�й�ҩ�þջ�Ʒ�ּ��ӹ�������Ǩ���о�

??Chrysanthemum morifolium has a long history of culture and use in China. Due to different germplasm resources, producing areas, and processing methods, many cultivated varieties have formed now. The varieties and processing methods of C. morifolium are affected by economic interests and processing cost, which change gradually. On the basis of spot investigation and related literature study, the changes of the varieties and processing methods of C. morifolium were summarized in this paper. It will provide theoretical evidence for the culture, processing, quality evaluation, and clinical application of C. morifolium.     

���׿����ؿ�������ţϥ��ָ����¶�̬�仯�о�

??OBJECTIVE To study the monthly dynamics of physical and chemical indexes in Achyranthis Bidentatae Radix(ABR, the dried root of Achyranthes bidentata Bl.) stored in simple and cool warehouses. METHODS ABR was stored in simple and cool warehouses for 27 months. The color was observed. The water content was determined based on the drying method. The contents of ??-ecdysone and 5-hydroxymethylfurfural (5-HMF) were determined by HPLC method. The accumulation of temperature difference between the simple and cool warehouses was evaluated with a relative temperature cumulation (RTC) method. The monthly dynamics of physical and chemical indexes of ABR was analyzed with RTC. RESULTS As the extension of storage time, the ABR stored in the simple warehouse showed deeper color and harder texture, but the ABR stored in the cool warehouse still had soft texture without significant color change. The contents of ??-ecdysone in ABR stored in the two warehouses both gradually decreased and dropped to lower than the limit of 0.030% ruled by China Pharmacopoeia when being stored for up to 27 months. The contents of 5-HMF of ABR stored in the two warehouses both increased and were higher for the sample in the simple warehouse than that in the cool warehouse. CONCLUSION The concept of RTC is put forward and used to study the monthly dynamics of chemical constituents in traditional Chinese medicine during storage for the first time. The physical and chemical indexes of ABR varies during storage. Two years of storage time of ABR is suggested.     

���޴��Ļ�ѧ�ɷ��о�

??OBJECTIVE To study the chemical constituents from Periplaneta americana. METHODS The 95% enthanol extract was isolated and purified by column chromatography on silica gel, Sephadex LH-20, ODS and semi-PHPLC. All compounds were identified by chemical and spectral analyses. RESULTS Fourteen compounds were isolated and purified from Periplaneta americana. Their structures were elucidated as salicylic acid (1), benzoic acid (2), phenylacetic acid (3), methyl 4-hydroxyphenylacetate (4), p-hydroxybenzoic acid (5), genistein (6), 3-hydroxybenzoic acid (7), methyl N-(2-hydroxybenzoyl) glycinate (8), 2,5-dihydroxybenzoic acid (9), (2-hydroxybenzoyl) glycine (10), uracil (11), cyclo(Val-Ala) (12), N-acetyldopamine (13), and cyclo(L-Pro-L-Tyr) (14), respectively. CONCLUSION Compounds 2, 4, 7-10, 12 and 14 are obtained from this genus for the first time.     

����ѿ����Һ��ʽ����ָʾ�����������о�

??OBJECTIVE To establish an oil bath method to determine the D values and Z value of biological indicators in spore suspension forms for moist heat sterilization. METHODS Spore suspension was sealed up in glass capillary, which was heated by thermostat oil bath. D value and Z value were determined by survivor curve method. RESULTS The D values of Geobacillus stearothermophilus ATCC7953 spores suspension at 117, 121 and 125 ?? were 7.04, 2.18 and 0.65 min, respectively, and the Z value was 7.75 ??. The D values of Clostridium sporogenes CMCC(B)64941 spores suspension at 95, 100 and 105 ?? were 11.36, 2.85 and 0.45 min, respectively, and the Z value was 7.14 ??. CONCLUSION By simulating the sterilization of aqueous liquid with oil bath method, the D values and Z values of biological indicators in spore suspension forms for moist heat sterilization can be determined conveniently and accurately(r² is above 0.980 0). The oil bath method can be used for heat resistance research of biological indicators in spore suspension form for moist heat sterilization.     

