动态流变实验评价温敏凝胶的方法研究

 目的应用动态流变实验测定温度敏感原位凝胶的流变性质,以预测其在体胶凝(相变)行为。方法以泊洛沙姆407 (P407)为基质制备地塞米松温度敏感原位凝胶(DSP-gel)。采用动态流变实验测定DSP-gel在不同温度下及相变过程中的流变参数,并与P407相比较。应用差示扫描量热法(DSC)测定DSP-gel胶凝温度。结果DSP-gel在低温时为黏弹性流体,温度升到27℃时开始胶凝,并在体温条件下保持凝胶状态。相转变表现为模量呈指数增长,全部过程约在7℃内完成。DSC测得相变温度为26.58℃,与流变学得到结果一致。结论动态流变实验能表征温敏凝胶的黏弹性流体力学性质,可用于体外评价。     

丹葛眼用即型凝胶及其普通凝胶的流变学特性评价

目的 应用动态流变实验评价丹葛眼用即型凝胶及其普通凝胶的流变学特性。方法 以泊洛沙姆为材料制备丹葛眼用温敏即型凝胶,以卡波姆为材料制备其普通凝胶。采用安东帕MCR302流变仪测定上述2种凝胶在不同温度下的流变学参数,并推测即型凝胶的胶凝温度及胶凝时间。结果 丹葛眼用即型凝胶在低温条件下以流体性质为主,黏性模量占主导,为牛顿流体;温度升至室温以上可快速发生相转变,形成凝胶状态,呈假塑性流体,有剪切变稀的性质;该即型凝胶的凝胶温度为（24.4±0.1）℃,胶凝时间为9 s。而丹葛普通凝胶以网状结构存在,在一定温度范围内,凝胶结构稳定,不随温度的变化而改变。结论 建立了丹葛眼用即型凝胶及其普通凝胶的流变学评价体系,运用动态流变学参数可更准确、科学地评价上述2种凝胶的流变学特性,为样品的全面质量控制提供参考依据。     

苦茶妇科凝胶的工艺研究及流变学参数考察

目的考察苦茶妇科凝胶的制备工艺,制备出在阴道环境中能够快速发生相变的温度敏感型原位凝胶。方法泊洛沙姆P188、P407为凝胶基质,乳酸、乳酸钠为酸缓冲溶液,采用星点设计法筛选原位凝胶的处方工艺,并测定其胶凝温度、胶凝时间、不同酸缓冲溶液对胶凝温度的影响、凝胶稳定性及相关流变学性质。结果在一定用量范围内,泊洛沙姆P188用量增大胶凝温度逐渐升高,泊洛沙姆P407用量增大胶凝温度逐渐下降,通过星点设计优化处方为泊洛沙姆P188的用量为3.51%,P407的用量为17.16%;在体外实验中,不同缓冲液的加入对凝胶的胶凝温度影响偏差在5%以内,但在阴道液中的影响偏差较大,柠檬酸-柠檬酸钠缓冲液在阴道液中的胶凝温度为68.5℃,乳酸-乳酸钠缓冲溶液在阴道液中的胶凝温度为35.8℃;流变学数据表明凝胶在体内滞留性好。结论苦茶妇科凝胶处方工艺符合星点设计模型,筛选工艺可制备出滞留性好,性质稳定的原位凝胶。     

黄芩苷外用温敏凝胶的处方设计及优化

目的: 通过不同数学模型及评价指标优选黄芩苷外用温敏凝胶的处方. 方法: 以泊洛沙姆407,188为凝胶基质,以胶凝温度为指标比较全样本多元线性模型及星点设计-效应面法优选的黄芩苷外用温敏凝胶处方.以胶凝时间及凝胶长度为评价指标进行处方优化. 结果: 星点设计-效应面法优选的处方置信度较高.黄芩苷外用温敏凝胶的最优处方为1%黄芩苷,17%泊洛沙姆407和1.5%泊洛沙姆188;胶凝温度、胶凝时间及凝胶长度分别为(30.3±0.1) ℃,(18.9±1.9) s,(0.7±0.6) cm. 结论: 制备的黄芩苷外用温敏凝胶符合局部迅速富集、提高患者顺应性的要求,指标评价应以人体测定的结果为准,为外用温敏凝胶的处方优选提供参考.     

