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1.
Herald of Medicine ; (12): 88-91, 2018.
Artículo en Chino | WPRIM | ID: wpr-665250

RESUMEN

Objective To determine the solubility of rhein in different vehicles and its partition coefficients in the n-octanol-water system for designing new formulations. Methods High performance liquid chromatography(HPLC) method was established to determine the concentration of rhein in water,different pH solutions and different solvents;the partition coefficients for the n-octanol- buffer solution systems were determined by shaking flask method. Results The equilibrium solubility of Rhein was 3.89 μg·mL-1and the lgP was 2.79 in water at 37 ℃.The solubility of rhein was increased with the raise of pH, which could reach 362.20 and 431.65 μg·mL-1in phosphate buffer solution at pH 6.8 and 7.4,respectively.Solubility of rhein in the semi polar solvent was relatively good,which can up to 2 971.74 μg·mL-1in PEG400.The oil-water partition coefficients of rhein were decreased with the increase of pH,and were 0.83 and 0.54 in phosphate buffer solution at pH 6.8 and 7.4,respectively. Conclusion Rhein is almost not soluble in water.With the raise of pH,the solubility is increased but the oil-water partition coefficient is decreased.

2.
Chinese Traditional Patent Medicine ; (12): 2034-2038, 2017.
Artículo en Chino | WPRIM | ID: wpr-660449

RESUMEN

AIM To investigate the equilibrium solubilities,oil-water partition coefficients and in vitro skin permeation features of brucine and strychnine in total alkaloids from Strychni Semen.METHODS Saturated dissolution method was applied to determining the equilibrium solubilities of two constituents in ethanol (10%,20%,30%,60%,90%,anhydrous ethanol),trichloromethane,n-octanol and surfactants (0.5% tween,0.5% sodium deoxycholate,0.5% oleic acid).Shake-flask method was adopted in detecting their oil-water partition coefficients in PBS (pH 2.5,4.0,5.0,5.8,6.8,7.0,7.4,9.0).Modified Franz diffusion cell method was used for evaluating their in vitro skin permeation features in PBS,20% ethanol and anhydrous ethanol.RESULTS Both brucine and strychnine showed the highest equilibrium solubilities in trichloromethane and the lowest equilibrium solubilities in surfactants.The equilibrium solubility of strychnine was higher than that of brucine in ethanol (> 20%) or PBS (pH < 8.0),which reached the highest in 60% ethanol and pH 2.5 PBS,respectively.The similar oil-water partition coefficients of two constituents,proportional to pH value,reached the highest at pH9.0.And they exhibited the highest accumulated transdermal absorptivities in anhydrous ethanol and pH 9.0 PBS,respectively.CONCLUSION Solvent type has obvious effects on the equilibrium solubilities,oil-water partition coefficients and in vitro skin permeation features of both brucine and strychnine.This study can provide a reference for the bioavailability improvement of transdermal drug delivery and development of related preparations.

3.
Chinese Traditional and Herbal Drugs ; (24): 3961-3969, 2017.
Artículo en Chino | WPRIM | ID: wpr-852485

RESUMEN

Objective To prepare multicomponent microemulsion of Chinese materia medica (CMM) with different oil-water partition coefficients (logP values) by simplex lattice method and evaluate its quality. Methods The surfactants, cosurfactants and oil phases were screened by saturated solubility method. Ochratins, ligustrazine, ferulic acid, puerarin and geniposide were model drugs to represent the complex components of CMM. Based on the pseudo-ternary diagram, simplex lattice method was adopted to optimize the multicomponent microemulsion of CMM with different logP values by appearance, particle size and polydispersity index as evaluation indexes. The experimental design and model building were constructed by Design Expert 8.06 software to optimize the response surface data analysis and validate the optimal prescription composition. The quality of microemulsion was evaluated by observing appearance and stability as well as measuring particle size and potential. Results The optimum formulation was oleic acid-Labrasol-propylene glycol-water (5.303:29.336:7.334:58.027). The prepared microemulsion was clear in appearance with good yellowish color and stable property. The average particle size was (118.77 ± 0.37) nm, PDI was 0.282 ± 0.02 and Zeta potential was (0.346 ± 0.05) mV. Conclusion The results indicated that the multicomponent microemulsion of CMM with different logP values is optimized and the drug loading was high. The multicomponents microemulsion of CMM with different logP values (-1.01-3.85) is established and optimized, providing a feasible microemulsion carrier for the multicomponent CMM to simplify its prescription screening work.

4.
Chinese Traditional Patent Medicine ; (12): 2034-2038, 2017.
Artículo en Chino | WPRIM | ID: wpr-657913

RESUMEN

AIM To investigate the equilibrium solubilities,oil-water partition coefficients and in vitro skin permeation features of brucine and strychnine in total alkaloids from Strychni Semen.METHODS Saturated dissolution method was applied to determining the equilibrium solubilities of two constituents in ethanol (10%,20%,30%,60%,90%,anhydrous ethanol),trichloromethane,n-octanol and surfactants (0.5% tween,0.5% sodium deoxycholate,0.5% oleic acid).Shake-flask method was adopted in detecting their oil-water partition coefficients in PBS (pH 2.5,4.0,5.0,5.8,6.8,7.0,7.4,9.0).Modified Franz diffusion cell method was used for evaluating their in vitro skin permeation features in PBS,20% ethanol and anhydrous ethanol.RESULTS Both brucine and strychnine showed the highest equilibrium solubilities in trichloromethane and the lowest equilibrium solubilities in surfactants.The equilibrium solubility of strychnine was higher than that of brucine in ethanol (> 20%) or PBS (pH < 8.0),which reached the highest in 60% ethanol and pH 2.5 PBS,respectively.The similar oil-water partition coefficients of two constituents,proportional to pH value,reached the highest at pH9.0.And they exhibited the highest accumulated transdermal absorptivities in anhydrous ethanol and pH 9.0 PBS,respectively.CONCLUSION Solvent type has obvious effects on the equilibrium solubilities,oil-water partition coefficients and in vitro skin permeation features of both brucine and strychnine.This study can provide a reference for the bioavailability improvement of transdermal drug delivery and development of related preparations.

5.
China Pharmacy ; (12)1991.
Artículo en Chino | WPRIM | ID: wpr-533441

RESUMEN

OBJECTIVE:To determine the oil-water partition coefficients (logP) of rosiglitazone at different pH values by two kinds of methods.METHODS:A shake flask-ultraviolet spectrophotometry method was used to determine plasma concentration of rosiglitazone in water phase and organic phase at variable pH values (0.95,2.0,3.0,4.0,5.07,5.7,6.55,7.06,7.5,8.15,9.21) to calculate logP by using with n-caprylic alcohol-water as simulation system.Above logP values were compared with that calculated by Pallas software.RESULTS:The logP value was lower than 1 when pH value was lower than 4;the logP value was higher than 1 when pH value was ranged from 5 to 9.Measured logP values were in good agreement with that calculated by Pallas software.CONCLUSION:Rosiglitazone exists in the form of hydrochloride salt with good water solubility (pH

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