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1.
Article in Chinese | WPRIM | ID: wpr-906185

ABSTRACT

Objective:To investigate the effect of the production process of Zushima Guanjie Zhitong Gao from solvent method to hot-pressed method on <italic>in vitro</italic> kinetic behavior of this preparation. Method:Solvent and hot-pressed methods were used to prepare three batches of samples above pilot scale, and <italic>in vitro</italic> release and percutaneous penetration of the index components (7,8-dihydroxycoumarin and methyl salicylate) in Zushima Guanjie Zhitong Gao were investigated by modified Franz diffusing cells. Result:The contents of 7,8-dihydroxycoumarin and methyl salicylate in Zushima Guanjie Zhitong Gao prepared by solvent method were 73.72, 494.67 μg/patch, and their contents in hot-pressed method samples were 159.21, 2 638.99 μg/patch, respectively. In the solvent method samples, the average cumulative release amounts of 7,8-dihydroxycoumarin and methyl salicylate in 24 h were 2.04, 12.21 μg, and their average cumulative release amounts in 24 h of hot-pressed method samples were 2.16, 36.24 μg, respectively. In the solvent method samples, the average cumulative permeation amounts of 7,8-dihydroxycoumarin and methyl salicylate in 24 h were 0.38, 2.79 μg, and they were 0.40, 7.49 μg in hot-pressed method samples. The cumulative release and permeation amounts in 24 h of 7,8-dihydroxycoumarin in the hot-pressed method samples were basically the same as those of the solvent method samples, but the cumulative release and permeation amounts in 24 h of methyl salicylate in the hot-pressed method samples were significantly higher than those of the solvent method samples (<italic>P</italic><0.05). Conclusion:The retention of 7,8-dihydroxycoumarin and methyl salicylate by hot-pressed method is better than that of the solvent method. The process change has no significant effect on the <italic>in vitro</italic> kinetics of 7,8-dihydroxycoumarin in Zushima Guanjie Zhitong Gao, however, after the change from the solvent method to the hot-pressed method, the methyl salicylate in this preparation has a higher cumulative release and permeation amounts.

2.
Article in Chinese | WPRIM | ID: wpr-906119

ABSTRACT

Objective:To identify the transdermal constituents of Euodiae Fructus and predict its molecular mechanism in treating diarrhea by transdermal drug delivery. Method:Ultra performance liquid chromatography-quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS) and integrated pharmacology methods were used. The rapid identification of transdermal constituents of Euodiae Fructus was realized by the means of comparison of reference substances, analysis of UNIFI system and mass spectrometry. On this basis, Integrative Pharmacology-based Research Platform of Traditional Chinese Medicine (TCMIP) v2.0, SymMap, DisGeNET databases and literature were used to collected potential targets of transdermal constituents of Euodiae Fructus and targets for diarrhea-related diseases. The disease targets and drug targets were topologically analyzed to obtain the core targets, which were used for the Gene Ontology (GO) function and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis. Finally, Cytoscape 3.6.0 was used to build up a network of transdermal constituents-core targets-key pathways. Result:A total of 19 chemical constituents were speculatively identified from Euodiae Fructus extract, including quinolone alkaloids, limonins, indole alkaloids, organic acids and sterols. A total of 174 core targets of Euodiae Fructus for treating diarrhea were obtained by a topology analysis, signaling pathways of inflammatory response, cell proliferation, nutrient regulation and energy metabolism, signal transduction, bacterial infection were obtained through the analysis of KEGG enrichment. Conclusion:In this study, the transdermal constituents of Euodiae Fructus are identified for the first time, they can participate in the regulation of intestinal inflammation, maintain the integrity of intestinal mucosa, repaire and adjust the metabolism of the body by acting on Rac protein family, phosphatidylinositol 3-kinase, cytochrome P450 enzymes and aldo-keto reductase, respectively. In general, the molecular mechanism of Euodiae Fructus in the treatment of diarrhea is preliminarily elucidated.