��֢���߱Ȱ�����Ⱥ��ҩ��ѧ�о�

??OBJECTIVE To research population pharmacokinetics of biapenem in critical patients after repeated dosing. METHODS Blood samples were collected according to the different time points after intravenous administration of 300 mg for many times in the group of critical patients. High-performance liquid chromatography (HPLC) was used to determine the drug concentration in plasma.And pharmacokinetic parameters was caculated. RESULTS The main pharmacokinetic parameters for critical patients were as follows: ??_max was (6.66??2.93)mg??L^-1,T_maxwas (0.51??0.04) h,AUC_0-?? was (18.98??16.95) mg??h??L^-1,T_1/2 was (2.06??1.93) h,Cl was (20.9??17.4) L??h^-1,Vd was (46.43??3.5) L. CONCLUSION The pharmacokinetic parameters of biapenem in critical patients with a significant difference was found in healthy people. So need according to pharmacokinetic characteristics of patients to develop personalized anti-infection plan.     

��ͬ��Դ�����㾫����ԭ��ҩ�������о�

??OBJECTIVE To study the qualities of protamine sulfate raw material from different species of fish. METHODS The identification and determination of protamine sulfate raw material from different fish species were conducted by HPLC, and the composition of amino acids was tested too. Heavy metals was tested by inductively coupled plasma mass spectrometry. The potency of protamine sulfate was measured by biological assay method. RESULTS At present, the sources of protamine sulfate on the market were mainly salmon and herring. CONCLUSION This HPLC method can be applied to effectively identify and determine protamine sulfate raw material in order to improve its quality control.     

�׻��ܽ��ݵĻ�ѧ�ɷ��о�

??OBJECTIVE To study the chemical constituents of Whole Plants of Patrinia villosa (Thunb.) Juss. METHODS Compounds were isolated by a combination of various chromatographic techniques including column chromatography over macroporous resin, Sephadex LH-20 and reversed-phase HPLC. Their structures were elucidated by physiochemical properties and spectral analysis. RESULTS Nine compounds were isolated and identified as (E,4R)-4-hydroxy-4,5,5-trimethyl-3-(3-oxobut-1-enyl)cyclohex-2-enone (1), vomifoliol (2), cis-4-hydroxymellein (3), dehydrovomifoliol (4), 3R,5S,6R,7E,9S-3,5,6,9-tetrahydroxy-7-megastigmane (5), loliolide (6), 4-methoxybenzyl alcohol (7), sphenanthin A (8), and urea (9). CONCLUSION Compounds 1-7 are isolated from Patrinia genus for the first time.     

�������ާ��ѧ�ɷ��о�

??OBJECTIVE To study the chemical constituents from the whole plants of Asplenium unilaterale. METHODS The methanol extract was isolated and purified by silica gel, Sephadex LH-20, and semi-preparative HPLC column chromatography. All compounds were identified on the basis of spectral analysis. RESULTS Fifteen compounds were isolated and identified as (Z)-4-(2,6,6-trimethylcyclohex-2-enylidene)butan-2-ol (1), icariside B₂(2), citroside A(3), (6R, 9R)-3-oxo-??-ionol-9-O-??-D-glucopyranoside(4), (6S,9R)-roseoside(5), 6-methyl-2H-chromen-2-one (6), 6,7-dihydroxy-2H-1-benzopyran-2-one (7), gibepyrone D(8), lupan-3-one(9), violanthin(10), 22,23-dimethylcholest-5-en-3-ol(11), 1-dotriacontanol (12), 5-hexylfuran-2(5H)-one(13), tocopherylquinone(14) and 2,4(1H,3H)-pyrimidinedione(15), respectively. CONCLUSION Compounds 1-15 are isolated from the genus for the first time.     

��ѩ�����ն�����Ƥ���������Ĵ����������о�

??OBJECTIVE To investigate the treatment effects of chronic ulcer in diabetic rats with asiaticosides.METHODS Totally 38 male CL grade SD rats were randomly divided into normal group and model group, and were feed in metabolic cage separately. The low (22.29 mg??cm^-2), medium (111.45 mg??cm^-2) and high (222.93 mg??cm^-2) dose of centella triterpenes cream were characterized and tested on excision ulcer wounds of streptozotocin-induced diabetic rats. After treatment, the weight, blood glucose, water intake and total urine output were measured in 3, 7, 10 and 14 d respectively. The wound healing rate was evaluated by image processing software of Adobe Photoshop CS5. Histopathological studies were conducted on the healed wound tissues to observe for epithelisation, fibroblast proliferation and angiogenesis. RESULTS It was found that at all time points the areas of wounds treated with asiaticosides were smaller compared with the controls. The expression of weight, water intake, total urine output and blood glucose increased statistically in the model group (P<0.05).Pathological results showed much better healing efficacy for the test samples compared with the control ones(P??0.05). The middle dose of centella triterpenes cream was the best (P<0.01). Histopathological studies had also shown that centella triterpenes cream treated wounds exhibited re-epithelisation, higher fibroblast proliferation, collagen synthesis, and angiogenesis. At 14 days post excision, the medium centella triterpenes cream treated group achieved complete repair. CONCLUSION These findings suggest that asiaticosides may have a potential application in the treatment of diabetic ulcers and chronic wound healing.     

