Evidence map›Paper›PMID 28000173›Full record

ArticleEuropean journal of drug metabolism and pharmacokinetics2017

In Vitro Evaluation of Absorption Characteristics of Peramivir for Oral Delivery.

Ying Li, Zhiyuan Wang, Xin Li, Wei Gong, Xiangyang Xie, Yang Yang, Wu Zhong, Aiping Zheng

Abstract read
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In one paragraph

Article in European journal of drug metabolism and pharmacokinetics, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

5 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Review
  5. Synthesis and Biological Evaluation ofMolecules (Basel, Switzerland) · 2019
    Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

8 authors.

Ying LiBeijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing, 100850, China. liying.sky@126.com.
Zhiyuan WangBeijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing, 100850, China.
Xin LiDepartment of Pharmacy, Chinese PLA General Hospital, 28 Fuxing Road, Beijing, 100853, China.
Wei GongBeijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing, 100850, China.
Xiangyang XieDepartment of Pharmacy, Wuhan General Hospital of Guangzhou Military Command, 627 Wuluo Road, Wuchang District, Wuhan, 430070, China.
Yang YangBeijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing, 100850, China.
Wu ZhongBeijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing, 100850, China.
Aiping ZhengBeijing Institute of Pharmacology and Toxicology, 27 Taiping Road, Beijing, 100850, China.

Funding

Beijing Natural Science Foundation 7162148National Natural Science Foundation of China 81102498National Natural Science Foundation of China (CN) 81573357
6 · The paper itself

Abstract

BACKGROUND AND

objectivePeramivir is a novel antiviral agent approved for the treatment of severe influenza. However, the development of oral formulation of peramivir has been severely hurdled by poor bioavailability (human, ≤3%). The present work aims to evaluate oral permeability characteristics of peramivir.

methodsIn vitro gastrointestinal stability, metabolic stability in human intestinal S9 fraction and Caco-2 permeability were performed. The liquid chromatography with tandem mass spectrometric (LC-MS/MS) was used to quantify peramivir in buffer and biological sample. Using GastroPlus™ software, intestinal effective permeability coefficient (P

resultsOur results indicated that peramivir maintained stability in pH 5.5 and 7.4 buffers, fasted state simulated gastric fluid and fasted state simulated intestinal fluid, and human intestinal S9 fractions. The apparent permeability coefficient (P

conclusionsThese results revealed that carrier-mediated transports, including OATP1B (organic anion transport 1B) and OCT1 (organic cation transport 1), might be involved in the absorption of peramivir. In conclusion, our results provide insight into the poor oral bioavailability of peramivir. Peramivir can be classified as a BCS-III (high solubility/low permeability) and BDDCS-III high solubility/poor metabolism) drug. The oral bioavailability of peramivir primarily depends on its permeability across cell membranes. Both of passive and active transports are involved in the permeability of peramivir.

Indexed as

Acids, CarbocyclicAdministration, OralAntiviral AgentsBiological AvailabilityBiological TransportCaco-2 CellsCell Line, TumorCyclopentanesGuanidinesHumansIntestinal AbsorptionIntestinal MucosaPermeabilitySolubilityAcids, CarbocyclicAntiviral AgentsCyclopentanesGuanidinesperamivirBreast Cancer Resistance ProteinInfluenzaOseltamivirParoxetineZanamivir

Identifiers

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Registered trials

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.