Garekani H Afrasiabi, Sadeghi F, Ghazi A
School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Drug Dev Ind Pharm. 2003 Feb;29(2):173-9. doi: 10.1081/ddc-120016725.
It was shown that the aqueous solubility of acetaminophen in the presence of polyvinylpyrrolidone (PVP) increased. The solubility at 25 degrees C increased from 14.3 m mL(-1) in the absence of PVP, to 19.7 mg m(-1) in the presence of 4% w/v PVP, and to 26.7mg mL(-1) in the presence of 8% w/v PVP. Dialysis studies indicated that there is a potential of binding between PVP and acetaminophen in their aqueous solutions. Dialysis studies also revealed that the nature of interaction between PVP and acetaminophen is physical and reversible, and there was no strong binding between PVP and acetaminophen in their solutions. Infrared spectroscopy of acetaminophen/PVP solid dispersion indicated that the mechanism of interaction between PVP and acetaminophen is via hydrogen bonding. Therefore, the increase in solubility of acetaminophen in the presence of PVP is probably attributed to its ability to form a water-soluble complex with PVP.
结果表明，在聚乙烯吡咯烷酮（PVP）存在下，对乙酰氨基酚的水溶性增加。25℃时，在不存在PVP的情况下溶解度为14.3mg mL⁻¹，在存在4% w/v PVP时增加到19.7mg mL⁻¹，在存在8% w/v PVP时增加到26.7mg mL⁻¹。透析研究表明，PVP与对乙酰氨基酚在其水溶液中有结合的可能性。透析研究还表明，PVP与对乙酰氨基酚之间相互作用的性质是物理的且可逆的，并且在它们的溶液中PVP与对乙酰氨基酚之间没有强结合。对乙酰氨基酚/PVP固体分散体的红外光谱表明，PVP与对乙酰氨基酚之间的相互作用机制是通过氢键。因此，在PVP存在下对乙酰氨基酚溶解度的增加可能归因于其与PVP形成水溶性复合物的能力。
