Preparation of Dendritic Mesoporous Silica Nanomaterials Loaded with Toosendanin-Fumaracetin and its Anti-Peripheral Pain Study
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Objective: A novel dendritic mesoporous silica nanomaterials (DMSN) was prepared and the traditional Chinese Medicine Component "Toosendanin-Tetrahydropalmatine" was loaded into DMSN in order to improve the solubility of Tetrahydropalmatine B, reduce the toxicity of Toosendanin, and enhance the anti-peripheral pain effect of the traditional. Chinese Medicine "Toosendanin-Tetrahydropalmatine" through preliminary pharmacodynamics study. Methods: DMSN were prepared using the sol-gel method and characterized by scanning electron microscope (SEM) and Fourier Transform Infrared Spectrometer (FT-IR). The preliminary study of the anti-peripheral pain pharmacodynamics of the drug-loaded system in mice was evaluated by the hot plate method. Results: The prepared DMSN has an excellent spherical shape in SEM, the size distribution of the DMSN is about 200nm, the size distribution is uniform, and the dispersion is good. The infrared results showed that the synthesized DMSN had organic functional groups and chemical structures. Compared with the control group, the pain threshold of DMSN loaded with the Toosendanin-tetrahydropalmatine group was prolonged by 45 seconds. Conclusion: The synthesized DMSN loaded with Toosendanin and Tetrahydropalmatine could release stably and continuously and had the effect of extending the pain threshold of mice. Therefore, DMSN drug delivery system has potential value in improving the bioabsorption of dangerous drugs and enhancing the bioavailability of poorly soluble drugs.Keywords:
Tetrahydropalmatine
Pharmacodynamics
Nanomaterials
Objective:The Absorptive characteristics of Tetrahydropalatine on rat intestinal and the influence of match-pair of Yuanhu-baizhi on rat intestinal Absorption of Tetrahydropalmatine was investigated,and the principle of match-pair of Yuan hu-baizhi was studied.Methods:A rat intestinal model in vitro was used to investigate the influence of different portions of intestines and different concentrations of Tetrahydropalmatine on rat intestinal Absorption ofTetrahydropalmatine;The Absorption of Tetrahydropalmatine after matching the active principle of baizhi with different proportion;Tetrahydropalmatine was used as the index,which is the principal active component in the Corydalis alkaloid,and its concentration in intestinal serosal fluid was detected by high-performance liquid chromatography(HPLC).Results:The intestinal Absorption of Tetrahydropalmatine in the Corydalis alkaloid increased significantly with the optimal ration among match-pair of Yuanhu-baizhi.Conclusions:It was confirmed that the match-pair of Yuanhu-baizhi is rational from the angle of the intestinal Absorption.
Tetrahydropalmatine
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Since the date that nanomaterial been developed, there’re numerous related explorations and application in biomedical field. Upon all kind of the nanomaterials, magnetic nanoparticles and gold nanomaterials are more extensively researched. Magnetic nanoparticles can be used in magnetic targeting, magnetic resonance imaging (MRI), etc., whereas gold nanomaterials can be applied in photothermal therapy because of the surface plasma resonance character of gold nanomaterials. Furthermore, the application of nanomaterials as anti-cancer drug carrier has been widely developed. For example, there’re many study about mesoporous silica nanomaterial, which can be used as drug carrier. Supposing that there’re stimuli-responsive caps attached on the mesoporous silica nanomaterial surface which can be the switch of the drug, we may attain the goal to control anti-cancer drug release. In addition, we may be able to use less amount of the drug to reach the effective cancer therapy. In this study, we take iron oxide coated gold nanoshell (Fe3O4@Au) as the core of the nanocarrier, which can be applied to magnetic targeting, MRI, and thermotherapy. Moreover, coating mesoporous silica shell on Fe3O4@Au core may render us to load doxorubicin (an anti-cancer drug) into the pores of mesoporous silica shell. At last, we use stimuli-responsive double stranded deoxyribonucleic acid (dsDNA) as the caps to cover the pore which loaded doxorubicin. Owing to the stimuli-responsive caps, we are able to use NIR laser light to trigger doxorubicin release, and achieve the purpose of controlling drug release.
