OBJECTIVETo analyze the content of tanshinone IIA in Radix Salviae Miltiorrhizae from different habitats are regularly altered and find out the deviation between the studies.

METHODThe data of the content of tanshinone IIA in samples of Radix Salviae Miltiorrhizae from different areas and related information since 1997 was collected and statistically analyzed.

RESULT AND CONCLUSIONThe content of tanshinone IIA in wild Salvia was generally higher than that in the cultivated Salvia, and the content in nearly half cultivated Salvia was less than 0.2%. There existed a big difference between the used statistical model, and the data related the content in samples from Sichuan was the most divisive. The coefficient of variation of wild Salvia was below the cultivated Salvia, and the cultivated Salvia from different areas showed different coefficients of variation. The content of tanshinone IIA was lower when samples were extracted using the heating reflux method.

Diterpenes, Abietane ; Phenanthrenes ; analysis ; Salvia miltiorrhiza ; chemistry

OBJECTIVETo compare the influence on the dissolution of tanshinone IIA (TS IIA) solid dispersions in complex carriers and single, which used in preparation of TS IIA solid dispersions, and further enhance the dissolution of TS IIA.

METHODThe TS IIA solid dispersions were prepared by solvent technique with polyvinylpyrrolidone K30 (PVPK30), poloxamer188 (F68) and combination of PVPK30 and F68 as carriers, respectively. The physical characteristics of TS IIA solid dispersions was studied using differential scanning calorimetry (DSC). Dissolution rates were studied using small cup method (CHP XC III). The solubility of TS IIA with the solid dispersions and pure drug form were determined by HPLC method.

RESULTThe DSC analysis suggested that TS IIA was dispersed as an amorphous form in the combination of PVPK30 and F68. Dissolution profile of the prepared solid dispersions could be described by Weibull equation (R>0.99). For tested three carries, Td value (calculated time to 63.2% of total drug release according to Weibull equation) were (90.40 +/- 2.82) min, (204.5 +/- 8.20) min and (25.83 +/- 0.13) min, respectively. The PVPK30/F68-TS IIA solid dispersion resulted in a significant increase of TS IIA solubility compared with prepared PVPK30-TS IIA and F68-TS IIA solid dispersions (P<0.01).

CONCLUSIONAs compared to single use of PVPK30 or F68, the combination of PVPK30 and F68 improve the dissolution rate and solubility of TS IIA significantly in the prepared solid dispersions (P<0.01). The application of complex carriers in solid dispersion technology should be paid more attention to improvement of poorly soluble drugs dissolution in the future.

Diterpenes, Abietane ; Phenanthrenes ; chemistry ; Solubility ; Temperature

The technique of liquisolid compress is a new technique developed in 1990s, which was considered to be the most promising technique to improve the dissolution of water-insoluble drugs. In this article, tanshinone II(A) and the extracts of the ester-solubility fractions were chosen as the model drugs to evaluate the effects of the liquisolid technique for enhancement of dissolution properties of tanshinone II(A). Several liquisolid tablets (LS) formulations containing different dosage of drugs and various liquid vehicle were pre-pared and for all the formulations, microcrystalline cellulose and silica were chosen as the carrier and coating materials to evaluate their flow properties, such as angle of repose, Carr's compressibility index and Hausner's ratio. The interaction between drug and excipients in prepared LS compacts were studied by differential scanning calorimetry(DSC) and X-ray powder diffraction (XRPD). The dissolution curves of tanshinone II(A) from liquisolid compacts were investigated to determine the technique's effect in improving the dissolution of tanshinone II(A) and its impacting factors. According to the results, the dissolution increased with the rise in the dissolution of the liquid-phase solvent. The R-value and drug dosage can significantly affect the drug release, but with less impact on active fractions. This indicated that liquisolid technique is a promising alternative for improvement of dissolution property of water-soluble drugs, and can make a synergistic effect with other ester-soluble constituents and bettern improve the release of tanshinone II(A). Therefore, the technique of liquisolid compress will have a better development prospect in traditional Chinese medicines.
Calorimetry, Differential Scanning ; Diterpenes, Abietane ; chemistry ; Solubility ; X-Ray Diffraction

OBJECTIVETo study chemical constituents from pine cone of Pinus annandii.

METHODThe constituents were isolated by chromatographic method and the structures were identified on the basis of spectral analysis.

RESULTSeven compounds were identified as sandaracopimaric acid (I), isodextropimaric acid (II), 12-hydroxyabietic acid (III), dehydroabietic acid (IV), 15-hydroxydehydroabietic acid (V), beta-sitosterol (VI) and daucosterol (VII).

CONCLUSIONCompounds I-IV were isolated from this plant for the first time.

Diterpenes ; chemistry ; isolation & purification ; Diterpenes, Abietane ; chemistry ; isolation & purification ; Fruit ; chemistry ; Pinus ; chemistry ; Plants, Medicinal ; chemistry ; Sitosterols ; chemistry ; isolation & purification

