RESUMEN
With Zang-Fu organs, meridians, Qi and blood, and body fluid as the physiological and pathological basis, traditional Chinese medicine(TCM) theory is guided by the holistic concept and characterized by syndrome differentiation. It has made significant contributions to human health maintenance and disease prevention. Modern TCM preparation is developed on the basis of inheriting and developing TCM preparations using modern science and technology under the guidance of TCM theory. At present, the incidence and mortality of common tumors are increasing. TCM has rich clinical experience in the treatment of tumors. However, in the current stage, some TCM preparations have a tendency to deviate from the guidance of TCM theory. With the modernization of TCM, it is worth considering how TCM theory guides modern TCM preparations. Taking tumor treatment as an example, this paper introduced the development of TCM nano-preparation under the influence of modern nanotechnology, summarized the research on the development of modern TCM nano-preparation from the aspects of TCM holistic concept, TCM treatment principles, and TCM theory application, and discussed the application prospect of TCM nano-preparation in overall therapy, drug pairing, carrier selection, and targeted substance selection under the guidance of TCM theory. This paper provides new references for further developing the combination of tradition and modernization of TCM nano-preparation.
Asunto(s)
Productos Biológicos , Medicamentos Herbarios Chinos , Neoplasias , Humanos , Medicina Tradicional China , Medicamentos Herbarios Chinos/uso terapéutico , Nanotecnología , Neoplasias/tratamiento farmacológicoRESUMEN
In the context of Pharma 4.0, the design tools that support the pharmaceutical Quality by Design(QbD) are iterating fast toward intelligent or smart design. The conventional development methods for traditional Chinese medicine(TCM) preparations have the limitations such as over dependence on experience, low dimensions for the designed experiment parameters, poor compatibility between the process and equipment, and high trial-and-error cost during process scale-up. Therefore, this paper innovatively proposed the intelligent co-design involving material, process, and equipment for manufacturing high-quality TCM preparations, and introduced the design philosophy, targets, tools, and applications with TCM oral solid dosage(OSD) as an example. In terms of design philosophy, the pharmaceutical design tetrahedron composed of critical material attributes, critical process parameters, critical equipment attributes, and critical quality attributes was developed. The design targets were put forward based on the product performance classification system. The design tools involve a design platform that contains several modules, such a as the iTCM material database, the processing route classification system, the system modeling and simulation, and reliability-based optimization. The roles of different modules in obtaining essential and universal design knowledge of the key common manufacturing units were introduced. At last, the applications of the co-design methodology involving material, process, and equipment in the high shear wet granulation process development and the improvement of the dissolving or dispersion capability of TCM formula granules are illustrated. The research on advanced pharmaceutical design theory and methodology will help enhance the efficiency and reliability of drug development, improve the product quality, and promote the innovation of high-end TCM products across the industry.
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Medicamentos Herbarios Chinos , Medicina Tradicional China , Reproducibilidad de los Resultados , Control de Calidad , Simulación por Computador , Comercio , Preparaciones FarmacéuticasRESUMEN
This study aimed to investigate the effects of nanoparticles PLGA-NPs and mesoporous silicon nanoparticles(MSNs) of different stiffness before and after combination with menthol or curcumol on the mechanical properties of bEnd.3 cells. The particle size distributions of PLGA-NPs and MSNs were measured by Malvern particle size analyzer, and the stiffness of the two nanoparticles was quantified by atomic force microscopy(AFM). The bEnd.3 cells were cultured in vitro, and the cell surface morphology, roughness, and Young's modulus were examined to characterize the roughness and stiffness of the cell surface. The changes in the mechanical properties of the cells were observed by AFM, and the structure and expression of cytoskeletal F-actin were observed by a laser-scanning confocal microscope. The results showed that both nanoparticles had good dispersion. The particle size of PLGA-NPs was(98.77±2.04) nm, the PDI was(0.140±0.030), and Young's modulus value was(104.717±8.475) MPa. The particle size of MSNs was(97.47±3.92) nm, the PDI was(0.380±0.016), and Young's modulus value was(306.019±8.822) MPa. The stiffness of PLGA-NPs was significantly lower than that of MSNs. After bEnd.3 cells were treated by PLGA-NPs and MSNs separately, the cells showed fine pores on the cell surface, increased roughness, decreased Young's modulus, blurred and broken F-actin bands, and reduced mean gray value. Compared with PLGA-NPs alone, PLGA-NPs combined with menthol or curcumol could allow deepened and densely distributed surface pores of bEnd.3 cells, increase roughness, reduce Young's modulus, aggravate F-actin band breakage, and diminish mean gray value. Compared with MSNs alone, MSNs combined with menthol could allow deepened and densely distributed surface pores of bEnd.3 cells, increase roughness, reduce Young's modulus, aggravate F-actin band breakage, and diminish mean gray value, while no significant difference was observed in combination with curcumol. Therefore, it is inferred that the aromatic components can increase the intracellular uptake and transport of nanoparticles by altering the biomechanical properties of bEnd.3 cells.
