Anticancer Activities of C18-, C19-, C20-, and Bis-Diterpenoid Alkaloids Derived from Genus Aconitum.

Cancer is one of the most common lethal diseases, and natural products have been extensively studied as anticancer agents considering their availability, low toxicity, and economic affordability. Plants belonging to the genus Aconitum have been widely used medically in many Asian countries since ancient times. These plants have been proven effective for treating several types of cancer, such as lung, stomach, and liver cancers. The main effective components of Aconitum plants are diterpenoid alkaloids-which are divided into C18-, C19-, C20-, and bis-diterpenoid alkaloids-are reportedly some of the most promising, naturally abundant compounds for treating cancer. This review focuses on the progress of diterpenoid alkaloids with different structures derived from Aconitum plants and some of their derivatives with potential anticancer activities. We hope that this work can serve as a reference for further developing Aconitum diterpenoid alkaloids as anticancer agents.

[Changes in plasma pharmacokinetics and urinary excretion characteristics before and after combined administration of Ephedrae Herba-Gypsum Fibrosum].

In this study, UPLC-MS/MS was adopted to determine the contents of five ephedrine alkaloids (Norephedrine, Norpseudoephedrine, Ephedrine, Pseudoephedrine, Methylephedrine) in plasma and urine in rats after the combined administration of Ephedrae Herba-Gypsum Fibrosum and calculate relevant pharmacokinetic parameters, in order to discuss the effect of the combined administration of Ephedrae Herba-Gypsum Fibrosum on plasma pharmacokinetics and urinary excretion characteristics. According to the results, after being combined with Gypsum, the five ephedrine alkaloids showed similar pharmacokinetic changes, such as shortened t(max), accelerated absorption rate, but reduced AUC(0-t) and V(z)/F, which may be related to the increase in urine excretion. Besides, Gypsum was added to enhance C(max) of Pseudoephedrine and prolong MRT(0-t) of Methylephedrine, so as to enhance the anti-asthmatic effect of Ephedrae Herba and resist the toxic effect of Norephedrine and Ephedrine. This study proved the scientific compatibility of Ephedrae Herba-Gypsum Fibrosum and provided a reference for studies on the prescription compatibility regularity and relevant practices.

[Pharmacokinetic and Tissue Distribution Study of Ephedrae Herba and Herbal Pair of Ephedrae Herba-Atractylodis Macrocephalae Rhizoma in Rats].

OBJECTIVE: Five kinds of Ephedra alkaloids (NME, NMP, E, PE and ME) in Ephedrae Herba extracts and Ephedrae Herba-Atractylodis Macrocephalae Rhizoma herbal pair extracts of plasma pharmacokinetic and tissue distribution study in rats were carried out, to discuss the changes of Ephedrae Herba compatibility with Atractylodis Macrocephalae Rhizoma before and after METHODS: HPLC- MS method was used and the condition was as flollows: ZORBAX SB-C18 column (100 mm x 2.1 mm, 3.5 µm), column temperature of 35 °C, mobile phase of ACE-0.1% formic solution in gradient elution mode, flow rate at 0.4 mL/min; MRM positive ion detection mode. RESULTS: The distribution trends of Ephedra alkaloids were changing in plasma and tissues of rats after Ephedrae Herba compati- bility with Atractylodis Macrocephalae Rhizoma. CONCLUSION: Ephedrae Herba compatibility with Atractylodis Macrocephalae Rhizoma may increase drug efficacy and reduce the toxicity of Ephedra alkaloids at the same time.

[Determination of ephedrine hydrochloride, pseudoephedrine hydrochloride and methylephedrine hydrochloride in maxingshigan decoction by CE].

