山梨酸在肌苷口服液中的防腐作用

为使肌苷口服液在贮存期内的色泽和成分含量稳定,在生产工艺上可取消灭茵工序,改为添加适宜的防腐剂。本实验对苯甲酸、苯甲酸钠、尼泊金、山梨酸、山梨酸钾等防腐剂进行了筛选,将其与灭菌处理对肌苷口服液的防腐作用做了比较。结果表明,山梨酸、苯甲酸抑制霉菌作用较强。山梨酸及其盐类具有使用安全,不影响药品原有色、香、味和药用成分的特点。     

滋阴清胃汤治疗复发性口腔溃疡的实验研究

目的:观察滋阴清胃汤抑菌、抗炎、镇痛及抗口腔溃疡作用。方法:①通过抑菌实验观察该药抑菌效果;②采用小鼠热板法观察该药的镇痛作用;③通过对二甲苯致小鼠耳廓肿胀观察抗炎作用;④将40只大鼠随机分为该药高、低剂量组,阳性对照组及模型对照组,用90%苯酚制造口腔溃疡模型,观察该药的抗溃疡作用。结果:该药对金黄色葡萄球菌、大肠埃希菌和甲型溶血性链球菌有不同程度的抑制作用;能明显提高小鼠热板刺激的痛阈值,2个剂量组均可明显改善大鼠口腔溃疡病理变化,缩短溃疡修复时间。结论:滋阴清胃汤能抑制金黄色葡萄球菌、大肠埃希菌和甲型溶血性链球菌,有抗炎、镇痛及抗口腔溃疡的作用。     

痔消带的药理作用研究

中药保健弹性三角兜带(简称痔消带,系以麝香、雄黄、三七、蜀椒等十余味中药制成的方剂。经临床观察,本品对治疗和预防肛门炎性疾病具有良好的效果,总有效率99.4%,治愈率83.08%。药效学研分证明:本品具有较强的抗炎和镇痛作用(P<0.05);对金黄色葡萄球菌有抑制作用;无刺激,无过敏性。现将结果报道如下:     

鼻渊康口服液主要药效学的研究

目的:探讨鼻渊康口服液的抗炎、解热和体外抑菌作用。方法:观察鼻渊康口服液对二甲苯所致小鼠耳廓炎症的影响,对大鼠棉球肉芽肿增生的影响,对细菌内毒素所致家兔体温升高的抑制作用,对金黄色葡萄球菌、表皮葡萄球菌、乙型溶血性链球菌、绿脓杆菌的体外抑制作用。结果:鼻渊康口服液对二甲苯所致小鼠耳廓炎症及小鼠腹腔毛细血管通透性增加有明显抑制作用,对大鼠棉球肉芽肿增生亦有明显抑制作用,此外,还对细菌内毒素所致家兔体温升高有抑制作用,对前述4种细菌有不同程度抑制作用。结论:鼻渊康口服液具有抗炎、解热和抑菌作用。     

上感口服液抗炎解热作用的研究

目的:研究上感口服液抗炎解热等药效作用,方法:观察上感口服液对二甲苯所致小鼠耳廓炎性肿胀的影响,对静脉注射脱脂牛奶致家兔发热的影响。对静脉注射刚果红后小鼠吞噬细胞吞噬功能的影响。以及对金黄色葡萄球菌、溶血性链球菌、白色葡萄球菌的体外抑制作用。结果:该药可抑制动物耳廓炎症,有较好的解热作用,可增强吞噬细胞功能,可明显抑制α溶血性链球菌、白色葡萄球菌生长。结论:上感口服液可拮抗急性渗出性炎症,增加非特异性免疫功能,有较好的解热、抑菌作用。     

皮康外洗液的药效学初步研究

目的:探讨皮康外洗液的抗炎、抗过敏及抗菌作用。方法:采用抗炎实验、迟发性过敏反应、体外抑菌试验等方法进行研究。结果:皮康外洗液对二甲苯诱导的小鼠耳廓肿胀及2,4-二硝基氟苯诱导的小鼠迟发性过敏反应均有明显抑制作用,对豚鼠脱毛区皮肤无刺激反应,抑菌实验表明对绿脓杆菌、金黄色葡萄球菌等多种致病菌有一定的抑制作用。结论:皮康外洗液具有较好的抗炎及抗菌作用,且对皮肤无刺激,本研究为该药治疗小儿皮肤病提供了初步的药效学资料。     

螺旋霉素的体外抗菌、抗炎活性研究

目的:考察螺旋霉素的体外抗菌及抗炎活性.方法:以金黄色葡萄球菌(Staphylococcus aureus),枯草芽孢杆菌(Bacillus subtilis),大肠杆菌(Escherichia coli)、绿脓杆菌(Pseudomonas aeruginosa)为供试菌种研究抗菌效果,采用微量肉汤稀释法测定MIC、M...     

