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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.
Subject(s)
Humans , Medicine, Chinese Traditional , Drugs, Chinese Herbal/therapeutic use , Biological Products , Nanotechnology , Neoplasms/drug therapyABSTRACT
Objective:A strong antithrombotic protein component， named PvQ， was purified and enriched from total protein of <italic>Pheretima vulgaris</italic>，<italic> </italic>a<italic> </italic>traditional Chinese medicine. Moreover， we evaluated its fibrinolytic and anticoagulant activity， and expected to provide reference for the research on antithrombotic substances of Pheretima. Method:A rapid <italic>in</italic> <italic>vitro</italic> activity-oriented separation combined with the AKTA-Pure protein purification system conducted on <italic>P. vulgaris</italic>. Meanwhile， the fibrinolytic and anticoagulant activities of PvQ were measured by fibrin plate method and fibrinogen-thrombin time （Fibg-TT） method. And the <italic>in vitro</italic> thrombolysis assay was used for evaluating the lysis ability of PvQ to thrombus. Then the stability of PvQ was also analyzed for its anticoagulant activity at different pH and temperature. Result:The PvQ was successfully enriched and its activity was determined to have significant fibrinolytic and anticoagulant activities. And the result of <italic>in vitro</italic> thrombolysis assay revealed that PvQ could hydrolyze more than 80% of thrombus after 5 h of incubation at 37 ℃. In addition， the changes of temperature and pH had significant effects on antithrombotic activity， and this study showed that PvQ was rapidly inactivated at ≥60 ℃ or in acidic conditions （pH<7）. While， the activity of PvQ was unaffected or less affected at ≤50 ℃ and under alkaline conditions. Conclusion:A feasible preparation method of PvQ is established， and it can affect fibrin and fibrinogen at the same time， thus exerting a dual fibrinolytic effect and possessing significant fibrinolytic and anticoagulant activities. It provides a scientific interpretation for the treatment of thrombotic diseases by PvQ and a reference for the development of antithrombotic protein products of Pheretima.
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Taohong Siwutang， originating from Fuke Bingjian by CHAI Dehua in the Qing Dynasty， has been included in the first batch of the 100 classical prescriptions published by the National Administration of Traditional Chinese Medicine（TCM）. Taohong Siwutang is composed of six Chinese medicinals， namely the wine-washed Angelicae Sinensis Radix， wine-washed Rehmanniae Recens Radix， wine-washed Carthami Flos， wine-processed Paeoniae Alba Radix， Persicae Semen undergoing peel-off process in hot water， and Chuanxiong Rhizoma， possessing the effects of nourishing blood， promoting blood circulation， and removing blood stasis， and it is mainly applicable to patients with blood deficiency and stasis syndrome. The textual research on the key information of classical prescriptions and the summarization of their ancient and modern applications are conducive to learning about the research status and confirming the subsequent research direction， thus better guiding the preparation of substance benchmarks and the in-depth exploration of preparations. By exploring the sources and historic evolution of Taohong Siwutang and each Chinese medicinal， this paper uncovered the prescription composition， origin of each Chinese medicinal， processing method， and prescription dose. The review of its clinical applications showed that the application scope in modern times has been extended and expanded in contrast to that recorded in ancient books. As revealed by the clinical application literature， it has been mainly employed for treating gynecological diseases such as dysmenorrhea and irregular menstruation， orthopedic diseases like fracture， dermatological diseases such as chloasma， and internal diseases such as coronary heart disease， all of which were differentiated into the blood deficiency and stasis syndrome. It could be seen that Taohong Siwutang had great clinical application value. This review of the ancient and modern literature concerned with Taohong Siwutang and the analysis and determination of its key information are expected to provide a reference for the rational clinical application and further research of Taohong Siwutang.
ABSTRACT
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.
Subject(s)
Benchmarking , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Powders , Quality Control , RhizomeABSTRACT
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.
Subject(s)
Benchmarking , Drugs, Chinese Herbal , Quality ControlABSTRACT
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.
Subject(s)
Benchmarking , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Quality ControlABSTRACT
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.
