胃散对胃溃疡模型大鼠胃黏膜保护作用的研究

目的 研究胃散对胃溃疡大鼠胃黏膜的保护作用。方法 采用乙酸烧灼型胃溃疡模型、幽门结扎型胃溃疡模型、乙醇损伤型胃溃疡模型,检测溃疡指数、胃酸总酸度、胃酸分泌速度和胃蛋白酶活性,综合考察胃散对胃溃疡模型大鼠胃黏膜的保护作用。结果 胃散在1、0.5、0.25 g/kg剂量下,对乙酸烧灼型胃溃疡有非常显著的促愈合作用;对幽门结扎型胃溃疡的形成有显著的抑制作用;对乙醇损伤的胃黏膜也有显著的保护作用;对胃液总酸度、胃酸分泌速度和胃蛋白酶活性有明显抑制作用,显著增加胃液分泌量。结论 胃散具有增加胃液分泌、抑制胃酸分泌、抑制胃蛋白酶活性、保护胃黏膜和防止胃溃疡的作用。     

铝镁硅油片对大鼠胃酸和胃蛋白酶的影响

目的考察铝镁硅油片对大鼠胃酸和胃蛋白酶活性的影响。方法以胃酸和胃蛋白酶活性测定作为药效学指标。结果和结论与对照组相比 ,本品不影响大鼠正常胃液分泌,但能显著升高胃液 pH和降低总酸排出量,高剂量组(600mg·kg-1)尚能显著降低胃液总酸度 ;能抑制大鼠胃蛋白酶活性,180mg·kg-1,600mg·kg-1 的作用更为显著(P<0.05,P<0.01),其剂量和酶活性抑制作用间呈良好的线性关系     

六叶能消胶囊抗大鼠胃溃疡的研究

目的 研究六味能消胶囊对幽门结扎型大鼠胃溃疡模型的影响及其作用机制.方法 采用幽门结扎法制备大鼠胃溃疡模型,观察溃疡指数.测其胃液量、胃液总酸度、胃蛋白酶活性;制备胃组织匀浆,测其一氧化氮(NO)、丙二醛(MDA)的含量及超氧化物歧化酶(SOD)的活性.结果 六味能消胶囊对幽门结扎型胃溃疡大鼠的溃疡、胃液量、总酸度及胃蛋白酶活性均有明显的抑制作用,能显著增加胃组织中NO含量和SOD活性,降低MDA的含量.结论 六味能消胶囊具有一定的抗胃溃疡作用.     

健脾消积颗粒对脾虚大鼠胃液、胃酸的分泌及胃蛋白酶活性的影响

目的:探讨健脾消积颗粒对脾虚大鼠胃液、胃酸分泌及胃蛋白酶活性的影响。方法:用大黄造成大鼠脾虚模型后,再灌服健脾消积颗粒药液,于末次灌胃后1 h,测定大鼠胃液、胃酸分泌量、胃蛋白酶活性。结果:健脾消积颗粒的胃液、胃酸分泌量和胃蛋白酶的活性与模型组比较,差异具有统计学意义(P<0.05或P<0.01)。结论:健脾消积颗粒对脾虚大鼠的健脾作用机制之一与其能使脾虚大鼠的胃液、胃酸分泌增加、胃蛋白酶活性提高有关。     

苗药良姜胃疡胶囊对胃溃疡模型大鼠的预防作用及机制研究

目的:研究苗药良姜胃疡胶囊对胃溃疡大鼠模型的预防作用及机制。方法:将大鼠随机分为正常组(生理盐水)、模型组(生理盐水)、阳性对照组(奥美拉唑,0.02 g/kg)和良姜胃疡胶囊低、中、高剂量组(0.3、0.6、1.2 g/kg),每组12只。每天灌胃给药1次,连续给药1周。末次给药1 h后,除正常组外,其余各组大鼠均灌胃无水乙醇复制胃溃疡模型。造模1 h后,测定各组大鼠胃液量、胃液pH、胃蛋白酶活力、胃溃疡面积及胃溃疡抑制率;苏木精-伊红(HE)染色后显微镜下观察各组大鼠胃黏膜组织病理学变化,酶联免疫吸附试验法检测各组大鼠血清中肿瘤坏死因子α(TNF-α)、白细胞介素6(IL-6)水平;Western blot法检测各组大鼠胃组织中核转录因子κB(NF-κB)通路相关蛋白[磷酸化核因子κB亚基65(p-NF-κB p65)、磷酸化核因子κB抑制蛋白α(p-IκBα)]的水平。结果:与正常组比较,模型组大鼠胃液量、胃蛋白酶活力、胃溃疡面积和血清中TNF-α、IL-6水平及胃组织中p-NF-κB p65、pIκBα水平均显著增加/升高(P<0.05),胃液p H显著降低(P<0.01);胃组织黏膜充血红肿、黏膜上皮细胞缺损明显、腺体结构破坏、细胞结构不完整。与模型组比较,阳性对照组和良姜胃疡胶囊中、高剂量组大鼠胃液量、胃蛋白酶活力、胃溃疡面积和TNF-α、IL-6水平均显著减少/降低(P<0.05或P<0.01),胃液p H显著升高(P<0.05);胃组织黏膜正常、腺体破坏减轻、细胞结构基本完整;良姜胃疡胶囊高剂量组大鼠胃组织中p-NF-κB p65、p-IκBα水平显著降低(P<0.05)。结论:良姜胃疡胶囊可通过升高胃液pH,抑制胃蛋白活力,减少炎症因子TNF-α、IL-6的释放,抑制NF-κB通路相关蛋白表达,从而发挥其对胃溃疡的预防作用。     

