title: Evaluation of the physicochemical characteristics of crospovidone that influence solid dispersion preparation.
abstract: A solid dispersion (SD) powder of indomethacin (IM) with crospovidone (CrosPVP) shows useful characteristics for manufacturing dosage forms. Four types of commercial CroPVP, Polyplasdone XL (XL) used as the initial carrier, Polyplasdone XL10 and INF-10 manufactured by milling XL, and Kollidon CL (CL) marketed by another company, were compared. The limit of the IM-CrosPVP weight ratio with which an SD can be prepared (maximum IM content) was calculated on the basis of the heat of fusion of physical mixtures of IM and CrosPVP with various weight ratios. When Polyplasdones were used, the maximum IM content increased with the specific surface area of the CrosPVP. When CL was used, however, it was about half of that obtained with XL, even though the difference between XL and CL was not observed in the physicochemical characteristics (particle size, specific surface area, flowability, glass transition temperature, IR spectra, and solid state NMR spectra). As determined by pore size distribution measurement, the volume of pore of which size is larger than the particle size of IM was less in CL than in XL. Therefore, the effective surface area of CrosPVP that comes in contact with IM is important for the preparation of the SD.
authors.affiliation: Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University, 3-3165 Higashi-Tamagawagakuen, Machida, Tokyo 194-8543, Japan.
authors.forename: Sayaka
authors.initials: S
authors.lastname: Nakanishi
authors.forename: Makiko
authors.initials: M
authors.lastname: Fujii
authors.forename: Yuka
authors.initials: Y
authors.lastname: Sugamura
authors.forename: Ayako
authors.initials: A
authors.lastname: Suzuki
authors.forename: Yusuke
authors.initials: Y
authors.lastname: Shibata
authors.forename: Naoya
authors.initials: N
authors.lastname: Koizumi
authors.forename: Yoshiteru
authors.initials: Y
authors.lastname: Watanabe
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry; D055598:Chemical Phenomena; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D006358:Hot Temperature; D007213:Indomethacin / Q000737:chemistry; D010316:Particle Size; D010592:Pharmaceutic Aids / Q000032:analysis / Q000737:chemistry*; D011205:Povidone / Q000032:analysis / Q000737:chemistry*; D011208:Powders / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties; D044366:Transition Temperature
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D005079:Excipients; D010592:Pharmaceutic Aids; D011208:Powders; D011205:Povidone; D007213:Indomethacin