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OBJECTIVE： To prepare Syringopicroside solid lipid nanoparticles （SYR-SLN）， and optimize the formula and characterize SYR-SLN. METHODS： SYR-SLN were prepared by emulsion evaporation method. Using entrapment efficiency as index， based on single factor， orthogonal design was adopted to optimize the mass ratio of lecithin-monoglyceride， volume ratio of organ phase to water phase， poloxamer 188 （F68） concentration and drug dosage. The optimal formula technology was established to investigate entrapment efficiency， drug-loading amount， morphology， particle size， Zeta potential， stability， etc. RESULTS： The mass ratio of lecithin-monoglyceride was 3 ∶ 1； the volume ratio of organic phase to water phase was 1 ∶ 2； the concentration of F68 was 0.4％； drug dosage was 10 mg. The optimal formula included that monoglyceride 80 mg， lecithin 240 mg， 0.4％ F68， syringopicroside 10 mg， absolute ethyl alcohol 5 mL， distilled water 10 mL， emulsification temperature at 65℃ and stirring at 600 r/min. Encapsulation efficiency of SYR-SLN was （42.35±0.60）％ （n＝3）； drug-loading amount was （5.33±0.03）％ （n＝3）； SYR-SLN had a spherical morphology and was evenly distributed. The average particle size was （180.30±5.31） nm with Zeta potential of （－41.9±0.8） mV， and the SYR-SLN could maintain stable for 15 days at 4℃. CONCLUSIONS： SYR-SLN is prepared successfully， and the technology is simple with high encapsulation efficiency.
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Excavating and characterizing the dosage forms characteristics of classic Chinese medicine preparations is the basis for the innovation of modern preparations of Chinese medicine. Through the combing statistics of the National Natural Science Foundation of China (NSFC) on the establishment of traditional Chinese medicine preparations, the research literature on Chinese medicine preparations at home and abroad, and the registration of new Chinese medicines in the past ten years, this paper finds that the research projects of classic Chinese medicines have been greatly reduced. The market share of traditional Chinese medicine classics has shrunk year by year. The modern preparation produced in the "preparation of traditional Chinese medicine by western medicine technology" mode dominates the market. However, because of its "degraded" effect, it is less competitive. Therefore, with the wave of classic dosage forms research promoted by national policies, accelerating the study of classical Chinese medicine preparations will not only promote the development of pharmaceutical discipline of traditional Chinese medicine, enhance the classic medical culture literacy, but also promote the protection and inheritance of classic medicine.
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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 optimize the preparation technology of Sinomenine topical paste. METHODS:Using“initial vis-cous force”,“holding viscous force”and“peeling strength”as index,heating and stirring time (A,h),heating temperature (B,℃) and the sequence of adding composition (softening agent,blank matrix and sinomenine)(C) as influential factors,the preparation technology of Sinomenine topical paste was optimized by orthogonal test and verified. At the same time,the content of sinomenine was determined by HPLC method. RESULTS:The optimal preparation technology of Sinomenine topical pasta was as follows as adding blank matrix and sinomenine,and then adding softening agent,heating at 80 ℃,stirring for 1 h. In verification test,RSD of comprehensive score for 3 batches of samples were 2.09%(n=3);average contents of samples were 6.7 mg/g, which was in line with the requirement of ≥6.0 mg/g. CONCLUSIONS:The optimal preparation technology of Sinomenine topical pasta is reasonable,stable and feasible. The paste shows good adhesiveness and is qualified in content.
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Objective To establish an UPLC method for the determination of sinomenine in Sinomenine External Applied Powder. Methods The UPLC method was carried out on a C18 column by using acetonitrile-water-ethylene diamine (50:50:0.25) as mobile phase. The flow rate was 0.2 mL/min; the sample quantity was 2 μL; the detection wavelength was 283 nm. Results The peak time was within 1 min or so. The calibration curve of sinomenine was in the linear range of 34.2–2188.0 ng. Conclusion The method is simple, rapid, stable and reliable, which can be used for the determination of sinomenine in Sinomenine External Applied Powder.
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Objective To study the process of hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion techniques for osthol. Methods The inclusion complex of osthol and HP-β-CD was prepared by unsaturated water solution and freeze-drying technique. Inclusion techniques were selected by screening on quadratic orthogonal rotation combination design method, and the entrapment efficiency was identified by HPLC. Results The optimal technical conditions were as follows:the ratio of HP-β-CD and drug was 4.5∶1;temperature for electric mixer was 35 ℃;the stirring time for thermostatic waterbath was 210 min. Conclusion This method is reasonable and it may have a prosperous future of development and application.