仁和正胃胶囊对胃液分泌功能影响的实验研究

目的研究正胃胶囊对胃液分泌的影响。方法制备正常大鼠胃液分泌及组胺刺激大鼠胃液分泌2个模型,正胃胶囊与对照组中药制剂(胃康灵胶囊、胃泰颗粒)、西药制剂(维U颠茄铝胶囊、铝碳酸镁片)比较,测定正胃胶囊的制酸止痛作用。结果正胃胶囊能显著抑制胃蛋白酶活力,对胃液的pH值有明显升高作用;对组胺刺激的胃液分泌量增加有明显的抑制作用;对正常大鼠胃液分泌量仅有轻度抑制作用。结论正胃胶囊在抑制胃蛋白酶活性、降低胃液pH值、抑制胃液过量分泌等有明显的临床应用优势。     

珍珠胃安丸药效学研究

目的:通过药效学试验,确证珍珠胃安丸对胃、十二指肠溃疡的治疗作用,为临床用药提供理论依据.方法:采用急性胃渍疡实验模型-大鼠水浸应激性胃渍疡模型,慢性胃渍疡实验模型-大鼠乙酸烧灼型胃溃疡,药物诱发胃溃疡实验模型-大鼠利血平性胃溃疡模型等3种类型胃渍疡模型,观察珍珠胃安丸对消化性溃疡的影响.采用胃酸滴定法和AnsonMirshy改良法观察珍珠胃安丸对大鼠胃液总量、总酸度和胃蛋白酶活性的影响.采用醋酸诱导小鼠扭体反应实验和二甲苯引至小鼠耳廓肿胀实验观察珍珠胃安丸对小鼠疼痛和炎症的影响.结果:珍珠胃安丸可明显降低三种胃溃疡的溃疡指数,对3种胃溃疡模型有良好的保护作用,其作用强于西咪替丁;可显著减少胃液分泌,降低总酸度,对胃蛋白酶有明显的抑制作用,其降低总酸度作用不如西咪替丁,但抑制胃蛋白酶活性作用强于西咪替丁;可明显降低小鼠扭体次数,提高抑制率和药物镇痛百分率,同时明显减轻小鼠耳廓肿胀.结论:珍珠胃安丸对溃疡具有良好的保护作用,可用于胃、十二指肠溃疡治疗.珍珠胃安丸对三种类型胃溃疡模型的保护作用及抑制胃蛋白酶活性作用强于西咪替丁.     

右旋雷贝拉唑钠对大鼠反流性食管炎模型的作用研究

目的考察右旋雷贝拉唑钠对大鼠反流性食管炎的改善作用。方法采用幽门结扎致大鼠单纯反流性食管炎模型为实验对象,以食管炎指数和抑制率、胃酸总分泌量、p H值及胃酸分泌抑制率、胃液胃蛋白酶活力等为指标,全面考察右旋雷贝拉唑钠对大鼠反流性食管炎的改善作用。结果右旋雷贝拉唑钠(4、2、1 mg·kg-1,iv),能明显降低反流性食管炎模型大鼠食管炎指数,增加胃液p H,减少胃酸总分泌量和降低胃蛋白酶活性。结论右旋雷贝拉唑钠对反流性食管炎模型大鼠有明显的改善作用。     

越鞠丸对大鼠胃酸胃蛋白酶的影响

目的:观察越鞠丸对大鼠胃酸、胃蛋白酶的影响。方法:将SD大鼠50只随机分为正常组、空白对照组、越鞠丸低剂量组、中等剂量组和高剂量组,每组10只。末次灌胃后收集胃液,测定各组大鼠胃液胃酸、胃蛋白酶浓度和胃蛋白酶活力的变化。结果:各实验组胃酸、胃蛋白酶浓度和胃蛋白酶活力均较正常组增加(P0.05),同时胃蛋白酶浓度和胃蛋白酶活力在低剂量组和高剂量组之间比较有显著差异(P0.05)。结论:越鞠丸通过提高胃液酸度、胃蛋白酶浓度及胃蛋白酶活力发挥行气解郁的生理功效,并且与高剂量相比,低剂量使用效力相当。     