Subject(s)
Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Powders , Prescriptions , WaterABSTRACT
Objective: To compare the effect of four kinds of decocting containers on the content of sinapine and the HPLC specific chromatograms of Sinapis Semen decoction,so as to optimize decocting container for the development of classical formulas. Method: Selecting four kinds of decoction vessels,named traditional casserole,ceramic pot,round-bottom flask and stainless-steel pot as the research object,the content of sinapine in Sinapis Semen decoction and its HPLC specific chromatograms were used as indexes to investigate the influence of different decoction vessels on the decoction.Similarity evaluation of specific chromatograms was performed by the "Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine"(edition of 2004A). Result: The contents of sinapine in the decoction prepared by traditional casserole,ceramic pot,round-bottom flask and stainless-steel pot were 0.04%,0.07%,0.84% and 0.97%,respectively.Compared with specific chromatograms of the decoction prepared by traditional casserole,the similarities of specific chromatograms of the decoction prepared by ceramic pot,round-bottom flask and stainless-steel pot were 0.98,0.82 and 0.68,respectively.Compared with specific chromatograms of the decoction prepared by ceramic pot,the similarities of specific chromatograms of the decoction prepared by round-bottom flask and stainless-steel pot were 0.79 and 0.62,respectively.Compared with specific chromatograms of the decoction prepared by round-bottom flask,the similarity of specific chromatograms of the decoction prepared by stainless-steel pot was 0.97. Conclusion: The content of sinapine and HPLC specific chromatograms of Sinapis Semen decoction obtained from different decocting containers are quite different.
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This paper compared and analyzed the relevant records of Chinese medicine pharmacy in the Han,Tang and Song dynasties,and summarized the changes of the dosage forms,preparation techniques and administration methods of Chinese medicine with the development of history.In this study,three classic medical works in the Han,Tang and Song dynasties,including Treatise on Febrile Diseases Caused by Cold,Valuable Prescriptions for Emergency and Formularies of the Bureau of People's Welfare Pharmacies,were taken as the research objects,and the development of the dosage forms,auxiliary materials,preparation technology and medication theory were summarized and explored by the ways of content analysis,comparative analysis and case analysis.The comparison showed that in the development process,the dosage forms gradually increased,but the liquid dosage forms gradually decreased,the solid dosage forms gradually increased.Not only the dosage forms varied in the number,types of excipients used more and more,but the level of preparation had been constantly improved while the methods of taking became more detailed.This evolution of dosage forms and pharmaceutical technologies in Chinese history is worth learning and thinking about it.Through exploring the traditional Chinese medicine(TCM) technologies and theories in the Han,Tang and Song dynasties,we can contribute to the inheritance of traditional preparations and it can provide the basis for the development of modern preparations with TCM characteristics.
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Bio-adhesive drug delivery system (BDDS) is a novel drug delivery system, which can prolong the retention time of the preparation, improve the stability of the drug, and improve the mucosa absorption and the targeting of the drug. With the development of polymer materials over the past 30 years, BDDS made a great progress. This paper reviews the muco-adhesion theory, adhesive materials, and methods to evaluate muco-adhesive properties and applications in traditional Chinese medicine according to domestic and foreign literatures, in order to provide new ideas for further studies.
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The borneol was included with β-CD and prepared Fufang Danshen intestinal adhesion pellets. GC method for determination of borneol in Fufang Danshen intestinal adhesion pellets was established to study its in vitro dissolution and make a comparison with the Fufang Danshen tablet, in this way, the rationality of dosage form was evaluated. The first method of dissolution determination was used for determining the in vitro dissolution of borneol in Fufang Danshen intestinal adhesion pellets in artificial intestinal juice, and Fufang Danshen tablet in artificial gastric juice and intestinal juice, respectively. Result shows: the concentration of borneol in Fufang Danshen intestinal adhesion pellets and Fufang Danshen tablet was 0.79% and 0.80%, respectively. Its in vitro dissolution was nearly 70% within 12 h in Fufang Danshen intestinal adhesion pellets, and in Fufang Danshen tablet, the dissolution was about 60% within 20 min and more than 90% within 40 min, and in artificial gastric juice, was less than 20% within 40 min but more than 80% till 150 min. Research suggests that in comparison with Fufang Danshen tablet, in vitro dissolution of borneol in the Fufang Danshen intestinal adhesion pellets showed an obvious sustained release behavior. The borneol in Fufang Danshen intestinal adhesion pellets was included with β-CD and prepared enteric preparations. To some extent, the stimulation on stomach and intestinal mucosa can be reduced and safety can be improved.
