Hussain Amjad, Farrukh Maryam, Abbas Nasir, Irfan Muhammad, Arshad Muhammad Sohail, Bukhari Nadeem Irfan
University College of Pharmacy, University of the Punjab, Lahore, Pakistan.
College of Pharmacy, Government College University, Faisalabad, Pakistan.
Pak J Pharm Sci. 2019 Sep;32(5(Supplementary)):2257-2260.
The present study was aimed to enhance the solubility and dissolution rate of Piroxicam, a poorly water soluble drug from BCS class II. Solid dispersions (SDs) of Piroxicam Solutol and Gelucire were prepared by applying fusion method. The prepared SDs were tested for their aqueous solubility and dissolution rate. These dispersions were characterized by PXRD and FTIR for any physical or chemical change, respectively. From the results it was revealed that the solubility value of drug was increased by 20-25 times (with Solutol) and 6-10 times (with Gelucire). Dissolution rate of piroxicam was 7-8 times quicker in SDs with Solutol while with Gelucire a slow drug release in first 20 min was noted that was further enhanced by adding a ternary component, i.e. silica. The real time stability studies show that the solid dispersions are quite stable after 6 months in terms of solubility and dissolution rate. The study concludes that binary solid dispersion with Solutol has effectively increased the solubility of piroxicam that in turn has increased its dissolution rate, therefore useful in enhancing the bioavailability of this poorly soluble drug. In case of piroxicam: Gelucire solid dispersion; a ternary component is required to achieve quick release of drug.
本研究旨在提高吡罗昔康(一种BCS II类难溶性药物)的溶解度和溶出速率。采用熔融法制备了吡罗昔康与聚氧乙烯蓖麻油和Gelucire的固体分散体(SDs)。对制备的固体分散体进行了水溶性和溶出速率测试。分别通过粉末X射线衍射(PXRD)和傅里叶变换红外光谱(FTIR)对这些分散体的任何物理或化学变化进行表征。结果表明,药物的溶解度值提高了20 - 25倍(与聚氧乙烯蓖麻油)和6 - 10倍(与Gelucire)。在含聚氧乙烯蓖麻油的固体分散体中,吡罗昔康的溶出速率快7 - 8倍,而在含Gelucire的固体分散体中,最初20分钟药物释放缓慢,加入三元组分即二氧化硅后进一步加快。实时稳定性研究表明,固体分散体在6个月后在溶解度和溶出速率方面相当稳定。该研究得出结论,含聚氧乙烯蓖麻油的二元固体分散体有效提高了吡罗昔康的溶解度,进而提高了其溶出速率,因此有助于提高这种难溶性药物的生物利用度。对于吡罗昔康:Gelucire固体分散体,需要一种三元组分来实现药物的快速释放。