清热解毒颗粒剂提取工艺及制剂处方组成的研究

为了优选清热解毒颗粒剂提取工艺及处方组成 ,以黄芩苷含量为指标采用正交法优选了清热解毒颗粒剂的提取工艺 ,并以综合评分法采用单因素实验设计筛选了颗粒剂的处方组成。结果最佳提取工艺为 :煎煮 3次 ,每次 1小时 ,每次加水量为处方药材量的 10倍。最佳处方组成为 :1份浸膏粉与 5份糖粉混匀 ,制粒。实验表明最优提取工艺条件提取率高 ,工艺稳定 ,合理可行。最佳处方所制颗粒溶解性好 ,成型率高 ,吸湿性小 ,较为理想     

Human exposure to bisphenol A

Bisphenol A (BPA), 2,2-bis(4-hydroxyphenyl)propane, is made by combining acetone and phenol. It has estrogenic activity and is acutely toxic to aquatic organisms. BPA is used mainly as a material for the production of epoxy resins and polycarbonate plastics. Due to an increase in products based on epoxy resins and polycarbonate plastics, human exposure to BPA has increased. The environment (aquatic environment, air and soil) can be one source of human BPA exposure, but the primary route of human exposure is foods. The daily human intake of BPA is <1 microg/kg body weight/day on the basis of several studies, and whether these doses can have an adverse endocrine disruptive effect on humans, especially fetuses, needs to be studied carefully.     

Toxicity of nanocrystal quantum dots: the relevance of surface modifications

With the development of nanotechnology, nanometer-sized products smaller than several 100 nm have been applied for all areas of science and technology. The nanometer-sized products, including carbon nanotubes, fullerene derivatives, and nanocrystals made of various materials, are widely employed as novel tools in various fields, not only in material engineering, electronics, plastics, automobile, aviation, and aerospace industries, but also even in cellular biology, molecular biology, and basic and clinical medical fields. In particular, nanocrystal quantum dots (QDs) have been widely used in biological and medical studies because of their far brighter photoemission and photostability. The physical and chemical properties of QDs have been circumstantially investigated, but little is known about the potential harmful effects of QDs on human health. In addition to the physical and chemical properties of the QDs, their toxicity and biological behavior are generally regulated by three other conditions: (1) the QD core material itself, (2) the surface modifications of the QD, and (3) the external environmental condition of the QDs. We herein report on the in vitro and in vivo toxicity and biological behavior of nanocrystals such as QDs. Accumulating evidence suggests that the QD-capping material, rather than the core metalloid complex, is responsible for the majority of their toxicity and biological activity. For example, molecules covered with a toxic agent showed cytotoxicity, whereas QDs conjugated with biomolecules retained the biological effects of the conjugate.     

2种地龙饮片不同提取法体外抗凝活性对比研究

目的 研究酒制对地龙体外抗凝活性的影响，为地龙临床应用提供科学依据。方法 分别采用传统水提法和仿生酶解提取法对生品地龙、酒制地龙进行提取，以活化部分凝血活酶时间（activated partial thromboplastin time，APTT）、凝血酶原时间（prothrombin time，PT）、凝血酶时间（thrombin time，TT）和抗凝血酶活力为指标进行抗凝活性测定，并采用BCA蛋白测定法测定可溶性蛋白、多肽含量。结果 采用水提取法时，PT和抗凝血酶滴定法均显示酒地龙与生地龙抗凝血活性相当，TT测定结果显示酒地龙抗凝血活性强于生地龙，APTT测定结果则显示地龙具有促凝血活性，且在一定范围内，浓度越高，促凝效果越强，蛋白、多肽含量为酒地龙大于生地龙；采用仿生酶解提取法时，APTT和PT测定结果显示酒地龙的抗凝血活性强于生地龙，并且蛋白、多肽含量测定结果显示酒地龙要多于生地龙，但TT和抗凝血酶滴定法并未比较出生品与酒制品之间的差异。结论 与传统水提法相比，仿生酶解提取法能更多地提取出蛋白多肽类成分，仿生酶解提取液具有更强的抗凝血活性，2种提取法均显示地龙酒制有利于可溶性蛋白、多肽的溶出，能增强体外抗凝血活性。     

Elimination of polymer interference in chromatographic analysis of estradiol degradation products in a transdermal drug delivery formulation by proper selection of extraction solvents

This article describes the proper selection of extraction solvents to eliminate interference from a polymer matrix to the quantitation of estradiol degradation products in a transdermal formulation by reversed-phase liquid chromatography. The separation is performed by gradient elution with acetonitrile and water as the mobile phase on Inertsil ODS columns. Severe band distortion and insufficient recovery are observed for two geometric degradation products (or impurities) when the sample is prepared by acetonitrile. It is anticipated that the poor resolution and recovery are caused by multiple retention processes due to the reversible binding of degradation products to the polymer matrix (or the impurity-polymer interaction). This interaction is eliminated by adding formamide, a solvent that possesses similar properties to the matrix, in the extraction solvent. It is believed that the favorable interaction between formamide and the polymer matrix releases the impurity molecules, and they can then be separated by a single retention mode. It has been confirmed experimentally that the use of formamide in the extraction solvent not only sharpens the peaks tremendously, but also recovers the degradation products completely.     

