M.V. Gavrilin, O.M. Markova, I.N. Dyakova, L.I. Shcherbakova, A.I. Medvetskyi

The method of receiving microparticles of alprasolam on the base of biodegraded polymer poly-DL-lactid-co-glycolide is offered. In difference from badly soluble and possessing low bioavailability alprasolam which can be used only orally, the received microparticles form stable water suspensions. This property was used for preparation of the prolonged parenteral medicinal alprasolam form. Studying of influence of a microparticles preparation method and polyvinyl alcohol concentration on their size and the medicinal substance including degree was carried out. As a result of researches it was established that including degree of the medicinal substance does almost not depend on a microparticles receiving method. However, the size of microparticles received with the help of a method I is much more less. Optimum concentration of the polyvinyl alcohol solution was 3 %. Prolongation of effect of offered medicine was carried out in in Vivo experiences. Influence of the prolonged parenteral alprasolam forms, received by using of a method I and II on duration of a drug sleep was studied. Pharmacological researches showed that inclusion alprasolam in microparticles on the base of poly-DL-lactid-co-glycolide prolongation of its action - about four weeks is observed. Received results prove that the prolonged medicinal forms of alprasolam on the base of copolymer of lactic and glycolic acids differ from usual forms of this medicine more effectiveness and action duration.