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Mentol , Nanopartículas , Animales , Ratones , Mentol/farmacología , Actinas/metabolismo , Células Endoteliales/metabolismo , Nanopartículas/químicaRESUMEN
Based on the concept of quality by design(QbD), the Box-Behnken design-response surface methodology combined with standard relation(SR) and analytic hierarchy process(AHP)-entropy weight method(EWM) was applied to optimize the extraction process of the classic prescription Yihuang Decoction. The content of geniposidic acid, phellodendrine hydrochloride, and berberine hydrochloride in Yihuang Decoction, the extract yield, and fingerprint similarity were used as the critical quality attributes(CQAs) of the extraction process. The extraction time, water addition, and extraction times were used as the critical process parameters(CPPs). After determining the levels of each factor and level through single-factor experiments, response surface experiments were designed according to the Box-Behnken principle, and the experimental results were analyzed. The SR between each sample and the reference sample under various evaluation indicators of different extraction parameters was calculated. The weights of the five evaluation indicators were determined using AHP-EWM, followed by comprehensive evaluation. A function model between CPPs and CQAs characterized by comprehensive scores was established to predict the optimal extraction process parameters. In the final comprehensive weight coefficients, the yield rate accounted for 43.1%, and the content of berberine hydrochloride, phellodendrine hydrochloride, and geniposidic acid accounted for 35.1%, 6.3%, and 15.5%, respectively. After comprehensive score analysis with SR, the established second-order polynomial model was statistically significant(P<0.01, and the lack of fit was not significant). The predicted optimal extraction conditions for Yihuang Decoction were determined as follows: 8-fold volume of water, extraction time of 1.5 h, and extraction once. The mean comprehensive score of the validation experiment was 85.77, with an RSD of 0.99%, and it met the quality control stan-dards for the reference sample of Yihuang Decoction. The results indicate that the optimized extraction process for Yihuang Decoction is stable and reliable, and the water extract is close in quality attributes to the reference sample. This can serve as a foundation for the research and development of granules in the future. Box-Behnken design-response surface methodology combined with SR and AHP-EWM can provide references for the modern extraction process research of other classic prescriptions.
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Berberina , Medicamentos Herbarios Chinos , Proceso de Jerarquía Analítica , Entropía , AguaRESUMEN
The detection method of characteristic spectrum for reference samples was established by preparing 15 batches of the reference samples of Huagan Decoction, and the peak attribution and the similarity range in the characteristic spectrum were clarified. The ranges of paste-forming rate, content, and transfer rate of the index components including geniposide, paeonol, and paeoniflorin were analyzed. The key quality attribute of the reference samples of Huagan Decoction was defined. The results showed that the 15 batches of the reference samples of Huagan Decoction had good similarities in the characteristic spectrum, which were all higher than 0.9. According to the information of characteristic peak, there were 18 characteristic peaks in the whole prescription, including seven common characteristic peaks from green tangerine peel and dried tangerine peel, four characteristic peaks from tree peony root bark(three of them were common characteristic peaks from tree peony root bark and red peony root), five characteristic peaks from cape jasmine fruit, one characteristic peak from paniculate bolbostemma, and one characteristic peak from oriental waterplantain rhizome.The paste-forming rate of the 15 batches of reference samples was 14.73%-18.83%. The content of geniposide was 1.68%-2.87%, with the average transfer rate of 70.05%±11.13%. The content of paeonol was 0.10%-0.16%, with the average transfer rate of 9.38%±1.78%. The content of paeoniflorin was 1.94%-2.74%, with the average transfer rate of 36.69%±4.63%. This study analyzed the quality value transfer of the reference samples of Huagan Decoction by the evaluation mode of combining the characteristic spectrum, the paste-forming rate, and the content of index components. The findings of this study initially established a stable and feasible standard decoction evaluation method and provided references for the quality control and the subsequent development of relevant preparations of Huagan Decoction.