Efficiency of supercritical fluid extraction for the production of non-volatile terpenoids from Taraxaci radix

Supercritical fluid extraction (SFE) is an extraction technique which exploits the solvent properties of fluids above their critical point. As a result supercritical fluid extraction was used to gain various active substances from plants. The use of SFE to obtain bioactive substances from medicinal plants over the past twenty years has been proved to be a viable alternative for the extraction of natural compounds. Dandelion (Taraxacum officinale Wiggers et Webers, Asteraceae) is one of the best known European medicinal plants, not only as a traditional medicine but perspective raw material for modern phytopharmaceuticals. From the characteristic principles our attention has been directed to triterpenes and phytosterols with anti-inflammatory activity, which were extracted with supercritical carbon dioxide. Designed experiments were carried out to determine the optimal extraction parameters. The products obtained by supercritical fluids extraction were compared to extracts prepared by traditional extraction method (Soxhlet) with n-hexane and ethyl alcohol solvents. The content of triterpenes and sterols was monitored after saponification by thin layer chromatography-densitometry. The products gained by supercritical fluid extraction were different from the traditional ones both in their appearance and composition. Triterpenes and their esters were extracted quantitatively by supercritical fluid extraction using CO2 as solvent and the extraction dynamic for triterpenes and phytosterols was different. Triterpenes had a higher concentration in the SFE product then in the extracts prepared by traditional methods.     

滋阴活血利咽颗粒超声波提取工艺研究

目的:首次在滋阴活血利咽颗粒剂制备工艺中采用超声波提取方法,并优化了超声波提取工艺条件.方法:采用正交试验方法,考察颗粒粒度、加水量、提取次数、提取时间对超声提取得率的影响.结果:颗粒柱度、加水量、提取时间等因素对提取效果的影响均没有显著性,提取次数对提取效果的影响有显著性.结论:超声提取具有能耗低,省时,提取转移率高,常温提取,生产成本低等优势.     

Experimental study on infusion devices containing polyvinyl chloride: to what extent are they di(2-ethylhexyl)phthalate-free?

The use of medical devices containing highly criticized phthalates including di(2-ethylhexyl) phthalate (DEHP) has been challenged by European directive 2007/47/CE, put into effect in March 2010. New plasticizers are now being used to soften PVC in medical devices: trioctyltrimellitate (TOTM), di-isononyl-cyclohexan-1,2-dicarboxilate (DINCH) and di(2-ethylhexyl) terephthalate (DEHT). To quantify DEHP in nine DEHP-free medical devices made of PVC softened by alternative plasticizers, high performance liquid chromatography analysis with ultraviolet detection at 220 nm wavelength was achieved. An NMR spectroscopy was performed to confirm DEHP presence. Only two medical devices out of the nine tested were truly without DEHP. One of them showed traces of DEHP exceeding the threshold contamination of 0.1% in plastic mass set by REACH regulations. TOTM plasticizer is still incriminated when polyvinyl-chloride (PVC) is contaminated with DEHP. Manufacturers must verify the purity of their raw material, not only on PVC, but also on other soft plastics entering into the composition of medical infusion devices. The clinical consequences of exposure to certain levels of DEHP have not been evaluated. A solution could be to use alternative PVC-free materials.     

The determination of residual ethylene oxide and halogenated hydrocarbon propellants in sterilized plastics

A specific and sensitive method is described for the determination of residual ethylene oxide, dichlorodifluoromethane and trichlorofluoromethane in sterilized plastic surgical equipment. Residues are isolated from the plastics by high vacuum distillation and analysed by gas chromatography using an exponential dilution apparatus, to avoid the use of solvents. Under the conditions specified, a lower limit of 1 ppm of each component could be detected in blood giving sets of which the main plastics material was PVC. The rate of loss of each component has been studied, to indicate the necessary holding time of the material before it can be considered safe to use.     