小儿增食灵合剂对小儿厌食症动物模型胃蛋白酶活性和胃酸分泌量的影响

目的：研究小儿增食灵合剂对实验性幼龄大鼠消化功能的影响。方法：采用病因模拟法建立小儿厌食症动物模型，测定模型动物胃蛋白酶的活性及胃酸含量。结果：小儿增食灵合剂可使胃游离酸和胃总酸分泌量增加，能提高大鼠胃蛋白酶活力，与空白对照组和模型对照组比较，均有统计学意义（P〈0．05或P〈0．01）。结论：小儿增食灵合剂治疗小儿厌食症的作用机制可能与其有效地增加胃游离酸及总酸度、提高胃蛋白酶的活性，从而达到促进消化的作用有关。     

Establishing objective detection limits for the pepsin digestion assay used in the assessment of genetically modified foods

Rationale: Guidelines for assessing the potential allergenicity of genetically modified (GM) organisms recommend testing the digestibility of the introduced protein by pepsin. Previous studies detailed the digestion procedure but have not described a simple objective measurement of the extent of digestion nor evaluated the impact of variation in pepsin activity.     

柴胡皂苷治疗胃溃疡作用的研究

目的研究柴胡皂苷对胃溃疡的作用。方法采用应激性大鼠胃溃疡模型,冰醋酸致大鼠胃溃疡模型,幽门结扎大鼠胃溃疡模型为实验对象,以其溃疡指数、溃疡面积、胃液分泌量为指标,评价柴胡皂苷对胃溃疡的作用。结果柴胡皂苷(50、100、200mg.kg-1,i.g)能明显降低胃溃疡模型大鼠胃粘膜的溃疡指数,缩小溃疡面积,抑制胃酸分泌,增加胃液pH,减少胃液分泌和降低胃蛋白酶活性。结论柴胡皂苷对胃溃疡模型大鼠有明显的改善作用。     

Effect of an inhibitor of pepsin proteolytic activity in the Exalto-Mann-Williamson ulcer.

The role of pepsin proteolytic activity in the Exalto-Mann-Williamson ulcer has previously not been established. Our studies show that a potent inhibitor of pepsin activity, when administered orally to E-M-W dogs, reduced both the incidence and severity of jejunal ulceration. These results indicate that pepsin may play a major role in the development of ulceration in this model.     

Osmotic stimulation of pepsin secretion in the rat

Summary The effect of the osmolarity of intragastric instillates on pepsin secretion was studied in rats anaesthetised with urethane. Irrigation of the stomach with solutions of sucrose and NaCl, resp. caused a concentration-dependent increase in pepsin output. A stimulation was observed already by hypotonic solutions and the maximal effect was obtained by 300 m-osmole/l of sucrose and by 600 m-osmole/l of NaCl (13-and 10-fold stimulation resp.). A similar time course in the increase of pepsin output was produced by hyperosmotic solutions (600 m-osmole/l) of sucrose, urea, NaCl and choline chloride. Pepsin output was stimulated maximally within 30 min and decreased thereafter, but remained at about 4–6-fold higher levels than during the previous irrigation with distilled water. Replacement of hyperosmotic instillates by distilled water reduced pepsin secretion to the inital level. Hypertonic ethanol (600 m-osmole/l) increased pepsin output only slightly. Vagotomy, pretreatment with atropine (1 mg/kg i.v.) or cimetidine (5 mg/kg i.v.), local anaesthesia of the gastric mucosa with 4% lidocaine or intravenous infusion of PGE₂ (2 g/kg x min) did not antagonise the stimulation of pepsin output induced by hyperosmotic NaCl (600 m-osmole/l). The results indicate that the increase of the osmolarity of intragastric instillates stimulates pepsin secretion in the rat without involvement of neural (vagal or local cholinergic reflexes) or hormonal mechanisms (release of gastrin) which are known to stimulate gastric secretion in the gastric phase.     

Pharmacokinetic and pharmacodynamic studies in man simulating acute and chronic treatment with oral pirenzepine

Summary Nine healthy, male subjects received controlled-rate i.v. infusions of a new formulation of pirenzepine to produce constant plasma levels of 40 ng/ml and 105 ng/ml. They also received stepped infusions resulting in plasma levels of 20, 40, 80 and 40 ng/ml for defined periods.Peptone-stimulated gastric acid and volume secretion and near point vision decreased dose dependently, whereas gastric acidity was unchanged. There was a significant correlation between inhibition of gastric acid secretion and the pirenzepine concentration in plasma and in gastric juice. During the stepped i.v. infusion, changes in near point vision were closely related to the plasma drug concentration. Antimuscarinic side-effects occurred more frequently when the plasma drug level was high.Overall, there was a close relationship between the plasma concentrations and the effects and side-effects of pirenzepine. Its gastric inhibitory action was characterized only by a reduction in gastric volume secretion. Increasing plasma concentrations during the first days of treatment may be essential for its efficacy as an antiulcer drug.     

