Study On Aceclofenac Sustained-Release Capsule With Microparticle-Coating Technology

Aceclofenac is a phenylacetic acid derivative with anti-inflammatory and its mean elimination half-life is about 3.5～4 hours. The anti-inflammatory activity of aceclofenac is relative to its plasma conceration. The aim of this work is to develop Aceclofenac sustained-release microparticle with a new fluid-bed technology to reduce dosing frequency and narrow the fluctuation of blood concentration.The article discuss the possibility of particle-coating of the 80～180μm aceclofenac particles by microparticle coating.HPLC method was utilized to determine the aceclofenac content in particles, UV method for assaying release of aceclofenac controlled release capsules. HPLC and UV methods were developed to analyze the intestinal absorption of aceclofenac in rats.The preformulation results showed that aceclofenac is not soluble in water or various physiological pH fluids.The solubility of aceclofenac in different media (pH value from 1.2 to 7.4)and the apparent partition coefficient in n-octanol/H_O system were determined.The absorption sites and the absorption kinetics were studied from various intestinal segments ligation using in situ perfusion method in rats. The research demonstrated that aceclofenac was absorbed in small intestine and colon in general and mostly absorbed in small intestine. The average absorb is 24.9% in small intestine and 7.62% in colon.The absorption fraction and absorption rate constant were 0.096,0.027 respectly. The mechanism of the gastrointestinal absorption of aceclofenac is transferred to intestine via passive...