BACKGROUND/AIMS: Ecabet sodium is known for its bactericidal effect against H. pylori. It was reported that a supplement of ecabet sodium to conventional triple therapy showed good results in Asia. The Aim of this study was to ascertain the efficacy of additional ecabet sodium on conventional triple therapy for eradication of H. pylori. METHODS: We reviewed the cases of 111 patients (Group A) with H. pylori infection who received ecabet sodium with triple therapy (20 mg of rabeprazole, 1 g of amoxicillin, 500 mg of clarithromycin and 1 g of ecabet sodium, twice daily for 7 days). Another 186 patients (Group B) received PPI-based triple therapy (same as the above, except without the ecabet sodium). Eradication was evaluated 4 weeks later after completion of treatment by 13C-UBT. RESULTS: Eradication rates were 74.8% (83/111) in group A and 70.4% (131/186) in group B by intention-to-treat analysis (p=0.420), and 75.2% (82/109) in group A and 70.7% (128/181) in group B by per protocol analysis (p=0.405). CONCLUSIONS: The addition of ecabet sodium to conventional triple therapy did not increase the eradication rate of H. pylori in this study. These findings imply that ecabet sodium as an additional agent cannot overcome antibiotic resistance, which is the most important cause of failure of triple therapy.
2-Pyridinylmethylsulfinylbenzimidazoles ; Amoxicillin ; Asia ; Clarithromycin ; Diterpenes, Abietane ; Drug Resistance, Microbial ; Helicobacter ; Helicobacter pylori ; Humans ; Korea ; Sodium

Porous silica was used as a carrier to prepare tanshinone solid dispersions (SDs). sThe effect of the spray drying method or the solvent method on the drug dissolution of SD was studied. The structure characteristics of SDs was analyzed by SEM, DSC,XPRD and FTIR. And in vitro dissolution was also investigated. The results showed that drugs were highly dispersed into SDs prepared by spray drying method and the solvent method in amorphous form. In addition, the results of the dissolution tested in vitro exhibited that the tanshinone I and tanshinone II A, accumulated dissolutions of SDs prepared using solvent achieved 80. 9% ,84. 6% and 86. 2% ,88. 7% within 45,60 min, respectively. And SDs prepared using spray-drying method were 92.7% ,95. 3% and 95. 8%, 97. 1% within 45,60 min, respectively. The tanshinone SDs were prepared successfully by spray drying method and solvent method. The SDs prepared by spray drying method was more conducive to improving the dissolution.
Calorimetry, Differential Scanning ; Diterpenes, Abietane ; chemistry ; isolation & purification ; Porosity ; Silicon Dioxide ; chemistry ; Spectroscopy, Fourier Transform Infrared

OBJECTIVETo 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.

METHODTaking 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.

RESULTThe 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.

CONCLUSIONThis 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.

Diterpenes, Abietane ; chemistry ; Hydrogen-Ion Concentration ; Oils ; chemistry ; Solubility ; Water ; chemistry

OBJECTIVETo develop an HPLC method for content determination of dehydroabietic acid and abietic acid in aqueous alkali extract of Liquidambaris Resina.

METHODThe determination was carried out on a DIONEX C18 column (4.6 mm x 250 mm, 5 microm) eluted with acetonitrile and water containing 0.1% acetic acid. The flow rate was 1 mL x min(-1), and the detected wavelength was set at 210, 240 nm.

RESULTThe peak areas and the sample quantity of the two components had good linear relationship in the range of 0.4-3.4 microg for dehydroabietic acid, and 0.6-4.8 microg for abietic acid. The average recoveries were 99.53%, 101.9%, respectively.

CONCLUSIONThe method was proved to be simple, accurate and used for the quality evaluation of Liquidambaris Resina.

Chromatography, High Pressure Liquid ; methods ; Diterpenes, Abietane ; analysis ; Drugs, Chinese Herbal ; analysis ; Liquidambar ; chemistry

OBJECTIVETo establish a method to determine the dissolution of Tanshinone IIA in xianling gubao capsules, and compare the dissolution of Xianling Gubao capsules prepared by different processes.

METHODThe small cup method was used at a rotary speed of 100 r x min(-1), the dissolubility was inspected in the following 6 mediums: (1) water; (2) 0.1 mol x L(-1) hydrochloric acid solution; (3) pH 6.8 phosphate buffer; (4) pH 6.8 phosphate buffer solution + 0.5% cholic acid; (5) pH 6.8 phosphate buffer solution + 1.0% cholic acid; (6) pH 7.6 phosphate buffer solution + 4. 0% cholic acid. A HPLC method was used to determine the dissolution samples of tanshione IIA in different dissolution mediums. The accumulative dissolution percentages were calculated, and the resemblance of release curves were compared by similarity factors (f2).

RESULTThe accumulative dissolution percentage was the highest while pH 7.6 phosphate buffer solution + 4.0% cholic acid was used as medium. The similarity factor values (f2) of tanshinone IIA dissolution curves of different preparation processes of Xianling Gubao capsules were all less than 50.

CONCLUSIONThere is significant difference in tanshinone IIA dissolution between Xianling Gubao capsules of different preparation processes. The accumulative dissolution percentages of the tanshinone IIA in new Xianling Gubao capsules is higher than that in the capsules prepared by other preparation processes.

Capsules ; Chromatography, High Pressure Liquid ; methods ; Diterpenes, Abietane ; Drugs, Chinese Herbal ; chemistry ; Phenanthrenes ; chemistry ; Solubility

In order to improve the dissolution in vitro of components by processing tanshinone with the pray drying method, the physical properties of tanshinone power was analyzed by BET, differential scanning calorimetry, scanning electron microscopy and X-ray powder diffraction, and its dissolution in vitro was also investigated. The results of characterization showed decreased power size and increased specific surface area of tanshinone powder, and its existence in an amorphous state. Within 4 h, the accumulated dissolutions of tanshinone I and tanshinone II(A) in components of tanshinone reached 78.3%, 81.9%, respectively. Therefore, the spray-drying method was conducive to enhance the dissolution of components of tanshinone.
Chemistry, Pharmaceutical ; methods ; Diterpenes, Abietane ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Particle Size ; Solubility