Abstract
The bioavailability and pharmacokinetics of molsidomine (SIN-10) from a capsule containing wax-coated beads, were compared with those from a conventional tablet in dogs and monkeys during the formulation study of a sustained release dosage form of SIN-10. Sustained-release capsules (SR capsules) A, B and C contained coated beads with different amounts of wax, and SR capsule D contained 20% immediate release beads and 80% wax-coated beads. In dogs, SR capsules A and B did not satisfactorily prolong the effective plasma concentration. With capsule C, although satisfactory maintenance of effective plasma concentration was obtained, the bioavailability was only to half of that after administration of a conventional tablet. On the other hand, in monkeys, reasonable prolongation of effective plasma concentration (depending upon the amount of wax coating) with satisfactory bioavailability was obtained for each SR capsule. With an SR capsule D, more than 12h duration of effective plasma concentration of molsidomine and control of blood pressure from immediately after administration of the capsule were achieved in monkeys.
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