Application and Comparison of Cocrystallization Techniques on Trospium Chloride Cocrystals

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22310%2F14%3A43897853" target="_blank" >RIV/60461373:22310/14:43897853 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/68378271:_____/14:00435103 RIV/60461373:22810/14:43897853

Výsledek na webu

<a href="http://dx.doi.org/10.1021/cg500226z" target="_blank" >http://dx.doi.org/10.1021/cg500226z</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1021/cg500226z" target="_blank" >10.1021/cg500226z</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Application and Comparison of Cocrystallization Techniques on Trospium Chloride Cocrystals

Popis výsledku v původním jazyce

To identify as many solid forms of active pharmaceutical ingredient (API) as possible and to monitor their cocrystallization potential, synthetic methods are needed. According to API properties (solubility, melting point, stability), suitable screening methods have to be considered. In this study, the performance of most of the commonly available cocrystallization techniques such as neat grinding, liquid-assisted grinding, slurrying, co-melting, and slow evaporation was compared. We applied them to four pharmaceutical cocrystals of trospium chloride (TCl, a muscarinic antagonist urinary antispasmodic) with adipic (AD), glutaric (GA), oxalic (OX), and salicylic acids (SA), which were identified as hits from previous slow evaporation experiments. Their structures were determined by single-crystal X-ray diffraction (TCl-SA and TCl-OX cocrystals) or from powder X-ray diffraction data (TO-AD and TCl-GA cocrystals). Other methods to characterize the cocrystal phases were applied (H-1 NMR, DSC, IR, and Raman spectroscopy). Comparison of cocrystallization methods and of the prepared cocrystals was discussed.

Název v anglickém jazyce

Application and Comparison of Cocrystallization Techniques on Trospium Chloride Cocrystals

Popis výsledku anglicky

To identify as many solid forms of active pharmaceutical ingredient (API) as possible and to monitor their cocrystallization potential, synthetic methods are needed. According to API properties (solubility, melting point, stability), suitable screening methods have to be considered. In this study, the performance of most of the commonly available cocrystallization techniques such as neat grinding, liquid-assisted grinding, slurrying, co-melting, and slow evaporation was compared. We applied them to four pharmaceutical cocrystals of trospium chloride (TCl, a muscarinic antagonist urinary antispasmodic) with adipic (AD), glutaric (GA), oxalic (OX), and salicylic acids (SA), which were identified as hits from previous slow evaporation experiments. Their structures were determined by single-crystal X-ray diffraction (TCl-SA and TCl-OX cocrystals) or from powder X-ray diffraction data (TO-AD and TCl-GA cocrystals). Other methods to characterize the cocrystal phases were applied (H-1 NMR, DSC, IR, and Raman spectroscopy). Comparison of cocrystallization methods and of the prepared cocrystals was discussed.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2014

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Crystal Growth &amp; Design

ISSN

1528-7483

e-ISSN

—

Svazek periodika

14

Číslo periodika v rámci svazku

6

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

6

Strana od-do

2931-2936

Kód UT WoS článku

000337018900030

EID výsledku v databázi Scopus

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