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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 oil∶EL-40∶water 3∶7∶90. Further, puera-rin successfully replaced up to 10% of the emulsifier in submicron emulsion. Eventually, the optimal drug-loading formula was determined as puerarin∶Chuanxiong oil∶EL-40∶water 7∶30∶63∶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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Emulsions , Isoflavones , Particle Size , SolubilityABSTRACT
@#AIM: To quantitatively assess choroid vascular sublayers in women with pre-eclampsia(PE)compared to healthy pregnant women.<p>METHODS: This cross-sectional observational study enrolled 100 subjects, including 40 healthy non-pregnant women, 23 healthy pregnant women, and 37 women with PE. Spectral-domain optical coherence tomography(SD-OCT)was used to measure the choroidal thickness(CT)at the fovea and four additional sites that were 750 μm nasal/temporal or 1 500 μm nasal/temporal to the fovea, and designated as subfoveal choroidal thickness(SFCT), N750, T750, N1500, and T1500, respectively. The thickness of two choroidal vessel layers, Sattler's and Haller's layers, also were quantitatively assessed. <p>RESULTS: No significant differences in mean age or spherical equivalent were observed among the three groups(<i>P</i>=0.240, 0.338). No difference was observed in gestational ages between the healthy pregnant women and PE patients(<i>P</i>=0.783). Significant differences were observed in large choroidal vessel thickness(LCVT), medium choroidal vessel thickness(MCVT), and SFCT at the five sites among the three groups(<i>P</i><0.05). Compared with normal non-pregnant women, a significant increase in LCVT, MCVT, and SFCT was detected at the five sites in healthy pregnant women(<i>P</i><0.05). LCVT and SFCT in PE patients were significantly greater at the five sites compared to normal pregnant women(<i>P</i><0.05), while MCVT was not different(<i>P</i>=0.709).<p>CONCLUSION: This study demonstrated that the vascular sublayer thickness of the choroid was significantly increased in pregnancy and PE. Moreover, the increase in CT thickness might be due to the thickening of Haller's layer. We also observed that the nasal CT increased more than the temporal CT in PE patients and normal pregnant women. We suggest that parasympathetic and sympathetic mediated regulation and nonvascular smooth muscle cells might play a role in the choroidal vascular sublayer thickness variations observed in pregnancy and PE.
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Objective: HPLC fingerprints of Banxia Xiexin Decoction (BXD) was established to analyze the quality value transmitting relationship between medical herbs-decoction pieces-whole decoction of Scutellariae Radix (SR) and Coptidis Rhizoma (CR). Methods: BXD was prepared by the decoction method recorded in Treatise on Febrile Diseases. BXD HPLC fingerprints was established, and the characteristic peaks were analyzed; The transfer rate, the dry extract rate and the similarity of fingerprint were used as indicators to analyze the quality value transmitting relationship between medical herbs-decoction pieces-whole decoction of SR and CR. Results: The transfer rate of baicalin from medical herbs to decoction pieces was between 81.08% and 119.82%; The transfer rate of baicalin from decoction pieces to BXD was between 44.55% and 59.05%; The transfer rate of berberine from medical herbs to decoction pieces was between 66.65% and 97.51%; The transfer rate of berberine from decoction pieces to BXD was between 7.83% and 22.93%; And the dry extract rate of the whole decoction was between 12.99% and 17.21%. The similarity of fingerprints of 15 batches of BXD ranged from 0.978 to 0.999. Conclusion: The quality evaluation method established by the fingerprint is applicable to the quality control of medical herbs-decoction pieces-whole decoction of SR and CR, which provides some reference for the establishment of the quality evaluation method of famous classic formula.