OBJECTIVE: To establish the method for determination of ephedrine hydrochloride, pseudoephedrine hydrochloride and methylephedrine hydrochloride in maxingshigan decoction by capillary electrophoresis. METHODS: The separation was performed on a fused silica capillary of 60 cm x 55 microcrpm ID (52 cm of effective length). 60 mmol/L NaB4O7 + 10% (V/V) CH3OH (pH 9.0) was selected as the running buffer. The separation voltage was 12 kV. The samples was injected by gravity (10 s, 15 cm). The detection wavelength was 210 nm and berberine hydrochloride was the internal standard. RESULTS: The linear range of determination for ephedrine hydrochloride, pseudoephedrine hydrochloride and methylephedrine hydrochloride were 20.0-160.0 microg/mL (r = 0.9999), 7.5-60.0 microg/mL (r = 0.9991) and 2.0-10.0 microg/mL (r = 0.9993). The average recoveries were 98.0%, 97.0% and 97.8%, the precisions of the method were 2.31%, 2.21% and 2.00% (n=6), respectively. CONCLUSION: The method is convenient, rapid and accurate for the quality control of maxingshigan decoction.

[Comparative analysis of volatile oils of Mahuang Fuzi Xixin decoction and its major constituted herbs by GC-MS].

OBJECTIVE: To evaluate the correlativity between volatile oils of Mahuang Fuzi Xixin decoction and its major constituted herbs in composition and proportion. METHODS: The chemical compositions of volatile oils obtained by wet distillation from Mahuang Fuzi Xixin decoction and its major constituted herbs (Herba Ephedrae, processed Radix Aconiti Lateralis, Herba Asari) were analyzed by GC-MS. RESULTS: 44 volatile components of Mahuang Fuzi Xixin decoction were identified, which mainly derived from its constituted herbs Mahuang and Xixin. 68, 8, 39 volatile components were respectively identified from volatile oils of Herba Epherae, processd Radix Aconiti Lateralis and Herba Asari. There were apparent changes in composition and proportion between volatile oils of Mahuang Fuzi Xixin decoction and its major constituted herbs. CONCLUSION: There are apparent changes not only in quantity but also in quality between decoction and its major constituted herbs. Meanwhile any changes in composition may lead to a change in efficacy.

San Wu Huangqin decoction regulates inflammation and immune dysfunction induced by influenza virus by regulating the NF-κB signaling pathway in H1N1-infected mice.

ETHNOPHARMACOLOGICAL RELEVANCE: The San Wu Huangqin Decoction (SWHD), which is made from the dried root of Sophora flavescens Aiton (Kushen in Chinese), the dried root of Scutellaria baicalensis Georgi (Huangqin in Chinese), and the dried root tuber of Rehmannia glutinosa (Gaertn.) DC. (Dihuang in Chinese), is a traditional Chinese formula used to treat prolonged fever and inflammatory diseases in clinics and proven to inhibit influenza virus effectively in our previous study. AIM OF THE STUDY: This work was performed to study the regulation of SWHD on inflammation and immune dysfunction induced by the influenza virus and the underlying mechanism in the treatment of SWHD. METHODS: In this study, the influenza virus A/PR/8/34 (H1N1)-infected mouse model was used to investigate the regulation of SWHD on inflammation and immune dysfunction induced by H1N1. The pathological changes, the capacity of proliferation of T and B lymphocytes, the cytotoxicity of natural killer (NK) cells, and the levels of IL-6, TNF-α, IL-1ß, IL-4, and IFN-γ in the serum, bronchoalveolar lavage fluid (BALF), and lung were analyzed. The effects of type 1 T helper cell (Th1) and type 2 T helper cell (Th2) immune responses were discussed indirectly. In addition, the expression levels of p-p65, p65, IKKα/ß, p-IκBα, and IκBα in relation to the NF-κB pathway were measured using Western blot analysis, or immunohistochemical assay. RESULTS: SWHD decreased the pathological changes in lung tissues, promoted the proliferation of T and B lymphocytes, enhanced NK cell activity, and accelerated the phagocytic function of macrophages in H1N1-infected mice. At the same time, SWHD decreased the levels of IL-6, TNF-α, IL-1ß, IFN-γ, and increased the level of IL-4 in the serum, BALF, and lung of model mice. Moreover, the p-p65, p65, and IκBα protein expression levels were inhibited, whereas the p-IκBα protein expression levels were improved in the lungs of H1N1-infected mice. CONCLUSIONS: SWHD can inhibit the replication of the H1N1 virus and reduced the excessive inflammation and immune dysfunction induced by the H1N1 virus in the body. This work provides rich experimental basis for further anti-inflammation research of SWHD and sets the foundation for the development of a viral inflammation drug of traditional Chinese medicine.