Subject(s)
Humans , Camphanes , Chemistry , Pharmacology , Chemistry, Pharmaceutical , Methods , Dosage Forms , Drugs, Chinese Herbal , Chemistry , Pharmacology , Intestinal Mucosa , Metabolism , Models, Biological , SolubilityABSTRACT
Traditional Chinese medicine has a long history of intranasal administration. Compared with the other administration routes, intranasal administration has the benefits of fast absorption, high bioavailability, high brain-targeting and non-invasive. In the past few years we take "Xingnaojing" and "Tongqiao Sanyu formula" as model drug and studied pharmacokinetics of effective components of different polarities. MDCK/MDCK-MDR1 cells were used to simulate blood brain barrier to study the permeate behaviors of different drug and the mechanism of enhancing effects of aromatic medicine. Then a microemulsion (modified by mPEG2000-PLA) was prepared for intranasal administration, and the pharmacokinetics and investigated tissue distribution were studied by fluorescence imaging. The irritation of the drug and different preparations were studied on human nasal epithelial cell (HNEC) cell and living animals. In this paper, we reviewed the achievements and hope that it can provide constructive suggestions for the future research.
Subject(s)
Animals , Humans , Administration, Intranasal , Methods , Biological Availability , Blood-Brain Barrier , Drugs, Chinese Herbal , PharmacokineticsABSTRACT
An HPLC method for the determination of geniposide concentration in mouse plasma was developed and the pharmacokinetics after intranasal administration of Xingnaojing microemulsion (XNJ-M) and mPEG2000-PLA modified Xingnaojing microemulsion (XNJ-MM) were investigated. Eighty mice were treated by XNJ-M and XNJ-MM nasally. The plasma samples were collected at different times and the drug in samples was detected by HPLC. The pharmacokinetic parameters were calculated by the software of Kinetica. The pharmacokinetic parameters of geniposide of XNJ-M were C(max) (4.36 +/- 2.69) mg x L(-1), t(max) 1 min, MRT (29.73 +/- 4.54) min, AUC (53.63 +/- 14.03) mg x L(-1) x min. The pharmacokinetic parameters of geniposide of XNJ-MM were C(max) (9.75 +/- 4.14) mg x L(-1), t(max) 1 min, MRT(22.34 +/- 2.90) min, AUC (131.87 +/- 40.13) mg x L(-1) x min. Geniposide can be absorbed into blood in a higher degree after intranasal administration with XNJ-MM compared to XNJ-M, which maybe caused by its less irritating and more absorption.
Subject(s)
Animals , Male , Mice , Drugs, Chinese Herbal , Chemistry , Emulsions , Iridoids , Blood , Pharmacokinetics , Lactic Acid , Chemistry , Polyesters , Polyethylene Glycols , Chemistry , Polymers , ChemistryABSTRACT
Using sustained release tablets of gardenia extract as model drug and DPPH radical scavenging capacity as antioxidant index, the feasibility of using pharmacodynamics index was explored to evaluate sustained release tablets. Applying the established quantifiable method of DPPH radical scavenging to the dissolved liquid of model drug, release profiles and biological effects profiles were drawn, and their correlation was discussed. A good correlation was observed by linear regression and f2 actor, suggesting that the indicator could be used to evaluate sustained release tabletsofextracts of gardenia in which iridoids were mainly involved.
