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999 _c11194
_d11194
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040 _aAIKTC-KRRC
_cAIKTC-KRRC
100 _912148
_aMelnikova, Nina
245 _a IMPROVEMENT OF BETULIN-3, 28-DIPHOSPHATE WATER- SOLUBILITY BY COMPLEXATION WITH AMINES–MEGLUMINE AND XYMEDON
250 _aVol.11(5)
260 _aM P
_bInnovare Academic Sciences Pvt Ltd
_c2019
300 _a48-55p.
520 _aObjective: To study betulin-3,28-diphosphate (BDP) water solub ility improved by forming salt complexes with hydro philic amino alcohols: meglumine as acidosis corrector and xymedon as the water-soluble antioxidant. Methods: We used 13 C-, 31 P-NMR, UV-spectroscopy and potentiometric titration to study the BDP-amine salt complexes formation an d their solubility using HPLC-analysis. Results: The participation of xymedon in the proton transfer reaction with BDP in aqueous solutions was confirm ed by the bathochromic shift of the carbonyl band from 299.1 nm to 304.2 nm, and by a hyperchromic effect (molar extinction ε from 850 8 to 10 441 l·mol -1 ·cm -1 ) in UV-spectra. BDP complexation with meglumine was estimated by UV -spectral molar ratio method at 256 nm. Molar ratio of BDP-amine complexes (1:4) was proved by 31 P-NMR. The chemical shift of phosphorus at C-3 atom of BDP (δ =-0.58 ppm) changed to+3.39 ppm, and at C-28 atom (δ =+0.28 ppm)– to+4.60 ppm. BDP solubility increased 100-600 fold according to HPLC-analysis. Conclusion: BDP interaction with amine in an aqueous solution w as shown to proceed via a proton transfer due to re latively weak forces such as London forces, hydrogen bonding, electrostatic and hydrophobic interactions. In general, the formation of BDP salt complexes with amines in solution determines BDP water solubility. Water-sol uble BDP enables to develop hydrophilic dosage form s.
650 0 _94639
_aPHARMACEUTICS
700 _912149
_aMalygina, Darina
773 0 _x2656-0097
_tInternational journal of pharmacy and pharmaceutical science
_dBhopal Innovare Academic Sciences Pvt Ltd
856 _uhttps://innovareacademics.in/journals/index.php/ijpps/article/view/32707/19864
_yClick here
942 _2ddc
_cAR