Apr 15, 2016 16:09
8 yrs ago
English term

Combinatorial Salt Screen

English to Russian Science Chemistry; Chem Sci/Eng
A salt screen was performed using six solvents (IPA, THF, acetone, acetonitrile, EtOH and EtOAc) and twenty-eight pharmaceutically acceptable acids (HCl, HBr, H3PO4, H2SO4, CH3SO3H, pTSA, BSA, naphthalene sulfonic acid, ethane sulfonic acid, methane sulfonic acid, adipic acid, ethane disulfonic acid, maleic acid, benzoic acid, L-malic acid, citric acid, L-lactic acid, hippuric acid, L-pyroglutamic acid, succinic acid, L-tartaric acid, formic acid, fumaric acid, glutaric acid, L-ascorbic acid, sorbic acid, benzoic acid, and malonic acid).
A 96-well plate was charged with 200 μL of a 20 mg/mL solution of compound (I) in MeOH in each well.
The solvent was then evaporated under a flow of nitrogen, leaving approximately 4 mg of the starting material in each well.
The primary solvent of interest was then added to each well (500 μL).
The plates were heated to 50 °C and stirred magnetically for 10 min to ensure complete dissolution of A. Each well was then charged with the designated counterion solution at a volume corresponding to 1.05 equivalents of each acid and allowed to equilibrate at temperature for 10 min. The plates were then cooled at 20 °C/h to 25 °C, at which point the master plate was daughtered by transferring 200 μL from each well into an evaporation plate.
The plates were then cooled to ambient temperature, stored overnight at 5 °C and checked for the presence of solids.
The solvent from the master plates was then removed by wicking with sorbent paper.
The master and evaporation plates were then dried under nitrogen overnight.
Wells that contained solid material were then scored and ranked for birefringence, unique Raman spectrum and threshold solubility.
Suitable solvent and counterion combinations were then reevaluated for salt formation with A at an increased scale.

Proposed translations

+2
2 hrs
Selected

комбинаторный скрининг (поиск) солевых форм (препарата)

http://ssci-inc.com/DrugSubstance/ScreeningPolymorphsSaltsCo...
Salt Screening and Salt Selection
SSCI's Salt Screen involves a search for solid salts of ionizable drug products using sources of pharmaceutically acceptable counterions as well as knowledge of their properties, frequency of use in drug products, and manufacturability. The desire to use a salt is usually due to poor drug substance properties such as lack of crystallinity, water solubility, or stability.
Peer comment(s):

agree Igor Andreev : очень похоже, в данном случае, возможно ... скрининг растворимости солевых форм (солей?). По ссылке описан более "глобальный" скрининг
1 hr
Спасибо.
agree Erzsébet Czopyk
1 day 7 hrs
Thank you, Erzsébet.
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4 KudoZ points awarded for this answer. Comment: "Спасибо за помощь"
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