TY - JOUR
T1 - Improved bioavailability of aceclofenac from spherical agglomerates: Development, in vitro and preclinical studies
AU - Mutalik, S.
AU - Usha, A.N.
AU - Reddy, M.S.
AU - Ranjith, A.K.
AU - Pandey, S.
N1 - Cited By :15
Export Date: 10 November 2017
Correspondence Address: Mutalik, S.; Department of Pharmaceutics, Manipal College of Pharmaceutical SciencesIndia; email: ssmutalik@yahoo.com
Chemicals/CAS: aceclofenac, 89796-99-6; acetone, 67-64-1; alginic acid, 28961-37-7, 29894-36-8, 9005-32-7, 9005-38-3; carrageenan, 9000-07-1, 9049-05-2, 9061-82-9, 9064-57-7; dichloromethane, 75-09-2; diclofenac, 15307-79-6, 15307-86-5; glucuronic acid, 36116-79-7, 576-37-4, 6556-12-3; povidone, 9003-39-8; water, 7732-18-5; 15307-86-5; 576-37-4; 89796-99-6; 9000-07-1; 9003-39-8; 9005-32-7; aceclofenac; Alginates; alginic acid; Analgesics, Non-Narcotic; Anti-Inflammatory Agents, Non-Steroidal; Carrageenan; Diclofenac; Emulsions; Glucuronic Acid; Hexuronic Acids; Povidone
Manufacturers: Himedia, India; Lupin Laboratories, India; SD, India
PY - 2007
Y1 - 2007
N2 - The objective of present study was to improve the solubility, dissolution rate, micromeritic properties and bioavailability of aceclofenac (NSAID) by formulating its spherical agglomerates. They were prepared with different water soluble polymers (polyvinylpyrrolidone-K30, polyvinylpyrrolidone-K90 and sodium alginate) by using acetone-water-dichloromethane solvent system. The agglomerates were subjected to various physicochemical properties, DSC, IR spectroscopy, scanning electron microscopy (SEM), micromeritic properties and dissolution studies. The in vivo studies (anti-inflammatory, analgesic and pharmacokinetic studies) were conducted in Wistar rats and Swiss albino mice. SEM studies showed that agglomerates were spherical in structure and formed by cluster of small crystals. The agglomerates prepared with polyvinylpyrrolidone- K90 exhibited improved solubility, dissolution rate and micromeritic properties compared to those prepared with other polymers and pure drug. These optimized agglomerates showed rapid analgesic and anti-inflammatory activity besides exhibiting improved bioavailability of drug when compared to pure drug.
AB - The objective of present study was to improve the solubility, dissolution rate, micromeritic properties and bioavailability of aceclofenac (NSAID) by formulating its spherical agglomerates. They were prepared with different water soluble polymers (polyvinylpyrrolidone-K30, polyvinylpyrrolidone-K90 and sodium alginate) by using acetone-water-dichloromethane solvent system. The agglomerates were subjected to various physicochemical properties, DSC, IR spectroscopy, scanning electron microscopy (SEM), micromeritic properties and dissolution studies. The in vivo studies (anti-inflammatory, analgesic and pharmacokinetic studies) were conducted in Wistar rats and Swiss albino mice. SEM studies showed that agglomerates were spherical in structure and formed by cluster of small crystals. The agglomerates prepared with polyvinylpyrrolidone- K90 exhibited improved solubility, dissolution rate and micromeritic properties compared to those prepared with other polymers and pure drug. These optimized agglomerates showed rapid analgesic and anti-inflammatory activity besides exhibiting improved bioavailability of drug when compared to pure drug.
M3 - Article
SN - 1011-601X
VL - 20
SP - 218
EP - 226
JO - Pakistan Journal of Pharmaceutical Sciences
JF - Pakistan Journal of Pharmaceutical Sciences
IS - 3
ER -