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Preparation, in vitro, preclinical and clinical evaluations of once daily sustained release tablets of aceclofenac.
Arch Pharm Res. 2007 Feb; 30(2):222-34.AP

Abstract

The objective of the present study was to develop "once daily" sustained release tablets of aceclofenac by direct compression using hydroxypropyl methylcellulose-K4M (HPMC). The solubility studies of aceclofenac were conducted to select suitable dissolution media. The drug-excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical, in vitro drug release and stability studies. Preclinical (anti-inflammatory, analgesic, pharmacokinetic and toxicity studies) and clinical pharmacokinetic studies were conducted for optimized tablets. Based on the preformulation results, microcrystalline cellulose (MCC), dicalcium phosphate and spray dried lactose (SDL) were selected as directly compressible vehicles. Because of the incompatibility with aceclofenac, SDL was excluded from the study. The physicochemical properties of tablets were found within the limits. By comparing the dissolution profiles with the marketed product, the tablet containing HPMC (45%) and MCC (30%) along with talc and magnesium stearate (1% w/w, each) (Tablet B7) was considered as a better formulation. This tablet exhibited almost similar drug release profile in different dissolution media as that of marketed tablet. Tablet B7 was stable in accelerated conditions for 6 months. The composition of this tablet showed almost similar preclinical pharmacological activities compared to marketed tablet composition and did not exhibit any toxicity in rats and mice with respect to tested haematological and biochemical parameters along with body weight, food and water intake. The pharmacokinetic study in healthy human volunteers indicated that B7 tablet produced an extended drug release of drug upto 24 h as that of marketed product with almost identical pharmacokinetic parameters.

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Authors+Show Affiliations

Mutalik S
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal 576 104, Karnataka State, India, Karnataka. srinivas.mutalik@manipal.edu
Naha A
No affiliation info available
Usha AN
No affiliation info available
Ranjith AK
No affiliation info available
Musmade P
No affiliation info available
Manoj K
No affiliation info available
Anju P
No affiliation info available
Prasanna S
No affiliation info available

MeSH

AnimalsAnti-Inflammatory Agents, Non-SteroidalArea Under CurveDelayed-Action PreparationsDiclofenacDrug Administration ScheduleDrug CompoundingDrug Evaluation, PreclinicalDrug StabilityEdemaExcipientsHalf-LifeHumansMaleMetabolic Clearance RateMicePainRatsSolubilityTabletsToxicity Tests, Chronic

Pub Type(s)

Journal Article
Randomized Controlled Trial

Language

eng

PubMed ID

17366745

Citation

Mutalik, S, et al. "Preparation, in Vitro, Preclinical and Clinical Evaluations of once Daily Sustained Release Tablets of Aceclofenac." Archives of Pharmacal Research, vol. 30, no. 2, 2007, pp. 222-34.
Mutalik S, Naha A, Usha AN, et al. Preparation, in vitro, preclinical and clinical evaluations of once daily sustained release tablets of aceclofenac. Arch Pharm Res. 2007;30(2):222-34.
Mutalik, S., Naha, A., Usha, A. N., Ranjith, A. K., Musmade, P., Manoj, K., Anju, P., & Prasanna, S. (2007). Preparation, in vitro, preclinical and clinical evaluations of once daily sustained release tablets of aceclofenac. Archives of Pharmacal Research, 30(2), 222-34.
Mutalik S, et al. Preparation, in Vitro, Preclinical and Clinical Evaluations of once Daily Sustained Release Tablets of Aceclofenac. Arch Pharm Res. 2007;30(2):222-34. PubMed PMID: 17366745.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation, in vitro, preclinical and clinical evaluations of once daily sustained release tablets of aceclofenac. AU - Mutalik,S, AU - Naha,A, AU - Usha,A N, AU - Ranjith,A K, AU - Musmade,P, AU - Manoj,K, AU - Anju,P, AU - Prasanna,S, PY - 2007/3/21/pubmed PY - 2007/3/30/medline PY - 2007/3/21/entrez SP - 222 EP - 34 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 30 IS - 2 N2 - The objective of the present study was to develop "once daily" sustained release tablets of aceclofenac by direct compression using hydroxypropyl methylcellulose-K4M (HPMC). The solubility studies of aceclofenac were conducted to select suitable dissolution media. The drug-excipient mixtures were subjected to preformulation studies. The tablets were subjected to physicochemical, in vitro drug release and stability studies. Preclinical (anti-inflammatory, analgesic, pharmacokinetic and toxicity studies) and clinical pharmacokinetic studies were conducted for optimized tablets. Based on the preformulation results, microcrystalline cellulose (MCC), dicalcium phosphate and spray dried lactose (SDL) were selected as directly compressible vehicles. Because of the incompatibility with aceclofenac, SDL was excluded from the study. The physicochemical properties of tablets were found within the limits. By comparing the dissolution profiles with the marketed product, the tablet containing HPMC (45%) and MCC (30%) along with talc and magnesium stearate (1% w/w, each) (Tablet B7) was considered as a better formulation. This tablet exhibited almost similar drug release profile in different dissolution media as that of marketed tablet. Tablet B7 was stable in accelerated conditions for 6 months. The composition of this tablet showed almost similar preclinical pharmacological activities compared to marketed tablet composition and did not exhibit any toxicity in rats and mice with respect to tested haematological and biochemical parameters along with body weight, food and water intake. The pharmacokinetic study in healthy human volunteers indicated that B7 tablet produced an extended drug release of drug upto 24 h as that of marketed product with almost identical pharmacokinetic parameters. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/17366745/Preparation_in_vitro_preclinical_and_clinical_evaluations_of_once_daily_sustained_release_tablets_of_aceclofenac_ L2 - http://ovidsp.ovid.com/ovidweb.cgi?T=JS&PAGE=linkout&SEARCH=17366745.ui DB - PRIME DP - Unbound Medicine ER -