Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
J Pharm Pharm Sci. 2010;13(2):152-61. doi: 10.18433/j3jg61.
A physically sound derivation for reciprocal power time (RPT) model for kinetic of drug release is given. In order to enhance ibuprofen dissolution, its solid dispersions (SDs) prepared by cogrinding technique using crospovidone (CP), microcrystalline cellulose (MC) and oleaster powder (OP) as a novel carrier and the model applied to the drug release data.
The drug cogrounds with the carriers were prepared and subjected to the dissolution studies. For elucidation of observed in vitro differences, FT-IR spectroscopy, X-ray diffraction patterns, DSC thermograms and laser particle size measurement were conducted.
All drug release data fitted very well to newly derived RPT model. The efficiency of the carriers for dissolution enhancement was in the order of: CP>OP>MC. The corresponding release kinetic parameter derived from the model, t50% (time required for 50% dissolution) for the carrier to drug ratio 2:1 were 2.7, 10.2 and 12.6 min, respectively. The efficiency of novel carrier, OP, was between CP and MC. FT-IR showed no interaction between the carriers and drug. The DSC thermograms and X-ray diffraction patterns revealed a slight reduced crystallinty in the SDs. Also grinding reduced mean particle size of drug from 150.7 to 44.4 microm.
An improved derivation for RPT model was provided which the parameter of the model, t50%, unlike to previous derivations was related to the most important property of the drug i.e. its solubility. The model described very well drug release kinetics from the solid dispersions. Cogrinding was an effective technique in enhancing dissolution rate of ibuprofen. Elaeagnus angostifolia fruit powder was suggested as a novel potential hydrophilic carrier in preparing solid dispersion of ibuprofen.
给出了用于药物释放动力学的互易功率时间（RPT）模型的物理推导。为了增强布洛芬的溶解度，采用共研磨技术将其与共聚维酮（CP）、微晶纤维素（MC）和沙枣粉（OP）制成固体分散体（SD），并将该模型应用于药物释放数据。
制备药物与载体的共研磨物，并进行溶解研究。为了阐明观察到的体外差异，进行了傅里叶变换红外光谱（FT-IR）、X 射线衍射图谱、差示扫描量热法（DSC）热谱和激光粒度测量。
所有药物释放数据均非常符合新推导的 RPT 模型。载体对溶解增强的效率顺序为：CP>OP>MC。从模型中得出的相应释放动力学参数 t50%（达到 50%溶解所需的时间）对于载体与药物比例为 2:1 的分别为 2.7、10.2 和 12.6 min。新型载体 OP 的效率介于 CP 和 MC 之间。FT-IR 显示载体与药物之间没有相互作用。DSC 热谱和 X 射线衍射图谱显示 SD 中结晶度略有降低。此外，研磨使药物的平均粒径从 150.7 微米减小到 44.4 微米。
提供了一种改进的 RPT 模型推导，与之前的推导不同，该模型的参数 t50%与药物最重要的性质即溶解度有关。该模型很好地描述了药物从固体分散体中的释放动力学。共研磨是一种增强布洛芬溶解速率的有效技术。沙枣果粉被建议作为一种新型潜在的亲水性载体，用于制备布洛芬的固体分散体。
