Nafarelin controlled release injectable: theoretical clinical plasma profiles from multiple dosing and from mixtures of microspheres containing 2 per cent, 4 per cent and 7 per cent nafarelin.

摘要: Nafarelin controlled release injectable (CRI) releases a decapeptide drug for target one month therapy. Nafarelin, luteinizing hormone releasing agonistic analogue, is microencapsulated in biodegradable poly(lactide-co-glycolide) microspheres and given by intramuscular injection. Clinical data from human single dose Phase I clinical study are modelled to develop theoretical multiple profiles mixtures of two or three formulations. Single injections nafarelin CRI (4 mg nafarelin) containing 2, 4, 7 per cent all achieve useful plasma levels throughout the 30 day interval. Therapeutic suppression testosterone was observed subjects participating phase study. Highest achieved 0-10 20-35 post-injection intervals. Theoretical dosing generated results show significant oscillations depending on particular interval selected. Thirty forty intervals yield variability at steady state; 15 less variability. study, so injection can be reduced therapies. certain 2 4 indicate that 60 product could achieved. In general, formulations their lowest during 10-20 Therefore any mixture these will likewise exhibit low this