通窍导浊颗粒治疗慢性细菌性前列腺炎的实验研究

目的研究通窍导浊颗粒治疗慢性细菌性前列腺炎的疗效及作用机理.方法通过体外抑菌实验、对大鼠细菌性前列腺炎模型影响的研究,观察通窍导浊颗粒在抑菌、抗炎方面的作用.结果体外研究表明,通窍导浊颗粒对金黄色葡萄球菌、大肠杆菌、表皮葡萄球菌具有显著的抑菌作用.动物试验表明,通窍导浊颗粒对金黄色葡萄球菌和大肠杆菌所致大鼠细菌性前列腺炎有治疗作用.结论通窍导浊颗粒具有抑菌、抗炎的作用,为本品用于慢性细菌性前列腺炎治疗提供了实验依据.     

10%氯化钾溶液防腐剂的筛选

目的选择10%氯化钾溶液最佳防腐剂。方法对含不同防腐剂和不含防腐剂的10%氯化钾溶液及09%氯化钠注射液人为污染10～100个微生物，在溶液与微生物接触1 h和7 d后测定和计算存活的菌落数。结果含羟苯乙酯、桂皮醛防腐剂的10%氯化钾溶液对枯草芽胞杆菌防腐效果弱，含苯甲酸、山梨酸的10%氯化钾溶液对大肠埃希菌、枯草芽胞杆菌、金黄色葡萄球菌、真菌、酵母菌等防腐效果好。结论 10%氯化钾溶液的最佳防腐剂是山梨酸。     

土贝母皂苷抗炎、抗肿瘤和抗促瘤的构效关系(英文)

目的:研究土贝母苷Ⅰ、Ⅱ和Ⅲ的抗炎、抗瘤和抗促瘤效果的构效关系。方法:从中药土贝母中分离土贝母苷Ⅰ、Ⅱ和Ⅲ,并研究它们的抗炎、抗瘤和抗促瘤活性及急性毒性。结果:土贝母苷Ⅰ、Ⅱ和Ⅲ是来自同一植物的齐墩果烷型三萜皂苷天然类似物。实验证实,它们都具有抗炎、抗瘤和抗促瘤效果。然而,土贝母苷Ⅱ的抗炎、抗瘤和抗促瘤效果比土贝母苷Ⅰ强,其急性毒性却比土贝母苷Ⅰ低;土贝母苷Ⅲ的抗炎、抗瘤和抗促瘤效果比土贝母苷Ⅱ高,其急性毒性也比土贝母苷Ⅱ强。结论:土贝母苷Ⅱ16位碳上的羟基对于增强土贝母苷Ⅱ的生物学活性和降低它的毒性具有重要意义;土贝母苷Ⅲ和土贝母苷Ⅱ在B和/或C位上化学结构的差异对于增强土贝母苷Ⅲ的生物活性和毒性起着重要作用。     

Evaluation of the genotoxic potential of sorbic acid and potassium sorbate.

The genotoxic potential of sorbic acid and potassium sorbate was investigated in vivo and in vitro. Oral administration of sorbic acid (up to 5000 mg/kg body weight) did not induce sister chromatid exchanges or the formation of micronuclei in bone marrow cells of mice. Intraperitoneal treatment of rats with 400-1200 mg potassium sorbate/kg body weight did not alter the elution profile of DNA from isolated liver cells in the in vivo alkaline elution assay. Sorbic acid did not induce DNA repair in cultured human A549 cells in the unscheduled DNA synthesis (UDS) assay. In vitro incubation of the cells with 1-1000 micrograms potassium sorbate/ml, in the absence or presence of rat liver homogenate, did not result in the formation of DNA single-strand breaks in the alkaline elution assay. These results demonstrate that sorbic acid and its potassium salt are not genotoxic in vivo or in vitro. In contrast to sorbic acid and potassium sorbate, sodium sorbate is very sensitive to oxidative degradation; the main oxidation product was identified to be 4,5-oxohexenoate, which was mutagenic in the Ames test.     

Effects of sorbic acid and its salts on chromosome aberrations, sister chromatid exchanges and gene mutations in cultured Chinese hamster cells

The ability of sorbic acid and its potassium and sodium salts to induce chromosome aberrations, sister chromatid exchanges (SCE) and gene mutations in cultured Chinese hamster V79 cells was examined. Sodium sorbate caused significant induction of chromosome aberrations and SCE, and also induced 6-thioguanine-resistant mutations in a dose-dependent manner. The clastogenic potency of sodium sorbate was found to be less than one hundredth of that of the potent clastogen N-methyl-N'-nitro-N-nitrosoguanidine. The induction of SCE by sodium sorbate was twice the control level, whereas that by methyl methanesulphonate, a potent inducer of SCE, was 14 times the control level. The mutagenic potency of sodium sorbate was less than one-tenth that of ethyl methanesulphonate, a potent inducer of mutation, when compared at an equitoxic level. Sorbic acid and its potassium salt induced chromosome aberrations, but only at the highest doses tested. These compounds also induced 1.2 times the control level of SCE, but neither compound induced 6-thioguanine-resistant mutations. The cytogenetic activity of sodium sorbate was concluded not to be due to the effect of osmotic pressure or an impurity. These results indicate that sodium sorbate is a genotoxic agent, although its potency seems to be weak, and that sorbic acid and potassium sorbate are less genotoxic than the sodium salt.     

