塩酸ブプレノルフィン坐剤の臨床第1相試験

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Phase I clinical study was performed in 6 healthy male subjects. Three of the subjects received a 0.3 mg suppository and the other 3 received a 0.6 mg suppository by rectal route, and the safety and blood levels of buprenorphine were determined. The results obtained were as follows. After the administration of a 0.3 mg or 0.6 mg suppository, there were no clinically significant changes in blood pressure, pulse rate, respiratory rate, and body temperature ; no abnormalities were observed on ECG. Cmax and AUC were 0.24ng/ml and 2 .60ng·hr/ml at a dose of 0.3mg and 0.47ng/ml and 5. 14 ng·hr/ml at a dose of 0. 6 mg, both of which increased in proportion with the increase in the dose. Tmax was 2. 17 hr at a dose of 0.3 mg and 1.67 hr at a dose of 0.6 mg. Subjective or objective findings included sedation, headache, dull headedness, dry mouth, dizziness, vomiting, sweating, and local uneasiness ; all of these were mild. No abnormal values were seen in hematology, biochemistry, and urinalysis. From these results, buprenorphine suppositories at doses of 0.3 mg and 0.6 mg were confirmed to be safe in healthy subjects and its clinical usefulness was considered to be promising.
一般社団法人日本臨床薬理学会の論文