Evidence map›Paper›PMID 33217948›Full record

ArticlePharmaceutics2020

Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A.

Anna K Krome, Tim Becker, Stefan Kehraus, Andrea Schiefer, Christian Steinebach, Tilman Aden, Stefan J Frohberger, Álvaro López Mármol, Dnyaneshwar Kapote, Rolf Jansen and 9 more

Open access · goldAbstract read
In one paragraph

Article in Pharmaceutics, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
0.9field-weighted citation impact, top 30% 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

12 citing papers in PubMed, 15 citations in OpenAlex.

  1. Article
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  8. PotentmSphere · 2022
    Article
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  11. International journal of pharmaceutics: X · 2021
    Article
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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

19 authors at 4 institutions in 1 country.

Anna K KromeDepartment of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, 53121 Bonn, Germany.ORCID 0000-0002-2222-8909
Tim BeckerDepartment of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, 53121 Bonn, Germany.
Stefan KehrausGerman Center for Infection Research (DZIF), Partner Site Bonn-Cologne, 53127 Bonn, Germany.
Andrea SchieferInstitute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, 53127 Bonn, Germany.
Christian SteinebachPharmaceutical & Medicinal Chemistry, University of Bonn, 53121 Bonn, Germany.ORCID 0000-0001-5638-1955
Tilman AdenInstitute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, 53127 Bonn, Germany.
Stefan J FrohbergerInstitute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, 53127 Bonn, Germany.
Álvaro López MármolDepartment of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, 53121 Bonn, Germany.
Dnyaneshwar KapoteDepartment of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, 53121 Bonn, Germany.ORCID 0000-0002-0331-0333
Rolf JansenDepartment of Microbial Drugs, Helmholtz Centre for Infection Research, 38124 Braunschweig, Germany.ORCID 0000-0002-3592-4807
Lillibeth Chaverra-MuñozDepartment of Microbial Drugs, Helmholtz Centre for Infection Research, 38124 Braunschweig, Germany.ORCID 0000-0001-9624-7339
Marc P HübnerInstitute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, 53127 Bonn, Germany.
Kenneth PfarrInstitute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, 53127 Bonn, Germany.ORCID 0000-0003-3096-2465
Thomas HesterkampTranslational Project Management Office (TPMO), German Center for Infection Research (DZIF), 38124 Braunschweig, Germany.
Marc StadlerDepartment of Microbial Drugs, Helmholtz Centre for Infection Research, 38124 Braunschweig, Germany.ORCID 0000-0002-7284-8671
Michael GütschowPharmaceutical & Medicinal Chemistry, University of Bonn, 53121 Bonn, Germany.ORCID 0000-0002-9376-7897
Gabriele M KönigInstitute for Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany.
Achim HoeraufInstitute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, 53127 Bonn, Germany.
Karl G WagnerDepartment of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, 53121 Bonn, Germany.ORCID 0000-0003-2864-7191
University of Bonn · DEUniversity Hospital Bonn · DEGerman Center for Infection Research · DEHelmholtz Centre for Infection Research · DE

Funding

Bundesministerium für Bildung und Forschung 16GW0229Deutsches Zentrum für Infektionsforschung TTU 09.807, 09.816, 09.914,
6 · The paper itself

Abstract

Novel-antibiotics are urgently needed to combat an increase in morbidity and mortality due to resistant bacteria. The preclinical candidate corallopyronin A (CorA) is a potent antibiotic against Gram-positive and some Gram-negative pathogens for which a solid oral formulation was needed for further preclinical testing of the active pharmaceutical ingredient (API). The neat API CorA is poorly water-soluble and instable at room temperature, both crucial characteristics to be addressed and overcome for use as an oral antibiotic. Therefore, amorphous solid dispersion (ASD) was chosen as formulation principle. The formulations were prepared by spray-drying, comprising the water-soluble polymers povidone and copovidone. Stability (high-performance liquid chromatography, Fourier-transform-infrared spectroscopy, differential scanning calorimetry), dissolution (biphasic dissolution), and solubility (biphasic dissolution, Pion's T3 apparatus) properties were analyzed. Pharmacokinetic evaluations after intravenous and oral administration were conducted in BALB/c mice. The results demonstrated that the ASD formulation principle is a suitable stability- and solubility-enhancing oral formulation strategy for the API CorA to be used in preclinical and clinical trials and as a potential market product.

Indexed as

anthelminticantibioticbiphasic dissolution (BiPHa+)copovidone (PVP/VA)corallopyronin A (CorA)pharmacokinetic analysispovidone (PVP)solubility enhanced formulationspray-dried amorphous solid dispersion (ASD)stability enhanced formulation

Identifiers

PMID33217948
PMCPMC7698778
OpenAlexW3105482720

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.