Subject(s)
Antioxidants , Metabolism , Pharmacology , Biphenyl Compounds , Metabolism , Delayed-Action Preparations , Metabolism , Pharmacokinetics , Free Radicals , Metabolism , Gardenia , Chemistry , Kinetics , Linear Models , Oxidation-Reduction , Picrates , Metabolism , Plant Extracts , Metabolism , Pharmacokinetics , TabletsABSTRACT
To establish a UPLC-MS/MS method for the simultaneous determination of geniposide, genipin 1-O-beta-D-gentiobioside and geniposidic acid in rat brains and study the brain pharmacokinetics of the three iridoid glycosides in stroke rat after the oral administration of Xingnaojing. In this experiment, brain samples were precipitated with protein for twice. Acquity BEH C18 column was adopted, with acetonitrile-0.1% formic acid-water as the mobile phase for gradient elution. ESI source was adopted for mass spectra; multiple reaction monitoring (MRM) was conducted to detect negative ions. The time for sample analysis was 3.5 min. the results showed good linear relations among the three iridoid glycosides, with the extraction recovery between 99.6% and 114.3%, good intra- and inter-day precisions and accuracies and stability in line with the requirements. The t1/2 and MRT in the three components were similar in brains of stroke rats. Geniposide and genipin 1-O-beta-D-gentiobioside showed double peaks; where as geniposidic acid showed a single peak. In conclusion, the method is so specific, sensitive, accurate and reliable that it can be used to study the brain pharmacokinetics of Xingnaojing oral preparation.
Subject(s)
Animals , Male , Rats , Brain , Metabolism , Brain Chemistry , Chromatography, High Pressure Liquid , Methods , Drug Stability , Drugs, Chinese Herbal , Chemistry , Pharmacokinetics , Iridoids , Chemistry , Pharmacokinetics , Rats, Sprague-Dawley , Tandem Mass Spectrometry , MethodsABSTRACT
<p><b>OBJECTIVE</b>To study the transdermal permeation and in vivo pharmacokinetics of effective constituent ferulic acid from Ligusticum chuanxiong, in order to establish the in vitro/in vivo correlation in transdermal permeation.</p><p><b>METHOD</b>Franz diffusion cell was adopted in the in vitro transdermal permeation, with CD-1 nude rat abdominal skin as the permeation medium. Linear probes were implanted in CD-1 nude rats. With PBS as perfusate, microdialysis was employed to study the pharmacokinetics. Ferulic acid concentrations in the receptor solution and dialysate were assessed by high performance liquid chromatography (HPLC). The study on correlation between in vitro and in vivo data was conducted by deconvolution methods.</p><p><b>RESULT</b>The transdermal permeation rate of ferulic acid from Ligusticum chuanxiong was (0.094 4 +/- 0.049 4) microg x cm2 x min, with Cmax of ferulic acid being 808.91 microg x L(-1), and Tmax being 183 min after dermal administration. The in vitro/in vivo correlation was 93.61.</p><p><b>CONCLUSION</b>Ferulic acid in extracts from L. chuanxiong can quickly penetrate skins. By using the in vitro/in vivo correlation in transdermal permeation, simple in vitro transdermal permeation method can be adopted to study the changes in its pharmacokinetics.</p>
Subject(s)
Animals , Rats , Administration, Cutaneous , Chromatography, High Pressure Liquid , Coumaric Acids , Pharmacokinetics , Drugs, Chinese Herbal , Pharmacokinetics , In Vitro Techniques , Metabolic Clearance Rate , Permeability , Rats, Nude , Skin , Metabolism , Skin AbsorptionABSTRACT
Xingnaojing (XNJ) is an effective clinical drug used to treat acute stroke. Compared with injection administration, its nasal administration has better brain targeting. Therefore, through nasal administration, XNJ microemulsion could help solve the drug load of compound components of different polarities contained in large-dose and high-concentration traditional Chinese medicines, and reduce irritation to nasal mucosa In this study, the modified volume correction method and the improved rat in situ nasal perfusion model were adopted to compare the nasal absorption of geniposide contained in different XNJ preparations. The results showed that the constant absorption rate of geniposide (GE) in XNJ-D was (2.95 +/- 0.25) x 10(-3) min(-1), whereas the constant absorption rate of GE in XNJ-M was (2.16 +/- 0.21) x 10(-3) min(-1). This indicated that the rat nasal absorption of GE in different XNJ preparations complied with the first-order process and could be considered as passive absorption. GE in XNJ-D was absorbed faster than that in XNJ-M, which provided basis for the development of nasal preparations of XNJ.
