Evidence map›Paper›PMID 32801637›Full record

ArticleDrug design, development and therapy2020

Soluplus-Mediated Diosgenin Amorphous Solid Dispersion with High Solubility and High Stability: Development, Characterization and Oral Bioavailability.

Pei Liu, Jian-Yu Zhou, Jin-Hua Chang, Xi-Gang Liu, He-Fei Xue, Ru-Xing Wang, Zhong-Si Li, Chun-Shi Li, Jian Wang, Cui-Zhe Liu

Open access · goldAbstract read
In one paragraph

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 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
2.3field-weighted citation impact, top 11% 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

20 citing papers in PubMed, 59 citations in OpenAlex.

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  18. Development and Characterization of EudragitPharmaceuticals (Basel, Switzerland) · 2022
    Article
  19. Article
  20. The Effects of Diosgenin on Hypolipidemia and Its Underlying Mechanism: A Review.Diabetes, metabolic syndrome and obesity : targets and therapy · 2021
    Review
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

10 authors at 2 institutions in 1 country.

Pei LiuDepartment of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
Jian-Yu ZhouHebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of China.
Jin-Hua ChangHebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of China.
Xi-Gang LiuHebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of China.
He-Fei XueHebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of China.
Ru-Xing WangHebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of China.
Zhong-Si LiHebei Province Key Laboratory of Research and Development for Chinese Medicine, Chengde Medical University, Chengde, Hebei 067000, People's Republic of China.
Chun-Shi LiKey Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.ORCID 0000-0002-4007-9951
Jian WangKey Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.ORCID 0000-0002-9589-4056
Cui-Zhe LiuDepartment of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
Chengde Medical University · CNShenyang Pharmaceutical University · CN

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

background and purposeThe traditional Chinese medicine, diosgenin (Dio), has attracted increasing attention because it possesses various therapeutic effects, including anti-tumor, anti-infective and anti-allergic properties. However, the commercial application of Dio is limited by its extremely low aqueous solubility and inferior bioavailability in vivo. Soluplus, a novel excipient, has great solubilization and capacity of crystallization inhibition. The purpose of this study was to prepare Soluplus-mediated Dio amorphous solid dispersions (ASDs) to improve its solubility, bioavailability and stability.

methodsThe crystallization inhibition studies were firstly carried out to select excipients using a solvent shift method. According to solubility and dissolution results, the preparation methods and the ratios of drug to excipient were further optimized. The interaction between Dio and Soluplus was characterized by differential scanning calorimetry (DSC), fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), powder X-ray diffraction (PXRD) and molecular docking. The pharmacokinetic study was conducted to explore the potential of Dio ASDs for oral administration. Furthermore, the long-term stability of Dio ASDs was also investigated.

resultsSoluplus was preliminarily selected from various excipients because of its potential to improve solubility and stability. The optimized ASDs significantly improved the aqueous solubility of Dio due to its amorphization and the molecular interactions between Dio and Soluplus, as evidenced by dissolution test in vitro, DSC, FT-IR spectroscopy, SEM, PXRD and molecular docking technique. Furthermore, pharmacokinetic studies in rats revealed that the bioavailability of Dio from ASDs was improved about 5 times. In addition, Dio ASDs were stable when stored at 40°C and 75% humidity for 6 months.

conclusionThese results indicated that Dio ASDs, with its high solubility, high bioavailability and high stability, would open a promising way in pharmaceutical applications.

Indexed as

Drug DevelopmentAdministration, OralAnimalsBiological AvailabilityChromatography, High Pressure LiquidCrystallography, X-RayDiosgeninDrug CompoundingDrugs, Chinese HerbalDrug StabilityExcipientsMaleMedicine, Chinese TraditionalMolecular ConformationMolecular Docking SimulationPolyethylene GlycolsDiosgeninDrugs, Chinese HerbalExcipientsPolyethylene Glycolspolyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymerPolyvinylsamorphous solid dispersionsbioavailabilitydiosgeninsolubilitystability

Identifiers

PMID32801637
PMCPMC7396739
OpenAlexW3043962811

What OpenQuestion holds

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LicenceCC BY-NC
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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.