Evidence map›Paper›PMID 35064418›Full record

ArticlePharmaceutical research2022

A New Saquinavir Mesylate-Sodium Decyl Sulfate Salt Discovered by Serendipity during an Anomalous Dissolution Test.

Cinira Fandaruff, Thiago Caon, Andrea Mariela Araya-Sibaja, Gabriela Schneider Rauber, Marcos Antônio Segatto Silva, Cláudia Maria Oliveira Simões, Carlos Eduardo Maduro de Campos, Adailton João Bortoluzzi, Jackson Antônio Lamounier Camargos Resende, Silvia Lucia Cuffini

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Article in Pharmaceutical research, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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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

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0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

4 · The record

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5 · Who and what money

Authors and funding

10 authors at 3 institutions in 1 country.

Cinira FandaruffLaboratório de Controle de Qualidade, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, UFSC Campus Reitor João David Ferreira Lima, s/n Trindade, Florianópolis, Santa Catarina, CEP: 88040-900, Brazil. cinira_fandaruff@hotmail.com.ORCID http://orcid.org/0000-0002-3644-2260
Thiago CaonLaboratório de Farmacotécnica e Cosmetologia, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Florianópolis, Brazil.
Andrea Mariela Araya-SibajaLaboratorio Nacional de Nanotecnología LANOTEC-CeNAT-CONARE, San José, 1174-1200, Costa Rica.
Gabriela Schneider RauberLaboratório de Controle de Qualidade, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, UFSC Campus Reitor João David Ferreira Lima, s/n Trindade, Florianópolis, Santa Catarina, CEP: 88040-900, Brazil.
Marcos Antônio Segatto SilvaLaboratório de Controle de Qualidade, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, UFSC Campus Reitor João David Ferreira Lima, s/n Trindade, Florianópolis, Santa Catarina, CEP: 88040-900, Brazil.
Cláudia Maria Oliveira SimõesLaboratório de Virologia Aplicada, Departamento de Microbiologia, Imunologia e Parasitologia, Universidade Federal de Santa Catarina, Florianópolis, Brazil.
Carlos Eduardo Maduro de CamposLaboratório de Difração de Raios-X, Departamento de Física, Universidade Federal de Santa Catarina, Florianópolis, Brazil.
Adailton João BortoluzziLaboratório de Bioinorgânica e Cristalografia, Departamento de Química, Universidade Federal de Santa Catarina, Florianópolis, Brazil.
Jackson Antônio Lamounier Camargos ResendePós-Graduação em Ciências dos Materiais, Universidade Federal de Mato Grosso, Instituto de Ciências Exatas e da Terra - CUA, Barra do Garças, Brazil.
Silvia Lucia CuffiniPós-Graduação em Engenharia e Ciências dos Materiais, Universidade Federal de São Paulo, São José dos Campos, Brazil.
Universidade Federal de Santa Catarina · BRUniversidade Federal de Mato Grosso · BRUniversidade Federal de São Paulo · BR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeTo understand the anomalous behavior of Saquinavir Mesylate (SQVM) in sodium decyl sulfate (SDS) medium during a dissolution test through a crystallographic analysis of the crystal obtained. As a result, it will be possible to elucidate its crystal structure and carry out a complete solid-state characterization of the API.

methodsThe solid form obtained was characterized by a structural analysis through X-ray single crystal and powder diffraction. The crystallographic structures of the new salt and the SQVM were compared. In addition, a complete solid-state characterization of SQVM raw material was carried out by techniques such as diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS), Raman spectroscopy, scanning electron microscopy and a dissolution method.

resultsA new salt consisting of SQVM and SDS was crystallized and its crystal structure was elucidated and reported herein for the first time. The anionic part of SDS interacts with the cationic segment of SQVM to obtain a new salt designated as SQV-DS, which precipitates. The main difference between the two structures occurs in the c-axis expansion, which increases from 15.966 (5) to 21.1924 (14), respectively.

conclusionsSome of the strategies to enhance the dissolution rate of poorly aqueous soluble APIs include the use of surfactants such as SDS in the dissolution medium, as well as in the formulated products. However, there have been constant reports of a dissolution rate slowdown by some surfactants. The interaction mechanisms between the APIs and the dissolution medium containing surfactants need to be carefully investigated in current pharmaceutical formulations. Graphical Abstract.

Indexed as

SaquinavirSodiumCalorimetry, Differential ScanningPharmaceutical PreparationsSolubilitySpectroscopy, Fourier Transform InfraredSulfatesX-Ray DiffractionPharmaceutical PreparationsSaquinavirSodiumSulfatesdissolutionrecrystallizationsaquinavir mesylatesingle crystalsodium decyl sulfate

Identifiers

PMID35064418
OpenAlexW4206951513

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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.