The Preparation And In Vitro Drug-releasing Study Of Amylose-ibuprofen Complexes

Amylose, as one host-molecular, could form complex assemblies with some guest moleculars.The starch is composed of amylose and amylopectin,however,only the amylose in the starch have the effect of inclusion complexation.Because amylose and starch both have good biocompatibility and biodegradability,the amylose and starch became the excellent durg carrier,which has the broad prospects in the pharmaceutical industry. Ibuprofen is one nonsteroidal antiinflammatory drugs in clinic and is widely used for the treatment of inflammation of diseases, but it has severe side effects for stomach and low releasing capacity.Hence,in order to enhance the controlled release-function and reduce side effects, the preparation structure and conrolled release of the ibuprofen-starch complexes and ibuprofen-amylose complexes were studied in my work respectively.The series of different ibuprofen-amylose ratio complexes[1/6(IBU/AS-C)、 1/8(IBU/AS-C)、1/10(IBU/AS-C)、1/12(IBU/AS-C)、1/15(IBU/AS-C)、 1/20(IBU/AS-C)、1/30(IBU/AS-C)、1/60(IBU/AS-C)]and the series of different ibuprofen-starch ratio complexes [1/7(IBU/ST-C). 1/10(IBU/ST-C)、1/16(IBU/ST-C)、 1/25(IBU/ST-C)、1/30(IBU/ST-C)]were both prepared by alkali solutions method. As for the ibu-amylose complex series, the IBU content was analyzed using UV-spectroscopy, wihich has the results showed that 1/8(IBU/AS-C)、1/10(IBU/AS-C) and 1/12(IBU/AS-C) have the most IBU content.The results of X-ray diffraction (XRD) and FTIR proved that 1/8(IBU/AS-C)、1/10(IBU/AS-C) and 1/12(IBU/AS-C) have the most obvious features of complex-structure among all the ibu-amylose samples. Then,in order to further ensure the complex-structure of 1/8(IBU/AS-C)、 1/10(IBU/AS-C) and 1/12(IBU/AS-C),the results of DSC and Solid 13C NMR showed that three samples were complexes.The results of the drug-release test in vitro of the above three samples showed that the ibuprofen of the above three samples was hardly released in the vitro simulated stomach conditions,which can be attributed to the great stability of three samples in the vitro simulated stomach conditions,but the ibuprofen can be released gradually from the above three samples in the vitro intestine conditions at 0h～8h.Therefore,the controlled release behavior of ibuprofen-amylose complex at 1/8～1/12 ratio is not only beneficial to reduce the gastric damage,but also helpful for the achievement of sustained medication clinically.Similarly, the series of different ibuprofen-starch ratio complexes were investigated via the above same research methods.It can be proved that the structure of 1/10(IBU/ST-C) and 1/16(IBU/ST-C) were the best complex-structure among the ibu-starch samples.In the vitro simulated stomach and intestine conditions,the controlled release behavior of ibuprofen-starch complexes at 1/10～1/16 ratio is optimal.