Aim To develop a reverse phase HPLC method for the determination of aloperine, an alkaloid that is newly extracted from Sophora alopecuraides and has shown wide pharmacological effects including antibacterial and...Aim To develop a reverse phase HPLC method for the determination of aloperine, an alkaloid that is newly extracted from Sophora alopecuraides and has shown wide pharmacological effects including antibacterial and antiinflammatory actions. Methods The samples were analyzed on a ODS column with methanol water triethylamine (3∶97∶0 1 V/V) as a mobile phase. The flow rate was 1 0 mL·min -1 , and UV detection wavelength 205 nm. Results Linear regression equation was A=1 6920C+1 7455 (r 2=0 9999, n =5) in concentratins ranging from 20 to 120 μg·mL -1 . The recoveries were 101 2±1 46 % at 80 μg·mL -1 , 100 5±0 75% at 100 μg·mL -1 , and 100 7±1 10% at 120 μg·mL -1 , respectively, and the precisions of aloperine within or between run were from 0 80% to 1 98% ( n =5). The relative contents of aloperine in three lots of tablets were 101 59±1 38%, 98 46±0 23%, and 99 41±1 09% ( n =3). Conclusion The newly developed reverse phase HPLC method is simple and useful for daily assay of aloperine tablets and can overcome the interference from excipient and other alkaloids in titration and UV detection.展开更多
AIM: To evaluate the possibility of using insulin as a carrier for carcinoma-targeted therapy mediated by receptor, and to investigate the expression of insulin receptor in human hepatocellular carcinoma and the recep...AIM: To evaluate the possibility of using insulin as a carrier for carcinoma-targeted therapy mediated by receptor, and to investigate the expression of insulin receptor in human hepatocellular carcinoma and the receptor binding characteristics of insulin-IUdR (iododeoxyuridine).METHODS: IUdR was covalently conjugated to insulin.Receptor binding assays of 125Ⅰ-insulin to human hepatocellular carcinoma and its adjacent tissue were performed.Competitive displacements of 125Ⅰ-insulin by insulin and insulin-IUdR to bind to insulin receptor were respectively carried out. Statistical comparisons between the means were made with paired t-test at a confidence level of 95%.RESULTS: The data indicated that there were high- and low-affinity binding sites for 125Ⅰ-insulin on both hepatocellular carcinoma and its adjacent tissue. Hepatocellular carcinoma had a significantly higher Bmax for high affinity binding site than its adjacent liver tissue (P＜0.05, t=2.275). Insulin-IUdR competed as effectively as insulin with 125Ⅰ-insulin for binding to insulin receptor. Values of IC501, C502, KI1 and KI2 for Values of IC50l and KI1 for insulin-IUdR were significantly higher than that for insulin (P＜0.01,t=4.537 and 4.813).CONCLUSION: It is possible to use insulin as a carrier for carcinoma-targeted therapy mediated by receptor.展开更多
Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin(HP-β-CD) on the solubility, dissolution rate and chemical stability of prostaglandin E_1 (PGE_1) ,thereby providing a basis for preparing a ...Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin(HP-β-CD) on the solubility, dissolution rate and chemical stability of prostaglandin E_1 (PGE_1) ,thereby providing a basis for preparing a stable solid or aqueous preparation of PGE_1 formulatedwith HP-β-CD. Methods The effect of HP-β-CD on the solubility of PGE_1 was studied by phasesolubility method. The formation of inclusion complexes of PGE_1 with HP-β-CD in the aqueoussolution was confirmed by UV spectra, circular dichroism spectroscopy, and that in the solid stateby IR spectra and X-ray diffractome-try. An solid inclusion complex of PGE_1 with HP-β-CD wasprepared by lyophilization. The dissolution rate and stability of the inclusion complex weredetermined and compared with those of PGE_1 alone. Meanwhile, the stability of PGE_1 aqueoussolutions in the presence of HP-β-CD was studied under different pH conditions. Results Thesolubility of PGE_1 increased linearly with increasing HP-β-CD concentration in various pH bufferedsolutions, showing typical A_L-type phase solubility diagrams. The stability and dissolution rateof the solid inclusion complex of PGE_1 were significantly increased, compared with those of purePGE_1 . The stability of PGE_1 in HP-β-CD solutions was also obviously improved under acidic andbasic conditions, but the stabilizing effect was absent under neutral conditions. Conclusions Thesolubility,dissolution rate and chemical stability of PGE_1 are markedly improved by complexationwith HP-β-CD: It is quite possible to prepare a stable PGE_1 inclusion complex-containing soliddosage forms, but almost impossible to obtain a stable aqueous preparation of PGE_1 formulated withHP-β-CD.展开更多
LNG and E2 microcrystals were prepared by the solvent conversion method. The secondary solvent system, rate of stirring and temperature were considered to have a significant effect on the forming of microcrystalline w...LNG and E2 microcrystals were prepared by the solvent conversion method. The secondary solvent system, rate of stirring and temperature were considered to have a significant effect on the forming of microcrystalline with different particle sizes.展开更多
A key-shaped lcvonorgcstrcl-rclcasing intrauterine device ( LNG-IUD ) was designed and fabricated. The IUD with a hollow vcrtlcal arm was made of modified ethylene-vinyl acetate copolymcr ( EVA ). The LNG paste was cn...A key-shaped lcvonorgcstrcl-rclcasing intrauterine device ( LNG-IUD ) was designed and fabricated. The IUD with a hollow vcrtlcal arm was made of modified ethylene-vinyl acetate copolymcr ( EVA ). The LNG paste was cncapsulcd in the vertical arm展开更多