可注射参麦温度敏感型原位凝胶的制剂学评价

目的:制备可注射用参麦温度敏感型原位凝胶制剂,并考察其体外释放特性.方法:采用冷溶法制备参麦温度敏感型原位凝胶制剂,HPLC测定入参皂苷Rb1含量,以透析法研究参麦温度敏感型原位凝胶的体外释放特性,并利用药物释放模型方程拟合释放曲线.结果:参麦温度敏感型原位凝胶的胶凝温度34.92℃,相应黏度1 579.52 mPa·a,胶凝时间110.67 s.随温度升高,该原位凝胶由牛顿流体转变为假塑性流体,其体外释放行为符合一级动力学方程.结论:参麦温度敏感型原位凝胶具有温敏特性及明显的缓释作用.     

温度敏感型盐酸小檗碱眼用原位凝胶的制备研究

目的 制备温度敏感型盐酸小檗碱眼用原位凝胶.方法 以泊洛沙姆407和188为温敏材料,采用搅拌子法测定溶液-凝胶相转变温度优化处方;采用高效液相色谱法测定盐酸小檗碱.结果 温度敏感型原位凝胶的胶凝温度随泊洛沙姆407浓度增大而降低,随泊洛沙姆188浓度增加先升高后降低,模拟泪液的稀释可使胶凝温度升高,建立了泪液稀释后相变温度与泊洛沙姆浓度的拟合方程,经Design-Expert软件优化盐酸小檗碱温敏型眼用原位凝胶的处方为25%泊洛沙姆407和4.19%泊洛沙姆188;优化处方在29.7℃为自由流动的液体,泪液稀释后在34.5℃能够发生相变形成凝胶.结论 该眼用温度敏感凝胶符合眼部应用要求,体现出良好的眼部应用前景.     

妇黄宁温敏凝胶的制备及体外释放研究

目的妇黄宁温敏凝胶的制备及体外释放研究。方法以泊洛沙姆407为凝胶材料,以泊洛沙姆188和丙二醇为胶凝温度调节剂,采用正交实验优选制备处方;采用试管倒置法测定妇黄宁温敏凝胶胶凝温度;采用高效液相色谱法测定妇黄宁温敏凝胶体外累积释放量,拟合释放曲线。结果妇黄宁温敏凝胶胶凝温度为(37±0.1)℃,胶凝时间5.3min;体外释放均符合Higuchi方程,溶蚀释放较扩散释放占主要影响。结论妇黄宁温敏凝胶制备处方合理、稳定;检测方法方便、稳定、高效,满足妇黄宁温敏凝胶体外释放研究检测要求;妇黄宁温敏凝胶符合阴道给药的设计要求。     

氢溴酸西酞普兰鼻用温敏凝胶的处方优化及体外性质评价

目的优化氢溴酸西酞普兰(citalopram hydrobromide,CTH)鼻用温敏凝胶的处方并对其体外性质进行评价。方法以泊洛沙姆407(F127)和卡波姆940(CP940)作为凝胶基质材料,胶凝温度与胶凝时间为观察指标,采用星点设计-效应面法和单因素实验法优化凝胶基质处方;同时,以离体羊鼻黏膜为模型,采用Franz透皮扩散池法筛选药物透皮吸收促渗剂,最后采用冷法制备CTH鼻用温敏凝胶并进行体外性质评价;采用无膜溶出法测定制剂的体外溶蚀率及体外释放率;采用透析膜法测定其体外释放度。同时,考察温度及pH对该制剂黏度的影响。结果CTH鼻用温敏凝胶最优处方组成为:CTH 8.0%、F12720.27%、CP9400.17%、DM-β-003.0%、尼泊金乙酯0.05%及适量水。该制剂的胶凝温度为32.5℃,胶凝时间为42s,PH值为5.0,55 min时体外累积溶蚀率与药物累积释放率均大于90%,且二者具有良好线性相关性(r^2=0.9986);该制剂在8 h内体外累积释药为92%,其释药过程符合Higuchi动力学方程。温度及pH对该制剂的黏度均有不同程度的影响。结论采用星点设计-效应面法和单因素法优化处方所制备CTH鼻用温敏凝胶其肢凝温度、胶凝时间及pH值适宜,符合鼻用制剂要求,其体外释药具明显缓释特征。     

