Evidence map›Paper›PMID 32523332›Full record

ArticleDrug design, development and therapy2020

Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug.

Usama Farghaly Aly, Hatem Abdel-Monsef Sarhan, Taha F S Ali, Hosny Abd El-Bakey Sharkawy

Abstract read
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Article in Drug design, development and therapy, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

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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

4 authors.

Usama Farghaly AlyDepartment of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt.
Hatem Abdel-Monsef SarhanDepartment of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt.
Taha F S AliDepartment of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia, Egypt.ORCID 0000-0002-8881-0408
Hosny Abd El-Bakey SharkawyDepartment of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeThe objective of this study was to compare different techniques to enhance the solubility and dissolution rate, and hence the bioavailability of candesartan cilexetil.

methodsTo achieve this target, various techniques were employed such as solid dispersions, inclusion complexes, and preparation of candesartan nanoparticles. Following the preparations, all samples were characterized for their physicochemical properties, and the samples of the best results were subjected to further bioavailability studies.

resultsResults of dissolution studies revealed an increase in the dissolution rate of all samples. The highest dissolution rate was achieved using solid dispersion of the drug with PVP K-90 (1:4). Physicochemical investigations (XR, DSC, and FT-IR) suggested formation of hydrogen bonding and changing in the crystalline structure of the drug. Regarding the inclusion complexes, more stable complex was formed between HP-β-CD and CC compared to β-CD, as indicated by phase solubility diagrams. Antisolvent method resulted in the preparation of stable nanoparticles, as indicated by ζ potential, with average particle size of 238.9 ± 19.25 nm using PVP K-90 as a hydrophilic polymer. The best sample that gave the highest dissolution rate (CC/PVP K-90 1:4) was allowed for further pharmacokinetic studies using UPLC MS/MS assay of rabbit plasma. Results showed a significant increase in the bioavailability of CC from ~15% to ~48%.

conclusionThe bioavailability of CC was significantly improved from ~15% to ~48% when formulated as SDs with PVP K-90 with 1:4 drug:polymer ratio.

Indexed as

AnimalsAntihypertensive AgentsBenzimidazolesBiological AvailabilityBiphenyl CompoundsMaleMolecular StructureNanoparticlesParticle SizeRabbitsSolubilitySurface PropertiesTetrazolesAntihypertensive AgentsBenzimidazolesBiphenyl Compoundscandesartan cilexetilTetrazolesinclusion complexnanoparticlespharmacokineticssolid dispersionUPLC MS/MS

Identifiers

PMID32523332
PMCPMC7234962

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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.