Pharmacokinetics and correlation between in vitro release and in vivo absorption of bio-adhesive pellets of panax notoginseng saponins

doi:10.1016/S1875-5364(17)30029-8

Chinese Journal of Natural Medicines

Volume 15, Issue 2, February 2017, Pages 142-151

https://doi.org/10.1016/S1875-5364(17)30029-8 Get rights and content

Abstract

The present study was designed to prepare and compare bio-adhesive pellets of panax notoginseng saponins (PNS) with hydroxy propyl methyl cellulose (HPMC), chitosan, and chitosan : carbomer, explore the influence of different bio-adhesive materials on pharmacokinetics behaviors of PNSbio-adhesive pellets, and evaluate the correlation between in vivo absorption and in vitro release (IVIVC). In order to predict the in vivo concentration-time profile by the in vitro release data of bio-adhesive pellets, the release experiment was performed using the rotating basket method in pH 6.8 phosphate buffer. The PNS concentrations in rat plasma were analyzed by HPLC-MS-MS method and the relative bioavailability and other pharmacokinetic parameters were estimated using Kinetica4.4 pharmacokinetic software. Numerical deconvolution method was used to evaluate IVIVC. Our results indicated that, compared with ordinary pellets, PNS bio-adhesive pellets showed increased oral bioavailability by 1.45 to 3.20 times, increased C_max, and extended MRT. What's more, the release behavior of drug in HPMC pellets was shown to follow a Fickian diffusion mechanism, a synergetic function of diffusion and skeleton corrosion. The in vitro release and the in vivo biological activity had a good correlation, demonstrating that the PNS bio-adhesive pellets had a better sustained release. Numerical deconvolution technique showed the advantage in evaluation of IVIVC for self-designed bio-adhesive pellets with HPMC. In conclusion, the in vitro release data of bio-adhesive pellets with HPMC can predict its concentration-time profile in vivo.

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This indicates that ginsenoside monomers such as Rb1 and Rg1 can be hydrolyzed by acidic environment in stomach and metabolized by intestinal enzymes, resulting in their decreased oral bioavailability. However, the enteric coating and controlled release coating of Panax notoginseng saponins pellets can cause the pellets to have a sustained release effect thus readily improving the bioavailability [19–21]. The studies [19–21] used R1, Rb1, and Rg1 as detection indicators to study the in vitro release and pharmacokinetics of Panax notoginsenoside preparations.
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Available online 20 Feb. 2017

[Research funding] This work was supported by the National Natural Science Foundation of China (No. 81274094).

These authors have no conflict of interest to declare.

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Pharmacokinetics and correlation between in vitro release and in vivo absorption of bio-adhesive pellets of panax notoginseng saponins

Abstract

J Ethnopharmacol

J Ethnopharmacol

J Funct Foods

J Ethnopharmacol

J Ethnopharmacol

Int J Pharm

Eur J Pharm Biopharm

Eur J Oper Res

J Chromatogr B

J Chromatogr B

J Chromatogr B

J Pharmaceut Biomed

J Pharmat Biomed

Fitoterapia

J Chromatogr B

Absorption profiles of sanchinoside Rl and ginsenoside Rgl in the rat intestine [J]

Eur J Drug Metab PH