Determination of Biflavones in Ginkgo biloba Leaves of Different Ages by UPLC-TQ-MS / 中国实验方剂学杂志

Objective: To establish an ultra-high performance liquid chromatography coupled with triple quadrupole mass for the determination of five biflavones. Method: Chromatographic separation was carried out on a ACQUITY UPLC BEH C18 column (2.1 mm×100 mm,1.7 μm) with gradient elution of acetonitrile and 0.10%formic acid at a flow rate of 0.3 mL·min-1,and the column temperature was set at 35℃. Result: Amentoflavone,bilobetin,ginkgetin,isoginkgetin,sciadopitysin showed a good linearity within the ranges of 0.02-13.20 mg·L-1(r=0.996 3),0.05-23.60 mg·L-1(r=0.995 5),0.09-18.60 mg·L-1(r=0.992 7),0.10-21.00 mg·L-1(r=0.998 8),0.06-16.00 mg·L-1(r=0.996 7),with average recoveries of 101.50%,98.78%,97.59%,97.24%,101.09%, and RSDs of 2.7%,2.7%,3.1%,2.8%,1.3%. The contents of amentoflavone,bilobetin,ginkgetin,isoginkgetin,sciadopitysin ranged between 121.30-434.74,268.39-847.14,251.80-1 297.10,195.87-691.10,477.48-3 003.90 μg·g-1. The total biflavones ranged between 1 474.45-5 635.40 μg·g-1. It shows a certain regularity that the low-vinegar leaves contain higher total flavonoids,and the total flavonoid content gradually decreases with the increase of tree age. Conclusion: The method was simple, and can be used for qualitative and quantitative analysis of biflavones.

Study on preparation of salvianolic acid phospholipid compound / 中国中药杂志

To prepare salvianolic acid phospholipid compound. With the compound of salvianolic acids and soybean phospholipid as the index, mono-factor experiment and orthogonal design experiment were conducted to screen its technical parameters. According to the results, the optimal preparation conditions of salvianolic acid phospholipid compound were that THF were taken as the reaction solvent, the concentration time was 3 h, the reactant concentration was 5 g x L(-1), the mass ratio of salvianolic acids and phospholipid was 1: 1.5, and the reaction temperature was 40 degrees C. The oil/water partition coefficient of the prepared salvianolic acid phospholipid compound significant increased in water and buffers with different pH values. The results of phase analysis such as DSC, XRD and FTIR indicated that salvianolic acids existed in phospholipid in an amorphous state.

Study thought of pharmaceutical preparations quality standards by dynamic quality control technology / 中国中药杂志

Pharmaceutical preparations, particularly as a "secret recipe" of traditional Chinese medicine in medical institutions, are the product of China's medical and health industry, and they are also an important means of competing of different medical institutions. Although pharmaceutical preparations have advantages and characteristics than institutes for drug and pharmaceutical companies, the quality standards of pharmaceutical preparations in medical institutions has not reached the desired level over the years. As we all know, the quality of pharmaceutical preparations is important to ensure the efficacy, especially under the environment of people pay more sttention on drug safety and effectiveness and contry increase emphasis on the stste of pharmaceutical preparations. In view of this, we will improve the grade, stability, and clinical efficacy of pharmaceutical preparations by the advanced equipment, testing instruments and the process dynamic quality control technology. Finally, we hope we can provide new ideas for the quality control of pharmaceutical preparations.

Preparation of genistein from genistin-HP-β-CD by enzymatic hydrolysis method / 中国药学杂志

OBJECTIVE: To prepare genistein from genistin-HP-β-CD inclusion complex by enzymic hydrolysis method. METHODS: The method of saturated water solution was applied to prepare genistin-HP-β-CD, then, genistin inclusion complex was transformed into genistein by snailase. Taking the bioconversion rate as the index, different factors were studied to obtain the feasible reaction conditions. An HPLC method was established to compare the bioconversion rates between genistin and genistin-HP-β-CD under the optimum conditions. Hydrolysis product was identified by H-NMR and C-NMR. RESULTS: The optimum reaction conditions were determined just as follows; the reaction medium was acetic acid-sodium acetate buffer solution of pH 5.0, the ratio of snailase; genistin-HP-β-CD was 4:5, and the reaction time was 12 h at 50°C. Under the above mentioned condition, the conversion rate of genistin-HP-β-CD was (90.17±2.40)%, 0.95 times higher than that of the genistin not entrapped with HP-β-CD. CONCLUSION: Preparing genistein by enzymatic hydrolysis method after entrapping genistin with HP-β-CD can significantly shorten the reaction time, and is suitable for industrialization.

