- 期刊
- OpenAccess
Depot of Ketorolac Tert-butyl Ester Has Long-acting Antinociceptive and Anti-inflammatory Effects in Rats
一個含Ketorolac Tert-Butyl酯之藥物貯存劑型在大白鼠測試有長效之抗發炎及止痛作用
摘要
目前在臨床上並無長效之非固醇類抗發炎劑可供治療為期較長的疼痛，本研究的目的在探討一個內含Ketorolac tert-butyl酯的新藥物貯存劑型是否具有長效的止痛及抗發炎作用。我們以大白鼠來進行二項實驗。實驗一：我們測量肌肉注射傳統劑型Ketorolac tromethamine水溶液的抗發炎及止痛作用。實驗二：我們測量肌肉注射含Ketorolac tert-butyl酯之新油性劑型的抗發炎及止痛作用。我們發現肌肉注射傳統Ketorolac tromethamine水劑240 μ mol/kg產生了顯著的止痛及抗發炎作用，但其效期僅有8小時。而肌肉注射新的Ketorolac tert-butyl酯油劑240 μ mol/kg卻產生了56小時的止痛及抗發炎作用。我們的結論為在大白鼠以肌肉注射Ketorolac tert-butyl酯之油劑可產生一個非常長的止痛及抗發炎作用，其效果為傳統Ketorolac tromethamine水劑的7倍長。
並列摘要
Currently, no long-acting nonsteriodal anti-inflammatory drug is available clinically for the treatment of long-lasting pain. The aim of the study was to evaluate the antinociceptive and anti-inflammatory effects and durations of actions of a novel depot formulation of ketorolac tert-butyl ester and to observe whether this depot formulation had a long-acting effect. Two studies in Sprague-Dawley rats were carried out. In study 1, the antinociceptive and anti-inflammatory effects of intramuscular ketorolac tromethamine were evaluated. In study 2, the antinociceptive and anti-inflammatory effects of intramuscular ketorolac tert-butyl ester were evaluated. We found that ketorolac tromethamine 240 μ mol/kg (in saline) produced significant antinociceptive and anti-inflammatory effects with duration of action of 8 h. Ketorolac tert-butyl ester at a dose of 240 μ mol/kg (in oil) produced significant long-acting antinociceptive and anti-inflammatory effects with duration of action of 56 h. We conclude that intramuscular injection of a novel depot formulation of ketorolac tert-butyl ester in rats produced long-acting antinociceptive and anti-inflammatory effects which were 7-fold longer than the traditional dosage form of ketorolac tromethamine did.
延伸閱讀
- Chen, K. T., Hu, O. Y. P., Ho, S. T., Chen, Y. W., & Wang, J. J. (2002). Nalbuphine及其長效前趨藥Nalbuphine Pivalate在大白鼠之止痛藥效研究. Acta Anaesthesiologica Sinica, 40(4), 191-195. https://doi.org/10.6955/AAS.200212.0191
- Wu, S. Z., Liu, K. S., Chu, K. S., Cheng, K. I., Kuei, C. H., Wang, J. J., & Tzeng, J. I. (2006). 在天竺鼠癸酸Buprenorphine之油性藥物貯存劑型產生一個和劑量相關的長效止痛作用. Acta Anaesthesiologica Taiwanica, 44(3), 161-168. https://www.airitilibrary.com/Article/Detail?DocID=02541319-200609-44-3-161-168-a
- Wu, R. S. C. (2005). Ketorolac丙酸酯在大白鼠止痛及抗發炎效應上的評估. Acta Anaesthesiologica Taiwanica, 43(2), 63-65. https://www.airitilibrary.com/Article/Detail?DocID=02541319-200506-43-2-63-65-a
- Wang, L. K., Wang, P. J., Hou, C. H., Chu, C. C., Tzeng, J. I., Shieh, J. P., & Wang, J. J. (2005). 在大白鼠測試Ketorolac丙酸酯的五種藥物貯積劑型之止痛及抗發炎效果. Acta Anaesthesiologica Taiwanica, 43(2), 85-92. https://www.airitilibrary.com/Article/Detail?DocID=02541319-200506-43-2-85-92-a
- Yang, C., Lan, K. M., Liu, K. S., Chen, Y. W., Tzeng, J. I., Ho, S. T., & Wang, J. J. (2004). Buprenorphine 及其長效酯 Buprenorphine Benzoate 在大白鼠之止痛效用測試. Acta Anaesthesiologica Taiwanica, 42(3), 135-139. https://www.airitilibrary.com/Article/Detail?DocID=02541319-200409-42-3-135-139-a