孙英华,施洁明,仲晖,何仲贵,王卓,李鸿滨
SUN Ying-hua1; SHI Jie-ming1; ZHONG Hui1; HE Zhong-gui1; WANG Zhuo2; LI Hong-bin3(1.School of Pharmacy;

• 1:沈阳药科大学药学院
• 2:沈阳药科大学药学院
• 3:沈阳药科大学药学院
• 4:沈阳药科大学药学院

摘要(Abstract)：

目的测定美洛昔康在不同浓度 2 羟丙基 β 环糊精溶液中的溶解度曲线 ,以及包合物的组成量比例和稳定性常数。方法在 2 5℃运用相溶解度法进行实验 ,采用紫外分光光度法测定美洛昔康在溶液中的浓度。结果随着 2 羟丙基 β 环糊精浓度增加和 pH的增大 ,美洛昔康的溶解度显著提高。计算了表观稳定常数、确定了不同pH条件下包合物的摩尔比。 结论难溶性药物美洛昔康与 2 羟丙基 β 环糊精可形成 1 :1包合物。
Objective To investigate the solubilization effects of the inclusion complex of meloxicam with 2-hydroxypropy1-β-cyclodextrin (HPCD) in aqueous solutions at various pH and to determine the constitutive molar ratio of meloxicam-2-hydroxypropy1-β-cyclodextrin inclusion compound and its stability constant.Methods The solubilization experiment was performed by the phase-solubility method at 25℃.The concentration of meloxicam was determined by the UV spectrophotometric method. Results The apparent solubility of meloxicam was enhanced noticeably with the increase of concentration HPCD and the increasing pH values.The apparent stability constants were calculated respectively.The molar ratio of the inclusion complex at various pH were studied.The application of HPCD to parenteral formulations of meloxicam was discussed preliminarily.Conclusion An inclusion compound of meloxicam and HPCD can be formed.

关键词(KeyWords)： 2-羟丙基β-环糊精;美洛昔康;溶解度
2-hydroxypropy1-β-cyclodextrin; meloxicam; solubility

Abstract:

Keywords:

基金项目(Foundation): 国家“九五”重点科技攻关项目 ( 96-90 2 -0 2 -0 9)

作者(Authors): 孙英华,施洁明,仲晖,何仲贵,王卓,李鸿滨
SUN Ying-hua1; SHI Jie-ming1; ZHONG Hui1; HE Zhong-gui1; WANG Zhuo2; LI Hong-bin3(1.School of Pharmacy;

参考文献(References)：

• [1]PeterLuger,KlausDaneck,WolfhardEngel,etal.Structureand physicochemicalpropertiesofmeloxi cam,anewNSAID [J].EuropeanJournalofPharma ceuticalSciences,1996,4:175-187.
• [2]毕殿洲.药剂学[M ].第4版.人民卫生出版社,1999.272-273.
• [3]何仲贵,唐星,陈宣福,等.β环糊精及其衍生物2羟丙基β环糊精对布洛芬的增溶作用[J].沈阳药科大学学报,1998,15(4):235-237.
• [4]陶涛.羟丙基倍他环糊精的特性及其药剂学运用[J].中国医药工业杂志,2002,33(6):304-308.
• [5]杨采琴,申世刚,王静,等.桂利嗪β环糊精包合物的制备[J].中国药师,2002,5(9):533-534.
• [6]TakeruHiguchi,KennethA .Connorsphase solubilitytechniques[J].AdvAnalChemInstr,1965,4:117.
• [7]JichaoKang,VijayKumar,DongYang,etal.Cyclodex trincomplexation:influenceonthesolubility,stability,andcytotoxicityofcamptothecin,anantineplasticagent[J].EuropeanJournalofPharmaceuticalSciences,2002,15:163-170.