Genotoxicity studies of glycidol fatty acid ester (glycidol linoleate) and glycidol

Glycidol fatty acid esters (GEs) are found in refined edible oils. Safety concerns have been alleged due to the possible release of glycidol (G), an animal carcinogen.     

盐酸地尔硫卓缓释片的制备及释药因素考察

目的制备日服1次的盐酸地尔硫卓缓释片并对释药因素进行考察。方法分别单独采用羟丙基甲基纤维素(HPMC)、联合应用HPMC与羧甲基纤维素钠(CMC-Na)作为基本骨架材料制备盐酸地尔硫卓缓释片,并对影响释药的因素进行考察。结果HPMC规格、压片压力对药物的释放几乎无影响;HPMC用量、稀释剂用量对药物的释放产生一定的影响;CMC-Na用量对药物的释放有较大影响。结论HPMC和CMC-Na联合应用可以有效地解决水易溶性药物盐酸地尔硫卓释药快的问题,加入一定比例的微晶纤维素(MCC)能促进药物中后期释放,以制备日服1次的盐酸地尔硫卓缓释片。     

椿乳凝胶成型工艺研究

目的:研究椿乳凝胶成型工艺,为临床治疗妇科疾病提供一种高效、低毒、方便的新剂型。方法:以凝胶形成及质量为考察指标,对4种材料进行筛选,并进行了药物加入及混合成型实验。结果:4%CMC-Na作为凝胶基质,药物以液态方式加入,外观均匀细腻,黏稠度适中。结论:该凝胶制备简单,质量易控,值得进一步研究开发。     

Metabolic profiling studies on the toxicological effects of realgar in rats by H NMR spectroscopy

The toxicological effects of realgar after intragastrical administration (1 g/kg body weight) were investigated over a 21 day period in male Wistar rats using metabonomic analysis of ¹H NMR spectra of urine, serum and liver tissue aqueous extracts. Liver and kidney histopathology examination and serum clinical chemistry analyses were also performed. ¹H NMR spectra and pattern recognition analyses from realgar treated animals showed increased excretion of urinary Kreb's cycle intermediates, increased levels of ketone bodies in urine and serum, and decreased levels of hepatic glucose and glycogen, as well as hypoglycemia and hyperlipoidemia, suggesting the perturbation of energy metabolism. Elevated levels of choline containing metabolites and betaine in serum and liver tissue aqueous extracts and increased serum creatine indicated altered transmethylation. Decreased urinary levels of trimethylamine-N-oxide, phenylacetylglycine and hippurate suggested the effects on the gut microflora environment by realgar. Signs of impairment of amino acid metabolism were supported by increased hepatic glutamate levels, increased methionine and decreased alanine levels in serum, and hypertaurinuria. The observed increase in glutathione in liver tissue aqueous extracts could be a biomarker of realgar induced oxidative injury. Serum clinical chemistry analyses showed increased levels of lactate dehydrogenase, aspartate aminotransferase, and alkaline phosphatase as well as increased levels of blood urea nitrogen and creatinine, indicating slight liver and kidney injury. The time-dependent biochemical variations induced by realgar were achieved using pattern recognition methods. This work illustrated the high reliability of NMR-based metabonomic approach on the study of the biochemical effects induced by traditional Chinese medicine.     

蜗牛酶在聚(N-异丙基丙烯酰胺)中的固定化及应用

将蜗牛酶固定到聚(N—异丙基丙烯酰胺)上得到一种热可逆的固定化酶。研究了固定化酶的性能和对几种不同底物的作用情况。结果表明蜗中酶对羧甲基纤维素钠、甲壳胺和可溶性棉花都有较好的降解活性。     

A bioactivity-guided study on the anti-diarrheal activity of Polygonum chinense Linn

Ethnopharmacological relevance

Polygonum chinense Linn., a folk medicine, has long been used for the treatment of diarrhea and enteritis in southwestern China. However, the components responsible for its anti-diarrheal activity are still poorly understood.

Aim of the study

To determine anti-diarrheal activities of Polygonum chinense L. and to identify its active components through bioactivity-guided isolation technique.

Materials and methods

Animals were orally administered with the extract of Polygonum chinense L. The anti-diarrheal effects of 75% ethanol extract, four fractions with different polarities from 75% ethanol extract, different eluates collected from Diaion HP-20 macroporous resin chromatography, ellagic acid and corilagin, were examined based on mouse models of castor oil- and magnesium sulfate-induced diarrhea.

Results

The results showed that the 75% ethanol extract of Polygonum chinense L. exhibited significant anti-diarrheal activities in a dose-dependent manner in two mouse models. Through in vivo bioactivity-guided fractionation processes, n-butanol and aqueous fractions were found to exhibit prominent anti-diarrheal activities, and two major compounds, ellagic acid and corilagin, from these active fractions were found to possess anti-diarrheal effects.

