Preparation and evaluation of glibenclamide-polyglycolized glycerides solid dispersions with silicon dioxide by spray drying technique.
Solid dispersions (SDs) of glibenclamide (GBM); a poorly water-soluble drug and polyglycolized glycerides (Gelucire with the aid of silicon dioxide (Aerosil 200); as an adsorbent, were prepared by spray drying technique. SDs and spray dried GBM in comparison with pure GBM and corresponding physical mixtures (PMs) were initially characterized and then subjected to ageing study up to 3 months. Initial characterization of SDs and spray dried GBM by DSC and XRPD showed that GBM was present in its amorphous form (AGBM). Improvement in the solubility and dissolution rate was observed for all samples. DRIFT spectroscopy revealed presence of hydrogen bonding in SDs. During ageing study, almost no decrease of in vitro drug dissolution was observed, over the period of 3 months as compare with freshly prepared SDs. Slight crystallinity in SDs was observed in the DSC and XRPD studies during ageing. Moreover in vivo study in Swiss Albino mice also justified the improvement in the therapeutic efficacy of amorphous GBM in SDs over pure GBM. Thus, present study demonstrated the high potential of spray drying technique for obtaining stable free flowing SDs of poorly water-soluble drugs using polyglycolized glycerides carriers with the aid of silicon dioxide as an adsorbent.
Chauhan
Bhaskar
B
Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune 411038, Maharashtra, India.
Shimpi
Shyam
S
Paradkar
Anant
A
D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004355:Drug Stability; D005079:Excipients / Q000737:chemistry*; D005223:Fats / Q000737:chemistry*; D005260:Female; D005951:Glucose Tolerance Test; D005905:Glyburide / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008855:Microscopy, Electron, Scanning; D009821:Oils / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000008:administration & dosage / Q000737:chemistry*; D033362:Powder Diffraction; D012822:Silicon Dioxide / Q000737:chemistry*; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D044366:Transition Temperature; D014961:X-Ray Diffraction
D005079:Excipients; D005223:Fats; D009821:Oils; C104509:gelucire 44-14; C071184:Gelucire 50-13; D011092:Polyethylene Glycols; D012822:Silicon Dioxide; D005905:Glyburide