Pharmacokinetics of main components in Salvia Miltiorrhizae Radix et Rhizoma diterpene quinones composition and its solid dispersion micro-pellets in rats in vivo / 中草药

Objective: To establish a UPLC-MS/MS method for determining the plasma concentration of dihydrotanshinone I, tanshinone I, cryptotanshinone, and tanshinone IIA in rats, and to study the pharmacokinetics of Salvia miltiorrhiza diterpene quinones composition (SMDQC) and its solid dispersion micro-pellets (SDMP). Methods: Sprague-Dawley rats were ig administered with SMDQC and its SDMP, respectively. Then the blood samples were obtained at different time points. Electrospray ionization (ESI) source was applied and operated in the positive ion mode. The plasma concentration of dihydrotanshinone I, tanshinone I, cryptotanshinone, and tanshinone IIA was then detected by UPLC-MS/MS, and the pharmcoknetic parameters were calculated by DAS 2.1.1 program. Results: The RSDs of intra- and inter-day precisions of all analytes were less than 14.6%, and the average recoveries of the four active constituents were more than 74.49%. The pharmacokinetic results showed that after ig administration of SDMP, Cmax and AUC0-∞ of the four active constituents increased significantly compared with those of SMDQC. Conclusion: The method has the high sensitivity and selectivity, and proves to be suitable for the pharmacokinetic study of SMDQC and its SDMP. The results show that the SDMP could enhance the solubility of SMDQC to improve its absorption. The relative bioavailability of the four representative constituents is 138%-204% of the crude drug.

Construction of analytical method for similarity of traditional Chinese medicine components on the basis of biopharmaceutic properties / 中国中药杂志

Traditional Chinese medicine components are a complex multi-component system. How to characterize and evaluate their diverse properties have long been key scientific problems in the modernization process of traditional Chinese medicines. According to the relevant regulations for biopharmaceutical properties, we made the criteria for evaluating similarity of Chinese medicine components, while establish an analytical method based on cosine and Grubbs to evaluate the dispersion degree of properties of representative components, so as to provide ideas and methods for classifying traditional Chinese medicine sub-components and evaluating the integrity of component properties.

Study on pharmaceutical screening of representative components of Salvia miltiorrhiza diterpene quinones / 中国中药杂志

<p><b>OBJECTIVE</b>To screen out the main components with no significant difference with Salvia miltiorrhiza diterpene quinones pharmacological action, in order to determine the compatible form of representative components that can describe the overall property of S. miltiorrhiza diterpene quinones.</p><p><b>METHOD</b>According to the results of the in vitro pharmacological experiment, the myocardial ischemia model of rats was induced through intraperitoneal injection of isoproterenol. The pharmacologic effects of S. miltiorrhiza diterpene quinones, combination with principal component A and combination with principal component B were compared in electrocardiogram (changes in J point), enzymology indicators (SOD, MDA, CK, LDH) and pathology (myocardial histological changes), so as to screen out the compatible form of representative components that can describe the overall property of S. miltiorrhiza diterpene quinones.</p><p><b>RESULT</b>The S. miltiorrhiza diterpenoid quinone high-dose group and the B high-dose group were similar in all pharmacological effects, with equal efficacy but no significant difference.</p><p><b>CONCLUSION</b>The S. miltiorrhiza diterpenoid quinone high-dose group and the B high-dose group showed a certain therapeutic effect on ISO-induced myocardial ischemia. Therefore, the four components in the B high-dose group can be used as representative components of S. miltiorrhiza diterpene quinones.</p>

Investigation on equilibrium solubility and apparent oil/water partition coefficient of diterpenoid tanshinone component by similarity analysis methods / 中国中药杂志

<p><b>OBJECTIVE</b>To study the equilibrium solubility and apparent oil/water partition coefficient of diterpenoid tanshinone component by similarity analysis methods, so as to lay the foundation for Salvia diterpenoid quinone component of the overall solubility characterization.</p><p><b>METHOD</b>Taking Salvia diterpenoid quinone component as model drug, determined the equilibrium solubility and partition coefficients of the components in different buffer, evaluated the degree of similarity of each component based on the cosine and Grubbs.</p><p><b>RESULT</b>The representative composition of Salvia diterpenoid quinone component, namely dihydrotanshinone I, tanshinone I, cryptotanshinone and tanshinone II(A) had similar properties of equilibrium solubility and partition coefficients in different pH buffer. This similarity was not only manifested in the trends, but also reflected the value.</p><p><b>CONCLUSION</b>This similarity assessment reflected the degree of deviation and dispersion of components, which was applicable to the study of the components; the similarity assessment could increase the science and rationality of component evaluation, and at the same time could optimize the structure of the component.</p>

Establishment of modern multi-component sustained-release preparations of oral traditional Chinese medicines / 中国中药杂志

Traditional Chinese medicines have a long history, with a large quantity of efficient traditional Chinese medicines and prescriptions. However, the vast majority of pharmaceutical dose forms remain common preparations, with very few efficient, long-lasting and low-dose preparations. The sustain-release preparation allows sustained drug release in a longer period of time, maintains blood drug concentration, reduces the toxic effect and medication frequency, and improves medication compliance. Unlike monomer drugs, the material base of traditional Chinese medicine and compounds is multi-component, instead of single or several active monomers. Therefore, under the guidance of the Chinese medicine theories, modern multi-component sustained-release preparations were developed for oral traditional Chinese medicines, with the aim of finally improving the clinical efficacy of traditional Chinese medicines.

