissolution of BCN. |
| 期刊： | 2023年第34卷第23期 |
| 作者： | 谢龙；赵雨芯；刘凯；古环；李小芳 |
| AUTHORS： | XIE Long，ZHAO Yuxin，LIU Kai，GU Huan，LI Xiaofang |
| 关键字： | 黄芩-甘草药对；黄芩苷；甘草酸；纳米晶；体外释放 |
| KEYWORDS： | couplet medicinals of Scutellaria baicalensis-Glycyrrhiza uralensis； baicalin； glycyrrhizic acid； nanocrystals； in |
| 阅读数： | 58 次 |
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