Study on Anti-tumor Effects of Artemether Self-microemulsifying Drug Delivery System on Subcutaneous Trans- plantation of Human Glioma in Mice / 中国药房

OBJECTIVE：To study the anti-tumor effect of artemether （ARM）self-microemulsifying drug delivery system （SMEDDS） on human glioma subcutaneously transplanted model mice. METHODS ：Human glioma cell line SHG 44 was inoculated and passed on to establish subcutaneous transplanted tumor model of nude mice. At the 5th，10th，15th，20th and 25th day after inoculation ，the tumor tissue volume was measured and the growth curve was drawn to confirm the initial stage of rapid tumor proliferation. Thirty nude mice was collected to establish subeutaneously transplanted tumor nude model ，and then divided into control group （normal saline ），ARM suspension group [ 60 mg/（kg·d）]，ARM-SMEDDS low-dose ，medium-dose and high-dose groups [ 10，20，30 mg/（kg·d）] at the initial stage of rapid tumor proliferation. They were given normal saline and relevant solution intragastrically once a day ，for consecutive 30 d. The weight change and general sibuation of mice were recorded. The change of tumor volume was determined and relative tumor proliferation rate was calculated. RESULTS ：The subcutaneously transplanted tumor tissue entered the initial stage of rapid tumor proliferation from the 10th day after transplantation. The general situation was normal ，and there was no obvious abnormal reaction in mice of each group during treatment. Since 10th day of administration，tumor tissue volume of mice in ARM-SMEDDS groups were shortened significantly than control group （P＜0.05）. At 15th day of administration ，tumor volume of mice in ARM-SMEDDS groups were shortened significantly than ARM suspension group（P＜0.05）. After last administration ，relative tumor proliferation rates of mice in ARM-SMEDDS groups were decreased significantly，compared with ARM suspension group （P＜0.05）. CONCLUSIONS ：ARM-SMEDDS show significant inhibitory effect on the proliferation of human glioma ，and are better than suspension with higher dosage.

Study on the Absorption of Silymarin Enteric Coated-PLGA Nanoparticles in Rat in situ Intestine Perfu-sion Model and Caco-2 Cell Model / 中国药房

OBJECTIVE:To study the absorption features of Silymarin enteric coated-polyllactic-co-glycolic acid (PLGA) nanoparticles in rat in situ intestine perfusion model and colonic adenoma Caco-2 cell model. METHODS:HPLC method was used to determine the content of silymarin. The absorption rate constant(Ka)and apparent absorption coefficient(Kapp)of Silymarin sus-pension,Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were investigated in duodenum,jejunum, ileum and colon of rat in situ intestine perfusion model;the apparent permeability coefficient (Papp) of those drugs containing low-concentration,medium-concentration and high-concentration(20,40,60 μg/mL)of silymarin in Caco-2 cell model were also investigated. RESULTS:Compared with Silymarin suspension,Ka and Kapp of Silymarin PLGA nanoparticles and Silymarin enteric coated-PLGA nanoparticles were all increased in duodenum,jejunum,ileum and colon(P0.05). CONCLUSIONS:Silymarin enteric coated-PLGA nanoparticles can effectively increase the intestinal ab-sorption,cellular uptake and transmembrane transport rate of silymarin.

Study on the Formulation Optimization of Entecavir PLGA Sustained-release Microspheres and Its Drug Release in vitro / 中国药房

OBJECTIVE:To optimize the formulation of entecavir PLGA sustained-release microspheres,and explore its drug release in vitro. METHODS:PLGA sustained-release microspheres was prepared by emulsification-solvent evaporation method. Us-ing composite score of entrapment efficacy and drug loading as indexes,orthogonal test was designed to optimize drug amount, drug-PLGA mass ratio,PLGA mass concentration,oil phase-aqueous phase volume ratio and polyvinyl alcohol (PVA) concentra-tion;and validation test was also conducted. The prepared microsphere morphology,particle size and durg release in vitro were de-tected. RESULTS:The optimized formulation was entecavir 20 mg,entecavir-PLGA mass ratio 1∶10,PLGA mass concentration 200 mg/ml,oil phase-aqueous phase volume ratio 1∶10,and PVA concentration 2%;entrapment efficacy was (86.52 ± 3.25)%, drug loading was(18.36±1.37)%,RSDs were lower than 5.0%(n=3);it was round and smooth in appearance with average par-ticle size of 58.35 μm;Q10 h,Q96 h and Q360 h were 9.6%,42.9% and 89.6%,and the drug release in vitro fitted to Higuchi model (r2=0.965 8). CONCLUSIONS:Entecavir PLGA sustained-release microspheres prepared by optimized formulation has good sus-tained-release performance.

Preparation optimization of palonosetron hydrochloride oral disintegrating tablets by orthogonal test / 重庆医学

Objective To prepare optimization of palonosetron hydrochloride oral disintegrating tablets by orthogonal test. Methods Palonosetron hydrochloride oral disintegrating tablets were prepared with direct compression process.The content of pal-onosetron hydrochloride was determined by HPLC.The formulation was optimized with disintegration time as evaluation indices. Results The optimal formulation(60 mg/tablet)was as follows:L-HPC 12%,mannitol∶SMCC= 2∶1,magnesium stearate 2%, stevia glycosides 3%.The oral disintegrating tablets showed dine appearance and tested better;the disintegration time was 12 sec-onds;the tablets featured a hardness of 3 kg;4 min dissolution rate was 99%.Conclusion The preparation method is simple and reasonable,and the tablets can disintegrate rapidly.