| Objective:Guipiwan composed of ten herbs such as Radix Codon opsis, Atractylodes macrocephala, Astragalus, etc.has strengthening spleen and nourishing heart Efficacy and Yiqi Buxue efficacy for eating less and tired body, pale chlorosis, forgetful insomnia, hear t palpitations and all kinds of hemorrhagic disease.Ultra-fine pow der technology for compound preparation can enhance the content of the active ingredients in pharmaceutical preparations,dissolution rate, bioavailability and clinical efficacy. In this paper, ultra-fine p owder technology applies to preparation of Guipiwan with a view to improve bioavailability and clinical efficacy, and advanced quali ty control of ultra-fine Guipiwan, apply experimental data for the clinical application.Methods:By comparing dissolution and bioavailability of effective ingredient, efficacy in animal vivo between the ultra-fine guipiwa n prepared by ultra-fine powder technology and the ordinary guipi wan, advanced quality control of ultra-fine guipiwan,apply experi mental data for the clinical application.1.The determination of di ssolution of Ferulic acid in vitro:Ferulic acid as a target index, determinated with HPLC and compared with ordinary guipiwan.2. Experimental research on bioavailability and pharmacokinetic para meters:selected HPLC-MS/MS as a good exclusive, high sensitivit y method determined concentration of the ferulic acid in rabbit pla sma.3.Pharmacodynamic Study:To observe the effect of ultra-fin e guipiwan on sub-acute aging mouse model induced by high dose D-galactose injection and the rats models of deficiency in both Qi and blood by determining superoxide dismutase (SOD), gl utathione peroxidase (GSH-Px) and malondialdehyde (MDA) in br ain and liver tissues and to compare with ordinary Guipiwan.Results:Through comparative study of Comparative in vitro dissol ution on the ordinary Guipiwan and ultra-fine Guipiwan, Show tha t the differences of TD and T50 between the ultra-fine Guipiwan a nd the ordinary Guipiwan have statistical significance;The TD and T50 of ferulic acid in the ultra-fine Guipiwan were lower than the ordinary Guipiwan, T50 of ultra-fine guipiwan was 10.80±0.28,TD was 18.58±0.52 and the ordinary T50 is 14.55±0.58,TD is 24.75±0.75.Pharmacokinetics study in rabbits found that the relative bioa vailability between ultra-fine guipiwan and ordinary guipiwan is 1. 47,it illustrate that after changed preparation process,at the same dosage, bioavailability of ultra-fine guipiwan is 1.47 times than t he ordinary guipiwan. By study the effects on sub-acute aging mo use model,it showed that guipiwan can enhance the SOD, GSH-P x levels and lower the MDA content, and have an impact on orga n index about thymus, liver, spleen of mouse.At the same dose, t he pharmacological effects of ultra-fine guipiwan had on the sub-a cute aging mice were stronger than that of ordinary guipiwan.Conclusion:By using Ultra-fine powder technology in the preparat ion of guipiwan, it could improve the extract, the active ingredient rate of extraction and in vitro dissolution. Through comparative a nimal experiments study, it has compared with the effects of ordin ary guipiwan and ultra-micro guipiwan on the aging mice model a nd its pharmacological effects in vivo bioavailability at the rabbit, and the study show that the ultra-fine powder technology in the p reparation of guipiwan can improve bioavailability in rabbit and th e experimental efficacy on animal mice models.The study has pro vided experimental data for the application of ultra-fine powder te chnology in ordinary Chinese medicine, compound preparation and has provided the experimental basis for enhance its clinical effica cy. |
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