Yanagihara Y, Ohtani M, Matsumoto M, Kariya S, Uchino K, Hiraishi T, Ashizawa N, Aoyama T, Yamamura Y, Iga T
Department of Pharmacy, Tokyo Posts and Telecommunications Hospital, Japan.
Yakugaku Zasshi. 1999 Dec;119(12):980-7. doi: 10.1248/yakushi1947.119.12_980.
Ketamine is known to have distinguished analgesic effects without anesthetic when administered in a low dose. Since ketamine is not commercially available except injection forms, we prepared ketamine tablets for the home-care medication of patients with neuropathic pain. The direct compression or wet granulation method was employed to form 150 mg of tablets containing 50 mg of ketamine. The latter method was superior to the former one in terms of content uniformity, weight variation and disintegration tests of the tablets. Ketamine contents in the tablet prepared by the wet granulation method were unchanged for 12 weeks under the conditions of 25 degrees C and 75% relative humidity (RH). The Cmax and AUC0-3 h values for ketamine after administration of the tablet were slightly smaller than those of the syrup in a healthy volunteer. However, analgesic effects of the tablet was similar to that of the syrup in a patient with neuropathic pain. And the tablet was also effective for another four patients with neuropathic pain. These results indicate that ketamine tablets are useful for the home-care medication of patients with neuropathic pain.
已知氯胺酮在低剂量给药时具有显著的镇痛作用而无麻醉作用。由于氯胺酮除注射剂外无市售剂型，我们制备了用于神经性疼痛患者居家护理用药的氯胺酮片剂。采用直接压片法或湿法制粒法制备含50mg氯胺酮的150mg片剂。在片剂的含量均匀度、重量差异和崩解试验方面，后一种方法优于前一种方法。在25℃和75%相对湿度（RH）条件下，采用湿法制粒法制备的片剂中氯胺酮含量在12周内保持不变。在健康志愿者中，服用该片剂后氯胺酮的Cmax和AUC0-3 h值略低于糖浆剂。然而，该片剂对神经性疼痛患者的镇痛效果与糖浆剂相似。并且该片剂对另外4例神经性疼痛患者也有效。这些结果表明，氯胺酮片剂可用于神经性疼痛患者的居家护理用药。