��Ī���ֳ���Ƭ���Ʊ����������ͷ������о�

??OBJECTIVE To prepare amoxicillin enteric-coated tablets and study the in vitro release properties. METHODS The drug-containing pellets were prepared by extrusion-spheronization process. Taking the cumulative release at 15 min as the response value, the optimization test was performed using the common rotation combination design and the optimal formulation was validated. The drug-containing pellets were coated with Eudragit L30D-55 to prepare enteric-coated pellets. The effects of different coating weight gains on the release characteristics of enteric-coated pellets, different amounts of plasticizer on the release characteristics of enteric-coated pellets and tablets, and different hardness of tablets on the release characteristics of enteric-coated tablets were investigated by single factor method. RESULTS The optimal formulation of the drug-containing pellets determined by response surface analysis method included 5% of croscarmellose sodium, 1.2% of polyoxyethylene 35 castor oil and 1% hydroxypropyl cellulose. The predictive value of the cumulative release at 15 min was close to the measured value. The coating weight gain of Eudragit L30D-55 should be about 20%, the amount of plasticizer should be 30% of solid content of Eudragit L30D-55, and the hardness of tablets was (130??20)N. CONCLUSION It is reasonable and reliable to optimize the formulation of drug-containing pellets by response surface analysis method. The enteric-coated tablets have good delayed release effect, and this product has the feasibility of industrial production.     

PLGA-克班宁纳米粒的制备、表征及体外释药规律分析

目的:制备并表征聚乳酸-羟基乙酸共聚物(PLGA)-克班宁纳米粒(PLGA-Cre-NPs),考察其体外释放特性,为克班宁的体内作用时间延长、毒性降低提供参考。方法:以PLGA为载体,采用乳化溶剂扩散法制备PLGA-Cre-NPs。以包封率、粒径、多分散指数(PDI)为评价指标,通过星点设计-效应面法优选PLGA-Cre-NPs的制备工艺。利用膜透析法考察PLGA-CreNPs的体外释药规律。结果:PLGA-Cre-NPs的最佳制备工艺为有机相与水相体积比(3∶10),丙酮-无水乙醇(8∶2),PLGA投入量90 mg。PLGA-Cre-NPs的包封率(84.69±2.54)%,粒径(155.3±14.2)nm,PDI=0.095±0.018,扫描电镜显示其呈规则球形结构。PLGA-Cre-NPs体外释放包括速释和缓释2个阶段,0~24 h符合Weibull方程,24~168 h符合Higuchi方程;半衰期18.06 h,168 h时累计释放率达78.77%。结论:优选的工艺条件稳定可行。制得的PLGA-Cre-NPs包封率较高、粒径均匀,有望制备成缓释制剂。     

�׷�˾ͪθ��������΢��Ƭ���Ʊ�����������ҩ�о�

??OBJECTIVE To prepare mifepristone gastric retentive multi-unit pellet system (MUPs), and study its release behaviors in vitro. METHODS A sustained release layer and mucous adhesive layer were coated onto extrusion spherized mifepristone pellets. The gastric retentive sustained release pellets were mixed with granules which were wet granulated from micronized mifepristone and compressed into MUPs tablets. Investigation and evaluation of the in vitro release of mifepristone MUPs tablets were carried out from different aspects.RESULTS The turning point of pH value for the solubility of mifepristone was 3.0.Micronized mifepristone showed higher dissolving rate and apparent solubility.The gastric retentive mifepristone MUPs tablets had faster release than marketed mifepristone tablets. The in vitro adhesive experiment with pig stomach showed that mucous adhesive mifepristone pellets could be entrapped into the gastric mucous and retained for a long time. The accelerated stability study showed that mifepristone MUPs tablets were as stable as marketed mifepristone tablets.CONCLUSION Novel mifepristone gastric retentive MUPs tablets are successfully prepared.The release characteristics in vitro indicate that the product may have higher bioavailability than marketed mifepristone tablets with significantly lower variability.     

