浏览全部资源
扫码关注微信
1.成都中医药大学西南特色中药资源国家重点实验室,成都 611137
2.成都中医药大学药学院,成都 611137
Published:15 December 2023,
Received:25 August 2023,
Revised:09 October 2023,
扫 描 看 全 文
谢龙,赵雨芯,刘凯等.黄芩苷-甘草酸纳米晶的制备工艺优化及体外释放考察 Δ[J].中国药房,2023,34(23):2829-2834.
XIE Long,ZHAO Yuxin,LIU Kai,et al.Optimization of preparation technology and in vitro release of baicalin-glycyrrhizic acid solid nanocrystals[J].ZHONGGUO YAOFANG,2023,34(23):2829-2834.
谢龙,赵雨芯,刘凯等.黄芩苷-甘草酸纳米晶的制备工艺优化及体外释放考察 Δ[J].中国药房,2023,34(23):2829-2834. DOI: 10.6039/j.issn.1001-0408.2023.23.03.
XIE Long,ZHAO Yuxin,LIU Kai,et al.Optimization of preparation technology and in vitro release of baicalin-glycyrrhizic acid solid nanocrystals[J].ZHONGGUO YAOFANG,2023,34(23):2829-2834. DOI: 10.6039/j.issn.1001-0408.2023.23.03.
目的
2
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
2
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
2
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,1 000 r/min搅拌15 min,100 MPa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
2
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。
OBJECTIVE
2
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
2
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
2
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
2
BCN-GA-SN is prepared successfully in this study with uniform particle size and even distribution, which can effectively improve the dissolution of BCN.
黄芩-甘草药对黄芩苷甘草酸纳米晶体外释放
baicalinglycyrrhizic acidnanocrystalsin vitro release
ZHAO T T,TANG H L,XIE L,et al. Scutellaria baicalensis Georgi. (Lamiaceae):a review of its traditional uses,botany,phytochemistry,pharmacology and toxicology[J]. J Pharm Pharmacol,2019,71(9):1353-1369.
SHEN C Y,SHEN B D,ZHU J J,et al. Glycyrrhizic acid-based self-assembled micelles for improving oral bioavaila- bility of paeoniflorin[J]. Drug Dev Ind Pharm,2021,47(2):207-214.
吕志阳,单聪,杨雨微,等. 经方中黄芩-甘草不同配伍比例对黄芩苷溶出的影响[J]. 亚太传统医药,2019,15(10):67-69.
LYU Z Y,SHAN C,YANG Y W,et al. Effect of baicalin in licorice by different compatibility proportions of Scutellariae Radix and Glycyrrhizae Radix[J]. Asia Pac Tradit Med,2019,15(10):67-69.
刘柳毅,温璐平,许男徽,等. 灯盏花素纳米晶的制备及质量评价[J]. 中国药房,2020,31(15):1861-1867.
LIU L Y,WEN L P,XU N H,et al. Preparation and quality evaluation of breviscapine nanocrystals[J]. China Pharm,2020,31(15):1861-1867.
NAGARWAL R C,KUMAR R,DHANAWAT M,et al. Nanocrystal technology in the delivery of poorly soluble drugs:an overview[J]. Curr Drug Deliv,2011,8(4):398-406.
刘罗娜,李小芳,仲粒,等. 以甘草酸为稳定剂制备黄芩苷固体纳米晶体[J]. 中草药,2019,50(9):2057-2064.
LIU L N,LI X F,ZHONG L,et al. Preparation of baicalin solid nanocrystal using glycyrrhizic acid as a natural stabilizer[J]. Chin Tradit Herb Drugs,2019,50(9):2057-2064.
国家药典委员会. 中华人民共和国药典:一部[M]. 2020年版.北京:中国医药科技出版社,2020:88-89,314-316.
Chinese Pharmacopoeia Commission. Chinese pharmacopoeia:volume Ⅰ[M]. 2020 edition. Beijing:China Medical Science and Technology Press,2020:88-89,314-316.
樊俐慧,张伟,孙静,等. 《伤寒杂病论》中黄芩的量效关系及用药规律[J]. 中成药,2021,43(4):1015-1017.
FAN L H,ZHANG W,SUN J,et al. Dose-effect relationship and medication law of Scutellaria baicalensis Georgi in Treatise on Febrile Diseases[J]. Chin Tradit Pat Med,2021,43(4):1015-1017.
刘楚妤,赵琰,屈会化. 经方中黄芩应用规律探讨[J]. 辽宁中医药大学学报,2021,23(12):139-143.
LIU C Y,ZHAO Y,QU H H. Discussion on the application rules of Scutellariae Radix in the classical prescriptions[J]. J Liaoning Univ Tradit Chin Med,2021,23(12):139-143.
0
Views
16
下载量
0
CSCD
Publicity Resources
Related Articles
Related Author
Related Institution