Preparation and evaluation of Vinpocetine self-emulsifying pH gradient release pellets

The main objective of this study was to develop a pH gradient release pellet with self-emulsifying drug delivery system (SEDDS), which could not only improve the oral bioavailability of Vinpocetine (VIN), a poor soluble drug, but reduce the fluctuation of plasma concentration. First, the liquid VIN SEDDS formulation was prepared. Then the self-emulsifying pH gradient release pellets were prepared by extrusion spheronization technique, and formulation consisted by the liquid SEDDS, absorbent (colloidal silicon dioxide), penetration enhancer (sodium chloride), microcrystalline cellulose, ethyl alcohol, and three coating materials (HPMC, Eudragit L30D55, Eudragit FS30D) were eventually selected. Three kinds of coated pellets were mixed in capsules with the mass ratio of 1:1:1. The release curves of capsules were investigated in vitro under the simulated gastrointestinal conditions. In addition, the oral bioavailability and pharmacokinetics of VIN self-emulsifying pH gradient release pellets, commercial tablets and liquid VIN SEDDS were evaluated in Beagle dogs. The oral bioavailability of self-emulsifying pH gradient release pellets was about 149.8% of commercial VIN tablets, and it was about 86% of liquid VIN SEDDS, but there were no significant difference between liquid SEDDS and self-emulsifying pH gradient release pellets. In conclusion, the self-emulsifying pH gradient release pellets could significantly enhance the absorption of VIN and effectively achieve a pH gradient release. And the self-emulsifying pH gradient release pellet was a promising method to improve bioavailability of insoluble drugs.     

Pharmacokinetics and N-acetylation metabolism of S-methyl-l-cysteine and trans-S-1-propenyl-l-cysteine in rats and dogs

1.?Pharmacokinetics and N-acetylation metabolism of S-methyl-L-cysteine (SMC) and trans-S-1-propenyl-L-cysteine (S1PC) were examined in rats and dogs. SMC and S1PC (2–5?mg/kg) were well absorbed in both species with high bioavailability (88–100%).

2.?SMC and S1PC were excreted only to a small extent in the urine of rats and dogs. The small renal clearance values (<0.03?l/h/kg) indicated the extensive renal reabsorption of SMC and S1PC, which potentially contributed to their long elimination half-lives (>5?h) in dogs.

3.?S1PC, but not SMC, underwent N-acetylation extensively in vivo, which can be explained by the relative activities of N-acetylation of S1PC/SMC and deacetylation of their N-acetylated forms, N-acetyl-S1PC/N-acetyl-SMC, in the liver and kidney in vitro. The activities for S1PC N-acetylation were similar to or higher than those for N-acetyl-S1PC deacetylation in liver S9 fractions of rat and dog, whereas liver and kidney S9 fractions of rat and dog had little activity for SMC N-acetylation or considerably higher activities for N-acetyl-SMC deacetylation.

4.?Our study demonstrated that the pharmacokinetics of SMC and S1PC in rats and dogs was characterized by high bioavailability and extensive renal reabsorption; however, the extent of undergoing the N-acetylation metabolism was extremely different between SMC and S1PC.     

明党参居群间根中水溶性成分HPLC分析

目的:分析我国明党参主要分布区内明党参居群间根中水溶性成分的相似性,为明党参种质资源评价及药材质量控制提供理论依据。方法:运用冷浸法和HPLC对10个居群明党参根中水溶性成分进行提取与分析,根据各居群明党参根中主要水溶性成分的相对含量,由夹角余弦法计算相似系数,采用UPGMA方法进行聚类,构建树状图。结果:明党参居群间根中水溶性成分差异显著。九华山居群水溶性浸出物的含量最高,大龙山和浮山2个居群水溶性浸出物的含量低于《中国药典》标准。各居群根中水溶性成分HPLC图谱差异明显,共有峰数目少。居群间根中水溶性成分的相似系数差距很大,为0.030 6~0.999 5。紫金山居群根中水溶性成分最为特殊,除与红山居群的相似系数达到0.969 7的较高水平之外,与其他7个居群的相似系数均较小。而老山、茅山、青龙山和琅琊山4个居群根中水溶性成分的组成极为相似,居群间的相似系数均在大于0.99的很高水平。聚类结果将10个居群的明党参分成3类。结论:明党参居群间根中水溶性成分存在丰富的多样性,明显地分为3个类型。     

