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ObjectiveTo screen the preparation technology of Baoyuan chewable tablets and to preliminarily elucidate its anti-fatigue effect and mechanism. MethodTaking encapsulation rate of volatile oil， extract rate and extraction rate of active ingredients as indexes， single factor test and orthogonal test were used to optimize the volatile oil inclusion， aqueous decoction and formulation molding processes of Baoyuan chewable tablets. ICR rats were randomly divided into the blank group， model group， Gaoshan Hongjingtian oral liquids group（6.01 mL·kg-1） and and Baoyuan chewable tablets low， medium， and high dose groups（2.1， 4.2， 8.4 g·kg-1）， 8 mice in each group， and were administered by gastric gavage at the corresponding dose once a day， the blank and model groups were given equal volume of saline for 15 d. After the last administration for 30 min， the mice were loaded with 5% of the body mass of lead at the tail and swam until exhaustion to establish the fatigue model， and the weighted swimming time of the mice in each group was recorded， meanwhile， the muscle tissues of the mice were sliced， stained by hematoxylin-eosin（HE） and subjected to pathological observation， and the levels of blood urea nitrogen（BUN）， lactic acid（LA）， liver glycogen（LG）， activities of lactate dehydrogenase（LDH） and creatine kinase（CK） in the serum were determined. ResultThe optimal inclusion process of cinnamon oil in Baoyuan chewable tablets was 10∶1 for β-cyclodextrin-volatile oil， and inclusion at 50 ℃ for 2 h with saturated aqueous solution method. The optimal water extraction process was to extract twice， adding 10 times of water to extract for 50 min for the first time， and adding 9 times of water to extract for 40 min for the second time. The ratio of the extract of Baoyuan chewable tablets with microcrystalline cellulose， maltodextrin， mannitol， citric acid， magnesium stearate was 63∶13∶8∶17∶17∶1∶1， the tablets were pressed by wet granulation， the each tablet weight was 1.2 g， and the hardness was 60-80 N. Compared with the model group， Baoyuan chewable tablets low， medium， and high dose groups could significantly prolong the exhaustion time of mice in weight bearing swimming（P<0.05， P<0.01）， and improve the exercise endurance of the body， and the results of HE staining showed that all dose groups of Baoyuan chewable tablets could significantly improve the muscle tissue damage caused by exercise， significantly reduce the levels of BUN， LA and the activities of LDH and CK in serum（P<0.01）， and significantly increase the content of LG（P<0.05， P<0.01）. ConclusionThe optimized preparation process of Baoyuan chewable tablets is stable and feasible， and the preparation can improve exercise endurance by increasing the LG level in liver tissue， and relieve muscle soreness by accelerating the removal of LA from the body， and reduce CK and LDH activities to exert anti-fatigue effects.
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OBJECTIVE To e stablish the fingerprint of Qings hen tiaozhi xiaoke tablets （QTXT）and carry out the analysis of chemical pattern recognition ，and determine the contents of seven active components simultaneously. METHODS Using coptisine hydrochloride as reference ，the Similarity Evaluation System for Chromatographic Fingerprint of TCM （2012 edition）was utilized to establish the HPLC fingerprints of 13 batches of QTXT and analyze their similarity. The common peaks were confirmed by comparing with the chromatogram of the mixed control ；the attribution of the common peak was determined by comparing the chromatograms of the sample solutions of single decoction pieces and negative sample solutions ；using SPSS 22.0 and SIMCA 14.1 software，cluster analysis （CA），principal component analysis （PCA）and orthogonal partial least squares-discriminant analysis （OPLS-DA）were carried out ，and the markers affecting the quality of QTXT were screened ，using the variable importance in projection（VIP）value greater than 1 as the standard. Using coptisine hydrochloride as internal reference ，the contents of naringin ， hesperidin，neohesperidin，berberine hydrochloride ，palmatine hydrochloride and lovastatin were determined by quantitative analysis of multicomponents by single marker （QAMS），and then compared wi th the result s（except for coptisine hydrochloride ） of external standard method. RESULTS There were 17 Δ 基金项目：江苏省“双创团队”项目[No.（2018）2024号] ＊硕士研究生。研究方向：中药新药药学。E-mail：2769544062@ common peaks in 13 batches of QTXT ，and the similarity was qq.com 0.987-0.999. Seven chromatographic peaks were identified ， # 通信作者：副研究员，硕士生导师，博士。研究方向：中药药剂 namely naringin （peak 4）， hesperidin （peak 5）， 学。