orabase and imperatorin

To screen the matrix and permeation enhancer of Duliang Patches.. Based on L9 (3(4)) orthogonal experimental design, the content of imperatorin of the release rate and transdermal osmolality were regarded as evaluation indexes to optimize the matrix and permeation enhancer of patches suing of Drug dissolution tester and Franz diffusion cell.. The best prescriplion of sustained-release patch of Duliang was: the quality percentage content of the starch, sodium carboxymethyl cellulose, glycerin, azone, propylene glycol and PEG400 was 6%, 2%, 30%, 1%, 15% and 2.5% respectively. The release behavior of sustained-release patches of Duliang tallied with Higuchi equation and the effect of sustained-release was apparent.. The sustained-release patches of Duliang have good property of sustained-release and transdermal in vitro and the stability of patches is also sound while the release in vivo awaits further inspection.

Topics: Animals; Carboxymethylcellulose Sodium; Chemistry, Pharmaceutical; Delayed-Action Preparations; Drugs, Chinese Herbal; Furocoumarins; Glycerol; Male; Mice; Plants, Medicinal; Propylene Glycol; Skin; Skin Absorption; Solubility; Transdermal Patch

We prepared and evaluated imperatorin (IMP) sustained-release tablets. IMP is an active compound in Angelica dahuricae, a Chinese herbal medicine. We used different polymers, such as hydroxypropyl methylcellulose (HPMC K4M, K15M, and K100M), carbopol 934P, sodium carboxymethyl cellulose (CMC-Na), and their combinations to prepare the matrix tablets and achieve the desired sustained release profile. The in vitro release profiles of these formulations were examined and fit to various kinetic release models. We also tested the effects of polymer combination ratios on the in vitro release rate. In vivo studies were performed for the optimized formulation in six beagle dogs, and pharmacokinetic parameters were compared with plain IMP tablets. IMP sustained-release tablets exhibited a more sustained plasma concentration than the plain tablets, with a relative bioavailability of 127.25%. The in vitro releases rates and in vivo absorption correlated for the initial 8 hours. These results demonstrate that the sustained-release tablet system can effectively control the release of IMP.

Topics: Acrylates; Angelica; Animals; Biological Availability; Carboxymethylcellulose Sodium; Delayed-Action Preparations; Dogs; Drug Carriers; Drugs, Chinese Herbal; Furocoumarins; Hypromellose Derivatives; Male; Methylcellulose; Polymers; Tablets; Time Factors