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??OBJECTIVE To prepare capsaicin-solid lipid nanoparticles (CAP-SLNs) and study their physical and chemical properties. Then, the CAP-SLNs were modified with chitosan (CTS) and the pharmacokinetics across colon of rats was studied in vivo. METHODS CAP-SLNs were prepared by emulsion-solvent evaporation method. The mean size, encapsulation efficiency and drug loading of the nanoparticles were investigated. RESULTS The average diameter of CAP-SLNs was (118.89??25.0) nm, the encapsulation efficiency was (38.56??2.6)%, and the drug-loading was (6.17??0.21)%. After colon-specific delivery in rats, the AUC_{0-360 min}(243.63??61.46) mg??min??L^-1 and ??_max(1.23??0.18) mg??L^-1 of CTS-CAP-SLNs were 1.81-fold and 1.95-fold higher than CAP. CONCLUSION It is simple and feasible to prepare CAP-SLNs by emulsion-solvent evaporation method. The pharmacokinetic parameters in rats are improved remarkably compared with CAP.     

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??OBJECTIVE To investigate and analyze the rational use of apatinib in cancer hospital. METHODS Retrospective study was applied. Through reviewing medical records, the patient's basic information, drug therapy information and adverse drug effects were collected and analyzed. RESULTS Apatinib is mainly used in patients with advanced metastatic gastric or esophagogastric junction cancer who have failed at least two chemotherapeutic regimens. The clinical common dose of apatinib was 0.25 or 0.5 g, less than the dose of 0.85 g recommended in drug instruction. CONCLUSION Apatinib is a new choice for gastric or esophagogastric junction cancer. It has demonstrated tolerable adverse effects in these patients.However, at present, more attentions should be paid to possible effect of drug dose on clinical outcome.     

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??OBJECTIVE To prepare and characterize paroxetine resinate, and evaluate the in vitro drug release rate and taste-masking effect. METHODS A full factorial design was first conceived and applied to screen some process and formulation parameters (reaction temperature, stirring speed, drug concentration in solution and the ratio of resin to drug) on the key responses of resinationprocess, such as drug utilization ratio, drug loading and complexation constant. The paroxetine resinate was then characterized and evaluated by scanning electronic microscope (SEM), differential scanning calorimetry (DSC), in vitro drug release test and panel test of taste-masking. RESULTS The resin/drug ratio and reaction temperature were identified as the most important factors on paroxetine resinate preparation.The drug-resin complex was successfully formed via ion exchange mechanism rather than physical absorption with complete in vitro drug release (>96%) in acidic or salt solution and good taste-masking effect.CONCLUSION Paroxetine resinate with good performance can be prepared via optimization of process and formulation parameters, which will facilitate the development of generic paroxetine suspension.     

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??OBJECTIVE To evaluate the pharmacokinetic properties and bioequivalence of two crystal forms of rifampicin. METHODS Drawing the dissolution curves of reference and test medicines in different solutions,and calculated the value of f₂. Twenty-nine healthy male volunteers were randomly administered in a crossover single 300 mg dose of reference and test medicines. Determining the concentration of rifampicin in plasma by HPLC-MS,and analyzed the relative bioavailability and bioequivalence of tablets using SAS program. RESULTS The values of f₂ were more than 50. The pharmacokinetic properties of reference and test tablets were as followsAUC_0→t:(28 476±8 050) vs (28 120±6 916) ng·mL·h^-1,ρ_max:(5 552±1 554) vs (5 911±1 700)ng·mL^-1,t_max:(2.0±1.0) vs (1.8±1.0)h,t_1/2:(2.8±0.5)vs(2.8±0.5)h. 90% CI of AUC and ρ_max of test medicine were 96.2%-106.4% and 98.6%-115.3%,respectively. And there were no significant difference of the t_max of rifampicin between the two medicines(P>0.05). CONCLUSION The results indicate that the two medicines made from rifampicin two crystal forms are bioequivalent completely.     

