Nagaraju Ravouru 1 , Subhash Chandra Bose Penjuri 2 , Saritha Damineni 3 , Raja Lakshmi Muni 1 , Srikanth Reddy Poreddy 2 . Show Affiliations »
Abstract
OBJECTIVES: 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. MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSION: 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. ©Copyright 2018 Turk J Pharm Sci, Published by Galenos Publishing House.
OBJECTIVES: 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. MATERIALS AND METHODS: 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. RESULTS: 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. CONCLUSION: 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. ©Copyright 2018 Turk J Pharm Sci, Published by Galenos Publishing House.
Entities: Chemical
Keywords:
Ibuprofen; anti-inflammatory activity; spherical agglomeration; ulcerogenic potential
Year: 2018
PMID: 32454634 PMCID: PMC7227892 DOI: 10.4274/tjps.09609
Source DB: PubMed Journal: Turk J Pharm Sci ISSN: 1304-530X