毛蕊异黄酮-磷脂复合物的处方研究

doi:10.19640/j.cnki.jtau.2019.04.016

Journal of Tianjin Agricultural University ›› 2019, Vol. 26 ›› Issue (4): 77-82.doi: 10.19640/j.cnki.jtau.2019.04.016

• Researches and Scientific Notes • Previous Articles Next Articles

Formulation optimization of calycosin phospholipid complex

SHI Zhuo-qi^a, LIU Li-yao^{a, b, Corresponding Author}, XIONG Qian^a, WANG Qing-kui^b

Tianjin Agricultural University, a. Department of Biopharmaceuticals, College of Basic Science; b. Tianjin Key Lab of Aquatic Ecology and Aquaculture, Tianjin 300384, China

Received:2019-01-13 Published:2020-01-19

Abstract

Abstract: ：Calycosin is an active substance extracted and separated from Astragalus membranaceus. It could combine with estrogen receptor and generate estrogen-like action, antitumor and immunoregulation effect. However, because of its poor lipophilicity, it is difficult to be utilized in medical preparation. And its in vivo bioavailability is usually extremely low. This study was designed to increase the lipophilicity of calycosin using phospholipid complexation technology. In this study, associative efficiency（AE）was set as screening parameter and optimal formulation of calycosin phospholipid complex was obtained using solvent evaporation method based on single factor screening and orthogonal design. Under the selected formulation, mass ratio of calycosin to phospholipid was 1∶5 and composite time was 60 minutes in ethanol of pH 6.0. For the selected formulation, AE of calycosin phospholipid complex could reach 90% and storage stability remained in 3 months under 4 ℃. Compared with calycosin material medicine, the lipophilicity of phospholipid complex was increased by 600 times, which provides the basis for practical application.

Key words: calycosin, phospholipid complex, orthogonal screening, formulation optimization

CLC Number:

SHI Zhuo-qi, LIU Li-yao, XIONG Qian, WANG Qing-kui. Formulation optimization of calycosin phospholipid complex[J]. Journal of Tianjin Agricultural University, 2019, 26(4): 77-82.

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References

[1] 于玲,王知斌,王秋红,等. 黄芪中黄酮类化合物药理作用研究进展[J]. 中医药信息,2018,35(2):104-108.
[2] 梁小银,严萍,詹若挺,等. 新胃乃安片中4种异黄酮成分的同时鉴别及抗氧化活性的初步筛选[J]. 湖南中医杂志,2018,34(7):186-187,206.
[3] 张亚洲,徐风,梁静. 蒙古黄芪中异黄酮类化学成分研究[J]. 中国中药杂志,2012,37(21):3243-3248.
[4] 张冬青,王海宝,王淑芳,等. 毛蕊异黄酮生物活性的研究进展[J]. 中国中药杂志,2015,40(22):4339-4345.
[5] 邝洁容,陈伯丛,梁晓燕. 毛蕊异黄酮葡萄糖苷自微乳给药系统的制备及质量控制[J]. 中国医院用药评价与分析,2017,17(7):885-888.
[6] 李楠,冯玲玲,蒋学华,等. 黄芩苷磷脂复合物大鼠在体胃肠道吸收研究[J]. 中国药学杂志,2016,51(12):994-998.
[7] 王梦姝,吕晓玲,赵焕焦,等. 黑米花色苷磷脂复合物的制备及生物利用度[J]. 食品科技,2017(5):242-245.
[8] 郑林. 磷脂复合物对中药制剂口服吸收的影响[J]. 中国抗生素杂志,2015,40(6):468-473.
[9] 张冬青,王海宝,王淑芳,等. 毛蕊异黄酮生物活性的研究进展[J]. 中国中药杂志,2015,40(22):4339-4345.
[10] Shi C,Tong Q,Fang J,et al.Preparation,characterization and in vivo studies of amorphous solid dispersion of berberine with hydrogenated phosphatidylcholine[J]. European Journal of Pharmaceutical Sciences,2015,74:11-17.
[11] Cui F,Shi K,Zhang L Q,et al.Biodegradable nanoparticles loaded with insulin-phospholipid complex for oral delivery:Preparation,in vitro characterization and in vivo evaluation[J]. Journal of Controlled Release,2006, 114(2):242-250.
[12] 余凤玮,聂绩,袁野. 穿心莲内酯磷脂复合物的制备及表征[J]. 中国药房,2016,27(10):1409-1411.
[13] 张红敏,李琬晴,高静,等. 羟基喜树碱-磷脂复合物的制备、表征及细胞毒性评价[J]. 国际药学研究杂志,2017,44(7):714-721.
[14] 张文华,张芳,王汉卿,等. 甘草黄酮磷脂复合物制备工艺研究[J]. 药学研究,2017,36(8):457-459,476.
[15] 孙静,史亚军,张小飞,等. 丹参片提取物磷脂复合物的制备及初步吸收评价[J]. 中药材,2017,40(1):164-166.

Formulation optimization of calycosin phospholipid complex

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