title: Degradation patterns of tetracycline antibiotics in reverse micelles and water.
abstract: The objective of this study was to determine the chemical stability of tetracycline and oxytetracycline hydro-chlorides in reverse micelles. Their reverse micellar solutions were prepared using cetyltrimethylammonium bromide, water and ethyl formate. The aqueous solutions of the tetracycline antibiotics were also prepared for comparison. The reverse micellar and aqueous solutions were stored at 37 degrees C. Samples were analyzed by high performance liquid chromatography. When evaluation was performed on an aqueous tetracycline HCl solution, its half-life was estimated to be 329 h. Its chemical stability was not improved after being dissolved in the reverse micelles, and a similar half-life of 330 h was observed. However, there were noticeable differences between the two systems in terms of degradation kinetics and degradation byproducts. On the other hand, oxytetracycline HCl was unstable in water so that its half-life was only 34 h. Very interestingly, pronounced improvement in stability was attained with the reverse micellar system: upon dissolving in the reverse micelles, its half-life was increased to 2402 h. There were also marked differences in degradation patterns and mechanisms of oxytetracycline HCl in water and the reverse micelles. Our study indicates that the reverse micellar system has potential applications in solubilizing and stabilizing oxytetracycline HCl, thereby contributing to the development of its dosage forms.
authors.affiliation: Department of Pharmaceutical Science, College of Pharmacy, Ewha Womans University, Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Korea. hsah@ewha.ac.kr
authors.forename: Hongkee
authors.initials: H
authors.lastname: Sah
mesh_terms: D000077286:Cetrimonium; D002593:Cetrimonium Compounds / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D008823:Micelles; D010118:Oxytetracycline / Q000737:chemistry; D011422:Propionates / Q000737:chemistry; D012995:Solubility; D013754:Tetracyclines / Q000737:chemistry*; D014867:Water
chemical_list: D002593:Cetrimonium Compounds; D008823:Micelles; D011422:Propionates; D013754:Tetracyclines; D014867:Water; C029658:propionic acid; D010118:Oxytetracycline; D000077286:Cetrimonium