The inclusion complex and multicomponent system of efavirenz to increase the solubility in anti - HIV therapy

摘要

The inclusion complex and multicomponent system of efavirenz to increase the solubility in anti - HIV therapy. This patent relates to the formulation of the inclusion complex and multicomponent system of efavirenz to increase the solubility in anti - HIV therapy.This patent relates to a pharmaceutical product as the main component is the input farmnacu00eautico active efavirenz (EFZ) whose chemical structure is the (s) - (-) - 6 - chloro - 4 - (ciclopropiletinil) - 4 - (trifluormetil).2,4 dihydro - L H - 3.1 - benzoxazin - 2 - one and the excipients methyl - - cyclodextrin (M 225 - 13 - CD) in different concentrations, and polivinilpirrolidonas (PVP K-30, PVP (k - 12 - 15 K, PVP, PVP PVP (k - K - 17, 25, PVP K - 60, PVP K-90 and PvP K - 120).The complex of inclusion between the EFZ and M - - 225 CD showed stable, noting it is efficiency in the complexation and an increase in solubility, which initially was 8 - 10 109 G / ml, and increased to 70 - 80 109 G / ml.This can be justified by the presence of methyl groups, because these groups are important for the enlargement of the cavity of CDs, favouring a more hydrophobic environment hidrofilico externally and internally by promoting the adaptability of drugs, through greater flexibi Time.The multicomponent systems between the EFZ - M - J - CD and polivinilpirrolidonas led to an increase in the solubility of EFZ of 8 - 10 225 G / ml for 50 - 90 225 G / ml.