黄原胶的流变学性质及助悬性能

 目的:测定黄原胶的流变学性质,考察其助悬性能。方法:在光照、冷冻(-18℃)、冷藏(+4℃)及辅料等因素影响下,采用NDJ-1型旋转粘度计测定黄原胶的流变学性质。以硫糖铝为模型药物,制备以黄原胶为助悬剂的100g·L^-1硫糖铝混悬液。结果:黄原胶水溶液为塑性结构并具有触变性。其作为硫糖铝混悬剂时的最佳浓度为3g·L^-1,在此浓度下该混悬液具有显著触变性。结论:光照、冷冻(-18℃)、冷藏(+4℃)均不影响其流变学性质。该水溶液可作为药物助悬剂。     

阿胶的一种简易鉴别法

阿胶及其它动物胶类多由胶原及其部分水解产物所组成,其成分基本上是蛋白质,水解产生多种氨基酸,阿胶含氮16.3-16.54%。在适当的条件下,阿胶及其它胶类溶液,有转变为粘性的半固体凝胶的胶凝现象,影响这些溶液的胶凝主要因素是温度和浓度。观察不同浓度胶类溶液的胶凝温度,可以区分真品阿胶和假阿胶。     

Effect of feeding Mucuna pruriens on helminth parasite infestation in lambs

Ethnopharmacological relevance

Mucuna pruriens is a tropical legume anecdotally reputed to have anthelmintic properties. This study was conducted to examine the validity of such claims.

Aim of the study

The aim of this study was to determine if ingestion of Mucuna seeds reduces helminth parasite infestation in lambs.

Materials and methods

Thirty-six Dorper × Katahdin ram lambs were assigned to three treatments, a cottonseed meal based control diet, a diet in which Mucuna replaced cottonseed meal and the control diet with levamisole (7.5 mg/kg body weight) administration. All diets were isonitrogenous and isocaloric. The 12 lambs in each treatment were assigned randomly to 4 pens, each containing 3 lambs. Lambs were trickle infected three times per week by gavage with infectious Haemonchus contortus larvae (2000 larvae/lamb) for 3 weeks.

Results

Levamisole treatment decreased fecal egg counts by 87% and abomasal worm counts by 83%. Mucuna intake did not statistically affect fecal egg counts or abomasal worm counts, though numerical (P > 0.10) reductions of 7.4% and 18.1%, respectively were evident. Anemia indicators, feed intake, and lamb growth were unaffected by treatment.

Conclusions

Levamisole reduced the Haemonchus parasite burden in lambs significantly but feeding Mucuna reduced the burden by levels unlikely to eliminate the clinical effects of parasitism.     

Investigation of plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts

Aim of the study

To investigate the activities of the 217 plant extracts in traditional medicine of the Brazilian Cerrado against protozoans and yeasts.

Materials and methods

Plant extracts were prepared by the method of maceration using solvents of different polarities. The growth inhibition of chloroquine-resistant Plasmodium falciparum strain (FcB1) was determined by measuring the radioactivity of the tritiated hypoxanthine incorporated. Activity against Leishmania (Leishmania) chagasi and Trypanosoma cruzi was measured by the MTT colorimetric assay. The antifungal tests were carried out by using the CLSI method. The active extracts were tested also by cytotoxicity assay using NIH-3T3 cells of mammalian fibroblasts.

Results

Two hundred and seventeen extracts of plants were tested against Plasmodium falciparum. The eleven active extracts, belonging to eight plant species were evaluated against L. (L.) chagasi, Trypanosoma cruzi, yeasts and in NIH-3T3 cells. The results found in these biological models are consistent with the ethnopharmacological data of these plants. The ethyl acetate extract of Diospyros hispida root showed IC₅₀ values of 1 μg/mL against Plasmodium falciparum. This extract demonstrated no toxicity against mammalian cells, resulting in a significant selectivity index (SI) of 435.8. The dichloromethane extract of Calophyllum brasiliense root wood was active against Cryptococcus gattii LMGO 01 with MIC of 1.95 μg/mL; and Candida albicans ATCC 10231 and Candida krusei LMGO 174, both with MIC of 7.81 μg/mL. The same extract was also active against Plasmodium falciparum and L. (L.) chagasi with IC₅₀ of 6.7 and 27.6 μg/mL respectively. The ethyl acetate extract of Spiranthera odoratissima leaves was active against Cryptococcus gattii LMGO 01 with MIC of 31.25 μg/mL, and against Plasmodium falciparum with IC₅₀ of 9.2 μg/mL and Trypanosoma cruzi with IC₅₀ of 56.3 μg/mL.

