Dayyih Wael Abu, Hamad Mohammed, Awwad Ahmad Abu, Mallah Eyad, Zakarya Zainab, Dayyih Alice Abu, Arafat Tawfiq
Faculty of Pharmacy and Medical Sciences, University of Petra, Amman, Jordan.
Department of Basic Sciences, College of Science and Health Professions, King Saud Bin Abdulaziz University for Health Sciences, Jeddah, Saudi Arabia.
J Anal Methods Chem. 2017;2017:8489471. doi: 10.1155/2017/8489471. Epub 2017 Aug 15.
Enalapril is an angiotensin-converting enzyme inhibitor used for treatment of hypertension and chronic heart disease. Enalaprilat is its active metabolite responsible for the activity. This study aimed to develop and validate a method for enalapril and enalaprilat analysis and to determine the bioequivalence of two tablet formulae of enalapril. LC-MS/MS bioanalytical method was developed and validated and then applied to evaluate the bioavailability of two enalapril formulae. Antihyperglycemic sitagliptin was used as internal standard (IS). The method was accurate for the within- and between-days analysis, and precise CV% was <5%, being linear over the calibration range 1.0-200.0 ng/ml. Stability was >85% and the LOD was 0.907 and 0.910 ng/ml for enalapril and enalaprilat, respectively, and LLOQ was 1 ng/ml. The pharmacokinetic parameters , , AUC, and AUC values of enalapril and enalaprilat of the two formulae were calculated and nonsignificant differences were found. A linearity, specific, accurate, and precise method was developed and applied for the analysis of enalapril and enalaprilat in human plasma after oral administration of two formulae of enalapril 20 mg tablets in healthy volunteers. Depending on the statistical analysis it was concluded that the two enalapril formulae were bioequivalent.
依那普利是一种用于治疗高血压和慢性心脏病的血管紧张素转换酶抑制剂。依那普利拉是其具有活性的代谢产物。本研究旨在开发并验证一种依那普利和依那普利拉的分析方法，并确定两种依那普利片剂配方的生物等效性。开发并验证了LC-MS/MS生物分析方法，然后将其应用于评估两种依那普利配方的生物利用度。降糖药物西他列汀用作内标（IS）。该方法在日内和日间分析中准确，精密度CV%<5%，在校准范围1.0 - 200.0 ng/ml内呈线性。依那普利和依那普利拉的稳定性>85% ,依那普利和依那普利拉的检测限分别为0.907和0.910 ng/ml，定量下限为1 ng/ml。计算了两种配方中依那普利和依那普利拉的药代动力学参数、、AUC和AUC值，未发现显著差异。开发了一种线性、特异、准确和精密的方法，并将其应用于健康志愿者口服两种20 mg依那普利片剂配方后人体血浆中依那普利和依那普利拉的分析。根据统计分析得出结论，两种依那普利配方具有生物等效性。
