ABSTRACT
To prepare the hawthorn leaves flavonoids self-microemulsifying membrane controlled-release coated drop pill, and to study its release rate in vitro and pharmacokinetics study in vivo. In order to improve the dissolution of hawthorn leaves flavonoids, self-microemulsifying technology was used to prepare the hawthorn leaves flavonoids self-microemulsion. Hawthorn leaves flavonoids self-microemulsifying drop pill was prepared with the PEG 6000. Studies were made on the in vitro release of flavonoids from hawthorn leaves self-micro-emulsifying membrane-moderated coated drop pills and the in vivo pharmacokinetic in rats. The prescription of flavonoids from hawthorn leaves self-micro-emulsifying drop pills was 0.25 g of flavonoids from hawthorn leaves, 0.25 g of iodophenyl maleimide, 0.375 g of polyethylene glycol 400, 0.375 g of cremophor RH 40 and 2 g of polyethylene glycol 6000. The optimized prescription was 4 g of ethyl cellulose 20, 0.64 g of polyethylene glycol 400, 1.8 g of diethyl phthalate, and the weight of coating materials increased by 3.5%. Flavonoids from hawthorn leaves self-micro-emulsifying membrane-moderated coated drop pills complied with the design of sustained-release in 12 h in terms of in vitro release and in vivo pharmacokinetic parameters in rats, and its bioavailability was 2.47 times of quick-release drop pills. Slightly soluble flavonoids from hawthorn leaves could be made into sustained-release preparations by the self-micro-emulsifying and coating technology.
Subject(s)
Crataegus/chemistry , Delayed-Action Preparations/pharmacokinetics , Drugs, Chinese Herbal/pharmacokinetics , Flavonoids/pharmacokinetics , Animals , Chemistry, Pharmaceutical , Delayed-Action Preparations/chemistry , Drugs, Chinese Herbal/chemistry , Flavonoids/chemistry , Male , Plant Leaves/chemistry , Rats , Rats, Sprague-DawleyABSTRACT
OBJECTIVE: To establish an optimum enrichment and purification process of total flavonoids in Microcos paniculata by macroporous resins. METHODS: Five kinds of resins were compared and the best one was chosen. Then the parameters of the process were optimized by single factor tests, uniform design and statistical methods. RESULTS: DI01 was selected for its excellent adsorption and desorption properties, 70% ethanol was found to be the best elution solution. As far as the yield was considered, the best result was based on the followings: feed rate-1.0 BV/h, elution flow rate-2.0 BV/h, sample concentration-7.88 mg/mL, eluting agent amount-2.0 BV, pH value 4.8; then the yield reached 90.18% and the purity was 54.37%. If the purity was considered, the best parameters wereas follows: feed rate-1.0 BV/h, elution flow rate-2.0 BV/h, sample concentration-2.0 mg/mL, eluting agent amount-2.8 BV, pH value 7.8; then the purity reached 61.77% and the yield was 80.25%. CONCLUSION: The total flavonoids of Microcos paniculata can be effectively purificated and separated by D101 macroporous resin.
Subject(s)
Flavonoids/isolation & purification , Plants, Medicinal/chemistry , Resins, Synthetic/chemistry , Technology, Pharmaceutical/methods , Tiliaceae/chemistry , Adsorption , Chromatography, High Pressure Liquid/methods , Ethanol/chemistry , Hydrogen-Ion Concentration , Plant Leaves/chemistry , Spectrophotometry, UltravioletABSTRACT
AIM: To study the chemical constituents of Paeonia lactiflora. METHODS: The constituents of P. lactiflora were separated by using various kinds of modern chromatography and was identified its structure on the basis of spectral analysis. RESULTS: A monoterpene glucoside named albiflorin R1 was isolated from the roots of Paeonia lactiflora Pall. In the structure of albiflorin R1, the aglycone connected with a glucose at its 2-OH while the hemiacetal hydroxyl in glucose moiety was free. CONCLUSION: Albiflorin R1 is a new monoterpene glycoside.