Subject(s)
Animals , Male , Rats , Absorption , Administration, Intranasal , Drugs, Chinese Herbal , Pharmacokinetics , Emulsions , Iridoids , Pharmacokinetics , Nose , Metabolism , Rats, Sprague-DawleyABSTRACT
Chonghe gel originated from the Chinese ancient prescription, can be used for the treatment of diabetic foot. This experiment was to study the transdermal absorbability of paeoniflorin and osthole in Chonghe gel . Franz diffusing cells method was adopted for the in vitro model of rat belly skins. Paeoniflorin and osthole in the receiving liquid, skins and gel were determined by HPLC. The receiving liquid were screened, and Chonghe gel and Chonghe ointment were compared by transdermal absorbability. Result showed that ethanol-normal saline (2: 8) solution was the appropriate receiving liquid. The penetration rates of paeoniflorin and osthole were 78.07, 7.08 microg x cm(-2) x h(-1). respectively. In 24 h, the accumulated penetration rates were (31.51 +/- 1.33)%, (12.38 +/- 1.28)%, respectively. The retention rates of paeoniflorin and osthole in skin were (0.92 +/- 0.45)%, (4.81 +/- 1.03) %, respectively. The retention of osthole in skins was a drug reservoir. Transdermal behavior of effective constituents in Chonghe gel was more efficient than that in ointment. In vitro, the transdermal behavior of paeoniflorin in Chonghe gel was close to a Weibull process, while the behavior of osthole was close to Higuchi process.
Subject(s)
Animals , Male , Rats , Chemistry, Pharmaceutical , Drugs, Chinese Herbal , Chemistry , Metabolism , Ethanol , Chemistry , Gels , Rats, Wistar , Skin , Metabolism , Skin AbsorptionABSTRACT
The aim of the present research was to study the transdermal absorbability of ferulic acid and imperatorin in Zhitong cataplasm. Using methanol to extract the effective components, HPLC was established to determine drug content in Zhitong cataplasm. The excised abdominal skin of nude rats was used as the permeation model Utilizing the modified Franz diffusion cell, the suitable receiving solution was elected. The contents of ferulic acid and imperatorin in Zhitong cataplasm were 455.10, 371.66 microg x g(-1), respectively. Taken 20% ethanol- PBS (pH 8) as receiving solution, ferulic acid and imperatorin could be detected maximize, with the steady-state infiltration rates of 1.29, 0.15 microg x h(-1) x cm(-2), respectively. After 24 h, their penetration quantities were 30.03, 3.31 microg x cm(-2), with the penetration rates of 41.45%, 5.60%, respectively. The residual quantities of ferulic acid and imperatorin in skin were 0.69, 2.60 microg x cm(-2), with the retention rates of 0.95%, 4.40%, respectively. The in vitro transdermal behavior of ferulic acid in Zhitong cataplasm was close to a zero-order process, with the stratum corneum playing a rate-limiting role; whereas the percutaneous behavior of imperatorin was closer to Higuchi model, where diffusion played an important role in drugs permeation.
Subject(s)
Animals , Rats , Analgesics , Chemistry , Metabolism , Therapeutic Uses , Coumaric Acids , Metabolism , Therapeutic Uses , Drugs, Chinese Herbal , Chemistry , Metabolism , Therapeutic Uses , Furocoumarins , Metabolism , Therapeutic Uses , Kinetics , Pain , Drug Therapy , Skin AbsorptionABSTRACT
<p><b>OBJECTIVE</b>To study transdermal absorption characteristics of eugenol in compound Nanxing pain-relieving cataplasm, and discuss the effect of gaultherolin on the transdermal absorption of the cataplasm.</p><p><b>METHOD</b>The improved franz diffusing cell was adopted with hairless mice skins as transdermal carriers. The content of eugenol in receptor liquid, skins and cataplasm were analyzed by HPLC and compared with the cataplasm without gaultherolin.</p><p><b>RESULT</b>The penetration rates of eugenol of cataplasms with and without gaultherolin were 13.18 and 9.58 microg x cm(-2) x h(-1), with the retention amount in skins of (185.02 +/- 19.23) and (160.23 +/- 16.54) microg x g(-1) and the retention amount in cataplasms was (1.96 +/- 0.12) and (1.71 +/- 0.15) mg, respectively.</p><p><b>CONCLUSION</b>Eugenol in compound Nanxing pain-relieving cataplasm has good pereutaoeous permeation. Gaultherolin in the cataplasm prescription can promote the absorption of eugenol.</p>