BIavailability of metronidazole from sugar-coated tablets in humans. I. Effect of gastric acidity and correlation with in vitro dissolution rate

The bioavailability of five commercial sugar-coated metronidazole tablets was studied. The dissolution rates of the five test tablets were determined by rotating flask, oscillating basket, rotating basket and paddle methods at pH values of 1.2, 3, 4, 5, 6 and 7.2. Though metronidazole dissolves easily in water, with a solubility of 11.6 mg/ml at a pH of 7, some sugar-coated tablets showed very slow dissolution at a pH of 5 or 7.2, in spite of very rapid dissolution at a pH of 1.2. This may be due to the pH-dependent dissolution of their water-proof coatings. The bioavailability of metronidazole from three tablets showing extremely slow dissolution at pH 5 or 7.2 varied significantly between human subjects having high and low gastric acidity. However, correlation between bioavailability and dissolution rate were shown to be poor.     

Enzymatic activity in the presence of surfactants commonly used in dissolution media,Part 1: Pepsin

The United States Pharmacopeia (USP) General Chapters Dissolution 〈711〉 and Disintegration and Dissolution of Dietary Supplements 〈2040〉 allows the use of enzymes in dissolution media when gelatin capsules do not conform to dissolution specifications due to cross linking. Possible interactions between enzymes and surfactants when used together in dissolution media could result in loss of the enzymatic activity. Pepsin is an enzyme commonly used in dissolution media, and in this work, the activity of pepsin was determined in the presence of different surfactants as usually found in case of dissolution tests of certain gelatin capsule formulations.Pepsin enzymatic activity was determined according to the Ninth Edition of the Food Chemicals Codex (FCC) 9 method, in dissolution conditions: simulated gastric fluid, 37 °C and 50 rpm. Sodium dodecyl sulfate (SDS), cetyltrimethyl ammonium bromide (CTAB), polysorbate 80 (Tween 80) and octoxynol 9 (Triton X100) in concentrations above and below their critical micellar concentrations were selected. Results showed a significant reduction in the activity of pepsin at all the concentrations of SDS assayed. On the contrary, CTAB, Tween 80, and Triton X100 did not alter the enzymatic activity at of pepsin any of the concentration assayed.This data demonstrates a rational selection of the surfactant to be used when pepsin is required in dissolution test.     

儿康宁配合胃蛋白酶治疗小儿厌食症疗效观察

目的:探讨儿康宁配合胃蛋白酶颗粒剂治疗小儿厌食症的临床疗效。方法:将124例小儿厌食症随机分为两组:治疗组64例,儿康宁5~10ml,Tid,胃蛋白酶颗粒 6g,Bid~Tid。对照组 60例,乳酸菌素片0.4~1.2g,Tid。疗程均为 4周。结果:治疗组食欲改善时间和总有效率均明显优于对照组(P＜0.01)。结论:儿康宁配合胃蛋白酶颗粒是治疗小儿厌食症较为有效的药物。     

Studies on the Preparation Properties and Drug Loading of theStarch Nanoparticles

On the basis of studies of starch microspheres, we carried out the research program of starch nanoparticles(SNP)which included preparation, physical and chemical properties and drug loading. The SNP was prepared using reversedphase-microemulsion polymerization method, with soluble starch as raw material. The particle size, quantity ofphosphorous, degradability, scanning electron microgragh, IR spectra and stability of SNP were investigated. Thepharmacodynamics and concentration-time curve of insulin starch nanoparticles were determined.     

神曲胃痛片抗实验性胃溃疡作用的实验研究

目的:探讨神曲胃痛片抗实验性胃溃疡的影响.方法:采用小鼠应激性胃溃疡、小鼠烧灼性胃溃疡、大鼠幽门结扎性胃溃疡和大鼠利血平性胃溃疡的模型,观察神曲胃痛片对溃疡的影响,同时在幽门结扎性胃溃疡模型中观察其对胃液量、胃蛋白酶活性、胃液游离酸酸度的影响.结果:神曲胃痛片可明显抑制应激性、幽门结扎性和利血平性胃溃疡的形成,且可促进烧灼性胃溃疡的愈合,对胃酸酸度和胃蛋白酶活性有明显的抑制作用.结论:神曲胃痛片具有明显的抗实验性胃溃疡作用.