[Effects of herba ephedrae, honey-fried herba ephedrae and maxingshigan decoction on autonomic activities of mice].

OBJECTIVE: To discuss the significance of processing and complex prescription with Herba Ephedrae, the effects of Herba Ephedrae, Honey-fried Herba Ephedrae and Maxingshigan decoction on autonomic activities in mice were compared. METHODS: 110 female Kunming mice were divided into 11 groups, namely normal saline group (NS), ephedrine group (E), high dose Herba Ephedrae group (MH-H), moderate dose Herba Ephedrae group (MH-M), low dose Herba Ephedrae group (MH-L) ,high dose Honey-fried Herba Ephedrae group (ZMH-H), moderate dose Honey-fried Herba Ephedrae group (ZMH-M),low dose Honey-fried Herba Ephedrae group (ZMH-L), high dose Maxingshigan decoction group (MX-H), moderate dose Maxingshigan decoction group (MX-M) and low dose Maxingshigan decoction group (MX-L). The numbers of autonomic activity in 15 minutes before intragastric administration (ig), and after ig 0.5, 1, 2, 3, 4 h were determined. RESULTS: There was interaction between time and groups. There were very significant differences between before ig and all time-points after ig (P < 0.01). 30 minutes after ig,there were significant differences between E and NS,E and ZMH-L,E and MX-L (P < 0.05). 1 h after ig, there were significant differences between MX-M and NS (P < 0.05). 3 h after ig, there were significant differences between MX-M and MH-L (P < 0.05). 30 minutes after ig, both ZMH-L and MX-L could reduce the number of autonomic activity in some extent compare with MH-L. 1 h or 2 h after ig, ZMH-L could reduce the number of autonomic activity in some extent compare with MH-L 4 h after ig, MX-L could reduce the number of autonomic activity in some extent compare with MH-L. CONCLUSION: Under the condition of this study, regarding autonomic activity as index, both ZMH-L and MX-L can reduce center stimulation in some extent.

[Analysis on the HPLC chromatographic fingerprint of gegen qinlian decoction].

OBJECTIVE: To investigate the multiple bioactive constituents in Gegen Qinlian decoction and evaluate its bioactivity and quality control. METHODS: A high performance liquid chromatography with diode array detection (HPLC-DAD) method for the simultaneous qualitative determination of multiple components was developed. The separation was performed on a Kromasil C18 column by gradient elution with acetonitrile and ammonium acetate (containing 0.3% triethylamine, and adjusted pH 4. 3 using 1% glacial acetic acid) as the mobile phase at a flow-rate of 0.7 mL/min, the column temperature was maintained at 30 degrees C, HPLC chromatographic comparison between Gegen Qinlian decoction, four medicinal material and 14 components were carried out to investigate components in the composite formula. RESULTS: 23 characteristic peaks were identified and could be dated back to four medicinal materials from Gegen Qinlian decoction, in which 12 peaks were identifed by standards. CONCLUSION: This readily available, low-cost and reliable HPLC-DAD method can be used for simultaneous analysis of multiple bioactive constituents of Gegen Qinlian decoction and will improve the quality control of Gegen Qinlian decoction.

[Qualitative analysis of the main chemical constituents of shuanghuanglian injection powder and their origin by HPLC-ESI/MS/MS spectrometry].

This paper is to report the analysis of the main chemical constituents of Shuanghuanglian injection powder and determination of their origin. The sample solution was analyzed by a Zorbax C18 column with a gradient mobile phase comprised of methanol and 0.25% acetic acid solution. Both UV and electrospray ionization mass spectrometry detector were used simultaneously, -Q1-scan detection mode was evaluated for the identification of the LC peaks. To analyze the mass spectrum of every LC peaks, 43 molecular mass from the ion chromatogram of Shuanghuanglian injection powder were identified and among them, structure of 20 compounds were elucidated, and the data were sorted to the three component herbs, separately.

[Studies on the chemical constituents in herb of Hedyotis diffusa].

