title: A systematic approach to design and prepare solid dispersions of poorly water-soluble drug.
abstract: The objective of the present study was to define a systematic approach to design and prepare solid dispersions of poorly water-soluble drug. The systematic approach can be defined in four phases. In the first phase, glass forming ability is assessed, and in the second phase, probable excipients are screened. The screened excipients are evaluated (third phase) for glass transition temperatures (Tg) and miscibility studies according to Florey-Huggins interaction parameter. The predicted excipients are used to prepare the solid dispersion and evaluated for Tg and any interactions using Fourier transfer infrared studies (fourth phase), and the findings are correlated with phase three predictions. For this investigation, cilostazol (CIL) was selected as model drug, which was classified as a poor glass former. As per the physical chemical properties of CIL, ten excipients, both polymeric and non-polymeric, were selected and screened. Out of these, povidone, copovidone, hypromellose and Eudragit EPO were found theoretically miscible with CIL. After going through phase 2 to phase 4, only povidone, copovidone and hypromellose were confirmed as polymer of choice for preparing the solid dispersion of CIL with a prediction of better physical solid-state stability on the basis of good miscibility between drug and carrier.
authors.affiliation: Centre for Pharmaceutical Sciences, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad, 500 085, India, sanjayverma9@yahoo.com.
authors.forename: Sanjay
authors.initials: S
authors.lastname: Verma
authors.forename: Varma S
authors.initials: VS
authors.lastname: Rudraraju
mesh_terms: D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D000077407:Cilostazol; D005079:Excipients / Q000737:chemistry*; D065347:Hypromellose Derivatives / Q000737:chemistry; D007700:Kinetics; D008956:Models, Chemical; D011205:Povidone / Q000737:chemistry; D011759:Pyrrolidines / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical / Q000379:methods; D013777:Tetrazoles / Q000737:chemistry*; D044366:Transition Temperature; D014753:Vinyl Compounds / Q000737:chemistry; D014867:Water / Q000378:metabolism*
chemical_list: D005079:Excipients; D011759:Pyrrolidines; D013777:Tetrazoles; D014753:Vinyl Compounds; C402301:poly(vinylpyrrolidone-co-vinyl-acetate); D014867:Water; D065347:Hypromellose Derivatives; D011205:Povidone; D000077407:Cilostazol