Conclusion

The active extracts for protozoans and human pathogenic yeasts are considered promising to continue the search for the identification and development of leading compounds.     

真菌的中药干预研究近5年进展

近年来真菌感染率逐年上升,传统抗真菌药物易产生耐药性,而中药在防治真菌感染方面具有一定的优势。本文就近5年来中药对白念珠菌、皮肤癣菌、曲霉菌、马拉色菌、串珠镰孢菌、申克孢子丝菌、新生隐球菌及真菌生物膜的干预研究进展进行综述。     

α-Glucosidase inhibitory activity of selected Philippine plants

Ethnopharmacological relevance

Antidesma bunius Spreng. (Phyllantaceae), Averrhoa bilimbi L. (Oxalidaceae), Biophytum sensitivum (L.) DC. (Oxalidaceae), Ceriops tagal (Perr.) C.B. Rob. (Rhizophoraceae), Kyllinga monocephala Rottb. (Cyperaceae), and Rhizophora mucronata Lam. (Rhizophoraceae) are used as remedies to control diabetes. In the present study, these plants were screened for their potential α-glucosidase inhibitory activity.

Materials and methods

The 80% aqueous ethanolic extracts were screened for their α-glucosidase enzyme inhibitory activity using yeast alpha glucosidase enzyme.

Results

Except for A. bilimbi with IC₅₀ at 519.86±3.07, all manifested a significant enzyme inhibitory activity. R. mucronata manifested the highest activity with IC₅₀ at 0.08±1.82 μg mL⁻¹, followed by C. tagal with IC₅₀ at 0.85±1.46 μg mL⁻¹ and B. sensitivum with IC₅₀ at 2.24±1.58 μg mL⁻¹.

Conclusion

This is the first report on the α-glucosidase inhibitory effect of the six Philippine plants; thus, partly defining the mechanism on why these medicinal plants possess antidiabetic properties.     

European medicinal polypores – A modern view on traditional uses

Ethnopharmacological relevance

In particular five polypore species, i.e. Laetiporus sulphureus, Fomes fomentarius, Fomitopsis pinicola, Piptoporus betulinus, and Laricifomes officinalis, have been widely used in central European folk medicines for the treatment of various diseases, e.g. dysmenorrhoea, haemorrhoids, bladder disorders, pyretic diseases, treatment of coughs, cancer, and rheumatism. Prehistoric artefacts going back to over 5000 years underline the long tradition of using polypores for various applications ranging from food or tinder material to medicinal–spiritual uses as witnessed by two polypore species found among items of Ötzi, the Iceman. The present paper reviews the traditional uses, phytochemistry, and biological activity of the five mentioned polypores.

Materials and methods

All available information on the selected polypore taxa used in traditional folk medicine was collected through evaluation of literature in libraries and searches in online databases using SciFinder and Web of Knowledge.

Results

Mycochemical studies report the presence of many primary (e.g. polysaccharides) and secondary metabolites (e.g. triterpenes). Crude extracts and isolated compounds show a wide spectrum of biological properties, such as anti-inflammatory, cytotoxic, and antimicrobial activities.

Conclusions

The investigated polypores possess a longstanding ethnomycological tradition in Europe. Here, we compile biological results which highlight their therapeutic value. Moreover, this work provides a solid base for further investigations on a molecular level, both compound- and target-wise.     

厚朴与凹叶厚朴群体遗传学研究

目的:对厚朴与凹叶厚朴的群体遗传学进行研究,为中药厚朴的质量控制提供分子生药学方面的依据。方法:对厚朴与凹叶厚朴15个居群应用2个叶绿体基因间序列psbA-trnH和trnL-trnF进行PCR扩增并测序,计算厚朴与凹叶厚朴单倍型频率,用程序HaploNst分析遗传多样性和遗传结构,应用TCS version 1.13软件构建单倍型网状进化树。结果:厚朴与凹叶厚朴均无特有单倍型存在,但单倍型频率存在显著差异,已开始出现遗传分化的趋势,NST略大于GST。结论:厚朴与凹叶厚朴在遗传上已出现遗传分化的趋势,但尚未完全分化成彼此独立的单系。     

Screening of the topical anti-inflammatory activity of the bark of Acacia cornigera Willdenow, Byrsonima crassifolia Kunth, Sweetia panamensis Yakovlev and the leaves of Sphagneticola trilobata Hitchcock

Ethnopharmacological relevance

An investigation of topical anti-inflammatory activity was undertaken on plants used in Central America traditional medicine.

