Part I: characterization of solid dispersions of nimodipine prepared by hot-melt extrusion.
The purpose of this study was to prepare and characterize solid dispersions of nimodipine with hydroxypropyl methylcellulose (HPMC, Methocel E5), polyvinylpyrrolidone/vinyl acetate copolymer (PVP/VA, Plasdone S630), and ethyl acrylate, methyl methacrylate polymer (Eudragit EPO). The goal was to investigate whether the solid dispersion prepared by hot-melt extrusion can improve the dissolution rate of nimodipine. The dissolution results indicated that three polymers are suitable carriers to enhance the in vitro dissolution rate of nimodipine in pH 4.5 medium. The solubility research and solubility parameters calculation was corresponded with dissolution data. XRPD and DSC data showed that the crystallinity was not observed in hot-melt extrudates. NMD acted as a plasticizer for PVP/VA and EPO and was miscible with the polymers as well as 10% NMD-HPMC systems, because a single T(g) was observed in these extrudates. However, two T(g)s were observed in the 30 and 50% NMD-HPMC samples, indicating phase separation. The weakening and shift of the N-H stretching vibration of the secondary amine groups of nimodipine as determined by FT-IR proved hydrogen bonding between the drug and polymers in the solid dispersion.
Zheng
Xin
X
Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning, P.R.China.
Yang
Rui
R
Tang
Xing
X
Zheng
Liangyuan
L
D000179:Acrylates / Q000737:chemistry; D002121:Calcium Channel Blockers / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers / Q000737:chemistry*; D006860:Hydrogen Bonding; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D008768:Methylmethacrylates / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D009553:Nimodipine / Q000737:chemistry*; D044367:Phase Transition; D010968:Plasticizers; D011108:Polymers / Q000737:chemistry*; D011759:Pyrrolidines / Q000737:chemistry; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D044366:Transition Temperature; D014753:Vinyl Compounds / Q000737:chemistry; D014961:X-Ray Diffraction
D000179:Acrylates; D002121:Calcium Channel Blockers; D004337:Drug Carriers; D008768:Methylmethacrylates; D010968:Plasticizers; D011108:Polymers; D011759:Pyrrolidines; D014753:Vinyl Compounds; C402301:poly(vinylpyrrolidone-co-vinyl-acetate); D065347:Hypromellose Derivatives; D009553:Nimodipine; C040833:ethyl acrylate; D008747:Methylcellulose