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Exploiting cells as vehicles combined with nanoparticles combined with therapy has attracted increasing attention in the world recently. Red blood cells, leukocytes and stem cells have been used for tumor immunotherapy, tissue regeneration and inflammatory disorders, and it is known that neutrophils can accumulate in brain lesions in many brain diseases including depression. -Acetyl Pro-Gly-Pro (PGP) peptide shows high specific binding affinity to neutrophils through the CXCR2 receptor. In this study, PGP was used to modify baicalein-loaded solid lipid nanoparticles (PGP-SLNs) to facilitate binding to neutrophils . Brain-targeted delivery to the basolateral amygdala (BLA) was demonstrated by enhanced concentration of baicalein in the BLA. An enhanced anti-depressant effect was observed and The mechanism involved inhibition of apoptosis and a decrease in lactate dehydrogenase release. Behavioral evaluation carried out with rats demonstrated that anti-depression outcomes were achieved. The results indicate that PGP-SLNs decrease immobility time, increase swimming time and climbing time and attenuate locomotion in olfactory-bulbectomized (OB) rats. In conclusion, PGP modification is a strategy for targeting the brain with a cell-nanoparticle delivery system for depression therapy.
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OBJECTIVE:To promote quality control management of TCM decoction piece in secondary and tertiary TCM hospitals, integrated traditional Chinese and western medicine hospitals, and to guarantee the safety of drug use in patients. METHODS:According to 2016 TCM Decoction Piece Management Special Test Score of National Medical Institution made by quality control center of TCM in Shanghai,TCM decoction piece management of 22 secondary and tertiary TCM hospitals, integrated traditional Chinese and western medicine hospitals (14 and 8,respectively) in Shanghai were scored (the total score is 100),summarized and analyzed by on-site inspection from 7 modules,such as pharmaceutical management,acceptance and storage maintenance, dispensing, decocting or outside processing, prescription standardization and prescription review. The suggestions were put forward. RESULTS & CONCLUSIONS:Average score of 22 hospitals was 91.97, and hospitals with excellent(the secondary and tertiary hospitals are 11 and 5,respectively)and good(the secondary and tertiary hospitals are 2 and 3,respectively) score accounted for 95.45％. Those hospitals obtained good score in respect of pharmaceutical management (the total score is 12,scored 11.73). But in many hospitals,there are shortcomings in acceptance and storage maintenance,dispensing, outside processing,prescription standardization and prescription review management. It is suggested to control TCM decoction piece purchase and acceptance,strengthen TCM decoction piece maintenance and storage,enhance TCM decoction piece batch number management, effectively monitor TCM decoction piece outside processing, improve prescription standardization, implement TCM decoction piece prescription comment and standardize prescription name of TCM decoction piece so as to improve total quality of TCM decoction piece management.
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Objective To explore the mechanism of Xiaoying decoction on experimental autoimmune thyroiditis (EAT) rats in view of regulatory T cells and Th17 cells.Methods SD rats were divided into five groups,normal control group,model control group,tripterygium glycoside group,Xiaoying decoction low and high dose groups.Except for normal control group,the other groups were established the model of EAT.Rats in the Xiaoying decoction low,and high dose groups were given Xiaoying decoction of 17.24 and 68.95 g·kg-1;rats in the tripterygium glycoside group were given tripterygium glycoside 6.25 mg·kg-1.The serum free triiodothyronine(FT3),free thyrocyte(FT4) and thyroglobulin antibody were detected by RIA method.Thyrocyte morphology was observed under optical microscope.The expression levels of Foxp3 mRNA and IL-17 mRNA were detected by real-time PCR.The changes of Treg cells and Th17 cells were analyzed by flow cytometry.Results Compared with the normal control group,FT3,FT4 and TgAb were increased in the model control group (P ＜0.01,P ＜0.01,P ＜0.05).Compared with the model control group,FT3,FT4 and TgAb were decreased in tripterygium glycoside group and Xiaoying decoction high dose group (P ＜ 0.05).The infiltration score in the normal control group,model control group,tripterygium glycoside group,Xiaoying decoction low and high dose groups were 0,4,4,3.5,2.Compared with model control group,the infiltration was improved (P ＜0.01).Foxp3 mRNA expression was decreased while IL-17 mRNA increased in the model control group as compared with the normal control group(P ＜ 0.01).In contrast,the expression of Foxp3 mRNA was increased and IL-17 mRNA expression was decreased in Xiaoying decoction low and high dose groups,tripterygium glycoside group as compared with the model control group (P ＜0.05).Compared with the normal control group,rats in the model control group had fewer Treg cells and more Th17 cells (P ＜0.01).Compared with the model control group,the percentage of Treg cells was elevated and Th17 cells was reduced in tripterygium glycoside group and Xiaoying decoction high dose groups (P ＜ 0.01).Conclusion The therapeutic mechanism of Xiaoying decoction on EAT rats may be related to changing the percentage of regulatory T cells and Th17 cells with up-regulating the expression of Foxp3 mRNA and down-regulating the expression of IL17mRNA.