Conclusion

Present study provides evidence of the utilization of Polygonum chinense L. for diarrhea, and ellagic acid and corilagin are two components contributing to the anti-diarrheal effect.     

Antihyperglycemic,hypolipidemic and antioxidant activities of total saponins extracted from Aralia taibaiensis in experimental type 2 diabetic rats

Ethnopharmacological relevance

As a well-known traditional Chinese medicine the root bark of Aralia taibaiensis has multiple pharmacological activities, including relieving rheumatism, promoting blood circulation to arrest pain, inducing diuresis to reduce edema, and antidiabetic action. It has long been used as a folk medicine for the treatment of traumatic injury, rheumatic arthralgia, nephritis, edema, hepatitis and diabetes mellitus in China.

Aim of study

To evaluate the antihyperglycemic, hypolipidemic and antioxidant activities of total saponins extracted from Aralia taibaiensis (SAT) in experimental type 2 diabetic mellitus (T2DM) rats.

Materials and methods

Acute toxicity was studied in rats to determine the safe oral dose of SAT. Then, SAT was given orally to normal and streptozotocin–nicotinamide induced T2DM rats at 80, 160 and 320 mg/kg doses for a series of 28 days to determine the antihyperglycemic activity. Glibenclamide (600 μg/kg), a standard antidiabetic drug, was used as a positive control drug. At the end of treatment, biochemical parameters and antioxidant levels were measured to evaluate the hypolipidemic and antioxidant activities of SAT.

Results

Oral administration of SAT did not exhibit toxicity and death at a dose not more than 2000 mg/kg. SAT dose-dependently improved the symptoms of polydipsia, polyuria, polyphagia and weight loss in diabetic rats. Compared with diabetic control group, administration of 320 mg/kg SAT resulted in significant (P<0.05) fall in the levels of fasting blood glucose, glycosylated hemoglobin, creatinine, urea, alanine transarninase, aspartate aminotransferase, total cholesterol, triglycerides, low density lipoprotein cholesterol and malondialdehyde, but significant (P<0.05) increase in the levels of serum insulin, superoxide dismutase and reduced glutathione. However, SAT did not have any effect on the normal rats.

Conclusions

SAT had excellent antihyperglycemic, hypolipidemic and antioxidant activities in T2DM rats and might be a promising drug in the therapy of diabetes mellitus and its complications.     

LHRH拮抗剂-CMC复合物的鉴别及含量测定

目的制备促黄体生成激素释放激素(LHRH)拮抗剂LXT-101与羧甲基纤维素钠的不溶性复合物,对形成的复合物进行鉴别,并测定其中多肽的含量。方法分别将LXT-101和羧甲基纤维素钠制成水溶液,混合制成不溶性复合物;采用DSC法对复合物进行鉴别,并以HPLC法测定了复合物中多肽的含量和不同溶媒中的溶解度。结果复合物、物理混合物和药物及辅料的DSC图谱明显不同;复合物中多肽含量达80%;以5%醋酸溶液作为多肽和复合物的溶解介质,在10~80μg·ml-1范围内,峰面积与药物浓度呈良好线性关系,r=0.9999;平均回收率99.8%,精密度RSD为0.54%;复合物的溶解度比原药明显降低。结论药物与羧甲基纤维素钠之间确已形成复合物;复合物在水和磷酸盐缓冲液中的溶解度明显降低,有望进一步制成缓释制剂。     

银杏提取物缓释片的制备及其体外释放度的研究

目的:制备银杏提取物缓释片并考察其体外释放度.方法:以溶胀性材料羧甲基纤维素钠和羟丙甲基纤维素为骨架材料,直接粉末压片制备银杏提取物缓释片.根据单因素试验中各因素对银杏提取物体外释放度影响结果,进行正交设计,优化处方和工艺,以f_2相似因子法评价释放的差异.结果:羟丙甲基纤维素与羧甲基纤维素钠的用量比、羟丙甲基纤维素的黏度、不同的稀释剂均对药物释放有一定的影响,而缓释片的硬度、片重等对药物的释放没有显著的影响.结论:以羟丙甲基纤维素和羧甲基纤维素钠为骨架材料,制得持续释药12 h的银杏提取物缓释片.     

茶碱亲水基质蚀解片的溶出

以羟丙基甲基纤维素（ＨＰＭＣ）为亲水基质制备茶碱控释片，研究了ＨＰＭＣ的粘度和加入量对片剂溶出状况的影响。少量羟甲基纤维素钠（ＣＭＣ－Ｎａ）也能影响片剂的溶出速率，改变片剂的溶出级数。调节ＨＰＭＣ和ＣＭＣ－Ｎａ的配比，可使茶碱控释片呈零级溶出。