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??OBJECTIVE To prepare montelukast sodium orally disintegrating tablets and investigate the bioequivalence in Beagle dogs.METHODS The orally disintegrating tablets were prepared by direct compression method,and the optimal formulation was screened by orthogonal test.HPLC-fluorescence method was developed for determination of montelukast sodium plasma concentration in Beagle dogs.RESULTS The optimized formulation(1 000 tablets) was montelukast sodium 10.4 g, microcrystalline cellulose 60 g, cross linked povidone 30 g, mannitol 15 g, magnesium stearate 2 g, aerosil 1 g, aspartame 1 g, flavor 0.6 g.CONCLUSION Montelukast sodium orally disintegrating tablets made of the optimized formulation could disintegrate rapidly. Relatively bioavailability of montelukast sodium orally disintegrating tablets is 90.7%.     

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??OBJECTIVE To investigate the chemical constituents from the stems of Lythrum salicaria L..METHODS The constituents were isolated and purified by silica gel, Sephadex LH-20 column chromatography, and TLC. The structures were identified on the basis of spectral data and physiochemical characteristics. RESULTS Twenty compounds were isolated from 70% ethanol extracts and identified as betulinic acid(1), 2??,3??,24-trihydroxy-12(13)-en-urs-28-oic acid(2), 6-O-(E)- sinapoylpoligalitol(3), feruloyl-6??-O-??-D-glucopyranoside(4), 7-oxo-??-sitosterol(5), en-tisolariciresinol(6), muramine(7), aesculetin(8), apigenin(9),(2E,6S)-2,6-dimethyl-6-O-??-D-xylpyranosyloxy-2,7-menthiafolic acid(10), quercetin3-O-(6??-caffeoyl)-??-D-galactopyranoside(11), cycloart-23-ene-3??,25-diol(12), (1??S,6??R)-8??-hydroxyabscisic acid-??-D-glucoside(13), 3??,5-dihydroxy-3,6,4??-trimethoxyl-7-O-??-D-glucopyranoside flavonoid(14), aurantiamide acetate(15), 5,6,3??,4??-tetrahydroxy-3,7-dimethoxy-flavone(16), ursolic acid(17), oleanolic acid(18), 4-O-11-methyl-oleoside-p-hydroxyphenyl-(6??-11-methyloleoside)-??-D-glucopyranoside(19), and 6-O-galloylarbutin(20). CONCLUSION Except for compounds 8 and 9, all the compounds were isolated from this plant material for the first time.
     

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??OBJECTIVE To study the pharmacokinetics and bioequivalence of hydroxysafflor yellow A (HSYA) and hydroxysafflor yellow A nanoemulsion (HYAN) in rats.METHODS Twelve male rats were randomly divided into two groups. The rats were administered intragastrically with HSYA or HYAN, respectively, and then blood was collected from the venous plexus at different time points. HPLC method was used for the determination of HSYA blood concentration.RESULTS The main pharmacokinetic parameters of HYAN were as follows: the area under curve (AUC_{0-24 h}), peak concentration (??_max), peak time (t_max) and clearance (CL) were (31.56??4.58) mg??L??h^-1, (12.75??2.64) mg??L^-1, (0.83??0.54) h and (1.89??0.93) L??h^-1??kg^-1, respectively. The AUC_{0-24 h}, ??_max and t_max of HYAN increased by 5.49, 10.22 and 2.50 times, respectively, and the CL of HYAN was only 1/4 of that of HSYA. The 90% confidence intervals for AUC_{0-24 h} and ??_max were not within the prescribed range of bioequivalence criteria.CONCLUSION Relative to HSYA, the high plasma concentration and prolonged peak time of HYAN in vivo can significantly improve the oral bioavailability of HSYA. HSYA solution and HYAN are not bioequivalent.     