3.
Article in Chinese | WPRIM | ID: wpr-905839

ABSTRACT

Objective:To screen qualitative preparation quality markers of Yuliantang, in order to provide data support for the selection of indicator components, and establish the direct connection between indicator components and efficacy (Xiehuo Zhitong) for achieving the quantity-effect combination. Method:The stability of preparation process of Yuliantang lyophilized powder was investigated by HPLC fingerprint technology, then, the components in Yuliantang lyophilized powder were identified by UHPLC-LTQ-Orbitrap-MS. By referring to the relevant literature, the pharmacological activities of these identified compounds were compared with the pharmacological effects corresponding to the efficacy of Yuliantang, and the composition of the qualitative preparation quality markers of Yuliantang lyophilized powder was determined. Result:The similarities between HPLC fingerprint of 10 batches of Yuliantang lyophilized powder and the control fingerprint were >0.9, indicating that the preparation process was stable and feasible. A total of 29 components were identified from Yuliantang, of which 23 alkaloids, 3 phenylpropanoids, 2 sesquiterpenoids and 1 limonoid, and there were 15 ingredients of<italic> </italic>Coptidis Rhizoma, 12 ingredients of<italic> </italic>Euodiae Fructus, and 2 ingredients of<italic> </italic>Aucklandiae Radix. The composition of the qualitative preparation quality markers of Yuliantang was initially determined as magnoflorine or 10-hydroxy-2,3,9-trimethoxyberberine, phellodendrine, menisperine, thalifendine, groenlandicine, dehydroevodiamine, coptisine, jatrorrhizine, columbamine, methylcoptisine, berberine, epiberberine, palmatine, evodiamine, rutaecarpine, neochlorogenic acid, cryptochlorogenic acid, chlorogenic acid, limonin, costunolide, dehydrocostus lactone. Conclusion:The method for researching and screening the preparation quality markers in Yuliantang lyophilized powder is scientific, reasonable and feasible, it can provide reference for the determination of component indicators in the process research of Yuliantang and qualitative and quantitative indexes in its quality standard.

4.
Article in Chinese | WPRIM | ID: wpr-887943

ABSTRACT

On the basis of the qualitative preparation quality markers of Yulian Decoction, we screened out the quantitative markers and explored a general strategy for analyzing the component migration in Chinese herbal pieces, preparations, and plasma. A method capable of simultaneously determining 28 chemical components in Yulian Decoction was established based on HPLC-MS/MS. This method was used to determine the migrated components in herbal pieces-lyophilized powder preparations-rat plasma after administration of Yulian Decoction. Liquid chromatography was performed under the following conditions: C_(18)-reversed phase chromatographic column(2.1 mm × 100 mm, 1.8 μm); acetonitrile-water(containing 0.1% formic acid) as the mobile phase for gradient elution; the flow rate of 0.2 mL·min~(-1). Electrospray ionization source was adopted for mass spectrometry detection, in which positive and negative ion modes and multiple reaction monitoring were applied. Confirmed by the methodological investigation in linear range, recovery(95.48%-103.4%), precision(RSD, 0.45%-3.8%), stability, and repeatability(RSD, 5.6%-14%), the established method was suitable for the detection and quantification of the components in Yulian Decoction. The results showed that in the lyophilized powder of Yulian Decoction, berberine was greater than 5% in mass fraction, magnoflorine, epiberberine, coptisine, palmatine, and limonin in the range of 1%-5%, and dehydroevodiamine, evodiamine, rutaecarpine, costunolide, and dehydrocostus lactone in the range of 0.002%-1%. Of the 28 components detected in pieces, 27 were found to migrate to the lyophilized powder, and 11 were detected in rat plasma. Fifteen components were preliminarily determined as quantitative preparation quality markers for Yulian Decoction, including berberine, epiberberine, coptisine, palmatine, evodiamine, rutaecarpine, limonin, costunolide, dehydrocostus lactone, magnoflorine, jatrorrhizine, columbamine, groenlandicine, chlorogenic acid, and neochlorogenic acid. In conclusion, the HPLC-MS/MS general strategy was established for analyzing the migration of multiple components in Chinese herbal pieces, preparations, and plasma, which can provide the basis for the screening of quantitative preparation quality markers and multi-index quality control of Yulian Decoction.


Subject(s)
Animals , Chromatography, High Pressure Liquid , Chromatography, Liquid , Drugs, Chinese Herbal , Rats , Spectrometry, Mass, Electrospray Ionization , Tandem Mass Spectrometry
5.
Article in Chinese | WPRIM | ID: wpr-877647