E-mail：tsliur411@sina.com neohesperidin（peak 6），coptisine hydrochloride （peak 8）， ·1204· China Pharmacy 2022Vol. 33 No. 10 中国药房 2022年第33卷第10期 palmatine hydrochloride （peak 9），berberine hydrochlo ride（peak 10），lovastatin（peak 14）. Peaks 7-10 were the exclusive peaks of Coptis chinensis ；peaks 3-6 and 11-13 were the exclusive peaks of bran-fried Fructus aurantii ；peak 14 was the exclusive peak of Monascus purpureus ；peak 1 was the common peak of C. chinensis and M. purpureus . Peak 2 and 15 were the common peak of bran-fried F. aurantii and M. purpureus ；peaks 16 and 17 were the common peaks of 6 traditional Chinese medicines. The results of CA showed that 13 batches of QTXT could be divided into three categories ，S2 was clustered into one category ，S1，S9，S10 were clustered into one category ，S3-S8 and S 11-S13 were clustered into one category. The results of PCA showed that accumulative variance contribution of the first three principal components was 85.120％. Compared with CA ，S1 was further distinguished from S9 and S 10 by PCA. OPLS-DA showed that 7 common peaks with VIP value greater than 1（from large to small ）were peak 10 （berberine hydrochloride ），peak 9（palmatine hydrochloride ），peak 5（hesperidin），peak 11 and peak 8（coptisine hydrochloride ）， peak 12 and peak 6（neohesperidin）. The contents of naringin ，hesperidin，neohesperidin，berberine hydrochloride ，palmatine hydrochloride and lovastatin measured by QAMS were 40.198-77.552，6.138-13.413，71.823-125.868，11.274-49.951，3.303- 5.367，1.821-3.185 mg/g，respectively. The contents of naringin ，hesperidin，neohesperidin，berberine hydrochloride ，coptisine hydrochloride，palmatine hydrochloride and lovastatin measured by external reference method were 41.454-79.976，6.404-13.993， 74.068-129.081，11.627-51.512，5.922-12.020，3.158-5.131 and 1.901-3.325 mg/g，respectively. The deviations of the two methods （except for coptisine hydrochloride ）were all less than 3.00％. CONCLUSIONS The established HPLC fingerprint and the method of QAMS are simple ，accurate and reproducible. Combined with chemical pattern recognition analysis ，it can be used for the quality evaluation of QTXT. Berberine hydrochloride ，palmatine hydrochloride and other components may be the markers affecting the quality of the drug.
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Objective To simultaneously determinate the contents of four active ingredients (Ephedrine Hydrochloride, Pseudoephedrine Hydrochloride, Amygdalin and Glycyrrhizinate) ofSan Ao Decoction by HPLC; To optimize the extracting process ofSan Ao Decoction.Methods The orthogonal test was employed. Volume of water, time of extraction and times of extraction were set as investigation factors; the transport rates of Ephedrine Hydrochloride, Pseudoephedrine Hydrochloride, Amygdalin and Glycyrrhizinate and the extraction rates were set as investigation indexes to conduct multi-indexes grading.Results The influence factors of the extraction ofSao Ao Decoction were the times of extraction > decoction time > the volume of water. The best extraction condition was: ten fold water; extract for three times; 1 h for each time.Conclusion The optimized extraction process is stable and feasible.
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This paper was aimed to study the dynamic changes of San-Ao(SA) decoction in different compatibility of ephedrine hydrochloride,pseudoephedrine hydrochloride,amygdalin and glycyrrhizic acid.HPLC was used to simultaneously determinate the transfer rate of SA decoction of ephedrine hydrochloride,pseudoephedrine hydrochloride,amygdalin and glycyrrhizic acid.Kromasil C18 (4.6 mm×250 mm,5μm) column was selected with methanol and 0.1% phosphoric acid as a mobile phase to gradient.The flow rate was 1 mL·min-1.The column temperature was 30℃.The injection volume was 10μL.Ephedrine hydrochloride,pseudoephedrine hydrochloride and amygdalin were detected at the wavelength of 208 nm.The glycyrrhizic acid was detected at the wavelength of 250 nm.The results showed that the transfer rate of ephedrine hydrochloride in decoction was more than that of the single preparation.The transfer rate of pseudoephedrine hydrochloride was the highest in the combination of ephedra and bitter almond.The transfer rate of amygdalin was the highest in the combination of ephedra and bitter almond.The transfer rate of glycyrrhizic acid in decoction was more than that of the single preparation.It was concluded that there were dynamic changes in the boiling process during herbal decoction preparation.The effectiveness and stability of Chinese medicine should be improved according to these changes.