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??OBJECTIVE To investigate whether there is significant difference between the GLP-1-Fc fusion protein(YD057) that is expressed by gene recombination and the marketed drug dulaglutide(Lilly). METHODS SDS-PAGE, SEC, CE-SDS and CIEF were used to analyze the differences in molecular weight, purity and charge heterogeneity. The amino acid sequence, biological activity and receptor binding analysis were measured to assess whether the cytological function and molecular binding capacity were consistent. Oligosaccharide distribution was measured to assess whether N-linked glycosylation modification ratio was consistent. RESULTS There was no significant difference in physicochemical properties, amino acid primary sequence, N-linked glycosylation modification ratio, cell biology function and receptor binding capacity between the biological similar drugs(YD057) and dulaglutide. CONCLUSION Their critical quality attributes are basically the same.     

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??OBJECTIVE To prepare ion-sensitive ophthalmic in situ gel containing bendazac lysine (BDZL-ISG) and preliminarily study its rheological behavior, in vitro drug release, corneal permeation, and pharmacokinetics in rabbit aqueous humor. METHODS Single factor investigation was carried out to optimize the formulation, taking viscosity and gelling capacity as evaluation indices. Using aqueous solution or eye drops as control, the in vitro release of the formulation was evaluated by dialysis membrane method. Then, the corneal permeation experiment of the optimum formulation was carried out with Franz diffusion cell. The pharmacokinetics of BDZL-ISG in rabbit aqueous humor was preliminarily studied by microdialysis. RESULTS Compared with the control group, the optimum formulation had shear thinning behavior and significant sustained release effect. There was no significant difference in the corneal permeation between the two groups. The RESULTS of pharmacokinetic study showed that ??_max (13.25 ??g??L^-1) and AUC_0-t of BZDL-ISG were 2.38 and 2.2 times higher than those of BDZL eye drops respectively, which suggested that the ocular bioavailability of BDZL was greatly enhanced by the optimum in situ gel formulation. CONCLUSION With significant sustained release effect, the ion-sensitive ophthalmic in situ gel will become a promising alterative formulation for bendazac lysine for treatment of cataracts.     

天麻液相色谱指纹图谱研究

目的建立天麻的液相色谱指纹图谱,为科学评价及有效控制天麻质量提供新方法。方法采用HPLC法分析不同产地的18个天麻样品,确定指纹峰并进行对照药材相似度、共有模式相似度的计算,用纯品随行对照结合LC-MS对主要指纹峰进行定性鉴定。结果建立了由27个指纹峰和17个共有峰组成的天麻液相色谱指纹图谱,指纹峰具有特征性,鉴定了其中12个主要的指纹峰。用对照药材相似度,可将天麻样品分为3类安徽河南产天麻、陕西四川产天麻和云南产天麻。两个相关系数分界点为0.80和0.58,夹角余弦分界点为0.88和0.73。结论所选指纹峰有特征性,建立的指纹谱可用来区别3个产地的天麻药材,并为进一步控制天麻质量提供依据。     

天麻的化学成分研究（II）

目的 研究天麻Gastrodia elata的化学成分。方法 利用柱色谱、凝胶柱色谱、高效液相色谱等各种色谱技术对天麻50%乙醇提取物进行分离,根据其所得化合物的理化性质与UV、IR、MS、NMR等光谱数据鉴定其结构。结果 从天麻50%乙醇提取物中分离得到9个化合物,分别鉴定为1-furan-2-yl-2-(4-hydroxy-phenyl)-ethane-1, 2-dione（1）、2, 4-bis (4-hydroxybenzl)-phenol（2）、4-(甲氧甲基)苯基-1-O-β-D-吡喃葡萄糖苷（3）、1-furan-2-yl-2-(4-hydroxy-phenyl)-ethanone（4）、巴利森苷B（5）、巴利森苷C（6）、{1-[4-(β-D-吡喃葡萄糖-(1→3)-β-D-吡喃葡萄糖氧)苄基], 2-[4-(β-D-吡喃葡萄糖氧) 苄基]}柠檬酸酯（7）、bis (4-hydroxybenzyl) sulfide（8）、对羟基苄基二硫醚（9）。结论 化合物1为未见报道的新化合物,命名为天麻呋喃二酮,化合物9为该属植物中首次分离得到。     