Construction of evaluation systems for traditional Chinese medicine multiple drug delivery system on basis of component level / 中国中药杂志

Traditional Chinese medicine (TCM) is a multi-component complex system and its research must consider its components characteristics of multi-component, multi-target and multi-effect. According to the whole concept of Chinese medicine, also combining with the status quo of Chinese drugs pharmaceutics and setting the material basis component as the premise, this study will develope TCM multiple drug delivery evaluation system, respectively from three aspects, namely in vitro release, in vivo bioavailability and PK-PD. At the same time, we will try to offer the new thoughts of the programly release, so as to provide new strategies and methods for the development of modern Chinese drug delivery systems.

Drug releasing characteristics evaluation to multi-drug delivery system of tongmai pellets / 中国中药杂志

<p><b>OBJECTIVE</b>To establish the drug release method of multi-drug delivery system of tongmai pellets.</p><p><b>METHOD</b>The drug releasing characteristics were researched by HPLC and UV spectrophotometric method. The drug releasing characteristics of the multi-drug delivery system of tongmai pellets between single unit and multiple drug delivery system were evaluated by HPLC.</p><p><b>RESULT</b>The four pellets release unit isoflavones pellets, tanshinone pellets, Sal pellets, chuanxiong acid by ultraviolet spectrophotometry and HPLC method of dissolution obtained similar curves, and the similarity factor f2 were 63.31, 81.59, 70.93, 68.08. The release unit after the formation of multiple drug delivery system had no influence on single unit.</p><p><b>CONCLUSION</b>Initial construction of multiple drug delivery system tongmai pellets improved the dissolution of insoluble components, the overall performance of the combination of rapid release and sustained release characteristics, in line with the design requirements.</p>

Design technology of traditional Chinese medicine component and formulation / 中国中药杂志

The development of traditional Chinese medicine lies in its significant clinical efficacy which is closely related to the bioavailability of drugs. The nature of the material foundation of compounds of traditional Chinese medicine is reflected in multi-component. As for the nature of components themselves, the level of their bioavailability depends on the biopharmaceutical properties, namely solubility and permeability, to a great extent. Therefore, under the guidance of the theory of traditional Chinese medicine and in the combination with modern preparation techniques, this essay reveals key techniques capable of improving the biopharmaceutical properties of components, in the hope of enhancing the clinical efficacy of components of traditional Chinese medicine.

Traditional Chinese medicine components and construction of components biopharmaceutical classification system / 中国中药杂志

Traditional Chinese medicine compound of material base is multi-components. It should be divided into groups to study traditional Chinese medicine biopharmaceutical properties. To study traditional Chinese medicine multi-component biopharmaceutical, this paper puts forward the scientific representative Chinese medicine integrated nature of the components of the composition, choose ideas. Secondly, this paper introduces the concept of "discrete degree" to examine difference about representative nature of each component. It should he more comprehensive evaluation of traditional Chinese medicine scientific nature of the components. With the comprehensive property value final components and discrete degrees, setting up a part of traditional Chinese medicine biopharmaceutical classification system, traditional Chinese medicine for the multi-composition biopharmaceutical nature study puts forward a new way and method.

Response surface method optimize of nano-silica solid dispersion technology assistant enzymatic hydrolysis preparation genistein / 药学学报

This article reports that nano-silica solid dispersion technology was used to raise genistein efficiency through increasing the enzymatic hydrolysis rate. Firstly, genistin-nano-silica solid dispersion was prepared by solvent method. And differential scanning calorimetry (DSC) and transmission electron microscopy (TEM) were used to verify the formation of solid dispersion, then enzymatic hydrolysis of solid dispersion was done by snailase to get genistein. With the conversion of genistein as criteria, single factor experiments were used to study the different factors affecting enzymatic hydrolysis of genistin and its solid dispersion. And then, response surface method was used to optimize of nano-silica solid dispersion technology assistant enzymatic hydrolysis. The optimum condition to get genistein through enzymatic hydrolysis of genistin-nano-silica solid dispersion was pH 7.1, temperature 52.2 degrees C, enzyme concentration 5.0 mg x mL(-1) and reaction time 7 h. Under this condition, the conversion of genistein was (93.47 +/- 2.40)%. Comparing with that without forming the genistin-nano-silica solid dispersion, the conversion increased 2.62 fold. At the same time, the product of hydrolysis was purified to get pure genistein. The method of enzymatic hydrolysis of genistin-nano-silica solid dispersion by snailase to obtain genistein is simple, efficiency and suitable for the modern scale production.