OBJECTIVE:To study the influence of both pH and complexation by hydroxypropyl-?-cyclodextrin(HPCD) on the overall solubility of hydroxycamptothecin(HCPT) with particular focus on the equilibrium between its lactone-and carboxylate-form.METHODS:Phase solubility studies at pH values and physiologically acceptable HPCD concentrations were performed,and the amounts of solubilized HCPT quantified by HPLC.The lactone-carboxylate-ratios from the equilibrium were studied.RESULTS:The solubility of HCPT increased with both increasing pH and HPCD concentration.The apparent complexation constant decreased with increasing pH.The lactone-carboxylate equivalence point shifted from a pH value of 6.5,7.0 and 7.3 with 0%,10% and 25% HPCD,respectively.Separate complexation constants for the carboxylate-HCPT and lactone-HCPT could thus be derived.CONCLUSION:The solubilizing and stabilizing effects of HPCD on HCPT in aqueous solution were good.

OBJECTIVE:To prepare Tetramethylpyrazine phosphate porosity osmotic tablet (TMPP) and to optimize its formulation and investigate its mechanism of drug release. METHODS: The formulation was optimized by the orthogonal experiment design through investigation of one factor; the accumulative drug release rates of preparations of different formulation were measured, and the mechanism of drug release of the tablets was discussed. RESULTS: The dosage of PEG 400 in coating solution, the content of hydroxy-propyl methyl cellulose (HPMC) in tablet core, the dosage of dibutylphthalate as plasticizer, and the weight gain of coating membrane were four important factors influencing drug release. The optimal formulation was to use 10% of PEG400, 5% of HPMC, 10% of dibutylphthalate and 12 mg coating membrane. The release behavior in vitro of the porosity osmotic tablets prepared in the above condition within 10 h complied with zero order release rule(r=0.999 81), with accumulative release rate of 94.2%. The tablets had good reproducibility in interassay and which was independent of the influence of gastrointestinal condition. The mechanism of drug release included osmotic pump mechanism and diffusion mechanism, but osmotic pump one was the main type. CONCLUSION: The formulation and preparation technology of the porosity osmotic tablets were simple but effective, showing an obvious zero order release within 12 h and good reproducibility, thus suitable for the industrial production of porosity osmotic tablets.

OBJECTIVE:To prepare Curcumine solid lipid nanoparticles(Cur-SLN).METHODS:Cur-SLN was prepared by emulsification evaporation-solidification at low temperature.The formulation of Cur-SLN was optimized by orthogonal experiment with the contents of curcumine,poloxamer 188,docosanoic acid glyceride lecithin used as factors and with entrapment efficiency as index;meanwhile,the appearance,particle size,surface potential,entrapment efficiency and the release profile of curcumine in vitro were studied.RESULTS:The optimized preparation conditions were as follows:the contents of curcumine,poloxamer,docosanoic acid glyceride lecithin were 8 mg,320 mg,140 mg and 320 mg,respectively.The Cur-SLN assumed spherical shape with particle size at(134?5)nm,entrapment efficiency at(67.4?1.3)% and mean surface potential at(-23.5?1.5)mV.The release profile of curcumine in vitro fitted Higuchi equation.CONCLUSION:It is feasible to prepare Cur-SLN by emulsion evaporation-solidification at low temperature,and the study results serve as experimental evidence for developing new curcumine injection.

OBJECTIVE:To study the fingerprint of Ligusticum chuanxiong Hort.concomitant with Angelica sinensis in different ratio boiled in water.METHODS:The gradient elution mode was applied in chromatographic separation.The stationary phase was Zorbax SB-C18(250mm? 4.6mm,5? m).The mobile phase consisted of methanol∶ water(containing 0.5% acetic acid).The UV detection was performed at 313 nm.RESULTS:No new substances were found in the water extracts of Li-gusticum chuanxiong Hort.concomitant with Angelica sinensis.Some ingredients released better when the two drugs boiled together with water.Ligusticum chuanxiong Hort.concomitant with Angelica sinensis at the ratio of 7∶ 3 had a bigger concentration of Ferrulic acid in water extract.CONCLUSION:The research provides the new way of R& D of cardiovascular drugs.

