OBJECTIVE:To provide reference for strengthening drug regulation in drug administration department. METH-ODS:Drug regulatory statistical yearbooks during 2011-2015 were collected. Literature analysis,content analysis,comparative analysis and secondary analysis were conducted to analyze and explore the drug production license,business license,advertising ap-proval,protection of TCM varieties,drug complaints,investigation and punishment of drug cases,etc. in statistical yearbook. RE-SULTS & CONCLUSIONS:The number of drug manufacturers and operating enterprises had been increasing year by year,while the retail chain stores in certified enterprises showed tendency to go beyond the single retail pharmacy. Compared with the down-ward trend of number of approved drug advertisements,the number of protected varieties of TCM decreased more obviously. The increase in number of drug complaints did not cause the number of investigated and punished drug cases at the same time,which showed a downward trend. It is suggested to further improve the quality and efficiency of drug regulatory work in China by strict drug production license approval,reforming drug advertising regulation and TCM varieties protection system,intensifying efforts to investigate and punish drug complaints and cases,and playing the supervision of public opinion role of the media and the masses.

OBJECTIVE:To prepare the puerarin cubic phase,and study its in vitro transdermal characteristics under micronee-dle. METHODS:Using glycerol monooleate,ethanol,puerarin and purified water as materials,injection method was used to pre-pare the puerarin cubic phase. Polarizing microscopy and small angle X-ray diffraction were used for characterizing. The in vitro transdermal characteristics of Puerarin 10% ethanol solution and puerarin cubic phase were comparatively studied by modified Franz diffusion cell,and the in vitro transdermal characteristics of puerarin cubic phase under microneedle were studied. RE-SULTS:Prepared puerarin cubic phase had no obvious phase distribution under polarizing microscope with dark green color,show-ing isotropic trait. The ratio of scattering peak position was √6:√8,indicating that its internal structure was spiral lattice. The trans-dermal rates of Puerarin 10%ethanol solution and puerarin cubic phase were 15.306,29.101μg/(cm2·h),and the cumulative trans-dermal amounts within 20 h were 190,545 μg/cm2,respectively. After the pretreatment on skin by 200 μm microneedle,the trans-dermal rates of puerarin cubic phase was 78.15 μg/(cm2·h),and the cumulative transdermal amounts within 20 h was 1450 μg/cm2. CONCLUSIONS:Puerarin cubic phase is successfully prepared,which shows stronger transdermal ability than puerarin ethanol aqueous solution and better transdermal ability when combined with microneedle administration.

OBJECTIVE:To prepare the Compound anisodamine and neostigmine sustained-release tablet and study the in vitro drug release behavior. METHODS:Using raceanisodamine and neostigmine methyl sulfate as main medicines,hydroxypropyl meth-yl cellulose as sustained release skeleton material,magnesium stearate as the lubricant,polyvinyl pyrrolidone as the adhesive,pre-gelatinized starch as the thinner,microcrystalline cellulose as the disintegrant and filler,Compound anisodamine and neostigmine sustained-release tablet was prepared by wet granulation method and direct compression method. The in vitro cumulative release rate within 12 h of the 2 main medicines was detected by HPLC method. RESULTS:Compound anisodamine and neostigmine sus-tained-release tablet was successfully prepared,and the in vitro release was basically completed within 12 h,with accumulative re-lease rate of 91.3% for anisodamine and 96.5% for neostigmine. CONCLUSIONS:Compound anisodamine and neostigmine sus-tained-release tablet that can cumulatively release for 12 h is successfully prepared.

OBJECTIVE:To optimize the extraction technology of polyphenols from Juglans regia branch and evaluate its anti-oxidant activity in vitro. METHODS:Using extraction amount of polyphenols from J. regia branch as response value,solvent-solid ratio,extraction temperature and ethanol volume fraction as response factors,based on single factor test,response surface method was used to optimize the extraction technology of polyphenols from J. regia branch. Using vitamin C as positive control,scaveng-ing on hydroxyl radicals and 1,1-diphenyl-2-picrylhydrazyl(DPPH)radicals and total reducing activities of polyphenols from J. re-gia branch were investigated. And its antioxidant activity in vitro was evaluated. RESULTS:Optimized extraction conditions for polyphenols from J. regia branch was as follow as solid-liquid ratio of 1:25(g/mL),extraction temperature of 50 ℃,ethanol vol-ume fraction of 70%. The extraction amount of polyphenols from J. regia branch was 9.30 mg/g(RSD=0.57%,n=3)in the veri-fication test. Clearance rate on hydroxyl radicals and DPPH radicals and total reducing activity of polyphenols from J. regia branch were respectively 50.24%,95.42%,1.118 when it was under the mass concentration of 12.0,3.0,3.0μg/mL;and the related data of vitamin C was 93.71%,46.17%,0.628 under the same mass concentration(P<0.05). CONCLUSIONS:Extraction technology of polyphenols from J. regia branch optimized by response surface method is stable and feasible;polyphenols from J. regia branch shows certain antioxidant activity in vitro.