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Medicamentos Herbarios Chinos , Paeonia , Cromatografía Líquida de Alta Presión , Prescripciones , Control de CalidadRESUMEN
This study aims to establish a method for determination of paeonol(Pae), eugenol(Eug), and piperine(Pip) content in receptor liquid and research on the permeability and pharmacokinetics of Huoxue Zhitong gel patch and microemulsion gel. The Franz diffusion experiment was conducted to assess the percutaneous permeability, and the microdialysis method was employed to assess pharmacokinetics of Huoxue Zhitong gel patch and microemulsion gel. The content of Pae, Eug, and Pip in receptor liquid in vitro and in vivo was determined by HPLC and UPLC-MS. The Q_n and J_(ss) of Pae, Eug, and Pip in the gel patch were significantly higher than those in the microemulsion gel, indicating that the drug release was faster in the gel patch. The C_(max), AUC_(0-760), and MRT of Pae, Eug, and Pip in the gel patch were higher than those in the microemulsion gel, indicating that the gel patch can promote the penetration and prolong the skin residence of the drug. The results of this study provide reference for improving the dosage form of Huoxue Zhitong patch.
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Absorción Cutánea , Espectrometría de Masas en Tándem , Administración Cutánea , Cromatografía Liquida , Emulsiones , Permeabilidad , Piel/metabolismoRESUMEN
Taste is an important factor affecting the medicinal properties of oral preparations and patient compliance with medication, and also an important evaluation index for oral preparation design and clinical application. How to characterize the taste objectively, accurately, simply, and efficiently is a bottleneck problem that restricts the taste design, development, and utilization of oral preparations. At present, the commonly used taste assessment methods for oral preparations are traditional human taste panel, electronic tongue, animal preference test, in vitro release study, and electrophysiological test. The traditional human taste panel is the first choice for taste evaluation, but it is limited by poor subjectivity and reproducibility. Therefore, despite some limitations, the other four taste assessment methods have been applied in the pharmaceutical industry as auxiliary methods. This study reviewed the detection principles, applicability, advantages, and disadvantages of the above methods to provide references for the taste correction research and taste assessment of oral preparations, improve patient compliance and the competitiveness of oral preparation products in the industry, and promote the development of oral preparation technologies.
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Preparaciones Farmacéuticas , Gusto , Administración Oral , Animales , Nariz Electrónica , Humanos , Reproducibilidad de los ResultadosRESUMEN
This study aimed to improve the transdermal permeation quantity of Baimai Ointment by investigating the enhancing effects of physical and chemical permeation promoting methods on transdermal permeation of Baimai Ointment. The improved Franz diffusion cell method was used for in vitro transdermal experiment. The abdominal skin of mice was used, and the skin was treated with 3% propylene glycol in the chemical enhancement group. Ultrasonic technology was introduced in the physical enhancement group. The conditions of ultrasonic technology were optimized by single factor trial. Taking Q_(EF) and ER as the indexes of penetration promotion performance, the enhancing effects of the two methods were compared. The results showed that the promotion performance of 3% propylene glycol for ammonium glycyrrhizinate, nardosinone and curcumin of the chemical enhancement group were 1.74, 1.60, and 3.73 times higher than those of the blank group, respectively. The overall permeation efficiency of the Baimai Ointment was significantly improved. The comprehensive promoting effect on each component was curcumin>ammonium glycyrrhizinate>nardosinone. In the physical enhancement group, the penetration promoting effect of ultrasonic power 1.0 W was better than that of 2.0 W and 0.5 W, ultrasonic time 5 min was better than 3 min and 8 min, and the ultrasonic frequency 1 MHz was better than 3 MHz. Therefore, the optimal ultrasonic condition was 1.0 W-5 min-1 MHz. Under this condition, in terms of the transdermal permeation for ammonium glycyrrhizinate, the Q_(EF) and ER of the ultrasonic technology were better than those of 3% propylene glycol. In terms of the transdermal permeation for nardosinone and curcumin, the QEF and ER of 3% propylene glycol were better than those of the ultrasonic technology. Therefore, 3% propylene glycol combined with ultrasonic technology can be used to promote permeation of Baimai Ointment that contains both water-soluble and fat-soluble components in the clinical application. This study provides a theoretical basis for the clinical application of Baimai Ointment and other transdermal preparations.
