Improved bioavailability of aceclofenac from spherical agglomerates: Development, in vitro and preclinical studies

S. Mutalik, A.N. Usha, M.S. Reddy, A.K. Ranjith, S. Pandey

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Abstract

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.
Original languageEnglish
Pages (from-to)218-226
Number of pages9
JournalPakistan Journal of Pharmaceutical Sciences
Volume20
Issue number3
Publication statusPublished - 2007

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Povidone
Non-Steroidal Anti-Inflammatory Agents
Biological Availability
Electron Scanning Microscopy
Solubility
Polymers
Pharmaceutical Preparations
Water
Methylene Chloride
Acetone
Wistar Rats
Spectrum Analysis
Pharmacokinetics
In Vitro Techniques
aceclofenac

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title = "Improved bioavailability of aceclofenac from spherical agglomerates: Development, in vitro and preclinical studies",
abstract = "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.",
author = "S. Mutalik and A.N. Usha and M.S. Reddy and A.K. Ranjith and S. Pandey",
note = "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",
year = "2007",
language = "English",
volume = "20",
pages = "218--226",
journal = "Pakistan Journal of Pharmaceutical Sciences",
issn = "1011-601X",
publisher = "Pakistan Journal of Pharmaceutical Sciences",
number = "3",

}

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

VL - 20

SP - 218

EP - 226

JO - Pakistan Journal of Pharmaceutical Sciences

JF - Pakistan Journal of Pharmaceutical Sciences

SN - 1011-601X

IS - 3

ER -