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Effect of paracellular permeation enhancers on intestinal permeability of two peptide drugs,enalaprilat and hexarelin, in rats

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Acta Pharmaceutica Sinica B 2021年第6期11卷 1667-1675页

作者： David Dahlgren Tobias Olander Markus Sjoblom Mikael Hedeland Hans Lennernas Department of pharmaceutical Biosciences Translational Drug Discovery and DevelopmentUppsala UniversityUppsala 75236Sweden Department of Neuroscience Division of PhysiologyUppsala UniversityUppsala 75236Sweden Department of Medicinal Chemistry Analytical Pharmaceutical ChemistryUppsala UniversityUppsala 75236Sweden Department of Chemistry Environment and Feed HygieneNational Veterinary Institute(SVA)Uppsala 75189Sweden

Transcellular permeation enhancers are known to increase the intestinal permeability of enalaprilat,a 349 Da peptide,but not hexarelin(887 Da).The primary aim of this paper was to investigate if paracellular permeability enhancers affected the intestinal permeation of the two *** was investigated using the rat single-pass intestinal perfusion model with concomitant blood *** luminal compositions included two paracellular permeation enhancers,chitosan(5 mg/mL) and ethylenediaminetetraacetate(EDTA,1 and 5 mg/mL),as well as low luminal tonicity(100 mOsm) with or without *** were evaluated by the change in lumen-to-blood permeability of hexarelin and enalaprilat,and the blood-to-lumen clearance of ^(51)chromium-labeled EDTA(CL_(Cr-EDTA)),a clinical marker for mucosal barrier *** two paracellular permeation enhancers increased the mucosal permeability of both peptide drugs to a similar *** data in this study suggests that the potential for paracellular permeability enhancers to increase intestinal absorption of hydrophilic peptides with low molecular mass is greater than for those with transcellular ***,the mucosal blood-to-lumen flux of ^(51)Cr-EDTA was increased by the two paracellular permeation enhancers and by luminal *** contrast,luminal hypotonicity did not affect the lumen-to-blood transport of enalaprilat and *** suggests that hypotonicity affects paracellular solute transport primarily in the mucosal crypt region,as this area is protected from luminal contents by a constant water flow from the crypts.

关键词： Permeation enhancers Absorption-modifying excipients Oral peptide delivery Intestinal permeability Intestinal perfusion pharmaceutical development

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Comprehensive analysis of antibacterial and anti-hepatoma activity of metabolites from jujube fruit

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Food Bioscience 2022年第3期47卷 474-483页

作者： Qianqian Shi Xi Li Dajun Zhu Junjun Jiang Xingang Li College of Forestry Northwest A&F UniversityYangling712100ShaanxiChina Key Comprehensive Laboratory of Forestry of Shaanxi Province Northwest A&F UniversityYangling712100ShaanxiChina Research Center for Jujube Engineering and Technology of State Forestry Administration Northwest A&F UniversityYangling712100ShaanxiChina

Jujube is one of the most produced dried fruits in China,and it is also a traditional Chinese medicine that enhances immunity and has anti-cancer *** fruit is rich in phenolic compounds,but few reports are available on its biological *** evaluate the biological activities of the phenolic compounds in dried jujube fruit,the composition and content of metabolites in dried jujube fruit were determined by metabolomics,and the antibacterial and anticancer activities of the phenolic compounds were analyzed in dried jujube *** results showed that 463 compounds were identified in dried‘Junzao’fruit,including 102 phenolic *** in vitro activity test showed that the jujube phenolic metabolites had extensive antibacterial effects and caused disruption and nuclear sclerosis of hepatocellular carcinoma(HepG2)*** correlation analysis showed that total phenolic content,quercetin-3-rutinose,and procyanidin B1 were the main active antibacterial and anticancer *** study provides data supporting the application of dried jujube fruit in the development of functional foods,pharmaceuticals and cosmetics.

关键词： Anticancer activity HepG2 cell Phenolic metabolites Chinese jujube pharmaceutical development

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Genotoxic(mutagenic) impurities in pharmaceuticals-a historical perspective on ICH M7

Genotoxic(mutagenic) impurities in pharmaceuticals-a histori...

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中国毒理学会第七次全国毒理学大会暨第八届湖北科技论坛

作者： Jianxun(Jack) Xie Lutz Mueller Roche Innovation Center

The qualification approach of ICH Q3A/B is appropriate for "ordinary" drug-related impurities but inappropriate for unusually toxic(DNA reactive) *** M7 guideline is to provide a practical framework that is applicable to the identification,categorization,qualification,and control of these mutagenic impurities to limit potential carcinogenic *** guideline went to Step 4(finalized) on Jun 23 rd 2014 and currently is in Step 5 of implementation *** to the complexity of guideline,it requires adjustments of processes in companies and Health *** general,application of this guideline in ICH regions is expected before the end of *** Europe,discussion of genotoxic impurities in pharmaceutical was triggered by differences in risk assessment approach between different EU member state agencies,but not triggered by pharmaceutical industry in early 21 *** US,problematic situation for industry emerged in 2004 when FDA issued several clinical holds based on issues with genotoxic impurities in clinical *** and then staged threshold of toxicological concern(TTC) approach for clinical trials was developed to define an acceptable intake for any unstudied chemical that poses a negligible risk of carcinogenicity or other toxic effects and mutually agreed in both *** M7 was then *** insufficient toxicological data is available for most genotoxic impurities in pharmaceuticals,which could serve as basis for a proper risk assessment,TTC as a pragmatic risk assessment tool that is based on the principle of establishing a human exposure threshold for all chemicals below which there is no appreciable risk of an event(eg cancer) occuring over a lifetime intake TTC could be *** methods upon which the TTC is based are generally considered to be very conservative since they involve a simple linear extrapolation from the dose giving a 50%tumor incidence(TD50) to a 1 in 10 incidence,using TD50 data for the most sensitive

关键词： Genotoxic impurity ICH M7 threshold of toxicological concern(TTC) pharmaceutical development risk assessment

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