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Objective:To study the formula of triptolide (TRI) self-microemulsifying drug delivery system (SMEDDS) and evaluate the pharmaceutical properties.Methods:The formula and preparation process of triptolide self-microemulsion were screened by the solubility test and pseudo-ternary phase diagram.With the average particle size and self-microemulsifying time as the indices,the further formula optimization of triptolide self-microemulsion was carried out.The pharmaceutical properties of triptolide self-microemulsion were evaluated.Results:The optimal formula of TRI SMEDDS was as follows:the amount of medium chain triglycerides (MCT) was 20%,that of polyoxyethylene castor oil (EL-35) was 40%,and that of polyethylene glycol 400 (PEG-400) was 40% in the oil phase.The average particle size was 43.48 nm,and the time of self-microemulsification was less than 30 s.Conclusion:The average particle size and the appearance of triptolide self-microemulsion are accordance with the requirements of pharmaceutics.Triptolide self-microemulsion has good sustained-release effect,which lays foundation for the further study on pharmacodynamics.
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Objective: To establish a method for the determination of norcantharidin in norcantharidin in situ gel .Methods:An optimal HPLC method was set up and an Agilent ZORBAX SB-C18 column (150 mm ×4.6 mm, 5μm) was adopted.The mobile phase was acetonitrile-phosphate buffer solution(1∶9, adjusting pH to 3.1 with phosphorjc acid).The flow rate was 0.8 ml· min-1 and the column temperature was 25℃.The detection wavelength was set at 210 nm and the injection volume was 20μl.Results:Norcanthari-din had a good linear relationship within the range of 0.02-1.00 mg· ml-1 (r=0.999 9).The average recovery was 97.5%and RSD was 0.98%(n=9).Conclusion:The method is accurate, simple and reproducible, which can be used for the determination of nor-cantharidin in norcantharidin in situ gel .
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Objective:To investigate the stability of flurbiprofen axetil lipid microspheres injection combined with 0. 9% sodium chloride injection or 5% dextrose injection, and provide theoretical basis for the clinical application. Methods:The content changes of flurbiprofen axetil in the mixture of flurbiprofen axetil lipid microspheres injection and 0. 9% sodium chloride injection or 5% dextrose injection were determined in 5 h at 25℃ away from light, and the changes in the appearance and particle size of flurbiprofen axetil lip-id microspheres were investigated. The changes in the appearance and particle size of flurbiprofen axetil lipid microspheres in the mix-ture of flurbiprofen axetil lipid microspheres injection and 0. 9% sodium chloride injection before and after freezing and thawing were also investigated. Results:The appearance, particle size and content had no significant changes in all mixtures in 5 h at 25 ℃ away from light. The appearance and particle size of flurbiprofen axetil lipid microspheres in the mixture before and after freezing and thawing had no significant changes as well. Conclusion:The mixture of flurbiprofen axetil lipid microspheres injection and 0. 9% sodium chlo-ride injection or 5% dextrose injection is stable in 5 h away from light.
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Several cytokines which play key role in asthma patients with chronic inflammation and reconstruction of air duct,are important targets for anti-asthma agents.In this review,we summarize the latest advancement of anti-asthma agents which targeted for cytokines(interleukins,TNF,eotaxin)and investigation development of new anti-asthma agents emerged in recent years.
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Objective To prepare ligustrazine-chitosan microspheres and to investigate the drug release behavior in vitro. Methods Microspheres were prepared using the spray drying method.The encapsulation efficiency was used to evaluate the influence of different formulation and preparation factors,the formulation was optimized by L9(34) orthogonal design.Results The optimal formulation and preparation factors were as follows: chitosan concentration(0.01 g/mL),ratio of chitosan to ligustrazine(1∶4),inlet temperature(120 ℃),air flow rate(500 L/h).The optimized microspheres had a spherical shape,the loading capacity was(18.60?0.15)%,entrapment efficiency was(93.01?0.76)%,the average diameter was(10.69?0.64) ?m.The drug release profile in vitro could be described by Higuchi equation Q=19.798 t1/2+25.209(r=0.997) at 1-15 h,which showed the prepared microspheres obviously had the sustained release effect.Conclusion The encapsulation efficiency of ligustrazine-chitosan microspheres is higher,the preparation method is simple,and the process is stable.It will provide the basis for realizing the industrialization in Chinese materia medica microspheres.
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Aim To prepare NT-Ⅰ loaded nanoparticles with different diameters modified by Methylated-polyethyleneglycol (Me-PEG) and evaluate their brain pharmacokinetics after administered nasally in rats. Methods NT-Ⅰ-NP was prepared by emulsion/solvent evaporation method and MePEG-PLA was used as the carrier material. Microdialysis technique and fluorospectrophotometry were used to determine NT-Ⅰ concentration after nasal administration in the brain of rats. Results The appearance of all NT-Ⅰ-NP groups was round or similar. The AUC(0-t) of below 100 nm NT-Ⅰ-NP was 1.22 fold as that of 100~200 nm NT-Ⅰ-NP,1.34 fold as that of 200~300 nm and 1.60 fold as that of exceed 300 nm NT-Ⅰ-NP(P