Preparation of Buprenorphine Sublingual Tablets and Clinical Effects

We tried to improve buprenorphine (BN) sublingual tablets (previous tablets) prepared previously [Yakuzaigaku, 46: 134-139 (1986)] by focusing on shortening the disintegration time because the disintegration of these tablets sublingually in man is quite long (7-9 minutes). Five different tablets (100mg) containing 100μg of BN were prepared, and the qualitative characteristics, pharmacokinetic behavior and clinical effect of BN were compared with the previous tablets. In the quality tests, one of the new tablets comprising 78.1 mg of 0.128% BN powder, 19.9 mg of lactose, 1 mg of magnesium stearate and 1 mg of powdered acacia per tablet was superior to the other products in terms of both disintegration and dissolution. The mean sublingual disintegration times fos the placebo of the new tablet in five healthy volunteers and five patients were 3.0 and 3.6 minutes, respectively, values which were significantly shorter than those (7.5 and 6.5 minutes) for the previous tablet. The plasma concentration of BN or analgesic effect arising after sublingual administratation of the new tablet in one healthy volunteer and two patients were closely comparable with those following sublingual administration of the previous tablet. The new tablet is biologically and pharmacologically equivalent to the previous one and is superior to the previous tablet in terms of disintegration characteristics.