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Dissolution Kinetics of a BCS Class II Active Pharmaceutical Ingredient
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-02-27 00:00:00 , DOI: 10.1021/acs.oprd.7b00365 Yuan Gao 1 , Brian Glennon 1 , Vamsi Krishna Kamaraju 2 , Guangyang Hou 2 , Philip Donnellan 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-02-27 00:00:00 , DOI: 10.1021/acs.oprd.7b00365 Yuan Gao 1 , Brian Glennon 1 , Vamsi Krishna Kamaraju 2 , Guangyang Hou 2 , Philip Donnellan 1
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This paper presents a laboratory study examining the dissolution kinetics of ibuprofen crystals in water containing a phosphate buffer (pH 7.20) at 37 °C, examining the influences of initial undersaturation ratio, agitation rate, crystal habit, and particle size. For each experiment, the concentration during the dissolution process was followed using UV spectroscopy, ATR-FTIR, and FBRM methods. The dissolution profiles were correlated using eight mathematical models, and the dissolution rate parameters were determined. The Weibull model, the Korsmeyer–Peppas model, and the first-order kinetics model gave better correlation results than the other models used in this paper for the dissolution of ibuprofen crystals. The particle size distribution slightly shifted to the right after dissolution, confirming that smaller particles with higher surface areas dissolved more rapidly. During dissolution, two distinct behaviors were obtained at different levels of undersaturation ratio; therefore, it is postulated that the mechanism of dissolution switches from being mass-transfer-limited at higher levels of undersaturation ratio to being limited by the rate of surface detachment at lower undersaturation ratio levels.
中文翻译：
BCS II类活性药物成分的溶解动力学
本文提出了一项实验室研究，研究了布洛芬晶体在37°C的含磷酸盐缓冲液（pH 7.20）的水中的溶解动力学，并考察了初始不饱和率，搅拌速率，晶体习性和粒径的影响。对于每个实验，使用紫外光谱，ATR-FTIR和FBRM方法跟踪溶解过程中的浓度。使用八个数学模型关联溶出曲线，并确定溶出速率参数。Weibull模型，Korsmeyer-Peppas模型和一阶动力学模型比布洛芬晶体溶解中使用的其他模型具有更好的相关性。溶解后，粒径分布略微向右移动，证实具有较高表面积的较小颗粒溶解更快。在溶解过程中，在不同的欠饱和度水平下获得了两种不同的行为；因此，据推测，溶解的机理从在较高的不饱和度水平下的传质受限转变为在较低的不饱和度水平下的表面脱离速率所限制。
更新日期：2018-02-27
中文翻译：
BCS II类活性药物成分的溶解动力学
本文提出了一项实验室研究，研究了布洛芬晶体在37°C的含磷酸盐缓冲液（pH 7.20）的水中的溶解动力学，并考察了初始不饱和率，搅拌速率，晶体习性和粒径的影响。对于每个实验，使用紫外光谱，ATR-FTIR和FBRM方法跟踪溶解过程中的浓度。使用八个数学模型关联溶出曲线，并确定溶出速率参数。Weibull模型，Korsmeyer-Peppas模型和一阶动力学模型比布洛芬晶体溶解中使用的其他模型具有更好的相关性。溶解后，粒径分布略微向右移动，证实具有较高表面积的较小颗粒溶解更快。在溶解过程中，在不同的欠饱和度水平下获得了两种不同的行为；因此，据推测，溶解的机理从在较高的不饱和度水平下的传质受限转变为在较低的不饱和度水平下的表面脱离速率所限制。
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