The effect of oil and water-soluble contrast medium in hysterosalpingography on thyroid function

Hysterosalpingography (HSG) using iodinated contrast medium is X-ray diagnostic test that examines the inside of the uterus and fallopian tubes in infertile women. In this study, we compared thyroid function (thyroid stimulating hormone: TSH and free-T4: FT4 levels) after HSG with an oil-soluble contrast medium (OSCM) and a water-soluble contrast medium (WSCM). One hundred and sixty-four and 94 patients with normal thyroid function received HSG with OSCM and WSCM, respectively. Approximately 25% of the women in the OSCM group developed subclinical hypothyroidism (SCH), whereas only less than 10% of the patients in the WSCM group developed SCH. Our data clearly indicate that WSCM is safe for thyroid function in women who plan to get pregnant.     

Rheum australe D. Don: a review of its botany, ethnobotany, phytochemistry and pharmacology

Ethnopharmacological relevance

Rheum australe D. Don (Polygonaceae) has been commonly used in traditional medicine for a wide range of ailments related to the circulatory, digestive, endocrine, respiratory and skeletal systems as well as to infectious diseases.

Aim of the review

To provide the up-to-date information that is available on the botany, traditional uses, phytochemistry, pharmacology and toxicology of Rheum australe. Additionally, to highlight the possible uses of this species to treat different diseases and to provide a basis for future research.

Materials and methods

The present review covers the literature available from 1980 to 2011. The information was collected from scientific journals, books, theses and reports via a library and electronic search (Google Scholar, Web of Science and ScienceDirect).

Results

Ethnomedical uses of Rheum australe have been recorded from China, India, Nepal and Pakistan for 57 different types of ailments. The phytochemical studies have shown the presence of many secondary metabolites belonging to anthraquinones, stilbenes, anthrones, oxantrone ethers and esters, chromones, flavonoids, carbohydrate, lignans, phenols and sterols. Crude extracts and isolated compounds from Rheum australe show a wide spectrum of pharmacological activities, such as antidiabetic, anti-inflammatory, antifungal, antimicrobial, antioxidant, anticancer, hepatoprotective and immune-enhancing activities, as well as a usefulness for improving renal function.

Conclusion

Rheum australe has been widely used source of medicine for years without any adverse effects. Many studies have provided evidence for various traditional uses. However, there is a need for additional studies of the isolated compounds to validate the traditional uses in human models. The present review on the botany, traditional uses, phytochemistry and toxicity has provided preliminary information for further studies and commercial exploitations of the plant.     

河南产丹参水溶性提取物提取工艺研究

目的：探讨丹参水溶性提取物的最佳提取工艺。方法：以酸水为溶剂,加热回流法提取丹参水溶性提取物,采用正交试验设计考察时间、温度、pH值、提取溶剂体积等4因素,对丹参水溶性成分的影响,筛选出最佳的提取工艺;以丹酚酸B为标准品,采用HPLC法测定含量。结果：丹参水溶性提取物以酸水做溶剂,最佳提取工艺为pH值为3的酸水,8倍量,温度100℃,加热回流4h。结论：本提取工艺所得提取物丹酚酸B含量较高,简单,经济,可行性强,适合工业大批量生产。     

