Aceclofenac topical dosage forms: in vitro and in vivo characterization.

Abstract

Aceclofenac is a new generation non-steroidal anti-inflammatory drug showing effective anti-inflammatory and analgesic properties. It is available in the form of tablets of 100 mg. Importance of aceclofenac as a NSAID has inspired development of topical dosage forms. This mode of administration may help avoid typical side effects associated with oral administration of NSAIDs, which have led to its withdrawal. Furthermore, aceclofenac topical dosage forms can be used as a supplement to oral therapy for better treatment of conditions such as arthritis. Ointments, creams, and gels containing 1% (m/m) aceclofenac have been prepared. They were tested for physical appearance, pH, spreadability, extrudability, drug content uniformity, in vitro diffusion and in vitro permeation. Gels prepared using Carbopol 940 (AF2, AF3) and macrogol bases (AF7) were selected after the analysis of the results. They were evaluated for acute skin irritancy, anti-inflammatory and analgesic effects using the carrageenan-induced thermal hyperalgesia and paw edema method. AF2 was shown to be significantly (p < 0.05) more effective in inhibiting hyperalgesia associated with inflammation, compared to AF3 and AF7. Hence, AF2 may be suggested as an alternative to oral preparations.

• Authors: Kamal Dua, Kavita Pabreja, Malipeddi Venkata Ramana
• Journal: Acta pharmaceutica (Zagreb, Croatia) (Acta Pharm) Vol. 60 Issue 4 Pg. 467-78 (Dec 2010) ISSN: 1846-9558 [Electronic] Poland
• PMID: 21169138 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Acrylic Resins
• Anti-Inflammatory Agents, Non-Steroidal
• Gels
• Ointments
• Diclofenac
• Hypromellose Derivatives
• Polyethylene Glycols
• carbopol 940
• Carrageenan
• Methylcellulose
• aceclofenac

Topics

• Acrylic Resins (chemistry)
• Administration, Topical
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (administration & dosage, chemistry, toxicity)
• Carrageenan
• Diclofenac (administration & dosage, analogs & derivatives, chemistry, toxicity)
• Edema (chemically induced, drug therapy)
• Gels
• Hyperalgesia (chemically induced, drug therapy)
• Hypromellose Derivatives
• Inflammation (drug therapy)
• Male
• Methylcellulose (analogs & derivatives, chemistry, metabolism)
• Ointments
• Polyethylene Glycols (chemistry)
• Rabbits
• Rats
• Rats, Wistar
• Skin Irritancy Tests
• Solubility