A comprehensive study of a new 1.75 hydrate of ciprofloxacin salicylate: SCXRD structure determination, solid characterization, water stability, solubility, and dissolution study.
英文:
A comprehensive study of a new 1.75 hydrate of ciprofloxacin salicylate: SCXRD structure determination, solid characterization, water stability, solubility, and dissolution study.
著者
和文:
Ilma Nugrahani,
Billgerd Tjengal,
Tutus Gusdinar,
Ayano Horikawa,
Hidehiro. Uekusa.
英文:
Ilma Nugrahani,
Billgerd Tjengal,
Tutus Gusdinar,
Ayano Horikawa,
Hidehiro. Uekusa.
One problem that often arises during the formulation of a dosage form is the soly. and dissoln. of the active ingredients. This problem arises in ciprofloxacin, which is a BCS class IV fluoroquinolone antibiotic. A pseudopolymorph is a kind of polymorph in which the no. of hydrates is different. In this study, a new pseudopolymorph comprised of ciprofloxacin and salicylic acid was found, namely the salt ciprofloxacin salicylate 1.75 hydrate form. This new solid phase was analyzed by Fourier-transform IR spectroscope (FTIR), Raman spectroscopy, and thermal anal. and proven by Powder X-ray Diffractometry (PXRD) anal. The crystal structure was successfully detd. by Single Crystal X-ray Diffractometry (SCXRD) anal. It was found that the piperazinyl group of ciprofloxacin is protonated by H+ from the carboxylic group of salicylic acid. In the unit cell, two ciprofloxacin and two salicylic acid mols. were independent with four water mols., in which one water mol. had 0.5 occupancy due to inversion symmetry. Interestingly, this hydrate crystal dehydrated by grinding for 105 min forms an anhyd. cryst. phase, which was analyzed with FTIR, Raman spectroscopy, thermal anal., and PXRD. The soly. and dissoln. tests were carried out using UV-Visible spectrophotometry and a multiple linear regression method. This new hydrate solid phase has a better profile than the original ciprofloxacin crystal, according to the soly. and dissoln. tests. [on SciFinder(R)]
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