Ethyleae-vinyl acetate copolymer ( EVA ) was mechanically blended with methylvinyl siloxane in order to increase the permeability of some steroids and to obtain an ideal material with membrane-controlled release of st...Ethyleae-vinyl acetate copolymer ( EVA ) was mechanically blended with methylvinyl siloxane in order to increase the permeability of some steroids and to obtain an ideal material with membrane-controlled release of steroids from the intrauterine展开更多
文摘Aim To develop a reverse phase HPLC method for the determination of aloperine, an alkaloid that is newly extracted from Sophora alopecuraides and has shown wide pharmacological effects including antibacterial and antiinflammatory actions. Methods The samples were analyzed on a ODS column with methanol water triethylamine (3∶97∶0 1 V/V) as a mobile phase. The flow rate was 1 0 mL·min -1 , and UV detection wavelength 205 nm. Results Linear regression equation was A=1 6920C+1 7455 (r 2=0 9999, n =5) in concentratins ranging from 20 to 120 μg·mL -1 . The recoveries were 101 2±1 46 % at 80 μg·mL -1 , 100 5±0 75% at 100 μg·mL -1 , and 100 7±1 10% at 120 μg·mL -1 , respectively, and the precisions of aloperine within or between run were from 0 80% to 1 98% ( n =5). The relative contents of aloperine in three lots of tablets were 101 59±1 38%, 98 46±0 23%, and 99 41±1 09% ( n =3). Conclusion The newly developed reverse phase HPLC method is simple and useful for daily assay of aloperine tablets and can overcome the interference from excipient and other alkaloids in titration and UV detection.
基金The National Natural Science Foundation of China,Grant No 30270415
文摘AIM: To evaluate the possibility of using insulin as a carrier for carcinoma-targeted therapy mediated by receptor, and to investigate the expression of insulin receptor in human hepatocellular carcinoma and the receptor binding characteristics of insulin-IUdR (iododeoxyuridine).METHODS: IUdR was covalently conjugated to insulin.Receptor binding assays of 125Ⅰ-insulin to human hepatocellular carcinoma and its adjacent tissue were performed.Competitive displacements of 125Ⅰ-insulin by insulin and insulin-IUdR to bind to insulin receptor were respectively carried out. Statistical comparisons between the means were made with paired t-test at a confidence level of 95%.RESULTS: The data indicated that there were high- and low-affinity binding sites for 125Ⅰ-insulin on both hepatocellular carcinoma and its adjacent tissue. Hepatocellular carcinoma had a significantly higher Bmax for high affinity binding site than its adjacent liver tissue (P＜0.05, t=2.275). Insulin-IUdR competed as effectively as insulin with 125Ⅰ-insulin for binding to insulin receptor. Values of IC501, C502, KI1 and KI2 for Values of IC50l and KI1 for insulin-IUdR were significantly higher than that for insulin (P＜0.01,t=4.537 and 4.813).CONCLUSION: It is possible to use insulin as a carrier for carcinoma-targeted therapy mediated by receptor.
文摘Aim To study the effect of complexation with hydroxylpropyl-β-cyclodextrin(HP-β-CD) on the solubility, dissolution rate and chemical stability of prostaglandin E_1 (PGE_1) ,thereby providing a basis for preparing a stable solid or aqueous preparation of PGE_1 formulatedwith HP-β-CD. Methods The effect of HP-β-CD on the solubility of PGE_1 was studied by phasesolubility method. The formation of inclusion complexes of PGE_1 with HP-β-CD in the aqueoussolution was confirmed by UV spectra, circular dichroism spectroscopy, and that in the solid stateby IR spectra and X-ray diffractome-try. An solid inclusion complex of PGE_1 with HP-β-CD wasprepared by lyophilization. The dissolution rate and stability of the inclusion complex weredetermined and compared with those of PGE_1 alone. Meanwhile, the stability of PGE_1 aqueoussolutions in the presence of HP-β-CD was studied under different pH conditions. Results Thesolubility of PGE_1 increased linearly with increasing HP-β-CD concentration in various pH bufferedsolutions, showing typical A_L-type phase solubility diagrams. The stability and dissolution rateof the solid inclusion complex of PGE_1 were significantly increased, compared with those of purePGE_1 . The stability of PGE_1 in HP-β-CD solutions was also obviously improved under acidic andbasic conditions, but the stabilizing effect was absent under neutral conditions. Conclusions Thesolubility,dissolution rate and chemical stability of PGE_1 are markedly improved by complexationwith HP-β-CD: It is quite possible to prepare a stable PGE_1 inclusion complex-containing soliddosage forms, but almost impossible to obtain a stable aqueous preparation of PGE_1 formulated withHP-β-CD.
文摘LNG and E2 microcrystals were prepared by the solvent conversion method. The secondary solvent system, rate of stirring and temperature were considered to have a significant effect on the forming of microcrystalline with different particle sizes.
文摘A key-shaped lcvonorgcstrcl-rclcasing intrauterine device ( LNG-IUD ) was designed and fabricated. The IUD with a hollow vcrtlcal arm was made of modified ethylene-vinyl acetate copolymcr ( EVA ). The LNG paste was cncapsulcd in the vertical arm
文摘Ethyleae-vinyl acetate copolymer ( EVA ) was mechanically blended with methylvinyl siloxane in order to increase the permeability of some steroids and to obtain an ideal material with membrane-controlled release of steroids from the intrauterine