OBJECTIVE: To study the chemical constituents of Hedyotis diffusa. METHODS: Column chromatographic techniques were used for isolation and purification of chemical constituents of this plant and their structures were identified by spectroscopic analysis. RESULTS: Five compounds were isolated and identified as scandoside methyl ester (I), deacetylasperulosidic acid methyl ester (II), 10-dehydrogeniposide (III), 2-hydroxy-3-methylanthraquinone (IV), stigmasterol (V), respectively. CONCLUSION: Compound II as iridoids was isolated from Hedyotis diffusa for the first time, compound III as iridoids was isolated from genus Hedyotis for the first time.

Antipyretic Effect of Herba Ephedrae-Ramulus Cinnamomi Herb Pair on Yeast-Induced Pyrexia Rats: A Metabolomics Study.

OBJECTIVE: To investigate the antipyretic mechanism of Herba Ephedrae (Eph)-Ramulus Cinnamomi (RC) herb pair on yeast-induced pyrexia in rats. METHODS: Totally 30 qualified male SD rats were randomly assigned to the normal control (NC) group, the pyrexia model (model) group, the Eph, RC and Eph-RC treatment groups by a random digital table, 6 rats in each group. Each rat received a 20% aqueous suspension of yeast (10 mL/kg) except the NC group. The 3 treatment groups were administered 8.1, 5.4 and 13.5 g/kg Eph, RC and Eph-RC respectively at 5 and 12 h after yeast injection, the NC group and the model groups were administered equal volume of distilled water. Rectal temperatures were measured at 0, 6, 8, 10, 12, 15, 18, 24 and 30 h and urine was collected prior to yeast injection and at 6, 10, 18, 24, 30, and 36 h after yeast injection. Then urine metabolomic profiling by gas chromatography tandem mass spectrometry, coupled with multivariate statistical analysis and pattern recognition techniques were used to explore the antipyretic effects of Eph-RC. Partial least squares discriminate analysis was used to analyze the metabolomics dataset including classification and regression in metabolomics plot profiling. RESULTS: Compared with the NC group, rectal temperatures were significantly higher in the model group (P<0.01), while 3 treatment groups decreased significantly compared with the model group (P<0.05 or P<0.01). Rectal temperatures of Eph-RC-treated rats started to go down at 6 h, and markedly decreased at 8, 12, 15, 18 and 24 h (P<0.05 or P<0.01), while those of the Eph and RC groups had decreased firstly at 8 h and were markedly lower at 12 h (P<0.05 or P<0.01). Seventeen potential biomarkers related to pyrexia were confirmed and identified, including pyruvic acid, L-phenylalanine, L-tyrosine, phenylacetic acid, hippuric acid, succinic acid, citrate and so on. Eight potential alterations of metabolic pathways including phenylalanine metabolism, citrate cycle, tryptophan metabolism, biosynthesis of valine, leucine and isoleucine, were identified in relation to the antipyretic effects of Eph-RC using MetPA software. CONCLUSION: The antipyretic effect of Eph-RC herb pair on yeast-induced pyrexia in rats involved correction of perturbed amino acid, fatty acid, and carbohydrate metabolism according to the metabolic pathway analysis with MetPA.

Effects of cinnamene enhancers on transdermal delivery of ligustrazine hydrochloride.

Cinnamene compounds, cinnamic acid, cinnamaldehyde and cinnamic alcohol, were employed as enhancers. The effects and mechanisms of penetration promoters on the in vitro percutaneous absorption of ligustrazine hydrochloride across hairless porcine dorsal skin were investigated. Transdermal fluxes of ligustrazine hydrochloride through porcine skin were determined in vitro by Franz-type diffusion cells. The results indicated that the penetration flux of ligustrazine hydrochloride by cinnamic acid was the greatest. Significant statistical differences (P<0.05) were found between cinnamic acid and other promoters. Fourier transform-infrared (FT-IR) were carried out to analyze the effects of enhancers on the biophysical properties of the stratum corneum and the permeation enhancement mechanisms. FT-IR results revealed that the changes of peak shift and peak area due to C-H stretching vibrations in the stratum corneum lipids were associated with the selected enhancers. All of them could perturb and extract the stratum corneum lipids to different extent. Morphological changes of the skin treated with enhancers were monitored by a scanning electron microscope. It was demonstrated that the extraction of the stratum corneum lipids by the enhancers led to the disruption of stratum corneum and the desquamation of stratum corneum flake. Apparent density was newly proposed to estimate the desquamated extent of stratum corneum flake. Correlation analysis revealed that there was a linear relationship between apparent density and decrease in peak area. The results showed that the permeation enhancement mechanisms of cinnamene were pleiotropic ones, including disordering the lipids, extracting the lipids and competitive hydrogen bonding between cinnamene enhancers and amides of ceramide head groups in stratum corneum.

