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)
Animals , Male , Rats , Chemistry, Pharmaceutical , Crataegus , Chemistry , Delayed-Action Preparations , Chemistry , Pharmacokinetics , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Flavonoids , Chemistry , Pharmacokinetics , Plant Leaves , Chemistry , Rats, Sprague-DawleyABSTRACT
<p><b>AIM</b>To study the chemical constituents of Paeonia lactiflora.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>Albiflorin R1 is a new monoterpene glycoside.</p>