OBJECTIVE:To optimize the drying technology of Zingiber officinale peel and establish its quality standard. METHODS:Moisture content was determined in samples after being dried for different time(0.5-10.0 h)under 50,60,70,80, 90 ℃. Optimal drying time under each temperature was screened by using moisture content of 7%-13% as dryness for controlling standard. Then contents of 6-gingerol,8-gingerol,6-shogaol,10-gingerol in samples dried for optimal drying time under different temperatures were measured,using the 4 gingerol contents as indexes to optimize the drying temperature and time. And verification test was conducted. The moisture,total ash,water soluble extract,volatile oil,6-gingerol,8-gingerol and 10-gingerol of Z. offici-nale peel from 10 different producing areas were detected to establish quality standard after being dried with the optimal technology. RESULTS:The drying time of Z. officinale peel under 50,60,70,80,90 ℃ was determined as 10.0,4.2,2.6,1.5,1.1 h,re-spectively. The optimal drying technology was 50 ℃ drying for 10.0 h. Verification test showed RSDs of 6-gingerol,8-gingerol, 6-shogaol,10-gingerol contents were 1.46%,1.09%,1.35%,1.12%(n=3),respectively. The quality standard of Z. officinale peel was suggested that total ash was no more than 18.0%;water soluble extract,volatile oil,6-gingerol,8-gingerol,10-gingerol were respectively no less than 18.0%,1.30%,0.730%,0.060%,0.100%. CONCLUSIONS:The optimized drying technology of Z. officinale peel is reasonable,reliable,stable and simple,which provides a scientific basis for standardizing the drying technolo-gy and quality standard of Z. officinale peel. The established quality standard is feasible.

OBJECTIVE:To observe the effect of Banxia Xiexin decoction on nuclear transcription factor κB p65 (NF-κB p65),NF-κB inhibitory protein α(IκB-α)and Toll-like receptor 4(TLR4)in colon tissue of rats with ulcerative colitis(UC),and explore the possible mechanism for UC treatment. METHODS:Rats were randomly divided into normal group (normal saline), model group (normal saline),Sulfasalazine enteric coated tablet (SASP,positive group,0.3 g/kg),Banxia Xiexin decoction low-dose,medium-dose,high-dose groups (3.9,7.8,11.7 g/kg),8 in each group. Except for normal group,other groups were used trinitrobenzene sulfonic acid-ethanol method to reduce UC model. After modeling,they were administrated,ig,once a day, for 3 weeks. After administration,NF-κB p65,IκB-α,TLR4 mRNA and protein expressions in colon tissue of rats in each group were detected. RESULTS:Compared with normal group,NF-κB p65,IκB-α,TLR4 mRNA and protein expressions in colon tissue of rats in other groups were significantly increased(P<0.05). Compared with model group,NF-κB p65,IκB-α,TLR4 mRNA and protein expressions in colon tissue of rats in each administration group were significantly decreased (P<0.05);showing certain dose-dependent,and the decreasing degree of above indexes in colon tissue of rats in Banxia Xiexin decoction high-dose group were higher than SASP group (P<0.05). CONCLUSIONS:Banxia Xiexin decoction can down-regulate the NF-κB p65,IκB-α, TLR4 mRNA and protein expressions in colon tissue of UC rats,which may be one of the mechanisms for UC treatment.

OBJECTIVE:To study the mechanism of histone deacetylase inhibitor RGFP109 in reversing resistance of glioma U251 cells. METHODS:TR/U251 cells resistance to temozolomide(TMZ)was extrablished. The test was divided into normal con-trol group,TMZ group(40 μmol/L)and TMZ(40 μmol/L)+RGFP109(0-120 μmol/L)different concentrations groups. After 24 h of adding into related medicines,CCK-8 was used to detect the cell survival rate and calculate the half inhibitory concentration (IC50). TUNEL and Annexin V/PI were used to detect the cell apoptosis in normal control group,TMZ group and TMZ+RGFP109 (42μmol/L)group. Immunoblotting was used to detect the O6-methyl guanine-DNA methyltransferase(MGMT),Survivin,B lym-phoma 2(Bcl-2),B lymphoma xL(Bcl-xL)protein expression;and gel migration test was used to detect the p65 acetylation level and its binding capacity with κB-DNA. RESULTS:Compared with normal control group,cell survival rate in TMZ+RGFP109 dif-ferent concentrations groups was obviously decreased (P<0.05),showing a concentration-dependent manner. When the RGFP109 concentration was 42 μmol/L,the sensitivity of TMZ to TR/U251 cells was the same with U251 cells. Compared with normal con-trol group,MGMT,Survivin,Bcl-2,Bcl-xL protein expressions in cells of TMZ groups were enhanced(P<0.01);p65 acetyla-tion level had no obvious changes,while the binding capacity of p65 and κB-DNA was strengthened (P<0.01). Compared with TMZ group,MGMT,Survivin,Bcl-2,Bcl-xL protein expressions in cells of TMZ groups were weakened(P<0.01);p65 acetyla-tion level was enhanced (P<0.01);and the binding capacity of p65 and κB-DNA was weakened (P<0.01). CONCLUSIONS:RGFP109 can reverse the resistance of U251 cells to TMZ by down-regulating the anti-apoptotic protein expressions adjusted by transcription factorκB(NF-κB)and weakening the binding of p65 andκB-DNA.