槲皮素-PLGA嵌段共聚物纳米粒冻干粉的制备及体外释放性能考察

目的:制备槲皮素-(聚乳酸-羟基乙酸共聚物)嵌段共聚物(QC-PLGA)纳米粒冻干粉并考察其体外释放规律。方法:采用乳化溶剂挥发法制备QC-PLGA纳米粒,通过正交试验确定最优处方工艺,通过单因素试验筛选冻干保护剂,通过动态透析技术考察QC-PLGA纳米粒冻干粉的体外释药规律。结果:最佳制备工艺为0.2%聚乙烯醇,PLGA质量浓度10 g·L~(-1),油/水相体积比1∶35,槲皮素用量5 mg,冻干保护剂为2%乳糖。QC-PLGA纳米粒冻干粉的外表光滑,形态无皱缩塌陷、结构致密且加入注射用水振摇后再分散性良好,体外释放规律基本符合Weibull方程的释药模型,释药动力学方程ln[ln(1/1-Q)]=0.399lnt-1.503(R~2=0.973)。结论:QC-PLGA纳米粒冻干粉制备工艺简单可行、性质稳定、易储存,相比槲皮素原料药具有明显的缓释作用。     

���ỷ��ɳ��θƯ������Ƭ����ơ��Ʊ�����������

??OBJECTIVE To investigate the effect of polymers , including hydrophilic polymers and swelling aids, on floatability and dissolution of ciprofloxacin hydrochloride gastro-retentive tablets. METHODS Hydroxypropyl methyl cellulose (HPMC),hydroxyethylcellulose (HEC ) and hydroxypropylcellulose (HPC) were used as hydrophilic swelling excipients , and disintegrants crospovidone (PVPP XL and PVPP XL-10) or croscarmellose sodium (CCS) were used as swelling agents to facilitate the swelling /floating and drug release. Initial floating time and floating duration were tested to evaluate buoyance, and drug dissolution was tested to evaluate the controlled release. RESULTS Using HPMC K250 and PVPP XL as excipients for ciprofloxacin hydrochloride gastro-retentive tablets could obtain products with rapid onset of floating, long floating durion and desirable drug release. CONCLUSION Variety and amount of polymers have dramatic effects on buoyance and drug release of gastro-retentive tablets. HPMC K250 and PVPP XL are suitable excipients for ciprofloxacin hydrochloride gastro-retentive tablets.     

紫花牡荆素壳聚糖微球的制备及体外释药性能考察

目的:制备紫花牡荆素壳聚糖微球,优化其制备工艺,并考察其体外释放性质。方法:以山梨糖醇酐单油酸酯和聚山梨酯-80为乳化剂,液体石蜡为油相,戊二醛作交联剂,采用乳化交联法制备紫花牡荆素壳聚糖微球。利用Design-Expert8.0.6软件优化紫花牡荆素壳聚糖微球的制备工艺,扫描电镜观察目标微球形态,动态透析法检测目标微球的体外释药性能。结果:紫花牡荆素壳聚糖微球最佳制备工艺条件为油水相比例6∶1,交联时间3 h,转速1 400 r·min~(-1);目标微球形态较圆整、粒径分布较为均匀,平均粒径7.92μm,载药量29.20%,包封率39.23%。紫花牡荆素壳聚糖微球在4 h的药物累计释放率26.75%,之后释药平缓,释放变慢,48 h的药物累计释放率95%。微球在磷酸盐缓冲溶液(pH 7.4)中的释放遵循Higuchi方程。结论:优化的制备工艺简单易行。紫花牡荆素壳聚糖微球载药量较高,具有一定的缓释作用。     