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OBJECTIVE:To explore the ideas for the prescription comment of TCM injections,and provide reference for clini-cal rational use. METHODS:Totally 9 457 prescriptions in PIVAS and 400 hospitalized medical records in our hospital in 2015 were collected. The prescriptions and hospitalized medical records which contained TCM injections were retrospectively commented in aspects of indications,usage and dosage,drug combination,solvent selection and repeat medication,and analysis of typical case. RESULTS:In 2015,there were 2 544 prescriptions(26.90%)in PIVAS and 195 medical records(48.75%)that used TCM injections;the irrational use was mainly inappropriate solvent selection(50.70%),inappropriate usage and dosage(27.00%),inap-propriate indications (10.33%),inappropriate combination therapy (7.51%) and repeat medication (4.46%). CONCLUSIONS:Prescription of TCM injections should be commented with the medical records and individual analyzed;in terms of unreasonable prescriptions and medical records TCM clinical pharmacists should actively intervene unreasonable prescriptions by the bed.
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OBJECTIVE:To provide reference for the implementation of Quality Management Guidance of TCM Trust-agent Decocting in Medical Institutions in Shanghai. METHODS:Stratified random sampling method was adopted for the questionnaire of TCM trust-agent decocting in 13 medical and health institutions in the suburb of Shanghai. RESULTS:A total of 13 question-naires were sent out and 13 valid questionnaires were received with the effective rate of 100%. In the 13 medical and health institu-tions,12 medical and health institutions partially or fully adopted trust-agent decocting,and the trust-agent decocting in the 12 med-ical and health institutions accounted for 92.3% in all trust-agent decocting;the 12 medical and health institutions with TCM trust-agent decocting service for patients included 9 pharmaceutical factories and 3 pharmacies;label related problems (including name error,oral and topical label error and stickers unclear) and leakage were the main quality problems,accounting for 33.0%and 31.0%,respectively;83.3% of the medical and health institutions didn’t establish the file of the quality control for TCM trust-agent decocting;decocting process was the most important factor that affects the quality. CONCLUSIONS:Implementing a re-gional Quality Management Guidance of TCM Trust-agent Decocting in Medical Institutions in Shanghai and establishing a system that drug administration,industry associations and medical and health institutions are participated in have great significance to pro-mote the healthy development of TCM trust-agent decocting service and ensure patients’medication safety.
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Objective To establish HPLC method to determine the content and the recovery of rosmarinic acid in common selfheal fruit-spike effective component of colon target tablets.Methods HPLC column was Diamonsil C18,200 mm×4.6 mm,5μm, wavelength was 330 nm, mobile phase methanol was 0.1% formic acid aqueous solution (45:55), flow rate was 1.0 ml/min, and the sample size was 20μl.Results The fine linear relation was shown at the rosmarinic acid methanol concentration of 2.99-119.6μg/ml, with 72 h in stable state. The method has fine precision, the spotting recovery was 95%-105%, andRSD was less than 2%. Conclusion The method has high specificity, meeting the demands for content determination.
