复方酚咖伪麻胶囊中对乙酰氨基酚溶出度研究

目的 研究复方酚咖伪麻胶囊中对乙酰氨基酚的溶出度。方法 照溶出度测定法[2000年版《中国药典（二部）》附录XC第一法转篮法]分别测定复方酚咖伪麻胶囊中对乙酰氨基酚溶出度，并考察转速、pH值对溶出度的影响。结果 样品累积溶出量基本一致，体外溶出度均一性良好，转速对溶出度有明显影响，而pH值对溶出度几乎无影响。结论 自制复方酚咖伪麻胶囊样品的溶出度符合要求。     

尼莫地平干乳的溶出度测定

目的测定尼莫地平脂肪乳干乳的体外溶出度，并比较其与尼莫地平进口片、尼莫地平脂肪乳、尼莫地平国产片及国产胶囊的体外溶出度差异。方法以紫外分光光度法作为定量方法，以人工胃液为溶出介质，采用转篮法测定溶出度。以相似因子法评价尼莫地平脂肪乳干乳的溶出度。结果尼莫地平脂肪乳干乳、尼莫地平脂肪乳和进口片的溶出度明显高于尼莫地平国产片和国产胶囊的溶出度，尼莫地平干乳的溶出度与尼莫地平脂肪乳和尼莫地平进口片的溶出度均相似，且与尼莫地平脂肪乳的相似程度更高。尼莫地平干乳的溶出度与国产片和国产胶囊的溶出度均不相似。结论尼莫地平干乳明显优于国产片和国产胶囊，而与进口片质量相似。     

对乙酰氨基酚口腔速溶片溶出度的研究

目的 比较对乙酰氨基酚口腔速溶片与对乙酰氨基酚普通片溶出度，并考察转速和pH值对其溶出度的影响。方法 利用中国药典2000版转篮法分别测定对乙酰氨基酚口腔速溶片的溶出度以及不同pH值、不同转速下速溶片的溶出度。结果 实验表明，与对乙酰氨基酚普通片相比，口腔速溶片溶出速度快，同时发现转速对其溶出度有明显影响，而pH对其溶出度几乎无影响。结论 对乙酰氨基酚口腔速溶片可被很快吸收，符合一般口腔速溶片溶出度的要求。     

复方戊酸雌二醇片的溶出度研究

目的 进行复方戊酸雌二醇片溶出度的方法学研究。方法 采用桨法，以0．25％十二烷基硫酸钠的磷酸盐缓冲波(pH7.3)为溶出介质，用高效液相色谱法测定溶出度。结果 本法的平均回收率高，产品的溶出度均一性好，与进口品溶出度曲线相近。结论 本法适用于该制剂的溶出度质量控制。     

四厂家阿奇霉素片溶出度考察

目的比较4厂家阿奇霉素片的溶出度，为临床用药提供参考。方法依据2005年版《中国药典（二部）》阿奇霉素片溶出度项下有关规定进行溶出度的测定。结果4厂家产品在45min时的累积溶出百分率均〉75％，但溶出度参数则差异明显（P〈0．01）。结论各厂家的阿奇霉素片的溶出度均符合《中国药典》规定，但溶出度参数有极显著性差异.     

影响甲硝唑片溶出度的因素

目的：考察影响甲硝唑片溶出度的因素。方法：压片前分别按5种不同比例加羧甲基淀粉钠(CMS—Na)及硬脂酸镁，混匀，压片，测其溶出度：分别以87℃与50’C的淀粉作粘合剂制软材，压片，测其溶出度；分别以不同大小、不同硬度的颗粒压片，测其溶出度：同批颗粒分别制成直径8，9，10mm三种规格的片剂，测其溶出度。结果：CMS—Na能显著提高甲硝唑片溶出度。     

罗红霉素在两种介质中的溶出度考察

目的 比较7厂家罗红霉素在两种介质中的体外溶出度。方法 采用紫外分光光度法测定含量和在两种不同介质中的溶出度。结果 7厂家罗红霉素在人工胃液中溶出度不符合要求，有2家在人工肠液中不符合要求。结论 罗红霉素在两种介质中溶出度有很大差异，各厂家之间的产品溶出度也存在差异。     

对乙酰氨基酚栓的溶出度测定

目的：测定对乙酰氨基酚栓的溶出度，考察不同厂家栓剂的质量。方法：用pH7．4的磷酸盐缓冲液为溶剂，浆法测定，紫外分光光度法涵定溶出度。结果：不同厂家的栓剂溶出度差异很大。结论：应建立溶出度涵定法以有效控制药品的质量。     

