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目的:以纳米碳酸钙及脂质体作为药物包覆载体材料,制备淫羊藿苷碳酸钙纳米微球(ICA/CaCO_3)、淫羊藿苷固体纳米脂质体(ICA-SLN),并考察其提高淫羊藿苷(ICA)在大鼠体内生物利用度的作用。为ICA临床剂型的合理使用提供实验基础数据,奠定其进一步的开发基础。方法:分别采用恒温振摇装载法制备ICA/CaCO_3,超声乳化与高温熔融低温固化结合法制备ICA-SLN。并运用LC-MS-MS测定灌胃ICA、ICA/CaCO_3及ICA-SLN后ICA在大鼠体内不同时间点的血药浓度,采用DAS 2.1药动学软件对数据进行统计学处理。结果:通过LC-MS/MS测定血药浓度,DAS 2.1药动学软件计算统计后得到ICA组的半衰期与最大吸收浓度分别为(1.51±0.42)h、(82.9±12.37)ng/m L,ICA/CaCO_3组的半衰期与最大吸收浓度分别为(4.12±1.01)h、(51.1±31.35)ng/m L,ICA-SLN组的半衰期与最大吸收浓度分别为(2.15±0.39)h、(165±25.16)ng/m L。结论:ICA通过纳米碳酸钙及脂质体包附后与ICA原料药相比,ICA原料药在体内的生物利用度得到了进一步的提高。ICA/CaCO_3与ICA原料药相比,其体内的释放时间得到了一定的延迟。从促进口服药物体内吸收率方面,ICA-SLN较ICA原料药有了一定提高,同时也优于ICA/CaCO_3。实验表明ICA/CaCO_3可在一定程度上延缓ICA在大鼠体内的释放,ICA-SLN可在一定程度上提高ICA在大鼠体内的吸收率。
OBJECTIVE: To prepare icariin-loaded calcium carbonate nanoparticles (ICA / CaCO 3) and icariin solid nano-liposomes (ICA-SLN) by using nano calcium carbonate and liposomes as drug-coated carriers. It improves the bioavailability of icariin (ICA) in rats. Provide basic experimental data for the rational use of ICA clinical dosage forms and lay a foundation for its further development. Methods: ICA / CaCO_3 was prepared by constant temperature shaking loading method, and ICA-SLN was prepared by low temperature solidification combined with ultrasonic emulsification and high temperature melting. The plasma concentrations of ICA in rats at different time points after ICA, ICA / CaCO 3 and ICA-SLN were measured by LC-MS-MS. The data were statistically analyzed by DAS 2.1 pharmacokinetic software. Results: The plasma concentration was determined by LC-MS / MS. The half-life and the maximum absorption of ICA were (1.51 ± 0.42) h and (82.9 ± 12.37) ng / m L, The half-life and the maximum absorption of ICA / CaCO 3 were (4.12 ± 1.01) h and (51.1 ± 31.35) ng / m L, respectively. The half-life and the maximum absorption of ICA-SLN were (2.15 ± 0.39) ± 25.16) ng / m L. CONCLUSION: The bioavailability of ICA APIs in vivo has been further improved when ICA is packaged with nano-CaCO3 and liposomes compared with ICA APIs. ICA / CaCO_3 compared with ICA API, the body’s release time was a certain delay. ICA-SLN has shown some improvement over ICA APIs in promoting the in vivo absorption rate of oral drugs, and is also superior to ICA / CaCO 3. Experiments show that ICA / CaCO 3 can delay the release of ICA in rats to a certain extent, ICA-SLN can improve the absorption rate of ICA in rats to some extent.