Esimone C O, Okoye F B C, Onah B U, Nworu C S, Omeje E O
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Enugu State, Nigeria.
J Vector Borne Dis. 2008 Mar;45(1):60-5.
BACKGROUND & OBJECTIVES: The availability of numerous brands of artesunate in our drug market today places clinicians and pharmacists in a difficult situation of choice of a suitable brand or the possibility of alternative use. The aim of the present study was to predict the bioequivalence of nine brands of artesunate tablets marketed in Nigeria using in vitro tests.
The in vitro dissolution study was carried out on the nine brands of artesunate tablets using the basket method according to US Pharmacopoeia (USP) guidelines. Other general quality assessment tests like hardness and disintegration time were also determined.
All the brands tested passed the British Pharmacopoeia (BP) standard for disintegration time. Only AT2, AT4, AT6 and AT9 passed the standard for hardness. There were significant differences in the dissolution profiles of the nine brands. All the brands except AT1, however, released >70% of artesunate within 30 min. Four of the brands AT5, AT6, AT7 and AT8 exhibited >90% dissolution in <10 min. The other brands AT1, AT2, AT3, AT4 and AT9 (innovator brand) have calculated similarity factors of 23.8, 59.8, 50, 54.8 and 100.
INTERPRETATION & CONCLUSION: Based on the in vitro tests, AT5, AT6, AT7 and AT8 are considered bioequivalent and interchangeable, while AT2, AT3 and AT4 are considered bioequivalent and interchangeable with the innovator brand (AT9). AT1 has very low dissolution rate, which will likely result in poor bioavailability. The results show the need for constant monitoring of new brands of artesunate introduced into the drug market to ascertain bioequivalence and conformity with pharmacopoeia standards.
当今我国药品市场上青蒿琥酯品牌众多，这使临床医生和药剂师在选择合适品牌或考虑替代使用方面陷入困境。本研究旨在通过体外试验预测在尼日利亚销售的9种品牌青蒿琥酯片的生物等效性。
按照美国药典（USP）指南采用篮法对9种品牌的青蒿琥酯片进行体外溶出度研究。还测定了其他一般质量评估试验，如硬度和崩解时间。
所有受试品牌均通过了英国药典（BP）规定的崩解时间标准。只有AT2、AT4、AT6和AT9通过了硬度标准。9种品牌的溶出曲线存在显著差异。然而，除AT1外，所有品牌在30分钟内释放的青蒿琥酯均>70%。AT5、AT6、AT7和AT8这4种品牌在<10分钟内的溶出度>90%。其他品牌AT1、AT2、AT3、AT4和AT9（原研品牌）计算得到的相似性因子分别为23.8、59.8、50、54.8和100。
基于体外试验，AT5、AT6、AT7和AT8被认为具有生物等效性且可相互替代，而AT2、AT3和AT4被认为与原研品牌（AT9）具有生物等效性且可相互替代。AT1的溶出速率非常低，这可能导致生物利用度较差。结果表明有必要持续监测引入药品市场的青蒿琥酯新品牌，以确定其生物等效性及是否符合药典标准。
