Evidence map›Paper›PMID 34145531›Full record

ArticlePharmaceutical research2021

Prediction of Free Drug Absorption in Cyclodextrin Formulation by a Modified Physiologically Based Pharmacokinetic Model and Phase Solubility 3-D Surface Graph.

Wei Wang, Defang Ouyang

Abstract read
PubMed Publisher
In one paragraph

Article in Pharmaceutical research, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.5field-weighted citation impact, top 42% of its field
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

2 citing papers in PubMed, 11 citations in OpenAlex.

  1. Review
  2. 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

2 authors at 1 institution in 1 country.

Wei WangInstitute of Chinese Medical Sciences, University of Macau, Macau, China.
Defang OuyangInstitute of Chinese Medical Sciences, University of Macau, Macau, China. defangouyang@um.edu.mo.ORCID http://orcid.org/0000-0002-8052-4773
University of Macau · MO

Funding

Macau FDCT Research Grant FDCT/0029/2018/A1Universidade de Macau MYRG2019-00041-ICMS
6 · The paper itself

Abstract

purposeCyclodextrin (CD) is commonly used to enhance the solubility of oral drugs. However, with the increase of CD concentrations, the fraction of free drug molecules decreases, which may potentially impede drug absorption. This study aims to predict the optimal ratio between drug and CD to achieve the best absorption efficiency by computational simulation.

methodsFirst, a physiologically based pharmacokinetic (PBPK) model was developed. This model can continuously adjust absorption according to free drug fraction and was validated against two model drugs, progesterone (PG) and andrographolide (AG). The further analysis involves 3-D surface graphs to investigate the relationship between free drug amount, theoretically absorbable concentration, and contents of drug and CD in the formulation.

resultsThe PBPK model predicted the PK behavior of two drugs well. The concentration ratio of drug to CD, leading to maximal free drug amount and the best absorption efficiency, is nearly the same as the slope determined in the phase solubility test. The new modified PBPK model and 3-D surface graph can easily predict the absorption difference of formulations with various drug/CD ratios.

conclusionThis PBPK model and 3-D surface graph can predict the absorption and determine the optimal concentration ratio of CD formulation, which could accelerate the R&D of CD formulation.

Indexed as

Intestinal AbsorptionModels, BiologicalAdministration, OralChemistry, PharmaceuticalComputer SimulationCyclodextrinsDiterpenesDrug CompoundingExcipientsHumansProgesteroneSolubilitySurface PropertiesandrographolideCyclodextrinsDiterpenesExcipientsProgesteronecyclodextrinfree fractionPBPKphase solubility

Identifiers

PMID34145531
OpenAlexW3169461714

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

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.