Comparative toxicity of physiological and biochemical parameters in Euglena gracilis to short-term exposure to potassium sorbate

Ecotoxicology - Potassium sorbate is the potassium salt of sorbic acid, is a widespread and efficient antioxidant that has multiple functions in plants, traditionally associated with the reactions...     

Mutagenicity and genotoxicity of sorbic acid-amine reaction products.

Sorbic acid as well as potassium and calcium sorbate (E202 and E203) are legally used as preservatives in numerous processed foods. Owing to its system of conjugated double bonds, sorbic acid is likely to undergo a nucleophilic attack, which may turn it into mutagenic products. The cyclic derivatives resulting from a double addition reaction between sorbic acid and various amines at two different temperatures (50 degrees C and 80 degrees C) have been analysed. A genotoxicity study has been performed with HeLa cells and plasmid DNA. A mutagenesis study has been carried out by using the Ames test. A SOS spot test and a cytotoxicity study have been realised as well. The results showed that the products involved exhibited neither mutagenic nor genotoxic activities.     

NMR analysis of ion pair formation between timolol and sorbic acid in ophthalmic preparations

Ion pair formation between timolol and sorbic acid was investigated using NMR spectroscopy in order to clarify their interactions within ophthalmic preparation. (13)C and (1)H NMR spectra of timolol, sorbic acid, and a mixture of the two were obtained, and the signal changes induced by pairing were observed. The carbon signals of the butylaminopropanol moiety of timolol were markedly shifted in the mixture, as were the carboxyl and conjugated carbons assigned to sorbic acid. The localizations of the changes in each molecule revealed the binding sites. The profiles of butylaminopropanol carbon chemical shifts plotted against a molar ratio of sorbate were synchronized, which suggested a single type of interaction with sorbic acid. The Job plot showed a typical pattern with a single-maximum at a mole function of 0.5, indicating the presence of a 1:1 complex of timolol and sorbic acid. The stability constants (K) of the timolol-sorbate and timolol-maleate pairs were 1.9x10(1) and 2.2x10(2)M(-1), respectively. The higher K value of the timolol-maleate interaction suggested that it was dominant to the timolol-sorbate interaction when maleate and sorbate coexisted within a timolol solution. Here, we demonstrated evidence of an interaction between timolol and sorbic acid using simple NMR measurements, which suggested the existence of ion pair formation derived from charge neutralization. Our analysis using NMR spectroscopy should advance the understanding and optimization of formulations that are based on ion pair.     

利巴韦林口服溶液中抑菌剂的筛选

目的:筛选适用于利巴韦林口服溶液的抑菌剂。方法:对利巴韦林口服液分别以不同浓度的苯甲酸钠(0.10%、0.20%、0.30%)、山梨酸钾(0.10%、0.20%、0.30%)和尼泊金甲、乙酯等量混合物(0.03%、0.04%、0.05%)作抑菌剂时对铜绿假单胞菌、金黄色葡萄球菌、大肠埃希菌、白色念珠菌和黑曲霉的抑菌活性进行试验,根据样品不同培养时间(0、14、28d)时存活菌数的常用对数值相对于初始值减少程度评价各抑菌剂的抑菌效力。结果:以0.30%的苯甲酸钠作为抑菌剂时,与0d菌数比较,样品在14d时细菌常用对数值下降值最大(大于1.0),28d时霉菌数目未见增长,真菌数目14、28d时未见增长。结论:选用0.30%的苯甲酸钠作为利巴韦林口服液的抑菌剂较为合适。     

Genotoxicity and cell transformation studies with sorbates in Syrian hamster embryo fibroblasts.

Sorbic acid, sodium sorbate and potassium sorbate were tested for their genotoxic potential in the Syrian hamster embryo (SHE) fibroblast micronucleus assay and the SHE cell transformation test in vitro. Sorbic acid and potassium sorbate showed no activity in either test system. When freshly prepared sodium sorbate solutions were used, no genotoxic or cell-transforming activity was detected. However, sodium sorbate as stored solution, which previously had been heated and sonicated to facilitate solubilization, yielded a positive response in both test systems. It is concluded that oxidation products of sodium sorbate that possess genotoxic and cell-transforming properties are formed under conditions of heating, sonication and storage.     

金铃子散及单味药镇痛抗炎作用的比较

目的:观察金铃子散及各单味药对小鼠镇痛抗炎作用的影响。方法:以热板法和醋酸扭体法观察金铃子散及各单味药的镇痛作用;制作由二甲苯致小鼠耳廓肿胀模型,观察小鼠金铃子散及各单味药的抗炎作用。结果:热板法显示各组均能明显提高小鼠的痛阈值,对醋酸所致的扭体也有明显的抑制作用,对二甲苯所致的耳廓肿胀也有明显的抑制作用,其中以金铃子散组作用较为明显,醋延胡索组强于炒川楝子组。结论:金铃子散效果优于单方;单方药物中醋延胡索的镇痛抗炎作用最强。