Evidence map›Paper›PMID 26857899›Full record

ArticlePharmaceutical research2016

New Perspectives for Fixed Dose Combinations of Poorly Water-Soluble Compounds: a Case Study with Ezetimibe and Lovastatin.

Manoela K Riekes, Axel Engelen, Bernard Appeltans, Patrick Rombaut, Hellen K Stulzer, Guy Van den Mooter

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Article in Pharmaceutical research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
3.5field-weighted citation impact, top 8% 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

14 citing papers in PubMed, 56 citations in OpenAlex.

  1. Co-amorphization for solubility and dissolution rate improvement: the case of low-crystallization-tendency drugs.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2026
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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

6 authors at 2 institutions in 2 countries.

Manoela K RiekesDepartment of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven, Campus Gasthuisberg ON2, Herestraat 49 b921, 3000, Leuven, Belgium.
Axel EngelenDepartment of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven, Campus Gasthuisberg ON2, Herestraat 49 b921, 3000, Leuven, Belgium.
Bernard AppeltansDepartment of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven, Campus Gasthuisberg ON2, Herestraat 49 b921, 3000, Leuven, Belgium.
Patrick RombautDepartment of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven, Campus Gasthuisberg ON2, Herestraat 49 b921, 3000, Leuven, Belgium.
Hellen K StulzerLaboratório de Controle de Qualidade, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Campus Reitor João David Ferreira Lima, Trindade, 88040-970, Florianópolis, SC, Brazil.
Guy Van den MooterDepartment of Pharmaceutical and Pharmacological Sciences, Drug Delivery and Disposition, KU Leuven, Campus Gasthuisberg ON2, Herestraat 49 b921, 3000, Leuven, Belgium. guy.vandenmooter@pharm.kuleuven.be.
KU Leuven · BEUniversidade Federal de Santa Catarina · BR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeAiming to improve the dissolution rate of ezetimibe (EZE) and lovastatin (LOV) in a fixed dose combination (FDC), co-amorphous systems and ternary solid dispersions were prepared by quench cooling and spray drying, respectively.

methodsFormulations were characterized through X-ray diffraction, modulated differential scanning calorimetry, infrared spectroscopy, scanning electron microscopy and laser diffraction, and evaluated by 'in vitro' dissolution. Stability studies were conducted at different conditions during 30 days with the ternary solid dispersion composed of 75% of Soluplus® (ELS 1:1 75%).

resultsSingle phase co-amorphous systems made up of the pure drugs were not able to increase the dissolution rate of EZE and LOV. However, ternary solid dispersions achieved high dissolution for both compounds, especially when Soluplus® was used as carrier. The dissolution efficiency increased up to 18 (EZE) and 6 (LOV) times in ternary solid dispersions, compared to the crystalline drugs. ELS 1:1 75% preserved its amorphous state during 30 days, in different stability conditions.

conclusionsA spray dried ternary solid dispersion able to enhance the dissolution rate of two poorly soluble, therapeutically complementary drugs, is reported for the first time. These promising results open new perspectives for the development of more advanced FDCs.

Indexed as

Anticholesteremic AgentsCalorimetry, Differential ScanningCrystallizationDesiccationDrug CombinationsDrug CompoundingDrug StabilityEzetimibeLovastatinWaterX-Ray DiffractionAnticholesteremic AgentsDrug CombinationsEzetimibeLovastatinWaterco-amorphous systemsezetimibefixed dose combinationslovastatinternary solid dispersions

Identifiers

PMID26857899
OpenAlexW2256155876

What OpenQuestion holds

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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.