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Objective To study the releasing properties and mechanism in vitro of the active ingredients of the gastric floating sustained-release tablet containning Zuojin Pellet extraction(ZJ-GFST).Methods The release rates of berberine,palmatine,evodiamine,and rutaecarpine from ZJ-GFST in vitro within 8 h were measured by using rotating basket method in Chinese Pharmacopeia.The cumulative curve of drug release data was fitted to zero order,first-order and Higuchi equation to ascertain the kinetic modeling of drug release.Release mechanism was ascertained using Peppas equation.Results The similar factors of the cumulative release curve of all the four ingredients mutually compared were more than 80%,indicating that the release of the four ingredients were similar.The cumulative release rate of all the four ingredients fitted Higuchi equation.The value of slopes of Peppas models of all the four ingredients were more than 0.45,indicating that drug released by concurrent action of diffusion and matrix erode(non-fickian diffusion).Conclusion The releasing properties in vitro of the active ingredients of ZJ-GFST is consistent.
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Object To investigate the effects of ultra-fine powder technique and granularity of pellets on dissolution rate in vitro. Methods The dissolution rate of ultra-fine ERMIAO PILL with different granule diameters in vitro was measured and compared with the index of berberine by UV spectro-photometry. Results The dissolution parameters T 50 and T d of four kinds of ultra-fine ERMIAO PILL are 61.60, 19.48, 17.84, 8.97 min and 102.3, 33.29, 26.98, 14.77 min, respectively. Those of general powder ERMIAO PILL with granule diameter of 2.4 mm are 89.61 and 155.68 min. Conclusion The dissolution rate of ultra-fine powder is quicker than that of general powder, and the rate increases with the granularity of PILL decreasing.
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AIM:To study the influence of material and configuration of microfiltration membranes on preparation of mono-ammonium glycyrrhizinate liposome(MGL) by membrane extrusion. METHODS: MGL were preparated by conventional rotary-evaporated film dispersion method and sonication,and MGL were extruding through 9 kinds of microfiltration membranes with 3 kinds of aperture specs of 0.1,0.2,0.45 ?m.The methods were evaluated by the filtration efficiency and the leakage rate of drug from liposomes. RESULTS: MGL were easily extruding through microfiltration membranes of NY6,PTFE,PVDF,PP and PC.MGL could not extruding through microfiltration membranes of PES,CN,CA and CA-CN.MGL become hardly to extrude through microfiltration membranes when increasing in the concentration of liposomes or the content of cholesterol.The leakage rate of drug from MGL was small when extruding through microfiltration membranes. CONCLUSION: The material and configuration of microfiltration membranes can remarkably influence the preparation of MGL by membrane extrusion method,and PC microfiltration membrane was selected.
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AIM: To elucidate the effect of HPMC on the floating and releasing performances of Zuojin Gastric Floating Sustained-Release Tablets(ZJ-GFST) and to select the optimum matrix adjuvant for ZJ-GFST. METHODS: Seven kinds of ZJ-GFST from pharmaceutical factories as main adjuvant respectively.The floating lag time and the sustained floating time were used to evaluate the floating performance of ZJ-GFST.The accumulative releasing rates of berberine and palmatine in vitro were used to evaluate the releasing efficiency of ZJ-GFST. RESULTS: The tablets prepared with HPMC MK-100000 and MK-15000 disintegrated quickly when contacting with water, and the tablets prepared with HPMC MK-100M and MK-4000 had too long floating lag time and low release speed.The tablets prepared with HPMC 60RT-50、K-4M and MK-1500 all possessed short floating lag time and long sustained floating time and suitable drug releasing rate. CONCLUSION: The selected HPMC is 60RT-50.
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AIM: To preparate brucine liposome. METHODS: Brucine liposomes were preparated by a combination of ammonium sulfate transmembrane gradients method and extrusion through microfiltration membranes.The methods were evaluated by particle morphology,the size range,and encapsulation efficiency. RESULTS: The optimal preparating process parameters of brucine nanometer liposome were lecithin-to-cholesterin ratio of 100∶15,the volume of 0.1 mol/L of water solution of ammonium sulfate being 66.7 times as large as lecithin,the volume of brucine being 0.0167 times than lecithin,the temperature and the time of incubating being 40 ℃ and 20 min,respectively.The encapsulation efficiency of this method was over 90%. CONCLUSION: Preparation of brucine liposomes by a combination of ammonium sulfate transmembrane gradients method and extrusion through microfiltration membranes is feasible.
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AIM: To study preparation of strychnine solid liposome. METHODS: Sorbitol carrier aggradation method and freeze drying method were used to prepare strychnine solid liposomes. They were evaluated by particle morphology, the size range, resolvable peculiarity in the water, encapsulation efficiency. RESULTS: The particles of liposome by sorbitol carrier aggradation method were less than that by freeze drying method, and its encapsulation efficiency was higher than that by freeze drying method. CONCLUSION: Sorbitol carrier aggradation method is better than freeze drying method.