10个厂家罗红霉素胶囊质量考察

目的：对10个厂家的罗红霉素胶囊进行溶出度和含量测定的考察。方法：转篮法，用紫外分光光度法测定溶出度，用抗生素微生物检定法测定含量。结果：含量测定符合规定，而溶出度存在显著性差异。结论：罗红霉素胶囊的溶出度差异很大，应引起有关生产厂家的关注，改进工艺水平。     

氨茶碱片的溶出度考察

采用紫外分光光度法，考察5家药厂生产的6批氨茶碱片的溶出度；结果表明，一厂家产品溶出度不合格，不同厂家及同一厂家产品之间，溶出度参数有显著差异。     

The debate on DDT

The paper reviews the early toxicologic and pharmacologic studies carried out by the author and his associates from 1943 to 1947, which were largely responsible for launching DDT as an agent for the control of typhus, malaria, yellow fever, and related vector-borne diseases. After reviewing recent studies conducted at the University of Miami, which dealt with organochlorine pesticides in human tissues, the tumorigenicity of aldrin, dieldrin and endrin (rat), six-generation mouse and three-generation dog reproduction studies, synergism of DDT and aldrin (dog), and the fate of DDT and aldrin during a period of severe starvation (rat), it is pointed out that it is primarily the overuse and misuse of DDT in pest control that have caused the pollution in our ecology. It is emphasized that the requirements for pest control differ the world over and that it must therefore be left to the national regulatory agencies to legislate the safe use of DDT and related pesticides. It is recommended that future human and animal studies with DDT and its derivatives give consideration to: (a) the balance and metabolism of the various hormones, (b) reproduction (estrus, libido, mammary development, milk production, (c) hepatic microsomal enzyme activities, (d) cancer prevention and cancer production, (e) excessive body weight changes induced by disease, unbalanced diet or starvation, and (f) the effects of DDT and its derivatives when absorbed in combination with other related and even unrelated compounds.Presented at the joint meeting of the Scandinavian and German Pharmacological Societies, Copenhagen, Denmark, July 20–23, 1971.     

肠道菌群与健康、疾病和药物作用的影响

肠道菌群作为人体内一个复杂的微生态系统,在维持人体微生态的稳态中,肠道菌群在维持宿主生理功能具有上非常重要的作用,也对许多代谢性疾病、免疫性疾病以及肿瘤都有着密切的关系,且对于药物治疗合理安全有效具有重要意义。本文从正视存在人体的细菌的有益性和有害性、肠道菌群与健康和寿命、肠道菌群与疾病以及药物作用的影响等4方面分析和讨论。肠道菌群与不同类型药物的关系已经成为近些年的热点研究领域,本文分别讨论免疫治疗、化学药物、抗生素和中药的相关问题,希望为认识药物治疗过程、科学合理用药、认识药物作用机制、新药研究开发等研究有所参考。     

Molecular handling of cadmium in transporting epithelia

Cadmium (Cd) is an industrial and environmental pollutant that affects adversely a number of organs in humans and other mammals, including the kidneys, liver, lungs, pancreas, testis, and placenta. The liver and kidneys, which are the primary organs involved in the elimination of systemic Cd, are especially sensitive to the toxic effects of Cd. Because Cd ions possess a high affinity for sulfhydryl groups and thiolate anions, the cellular and molecular mechanisms involved in the handling and toxicity of Cd in target organs can be defined largely by the molecular interactions that occur between Cd ions and various sulfhydryl-containing molecules that are present in both the intracellular and extracellular compartments. A great deal of scientific data have been collected over the years to better define the toxic effects of Cd in the primary target organs. Notwithstanding all of the new developments made and information gathered, it is surprising that very little is known about the cellular and molecular mechanisms involved in the uptake, retention, and elimination of Cd in target epithelial cells. Therefore, the primary purpose of this review is to summarize and put into perspective some of the more salient current findings, assertions, and hypotheses pertaining to the transport and handling of Cd in the epithelial cells of target organs. Particular attention has been placed on the molecular mechanisms involved in the absorption, retention, and secretion of Cd in small intestinal enterocytes, hepatocytes, and tubular epithelial cells lining both proximal and distal portions of the nephron. The purpose of this review is not only to provide a summary of published findings but also to provide speculations and testable hypotheses based on contemporary findings made in other areas of research, with the hope that they may promote and serve as the impetus for future investigations designed to define more precisely the cellular mechanisms involved in the transport and handling of Cd within the body.     