The synthesis,production & economic feasibility of manufacturing PLA from agricultural waste

Synthetic plastics are extensively used in several applications including packaging, containers, bottles, trays, and boxes. However, these plastics are based on synthetic components which are not biodegradable, thus they rigorously effect the environment causing water, air pollution and high health risks. Moreover, Individuals are exposed to chemicals during manufacturing or usage of synthetic plastic that can easily migrate to the surrounding such as styrene from polystyrene, plasticizers from polyvinyl chloride (PVC), antioxidants from polyethylene, and acetaldehyde from polyethylene terephthalate (PET), and they lead to several human diseases. The authors studied the economic feasibility of producing Polylactic Acid (PLA) as a replacement for synthetic polymers. The results suggest that by replacing all synthetic plastic products with PLA materials, and recycling all plastics produced annually, the world can reduce 800 million tons GHG emissions every year. Furthermore, the economic feasibility analysis show that PLA pellets are more feasible economically than synthetic plastics if quality requirements are met.     

当归、枳壳挥发油的提取与包合工艺研究

目的 优选当归和枳壳挥发油的提取工艺及β-环糊精包合工艺.方法 采用单因素考察法,以药材粉碎度、蒸馏时间、浸泡时间、加水量为考察因素,挥发油提取量为指标,优选其提取工艺.以挥发油包合率为指标,对饱和水溶液法、研磨法及超声法进行比较,采用正交实验法,优选出最佳包合工艺;并对包合物进行TLC及IR检验.结果 最佳提取工艺为药材粉碎成粗粉(20目),8倍量水,浸泡0.5h,提取5 h;最佳包合方法是研磨法,挥发油和β-环糊精的比例为1∶8(mL∶g),加4倍量的水,研磨3h.结论 本法确定的最佳提取与包合工艺,可有效地提取与保留当归和枳壳的活性成分挥发油,为其进一步研究打下基础.     

Pharmacologic considerations in the design of toxicology experiments

Final assessment of product acceptance must be based on value judgments that include (a) social, (b) economic, and (c) environmental factors as well as risk factors, and not on simple safety statements about the end product. The goal of toxicologic experiments should be to provide sufficient data to allow benefit-to-risk judgments about products. Benefit-to-risk judgments need to be made on a broad data base which includes: manufacturing, distribution, and use factors. Safety assessments begin with concerns associated with initial manufacture of raw materials and end with concerns related to disposal of the end products of use. Current experimental design needs to include biopharmaceutic considerations of the dose form, pharmacokinetic aspects, and pharmacodynamic factors as well as pathologic concerns. These factors stress the point that toxicology is a quantitative science because toxicity resides in the dose and dose form and not in the chemical entity.     

Economics and structure of the generic pharmaceutical industry

OBJECTIVE: To review key economic trends of the generic medication market and analyze the changing structure of the generic medication industry. DATA SOURCES: Articles were indexed initially using terms such as generic medications, generic drugs, multisource medications, and multisource drugs. These terms were used to search indexing services such as MEDLINE, International Pharmaceutical Abstracts, CINAHL (a database of nursing and allied health literature), Science Citation Index, Psychological Abstracts, and Wilson Indexes to Journal Articles. STUDY SELECTION: Performed by the authors. DATA EXTRACTION: Not applicable. DATA SYNTHESIS: The generic pharmaceutical market has the potential to play an important role in containing drug costs, although the amount that could be saved through the use of generic medications is not easy to measure. If estimates for the future growth in the use of generic products prove correct, the proportion of pharmaceutical sales attributable to generic products will remain in the 9% to 10% range through the first decade of the 21st century. The generic pharmaceutical industry includes several categories of companies based on business strategies. Further consolidation is expected as more resources are needed to address patent challenges stimulated by the Drug Price Competition and Patent Restoration Act. Companies are also entering into partnerships with research manufacturers to share profits from proprietary products. Future growth of the generic market will require more than increased use of generic products. Therapeutic interchange, involving switching from single-source, patent-protected products to products within the therapeutic class for which there are generic equivalents, represents a major growth opportunity for generic drug manufacturers because the savings potential is more significant than that for straightforward substitution of generic for brandname products. CONCLUSION: As it responds to challenges and opportunities, the generic pharmaceutical industry will continue to be a major force shaping the economics of medication use.     

响应曲面法优化山菠萝中黄酮的提取工艺

目的：以响应曲面法优化山菠萝黄酮的提取工艺。方法：在单因素试验的基础上,采用响应曲面法研究乙醇的浓度、提取时间、料液比和提取次数对山菠萝中总黄酮含量的影响。结果：山菠萝中黄酮提取的的最佳工艺条件为：乙醇浓度为80%、提取时间为94.2min、料液比为1：20、提取次数为2次的条件下,山菠萝中总黄酮的含量为14.37mg.g_-1。结论：响应曲面法工艺简单,得率较高,可用于山菠萝中总黄酮的提取。     

Loss of antibacterial preservatives from contact lens solutions during storage.