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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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Objective To compare different layers of subfoveal choroidal thickness (SFCT) in normal subjects,healthy pregnant women and patients with pre-eclampsia (PE) using optical coherence tomography (OCT).Methods Twenty-two normal subjects,22 healthy pregnant women and 22 PE patients were included.All patients underwent the examinations including the best corrected visual acuity (BCVA),intraocular pressure,slit lamp,and OCT.The OCT examination was performed to measure SFCT,large choroidal vessel thickness (LCVT),and choroidal capillaries/medium choroidal vessel thickness (MCVT),and the differences between the three groups were compared.Results The differences in age and spherical equivalent among normal subjects,healthy pregnant women and patients with pre-eclampsia were not significant (all P ＞ 0.05).The differences in the gestational weeks between healthy pregnant women and PE patients was not significant (P ＞ 0.05).The mean SFCT of the normal group,healthy pregnant group and PE patient group was (263.45 ± 69.66) μm,(310.55 ±55.63) μm,and (350.41 ± 54.32) μm,accordingly,the mean LCVT of the normal group,healthy pregnant group and PE patient group was (188.25 ± 60.88) μm,(213.27 ±65.31) lμm,and (264.77 ± 56.21) μm,respectively;the mean MCVT of the normal group,healthy pregnant goup and PE patient group was (75.20 ± 33.65) μm,(97.27 ±22.14) μm,(85.64 ± 20.93) μm,respectively,with statistically significance in pairwise comparison (all P ＜ 0.05).The mean SFCT and MCVT of healthy pregnant women was significantly increased than that of the normal subjects (both P ＜ 0.05),but not for LCVT (P ＞ 0.05);whereas SFCT and LCVT of PE patients were significantly increased than those of healthy pregnant women (both P ＜ 0.05),but not for MCVT (P ＞ 0.05).Conclusion The SFCT and LCVT in PE patients are both higher than those in healthy pregnant women,and there is no significant difference in MCVT.
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Objective To evaluate the efficacy and safety of intravitreal injection of conbercept for diabetic macular edema (DME) and the changes of ellipsoid zone (EZ).Methods A retrospective study was conducted in 14 patients (16 eyes) and the clinical data were reviewed and analyzed.All the patients were administrated with conbercept intravitreally,and rechecked 1 month,2 months,3 months after injection including the best corrected visual acuity (BCVA) and optical coherence tomography (OCT).Then a comparison was performed in logMAR BCVA,central foveal thickness (CFT) and macular volume before treatment and 1 month,2 months and 3 months after conbercept injection,as well as the cross-sectional length of incomplete portion in EZ before treatment and 3 months after injection.Results The value of logMAR BCVA before treatment and 1 month,2 months and 3 months after conbercept injection was 0.79 ± 0.08,0.65 ± 0.07,0.56 ± 0.06 and 0.52 ± 0.06,respectively;the average CFT before treatment and 1 month,2 months and 3 months after treatment was (536.44 ±35.87) μm,(385.63 ± 22.60) μm,(336.13 ± 21.91) μm and (292.38 ± 22.54) μm accordingly;the macular volume before treatment and 1 month,2 months and 3 months after treatment was (11.27 ± 0.37) mm3,(10.21 ± 0.22) mm3,(9.69 ± 0.17) mm3 and (9.30 ±0.20) mm3,respectively,with statistically significance in palrwise comparison.Moreover,the cross-sectional length of disrupted EZ before treatment and 3 months after injection was (3116.69 ± 385.55) μm and (1784.88 ± 362.39) μm respectively,and there was statistically significant difference (P ＜ 0.05).Conclusion Intravitreal injection of conbercept to treat DME can alleviate macular edema and restore the disrupted ellipsoid zone.
