Aceclofenac: An Experimental Study

The present study relates to the stable fixed dose combination comprising of Aceclofenac as a glycolic acid ester of diclofenac having analgesic and anti-inflammatory action and Thiocolchicoside, as a glycosulfurated analogue of colchicine which is well known centrally acting muscle relaxant in unit dosage form and to the preparation method thereof. Aceclofenac is very susceptible to decomposition under hydrolytic, oxidative stress and exposure to light. The major degradation product identified was diclofenac, which was detected as an impurity in the2 formulation. Many of the marketed formulation of Aceclofenac tablets having issue of high content of diclofenac impurity. Diclofenac having more gastrointestinal adverse effects such as gastritis,

Chemical interactions between API and excipients result in a degradation of the API, which can influence the absorption and therapeutic effect. Physical interactions can alter the physicochemical parameters of the components, e.g. the solubility, the dissolution rate and finally the bioavailability. Adsorption of drug molecules onto the surface of excipients can render the drug unavailable for dissolution and diffusion, which can result in reduced bioavailability. For example, antibacterial activity of cetylpyridinium chloride was decreased when magnesium stearate was used as lubricants in tablet containing cetylpyridinium chloride; this was due to adsorption of cetylpyridinium cation by stearate anion on magnesium stearate particle[9]. In one of the investigation, it was observed that dissolution of drug was decreased due to adsorption of drug on the surface of microcrystalline cellulose. In a similar context, adsorption of novel k-opoid agonist by microcrystalline cellulose led to incomplete drug release from the capsules. Adsorption may also initiate chemical breakdown. Colloidal silica was shown to catalyze nitrozepam degradation in tablet dosage form, possibly by adsorptive interactions altering electron density in the vicinity of the labile azo group and thus facilitating attack by hydrolyzing entities[10]. Investigation of the incompatibility between the components of the dosage form is critical in the early stages of the development of a stable dosage form. Differential scanning calorimetry (DSC) has been widely used to assess incompatibility between formulation components, because the method is fast and versatile and requires very small quantity of