海星皂苷生物活性与制备研究进展

海洋是全球药物研发的重要宝库，提高海洋生物资源深度开发和高值化利用能力，是我国海洋强国战略的重要组成部分，也是促进海洋经济可持续发展及实施“蓝色药库”的关键途径之一。海星属典型的棘皮动物，进化地位和生物学特征独特，是国际公认的药用/保健用海洋生物。海星中含有皂苷、多糖、多肽、氨基酸、胶原蛋白、甾醇及生物碱等多种营养成分和活性物质，其中海星皂苷在抗肿瘤、抗炎、抗衰老及降血脂等方面展现出良好的生物活性，在食品和药物研发领域具有巨大的发展潜力和广阔的应用前景。本文系统检索了近30年海星皂苷的研发现况，并且对近15年来海星皂苷的生物活性、提取分离及相关专利等方面取得的研究进展进行梳理，进而为其在营养保健和药物研发中的应用提供相关理论支持。     

Effects of DN-2327, a new anxiolytic,diazepam and buspirone on exploratory activity of the rat in an elevated plus-maze

In the present study, the effects of a new anxiolytic, DN-2327, were compared to those of diazepam and buspirone in rats in the elevated plus-maze test. Two indices of anxiety were obtained in this test: the number of entries into the open arms expressed as a percentage of the total number of arm entries and the percentage of time spent on the open arms. Both a typical anxiolytic, diazepam, at 2.5, 5 and 10 mg/kg, PO and a new anxiolytic, DN-2327, at 2.5 and 5 mg/kg, PO dose-dependently increased the two indices: the percentage of time spent on the open arms and the percentage of open-arm entries. On the other hand, pentylenetetrazol (PTZ) at 10 and 20 mg/kg, IP decreased the two indices dose dependently as did yohimbine at 1.5 and 3 mg/kg, IP. DN-2327 at 2.5 and 5 mg/kg, PO and diazepam at 5 and 10 mg/kg, PO dose dependently and significantly increased the two indices that were suppressed following administration of PTZ at 10 mg/kg, IP. The effects of both DN-2327, 5 mg/kg, PO, and diazepam, 10 mg/kg, PO, on the two indices were significantly antagonized by the benzodiazepine (BZD) receptor antagonist flumazenil, 20 mg/kg, IP. Buspirone (2.5–20 mg/kg, PO) did not affect either of the two responses but dose dependently decreased the number of rearings, although in the Vogel conflict test, the anti-conflict activity of buspirone was equipotent to that of diazepam and DN-2327 at the minimum effective dose (10 mg/kg, PO) of each drug. In conclusion, the present experiment revealed that the anxiolytic effect of DN-2327 in this test was clear, whereas buspirone showed no apparent effect.     

Subacute toxicity evaluation of a new camptothecin anticancer agent CKD-602 administered by intravenous injection to rats

The subacute toxicity of a new camptothecin anticancer agent, CKD-602, was investigated after 4-week repeated intravenous administration of the chemical in Sprague-Dawley rats. The test chemical was administered intravenously to rats at dose levels of 0, 0.003, 0.013, or 0.067 mg/kg/day for males and 0, 0.004, 0.018, or 0.089 mg/kg/day for females. At the end of the treatment period, 10 rats/sex/group were sacrificed. The remaining 5 rats/sex in the vehicle control and high dose groups continued the study without treatment for 2 weeks (recovery period). During the test period, clinical signs, mortality, body weights, food and water consumption, ophthalmoscopy, urinalysis, hematology, serum biochemistry, gross findings, organ weights, and histopathology were examined. In both sexes of the high dose group, an increase in the incidence of abnormal clinical signs and paleness of the eyes, a reduction in the body weight gain, food consumption and urine protein, and an increase in the water consumption were observed. Hematological investigations revealed a decrease in the red blood cells, hemoglobin and hematocrit and an increase in the mean corpuscular volume, mean corpuscular hemoglobin, platelets, and reticulocytes in a dose-dependent manner. Serum total cholesterol and total protein values were lower in females than those of controls, but not in males. An increase in the heart and liver weights and a decrease in the thymus weight were also found. Histopathological alterations included an increase in the incidence of atrophy of the sternal marrow, atrophy, fibrosis and mast cell hyperplasia of the femoral marrow, atrophy of the white pulp and extramedullary hematopoiesis of the spleen, atrophy of the thymus, auricular hypertrophy of the heart, extramedullary hematopoiesis and centriacinar telangiectasis of the liver, follicular degeneration of the ovary, and inflammation of the tail. The major treatment-related effects were not recovered at the end of 2-week recovery period. There were no adverse effects in the low and middle dose groups of both genders. In the present experimental conditions, the target organs were determined to be bone marrow, blood cells, spleen, liver, thymus, and heart. The no-observed-adverse-effect level was considered to be 0.013 mg/kg/day for males and 0.018 mg/kg/day for females.     