左金胃漂浮-生物黏附小丸的制备及体外释放度考察

目的:优选左金胃漂浮-生物黏附小丸的制备工艺并考察其体外释放度。方法:以盐酸小檗碱释放度为考察指标,采用单因素试验优选左金胃漂浮-生物黏附小丸丸芯的处方组成,以丸芯的圆整度和收率为评价指标,利用正交试验优化挤出滚圆的工艺参数,丸芯用卡波姆和碳酸氢钠的混合溶液包衣。结果:以羟丙甲纤维素(HPMC K4M)为骨架材料,微晶纤维素(MCC PH301)为成球材料和崩解剂,碳酸氢钠为助漂材料,以挤出速度30 r·min-1,滚圆速度800 r·min-1和滚圆时间20 min制备丸芯,包衣后的左金胃漂浮-生物黏附小丸均能在1 min内起漂,10 h时持续漂浮率约80%,生物黏附率83.7%~86.8%,主要成分盐酸小檗碱在12 h的累积释放率90%。结论:制备的左金胃漂浮-生物黏附小丸外观均匀,具有良好的释放性能,且工艺简单易行、生产成本低。     

新型利培酮PLGA微球的制备及体外释放研究

 目的 制备新型利培酮微球,并快速评价微球的体外释放性质。方法 采用O/W乳化溶剂挥发法制备微球,研究PLGA浓度、乳化均质转速、油相与水相比例等对微球粒径和包封率的影响。通过升高释放介质温度建立体外释放加速评价方法。结果 在37 ℃ pH 7.4 PBS中,利培酮微球以零级释放模式缓释15 d,快速释放的时间与上市利培酮微球基本一致而无延滞期。采用45 ℃加速释放可提高释放速度5倍,在3 d内完成评价,加速释放评价与长期释放相关性好。结论 本实验所制备的利培酮微球,可开发为释放两周的制剂。由于无延滞期,在临床使用和提高患者顺应性上比已上市产品更具优势。加速评价方法可对产品进行快速质量控制。     

������/�����˫��ҩ���������Ʊ���������ҩ���о�

??OBJECTIVE To prepare calcitonin/puerarin-PLGA-dual-loaded nanoparticles modified by chitosan, and investigate theirin vitro release behavior.METHODS CS-CT/PR-NPs were prepared by the double emulsion solvent evaporation technique with PLGA as a carrier material; the formulation of CS-CT/PR-NPs was optimized by orthogonal design; the morphology of CS-CT/PR-NPs was observed by transmission electron microscope;the mean particle size,particle size distribution and Zeta potential were measured by laser particle size analyzer; the entrapment efficiency and drug loading were measured by ultracentrifugation; the in vitro release behavior was studied by dialysis. RESULTS CS-CT/PR-NPs were spherical in shape with the mean particle size of(190??2.65) nm, particle size distribution of (0.117??0.027) and Zeta potentialof(16.5??1.08) mV. The entrapment efficiency was (75.7??1.15)%, and the drug loading of CT was (3.47??0.31)%, while those of PR were (50.9??1.08)% and (4.68??0.19)%, respectively. The profiles of in vitro release had the features of sustained-release. CONCLUSION CS-CT/PR-NPs are prepared successfully and show a sustained-release characteristic with high entrapment efficiency, which may improve the oral bioavailability of CT and provide the experimental reference for preparing the dual-loaded nanoparticles.     

斑蝥素载药胶束的制备及其体外释药性能考察

目的:制备pH敏感斑蝥素聚合物胶束纳米制剂,以提高斑蝥素在水中的溶解度,并考察该制剂在弱酸性条件下的体外释药特性。方法:以聚乙二醇-聚乳酸共聚物[poly(ethylene glycol)-b-polylactide,PELA]和聚乙二醇-聚乳酸-聚(β-氨基酯)[poly(ethylene glycol)-b-polylactide-b-poly(β-amino ester),PELA-PBAE]为载体,采用薄膜水化法制备斑蝥素胶束。通过透射电子显微镜观察胶束的微观形态,采用粒度分析仪测定粒径,HPLC测定其载药量和包封率,透析袋透析法测定纳米胶束在不同p H条件下的释放特性。结果:斑蝥素胶束呈明显的球状结构,PELA载药(PELA-C)胶束和PELA-PBAE载药(PELAPBAE-C)胶束的粒度分别为21.6,21.2 nm,且至少在5 d内稳定;载药量分别为1.68%和1.72%,包封率分别为92.0%和88.8%;在p H 5.5下的8 h累计释放率分别为24.7%和79.1%,在p H 6.5下的8 h累计释放率分别为13.6%和50.0%,在p H 7.4下的8 h累计释放率分别为10.2%和13.9%。结论:PELA-PBAE作为纳米载体能明显提高斑蝥素的水溶性,体外释药具有显著的p H响应性能,在抗肿瘤药物的开发方面具有较好的应用前景。