Increasing the aqueous solubility of acetaminophen in the presence of polyvinylpyrrolidone and investigation of the mechanisms involved

Increasing the aqueous solubility of acetaminophen in the presence of polyvinylpyrrolidone and investigation of the mechanisms involved
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DOI:
10.1081/ddc-120016725
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发表时间:
2003-01-01
影响因子:
3.4
通讯作者:
Ghazi, A
Ghazi, A
中科院分区:
医学4区
文献类型:
--
作者:
Garekani, HA;Sadeghi, F;Ghazi, A

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结果表明,在聚乙烯吡咯烷酮(PVP)存在下,对乙酰氨基酚在水中的溶解度增加。在25℃时的溶解度从不加PVP时的14.3 mg mL(-1),增加到4%w/v PVP时的19.7 mg mL(-1),和加入8%w/v PVP时的26.7 mg mL(-1)。透析研究表明,PVP与对乙酰氨基酚的水溶液之间存在结合的潜力。透析研究还表明,PVP与对乙酰氨基酚之间的相互作用是物理的和可逆的,PVP和对乙酰氨基酚的溶液中没有很强的结合。对乙酰氨基酚/PVP固体分散体的红外光谱表明,PVP与对乙酰氨基酚的相互作用机理为氢键作用。因此,对乙酰氨基酚在PVP存在下的溶解度增加可能归因于其与PVP形成水溶性络合物的能力。
It was shown that the aqueous solubility of acetaminophen in the presence of polyvinylpyrrolidone (PVP) increased. The solubility at 25degreesC increased from 14.3 mg mL(-1) in the absence of PVP, to 19.7 mg mL(-1) in the presence of 4% w/v PVP, and to 26.7 mg 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.