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Compuestos de Amonio , Curcumina , Ratones , Animales , Absorción Cutánea , Curcumina/farmacología , Ultrasonido , Administración Cutánea , Piel , Propilenglicol/metabolismo , Propilenglicol/farmacología , Compuestos de Amonio/metabolismo , Compuestos de Amonio/farmacología , PermeabilidadRESUMEN
By preparing 15 batches of Zhenwu Decoction substance benchmarks,the characteristic map,index component content and paste-forming rate were determined to define the peak attribution,similarity range,paste-forming rate range,paeoniflorin and6-gingerol content range and transfer rate range. The similarity between the substance benchmark characteristic map and the control map R generated from the 15 batches of substance benchmarks was higher than 0. 970. There were 19 characteristic peaks in total. By further summarization of the characteristic peaks,it could be seen that tuckahoe had 3 characteristic peaks,white peony root had 10 characteristic peaks,atractylodes had 3 characteristic peaks,ginger had 1 characteristic peak,and Aconite root had 3 characteristic peaks; among them,white peony root and aconite root had 1 common peak. The contents and transfer rates of the 15 batches were0. 50%-0. 93 and 16. 11%-26. 20%; those for 6-gingerol were 0. 018 2%-0. 033 9% and 13. 16%-24. 10%,respectively. The pasteforming rate ranged from 10. 00% to 14. 85%. In this study,the transfer process of substance benchmark value of classic formula Zhenwu Decoction was analyzed based on the characteristic map,the paste-forming rate and the content of the index components; a scientific and stable substance benchmark quality evaluation method was preliminarily established to provide a basis for subsequent development of classic formula Zhenwu Decoction and quality control of relevant preparations.
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Benchmarking , Medicamentos Herbarios Chinos , Cromatografía Líquida de Alta Presión , Control de CalidadRESUMEN
By preparing 10 batches of substance benchmarks freeze-drying powder( lyophilized powder),the methodology of the characteristic spectrum and the content of index component for substance benchmarks of Qingwei San was established. The characteristic peaks and the similarity range of the characteristic spectrum,the contents and the transfer rate range of isoferulic acid,palmatine and paeonol,and the paste-forming rate range were determined to define key quality attributes of substance benchmarks of Qingwei San. In the10 batches of substance benchmarks of Qingwei San,the similarity of characteristic spectrum was higher than 0. 90. In further comparison of the characteristic peak information,a total of 16 characteristic peaks were identified,including 5 characteristic peaks from Cimicifugae Rhizoma,5 characteristic peaks from Coptidis Rhizoma,2 characteristic peaks from Angelicae Sinensis Radix and 4 characteristic peaks from Moutan Cortex. The content of isoferulic acid was 0. 10%-0. 18%,with the average transfer rate of 49. 82%±4. 02%. The content of palmatine was 0. 17%-0. 31%,with the average transfer rate of 15. 84% ±2. 39%. The content of paeonol was 0. 41%-0. 75%,with the average transfer rate of 23. 41%±3. 23%. The paste-forming rate of the 10 batches of substance benchmarks were controlled at 27%-33%,with the transfer rate between the theoretical paste-forming rate and the actual paste-forming rate was 86. 59%±3. 39%. In this study,the quality value transfer of substance benchmarks of Qingwei San was analyzed by the combination of characteristic spectrum,the content of index component and the paste-forming rate. A scientific and stable evaluation method was preliminarily established,so as to provide the basis for subsequent development and quality control of relevant preparations of Qingwei San.
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Benchmarking , Medicamentos Herbarios Chinos , Cromatografía Líquida de Alta Presión , Polvos , Control de Calidad , RizomaRESUMEN
This study was mainly based on the compatibility of Puerariae Lobatae Radix and Chuanxiong Rhizoma to prepare submicron emulsion and evaluated its physical and pharmaceutical properties. Firstly, pseudo-ternary phase diagrams were drawn by dripping method which took Chuanxiong oil as the oil phase and the area of microemulsion region as the index. On this basis, suitable emulsifier and co-emulsifier were screened for the preparation of Chuanxiong oil submicron emulsion. Then, the formula realizing the largest oil loading was selected. Finally, puerarin substituted part of emulsifier and co-emulsifier to lower their content, so as to form puerarin-Chuanxiong oil submicron emulsion featuring the combination of medicine and adjuvant. Its particle size, zeta potential, centrifugal stability and storage stability were determined, and the in vitro drug release behavior was investigated by dialysis bag method, based on which the quality of the as-prepared submicron emulsion was evaluated comprehensively. The proposed method was proved feasible for the preparation of Chuanxiong oil submicron emulsion, which adopted polyoxyethylene castor oil(EL-40) as the emulsifier and was free from co-emulsifier. The formula of the maximum oil loading was found as Chuanxiong oilâ¶EL-40â¶water 3â¶7â¶90. Further, puera-rin successfully replaced up to 10% of the emulsifier in submicron emulsion. Eventually, the optimal drug-loading formula was determined as puerarinâ¶Chuanxiong oilâ¶EL-40â¶water 7â¶30â¶63â¶900. The quality evaluation results of the as-prepared submicron emulsion demonstrated that the average emulsion droplet size was 333.9 nm, the PDI 0.26, and the zeta potential-10.12 mV. The submicron emulsion had a good centrifugal stability and did not present any instable phenomena such as delamination and precipitation during its standing still for 50 days. The evaluation of in vitro drug release behavior indicated that the submicron emulsion was capable of releasing the drug completely. The puerarin-chuanxiong oil submicron emulsion prepared in this study possessed a stable quality and to some extent increased the solubility of puerarin along with a sustained-release effect. This study provided ideas for the clinical application of puerarin.
