Objective To prepare the pH-dependent Yuchangning Tablet for colon-specific delivery(PYTCSD) used in treating the ulcerative colitis and evaluating the releasing property in vivo and in vitro.Methods The coating prescription was screened by the in vitro delivery of matrine and oxymatrine.The in vitro releasing property of the preparation was examined by the method of in vitro delivery. The in vivo releasing property of the preparation was evaluated by the shadowgraph technique of barium sulfate.Results The preparation method of the PYTCSD was obtained.The core of the tablet was coated by the alcohol solution mixed with 3.70%(g/mL) Eudragit Ⅲ,0.37%(g/mL) DEP,and 0.93%(g/mL) talcum power.The weight of the core was increased 8%.From the in vitro delivery,matrine and oxymatrine were not detected in the simulated gastric fluid after 2 h.The quantities of matrine and oxymatrine were less 10% in the simulated intestinal fluid after 4 h.The quantities of matrine and oxymatrine were 86.5% and 86.8% in the simulated colon fluid after 1 h.On the basis of the in vivo delivery by treating eight volunteers,the PYTCSD could completely get to the ileocecum or ascending colon and disintegrate in that part.Conclusion The PYTCSD can be prepared and the preparation is significantly delivered in the specific colon.

AIM To study the effects of degreasing-frosting on reducing toxicity and enhancing efficacy of Periplaneta americana L..METHODS The 95％ ethanol extracts from P.americana raw powder and processed products were extracted by petroleum ether,ethyl acetate,n-butanol and water.TLC was applied to comparing the component changes in various fractions.GC-MS was used for analyzing the kinds and contents of liposoluble constituents before and after processing.Shaking flask method combined with UV spectrophotometry method was adopted in the determination of Papp values in octanol-water and different pH values (2.23,3.28,4.22,5.23,6.12,7.24,8.23,9.10,10.15 and pure water) of buffer solutions.RESULTS After the petroleum ether fraction was processed,the colors of TLC spots became much shallower,which changed more significantly with the prolonging of processing time and increase of pressure.The TLC spots in the n-butanol and water fractions were clear without obvious changes.And no TLC spots were found in the ethyl acetate fraction.The kinds of liposoluble constituents were the same before and after processing,whose absolute contents were decreased after processing.Compared with raw powder,the Papp values of minor polypeptides in various processed products at different pH values exhibited significant differences (P ＜0.05,P ＜0.01),which also showed certain differences at the same pH values.CONCLUSION Degreasing-frosting can affect the contents of liposoluble constituents in P.americana and Papp values of minor polypeptides,which may be the mechanism of reducing toxicity and enhancing efficacy.

AIM: To study the processing of Indigo Naturals. METHODS: Study on the microstructure of Indigo Naturals with scanning electron microscope (SEM) and X ray diffractometer (XRD) were carried out. RESULTS: Through the SEM, it is clear that Indigo attached to the surface of some white substance, and the XRD proves that the white substance in Indigo Naturals is calcium carbonate (CaCO 3). CONCLUSION: The study about the processing of Indigo Naturals indicates that Indigo Naturals consists of Indigo and other effective compositions attached the surface of calcium carbonate (CaCO 3).

AIM: To apply the natural fermentation technology to produce indigo. METHODS: Fresh leaves of conehead were put in water and let its ferment naturally, then add lime to fermentation liquor to naturalize,indigo content was determined by HPLC. RESULTS: Fermentative temperature at 28 ℃ and oxygen supply were most important condition. CONCLUSION: Fungi can be successfully applied to indigo production.

AIM: To optimize the preparation of cholic acid-hydroxypropy-?-cyclodextrin inclusion complex,and its phase solubility analysis. METHODS: Orthogonal test,including molar ratio,inclusion temperature,mixing time and liquid dropping rate of cholic acid-HP-?-CD,was adopted to screen the optimal preparation,based on the inclusion efficiency by HPLC method.The solubilization effect was evaluated by using phase solubility.(RESULTS): The optimal preparation consisted of the molar ratio of cholic acid-HP-?-CD was 1∶3,60 ℃ inclusion temperature,60 min mixing time,1.6 mL/min liquid dropping rate;A_L type of phase solubility curve,K=564.30 L/mol,and 11.81 times solubilization. CONCLUSION: The optimal preparation is stable,reasonable and practicable with the encapsulation efficiency of 97.1%.Inclusing cholic acid with HP-?-CD is feasible,and the solubilization effect is significant.

Objective To improve the permeation of nasal mucosa by preparing the cholic acid-hydroxypropyl-?-cyclodextrin(HP-?-CD) and characterize the inclusion complex.Methods The inclusion complex was characterized by using phase solubility,scanning electron microscope(SEM),Fourier transform-infrared(FT-IR),differential scanning calorimetry(DSC),and superconducting NMR;In an effort to investigate the effect of HP?-CD on cholic acid,the studies of in vitro permeation of nasal mucosa was performed.Results Phase solubility curve was AL type,K=564.30 L/mol,and the characterization de-monstrates the formation of inclusion complex;The permeability coefficients and steady state fluxes through ovine and porcine nasal mucosa were enhanced by the formation of inclusion complex with HP-?-CD about 1.46 and 1.44 times of the uncomplexed cholic acid,respectively.Conclusion The inclusion complex is formed and it could increase the permeability of nasal mucosa by preparing the cholic acid-HP-?-CD.

