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Enhancement of dissolution rate and bioavailability of aceclofenac: a chitosan-based solvent change approach.
Int J Pharm. 2008 Feb 28; 350(1-2):279-90.IJ

Abstract

In this study the significant effect of chitosan on improving the dissolution rate and bioavailability of aceclofenac has been demonstrated by simple solvent change method. Chitosan was precipitated on aceclofenac crystals using sodium citrate as the salting out agent. The pure drug and the prepared co-crystals with different concentrations of chitosan (0.05-0.6%) were characterized in terms of solubility, drug content, particle size, thermal behaviour (differential scanning calorimetry, DSC), X-ray diffraction (XRD), morphology (scanning electron microscopy, SEM), in vitro drug release and stability studies. The in vivo performance was assessed by preclinical pharmacodynamic (analgesic and anti-inflammatory activity) and pharmacokinetic studies. The particle size of the prepared co-crystals was drastically reduced during the formulation process. The DSC showed a decrease in the melting enthalpy indicating disorder in the crystalline content. The XRD also revealed a characteristic decrease in crystallinity. The dissolution studies demonstrated a marked increase in the dissolution rate in comparison with pure drug. The considerable improvement in the dissolution rate of aceclofenac from optimized crystal formulation was attributed to the wetting effect of chitosan, decreased drug crystallinity, altered surface morphology and micronization. The optimized co-crystals exhibited excellent stability on storage at accelerated conditions. The in vivo studies revealed that the optimized crystal formulation provided a rapid pharmacological response in mice and rats besides exhibiting improved pharmacokinetic parameters in rats.

Authors+Show Affiliations

Manipal College of Pharmaceutical Sciences, Manipal University, Manipal 576104, Karnataka, India. ssmutalik@yahoo.comNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

17945447

Citation

Mutalik, Srinivas, et al. "Enhancement of Dissolution Rate and Bioavailability of Aceclofenac: a Chitosan-based Solvent Change Approach." International Journal of Pharmaceutics, vol. 350, no. 1-2, 2008, pp. 279-90.
Mutalik S, Anju P, Manoj K, et al. Enhancement of dissolution rate and bioavailability of aceclofenac: a chitosan-based solvent change approach. Int J Pharm. 2008;350(1-2):279-90.
Mutalik, S., Anju, P., Manoj, K., & Usha, A. N. (2008). Enhancement of dissolution rate and bioavailability of aceclofenac: a chitosan-based solvent change approach. International Journal of Pharmaceutics, 350(1-2), 279-90.
Mutalik S, et al. Enhancement of Dissolution Rate and Bioavailability of Aceclofenac: a Chitosan-based Solvent Change Approach. Int J Pharm. 2008 Feb 28;350(1-2):279-90. PubMed PMID: 17945447.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Enhancement of dissolution rate and bioavailability of aceclofenac: a chitosan-based solvent change approach. AU - Mutalik,Srinivas, AU - Anju,Parambil, AU - Manoj,Krishnan, AU - Usha,Achutha Nayak, Y1 - 2007/09/12/ PY - 2007/07/23/received PY - 2007/09/03/revised PY - 2007/09/03/accepted PY - 2007/10/20/pubmed PY - 2008/4/9/medline PY - 2007/10/20/entrez SP - 279 EP - 90 JF - International journal of pharmaceutics JO - Int J Pharm VL - 350 IS - 1-2 N2 - In this study the significant effect of chitosan on improving the dissolution rate and bioavailability of aceclofenac has been demonstrated by simple solvent change method. Chitosan was precipitated on aceclofenac crystals using sodium citrate as the salting out agent. The pure drug and the prepared co-crystals with different concentrations of chitosan (0.05-0.6%) were characterized in terms of solubility, drug content, particle size, thermal behaviour (differential scanning calorimetry, DSC), X-ray diffraction (XRD), morphology (scanning electron microscopy, SEM), in vitro drug release and stability studies. The in vivo performance was assessed by preclinical pharmacodynamic (analgesic and anti-inflammatory activity) and pharmacokinetic studies. The particle size of the prepared co-crystals was drastically reduced during the formulation process. The DSC showed a decrease in the melting enthalpy indicating disorder in the crystalline content. The XRD also revealed a characteristic decrease in crystallinity. The dissolution studies demonstrated a marked increase in the dissolution rate in comparison with pure drug. The considerable improvement in the dissolution rate of aceclofenac from optimized crystal formulation was attributed to the wetting effect of chitosan, decreased drug crystallinity, altered surface morphology and micronization. The optimized co-crystals exhibited excellent stability on storage at accelerated conditions. The in vivo studies revealed that the optimized crystal formulation provided a rapid pharmacological response in mice and rats besides exhibiting improved pharmacokinetic parameters in rats. SN - 0378-5173 UR - https://www.unboundmedicine.com/medline/citation/17945447/Enhancement_of_dissolution_rate_and_bioavailability_of_aceclofenac:_a_chitosan_based_solvent_change_approach_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(07)00760-0 DB - PRIME DP - Unbound Medicine ER -