OBJECTIVE:To establish a method for the plasma concentration determination of carboplatin,and study the phar-macokinetics of carboplatin in female rats after intravenous injection and intraperitoneal injection. METHODS:HPLC was per-formed on the column of Agilent TC-C18 with mobile phase of methanol-water(5:95,V/V)at a flow rate of 1.0 mL/min,detection wavelength was 229 nm,and column temperature was 25 ℃. The inner standard was 5-bromouracil,and injection volume was 20 μL. 24 SD rats were randomly divided into 4 groups,6 in each group. The rats were intravenously injected and intraperitoneally in-jected carboplatin 20,40 mg/kg respectively. 0.5 mL blood sample was taken from eyes before administration and after administra-tion of 0.25,0.5,1,1.5,2,4,6,8,10,12 h. The plasma concentration of carboplatin was determined,and DAS 2.0 was used to calculate the pharmacokinetic parameters. RESULTS:The linear range of carboplatin in plasma was 0.30-60.00 μg/mL (r=0.9991);RSDs of intra-day,inter-day precision were lower than 10%(n=5);RSD of peak area in stability test was lower than 10%(n=5);method recovery was 98.7%-102.4%(RSD≤6.08%,n=5),and extraction recovery was 83.38%-85.45%(RSD≤5.97%,n=5). AUC0-12 h of carboplatin 20,40 mg/kg by intravenous injection and intraperitoneal injection in female rats were (15.503 ± 4.172),(23.402 ± 4.266),(6.716 ± 2.306),(9.384 ± 2.205)μg·h/mL;AUC0-∞ were (16.424 ± 4.846),(23.404 ± 4.266),(6.790±2.378),(9.765±2.095)μg·h/mL;t1/2z were(1.246±0.765),(0.394±0.058),(0.513±0.156),(0.884±0.460) h;and tmax were(0.700±0.274),(0.400±0.335),(0.542±0.368),(0.833±0.289)h,respectively. CONCLUSIONS:The meth-od is simple,economic and accurate,with suitable internal standard,and can be used for the plasma concentration determination of carboplatin in female rats and the pharmacokinetic studies.

OBJECTIVE:To study the stability of baicalin magnesium salt. METHODS:The stability of baicalin magnesium salt at high temperature(60 ℃),high humidity(90%),strong illumination(4000 lx),different temperatures(20,37,50,60 ℃) and pHs(6.80,5.70,4.60,4.30,3.90,3.60,3.20) was investigated,and HPLC was used to detect the drug contents. RESULTS:High humidity test indicated that the quality of baicalin magnesium salt was increased by (6.17 ± 0.12)% in the 5th day and in-creased by(6.92±0.05)% in the 10th day. Drug contents in the 10th day were respectively(94.78±0.12)%,(94.79±0.20)%, (94.66±0.15)% in the high temperature,high humidity,strong illumination tests(n=3). In phosphate buffer solution(pH 6.80), baicalin magnesium salt was stable only when the temperature was below 20 ℃;and it was yet stable in pure water(pH 6.76)at 37 ℃. pH stability test showed that the most stable pH was 4.30. CONCLUSIONS:Baicalin magnesium salt has hygroscopicity to some extent. Strong illumination affects the stability more seriously than high temperature and high humidity. The stability of ba-icalin magnesium salt in pure water is superior to in phosphate buffer solution,and the salt is stable in weak acid solution.

OBJECTIVE:To investigate the improvement effect of Prostatitis capsule on chronic non-bacterial prostatitis(CNP) model rats. METHODS:60 rats were randomly divided into sham operation group (distilled water),model group (distilled wa-ter),Pule'an tablet group(positive control,2 g/kg)and Prostatitis capsule high-dose,medium-dose,low-dose groups(16,8,4 g/kg). Except for sham operation group,other 5 groups were injected Xiaozhiling injection 0.2 mL to reduce CNP model. After 7 d of modeling,they received related medicines,ig,once a day,for 45 d. After 24 h of last administration,prostate lesions were ob-served by eyes and wet quality was weighed. White blood cell(WBC)count and lecithin body(SPL)count were conducted under microscope,and prostate tissue slices were pathologically observed. RESULTS:Compared with sham operation group,prostate showed gray nodules,adhesion in glands and surrounding tissue;wet quality of prostate and WBC,SPL count in prostate tissue were significantly increased(P<0.01);under microscope,there were significant congestion,edema and a variety of inflammatory cell infiltration in prostate interstitial. Compared with model group,gray nodules in prostate in Pule'an tablet group and Prostatitis capsule group were reduced,as well as adhesion degree in prostate and surrounding tissue;wet quality of prostate and WBC,SPL count in prostate tissue were significantly decreased(P<0.01);pathological changes had improved to varying degrees under micro-scope,especially the changes in Prostatitis capsule high-dose group,and prostate tissue only showed mild congestion,edema and little inflammatory cell infiltration. CONCLUSIONS:Prostatitis capsule has a certain improvement effect on CNP model rats.