Preparation Study and Quality Evaluation of Pudilan Sustained-release Capsule
|School||Wuhan University of Technology|
|Keywords||Pudilan solid dispersion sustained-release release HPLC|
Pudilan is a Chinese herbal compound preparation which is composed of taraxaci herba, scutellariae radix, isatidis radix and corydalis bungeanae herba, now Pudilan Xiaoyan Pian is the main commercial varieties. As Pudilan Xiaoyan Pian is a Chinese herbal compound preparation and the concentration of active ingrediengt of drug is not high, resulting its dose is huge and the need of taking four times daily and frequently administration. The solid dispersion technology is an effective method that can increase drug dispersion, regulate solubility and dissolution rate of drug, increase drug bioavailability. This study was designed to obtain extracts from four Chinese herbal medicines by modern extraction and separation technology and pudilan susta-ined-release capsule was prepared with extracts by using solid dispersion technology, thereby reducing the medication dose and frequency, significantly increasing patient’s compliance.In this study, we separately conducted the work that extracted and purificated baicalin from scutellariae radix, caffeic acid from taraxaci herba and corydalis bunge-anae herba, indirubin from isatidis radix through water decocting, the yield of extracts were:8.01%、30.27%and33.10%; and we individually conducted the content determ-ination through the establishment of HPLC, measured the content of active ingredi-ents of extracts were:78.02%、38.41%and89.26%. The results show that by taking the process conditions can make the active ingredients to a higher yield, the content determination is a reliable analytical method, good quality control and in line with the requirements of industrial production.Refering to an existing prescription and the actual situation we determined the ratio of the active ingredients of the drug:extract of scutellariae radix:extract of taraxaci herba and corydalis bungeanae herba:extract of isatidis radix=(48.06:133.70:49.65). We selected the method of solvent as the preparation of solid dispersions, determined the amount of ethyl cellulose, hydroxypropyl methyl cellulose and lactose as the main factors through one-factor experimental design, obtained the optimum prescription and process by orthogonal experimental design:ethyl cellulose(2.00g), hydroxypropyl methyl cellulose(0.20g) and lactose(2.00g). Study of the preparation process stability show it is stable and controllable and the drug release has a better reproducibility. The release curve equation is close to A equation model release, therefore, it achieves the effect of sustained-release. By thermal analysis we confirmed that drug and carriers formed solid dispersion, TLC also confirmed the main active ingredients of the drug. We separately established the analysis methods for determination of content and release in vitro through HPLC, The results show that the analysis methods are highly sensitive and specific. Through this analysis methods we can measure the content of baicalin in sample is17.38mg/100mg, and the sample release meet the requirement of sustained-release, the homogeneity of release is Good. By preliminary stability study we know that high temperature has almost no effect on the drug and high humidity and light have some effects, so the drug should be sealed and placed in dark and dry place. We know that this drug’s balance time of moisturizing is72h and critical relative humidity is72%through the study of critical relative humidity. Drug’s angle of repose is less than40°which shows liquidity is good; bulk density is0.5390g/ml, therefore we choose1st capsules to fill powder, and determine daily dose is two times and two each.The inspections of load difference, moisture content, arsenic salt content, heavy metal content and microbial limit show the indicators of this product meet the requirements.