The preservative content of 34 commercially available contact lens solutions has been determined. Over half of the solutions contained less than 90% of the stated preservative content. Storage tests conducted at 40 degrees, using both simulated and commercially available contact lens solutions in plastics containers of the type used to present these products showed that thiomersal and chlorbutol appeared to be sorbed by these containers in contrast to benzalkonium chloride and chlorhexidine gluconate which interacted mainly by a surface adsorption process. The extent of any interactions was dependent upon the type of plastics material used to fabricate the container.     

免洗丁基橡胶输液瓶塞的清洗必要性研究

目的:探讨免洗丁基橡胶输液瓶塞使用前是否需要清洗。方法:选择A、B厂家的免洗丁基橡胶输液瓶塞进行预试验,确定胶塞清洗的最少次数为1次,并选定A厂家生产的胶塞进行扩大试验。取A厂家的2个不同批号的免洗丁基橡胶输液瓶塞,均作不清洗、用注射用水清洗1次的处理,用于本院制剂室的所有输液品种的灌装,并测定产品的不溶性微粒。结果:使用未经清洗的胶塞的产品所含的不溶性微粒不符合《中国药典》规定,使用清洗1次的胶塞的产品所含的不溶性微粒符合《中国药典》规定。结论:免洗丁基橡胶输液瓶塞使用前必须用注射用水清洗1次,否则将影响产品质量。     

Loss of antibacterial preservatives from contact lens solutions during storage*

The preservative content of 34 commercially available contact lens solutions has been determined. Over half of the solutions contained less than 90% of the stated preservative content. Storage tests conducted at 40°, using both simulated and commercially available contact lens solutions in plastics containers of the type used to present these products showed that thiomersal and chlorbutol appeared to be sorbed by these containers in contrast to benzalkonium chloride and chlorhexidine gluconate which interacted mainly by a surface adsorption process. The extent of any interactions was dependent upon the type of plastics material used to fabricate the container.     

眼络通颗粒的提取工艺研究

目的:研究眼络通颗粒的提取工艺。方法:采用正交设计试验,以葛根中葛根素转移率为指标,考察乙醇浓度、溶剂倍数、提取时间、提取次数对葛根乙醇提取效率的影响;采用水蒸气蒸馏法提取川芎、三棱中的挥发油,并制成β-环糊精包合物;采用水煎煮法提取其它药材中的水溶性成分。结果:葛根的最佳提取条件为取葛根药材8倍量的70%乙醇浸泡75min,再加热回流提取3次,每次2h;挥发油β-环糊精包合物制备方法为取15倍处方量川芎、三棱药材,加10倍量水,水蒸气蒸馏提取4h,用β-环糊精15g进行包合。结论:本工艺条件能最大限度提取药材中的有效成分。     

Evaluation of dermal and eye irritation and skin sensitization due to carbon nanotubes

The present paper summarizes the results of our studies on dermal and eye irritation and skin sensitization due to carbon nanotubes (CNTs), whose potential applications and uses are wide and varied, including CNT-enhanced plastics, electromagnetic interference/radio-frequency (EMI/RFI) shielding, antistatic material, flexible fibers and advanced polymers, medical and health applications, and scanning probe microscopy. Skin and eyes have the highest risk of exposure to nanomaterials, because deposition of nanomaterials to the surficial organs has the potential to be a major route of exposure during the manufacturing, use, and disposal of nanomaterials. Two products composed of single-walled carbon nanotubes (SWCNTs) and two products composed of multi-walled carbon nanotubes (MWCNTs) were tested regarding acute dermal and acute eye irritation using rabbits, and skin sensitization using guinea pigs. The concentrations of the CNTs in the substances were the maximum allowable for administration. The two products of SWCNTs and one of the products of MWCNTs were not irritants to the skin or eyes. The other product of MWCNTs caused very slight erythema at 24 h, but not at 72 h, after patch removal in the dermal irritation experiments and conjunctival redness and blood vessel hyperemia at 1 h, but not at 24 h, in eye irritation experiments. These findings showed that one product of MWCNTs was a very weak acute irritant to the skin and eyes. No products of SWCNTs and MWCNTs exhibited skin-sensitization effects. Our knowledge of the toxicological effects of CNTs is still limited. Further information is needed to clarify the potential for irritation and sensitization given the complex nature of CNTs.