OBJECTIVE:To establish a method for simultaneous determination of ferulic acid(FA)and TMP in serum sample.METHODS:After deprotein with boiling water-bath,RP-HPLC was performed on ODS C 18 column(250mm?4.6mm)with methanol-water(containing0.1%acetic acid)=8∶17as the mobile phase and UV detection at280nm.RESU LTS:The calibration curve of FA was linear within the range of30.2～70.8?g/ml,Y=57.51+413.12X,r=0.9974;the curve of TMP was linear within the range of10.1～50.7?g/ml,Y=41.32+308.64X,r=0.9922.CONCLUSION:Compared with the traditional extraction,the method is simple,rapid and sensitive,and can be used for simultaneous determination of the contents of active compositions in Chinese materia medica.

OBJECTIVE:To establish high performance liquid phase fingerprint for chuanxiong so as to control its quali-ty.METHOD:The chromatographic column was Zorbax SB-C 18 with column temperature at25℃and flow rate at1.0ml/min;the detection wavelength was323nm;the gradient elution was conducted with methanol and0.1%glacial acetic acid water solution.To study the effects of chuanxiong by different extraction methods on fingerprints;the isocratic elution was conducted to investigate the fingerprints of chuanxiong under different detecting wavelength.RESULTS:The ultrasonic method had a good effect in the gradient elution.CONCLUSION:The method is simple,reliable and reproducible,which can be used to es-tablish fingerprint for chuanxiong.

Objective:To optimize the formula and preparation process of prepare sorafenib dry suspension and detect the content by HPLC. Methods:The influence of single factor including different fillers, suspending agents, adhesives and disintegrants on the sedimentation rate, redispersibility and drying shrinkage of sorafenib dry suspension was observed. Orthogonal design was used to opti-mize the formula and preparation process of the suspension, and HPLC was used to determine the content of sorafenib. The chromato-graphic column was Inertsil ODS-3 (250 mm × 4. 6 mm, 5μm), the mobile phase was 20 mmol·L-1 ammonium acetate buffer-aceto-nitrile(28 ∶72), the detection wavelength was 266 nm, the flow rate was 1. 0 ml·min-1, the column temperature was 40℃, and the sample size was 20 μl. Results:The optimal formula and preparation process were as follows:sucrose (48%) was used as the filler, xanthan gum (28%) and CMC-Na (12%) were the suspending agents, MCC (10%) was used as the disintegrant, and 6% PVP (in 50% ethanol) was the adhesive. The linear range of sorafenib was 1-100 μg·ml-1(r=0.999 8), and the recovery was 98.96%(RSD=0. 75%, n=9). Conclusion:The optimal formula and preparation process are repeatable. The HPLC method is simple and specific, which can be used to determine sorafenib.

OBJECTIVE: To establish a HPLC method for the simultaneously determination of Vitamin D2, Vitamin A and Vitamin E in Cernevit-12 for injection. METHODS: An Inertsil(ODS-2) C18 column was selected as separation column at 30℃. The mobile phase consisted of acetonitrile-methanol-methylene chloride (80∶10∶10) at a flow rate of 1.0mL?min-1. The detection wavelength was set at 265nm and the injection volume was 10?L. RESULTS: The linear ranges of Vitamin D2, Vitamin E acetic ester and Vitamin A palmitate were 0.61～1.43?g?mL-1, 222.6～519.4?g?mL-1 and 1.21～2.82mg?mL-1 respectively. The average recoveries were 99.79%, 99.53% and 101.63%, with RSD of 1.66%, 0.184 6%, 0.113 4%. CONCLUSION: The method is simple, rapid and accurate, and suitable for the determination of Cernevit-12.

OBJECTIVE:To prepare tongmai oral liquid and study its quality control method.METHODS:The danshen root in tongmai oral liquid was identified by TLC.The content of ferulic acid in the oral liquid was determined by HPLC.RESULTS:Danshen root showed a good specificity in qualitation identification.The linear range of ferulic acid was5.12～71.68?g/ml(r=0.9998).The mean recovery was99.96%(RSD=1.3%).CONCLUSIONS:The preparation technology is practicable and quality control method is reliable.

Nuciferine is a major aporphine alkaloid in the leaves of Nelumbo nueifera. It has great effects such as lipid-lowering,anti-oxidation,antimicrobial activitity and anti-cancer. The review focused on its pharmacological effects and pharmacokinetic characters reported in recent years,which can be helpful to the further researches on nuciferine.