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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Randhawa M A, Iqbal A, Nasimullah M, Akhtar M, Yousaf S M, Turner P

Department of Pharmacology and Therapeutics, Rawalpindi Medical College, Pakistan.

Gen Pharmacol. 1995 Jul;26(4):875-9. doi: 10.1016/0306-3623(94)00256-m.

The transmembrane diffusion of weakly acidic or basic drugs is being commonly assessed from their degree of ionization or ratio unionized/ionized forms (ratio U/I) as calculated from Henderson-Hasselbalch equation (HHEq). 2. Buccal drug absorption (BA) at pH 5-9 has been proposed as an in vivo model for passage of drugs across lipid membranes. 3. Area under the curve (AUC) of BA against pH 5-9 of 18 basic drugs has been reported to be significantly related to their pH dependent renal excretion. 4. We have calculated, using HHEq, ratios U/I of 10 weak bases at pH 5-9 and 10 weak acids at pH 4-8, whose percentage BA at these pH levels was available in the literature. 5. These ratios were not related to their %BA at corresponding pH levels. 6. Therefore it is proposed that HHEq is inadequate in the anticipation of transmembrane diffusion of drugs and AUC of %BA of drugs at pH 4-9 is a useful alternative.

弱酸性或碱性药物的跨膜扩散通常根据其电离程度或根据亨德森-哈塞尔巴尔赫方程（HHEq）计算的非离子化/离子化形式的比率（U/I比率）来评估。2. 已提出pH值为5至9时的颊部药物吸收（BA）作为药物跨脂质膜转运的体内模型。3. 据报道，18种碱性药物的BA相对于pH值5至9的曲线下面积（AUC）与其pH依赖性肾排泄显著相关。4. 我们使用HHEq计算了pH值为5至9时10种弱碱和pH值为4至8时10种弱酸的U/I比率，这些pH水平下的BA百分比在文献中是可获得的。5. 这些比率与相应pH水平下的BA百分比无关。6. 因此，有人提出HHEq在预测药物的跨膜扩散方面是不足的，pH值4至9时药物BA的AUC是一种有用的替代方法。

Randhawa M A, Iqbal A, Nasimullah M, Akhtar M, Yousaf S M, Turner P

Department of Pharmacology and Therapeutics, Rawalpindi Medical College, Pakistan.

Gen Pharmacol. 1995 Jul;26(4):875-9. doi: 10.1016/0306-3623(94)00256-m.

The transmembrane diffusion of weakly acidic or basic drugs is being commonly assessed from their degree of ionization or ratio unionized/ionized forms (ratio U/I) as calculated from Henderson-Hasselbalch equation (HHEq). 2. Buccal drug absorption (BA) at pH 5-9 has been proposed as an in vivo model for passage of drugs across lipid membranes. 3. Area under the curve (AUC) of BA against pH 5-9 of 18 basic drugs has been reported to be significantly related to their pH dependent renal excretion. 4. We have calculated, using HHEq, ratios U/I of 10 weak bases at pH 5-9 and 10 weak acids at pH 4-8, whose percentage BA at these pH levels was available in the literature. 5. These ratios were not related to their %BA at corresponding pH levels. 6. Therefore it is proposed that HHEq is inadequate in the anticipation of transmembrane diffusion of drugs and AUC of %BA of drugs at pH 4-9 is a useful alternative.

弱酸性或碱性药物的跨膜扩散通常根据其电离程度或根据亨德森-哈塞尔巴尔赫方程（HHEq）计算的非离子化/离子化形式的比率（U/I比率）来评估。2. 已提出pH值为5至9时的颊部药物吸收（BA）作为药物跨脂质膜转运的体内模型。3. 据报道，18种碱性药物的BA相对于pH值5至9的曲线下面积（AUC）与其pH依赖性肾排泄显著相关。4. 我们使用HHEq计算了pH值为5至9时10种弱碱和pH值为4至8时10种弱酸的U/I比率，这些pH水平下的BA百分比在文献中是可获得的。5. 这些比率与相应pH水平下的BA百分比无关。6. 因此，有人提出HHEq在预测药物的跨膜扩散方面是不足的，pH值4至9时药物BA的AUC是一种有用的替代方法。