- Aspirin. Glucose Covalent Complexes Synthesis And In Vitro Release Study

For improving the drug effect of aspirin, reducing its side effect. In the paper, Glucose-aspirin conjugate was synthesized via a reaction of o-acetoxybenzoyl chloride and glucose in normal pressure, at 50℃, pyridine was used as catalyst in the reaction. Its structure was characterized by FTIR and 1HNMR. The drug-loading ratio was measured by UV spectrophotometry, its result was about 54.9%, and converting efficiency of o-acetoxybenzoyl chloride was 10.7%. In the different release medium, vitro release study showed that release rate of the conjugate was nearly zero order with no abrupt release. With the reduction of artificial gastric juice acidity, the release time of zero order grow. When PH=5, the release time of zero order was about 25h; the release time of zero order was about 28h in the artificial intestinal juice. It shows that the conjugate may lead to less side-effect and relieving stimulation of ASA on gastrointestinal tract.In addition, five new salicylic acid compounds in ether derivatives are prepared by the reaction of the salicylic acid and dibromoalkane with tetrabutylammonium bromide in DMF and deioned water, under the condition of atmospheric pressure and hot reflux, and their yields are above ninety percents. Their structures are characterized by FT-IR,GC-MS,H-NMR. Vitro release study showed that water-solubility of these compounds was very lower.