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Isoflavonas , Emulsiones , Tamaño de la Partícula , SolubilidadRESUMEN
By preparing 15 batches of substance benchmarks of Taohong Siwu Decoction, the methodology of the characteristic spectrums of substance benchmarks was established. The paste-forming rate range, the contents and the transfer rate range of the index components, hydroxy safflower yellow A, ferulic acid and paeoniflorin, the characteristic peaks and the similarity range of the characteristic spectrums of Taohong Siwu Decoction were determined to define key quality attributes of substance benchmarks of Taohong Siwu Decoction.In the 15 batches of substance benchmarks of Taohong Siwu Decoction, the similarity of characteristic spectrums was higher than 0.9. Furthermore, based on summarization of the characteristic peak information, there were 13 characteristic peaks in the whole decoction. Baishao had three characteristic peaks, Honghua had seven characteristic peaks, and Chuanxiong and Danggui had three characteristic peaks. The paste-forming rate of the 15 batches of substance benchmarks was controlled at 33.11%-40.62%. The content of hydroxy safflower yellow A was 0.129%-0.203%, with the average transfer rate of 16.596%±0.669%.The content of ferulic acid was 0.043%-0.055%, with the average transfer rate of 20.489%±1.772%.The content of paeoniflorin was 0.676%-0.943%, with the average transfer rate of 29.112%±3.273%.The quality value transfer of substance benchmarks of classical prescription Taohong Siwu Decoction was analyzed by the combination of characteristic spectrums, paste-forming rate and the content of index components. The established substance benchmark quality evaluation method was stable and feasible, and could provide a basis for quality control and subsequent development of relevant preparations of Taohong Siwu Decoction.
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Benchmarking , Medicamentos Herbarios Chinos , Control de CalidadRESUMEN
In this experiment, by determination of the HPLC characteristic spectrum of the classical prescription Qingwei San decoction, the contents of isoferulic acid, palmatine and paeonol in Qingwei San decoction and the extraction rate were investigated. The factors such as the crushing degree of decoction pieces, the amount of decocting water, the decocting time, the filter material and the decocting container involved in Qingwei San decoction process were examined to make a detailed comparison of Qingwei San's decoction processes during the development.HPLC characteristic spectrum method of Qingwei San was established, and then the decoction process parameters of Qingwei San were optimized, with the similarity of characteristic spectrum, the concentration of the index components and the extraction rate as indexes. The decoction process of Qingwei San was determined as follows: Qingwei San decoction pieces were weighed according to the prescription amount and pulverized into the most coarse powder; the powder was put in a ceramic pot, added with 225 mL water, heated to boiling, cooked for 50 minutes with gentle heat(100 W), and filtered with a layer of 300 mesh nylon cloth.The similarity of Qingwei San's characteristics pectrum of different decoction methods was all above 0.9, and the concentration of isoferulic acid, palmatine and paeonol in Qingwei San under determined decoction process was 40.74, 26.73, 65.73 µg·mL~(-1), respectively, with an extraction rate of 33.80%.The characteristic spectrum determined in this experiment can better express the information and index components of Qingwei San, and if combined with the extraction rate information, it can provide the general information, index component content and extraction information. The decoction process after detailed investigation can better reflect the quality of Qingwei San decoction, with easier control and operation. It can provide a basis for the subsequent research and development of Qingwei San decoction standard, and can also provide experimental basis and reference for the decoction process research of other classical prescriptions.