Aim of study

Four herbal drugs used in the folk medicine of Central America to treat inflammatory skin affections (Acacia cornigera bark, Byrsonima crassifolia bark, Sphagneticola trilobata leaves and Sweetia panamensis bark) were evaluated for their topical anti-inflammatory activity.

Materials and methods

Petroleum ether, chloroform and methanol extracts were obtained for herbal medicines and then extracts were tested on Croton oil-induced ear dermatitis model in mice.

Results

Almost all the extracts reduced the Croton oil-induced ear dermatitis in mice and the chloroform ones showed the highest activity, with ID₅₀ (dose giving 50% oedema inhibition) values ranging from 112 μg/cm² (Byrsonima crassifolia) to 183 μg/cm² (Sphagneticola trilobata). As reference, ID₅₀ of the non-steroidal anti-inflammatory drug indomethacin was 93 μg/cm².

Conclusions

Lipophilic extracts from these species can be regarded as potential sources of anti-inflammatory principles.     

Antiplasmodial activity of extracts from seven medicinal plants used in malaria treatment in Cameroon

Aim of the study

In a search for new plant-derived biologically active compounds against malaria parasites, we have carried out an ethnopharmacological study to evaluate the susceptibility of cultured Plasmodium falciparum to extracts and fractions from seven Cameroonian medicinal plants used in malaria treatment. We have also explored the inhibition of the Plasmodium falciparum cysteine protease Falcipain-2.

Materials and methods

Plant materials were extracted by maceration in organic solvents, and subsequently partitioned or fractionated to afford test fractions. The susceptibility of erythrocytes and the W2 strain of Plasmodium falciparum to plant extracts was evaluated in culture. In addition, the ability of annonaceous extracts to inhibit recombinant cysteine protease Falcipain-2 was also assessed.

Results and discussion

The extracts showed no toxicity against erythrocytes. The majority of plant extracts were highly active against Plasmodium falciparumin vitro, with IC₅₀ values lower than 5 μg/ml. Annonaceous extracts (acetogenin-rich fractions and interface precipitates) exhibited the highest potency. Some of these extracts exhibited modest inhibition of Falcipain-2.

Conclusion

These results support continued investigation of components of traditional medicines as potential new antimalarial agents.     

中国石斛属植物文献计量研究

石斛是珍稀濒危中药材,目前正处于快速发展阶段。为全面了解我国石斛属植物研究的历史和发展现状,作者以1954～2010年"中国知网中国学术期刊网络出版总库"收录的石斛研究文献为依据,采用文献计量学的原理和方法,对我国石斛属植物研究文献从文献年代分布、期刊分布与被引频率、主题分布、研究对象分布、作者与研究机构分布等方面进行了统计与分析。结果表明,我国石斛研究明显分为起步(2个)、停滞、平稳发展、快速上升5个阶段;期刊分布存在离散性与集中性并存的现象,已形成核心期刊研究群,并以《中国中药杂志》、《中草药》和《陕西中医》为代表;研究主题广泛涉及临床与药理、组织培养与种苗繁育、成分分析等多个领域,已经形成比较稳定的研究机构和团队,但研究对象差异显著,以铁皮石斛、金钗石斛和霍山石斛最为集中。我国石斛属植物的研究已取得显著成果,但种植产业发展缓慢,供需矛盾突出,预计种苗繁育与人工种植、产品开发、化学与药理等方面是未来的研究热点,其文献报道仍将进一步上升。     

列当属、肉苁蓉属和草苁蓉属植物传统药物学调查

通过野外资源调查、整理各大标本馆标本原始记录和查阅文献记载等方法,系统整理、总结、归纳了列当属、肉苁蓉属和草苁蓉属民族药用植物种类、功效及民间使用情况,结果表明列当属6种药用植物在4个少数民族间作为7种民族药应用,草苁蓉属2种药用植物在8个少数民族间作为10种民族药应用,肉苁蓉属2种药用植物在3个少数民族间作为3种民族药应用,且同种药用植物常作不同民族药;发现3属植物的传统疗效主要集中在补肾壮阳、止血和止痛3个方面,并且该传统疗效与现代药理研究结果基本吻合。因此深入研究植物种类丰富的列当属植物资源对缓解肉苁蓉植物资源匮乏局面和扩大药源具有积极意义。