银杏内酯固体分散体的辅料优选

马颖; 吕志阳; 狄留庆; 李俊松; 康安

银杏内酯固体分散体的辅料优选

马颖¹,
吕志阳²,
狄留庆^1,3,,
李俊松^1,3,
康安¹

1.
南京中医药大学药学院，江苏南京 210023
2.
南京中医药大学翰林学院，江苏泰州 225300
3.
江苏省中药高效给药系统工程技术研究中心，江苏南京 210023

计量
- 文章访问数: 1061
- HTML全文浏览量: 3
- PDF下载量: 1263
- 被引次数: 0
出版历程
- 收稿日期: 2014-11-18
- 修回日期: 2015-01-26
- 刊出日期: 2015-03-10

The Choice of Preferred Materials of Ginkgolide Solid Dispersions

MAYing¹,
LYUZhi-yang²,
DILiu-qing^{1,3
,},
LIJun-song^1,3,
KANGAn¹

1.
College of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, 210023, China
2.
Hanlin College, Nanjing University of Chinese Medicine, Taizhou, 225300, China
3.
Jiangsu Engineering Research Center for Efficient Delivery System of TCM, Nanjing, 210023, China

摘要

摘要: 目的通过优选最佳辅料及配比来制备银杏内酯固体分散体，以提高银杏内酯体外溶出度。方法选取聚丙烯酸树脂EPO(Eudragit EPO)、聚维酮K30(PVP K30)分别与银杏内酯以不同配比运用溶剂法制备固体分散体，测定银杏内酯B(ginkgolide B，GB)溶出度，并用差示扫描量热（DSC）、X-射线衍射（X-RD）、扫描电镜（SEM）进行物相表征。结果以银杏内酯/EPO配比为1∶2、1∶4、1∶6、1∶8制备的固体分散体5 min内GB溶出度分别为65%、68%、70%、71%；银杏内酯/PVP K30在相应配比下制备的固体分散体5 min内GB溶出度分别为40%、50%、66%、70%，而5 min内原料药溶出度为10%。物相鉴别结果表明银杏内酯在2种载体制备的固体分散体中均以无定型状态均匀分散。结论以银杏内酯/EPO配比为1∶2制备的固体分散体载药量高、溶出效果佳，是制备银杏内酯固体分散体的最佳选择，具有较好的应用前景。
- 银杏内酯 /
- 固体分散体 /
- 溶出度 /
- 优选辅料
Abstract: OBJECTIVE Choosing the optimizing assistance materials and the best proportional to make the solid dispersion of Ginkgolides， which so that can tremendously improve the dissolution rate of Ginkgolides. METHODS We determine the dissolution rate of the solid dispersion respectively， which are made by Eudragit EPO and PVP K30 in different drug-material ratio. In addition， quantitative phase determination of them are measured by DSC， X-RD and SEM. RESULTS The dissolution rate of the solid dispersion with the Ginkgolides -EPO ratio in 1∶2， 1∶4， 1∶6， 1∶8 were 65%， 68%， 70% and 71% respectively in five minutes. In the corresponding proportion， The dissolution rate of the solid dispersion made by PVP K30 were 40%， 50%， 66%， 70% respectively. In the same time， the dissolution rate of the drug substance were 10%. Phase identification results showed that Ginkgolides can evenly dispers in amorphous state in the solid dispersion. CONCLUSION The solid dispersion with the Ginkgolides -EPO ratio of 1∶2 is the best choice to preparation， which has the tremendous drug-loading and dissolution efficiency， thereby having a excellent prospect of application.
- Ginkgolides /
- solid dispersion /
- dissolution rate /
- optimization assistance materials

HTML全文

参考文献(15)

[1]	陈维军，谢笔钧，胡慰望．银杏萜内酯的化学结构及药理作用研究进展[J]．中国药学杂志，1998（9）：6-9．
[2]	Chen WJ， Xie BJ， Hu WW. The chemical compositions and medicinal virtues of Ginkgo Biloba Terpene Lactones[J]. Chin Pharm J， 1998(9): 6-9.
[3]	马琳怡，韩丽妹，张志荣，等．银杏内酯固体分散体的制备和体外特性研究[J]．中国中药杂志，2009（11）：1368-1372．
[4]	Ma LY， Han LM， Zhang ZR， et al.Preparation and characterization of solid dispersions of ginkgolides[J]. China J Chin Mater Med， 2009(11): 1368-1372.
[5]	蒋艳荣，张振海，夏海建，等．基于共聚维酮的丹参酮Ⅱ_A固体分散体的研究[J]．中国中药杂志，2013（2）：174-178．
[6]	Jiang YR， Zhang ZH， Xia HJ， et al. Study on solid dispersion of copovidone-based tanshinone II_A[J]. China J Chin Mater Med， 2013(2): 174-178.
[7]	〖JP2〗Moustafine RI， Bobyleva VL， Bukhovets AV， et al. Structural transformations during swelling of polycomplex matrices based on countercharged (meth)acrylate copolymers (EudragitR EPO/EudragitR L 100-55)[J]. J Pharm Sci， 2011， 100(3): 874-885.〖JP〗
[8]	Lv H， Wang GJ， Wu XL， et al. Transport characteristics of ginkgolide B by Caco-2 cells and examination of ginkgolide B oral absorption potential using rat in situ intestinal loop method[J]. Int J Pharm， 2008， 351(1/2): 31-35.
[9]	〖JP2〗Onoue S， Kojo Y， Aoki Y， et al. Physicochemical and pharmacokinetic characterization of amorphous solid dispersion of tranilast with enhanced solubility in gastric fluid and improved oral bioavailability[J]. Drug Metab Pharmacokinet， 2012， 27(4): 379-387.〖JP〗
[10]	Huang SH， Lewis TM， Lummis SC， et al. Mixed antagonistic effects of the ginkgolides at recombinant human rho1 GABAC receptors[J]. Neuropharmacology， 2012， 63(6): 1127-1139.
[11]	Jensen AA， Bergmann ML， Sander T， et al. Ginkgolide X is a potent antagonist of anionic cys-loop receptors with a unique selectivity profile at glycine receptors[J]. J Biol Chem， 2010， 285(13): 10141-10153.
[12]	Van Beek TA. Ginkgolides and bilobalide: Their physical， chromatographic and spectroscopic properties[J]. Bioorg Med Chem， 2005， 13(17): 5001-5012.
[13]	Prasad D， Chauhan H， Atef E. Amorphous stabilization and dissolution enhancement of amorphous ternary solid dispersions: combination of polymers showing drug-polymer interaction for synergistic effects[J]. J Pharm Sci， 2014，103(11)：3511-3523.
[14]	〖JP2〗Wegiel LA， Mauer LJ， Edgar KJ， et al. Mid-infrared spectroscopy as a polymer selection tool for formulating amorphous solid dispersions[J]. J Pharm Pharmacol， 2014， 66(2):244-255.〖JP〗
[15]	Wegiel LA， Mauer LJ， Edgar KJ， et al. Crystallization of amorphous solid dispersions of resveratrol during preparation and storage-Impact of different polymers[J]. J Pharm Sci， 2013， 102(1): 171-184.