天麻饮片等级研究

探讨天麻饮片等级分类方法。在文献研究及产地调研的基础上,结合传统评价和现代评价方法综合评价天麻饮片,并对其进行等级分类。根据调研,天麻药材已有等级分类,饮片大都以统货形式销售;所调查的中药饮片生产企业、医院及药房销售的天麻饮片并未分级;对已分级的饮片一般只有一级和统货2个等级,而只有冬麻加工的饮片有分级。天麻饮片等级的综合评价有助于提高饮片质量,实现"优质优价",该研究可为其他中药饮片的等级划分提供思路和借鉴。     

天麻花茎的化学成分研究

目的 研究天麻Gastrodia elata花茎的化学成分。方法 利用硅胶、Sephadex LH-20等各种色谱技术进行分离纯化,通过核磁图谱、IR、UV、质谱等多种方法并结合文献对分离得到的化合物进行结构鉴定。结果 从天麻花茎95%乙醇提取物的醋酸乙酯萃取物中分离得到13个化合物,分别鉴定为(S)-6,12-二羟基-9-甲氧基-3,3-二甲基-8,9-二氢-3H,7H-苯并[2,3]氧杂?并[4,5-b]吡喃并[2,3-h]苯并吡喃-7-酮（1）、2-(2,4-二羟基苯基)-5-羟基-3-(2-羟基-3-甲基丁-3-烯-1-基)-8,8-二甲基-4H,8H-吡喃并[2,3-f]苯并吡喃-4-酮（2）、桑黄酮C(3)、黑桑素H(4)、新环桑色烯（5）、morusin hydroperoxide(6)、桑辛素（7）、licofavone C(8)、环桑素（9）、交链孢酚（10）、3,4-dihydroxy-benzoic(11)、对羟基苯甲醇（12）、N-trans-grossamide(13)。结论 化合物1为新化合物,命名为降环桑色烯;化合物2～9为首次从该植物中分离得到。     

天麻药理研究新进展

综述了关于天麻药理研究的英文文献。这些文献主要研究了天麻对中枢神经系统的作用,包括抗惊厥、神经保护和改善学习记忆等方面。上述药理作用与其多种酚性成分密切相关。     

天麻中糖基转移酶基因GeGT1的克隆及原核表达分析

目的 克隆天麻糖基转移酶基因(glycosyltransferase,GeGT1)的全长cDNA序列,进行序列分析和原核表达分析,并探究该基因在天麻不同器官中的表达规律.方法 在天麻转录组数据库中通过注释和比对,用Primer Premier 5.0软件设计基因特异性引物.通过反转录聚合酶链式扩增(reverse tr...     

基于SRAP分子标记的天麻遗传多样性研究

目的 利用SRAP分子标记技术对天麻种质资源进行遗传多样性研究,为天麻不同亲缘物种间的分类及其优良种质资源的筛选提供依据。方法 采集7个不同生态区域的天麻种质资源,包括红杆G.elata f.elata、乌杆G.elata f.glauca和绿杆G.elata f.viridis 3种变型和红乌杂交天麻,共24份样品。运用SRAP分子标记方法构建天麻种质的DNA指纹图谱,从分子水平检测其遗传多样性。结果 33对引物扩增出637条多态性条带,多态性百分率达73.16%。24份天麻种质样品间相似度分布于0.404 0~0.908 0,整个群体之间的相似程度差异较大。其中红天麻样品间的相似度在0.906 6~0.996 4,遗传差异较小;乌天麻、杂交天麻和绿天麻样品间的相似度分别在0.410 4~0.999 6、0.541 0~0.950 4和0.578 2,遗传差异较大。AMOVA分析结果显示,天麻变型内变异大于变型间变异,天麻各变型间有很大的遗传分化(FST=0.33,P<0.05)。另外,人工栽培对遗传分化有影响,但不显著。结论 SRAP分子标记方法得到的24份天麻样品多态性丰富,能有效地反映出天麻的遗传多样性。红杆天麻的遗传性状较为稳定,与其他变型间缺乏基因交流,遗传多样性匮乏;其他2个变型具有较高的遗传多样性。     