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Chinese medicine dispensing granule is made by qualified decoction pieces with modern pharmaceutical technology, which has the characteristics of flexible prescription, flexible dose, fast onset and easy absorption. However, there is great controversy in whether it has curative effects, also there are problems with non-conformant standard of prescription, high price, and incomplete varieties. In this case, advantages and disadvantages of present Chinese medicine dispensing granule are analyzed and discussed thoroughly in this article so that we can provide references for the benign development of Chinese medicine dispensing granule industry.
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The present work is to investigate the correlation between physical properties and deformation behaviors of tablet excipients, and rank them according to their plastic performances during compaction. The excipients selected were compacted using Korsch XP1 after measuring their physical properties where the compression parameters for evaluating deformation behaviors were Heckle equation, compression work and elastic stretch in die. The correlations between compaction descriptors and physical parameters were analyzed by canonical correlation analysis, and factor analysis was simultaneously employed to synthetically assess deformation behaviors for all our samples. The canonical variables show that true density (Pa) correlated negatively with plastic coefficient (PL) and positively with yield pressure (YP); compression degree (Cp) correlated negatively with fast elastic stretch (FES) as well as YP and positively with PL. When factor scores were used in combination with original data, the plasticity of our samples was sorted and ranked as high (-0.56 < F' < 0.21), intermediate (-0.16 < F' < 0.36), or low (0.38 < F' < 0.84), which are in accord with plasticity rankings previously reported in literature. This study indicates factor analysis can be an approach to evaluate deformation behaviors of pharmaceutical powders.
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Objective To evaluate and improve the geometrical accuracy of the magnetic resonance imaging used for gamma knife radiosurgery localization. Methods Four common MRI scan programs were used in this study. The images were transferred to the Gamma Plan treatment planning system.Deviations between stereotactic coordinates based on MR images and real geometrical positions given by the construction of the phantom insert were evaluated for each study.The deviations were further investigated as a function of the spatial position of measured points in the investigated volume.Results The geometrical coordinate errors for axial and coronal images of the selected scan programs were all less than 1 mm.Optimal imaging procedure in terms of geometrical accuracy was observed using spin echo T1 and 3D FSPGR MRI sequences in the unit.Statistically significant differences were found in axial images amongSE T1,FSE T2,FRFSE Pd,FSPGR 3D sequences (F=1497.51,1873.63,2.87,3.00,P ＜0.05).The error increased along with the increase of the distance between node point and centricity.Conclusions The geometrical coordinate errors is related with the imaging program in M(il)l. Proper imaging programs and parameters should be selected according to the imageology character of patients' lesions when the radiosurgery is performed.
