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

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

The fibrous roots are the residues of production of cut crude drug of Danshen (Salvia miltiorrhiza). Enzymatic pretreatment and ultrasonic extraction are beneficial to extract effective constituents from fibrous roots more effectively. The present research was to optimize the enzymatic parameters by the central composite design and response surface method. Under the best conditions, the yields of total tanshinones and total salvianolic acids in the extracts of enzymatic pretreatment increased by 113.92% and 30.64%, comparing with the non-enzymatic extraction, respectively. TLC analysis also showed that the types of effective constituents in the two samples were not affected by enzymatic hydrolysis. Meanwhile, the complex correlation coefficients of the mathematical models were high, which provided a good prediction.
Diterpenes, Abietane ; Drugs, Chinese Herbal ; chemistry ; Phenanthrenes ; chemistry ; Plant Roots ; chemistry ; Salvia miltiorrhiza ; chemistry

OBJECTIVETo isolate and elucidate the constituents from rhizome of Arundina graminifolia.

METHODTheconstituents were extracted with 95% alcohol and isolated by chromatography on silica gel, Sephedax LH-20. The structures were determined by UV, IR, NMR and MS spectral analysis.

RESULTFive phenanthrene constituents were identified as 7-hydroxy-2, 4-dimethoxy-9, 10-dihydrophenanthrene( I ), 4, 7-dihydroxy-2-methoxy-9, 10-dihydrophenanthrene ( II ), 2, 7-dihydroxy-4-methoxy-9, 10-dihydrophenanthrene ( III ), 7-hydroxy-2-methoxyphenanthrene-1,4-dione ( IV ), 7-hydroxy-2-methoxy-9, 10-dihydrophenanthrene-1,4-dione (V), respectively.

CONCLUSIONAll compounds were isolated from rhizome of A. graminifolia for the first time.

Orchidaceae ; chemistry ; Phenanthrenes ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry

Nowadays,the advantages of traditional Chinese medicine(TCM) for treatment of tumors are increasingly prominent.Triptolide shows wide-spectrum and highly effective anti-tumor activity. Moreover,nano-carrier-based triptolide drug delivery system is more powerful in improving water solubility and pharmacokinetic behavior of the drug,but it is easy to cause toxic and side effects that should not be neglected on human body. Because of tumor vascular heterogeneity and PEGylation dilemma,nanoparticulate drug delivery systems need to overcome multiple physiological and pathological barriers from drug administration to functioning. It is difficult for traditional triptolide nanoparticulate drug delivery systems to achieve active accumulation of nano-drug in tumor tissues and specific drug release in tumor target site solely relying on enhanced permeability and retention effect of solid tumor,limiting their application and clinical transformation in treatment of tumors. Based on the traditional nano-preparation system,the new functionalized nano-drug delivery system further enhances the nano-drug enrichment,penetration and controlled release at the tumor sites,which is of great significance in improving bioavailability,anti-tumor efficacy and reducing the side effects of drugs. In this paper,we summarized and analyzed the researches on new triptolide functionalized nano-drug delivery system from four perspectives,including tumor active targeting,tumor microenvironment response,polymer-drug conjugates,and multidrug co-delivery for tumor treatment,expecting to provide ideas for in-depth research and clinical application of triptolide and some other active anti-tumor TCM ingredients.
Diterpenes/chemistry* ; Drug Delivery Systems ; Epoxy Compounds/chemistry* ; Humans ; Nanoparticles ; Phenanthrenes/chemistry*

AIMTo study the chemical constituents of Cypripedium tibeticum.

METHODSCompounds were isolated by repeated silica gel chromatography and purified on Sephadex LH-20 and structures were determined by spectral analysis.

RESULTSCypritibetquinones A and B were isolated from the ethyl acetate residue and their structures were determined as 7-hydroxy-2-methoxy-1 4-phenanthraquinone (1) and 7-hydroxy-2, 10-dimethoxy-l1 4-phenanthraquinone (2), respectively, by extensive spectral analyses.

CONCLUSIONCypritibetquinones A and B are two new phenanthraquinones.

Anthraquinones ; chemistry ; isolation & purification ; Molecular Conformation ; Molecular Structure ; Orchidaceae ; chemistry ; Phenanthrenes ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Rhizome ; 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

OBJECTIVETo investigate the feasibility of extracting the fat-soluble and the water-solubility substances from Salviae Miltiorrhizae with O/W Microemulsion.

METHODWith the yield of Tanshinone IIA and Salvianolic acid B as index, compere with efficiency of extracting Salviae Miltiorrhizae by suing the different media (water, alcohol and microemulsion), using different extraction methods (heat, microwave, ultrasonic), using different formulations of O/W microemulsion.

RESULTThe extracting yield of Tanshinone IIA and Salvianolic acid B are more than 70% by using microemulsion at mean time. It is good of the abilities of extraction of liposolubility compounds such as the Tanshinone IIA by the microemulsion. The formulations of microemulsion have remarkable effect for extracting Salviae Miltiorrhizae.

CONCLUSIONIt is feasibiale that extracted Salviae Miltiorrhizae by using O/W microemulsion as a solvents.

Benzofurans ; chemistry ; isolation & purification ; Diterpenes, Abietane ; Drugs, Chinese Herbal ; chemistry ; Emulsions ; chemistry ; Oils ; chemistry ; Phenanthrenes ; chemistry ; isolation & purification ; Reproducibility of Results ; Salvia miltiorrhiza ; chemistry ; Water ; chemistry

OBJECTIVETo develop an identitication and quantitation method for Radix Salviae Miltiorrhizae.

METHODThe powder X-ray Diffraction Fourier Fingerprint Pattern technique was used for this purpose. The high performance liquid chromatography method was used to evaluate the quantity of Tanshinone II A in 9 samples and 1 drug reference substance. The relationship of diffraction peak intensity and content of Tanshinone II A was investigated.

RESULT AND CONCLUSIONThe powder X-ray diffraction Fourier Fingerprint Pattern analysis technique can be used to identify Radix Salviae Miltiorrhizae and to evaluate the quantity of Tanshinone II A in the drug at the same time.

Chromatography, High Pressure Liquid ; Diterpenes, Abietane ; Drugs, Chinese Herbal ; chemistry ; Phenanthrenes ; chemistry ; Salvia miltiorrhiza ; chemistry ; X-Ray Diffraction ; methods

OBJECTIVETo study the chemical constituents of effective part of Gastrodia elata.

METHODThe constituens were isolated by column chromatographies with silica gel and ODS, and identified by NMR, MS spectra.

RESULTSix compounds were isolated and identified.

CONCLUSIONThree compounds were isolated from this plant for the first time.

Gastrodia ; chemistry ; Molecular Structure ; Phenanthrenes ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Quinones ; chemistry ; isolation & purification ; Sitosterols ; chemistry ; isolation & purification ; Sulfides ; chemistry ; isolation & purification