ABSTRACT

OBJECTIVE@#To observe the effect of acupoint application of gel plaster on quality of sleep and life in patients with insomnia.@*METHODS@#A total of 63 patients with insomnia were randomized into a gel plaster group (32 cases, 1 case dropped off) and a placebo plaster group (31 cases). Acupoint application of gel plaster was applied at Yintang (GV 29) and Yongquan (KI 1) in the gel plaster group, placebo plaster was applied at the same acupoints in the placebo plaster group. The treatment was given from bedtime to early moming of the next day, 5 days were as one course, with 2-day interval, totally 4 courses were required in the both groups. Pittsburgh sleep quality index (PSQI), Epworth sleepiness scale (ESS) and Flinders fatigue scale were used to evaluate the sleep quality and fatigue level of the patients in the both groups before and after treatment and at 2 weeks of follow-up. The variations of insomnia TCM syndrome score and the 36-item short-form health survey (SF-36) score before and after treatment were observed.@*RESULTS@#Compared before treatment, the scores of PSQI, ESS and FFS after treatment and at follow-up were decreased in the both groups (@*CONCLUSION@#Acupoint application of gel plaster can effectively improve the quality of sleep and life in patients with insomnia.


Subject(s)
Acupuncture Points , Acupuncture Therapy , Humans , Sleep , Sleep Initiation and Maintenance Disorders/therapy , Treatment Outcome
6.
Article in Chinese | WPRIM | ID: wpr-872995

ABSTRACT

Objective::To study on the feasibility of a new method for determination of astragaloside Ⅳ in Astragali Radix. Method::By summarizing the literatures about the method for determining the content of astragaloside Ⅳ in Astragali Radix and analyzing the results of the preliminary test, a new method for preparing a test solution of astragaloside was established, named " Reflow alkalization derivatization method" . The content determination test was carried out, and the content data of astragaloside Ⅳ in different batches of Astragali Radix measured by the pharmacopoeia method were compared with that by the Reflow alkalization derivatization method. Result::The new method for the determination of astragaloside Ⅳ conformed to the corresponding regulations. The content of astragaloside Ⅳ in astragali radix determined by the new method was higher than that by the pharmacopoeia method. The standard curve was Y=1.315X+ 6.311 2(r=0.999 7, n=6, linear range is 0.044 6-8.92 μg). The RSDs of intraday precision and daytime precision were 0.5% and 0.6%, respectively. The RSD of the repetitive experiment was 1.2%. The RSD of the 48 h stability test was 2.1%, and the RSD of the recovery test was 2.0%. The contents of astragaloside Ⅳ in 16 batches of Astragali Radix determined by Reflow alkalization derivatization method and pharmacopoeia method were 0.371%, 0.203%, 0.315%, 0.218%, 0.386%, 0.221%, 0.353%, 0.192%, 0.303%, 0.197%, 0.373%, 0.188%, 0.361%, 0.114%, 0.349%, 0.112%; 0.243%, 0.152%, 0.214%, 0.168%, 0.274%, 0.157%, 0.221%, 0.133%, 0.203%, 0.141%, 0.257%, 0.132%, 0.238%, 0.084%, 0.242%, and 0.096%. Conclusion::The Reflow alkalization derivatization method can be used to determine the content of astragaloside Ⅳ in Astragali Radix. This method is simpler to operate than the pharmacopoeia method, and the conversion efficiency of astragalus glycosides derivatives is better and reproducible. This method can provide reference for the formation of a fast, scientific and accurate method for the determination of astragalus Ⅳ.

7.
Article in Chinese | WPRIM | ID: wpr-802433

ABSTRACT

Objective: In this paper,the effect of microemulsion in Chuanqi ophthalmic microemulsion in situ gel was investigated. Method: The effect of microemulsion was confirmed by the parallel comparison between the Chuanqi microemulsion in situ gel and normal in situ gel,including study of pharmaceutical characterization and tissue distribution. Result: The average particle sizes of Chuanqi microemulsion in situ gel and normal in situ gel were (38.20±0.13) nm and (985±37) nm,respectively.Microemulsion could maintain the properties of nanocarrier in a microemulsion in situ gel composite system.The result of tissue distribution study showed that only ligustilide could be detected.This was related to the nature of these three indicator components(ligustrazine,ligustilide and astragaloside A).The common logarithm of oil and water partition coefficient of ligustilide(lgP) was 2.87,which was consistent with the range of lgP of ideal ophthalmic drugs(lgP=2.0-3.0).The ligustilide from Chuanqi microemulsion in situ gel could be detected in the cornea,vitreous body and retina,and this compound from normal in situ gel could only be detected in the cornea with low content.At the same time,microemulsion could increase the content of ligustilide in corneal tissues. Conclusion: The characteristics of microemulsion nanocarriers can increase the solubility of ligustilide,compared with normal in situ gel,it can be better distributed in the tears outside the corneal,it reaches the cornea with a higher concentration,and forms a corneal concentration gradient,and ligustilide is transported from the anterior ocular region to the posterior ocular region through the transocular barrier.