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Medicamentos Herbarios Chinos , Cromatografía Líquida de Alta Presión , Polvos , Prescripciones , AguaRESUMEN
In this experiment, the decoction process of famous classical formula Xiebai San was determined by optimizing the particle size of "Cuo san" and investigating the decoction process parameters, such as boiling container, water volume and duration. Xiebai San was taken as an example to explore the study method of the "Cuo san" in the famous classical formulas. The specific chromatogram of Xiebai San and the determination method of glycyrrhizin and glycyrrhizic acid in Xiebai San were established. Different particle sizes of "Cuo san" and decoction parameters were optimized based on the similarity of specific chromatogram, the specific chromatogram's peak area, the content of glycyrrhizin, the content of glycyrrhizic acid and extract yield rate.The particle size of Xiebai San powder was determined to be 2.00-4.75 mm(by four-mesh sieves). The decoction process was determined as follows: put the prescription amount into a ceramic pot, add 420 mL of water, and boil and simmer until the volume is 300 mL.The similarity of specific chromatogram was above 0.9, the specific chromatogram's peak area was larger, the content of glycyrrhizin was 0.12%, the content of glycyrrhizic acid was 0.21%,and the extract yield rate was 15.05%. The finally determined particle size of "Cuo san" can better represent the quality of Xiebai San, and is easy to prepare and suitable for industrial production.This experimental research method can comprehensively investigate the quality of Xiebai San as a whole, the content of active ingredients, and the situation of extract yield.It is a more comprehensive and objective evaluation method, and can provide experimental basis and reference for the study of other "Cuo san" famous classical formulas.
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Medicamentos Herbarios Chinos/química , Ácido Glicirrínico/análisis , Tamaño de la Partícula , Tecnología Farmacéutica , PolvosRESUMEN
Famous traditional formula Sanpian Decoction(SPD)comes from Dialectical Records of Chen Shiduo of the Qing Dynasty,and ranks among 100 classic prescriptions of Classic Famous Traditional Formula catalogue(the First Batch). SPD was prepared according to Management Standards for Traditional Chinese Medicine Decoction Room in Medical Institutions. According to the polarity of different components in SPD,two HPLC fingerprints were established, in which six herbs, namely Chuanxiong Rhizoma, Paeoniae Randix Alba, Sinapis Semen, Glycyrrhizae Radix et Rhizoma, Pruni Semen, Angelicae Dahuricae Radix,are all reflected in the fingerprints; The dry extract rate, transfer rate and similarities of fingerprints were used as indicators to study the relationship between the quality value transmitting of medicinal herbs-decoction pieces-whole decoction of Chuanxiong Rhizoma. Experiment result shows that,the transfer rate of ferulic acid from medicinal herbs to decoction pieces is between 72.00% and 108.36%; the transfer rate of ferulic acid from decoction pieces to SPD is between 31.76% and 64.09%; the dry extract rate of the whole decoction is between 14.69% and 20.16%;The similarity range of fingerprint 1 of 15 batches of SPD is between 0.971 and 0.998, and the similarity range of fingerprint 2 is between 0.980 and 0.996. The established fingerprint has rich information,and the established quality evaluation method is suitable for the quality control of medicinal herbs-decoction pieces-whole decoction of Chuanxiong Rhizoma, which can provide a certain reference for developing the quality control evaluation method for formulated granules, famous formulae and other terminal products derived from traditional Chinese medicine decoction.
