Spray-dried amorphous solid dispersions of simvastatin, a low tg drug: in vitro and in vivo evaluations

摘要: To obtain free flowing, stable, amorphous solid dispersions (SDs) of simvastatin (SIM), a drug with relatively lower glass transition temperature (Tg) by spray drying technique, and to perform comparative in vivo study rats, which could justify the improvement rate extent vitro release. Dichloromethane suspensions SIM either alone or combination PVP (1:1 1:2 parts weight) were dried proposed quantity Aerosil 200 (1:1, 1:1:1, 1:2:2 weight SIM, PVP, respectively). SDs characterized initially comparison pure corresponding physical mixtures same ratios content, saturation solubility, SEM, DSC, XRPD, IR, SD was further subjected accelerated stability testing checked for release presence crystallinity using DSC XRPD. In addition, from justified rats. Combination surface adsorption techniques has been attempted overcome limitations technique amorphization low Tg drugs. Based on powder characteristics, feasibility processing into tablets; selected as optimized formulation. During initial characterization, XRPD analyses confirmed form 1:2:2. IR spectroscopy revealed possibility hydrogen bonding interaction between SDs. Also, there dramatical Insignificant decrease dissolution observed no evidence during studies Moreover rats also therapeutic efficacy over SIM. Thus, present demonstrates high potential obtaining stable