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<p><b>OBJECTIVE</b>To observe the pharmacokinetic effect of Shaoyao Gancao compound on rats using different decocting methods, and to pharmacokinetically detect the the compatibility of the component compounds of the Shaoyao Gancao compound from the pharmacokinetic viewpoint.</p><p><b>METHOD</b>Based on the established HPLC analytical method of plasma effective constituents, rats were orally administered with a single or mixed decoction of Shaoyao and Gancao. Blood at different times after administering these decoctions were collected, and then variance analysis was made for pharmacokinetic parameters.</p><p><b>RESULT</b>The results of all six rats indicated that the absorption of the mixed decoction of Shaoyao and Gancao was greater than that of the single decoction. While, the absorption of the characteristic peaks at the retention time of 5.2, 11.0, 12.0, 14.6 min had statistical significance.</p><p><b>CONCLUSION</b>Shaoyao Gancao compound was proved better than that of the single decoction from the pharmacokinetic viewpoint.</p>
Subject(s)
Animals , Male , Rats , Administration, Oral , Biological Availability , Chromatography, High Pressure Liquid , Drug Compounding , Methods , Drugs, Chinese Herbal , Pharmacokinetics , Paeonia , Chemistry , Plasma , Chemistry , Rats, Sprague-DawleyABSTRACT
<p><b>OBJECTIVE</b>To establish an accurate and simple qualitative analytical method in vivo in the study on HPLC characteristic fingerprint of active components of dachuanxiong fang in plasma and cerebrospinal fluid, in order to lay a foundation for studies on components found in plasma and cerebrospinal fluid and provide basis for compatible regularity of initiators.</p><p><b>METHOD</b>HPLC characteristic fingerprint of active components of dachuanxiong fang in plasma and cerebrospinal fluid was established.</p><p><b>RESULT</b>The similarity of fingerprints of all of six batches of samples was above 0.85, RSD of their relative retention times in common peaks was less than 2. 0%.</p><p><b>CONCLUSION</b>The fingerprints of active components of dachuanxiong fang in plasma and cerebrospinal fluid were stable and accurate that they can be used in qualitative analysis on in vivo components.</p>
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Animals , Male , Rats , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Metabolism , Medicine, Chinese Traditional , Plant Extracts , Blood , Cerebrospinal Fluid , Quality Control , Rats, Sprague-DawleyABSTRACT
<p><b>OBJECTIVE</b>To characterize the flowability of traditional Chinese medicine (TCM) powders by using appropriate methods.</p><p><b>METHOD</b>With highly flowable direct compression excipients and Chinese traditional medicine powder as raw materials, the flowability of material powders is determined by the Carr method and the Jenike method.</p><p><b>RESULT</b>The Carr method and the Jenike method for the determination of the flowability of Chinese herb extract powder and direct-pressing excipients have no obvious difference. But the flowability of Chinese herb extract powder is not as good as direct compression excipients.</p><p><b>CONCLUSION</b>From the characterization results of both methods, we can find that the Carr method better reflects the actual flowability of TCM extracts, while the Jenike method can be used for guiding the design of the hopper device.</p>
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Medicine, Chinese Traditional , Particle Size , Powders , ChemistryABSTRACT
The extracellular matrix metalloproteinase inducer (EMMPRIN) has been known to play a key regulatory role in pathological angiogenesis. A elevated activation of vascular endothelial growth factor (VEGF) following radiation injury has been shown to mediate blood-brain barrier (BBB) breakdown. However, the roles of EMMPRIN and VEGF in radiation-induced brain injury after gamma knife surgery (GKS) are not clearly understood. In this study, we investigated EMMPRIN changes in a rat model of radiation injury following GKS and examined potential associations between EMMPRIN and VEGF expression. Adult male rats were subjected to cerebral radiation injury by GKS under anesthesia. We found that EMMPRIN and VEGF expression were markedly upregulated in the target area at 8-12 weeks after GKS compared with the control group by western blot, immunohistochemistry, and RT-PCR analysis. Immunofluorescent double staining demonstrated that EMMPRIN signals colocalized with caspase-3 and VEGF-positive cells. Our data also demonstrated that increased EMMPRIN expression was correlated with increased VEGF levels in a temporal manner. This is the first study to show that EMMPRIN and VEGF may play a role in radiation injuries of the central nervous system after GKS.
