| The ingredients of Xiao'er Qingre Zhike Orally Solution is listed in the Volume I of "Pharmacopoeia of the People's Republic of China". It consists of Herb a Ephedrae, Semen Armeniacae Amarum, Gypsum Fibrosum, Radix Glycirrhizae, Radix Scutellariae, Radix Isatidis and Rhizoma Menispermi. Its action is to remove heat, release stagnated lung-qi, relieve asthma and soothe the sore throat. It is primarily applied to affection by exopathogen of infants, cough and yellow-phlegm et al. In this study, using this ingredients as the model drug, the production of the orally dissolving tablets of traditional drug was approached; the quality standard was created; the stability of preparation was studied; and the pharrnacodynamics was compared with the orally solution in the market.The completely quality standard of Xiao'er Qingre Zhike Orally Dissolving Tablets (QRZK-ODT) was formed in this paper. TLC method was used to identify the four kinds of main materia medica: Herba Ephedrae, Radix Scutellariae, Semen Armeniacae Amarum, Radix Glycirrhizae. The determination of disintegration and friability of tablets were carried out. HPLC-Diode Array Detector was used to assay Ephedrine, Baicalin and Glycyrrhizic acid.In this study, it was focused on the production of QRZK-ODT. At first, the extraction method in the Pharmacopoeia was used to assure to get the effective components and the extracted liquid was spray-dried. Taking the high content of effective components and the low water content as the aim, the spray-dry parameter was optimized. The temperature of inlet air was 160~180 癈, the rate of extract addition was 15ml/min, the pressure of nozzle air was 1.0-1.2kg/cm2. The obtained powder was granulated with the top-spray & rotate fluid-bed instrument. Through the basis of single-factor experiments, it was found that the three key parameters were: the temperature of inlet air, the rate of binder addition, thevolume of atomizing air. Using the pellets size distribution and friability as the criterion, the orthogonal-designed method was used to optimize the process condition. When the forenamed parameters were set as 50 癈, 4ml/min, 60L/min respectively, the volume of inlet air was 10~30m3/h and rotating speed is 200r/min. The produced particles were as follows: yield components of #75~150#m was 69%, DSO was 95#m, Fr was 6%. After compared several coating process and materials, the preparation was decided to use bottom-spray method to coat with SURELEASE. According to the degree and efficiency of taste-mask and through the orthogonal-design, the conditions were: inlet air temp, was 72 癈, spraying rate was 3ml/min, atomization air volume was 85L/min, inlet air volume was 20~40m3/h, the mass addition of coating material (EC) is 20%. After coating, these particles were mixed with water-soluble excipient and pressed to tablets at the pressure of 0.5MPa. The products not only disintegrated in a short time, but also tasted well.The results of the stability tests showed: QRZK-ODT were stable to light, air and 40 癈. However, limited with the characters of excipient, QRZK-ODT's nature was changed under the following conditions: high temperature of 60 癈 or high humidity of RH75%. So, QRZK-ODT should be tightly closed and stored at cool place.The pharmacodynamics experiments of inhibition of cough, inflammation and fever were done. The results show that QRZK-ODT could obviously remove heat, relieve cough and have anti-inflammatory effect. There was no difference between QRZK-ODT and the oral solution in market.This study prove the method that the granules can be directly-pressed after powder taste-mask coating by fluid-bed, and it is suitable for producing the orally dissolving tablets. |
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