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<p><b>OBJECTIVE</b>To study the intestinal absorption mechanism of traditional Chinese medicine monomer syringopicroside in rats.</p><p><b>METHOD</b>The in situ rat single-pass intestinal perfusion model was established to detect the concentration of syringopicroside by HPLC. The absorption at different intestine segments in rat and the influence of concentration, pH and P-glycoprotein inhibitors of the drug solution on the absorption of syringopicroside were also observed.</p><p><b>RESULT</b>The absorption rate constant (K,) of syringopicroside at duodenum, jejunum, ileum, and colon were 0.00255, 0.00630, 0.00900, 0.00799 min- , respectively; Ka from intestine at syringopicroside concentration of 0.090, 0.180, 0.360 g x L(-1) were 0.00370, 0.00708, 0.00694 min(-1), respectively; and Ka at pH of 7.4, 6.8 and 5.0 were 0.00733, 0.00747, 0.00362 min(-1), respectively. P-glycoprotein inhibitor on the intestinal absorption of syringopicroside showed significant influence (P < 0.05).</p><p><b>CONCLUSION</b>Syringopicroside is well absorbed at the lower small intestine. When the drug concentration is low, the absorption rate constant is low, where as Ka increases at medium and high concentrations; the Ka is low at pH 5.0 and increases at pH 6.8 and pH 7.4. Syringopicroside is proved to be a substrate of P-glycoprotein.</p>
Subject(s)
Animals , Male , Rats , ATP Binding Cassette Transporter, Subfamily B, Member 1 , Physiology , Glycosides , Pharmacokinetics , Hydrogen-Ion Concentration , Intestinal Absorption , Rats, Sprague-DawleyABSTRACT
Objective To observe the effect of recombinant human tumor necrosis factor receptor Fc fusion Protein (rhTNFR:Fc) treatment on IgM-RF,IgG-RF,IgA-RF of patients with rheumatoid arthritis.Methods A randomized,active-comparator controlled,parallel group study were conducted.110 patients were enrolled and were randomly divided to the treatment group,in which patients were treated with twice weekly subcutaneous injection of rhTNFR:Fc (25 mg) (rhTNFR:Fc treatment group,n=55),and the MTX froup,in which MTX (the mean dosage was 15 mg/week) (MTX group,n=55) for 24 weeks.Blood routine,IgM-RF,IgG-RF,IgA-RF,and disease activity score 28 (DAS28) were monitored.Student's t-test was used for statistical analysis.Results The level of IgM-RF decreased significantly in the rhTNFR:Fc treatment group 24 week(29±16) U/ml later.However,the level of IgG-RF(145±20) U/ml,IgA-RF(153±34) U/ml increased significantly in the rhTNFR:Fc group,and the level of IgG-RF (62±14) U/ml,IgA-RF (66-±19) U/ml decreased significantly in the MTX group.Conclusion Although rhTNFR:Fc,is effective in treating the clinical symptoms of RA,it seems to affect RF producing-B cells either directly or indirectly.
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The cyclotides are a family of cyclic "mini" proteins that occur in Violaceae, Rubiaceae and Cucurbitaceae plant families and contain a head-to-tail cyclic backbone and a cystine knot arranged by three disulfide bonds. To study the natural cyclotides of V tianshanica, dried herb was extracted with 50% ethanol, and the concentrated aqueous extract was subjected to a solvent-solvent partitioning between water and hexane, ethyl acetate and n-butanol, separately. The n-butanol extract containing cyclotides was subjected to column chromatography over Sephadex LH-20, eluted with 30% methanol. The subfractions were directly reduced by DTT and analyzed by reverse-phase HPLC. The peaks with different retention times were shown on the profile of RP-HPLC and collected. The cyclotides were speculated based on masses range from 3 000 to 3 500 Da. The purified cyclotides were reduced with DTT, alkylated with iodoacetamide, and then were cleaved with endoproteinase Glu-C, endoproteinase Lys-C and Trypsin, separately. The digested peptides were purified on RP-HPLC and analyzed on MALDI TOF/TOF analyzer. A new cyclotide, cycloviolacin T1 and a reported cyclotide varv E were systemically determined using MALDI TOF/TOF system. So the method for the isolation and characterization of cyclotides was quickly built up in succession.
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Objective To study the effect of escin on proteinuria and renal function of BXSB mice. Methods BXSB mice were divided randomly into group A (control group), B (steroid treatment group), C(steroid combined with high-dose esein treatment group) and D (streroid combined with low-doze escin group). The proteinufia and renal function were detected by albustix and automatic biochemistry analyzer after a month's treatment. Results Group C reduced the level of proteinuria and parameters of renal function (BUN and Cr) significantly when compared with other three groups (P<0.05). Conclusion Escin can reduce the level of proteinuria and protect renal function of BXSB mice.
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AIM: To investigate the chromatographic fingerprints of Guangyanling Injection(Syringa oblata Lindl) by HPLC. METHODS: The separation was performed on a Water SunFire~ TM C_ 18 4.6 mm?250 mm 5 ?m analytical column with the mobile phase consisting of methanol-water as gradient eluent at the flow rate of 1 mL/min. The UV detection was set at 280 nm. RESULTS: The HPLC-UV fingerprints of Guangyanling Injection was obtained with perfect isolation. CONCLUSION: The fingerprints could be used for the control of Guangyanling Injection.
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AIM: A quantitative method was developed for the determination of deoxyschizandrin and schisandrin B in Liganlong Tablet(Fructus Schisandrae Chinensis,Radix Astragali,Radix Angelicae Sinensis,Radix et Rhizoma seucaulis Acanthopanacis Senticosi,etc.) by HPLC. METHODS: The chromatographic conditions included column Symmetry shield~(TM) RP_(18) 5 ?m,3.9 mm?150 mm,mobile phase: methanol-tetrahydrofuran-water(64∶4∶32),flow rate at 1 mL/min,wavelength at 220 nm. RESULTS: The number of theoretical plates is 3555.5.The Deoxyschizandrin liner is 0.068～0.340 ?g (r=0.999 9) and the Schisandrin liner range is 0.06～0.30 ?g (r=0.999 8).The resolutions are 5.09,1.12,respectively. CONCLUSION: The method is sensitive,quick and accurate for the determination of deoxyschizandrin and schisandrin B in Liganlong Tablet.