OBJECTIVETo investigate the regulation of geniposide nasal absorption.

METHODWe used rat in situ nasal recirculation method as experimental model. The effects of perfusion volume, flow rate, perfusion concentration on nasal absorption of geniposide were studied.

RESULTGeniposide was stable in rats nasal lavage solution. At the perfusion volume 5 mL and flow rate 2.5 mL x min(-1), the absorption rate of geniposide remains constant in a dose-independent manner.

CONCLUSIONThe mechanism of geniposide nasal absorption is passive diffusion following first order kinetics and the absorption rate constant is 4.20 x 10(-3).

Absorption ; Administration, Intranasal ; Animals ; Diffusion ; Drugs, Chinese Herbal ; administration & dosage ; metabolism ; Iridoids ; administration & dosage ; metabolism ; Kinetics ; Linear Models ; Male ; Nose ; metabolism ; Perfusion ; Rats ; Sensitivity and Specificity ; Solutions

OBJECTIVE： To prepare standard decoction of fried Perilla frutescens seed and study the quality standard. METHODS： According to the preparation requirements of standard decoction， 17 batches of standard decoction of fried P. frutescens seed were prepared， and the yield of paste was calculated. HPLC method was used for quantitative analysis of rosmarinic acid in standard decoction of fried P. frutescens seed. The determination was performed on Agilent 5 TC-C18（2） column with mobile phase consisted of methanol-0.1％ formic acid solution （40 ∶ 60， V/V） at the flow rate of 1.0 mL/min. The detection wavelength was set at 330 nm， and column temperature was 30 ℃. The sample size was 5 μL. The transfer rate was calculated. HPLC fingerprint was established for 17 batches of standard decoction of fried P. frutescens seed， and analyzed by using TCM Chromatogram Fingerprint Similarity Evaluation System （2012 edition）. The chromatogram peaks were identified by comparing retention time of common peak. RESULTS： The yield of paste were 5.55％-9.75％ in 17 batches of standard decoction of fried P. frutescens seed. The contents of rosmarinic acid were 0.44％-1.58％， and average content was 1.08％. The transfer rates of rosmarinic acid were 18.31％-34.32％， and average transfer rate was 25.42％. In HPLC fingerprints for 17 batches of standard decoction of P. frutescens seed， a total of 11 common peaks were identified， and the similarity was higher than 0.95. Five common peaks were identified， namely caffeic acid （peak 3），luteolin （peak 5）， rosmarinic acid （peak 8） ， luteolin （peak 9）， apigenin （peak 10）. CONCLUSIONS： The quality control method of standard decoction of fried P. frutescens seed is established， which can provide reference for the formulation of the quality standard of fried P. frutescens seed granules and related preparations.

Traditional Chinese herbs (TCH) are currently gaining attention in disease prevention and health care plans. However, their general bitter taste hinders their use. Despite the development of a variety of taste evaluation methods, it is still a major challenge to establish a quantitative detection technique that is objective, authentic and sensitive. Based on the two-bottle preference test (TBP), we proposed a novel quantitative strategy using a standardized animal test and a unified quantitative benchmark. To reduce the difference of results, the methodology of TBP was optimized. The relationship between the concentration of quinine and animal preference index (PI) was obtained. Then the PI of TCH was measured through TBP, and bitterness results were converted into a unified numerical system using the relationship of concentration and PI. To verify the authenticity and sensitivity of quantified results, human sensory testing and electronic tongue testing were applied. The quantified results showed a good discrimination ability. For example, the bitterness of Coptidis Rhizoma was equal to 0.0579 mg/mL quinine, and Nelumbinis Folium was equal to 0.0001 mg/mL. The validation results proved that the new assessment method for TCH was objective and reliable. In conclusion, this study provides an option for the quantification of bitterness and the evaluation of taste masking effects.

Heart failure (HF) is a global public health problem with high morbidity and mortality. A large number of studies have shown that HF is caused by severe energy metabolism disorders, which result in an insufficient heart energy supply. This deficiency causes cardiac pump dysfunction and systemic energy metabolism failure, which determine the development of HF and recovery of heart. Current HF therapy acts by reducing heart rate and cardiac preload and afterload, treating the HF symptomatically or delaying development of the disease. Drugs aimed at cardiac energy metabolism have not yet been developed. In this review, we outline the main characteristics of cardiac energy metabolism in healthy hearts, changes in metabolism during HF, and related pathways and targets of energy metabolism. Finally, we discuss drugs that improve cardiac function