乳糖酸和非离子表面活性剂作为克拉霉素注射用制剂增溶剂的应用。
Application of lactobionic acid and nonionic surfactants as solubilizing agents for parenteral formulation of clarithromycin.
作者信息
Zakeri-Milani Parvin, Mousavian-Fathi Niaz, Ghanbarzadeh Saeed, Zarrintan Mohammad-Hosein, Valizadeh Hadi
机构信息
Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. ; Liver and Gastrointestinal Diseases Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
出版信息
Adv Pharm Bull. 2012;2(1):37-42. doi: 10.5681/apb.2012.006. Epub 2012 Feb 15.
PURPOSE
The purpose of this paper is to enhance the solubility of clarithromycin (CLR) using nonionic surfactants and some type of acids for preparation of the new formulations.
METHODS
Myrj 52 and chremophor (2.5 and 5% w/v) were used in two concentrations. To investigate solubility, the formulations were shaken for 48 hours at room temperature. For stability test, lyophilized samples were maintained in refrigerator at 4° C, and in oven at 40° C. Drug analysis was performed by reverse phase high performance liquid chromatography (HPLC) with ultraviolet detection.
RESULTS
Solubility tests indicated that lactobionic acid was the most effective to increase clarithromycin solubility and chremophor showed higher enhancing effect than myrj 52 on CLR solubility. The stability tests results also confirmed that shelf-lives of all formulations have been the equivalent to 24 months.
CONCLUSION
On the whole, formulations described in this article may be very suitable for industrial-scale manufacturing and clinical application.
目的
本文旨在使用非离子表面活性剂和某些类型的酸来提高克拉霉素（CLR）的溶解度，以制备新制剂。
方法
使用两种浓度的聚山梨醇酯52和聚氧乙烯蓖麻油（2.5%和5% w/v）。为研究溶解度，将制剂在室温下振荡48小时。对于稳定性测试，冻干样品保存在4°C的冰箱中以及40°C的烘箱中。通过带有紫外检测的反相高效液相色谱法（HPLC）进行药物分析。
结果
溶解度测试表明乳糖酸对提高克拉霉素溶解度最有效，并且聚氧乙烯蓖麻油对CLR溶解度的增强作用比聚山梨醇酯52更高。稳定性测试结果也证实所有制剂的货架期相当于24个月。
结论
总体而言，本文所述制剂可能非常适合工业规模生产和临床应用。
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