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Animals , Male , Rats , Basigin/metabolism , Brain/blood supply , Brain Injuries/metabolism , Caspase 3/metabolism , Gamma Rays/adverse effects , Immunohistochemistry , Microscopy, Electron, Transmission , Parietal Lobe/metabolism , Radiation Injuries, Experimental/metabolism , Radiosurgery/adverse effects , Rats, Wistar , Time Factors , Vascular Endothelial Growth Factor A/metabolismABSTRACT
The pharmacokinetics of a long-circulating PEGylated Radix Ophiopogonis polysaccharide (ROP) was investigated in rats following i.v. or s.c. administration at three dose levels (9, 20, 50 mg x kg(-1)). A moderate coupling reaction between the hydroxyl-activated ROP and the amino-terminated mPEG was chosen to produce PEGylate ROP. The grafting degree of the prepared conjugate was 1.03, and the molecular mass of mPEG used was 20 kDa. High-performance gel permeation chromatorgraphy with fluorescein isothiocyanate prelabeling was established to determine levels of the conjugate in plasma. The results showed that the elimination half-life of the conjugate following s.c. administration was basically identical to that after iv administration. An accurate linear correlation was observed between administration doses and areas under the curve of plasma conjugate level vs. time profile, regardless of the administration route. The absolute bioavailability of the conjugate following sc administration was approximately 56%, and the mean in vivo residence time was 52.1 h, increased 2.4 times compared to those of iv administration. In general, linear pharmacokinetics was observed for the conjugate within the dose range studied, and sc should be a promising administration route for the conjugate.
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<p><b>OBJECTIVE</b>To prepare sustained-release pellets of active components from Ligusticun chuanxiong by coating in the fluid-bed.</p><p><b>METHOD</b>The fast-release pellets were prepared by the extrusion-spheronization process. The coating formulation was optimized with the release of ferulic acid as criteria. The micromeritic properties and drug dissolution behaviors of the prepared pellets were evaluated.</p><p><b>RESULT</b>The pellets presented perfect sphericity. The obviously sustained-release effects were shown in 12 h. The coating weight gain was the major factor impacting drug release.</p><p><b>CONCLUSION</b>The coating pellets show the obviously sustained-release effects.</p>
Subject(s)
Coumaric Acids , Delayed-Action Preparations , Ligusticum , Chemistry , Technology, PharmaceuticalABSTRACT
<p><b>OBJECTIVE</b>To investigate the substance basis of Gastrodia elata in Dachuanxiong Fang (DF) by serum pharmacochemistry, so that the quality of DF as well as its preparations can be effectively and systemically controlled.</p><p><b>METHOD</b>The chromatographic peaks of blank plasma, blank cerebrospinal fluid, drug-contained plasma and cerebrospinal fluid were compared by HPLC fingerprints. The absorbed ingredients of the active parts extracted from G. elata were structurally identified by HPLC-DAD-MS".</p><p><b>RESULT</b>Two components, which were definitely detectable in rat plasma following the oral administration of the active parts from G. elata, were identified as gastrodin and parishin. In rat cerebrospinal fluid, there are, however, no obvious peaks that belong to the ingredients from G. elata.</p><p><b>CONCLUSION</b>Research on in vivo transmigration of ingredients from G. elata is favorable to the clarification of its active substance basis.</p>
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Animals , Male , Rats , Administration, Oral , Chromatography, High Pressure Liquid , Drugs, Chinese Herbal , Pharmacokinetics , Gastrodia , Chemistry , Rats, Sprague-DawleyABSTRACT
<p><b>OBJECTIVE</b>To study the correlation of dry granulation with Chinese extract powder physical properties and dry granulating process parameters to find out the main factors affecting the granulation progress.</p><p><b>METHOD</b>The correlation with the physical properties including angle of repose, compression degree, cohesion, water content, feeding speed, wheel speed and wheel pressure with the yield of grain was investigated by multiple regression analysis.</p><p><b>RESULT</b>The results showed that compression degree, water content, feeding speed and wheel pressure was positively correlated with the yield of grain in measured range. The angle of repose, cohesion, wheel speed was negative correlated with the yield of grain in measured range.</p><p><b>CONCLUSION</b>Dry granulating was highly influenced by the physical properties of herbal extracts and the parameters of dry granulating process. The greater impact on grain dry method are compression, cohesion and wheel speed.</p>
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Drugs, Chinese Herbal , Chemistry , Powders , ChemistryABSTRACT
The paper is to report the observation of pharmacokinetic changes of the characteristic ingredients in the combinations of different-dose herbs of Shaoyao-Gancao decoction. After the establishment of HPLC analytical method of plasma effective constituents, rats were orally administered with different-dose herbs of Shaoyao-Gancao decoction. Blood samples at different times after administering these decoctions were collected, and then were analyzed by HPLC fingerprints technology. Pharmacokinetic parameters of characteristic peaks were analyzed by SPSS 15.0 software and DAS 2.0. At last, we looked for the correlation of those pharmacokinetic parameters and the dosage of Gancao. The best dose of Shaoyao-Gancao decoction was at the ratio of 4 to 4, which was consistent with the dose commonly used in ancient times. The absorption of characteristic peaks from Shaoyao-Gancao decoction was related with the dosage of Gancao, and there existed interaction between each characteristic ingredients. There existed the right dose-ratio of Shaoyao and Gancao to get the best effect. The absorptions of effective constitutents were mutual waxing and waning in order to increase biological effects together. It's demonstrated the compatibility connotation at a right dose-ratio of Shaoyao-Gancao decoction through the angle of pharmacokinetics.
