Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Nagar, India.
Drug Test Anal. 2011 Jun;3(6):363-72. doi: 10.1002/dta.229. Epub 2010 Dec 29.
Paromomycin (PM) is an aminoglycoside antibiotic, first isolated in the 1950s, and approved in 2006 for treatment of visceral leishmaniasis. Although isolated six decades back, sufficient information essential for development of pharmaceutical formulation is not available for PM. The purpose of this paper was to determine thermal stability and development of new analytical method for formulation development of PM. PM was characterized by thermoanalytical (DSC, TGA, and HSM) and by spectroscopic (FTIR) techniques and these techniques were used to establish thermal stability of PM after heating PM at 100, 110, 120, and 130 °C for 24 h. Biological activity of these heated samples was also determined by microbiological assay. Subsequently, a simple, rapid and sensitive RP-HPLC method for quantitative determination of PM was developed using pre-column derivatization with 9-fluorenylmethyl chloroformate. The developed method was applied to estimate PM quantitatively in two parenteral dosage forms. PM was successfully characterized by various stated techniques. These techniques indicated stability of PM for heating up to 120 °C for 24 h, but when heated at 130 °C, PM is liable to degradation. This degradation is also observed in microbiological assay where PM lost ∼30% of its biological activity when heated at 130 °C for 24 h. New analytical method was developed for PM in the concentration range of 25-200 ng/ml with intra-day and inter-day variability of < 2%RSD. Characterization techniques were established and stability of PM was determined successfully. Developed analytical method was found sensitive, accurate, and precise for quantification of PM. Copyright © 2010 John Wiley & Sons, Ltd.
巴龙霉素(PM)是一种氨基糖苷类抗生素,于 20 世纪 50 年代首次分离出来,并于 2006 年获准用于治疗内脏利什曼病。尽管它是在六十年前分离出来的,但对于 PM 的药物制剂开发来说,仍然缺乏足够的必要信息。本文的目的是确定 PM 的热稳定性并开发新的分析方法,用于 PM 的制剂开发。通过热分析(DSC、TGA 和 HSM)和光谱(FTIR)技术对 PM 进行了表征,并使用这些技术在 100、110、120 和 130°C 下加热 PM 24 小时后,确定了 PM 的热稳定性。还通过微生物测定法测定了这些加热样品的生物活性。随后,使用 9-芴甲基氯甲酸酯进行预柱衍生化,开发了一种简单、快速和灵敏的反相高效液相色谱法(RP-HPLC),用于定量测定 PM。所开发的方法用于两种注射剂剂型中 PM 的定量估计。PM 通过各种规定的技术成功地进行了表征。这些技术表明,PM 在 120°C 加热 24 小时内是稳定的,但在 130°C 加热时,PM 容易降解。在微生物测定中也观察到了这种降解,当 PM 在 130°C 加热 24 小时时,其生物活性损失了约 30%。开发了一种新的分析方法,用于 PM 的浓度范围为 25-200ng/ml,日内和日间变异系数均小于 2%RSD。成功地建立了表征技术并确定了 PM 的稳定性。开发的分析方法对于 PM 的定量测定具有灵敏、准确和精密的特点。版权所有©2010 约翰威立父子公司