天麻防治神经精神疾病的研究进展

天麻是我国名贵中药材,在治疗头痛、改善学习记忆、抗抑郁等神经精神药理方向均显示良好的作用。通过查阅CNKI和Pub Med两大常用数据库的相关文献资料,对10年来天麻的神经精神药理作用及相应的药效物质基础进行了归纳分析,并结合国家食品药品监督管理总局官网,查询天麻相关药品与保健品开发情况,为天麻防治神经精神疾病产品研发提供参考。     

RP-HPLC同时测定天麻中4种成分的含量

目的：建立RP-HPLC同时测定天麻药材中天麻素、腺苷、对羟基苯甲醇和对羟基苯甲醛的含量。方法：采用Kromasil C₁₈色谱柱(4.6 mm×250 mm,5 μm),以甲醇-0.1%醋酸水溶液为流动相,梯度洗脱,流速1.0 mL·min^-1,检测波长270 nm,柱温35 ℃。结果：天麻素、腺苷、对羟基苯甲醇和对羟基苯甲醛分别在19.1～383 μg·mL^-1(r=0.999 9),0.620～12.4 μg·mL^-1(r=0.999 9),2.45～49.0 μg·mL^-1(r=0.999 9),0.280～5.63 μg·mL^-1(r=0.999 6)与峰面积线性关系良好;平均加样回收率(n=9)均在96.7%～97.7%,RSD均小于1.6%。结论：本法准确可靠,分离度好,适用于天麻药材中天麻素、腺苷、对羟基苯甲醇和对羟基苯甲醛的含量测定。     

乌天麻二氯甲烷萃取部位化学成分及其胆碱酯酶抑制活性的研究

目的 研究乌天麻Gastrodia elata二氯甲烷萃取部位的化学成分及其胆碱酯酶抑制活性。方法 采用Ellman法测定了二氯甲烷萃取部位对乙酰胆碱酯酶（acetyl cholinesterase,AChE）和丁酰胆碱酯酶（butyryl cholinesterase,BuChE）的抑制活性;利用硅胶柱色谱、Sephadex LH-20柱色谱、半制备高效液相色谱等方法进行分离纯化;利用NMR、MS等技术鉴定化合物结构;测定所有单体化合物的胆碱酯酶抑制活性。结果 乌天麻二氯甲烷萃取部位对AChE和BuChE均有显著的抑制活性,半数抑制浓度（median inhibition concentration,IC₅₀）分别为10.45、9.20μg/mL;从中分离得到11个化合物,分别鉴定为环[甘氨酸-l-S-(4''-羟基苯基)半胱氨酸]（1）、5''-甲硫基腺苷（2）、对羟基苄胺（3）、对羟基苯甲醇（4）、对羟基苯甲醛（5）、2-甲基-3-羟基吡啶（6）、4-乙酰氧甲苯基-β-D-吡喃葡萄糖苷（7）、4-(乙氧基甲基)苯酚β-D-吡喃葡萄糖苷（8）、小檗碱（9）、(＋)-thalirugidine（10）和(＋)-海兰地嗪（11）。结论 化合物1～3和9～11为首次从天麻属中分离得到。化合物9（IC₅₀＝5.93μmol/L）和10（IC₅₀＝42.49μmol/L）对AChE有抑制活性,化合物10（IC₅₀＝21.20μmol/L）对BuChE有抑制活性。