[Effects of among compositions of Herba Ephedrae decoction on genic xpression of 5-lipoxygenase activating protein, IL-4 and leukotriene C4 in asthmatic mice].

OBJECTIVE: To explore the regularity of recipe composition by observing inhibitory effects on the genic expression of 5-lipoxygenase activating protein, IL-4 and the leukotriene C4 in asthmatic mice. METHOD: The mice were challenged with OVA and administered ig with the Herba Ephedrae decoction (HED), separated compositions (2500 mg x kg(-1), calculated by Herba Ephedrae) and dexamethasone (2 mg x kg(-1)) respectively once daily for seven days. The real-time fluorescence quantitative PCR method was employed to measure the contents of FLAP mRNA and IL-4 mRNA expressions in lung and the ELISA method was used to determine the content of LTC4 in the washing solution of pulmonary alveolus and bronchi. RESULT: In the lung of asthma mice, the expressions of FLAP and IL-4 and the content of LTC4 were significantly augmented compared with the control group. The HED and the separated compositions could suppress the expressions of FLAP and IL-4 and LTC4 release to a great extent in mice. CONCLUSION: The HED had the remarkable effects of antianaphylaxis asthma and the original formula HED worked best. These results confirmed the rationality and scientific level of HED.

Comparative Study on the Antivirus Activity of Shuang-Huang-Lian Injectable Powder and Its Bioactive Compound Mixture against Human Adenovirus III In Vitro.

Shuang-Huang-Lian injectable powder (SHL)-a classical purified herbal preparation extracted from Scutellaria baicalensis, Lonicera japonica, and Forsythia suspense-has been used against human adenovirus III (HAdV3) for many years. The combination herb and its major bioactive compounds, including chlorogenic acid, baicalin, and forsythia glycosides A, are effective inhibitors of the virus. However, no comprehensive studies are available on the antiviral effects of SHL against HAdV3. Moreover, it remains unclear whether the mixture of chlorogenic acid, baicalin, and forsythia glycosides A (CBF) has enhanced antiviral activity compared with SHL. Therefore, a comparative study was performed to investigate the combination which is promising for further antiviral drug development. To evaluate their antivirus activity in parallel, the combination ratio and dose of CBF were controlled and consistent with SHL. First, the fingerprint and the ratio of CBF in SHL were determined by high performance liquid chromatography. Then, a plaque reduction assay, reverse transcription polymerase chain reaction (PCR), real-time polymerase chain reaction (qPCR), and enzyme-linked immunosorbent assay (ELISA) were used to explore its therapeutic effects on viral infection and replication, respectively. The results showed that SHL and CBF inhibited dose- and time-dependently HAdV3-induced plaque formation in A549 and HEp-2 cells. SHL was more effective than CBF when supplemented prior to and after viral inoculation. SHL prevented viral attachment, internalization, and replication at high concentration and decreased viral levels within and out of cells at non-toxic concentrations in both cell types. Moreover, the expression of tumor necrosis factor alpha (TNF)-α, interleukin (IL)-1ß, and IL-6 was lower and the expression of interferon (IFN)-γ was higher in both cell types treated with SHL than with CBF. In conclusion, SHL is much more effective and slightly less toxic than CBF.

Evaluation of antinociceptive and anti-inflammatory effects of aqueous extract of Armadillidium vulgare Latreille.