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<p><b>OBJECTIVE</b>To study the changes of the in vitro and in vivo material base of Shaoyao Gancao decoction (SGD) based on HPLC-DAD-ESI-MS, and confirm the migrational constituents in plasma.</p><p><b>METHOD</b>Kormasil C18, (4.6 mm x 250 mm, 5 microm with protection column) was employed; acetonitrile and 0.5% acetic acid/water was used as mobile phase for gradient elution, flow rate was set at 0.8 mL x m min(-1), column temperature was 25 degrees C, and methanol was used to remove the protein. A LCQdeca mass spectrometer system equipped with an electrospray ionization iontrap source was used as the detector and operated in the positive ion mode. Ions was scanned from the m/z 100 to m/z 1000, and characteristic ion were secondary schizolysised to obtain data of second order MS.</p><p><b>RESULT</b>The main constitutes of SGD were peoniflorin, Catechin-5-O-glucoside, albiflorin, liquiritin and glycyrrhizic acid etc, and glucosides were found in the plasma samples of rats administered with SGD, which were glucuronide conjunctions of liquiritigenin and isoliquiritigenin.</p><p><b>CONCLUSION</b>Liquid chromatography-mass spectrometry technology provides a convenient and high speed method to analyze the migrational constituents of plasma of rats administered with SGD, therefore, it has a good value in studies on the changes in the material base of traditional Chinese medicine (TCM).</p>
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Animals , Male , Rats , Blood Chemical Analysis , Chromatography, High Pressure Liquid , Methods , Drugs, Chinese Herbal , Pharmacokinetics , Rats, Sprague-Dawley , Spectrometry, Mass, Electrospray Ionization , MethodsABSTRACT
<p><b>OBJECTIVE</b>To investigate suitable oral absorption enhancer (s) for Ophiopogon japonicas polysaccharides (OJP) and provide bases of utilizing the absorption enhancer to realize the oral administration of OJP.</p><p><b>METHOD</b>The absorption enhancement effects and cytotoxicity of clove oil, peppermint oil, borneol, Sanqi saponins, Maidong saponins, Ginseng saponin Rg1, Sanqi saponin R1 and sodium caprate (SC) were evaluated via Caco-2 cell culture model. The absorption of OJP from rat intestinal segments and the absorption enhancement effect of SC were investigated by in situ experiments of rat intestinal segments.</p><p><b>RESULT</b>SC was an effective and safe absorption enhancer. However, the absorption enhancement effects of clove oil, peppermint oil and Maidong saponins were highly correlated with their cytotoxicity. OJP alone was poorly absorbed from all the rat intestinal segments. It was rapidly absorbed when co-administered with SC, and the absorption increase was significant and the best absorption enhancing site of SC for OJP was colon.</p><p><b>CONCLUSION</b>The absorption enhancement effects of absorption enhancers are often correlated with their cytotoxicity. Co-administrating a powerful and safe absorption enhancer is an effective and valuable method of enhancing oral absorption of OJP.</p>