37 1 Vol37 No1 2018 3 Journal of South-Central University for NationalitiesNatSciEdition Mar2018 * 430074 RDF K30PVP K30 188F68 X XRD IR DSC SEM TFDB PVP K30 F68 181 F68 K30 188 TQ461 A 1672-4321201801-0061-05 Preparation and Characterization of Solid Dispersion of Total Flavonols from Resina Draconis Wang ShaobingLuo LingTian BingCao BingbingHe JiandanZhao Haiyan School of Pharmaceutical SciencesSouth-Central University for NationalitiesWuhan 430074China Abstract In order to prepare the solid dispersion of total flavonols from Resina Draconis the dissolution was improved and the solid dispersion was characterized Three-phase solid dispersions were prepared by using polyvinylpyrrolidone K30 PVP K30and poloxamer 188 F68as the excipients Then the solid dispersion was prepared by in vitro dissolution test and the performance of the solid dispersion was characterized by XRDIRDSC and SEM The results showed that the formulation of the solid dispersion was seleted as TFDB /PVP K30 /F68 with a mass ratio of 1 8 1 No interaction occurred between the drug and the carrier materialsand the improvement of the drug dissolution was mainly attributed to the decreasing size of the drug in solid dispersion and the madefaction and solubilization of F68 So the ternary solid dispersion technique can significantly increase in vitro dissolution of TFDBwhich pay a theoretical foundation for improving the dissolution of the insoluble ingredients of traditional Chinese medicine Keywords Resina Draconis flavonesternary solid dispersionin vitro dissolutionpvp K30poloxamer 188 1 2 3 4-6 7 2016-12-28 * E-mailzhaohaiyan01@ sinacom 1977- E-mailpharmawang@ sinacom 81101144 2015CFB181 BZY14035 CZZ15006
62 37 PVP K30 60 8 100 - RDF 95% 9 K30 PVP K30 60 100 188F68 RDF 100 1 11 Lambda 35 Perkin Elmer CP214 78X-3A XC 100 r 獉 min -1 37±05 ZKXFB-2 1000 ml NICOLET 6700 Thermo Scientific5 10 30 60 90 150 min 4 ml022 μm SEM SU-8010 Hitachi X XRD D8 Bruker B X XRD RDF δpvp K30 98 5% 188F68= 81 X BASF WPCI514B 20110221 20141125 4000 20130618 20150108 DSC RDF 20140520 5 mg 10 獉 20150410 min -1 0 ~ 200 20140927 IR RDF 12 PVP K30 F68 RDF 220 ~ 400 nm 277 nm RDF SEM RDF 1 24 248 496 744 992 124 μg 獉 ml -1 B c A A = 50 3038 c 00219 r = 09995 B 124 ~ 124 μg 獉 ml -1 13 F68PEG 4000 TFDB 14 RDF 82 mg 2010 RDF 5461%15 20140311 K30 5 ~ 80 Cu 50 kv 200 ma 2θ 2 21 RDF 18 RDF 95%
1 63 PEG4000 PVP K30 1 1 PVP K30 Fig1 1 RDF Dissolution curves of TFDB solid dispersions with different carriers PVP K30 F68 105 11 F68 PVP K30 RDF 12 RDF F68 11 SDS Na 2 HPO 4 PVP K30 1 10 RDF 2 2 PVP K30 188 188 10 PVP K30 F68 4 RDF 2 Fig2 RDF Dissolution curves of RDF solid dispersions with different surfactants 22 - δrdfpvp K30= 18 3 Fig 3 PVP K30 Dissolution curves of solid dispersions with different proportions of PVPK30 222 F68 δrdfpvp K30= 18 F68 RDF 05 1 2 4 4 Fig 4 F68 Dissolution curves of solid dispersions with different proportions of F68 23 RDF PVP K30 F68 181 5 5 11 30 min PVP K30 F68 221 PVP K30 F68 δrdff68= 11 PVP K30 PVP K30 RDF 30 min 3 3 PVP K30 δrdfpvp K30= 18 PVP K30
64 37 5 Fig 5 RDF 1 2 34TFDB Dissolution curves ofrdfphysical mixture and solid dispersions 24 241 X XRD XRD 66 RDF 20 18 23 2 PVP K30 F68 12 F68 F68 7 Fig7 RDF DSC DSC pattern of RDFphysical mixtures and solid dispersions == O RDF 1 2 34TFDB 6 Fig6 RDF XRD XRD pattern of RDFphysical mixtures and solid dispersions 242 DSC DSC 7 7 RDF 48 2000 F68 13 RDF 108 PVP K30 14 15 46 F68 F68 43 F68 243 IR 81 RDF RDF IR 8 RDF XRD IR DSC 8 RDF 3463 cm -1 OH 1662 cm -1 C == O PVP K30 3463 cm -1 O H 1662 cm -1 C Fig8 8 1 2 3RDF 4 5F686PVP K30 RDF IR IR spectrum of RDFphysical mixtures and solid dispersions 244 SEM SEM 9 9 500 F68 PVP K30 RDF 3 PVP K30 188 SEM
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