健脾扶运汤的“健脾”作用研究

本研究表明，健脾扶运汤对家兔离体肠管运动有双向调节作用，当肠管强直性收缩时有解痉作用，当肠管活动处于抑制状态时则有兴奋作用。对小鼠小肠推进运动有促进作用。对脾虚模型小鼠明显改善症状和增加体重。因此，调节胃肠运动功能可能是健脾扶运汤“健脾”作用的主要机理。     

健脾敛疡胶囊止泻作用的实验研究

目的:探讨健脾敛疡胶囊对实验性脾虚泄泻小鼠的止泻作用。方法:采用100%大黄水煎液复制小鼠脾虚泄泻模型,治疗组用不同剂量健脾敛疡胶囊,对照组中药用参苓白术散、西药用易蒙停,通过观察湿粪数及小肠炭末推进率,分析健脾敛疡胶囊对脾虚泄泻小鼠胃肠运动的影响。结果:健脾敛疡胶囊可使模型小鼠炭末在肠管的推进率降低,且大剂量组湿粪数明显减少。结论:小鼠湿粪数试验结果表明健脾敛疡胶囊大剂量作用与易蒙停接近,但不及参苓白术散。小肠炭末推进率试验表明大剂量健脾敛疡胶囊作用与参苓白术散及易蒙停接近。     

健脾止泻颗粒对脾虚泄泻小鼠微生态及小肠和胸腺超微结构影响的实验研究

目的：探讨健脾止泻颗粒对脾虚泄泻小鼠微生态及对小肠和胸腺超微结构的作用。方法：用100％大黄水浸液复制小鼠脾虚泄泻模型，观察健脾止泻颗粒对小鼠微生态的影响，通过电镜观察对受损小肠黏膜和胸腺的修复作用。结果：健脾止泻颗粒对实验性脾虚泄泻小鼠的肠道菌群有调节作用，能使受损的小肠上皮细胞微绒毛结构明显改善，促进小鼠胸腺线粒体等细胞器的复制。结论：健脾止泻颗粒可通过调节肠道微生态平衡，改善小肠吸收细胞微绒毛的结构和促进线粒体的复制而发挥治疗作用。     

逍遥散健脾补虚药理作用研究

目的:研究逍遥散健脾补虚的药理作用。方法:实验分为6组,即正常对照、模型、肝复乐(0.1g.kg-1)和逍遥散高、中、低剂量(30.4、15.2、7.6g.kg-1)组。小鼠通过iv利血平注射液复制脾虚消瘦、倦怠乏力的模型[1]。测定小鼠的体重和自主活动次数以及游泳时间长短。结果:与正常对照组比较,模型组小鼠体重减少,自主活动次数和游泳时间显著减少。与模型组比较,逍遥散各剂量组小鼠体重增加,自主活动次数显著增加,游泳时间显著延长。结论:逍遥散对脾虚引起的消瘦、倦怠乏力有补益作用。     

健脾升白合剂升高白细胞作用研究

目的:观察健脾升白合剂对化疗引起的白细胞减少症的预防和治疗作用.方法:以环磷酰胺腹腔注射造成小鼠白细胞减少症模型,用健脾升白合荆进行治疗,对模型小鼠外周血象和骨髓造血功能进行检测.结果:健脾升白合剂可明显对抗模型小鼠的白细胞减少.结论:健脾升白合剂可保护小鼠外周血中白细胞免受环磷酰胺的伤害.同时对白细胞的提高有一定的促进作用.     

干姜醇提取物对肠道平滑肌运动的影响

目的 研究干姜醇提取物(EDGE)对肠道平滑肌运动的影响及其作用机制. 方法 通过小鼠小肠墨汁推进实验观察EDGE对正常、亢进及抑制状态下肠道运动的影响, 并采用兔体外肠管实验从胆碱能通路初步探讨其作用机制. 结果EDGE能显著促进正常和抑制状态的小鼠小肠运动,对亢进状态的小鼠小肠运动却有明显抑制作用. EDGE能显著促进正常体外肠管收缩,对阿托品预孵育的体外肠管也有明显促进收缩作用,对乙酰胆碱(Ach)引起的肠管收缩反应却有拮抗作用,并存在量效关系. EDGE(1 mg•mL^-1)使无钙离子蒂罗德液中Ach收缩肠管作用明显减弱,但不影响氯化钙引起的肠管收缩. 结论 EDGE对肠道平滑肌运动有双向调节作用,这种作用与胆碱能受体有关.     

