Imperatorin sustained-release tablets: In Vitro and pharmacokinetic studies.

by DrSteve on September 8, 2010

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Dr.Steve’s BOTTOM LINE: Angelica is a genus with about 50 species within and Angelica dahurica is within this grouping, known as bai zhi in Chinese.  It is known as an anti-inflammatory and has antiobiotic properties, among other uses including immune modulation and blood pressure lowering effects.  Imperatorin is an active single derivative of this herb and has anti-HIV effects as well as effects on abnormal heart muscle thickening (hypertrophy), but can also have some neurotoxic effects.

The point here is that this small study has looked into isolating and possibly improving the delivery of this potentially beneficial derivative.  This again raises the question regarding the consumption of herbs which may cause BOTH beneficial and adverse effects vs. isolating and trying to focus the effects, while trying to eliminate the toxic parts. A work in progress and certainly not agreed upon by those in the natural healing arts, but is a potential avenue nonetheless……

Imperatorin sustained-release tablets: In Vitro and pharmacokinetic studies.

Arch Pharm Res. 2010 Aug;33(8):1209-16

Authors: Pan J, Lu W, Li C, Wang S, He L

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.

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