OBJECTIVE: To assess the antinociceptive and anti-inflammatory properties of the aqueous extract of Armadillidium vulgare (AV). METHODS: The antinociceptive effect of AV (400, 600 and 800 mg/kg) was investigated in mice using the acetic acid-induced writhing, formalin-induced nociceptive, and hot plate tests. Phlogogen-induced paw edema using carrageenan, dextran, or compound 48/80 as phlogogen was used as inflammatory models to evaluate AV's anti-inflammatory effect. Additionally, the bioactive substances glucosamine (GLcN) and taurine in AV were determined using high-performance liquid chromatography. RESULTS: Oral treatment of the mice with AV (600 and 800 mg/kg) significantly reduced the number of writhes in the acetic acid-induced writhing test (P<0.01) but not the hot plate test (P>0.05). All doses tested significantly inhibited paw-withdrawal during the second phase of the formalin-induced nociceptive model (P<0.01). AV demonstrated a strong anti-inflammatory effect in all those inflammatory models (P<0.05). CONCLUSIONS: AV has antinociceptive and anti-inflammatory effects, providing scientific evidence of the efficacy of its traditional use in pain treatment. Furthermore, GLcN and taurine contribute, at least in part, to the anti-inflammatory activity of AV.

Comparative pharmacokinetics of three phenylpropanoids in rat plasma after oral administration of Ramulus Cinnamomi and Ramulus Cinnamomi-Ephedrae Herba herb-couple extract.

OBJECTIVE: To investigate the pharmacokinetic characteristics of three phenylpropanoids (cinnamic acid, cinnamic alcohol and coumarin) in Ramulus Cinnamomi (GZ) and Ramulus Cinnamomi-Ephedrae Herba (MH) herb-couple (GZMH). METHODS: Twelve male Sprague-Dawley rats were randomly and equally divided into the GZ and GZMH herb-couple groups. Blood samples were collected at 0, 0.08, 0.25, 0.5, 0.75, 1.5, 3, 4, 6, 8, 12, 24, 36 and 48 h after oral administration. The three phenylpropanoids in rat plasma were quantified using an ultra-performance liquid-chromatography with tandem mass spectrometry (UPLC-MS/MS) method for pharmacokinetic study. RESULTS: In GZMH group, the area under the curve (AUC), mean retention time (MRT) of cinnamic acid and coumarin were increased significantly (P<0.01, respectively), and biological half-life (t1/2z) was obviously shorter (P<0.05) compared with the GZ group. There were no significant differences in the mean retention time from 0 to ∞ (MRT0-∞), the peak concentration (Cmax), the time to peak (Tmax) and t1/2z, except for AUC and MRT0-t (the mean retention time from 0 to t) of cinnamic alcohol in the GZMH group by comparison to the GZ group (P<0.01, respectively). The AUC, MRT (both P<0.01) and t1/2z (P<0.05) of coumarin were increased significantly, while Cmax, and Tmax were decreased slightly by comparison to the GZ group (P>0.05). CONCLUSIONS: There were statistically significant differences in some pharmacokinetic parameters of the three compounds between GZ and GZMH groups, which meant that MH could affect the absorption and elimination of the three compounds.

[Effects of D-limonene and L-limonene on transdermal absorption of ligustrazine hydrochloride].

AIM: To investigate the effects and permeation mechanism of D-limonene and L-limonene on transdermal delivery of ligustrazine hydrochloride (LH). METHODS: Transdermal flux of LH through porcine skin was determined in vitro by Franz-type diffusion cells. The peak shift and peak areas of C-H stretching vibration absorption were estimated by Fourier transform-infrared (FTIR). Morphological changes in the stratum corneum (SC) treated with enhancers were observed by a scanning electron microscope (SEM) and apparent density, a new concept, was proposed to estimate the desquamated extent of SC for the first time. RESULTS: There were no statistic difference (P > 0.05) between the transdermal fluxs of the enantiomer enhancers which were higher than those of control and azone. But the lag time of L-limonene was 2.55 times than that of D-limonene. The FTIR results revealed that the shift and decreased peak area of C-H stretching vibrations in the SC lipids were dependent on the enhancers. The enantiomers permeation enhancers, D-limonene and L-limonene, were able to perturb and extract the SC lipids to different extent. The disordering and extracting lipids activity of L-limonene was stronger than that of D-limonene. SEM studies demonstrated that the extraction of lipids was depended on the selected penetration promoters. CONCLUSION: D-limonene was the most effective enhancer which had the greater transdermal flux of LH and the least lag time. The results showed that the permeation enhancement mechanism of the enantiomer enhancers to LH was multiple ones including disordering and extracting the SC lipids and probably including stereoselective mechanism.