高山红景天挥发油水溶性部分GC－MS分析

目的: 分析吉林长白山产高山红景天（Rhodiola sachalinensis A.Bor.）干燥根的挥发油水溶性部分化学成分。方法: 采用水蒸汽蒸馏法提取挥发油水溶性部分并利用气相色谱-质谱（GC-MS）对其成分进行分析。结果: 共分离出25个峰,鉴定出18种化合物,根据面积归一法测其相对含量为90.17%。高山红景天挥发油水溶性部分中主要成分为桃金娘烯醇（28.04%）,顺式氧化芳樟醇（16.90%）,正辛醇（10.05%）等。结论: GC-MS结果为红景天的产品开发提供了理论基础。     

附子水溶性生物碱提取纯化工艺研究

目的研究附子水溶性生物碱的提取纯化工艺。方法采用UPLC-MS/MS技术,以14种生物碱(多根乌头碱、宋果灵、附子灵、尼奥灵、塔拉萨敏、新乌头原碱、乌头原碱、次乌头原碱、苯甲酰新乌头原碱、苯甲酰乌头原碱、苯甲酰次乌头原碱、新乌头碱、乌头碱、次乌头碱)的总量为考察指标,采用单因素实验和正交试验方法筛选最佳提取工艺;以8种水溶性生物碱(乌头原碱、新乌头原碱、次乌头原碱、附子灵、尼奥灵、塔拉萨敏、宋果灵、多根乌头碱)的量为考察指标,对5种大孔树脂吸附和解吸附性能进行考察,优选最佳纯化工艺。结果最佳提取纯化工艺为蒸附片加10倍量pH值3.5的酸水,煎煮3次(维持pH值约3.5),每次2 h,合并水煎液,用20%NaOH溶液调pH值10.0,加热回流水解2 h后,放冷,调pH值11.0,上大孔树脂HPD 300,上样量为生药2.5 g/mL树脂,6 BV水洗除杂,4 BV 80%乙醇洗脱,收集乙醇洗脱液,减压浓缩干燥,即得附子水溶性生物碱提取物。该提取物收率为1.69%,其中新乌头原碱、乌头原碱、次乌头原碱、附子灵、尼奥灵、塔拉萨敏、多根乌头碱、宋果灵的总量高达约15%。结论优选得到的提取纯化工艺稳定可行,为附子水溶性生物碱的研究应用提供参考。     

对注射用水溶性维生素细菌内毒素检查法的商榷

目的用细菌内毒素检查用水替代“盐酸三羟甲基氨基甲烷缓冲液”作为注射用水溶性维生素的稀释剂,进行细菌内毒素检查,以简化操作步骤,提高检验结果的准确性和可靠性。方法通过用细菌内毒素检查用水作稀释剂,进行注射用水溶性维生素细菌内毒素检查干扰试验,确定其最大不干扰浓度。结果每瓶先用细菌内毒素检查用水10mL溶解,再用细菌内毒素检查用水4倍稀释后对细菌内毒素检查无干扰作用。结论进行注射用水溶性维生素细菌内毒素检查时,用细菌内毒素检查用水作稀释剂替代“盐酸三羟甲基氨基甲烷缓冲液”不仅是可行的,而且方法简便、结果可靠。     

不同炮制条件对何首乌水溶性糖含量和分子量的影响及其药效相关性研究

目的研究比较炮制条件对何首乌水溶性多糖含量和分子量的影响,并探讨其与药效的相关性。方法制首乌样品制备分别采用传统笼屉蒸法和流通蒸汽锅蒸法,并设定不同的蒸制时间。采用蒽酮-硫酸法测定样品中水溶性糖的含量;样品总糖溶液用不同分子量超滤膜过滤,并测定滤液中的糖含量,比较不同分子量多糖含量变化。建立大鼠血虚动物模型,比较样品粗多糖的药效差异。结果生何首乌及不同炮制品水溶性糖含量及其分子量分布不同。除炮制72h的制何首乌外,生首乌粗多糖和其他各制首乌样品粗多糖对模型大鼠红系指标均有一定改善作用。结论多糖为何首乌药效物质,炮制可导致何首乌多糖分子量的改变,其药效与分子量有关。