Ravouru Nagaraju, Penjuri Subhash Chandra Bose, Damineni Saritha, Muni Raja Lakshmi, Poreddy Srikanth Reddy
Sri Padmavati Mahila Visvavidyalayam, (Women's University), Institute of Pharmaceutical Technology, Tirupati, Andhra Pradesh, India.
MNR College of Pharmacy, Department of Pharmaceutics, Sangareddy, Telangana, India.
Turk J Pharm Sci. 2018 Apr;15(1):7-15. doi: 10.4274/tjps.09609. Epub 2018 Apr 2.
Ibuprofen, an anti-inflammatory drug, is characterized by poor water solubility, which limits its pharmacologic effects. The present work aimed to the study the effect of agglomeration on the micromeritic properties and dissolution of ibuprofen.
Ibuprofen agglomerates were prepared by solvent change method using water, dichloromethane and DMSO as poor solvent, bridging liquid and good solvent respectively in the ratio of 57.5:12.5:30. Process variables such as amount of bridging liquid, mode of addition, temperature and stirring rate were optimized.
SEM studies indicate that agglomerates produced were spherical and exhibit irregular shape. X-Ray Powder Diffraction spectra revealed the absence of polymorphism. DSC spectra showed no change in melting point indicating absence of crystal modification. The agglomerates exhibited improved solubility, dissolution rate and micromeritic properties compared to pure drug.
Anti-inflammatory studies were conducted in Wistar strain male albino rats and ibuprofen agglomerates showed more significant activity than the pure drug which may be due to better absorption. Ulcerogenic potential study was carried out for pure ibuprofen and agglomerates. Better ulcerogenic potential was observed in ibuprofen agglomerates treated rats.
布洛芬是一种抗炎药物，其特点是水溶性差，这限制了它的药理作用。本研究旨在探讨团聚对布洛芬的粉体学性质和溶出度的影响。
采用溶剂变换法制备布洛芬团聚体，分别以水、二氯甲烷和二甲基亚砜作为不良溶剂、架桥液和良溶剂，比例为57.5:12.5:30。对架桥液用量、添加方式、温度和搅拌速度等工艺变量进行了优化。
扫描电子显微镜研究表明，制备的团聚体呈球形且形状不规则。X射线粉末衍射光谱显示不存在多晶型现象。差示扫描量热光谱表明熔点没有变化，表明不存在晶体改性。与纯药物相比，团聚体的溶解度、溶出速率和粉体学性质均有所改善。
在Wistar品系雄性白化大鼠中进行了抗炎研究，布洛芬团聚体显示出比纯药物更显著的活性，这可能是由于更好的吸收。对纯布洛芬和团聚体进行了致溃疡潜力研究。在接受布洛芬团聚体治疗的大鼠中观察到更好的致溃疡潜力。