[Preparation and in vitro and in vivo evaluations of topically applied capsaicin transfersomes].

AIM: To prepare capsaicin transfersomes and evaluate them in vitro and in vivo. METHODS: Capsaicin transfersomes were prepared by high shear dispersing machine and evaluated by entrapment efficiency, release rate, in vitro skin permeation and distribution in different tissues in vivo. RESULTS: Capsaicin transfersomes were composed of single unilamellar vesicles with an average diameter of 150.6 nm. Capsaicin entrapment efficiency increased distinctly with increasing of concentration of lecithin and entrapment efficiency is 96.7% while concentration of lecithin to 8%. Cumulative release amount of capsaicin is in direct proportion to the ethanol concentration in the receptor medium. In vitro capsaicin cumulative penetration amount showed higher levels in transfersomes than cream and suspension in rat abdominal skin. Abdominal skin cumulative penetration amount in vitro of capsaicin transfersomes in mouse was significantly higher than that from rat and men. In the same way, abdominal skin epidermal membrane cumulative penetration amount in vitro of capsaicin transfersomes was significantly higher than that from derma and full skin in human abdominal skin. The capsaicin tissue distribution of capsaicin injection by multiple celiac injections in rats is different: bone > plasma > skin > muscle. There is a similar result by multiple thigh topical application of capsaicin transfersomes: bone > skin > plasma > muscle. CONCLUSION: Entrapment efficiency of capsaicin transfersomes reached the criterion of China Pharmacopoeia (> 80%) and capsaicin skin penetration can be increased by capsaicin transfersomes. It should be noted that the diverse characters and levels of skin may probably affect the permeating capability of capsaicin. Capsaicin tissue distribution in bone and muscle is similar and is different in plasma and skin by multiple injections and topical skin apply.

[Research on the influence of compatibility on fingerprint of Glycyrrhiza uralensis in mahuang decoctions by HPLC].

OBJECTIVE: To set up the HPLC fingerprint of Glycyrrhiza uralensis in decoctions prepared from various combinations of the recipe named Mahuang decoctions and study the influence of compatibility on fingerprint of G. wralensis in decoctions. METHOD: The RP-HPLC method was used, chromatography conditions were Zorbax SB-C18 column (4.6 mm x 250 mm, 5 microm), the acetonitrile-1.2% acetic acid (gradient elution) as mobile phase and detective wavelength at 254 nm. RESULT: The method is stable and reliable with a good reproducibility and provides a reference standard for the quality control of G. uralensis, it can be used to determine the fingerprint of G. aralensis in Mahuang decoctions. The result showed that 8 peaks were common in the fingerprint of G. uralensis in Mahauang decoctions. The area changes of 8 common peaks in decoctions prepared from various combinations of Mahuang decoctions were studied. CONCLUSION: The fingerprint of G. uralensis in Mahuang decoctions is markedly influenced by herba ephedrae and ramulus cinnamomi and semen armeniacae amarum. The areas of 7 common peaks were reduced obviously, while the relative areas of 6 common peaks were increased remarkably.

[Study on application of activated carbon in paclitaxel injection].

OBJECTIVE: To inspect the effect of activated carbon with different dosage and temperature on quality of paclitaxel injection. METHOD: Determinations in WS1-(X-026)-2001Z-paclitaxel injection were refered to compare the effect of different dosage and temperature for activated carbon on the taxol content, related material, clarity and bacterial endotoxin. RESULT: When used with 0.25% and 35 degrees C, activated carbon will ensure the quality of paclitaxel injection. CONCLUSION: 0.25% and 35 degrees C are the best condition when activated carbon is used in paclitaxel injection.