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Medicamentos Herbarios Chinos/química , Control de Calidad , Cromatografía Líquida de Alta Presión , Medicina Tradicional China , RizomaRESUMEN
The antipyretic effects of Qingkailing soft capsules and hard capsules were compared based on metabonomics technology,so as to provide basis for clinical rational use and quality control evaluation of its preparations. By using ultra high performance liquid chromatography-linear ion trap/orbitrap high resolution mass spectrometry( UPLC-LTQ/Orbitrap),and multivariate tatistical methods such as principal component analysis( PCA),partial least squares-discriminate analysis( PLS-DA) and orthogonal signal correction partial least square discriminant analysis( OPLS-DA),the changes of plasma endogenous metabolites in rat fever model induced by dry yeast were studied,so as to look for biomarkers related to fever. Based on these results,the antipyretic effects of two types of Qingkailing preparations were compared. The results indicated that metabolic profiles of the experimental groups could be distinguished distinctly,and 8 endogenous metabolites showed differences as compared with the normal control group( P<0. 05),including nicotinic acid,choline,hippuric acid,phosphocholine,Lyso PC( 14 ⶠ0),Lyso PC [16 ⶠ1( 9 Z) ],Lyso PC( 18 ⶠ0) and Lyso PC [20 ⶠ3( 5 Z,8 Z,11 Z) ]. They could be regarded as biomarkers related to fever. Qingkailing soft capsule and hard capsule had different effects on the regulation of plasma metabolites in yeast-induced fever model rats. Qingkailing soft capsule had different degrees of callbacks on eight biomarkers,including significant callbacks on nicotinic acid( P<0. 05),hippuric acid( P< 0. 01),phosphocholine( P< 0. 05),and Lyso PC [20 â¶3( 5 Z,8 Z,11 Z) ]( P<0. 05),while hard capsule only had significant callbacks on nicotinic acid( P<0. 05),hippuric acid( P<0. 01),and phosphocholine( P< 0. 05),with no callbacks on choline,Lyso PC( 14 ⶠ0),Lyso PC [16 ⶠ1( 9 Z) ],Lyso PC( 18 â¶0),and Lyso PC [20 â¶3( 5 Z,8 Z,11 Z) ]. This indicated that Qingkailing soft capsule had better callback effect than hard capsule. In this study,Qingkailing soft capsules and hard capsules were used to intervene the changes of related biomarkers in yeast-induced fever rat models,and then the antipyretic effect and mechanism between these two kinds of capsules were compared. The two dosage forms played an antipyretic role mainly by regulating lipid metabolism and controlling inflammation. The callback effect of soft capsule on the potential biomarkers of lysophosphatidylcholine was significantly higher than that of hard capsule. The differences in antipyretic effect of Qingkailing soft capsule and hard capsule were expounded from the point of metabonomics,providing experimental data and theoretical basis for the selection of clinical dosage forms.
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Antipiréticos/farmacología , Medicamentos Herbarios Chinos/farmacología , Animales , Biomarcadores/sangre , Cápsulas , Metabolómica , RatasRESUMEN
To establish a determination method for the contents of ammonium glycyrrhetate,nardosinone,and curcumin in transdermal receptor liquid of Baimai Ointment,and investigate the percutaneous permeability of Baimai Ointment and the effects of two kinds of penetration enhancers on percutaneous absorption of three components. The contents of ammonium glycyrrhetate,nardosinone,and curcumin in transdermal receptor liquid were determined by high pressure liquid chromatography( HPLC). The vertical modified Franz diffusion cell was used to perform a transdermal experiment in vitro with the abdominal skin of mice( treated and untreated). The transdermal receptor liquid was preferably used to investigate the transdermal absorption rule of the Baimai Ointment and the effect of the penetration enhancer. The results showed that the comprehensive solubility of PEG-ET-NS( 3 â¶3 â¶4) was best among three types of receptor liquid PG-ET-NS( 3 â¶3 â¶4),PEG-ET-NS( 3 â¶3 â¶4),ET-NS( 3 â¶7). PEG-ET-NS was used as the receptor liquid for in vitro transdermal experiments. The cumulative permeation area of ammonium glycyrrhetate,nardosinone and curcumin within 24 h was 5. 73,18. 99,0. 38 µg·cm~(-2)respectively. Taking QEFand ER as comprehensive evaluation indicators of permeation performance,the comprehensive penetration-promoting performance of ammonium glycyrrhizinate: 3% PEG 400-ethanol-normal saline ≈ 1. 19 times( 3%azone) = 1. 94 times( blank); comprehensive penetration-promoting performance of nardosinone: 3% PEG 400-ethanol-normal saline≈1. 28 times( 3% azone) = 1. 37 times( blank); the comprehensive penetration performance of curcumin: 3% PEG 400-ethanol-normal saline≈1. 77 times( 3% azone) ≈3. 42 times( blank). The comprehensive penetration enhancement properties of the two penetration enhancers were as follows: 3% PEG 400-ethanol-normal saline>3%azone>blank. The transdermal absorption curve of ammonium glycyrrhetate,nardosinone and curcumin in Baimai Ointment were consistent with the zero-order equation,indicating that the transdermal absorption process was irrelevant to the concentration of three components,and its was a diffusion process. This experiment provides reference for the study of ointment transdermal preparations.
