Study On Preparation And Application Of New Pharmaceutical Excipients

Pharmaceutical excipient refers to the part in addition to the main drug in the pharmaceutical preparations, also can be referred to as the auxiliary materials. The pharmaceutical excipient plays an important role in the quality of medicines. In this study, waxy rice starch was used as raw material and subjected to enzymatic, cross- linking combined and enzymatic to obtain a series of different hydrolysis degree of starch samples. Furthermore, the morphology, iodine adsorption capacity, relative molecular weight distribution and so on of different hydrolysis degree of starch samples were characterized by scanning electron microscope(SEM), uv,HPLC, respectively. The liquid and filling of powder were comparison to select the best sample, which was applied to the pressure in the preparation of ibuprofen tablets directly as a new drug excipient. The quality of ibuprofen tablets were checked in order to get a kind of new pharmaceutical excipient. The research results have important and practical significance.(1) The native waxy rice starch was applied to prepare dextrin with different hydrolysis degrees by using β-amylase at different time, and the physicochemical properties of the dextrin were also investigated. Results showed that starch treated with β-amylase for 20 hours reached the maximum starch hydrolysis rate. Scanning electron microscopy(SEM) results showed that all enzyme-treated samples had more irregular fragments without granular structures. The maximum absorbance and iodine binding of enzyme-treated starches were reduced compared with their native starch parents. The position of maximum absorption peak of starch sample shifted obviously as increasing the hydrolysis degree. As the time of hydrolysis, macromolecules were reduced and small molecules were increased. At the same temperature, the solubility of enzyme treated starch were higher than that of native starch, which was different from the swelling power. Meanwhile, the solubility and swelling power increased with the increase of hydrolysis degree and the temperature. Compared wit h native waxy rice starch, the samples with enzyme-treated revealed more remarkable improvement on transparency; but which were constantly descending with the hydrolysis degree increasing.(2) The waxy rice starch was treatments by cross- linking. The experimental factors include the agent of cross- linking, the p H of reaction time and temperature were investigated. The highest phosphorus content(0.37% < 0.4%) and deposit amount(3.05) were reached when the waxy rice starch with 3% at 40 oC for 3h in p H of 11. The native and cross- linking starch showed A-type X-ray diffraction pattern. As the cross-linking reaction with the increase of time, the degree of substitution increased, the proportion of the crystalline area reduce 1.8-8.5%, the pasting temperature of the cross- linking starch were high than native for 1.13-6.56 oC,the enthalpy of gelatinization of the cross- linking starch were reduced than native for 3.88-6.56 J/g. Solubility, swelling and transparency were reduced than the native starch.The cross- linking starch was applied to prepare dextrin with different hydrolysis degrees by using β-amylase at different time. The maximum hydrolysis rate was 80.94%. The result of SEM show that the particle structures were broken after enzymatic fragmentation, increasing of the hydrolysis, the molecular weight of samples were gradually reduced; with increasing temperature, the solubility of cross-linking starch was lower than samples; hydrolysis rate increases transparency, but also higher than the cross-linking starch and raw starch.(3) Powder samples were prepared by the nature of measurement: the fluidity and filling property of power were characterized by bulk density, tapped density, Hausner ratio, Carr’s index and angle of repose and Kawakita equation parameters. Comprehensive analysis of various samples powder indexes, the cross- linking starch was enzymatic for 20 h and then applied to direct compression tablets as pharmaceutical excipients.(4) Lβ-20 was applied to ibuprofen tablets as pharmaceutical excipients. The prescription tablet was determined by the indicators of dissolution. The dissolution and content of the tablets were up to the 2010 edition of ―Chinese Pharmacopoeia‖ bipartite standards. According to the principles of the 2010 edition of ―Chinese Pharmacopoeia‖ concerning the stability of a set of high-temperature stability(60oC±2oC), humidity(RH90±5%), light(4500±500lx) and other conditions. Experimental results show that the tablets have glare-resistant, high-temperature. But the high- humidity environment has a certain influence on the tablets.