8.
Article in Chinese | WPRIM | ID: wpr-687435

ABSTRACT

In this paper, classic preparations in Treatise on Febrile Diseases were systematically investigated to obtain their process parameters, and provide literature evidence and technical support for drug research and development. This paper includes the following sections: drug dose, solvents, excipients, and process parameters of classic preparations. The drug dose in Treatise on Febrile Diseases was not consistent with that in Pharmacopoeia of the People's Republic of China 2015, for example, "Yi-Liang" was about 15.625 g, and "Yi-Sheng" was about 200 mL. The solvents of classic preparations can be divided into two types: wine and water. There were eight kinds of water: water, "Dongliu water" "Ganlan water" "acid pulp" "Jinghua water" "Lao water" "Mafei Tang" "spring water". There four kinds of wines: "wine" "Bai wine" "Qing wine" "Ku wine". There were two kinds of excipients: rice and honey. Classic prescription powder had two kinds of processes: "whole prescription powder" and "Yidaoshai Hezhizhi powder". Classic prescription pills had three kinds of processes: direct whole prescription pilling, pilling after extraction, and pilling with excipients after smashing. Classic prescription decoction had six kinds of processes: "wine Tang", "Mafei Tang", "Jingmi Tang", "Mijian Tang", "water Tang" "Zhugao Tang". Drug dose, solvents, excipients, processes and other key parameters of classic preparations were systemically reviewed in this study, and the process parameters were clarified to provide literature evidence and technical support for drug development.

9.
Article in Chinese | WPRIM | ID: wpr-707009

ABSTRACT

Objective To analyze usage and development trend of TCM decoction pieces in First Hospital of Zhangjiakou City (hereinafter referred to as "our hospital") from 2014 to 2016; To provide the basis for making reasonable purchase plan, reserving TCM decoction pieces and guaranteeing clinical medication.Methods Computer medicine management system was used to conduct statistical analysis on the prescription or order number, dosage, sales, and top 10 TCM decoction pieces among annual consumption and sales of TCM decoction pieces from 2014 to 2016.Results The results showed that the prescription and the order, dosage and sales of TCM decoction pieces decreased year by year. The top 10 TCM decoction pieces in the three years were the same with nine kinds, namely Astragali Radix, Poria, Angelicae Sinensis Radix, Salviae Miltiorrhizae Radix et Rhizoma, Atractylodis Macrocephalae Rhizoma, Ophiopogonis Radix, Coicis Semen, Citri Reticulatae Pericarpium, and Lycii Fructus. Conclusion The usage of TCM decoction pieces in our hospital is reasonable and the structure of medication is stable.

10.
Article in Chinese | WPRIM | ID: wpr-275487

ABSTRACT

In this review, the authors summarized the drugs in treatment of the age-related macular degeneration (AMD or ARMD), including the pathogenesis of the age-related macular degeneration at home and abroad, dosage forms used in the treatment, and the drugs research and development directions in the future. AMD disease is the third largest blinding diseases all over the world, with an incidence of 6.62%. The dosage form of the traditional medicine is mostly oral formulations, playing a role in body, while the newly dosage form is topical drug delivery formulation. Traditional Chinese medicine (TCM) has certain advantages in the treatment of AMD disease and the development of topical drug delivery preparations with newly preparation technologies would have a very bright prospect in the future.

11.
Article in Chinese | WPRIM | ID: wpr-341817

ABSTRACT

To evaluate in vitro release and transdermal behaviors of Huoxue Zhitong gel, modified Franz diffusion cell methods was applied to investigate in vitro transdermal absorption of Huoxue Zhitong gel and the content of paeonolan in receptor fluid composed of PEG400%-95% ethanol-water (l:3:6)were determined by HPLC. The results were processed and different equations were fitted. The release law were in accordance with Weibull equation and the fitting equation was In[-1/(1 - Q)] = -0.790 51nt - 1.7012 (r = 0.9809). In 8 hours, cumulative release of paeonol was 85. 18% and the release rate was 2.827 µg . cm-2 h-1. Transdermal actions were consistent with zero-level model fit and the fitting equation was Q(t) = 1.7579t + 0. 7213 (r = 0.9991). In 8 hours, cumulative transdermal rate and transmission rate of paeonol was 54. 85%, 1. 820 µg . cm-2 h-1. So the Huoxue Zhitong gel had a good release and transdermal properties.


