Preparation and Characterization of Solid Dispersion of Total Flavonols from Resina Draconis

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1 37 1 Vol37 No Journal of South-Central University for NationalitiesNatSciEdition Mar2018 * RDF K30PVP K30 188F68 X XRD IR DSC SEM TFDB PVP K30 F F68 K TQ461 A 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 China 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 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 * zhaohaiyan01@ sinacom pharmawang@ sinacom CFB181 BZY14035 CZZ15006

2 62 37 PVP K RDF 95% 9 K30 PVP K F68 RDF Lambda 35 Perkin Elmer CP214 78X-3A XC 100 r 獉 min -1 37±05 ZKXFB ml NICOLET 6700 Thermo Scientific min 4 ml022 μm SEM SU-8010 Hitachi X XRD D8 Bruker B X XRD RDF δpvp K % 188F68= 81 X BASF WPCI514B DSC RDF mg 10 獉 min -1 0 ~ IR RDF 12 PVP K30 F68 RDF 220 ~ 400 nm 277 nm RDF SEM RDF μg 獉 ml -1 B c A A = c r = B 124 ~ 124 μg 獉 ml F68PEG 4000 TFDB 14 RDF 82 mg 2010 RDF 5461% K30 5 ~ 80 Cu 50 kv 200 ma 2θ 2 21 RDF 18 RDF 95%

3 1 63 PEG4000 PVP K PVP K30 Fig1 1 RDF Dissolution curves of TFDB solid dispersions with different carriers PVP K30 F F68 PVP K30 RDF 12 RDF F68 11 SDS Na 2 HPO 4 PVP K RDF 2 2 PVP K 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 PVPK F68 δrdfpvp K30= 18 F68 RDF Fig 4 F68 Dissolution curves of solid dispersions with different proportions of F68 23 RDF PVP K30 F min PVP K30 F PVP K30 F68 δrdff68= 11 PVP K30 PVP K30 RDF 30 min 3 3 PVP K30 δrdfpvp K30= 18 PVP K30

4 Fig 5 RDF TFDB Dissolution curves ofrdfphysical mixture and solid dispersions X XRD XRD 66 RDF PVP K30 F68 12 F68 F68 7 Fig7 RDF DSC DSC pattern of RDFphysical mixtures and solid dispersions == O RDF TFDB 6 Fig6 RDF XRD XRD pattern of RDFphysical mixtures and solid dispersions 242 DSC DSC 7 7 RDF F68 13 RDF 108 PVP K F68 F68 43 F IR 81 RDF RDF IR 8 RDF XRD IR DSC 8 RDF 3463 cm -1 OH 1662 cm -1 C == O PVP K cm -1 O H 1662 cm -1 C Fig RDF 4 5F686PVP K30 RDF IR IR spectrum of RDFphysical mixtures and solid dispersions 244 SEM SEM F68 PVP K30 RDF 3 PVP K SEM

1 65 a btfdbc d e f 23/241068-1075 9 RDF SEM 10Sharma AJain C P Solid dispersiona promising Fig9 SEM results of RDFphysical mixtures and solid dispersions technique to enhance solubility of poorly

5 1 65 a btfdbc d e f 23/ RDF SEM 10Sharma AJain C P Solid dispersiona promising Fig9 SEM results of RDFphysical mixtures and solid dispersions technique to enhance solubility of poorly water soluble drug J Int J Drug Deliv RDF RDF 11 J Sancheti P PVyas V MShah Met al Development and characterization of bicalutamide-poloxamer F68 solid dispersion systems J Pharmazie J J J Bikiaris D N Solid dispersionspart Irecent evolutions and future opportunities in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs J Expert Opin Drug Deliv Vasconcelos TSarmento BCosta Pet al Solid dispersions as strategy to improve oral bioavailability of poor water souble drugs J Drug discov Today Fini ACavallari COspitali Fet al Raman and thermal analysis of indomethacin/ PVP solid dispersion enteric 1 microparticles J Eur J Pharm Biopharm J Sethia SSquillante E Solid dispersion of carbamazepine 2 J in PVP K30 by conventional solvent evaporation and supercritical methods J Int J Pharm HPLC J 15Tapas A R Ingle V PKawtikwar P Set al Enhanced dissolution profile and antihyperlipedimic activity of 4 simvastatin by solid dispersion with pluronic F68J J Drug Deliv Lett

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