Asunto(s)
Administración Cutánea , Pomadas/farmacocinética , Absorción Cutánea , Piel , Animales , Ratones , PermeabilidadRESUMEN
In recent years,the development and application of classical famous prescriptions have attracted much attention. However,the differences between ancient and modern conditions lead to difficulties in carrying out practical work. In this paper,with Houpu Wenzhong Decoction as an example,the key technologies of boiling granularity,water addition,boiling time and sample pretreatment methods were investigated on the basis of sufficient literature research. The experimental results showed that there was no significant difference in the concentration of index components between those with different granularity( 2 mm and 3-5 mm) and different decocting time( 30 min and 60 min),but the extraction rate of index components was relatively high when the granularity of powder was 2 mm and decocting time was 30 min. With the increase of water content,the concentration of index components and the extraction rate were increased in varying degrees. A certain proportion of methanol aqueous solution was used as the resolvent before content determination of the reference sample of Houpu Wenzhong Decoction,which could take into account both the spectral information of water-soluble components and fat-soluble components in the prescription,and help to display the overall information of the prescription' s chemical components more comprehensively. At the same time,the boiling and dispersing classical prescriptions in the Catalogue of Ancient Classical Prescriptions( the first batch) were collected and summarized in this study; the key influencing factors of decocting process were analyzed from different angles,and preliminary research suggestions were put forward,so as to provide a certain direction and reference for the establishment of quality standard of Houpu Wenzhong Decoction,as well as for the development,research and clinical application of boiling and dispersing classical prescriptions.
Asunto(s)
Medicamentos Herbarios Chinos/normas , Polvos , PrescripcionesRESUMEN
By preparing 10 batches of the material reference of Linggui Zhugan Decoction,the methodology of the characteristic spectrum of the material reference was created. The creaming rate range,the contents and the transfer rate range of cinnamaldehyde,glycyrrhizin and glycyrrhizic acid,the characteristic peaks and the similarity range of the characteristic spectrum of Linggui Zhugan Decoction were determined to clarify key quality attributes of the material reference of Linggui Zhugan Decoction. In the 10 batches of the material reference of Linggui Zhugan Decoction,the similarity of characteristic spectrum was higher than 0. 9. Furthermore,after summarizing the characteristic peak information,we knew that Fuling had two characteristic peaks,Guizhi had six characteristic peaks,Baizhu had two characteristic peaks and Gancao had 11 characteristic peaks. The average creaming rate of the material reference of the ten batches was( 12. 13 ± 0. 35) %. The average content of cinnamaldehyde was 0. 32%,the average transfer rate was 10. 69%,the content of cinnamaldehyde in the different batches was between 0. 22% and 0. 42%,and the transfer rate was between 7. 48% and13. 90%. The average content of glycyrrhizin was 0. 84%,the average transfer rate was 50. 39%,the content of glycyrrhizin in the different batches was between 0. 42% and 1. 26%,and the transfer rate was between 35. 27% and 65. 51%. The average content of glycyrrhizic was 1. 88%,the average transfer rate was 40. 74%,the content of glycyrrhizic in the different batches was between 0. 94% and2. 82%,and the transfer rate was between 28. 52% and 52. 96%. In this paper,the quality value transmitting of substance benchmarks of Linggui Zhugan Decoction was analyzed by the combination of characteristic spectrum,creaming rate and the content of index component. A scientific and stable method was preliminarily established,which provided scientific basis for the quality control and formulation development of Linggui Zhugan Decoction.
Asunto(s)
Medicamentos Herbarios Chinos/normas , Extractos Vegetales/normas , Control de Calidad , Cromatografía Líquida de Alta Presión , Medicamentos Herbarios Chinos/análisis , Glycyrrhiza , Ácido Glicirrínico/análisis , Extractos Vegetales/análisisRESUMEN
The aim of this research is to investigate the effects of paeoniflorin and menthol on the physiological function of Calu-3 cell membrane during the transport of puerarin. Calu-3 cell was used as the in vitro cell model to simulate nasal mucosa tissues, and the cell membrane fluidity, Naâº-Kâº-ATPase activity and Ca²âº-ATPase activity were detected by fluorescence recovery after photobleaching(FRAP) and ultramicro enzyme activity testing, in order to explore the mechanism of compatible drugs on promoting puerarin transport. The results showed that when puerarin associated with low, middle and high concentration of menthol or both paeoniflorin and menthol, the fluorescence recovery rate was increased significantly, while Naâº-Kâº-ATPase activity had no significant change and Ca²âº-ATPase activity was enhanced significantly as compared with puerarin alone. Therefore, it was concluded that menthol had the abilitî of promoting the transport and the mechanism might be related to increasing membrane fluidity and activating Ca²âº-ATPase.