The concept of conditional pharmacology and toxicology

The concept of conditional pharmacology as initially elucidated by Dr Michael Whitehouse and his colleagues from their studies of drug-disease interactions has broad import in a rational drug discovery and development programme. The concept can be extended to toxicology and thus can be viewed as encompassing virtually all means and methods of discovering and enhancing the efficacy, while reducing the toxicity of drugs and biologics. The concept involves employing the physiological or metabolic activity, genetic and/or molecular structure of the host, of the disease process and/or of the parasite to activate and target the drug or biologic, as well as to regulate and delimit its activity. Thus, the concept not only applies to the treatment of inflammatory diseases, but also to the treatment of neoplastic and infectious diseases, to facilitating wound healing, and is in fact an underlying assumption, and expected consequence, of successful gene therapy. The concept applies to clinical studies as well, arguing for more pharmacokinetic and chrono-pharmacological studies in the early phases of clinical testing and the inclusion in later-stage clinical trials of more diverse populations, as regards age, gender and ethnicity, if the indication warrants. Facilitating and monitoring compliance, post-as well as pre-market approval, also are critical components of the fully implemented concept.     

新疆高寒地区家畜、家禽胆汁与肠内容物中的弯曲菌带菌情况的调查分析

目的调查高寒地区家畜、家禽胆汁与肠内容物中弯曲菌的分布情况。方法对12种家畜、家禽胆汁与肠内容物中的弯曲菌进行分离、培养、鉴定,并观察7种家畜、家禽胆汁弯曲菌的存活时间。结果在1814份家畜、家禽胆汁中发现,猪、牛、马、羊、狗、猫、鸡、鹅、鸭、鹌鹑、鸽子、家兔的胆汁中弯曲菌带菌率分别为6.67%、4.17%、4.94%、3.64%、8.93%、19.05%、6.41%、2.78%、6.48%、24.39%、5.66%、0。体外实验证明,弯曲菌在胆汁中可存活4～7周。结论高寒地区家畜、家禽肠内容物的带菌率均高于同种家畜、家禽的胆汁带菌率,提示该区家畜、家禽是弯曲菌的重要传染源。     

山葡萄素抗动脉粥样硬化分子机制研究

目的对从山葡萄籽来源的山葡萄素A和二脱氢山葡萄素A发挥抗动脉粥样硬化作用的分子机制进行深入的研究。方法采用体外培养的人脐静脉内皮细胞Hy926、鼠巨噬细胞RAM264.7和佛波酯(PMA)诱导的人单核细胞源性巨噬细胞THP-1,加入氧化低密度脂蛋白(ox-LDL)和脂多糖(LPS)损伤后,通过检测细胞活力(MTT法和LDH法)、活性氧、一氧化氮、丙二醛(MDA)和超氧化物歧化酶(SOD)的含量,以及细胞上清中细胞因子肿瘤坏死因子(TNF-α)和白介素1β(IL-1β)的分泌,单核细胞THP-1和内皮细胞Hy926的黏附作用,考察化合物的作用。结果化合物对ox-LDL导致的内皮细胞和巨噬细胞损伤有较明显的保护作用,并且抗氧化,减少氧、氮自由基产生,抑制LPS所致的巨噬细胞炎性因子释放,抑制单核细胞和内皮细胞黏附。结论山葡萄素A和二脱氢山葡萄素A对动脉粥样硬化(atherosclerosis,AS)发生早期事件的多个关键环节均有作用,提示其可能的动脉粥样硬化保护分子机制涉及多个靶点和通路的相互作用。     

虎杖的化学成分及药理作用研究进展

对近10年来中外期刊有关虎杖Polygonum cuspidatum的研究成果进行了检索,对从虎杖中分离并鉴定的化学成分及药理活性研究进展进行总结。虎杖中主要含有蒽醌类、二苯乙烯类、黄酮类、香豆素类以及一些脂肪酸类化合物,具有多种药理作用,包括抗炎、抗病毒、抗菌、调血脂、抗血栓、改变血流变、扩张血管、保护心肌、抗氧化、抗肿瘤,改善阿尔茨海默病及预防艾滋病等。多年来对虎杖的研究成果证明了其应用前景和开发价值,为更好地利用该资源提供依据。