布洛芬-β-CD包含物: 制备、性质、物理化学特性及体外溶出研究

布洛芬-β-CD包含物: 制备、性质、物理化学特性及体外溶出研究

马吉德, 朱家壁

1. 巴基斯坦戈马尔大学药学院 Dera Ismail Khan, N.W.F.P;
2. 中昆药剂研究所, 中国药科大学, 南京 210009

收稿日期:1997-06-24 修回日期:1998-01-08 出版日期:1998-06-15 发布日期:1998-06-15

Ibuprofen-β-cyclodextrin Inclusion Complex: Preparation, Characterization, Physico-Chemical Properties and In vitro Dissolution Behavior

Gul Majid Khan, Jia-Bi Zhu

1. Faculty of Pharmacy, Gomal University, Dera Ismail Khan, N.W.F.P., Pakistan;
2. Zhong Kun Pharmaceutical Research Institute, School of Pharmacy, China Pharmaceutical University, Nanjing 210009

Received:1997-06-24 Revised:1998-01-08 Online:1998-06-15 Published:1998-06-15

摘要/Abstract

摘要： 本文对布洛芬(IBF)和-β-CD包合物的性质进行了研究。相溶试验表明在室温23 ºC及37 ºC下包合物中IBF和-β-CD的比例分别为1:3及2:3。本文采用均匀共沉淀法制备了固体包合物, 并采用了扫描电镜、差热扫描、红外光谱及X线衍射来考察包合物的性质。包合物的溶解度及溶出速度较之它们的物理混合物及药物本身有了明显的提高, 由此表明β-CD在布洛芬的溶解性中发挥了重要作用。

关键词: 布洛芬, β-CD, 包合物, 溶解度, 体外溶出速度

Abstract: Inclusion complexation between ibuprofen (IBF) and β cyclodextrin (β-CD) was investigated. Phase solubility studies of the complexation suggested the formation of a 1:3 complex and a 2:3 complex between IBF and β-CD at room temperature (23 ºC) and at 37 ºC respectively. Solid inclusion complexes were prepared by the homogeneous coprecipitation method. Scanning electron microscopy, differential scanning calorimetry, IR spectroscopy, and Xray diffractometry were used for the characterization and evaluation of the complexes. The solubility and dissolution rate of the complexes formed were found to have improved considerably over that of the physical mixture and the drug alone, indicating that β-cyclodextrin played an important role in the solubilization of ibuprofen.

Key words: Ibuprofen, β-Cyclodextrin, Inclusion complexation, Solubility, In vitro dissolution rate

Supporting:

马吉德, 朱家壁. 布洛芬-β-CD包含物: 制备、性质、物理化学特性及体外溶出研究[J]. .

Gul Majid Khan, Jia-Bi Zhu . Ibuprofen-β-cyclodextrin Inclusion Complex: Preparation, Characterization, Physico-Chemical Properties and In vitro Dissolution Behavior[J]. .

参考文献

[1] Martin A, Swarbrick J, Cammarata A. Physical Pharmacy, 3rd ed., Lea & Febiger, Philadelphia, 1983: 272.
[2] Repta AJ, Shafter E. In : Yalkovsky SH, ed. Techniques of Solubilization of Drugs, Dekkar, New York, 1981: 135, 159.
[3] Lofts T, Guomundsdottir TK, Frioriksdottir H. Drug Dev Ind Pharm, 1996, 22: 401.
[4] Szejtli J. In: Samolen VF, Ball L, Willey A. eds. Cont rolled Drug Bioavailability . Vol. 3, Inter Science Publications, 1985: 365.
[5] Sanghavi NM, Choudri KB, Matharu RS, et al. Drug Dev Ind Pharm, 1993, 19: 701.
[6] Labendera JT, Lopez ME, Penin LS, et al. J Pharm Biopharm, 1993, 39: 225.
[7] Pitha J, Szente L, Szejtli J. Molecular Encapsulation of Drugs by CDs and Congeners. In: Bruck SD, Controlled Drug Delivery, Vol. 1. Basic Concepts. CRC Press Inc, Boca Raton, 1983: 125.
[8] Jones SP, Grand DW, Parr GD. Acta Pharm Tecnol, 1984, 30: 213.
[9] Loftsson T, Olafsdottir BJ. Int J Pharm, 1985, 66: 289.
[10] Puglisi G, Santagati NA, Ventura CA, et al. J Pharm Pharmacol, 1991, 43: 430.
[11] Duchene D, Glomot F, Vaution C. In: Duchene D and Desante, eds. Cyclodext rins and Their Industrial Uses. Paris, 1987: 6.
[12] Duchene D, Vaution C, Glomot F. Amelioration de la Dissolution et de la Biodisponibilitides Principles Actifs par Inclusion dans les CDs, S TP Pharma, 19852b : 1, 323.
[13] Duchene D, Debrueres B, Vaution C. Improvement of Drug Stability by Cyclodextrin Inclusion Complexation, STP Pharma, 19852a : 1, 37.
[14] Higuchi T, Conners KA. Phase Solubility Techniques. A dv A nal Chem Inst r, 1965 : 4, 117.
[15] Nagarsenkar MS, Shenai H. Drug Dev Ind Pharm, 1996, 22 : 987.
[16] Nakai Y. Drug Dev Ind Pharm, 1986, 12 : 1017.
[17] Szejtli J . Cyclodext rins and Thei r I nclusion Complexes . Akademia Kiado, Budapest, 1982 : 95.
[18] Green AR, Miller ES, Guillory J K. J Pharm Sci, 1991, 80 : 186.
[19] Najeeb N, Suleiman M. Drug Dev Ind Pharm, 1985, 11 : 2169.
[20] Hassegawa A, Kawamura R, Nakagawa H, et al. Chem Pharm B ull, 1986, 34 : 2183.
[21] Martin A, Swarbrick J, Cammarata A. Physical Pharmacy 3rd ed., Lea & Febiger. Philadelphia, 1983: 513.
[22] Sekikawa H, Nakano M, Arita T. Chem Pharm B ull, 1978, 26: 118.
[23] Kislalioglu MS, Khan MA, Blont C. J Pharm Sci, 1991, 80: 799.
[24] Vromans H, Eissons AC, Coenraad FL. Drug Dev Ind Pharm, 1989, 35: 250.