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<p><b>OBJECTIVE</b>To observe the synergistic effect of beta-elemene Injection (betaI) combined Paclitaxel Injection (PI) on breast cancer MB-468 cells and to study possible mechanisms.</p><p><b>METHODS</b>Breast cancer MB-468 cells were treated with betaI (2.5, 5.0, 10.0, 20.0, 40.0, 80.0, 160.0, 320.0, and 640.0 microg/mL), PI (0.00100, 0.00200, 0.00400, 0.00800, 0.01600, 0.03125, 0.06250, 0.12500, and 0.25000 microg/mL), and betaI combined PI for 24 h and 48 h respectively. Cell proliferation was determined using SRB assay. Cell apoptosis and cell cycle phase distribution were detected using flow cytometry. The post-intervention expressions of cell cycle proteins [cyclin-dependent kinase (CDK1), cyclin-B1, P21(cip1), and P27(kip1)] were detected by Western blot.</p><p><b>RESULTS</b>Beta-elemene or paclitaxel inhibited the growth of MB-468 cell line. The IC50 and IC20 values treated with beta-elemene for 24 h were 34.20 and 52.59 microg/mL and for 48 h were 10.15 and 17.81 microg/mL respectively, while the IC50 values treated with paclitaxel for 24 h and 48 h were 2.449 and 1.698 microg/mL respectively. Beta-elemene (20 and 40 microg/mL respectively) and Paclitaxel (0.016 and 0.008 microg/mL respectively) synergistically inhibited cell proliferation of MB-468 cells, with Q value > 1.15. Beta-elemene alone (52.59 microg/mL) apparently decreased the expression of cyclin-B1 protein. The expression of cyclin-B1 protein in the combined group was also lower than that in the PI group (1.698 microg/mL). The expression of P27(kip1) was up-regulated when compared with that in the betaI group or the PI group.</p><p><b>CONCLUSION</b>Beta-elemene had synergistic effect with Paclitaxel, and its possible mechanism might be correlated with down-regulating the cell cycle protein cyclin-B1 expression and up-regulating the P27(kip1) expression.</p>
Subject(s)
Female , Humans , Antineoplastic Agents, Phytogenic , Pharmacology , Breast Neoplasms , Drug Therapy , Cell Cycle , Cell Cycle Proteins , Metabolism , Cell Line, Tumor , Drug Synergism , Paclitaxel , Pharmacology , Sesquiterpenes , PharmacologyABSTRACT
<p><b>OBJECTIVE</b>To compare the efficacy of second-line EGFR-TKIs followed by third-line pemetrexed with second-line pemetrexed followed by third-line EGFR-TKIs in patients with advanced lung adenocarcinoma.</p><p><b>METHODS</b>From March 2007 to August 2008, 83 patients with advanced lung adenocarcinoma who failed standard first-line chemotherapy were included in this study. The patients who received EGFR-TKIs as second-line therapy followed by third-line pemetrexed were designated as group A (n = 45). The patients who received pemetrexed as second-line therapy followed by third-line EGFR-TKIs were designated as group B (n = 38). PFS and MST were estimated with Kaplan-Meier analysis and the difference between groups were compared with Log-rank test.</p><p><b>RESULTS</b>The progression-free survival (PFS) after second-line therapy in the groups A and B was 8.05 months (95% CI, 5.90 to 10.20) and 4.20 months (95% CI, 3.33 to 5.06), respectively (P = 0.001). The PFS after second-line therapy in smokers and non-smokers was 3.69 months (95% CI, 5.00 to 7.59) and 7.12 months (95% CI, 5.51 to 8.38), respectively (P = 0.007). The PFS of male and female patients was 5.56 months (95% CI, 4.02 to 7.10) and 6.85 months (95% CI, 4.98 to 7.58), respectively (P = 0.279). The PFS after third-line therapy in groups A and B was 6.88 months (95% CI, 5.07 to 8.69) and 7.60 months (95% CI, 5.59 to 9.12) respectively, (P = 0.899). The PFS after third-line therapy in smokers and non-smokers was 4.95 months (95% CI, 2.83 to 7.05) and 8.49 months (95% CI, 6.27 to 10.76), respectively (P = 0.050). The PFS after third-line therapy in male and female patients was 5. 96 months (95% CI, 4.02 to 7.91) amd 8.38 months (95% CI, 5.68 to 11.07), respectively (P = 0.176). The MST in groups A and B was 23.60 months (95% CI, 19.23 to 28.00) and 15.58 months (95% CI, 11.85 to 19.32), respectively (P = 0.021). The MST in smokers and non-smokers was 11.99 months (95% CI, 8.55 to 15.49) and 23.18 months (95% CI, 19.33 to 27.02), respectively (P = 0.001). The MST in male and female patients was 17.40 months (95% CI, 13. 19 to 21.61) and 22.74 months (95% CI, 18.29 to 27.19), respectively (P = 0.111).</p><p><b>CONCLUSIONS</b>Second line EGFR TKIs followed by third line pemetrexed regimen improves the PFS and MST compared with the regimen second line pemetrexed followed by third line EGFR TKIs in patients with advanced lung adenocarcinoma. Smoking status is an independent prognostic factor. Survival is not influenced by gender. Prospective clinical trials are needed to confirm these findings.</p>