Subject(s)
Acetophenones , Pharmacokinetics , Administration, Cutaneous , Animals , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Pharmacokinetics , Gels , Mice , Skin Absorption
12.
Article in Chinese | WPRIM | ID: wpr-319681

ABSTRACT

<p><b>OBJECTIVE</b>To study the transdermal behavior of Xiaozheng Zhitong cataplasm in rats.</p><p><b>METHOD</b>With tetrahydropalmatine as the index, the Franz diffusion cell method was adopted for the experiment. Sample content was determined with HPLC.</p><p><b>RESULT</b>The transdermal permeability and the transmission rate of tetrahydropalmatine accumulated for 24 h were 20.20% and 0.744 1 microg x cm(-2) x h(-1), respectively.</p><p><b>CONCLUSION</b>The transdermal behaviors of Xiaozheng Zhitong cataplasm were ideal in conformity with the zero order kinetic model.</p>


Subject(s)
Administration, Cutaneous , Animals , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Pharmacokinetics , Female , Permeability , Rats , Rats, Wistar , Skin Absorption
13.
Article in Chinese | WPRIM | ID: wpr-315037

ABSTRACT

To evaluate in vitro release and transdermal behaviors of Zhitong cataplasm, modified Franz diffusion cell method was applied to investigate in vitro transdermal absorption of Zhitong cataplasm and the content of tetrahydropalmatine was determined by HPLC. In 24 hours, accumulative release rate of tetrahydropalmatine was 81. 9%, transmission rate was 2.26 microg x cm(-2) x h(-1). In 48 hours, accumulative transdermal rate and transmission rate of tetrahydropalmatine were 20.31%, 0.22 pg x cm(-2) x h(-1). So Zhitong cataplasm had a good release and transdermal properties and transdermal actions were consistent with zero-order kinetics process.


Subject(s)
Administration, Cutaneous , Animals , Berberine Alkaloids , Chemistry , Pharmacokinetics , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Male , Mice , Plant Extracts , Chemistry , Pharmacokinetics , Skin , Metabolism , Skin Absorption
14.
Article in Chinese | WPRIM | ID: wpr-346891

ABSTRACT

<p><b>OBJECTIVE</b>To establish a LC-MS/MS method for determining the concentration of tanshinone IIA, salvianolic acid B and paeoniflorin of refined coronary cataplasm in rabbit plasma, in order to determine the concentration of the three main ingredients in blood after transdermal administration and calculate their pharmacokinetic parameters.</p><p><b>METHOD</b>Rabbits were given refined coronary cataplasm on the basis of 15 g x kg(-1) by transdermal administration to detect the plasma concentration of the three main ingredients using LC-MS/MS. Winnonlin software was used to calculate their major pharmacokinetic parameters.</p><p><b>RESULT</b>Tanshinone IIA, salvianolic acid B and paeoniflorin showed good linearity (r>0.999) at 1-100, 50-1 000, 10-1 000 microg x L(-1) respectively in plasma, with average recovery rate of 96.57%, 91.90%, 95.93%, respectively. The RSD within day were less than 15%. After transdermal administration of refined coronary cataplasm in rabbits, the main pharmacokinetic parameters of tanshinone IIA, salvianolic acid B or paeoniflorin were as follows: Cmax (20.85 +/- 12.68), (636.25 +/- 386.91), (787.80 +/- 395.64) microg x L(-1); Tmax (0.49 +/- 0.28), (0.44 +/- 0.27), (0.46 +/- 0.30) h.</p><p><b>CONCLUSION</b>The LC-MS/MS method is highly selective and sensitive to determine the concentration of samples in rabbit plasma. The pharmacokinetic characteristics of tanshinone IIA, salvianolic acid B and paeoniflorin are suitable to assess the percutaneous absorption of refined coronary cataplasm.</p>


Subject(s)
Animals , Benzoates , Pharmacokinetics , Benzofurans , Pharmacokinetics , Bridged-Ring Compounds , Pharmacokinetics , Chromatography, Liquid , Methods , Coronary Disease , Drug Therapy , Abietanes , Pharmacokinetics , Drugs, Chinese Herbal , Pharmacokinetics , Glucosides , Pharmacokinetics , Humans , Male , Monoterpenes , Rabbits , Tandem Mass Spectrometry , Methods
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