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AIM: To select optimum purification of Qingluotongbi decoction (Caulis Sinomenii etc.). METHODS: Qingluotongbi decoction was refined respectively by ceramic membrane microfiltration, ultrafiltration, alcohol sedimentation, high speed centrifugalization, flocculation and macroporous resin absorption. Their refining effect was compared according to indexes of color, clarity, loss rate of sinomenine, removal ratio of impurity. RESULTS: All kinds of purification made decoction light and clear. Removal ratio of impurity by macroporous resin absorption was the highest and reached 80% or more. Removal ratio of impurity by ceramic membrane microfiltration was 21.17% , less than that by alcohol sedimentation or ultrafiltration, but more than that by flocculation and centrifugalization. Loss rate of sinomenine by AB 8 type macroporous resin absorption was the lowest and reached 6.39% , and that by ceramic membrane microfiltration was 15.31% , less than that by ultrafiltration, alcohol sedimentation, centrifugalization and flocculation. The chromatogram of decoction disposed by macroporous resin was different from that of decoction unsettled, but that disposed by ceramic membrane was similar to that of decoction unsettled. CONCLUSION: The technique of ceramic membrane microfiltration is optimum purification of Qingluotongbi decoction with the virtues of moderate removal ratio of impurity, small amount lose rate of sinomenine and simple process.
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Objective: To evaluate effect of refining of decoctions of medicinal materials of radix and rhizome by microfiltration of inorganic ceramic membrane. Methods: The decoctions of 7 medicinal materials of radix and rhizome were processed by inorganic ceramic membrane, and the whole solids and effective ingredients were determined. Results: The decoctions of Chinese traditional medicine became clear after microfiltration. The whole solids were decreased by 15～38%, and the lost rate of effective ingredients was lower than that of whole solids. Conclusion: The microfiltrating technology of inorganic ceramic membrane can make decoctions of Chinese Traditional Medicine clear.
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Objective: To evaluate effect of refining of the aqneous extract solution of compound Chinese traditional medicine by microfiltration technique of inorganic ceramic membrane. Methods: The aqneous extract solution of Ephedra, Apricot kernel, Gypsum, and Licorice Decoction and Redujing Granules were processed by microfiltration technique of inorganic ceramic membrane. The changes in the characters, whole solids and effective componds before and after process were studied. Results: The aqueous extract solution of compound Chinese traditional medicine all were turbid before microfiltering and became clear after microfiltrating. The whole solid of Ephedra, Apricot kernel, Gypsum, and Licorice Decoction were decreased by 16.12%, and the lost rates of ephedrine and amygdalin were 20.11% and 18.06% respectively. The whole solid of Redujing Granules were decreased by 27.58%, and the lost rates of chlorogenic acid and rhein were 18.28% and 22.86% respectively. Conclusion: The microfiltration technology of inorganic ceramic membrane has the better effects of clarification and removing impurity on the aqueous extract solution of compound Chinese traditional medicine.
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Aim To evaluate the effects of Brucine of restraining transplanted tumor growth,prolonging their survival time and its toxicity on haematopoietic and immune systems as well as hepatic and renal function in mice transplanted with Hepatocarcinoma Heps cells.Methods ICR male mice of Hepatocarcinoma Heps tumor model(Heps mice)was made through Heps cells inoculation.Anti-tumor activity of Brucine was evaluated in terms of tumor inhibitory ratio and life elongational ratio of mice transplanted with Heps tumor.The toxicity of Brucine was measured the mice weight,immune organ weight,blood cell index(leukocyte,erythrocyte,platelet,and hemachrome protein),and hepatic function index(ALT,AST)as well as renal function index(BUN) of Heps mice.Results Brucine had significant restraining effect on the growth of Heps tumor in mice.Its inhibitory rate was 30.34%(1.61 mg?kg~(-1)),46.21%(3.23 mg?kg~(-1))and 42.07%(6.46 mg?kg~(-1))respectively,and 3.23 mg?kg~(-1)(1/20 LD_(50)) was the best dosage of Brucine for treating Heps tumor in vivo,while Brucine had no distinct effect of prolonging the life of Heps mice.Moreover,it enhanced the weight of body and thymus index as well as spleen index,and had no distinct influence on blood cell index as well as ALT,AST and BUN in Heps mice.Conclusion Brucine can inhibit the growth of transplanted Heps tumor,enhance the weight of immune organ index significantly,and has no toxicity on haematopoietic and immune systems as well as hepatic and renal function of mice transplanted with Heps tumor.It may be developed into a promising anticancer drug through further study