| Coix Seed Oil (CSO) is extracted from the mature seed of the Coix laohryma-jobi. It has a variety of pharmacological activities, such as anti-cancer, lowering blood fat, increasing immunity, anti-inflammatory swelling, and anti-inflammatory bleeding. Recently, the Coix Seed Oil used in the clinically application is kanglaite Injection. But high pressure sterilization can cause a decline in the active ingredient content, poor stability and other adverse reactions in the production of injection. In this experiment, we use β-CD as experimental material, EPI as cross linking agent and CDP as carrier to prepare CSO-CDP. The main contents and results of the experiment are as follows:1 The preparation of CSO-CDP① Using P-CD as experimental material and EPI as cross linking agent to prepare CDP. To confirm the formulation of CDP, we use UV, SEM, IR and XRD.② A HPLC method was established by using Coixol as the index components and methodological investigation was carried out to evaluate the method. The results of HPLC showed that the peak area of Coixol had a good linear relationship. The regression equation of Coixol was Y=174901X-74436 (r2=0.9993). The specificity, precision and stability all meet the requirement which showed that the HPLC method can be used to determine the Coix Seed Oil inclusion compound.③ Using CDP content, inclusion time, inclusion temperature, stirring speed and ethanol content to inspect the entrapment rate. Response surface experiment was carried out to optimize the preparation process of Coix Seed Oil inclusion compound based on single factor experiments. The optimum preparation process of Coix Seed Oil inclusion compound was as follows:CDP content was 10.05 g, inclusion temperature was 24.92 ℃, and alcohol content was 0.19 g.2 The preparation of CSO-CDP lyophilized powder① Using appearance, hydration speed and leakage rate as test materials, We select the drying method from vacuum drying, freeze drying, and rotary evaporation drying. The results showed that we can get pure white inclusion compound which had a faster rehydration speed from vacuum freeze drying.② Using pre-freezing time, sample loading quantity and drying time to inspect the leakage rate. Response surface experiment was carried out to optimize the best vacuum freeze-drying process. The result was as follows:pre-freezing time was 11.85 h, sample loading quantity was 1.26 g, drying time was 48.53 h.3 The quality inspection of CSO-CDP lyophilized powder① Use SEM、IR and XRD to characterize the phases of CSO-CDP lyophilized powder and to verify the formation of the inclusion compound. The results indicated that the CSO-CDP lyophilized powder was significantly different from the CDP, which can be used to confirm the formulation.② The stability of the CSO-CDP lyophilized powder was detected by putting them under the condition of illumination, high temperature and high humidity. The results showed that CSO-CDP had good stability under illumination and high temperature. The lyophilized powder became toughness and agglomerate at high humidity condition which indicated that we need to keep dry during the procedure of preparation storage and transport of CSO-CDP lyophilized powder.③ According to the legend items of the solubility in the China Pharmacopoeia (version 2015),we determined the solubility of the CSO-CDP lyophilized powder. The results showed that the CSO-CDP had good solubility in distilled water, artificial gastric juice and artificial intestinal fluidIn this study, we prepare CSO-CDP lyophilized powder successfully and study the preparation process, the stability and the solubility.The lyophilized powder can improve the solubility and the stability of Coix Seed Oil significantly. |
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