Nanomaterials
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Objective: To establish a method for determination of tetrahydropalmatine in Anwei tablets. Methods: tetrahydropalmatine in Anwei Tablets was extracted by chloroform and determined by dual wavelength TLC scanning (λ s=275nm,λ R=340nm).Results: The average recovery was 95%.17%, RSD was 2.50% (n=5). The contents of tetrahydropalmatine in three batches were 7.45,7.17 and 7.90μg/tablet, respectively.Conclusions: The method is stable and feasible.
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A new method for the determination of tetrahydropalmatine using flow injection chemiluminescence was studied. It is based on the chemiluminscence reaction of tetrahydropalmatine-KMnO4-Na2S2O4. The main factors which affect the determination were investigated. Under optimum conditions, the linear range for the determination of tetrahydropalmatine was 1 × 10-8~8 × 10-6 g/mL and the determination limit was 3. 2 × 10-9 g/mL. The method has been applied to the determination of tetrahydropalmatine in Rotundine. tablets and their reults are in good agreement with those obtained by classical method.
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Objective To establish an assay method of tetrahydropalmatine in Rhizoma Corydalis.Methods By RP-HPLC, using a C 18 column with acetonitrile-2% acetic acid glacial(adjusted pH to 5.0 with triethylamine)(25∶75)as mobilephase and detected at 282 nm.Results The calibration curve of tetrahydropalmatine was linear from 1.004 μg/mL to 50.20 μg/mL with r=0.999 9.The average recovery was 98.63 % with RSD 1.95%.Conclusion This method was proved to be accurate and quick, and can be selected to control the quality of the medicinal materials.
Tetrahydropalmatine
Triethylamine
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OBJECTIVE To study the purification of tetrahydropalmatine in extracts of vinegar-prepared Corydalis yanhusuo.METHODS A method for the determination of tetrahydropalmatine was established at first.The transfer rate of tetrahydropalmatine,dry extracts yield and the content of tetrahydropalmatine in dry extracts yield were used as indics to evaluate the lime milk-sulfuric acid method,water extract-alcohol extraction method,D101 macroporous resin method and 732 cation exchange resin method.RESULTS The 732 cation exchange resin method was more effective than the other three methods,and the transfer rate of tetrahydropalmatine could reach at least 70%.The dry extracts yield could be controlled under 2.5%,and the content of tetrahydropalmatine in dry extracts yield was 1.2%,which was 30 times the content of the herb.CONCLUTION Among the four methods,the 732 cation exchange resin method can reach the best result.In addition,the purification process is stable and feasible.
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Tetrahydropalmatine
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Tetrahydropalmatine is a kind of food additive with useful medicine value (dietary supplement), the tetrahydropalmatine synthetic process by using high performance liquid chromatography method was researched in the study, the experiments show that the dissolution rate of active ingredients in the tetrahydropalmatine water extract synthesized by this method has increased and the amount of active ingredient has greatly improved.
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Objective To establish a method for the determination of tetrahydropalmatine in Yanjishen capsules. Methods To determine the content of tetrahydropalmatine in Yanjishen capsules by TLC-scanning. Results The linear range of concentration was 2.0～12.0 μg, r=0.999 1. The average recovery was 99.12%(n=5), RSD was 2.4%. Conclusions The method is rapid, accurate and can be used for quality control of Yanjishen capsules.
Tetrahydropalmatine
Linear relationship
Content determination
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OBJECTIVE To establish the quality standards of L-tetrahydropalmatine dispersible tablets. METHODS L-tetrahydropalmatine in L-tetrahydropalmatine dispersible tablets were identified by TLC and HPLC,using HPLC method for the content determination of L-tetrahydropalmatine dispersible tablets. RESULTS L-tetrahydropalmatine could be identified qualitatively,the appearance,dissolution rate,dispersible uniformity and content uniformity of dispersible tablets were in line with quality standards. The Linear relationship of L-tetrahydropalmatine was good in the range of 0. 2032-2. 0320 μg( r = 0. 9999). The average recovery was99. 30% with a RSD of 1. 77%. The average content of 3 batches were 98. 26%,99. 27% and 99. 88%,respectively. CONCLUSION The method is simple,accurate and specific. It can be used for the quality control of products.
Tetrahydropalmatine
Linear relationship
Content determination
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