益气健脾汤治疗脾虚泄泻

目的观察益气健脾汤治疗脾虚泄泻的疗效。方法60例患者随机分为2组,A组(n=30)为治疗组,给予益气健脾汤口服。B组(n=30)为对照组,给予人参健脾丸口服。结果A组总有效率为90%,B组总有效率为60%,经X2检验,两组总有效率有显著差异(P<0.05)。结论益气健脾汤治疗脾虚泄泻疗效较好。     

山药苡仁健脾粉及其拆方的药理作用研究

目的:研究山药苡仁健脾粉及其拆方的药理作用。方法:通过环磷酰胺抑制免疫和碳廓清实验,观察山药苡仁健脾粉及其拆方对小鼠免疫调节功能的影响;采用小肠推进实验评价山药苡仁健脾粉及其拆方对肠蠕动的影响;采用转棒实验观察山药苡仁健脾粉及其拆方的抗疲劳功能;采用四氧嘧啶复制高血糖模型,观察山药苡仁健脾粉及其拆方对模型小鼠高血糖的影响。结果:山药粉、薏苡仁粉与山药苡仁健脾粉均能有效提高小鼠的免疫力,增加碳廓清率,对抗环磷酰胺所致的白细胞数量的减少,均有明显的抗疲劳作用;山药粉和山药苡仁健脾粉能促进小肠蠕动和有明显的降血糖作用,而薏苡仁粉作用不显著。结论:山药苡仁健脾粉具有促进肠蠕动、免疫调节、抗疲劳和降糖等保健功能,具有进一步开发的价值。     

脾虚泄泻患者健脾益肾汤临床治疗研究

脾虚泄泻患者健脾益肾汤临床治疗研究福建医学院附属协和医院林谷珍，王小众，王平，杨发端，林峻，陈红绉，林其信，金斌福建省中医药研究院林求诚，叶盈，方素钦本文采用健脾益肾汤，对７６例脾虚泄泻患者进行临床治疗，并观察治疗前后患者临床免疫功能改变及肠粘膜嗜银...     

肝舒胶囊对实验性脾虚及胃肠功能的影响

为了进一步探讨肝舒胶囊防治肝炎的机理，进行了肝舒胶囊对利血平致小鼠脾虚、小鼠胃排空、甲基硫酸新斯的明致小鼠小肠运动亢进和大鼠胃蛋白酶活性的影响试验，结果表明其对实验性脾虚及肠胃功能有明显的改善作用。     

Absorption of a novel prodrug of L-dopa, L-3-(3-hydroxy-4-pivaloyloxyphenyl)alanine (NB-355). In vitro and in situ studies

Absorption mechanism and absorption site of a prodrug of L-DOPA, L-3-(3-hydroxy-4-pivaloyloxyphenyl)alanine (NB-355, 1) was investigated using rats. Prodrug 1 (0.5 mM) was taken up by intestinal tissue segments time-dependently in vitro at pH 6.0. However, the rate of uptake was less than that of L-dopa. Inhibitors of the amino acid active transport system (L-Phe, dinitrophenol, ouabain) had no effect on the uptake of prodrug 1. In the intestinal tissue segments, prodrug 1 was extensively hydrolyzed by diisopropylfluorophosphate-sensitive esterase(s). To characterize the absorption site, gastrointestinal tracts were ligated to make acute loops in situ and prodrug 1 or L-dopa was injected into the loops. L-dopa disappeared rapidly from the lumen of the jejunum. In contrast, prodrug 1 disappeared rapidly from the ileum rather than the duodenum or jejunum. From these results, it was suggested that prodrug 1 was slowly absorbed primarily from the lower small intestine.     

Inhibitory effect of JTP-59557, a new triazole derivative, on intestinal phosphate transport in vitro and in vivo

JTP-59557 [(-)-4-(2-tert-Butyl-4,5-dichlorophenyl)-5-(5-trifluoromethylpyridin-2-ylsulfanyl)-4H-[1,2,4]triazol-3-ol] showed an inhibitory effect on Na(+)-dependent inorganic phosphate (Pi) transport in intestinal brush border membrane vesicles with an IC(50) value of 0.40 microM in rabbit and with an IC(50) of 0.19 microM in rat, without affecting Na(+)-independent Pi and Na(+)-dependent d-glucose transport activities. In Chinese hamster ovary (CHO) cells expressing human type IIb Na/Pi cotransporter (type IIb), JTP-59557 decreased human type IIb-mediated Pi uptake with an IC(50) of 0.12 microM. In rabbit intestinal brush border membrane vesicles, JTP-59557 behaved as a noncompetitive inhibitor with respect to Pi. In an in vivo study, single administration of JTP-59557 significantly decreased the intestinal Pi absorption rate, when either Pi solution or laboratory chow was given to rats. In this report, we show that JTP-59557 is a potent, selective, stereospecific, noncompetitive inhibitor of intestinal Na/Pi cotransporters including type IIb, and it may represent a new class of intestinal Pi absorption inhibitor.     

阿昔洛韦在大鼠胃肠道吸收的研究

目的：了解阿昔洛韦在大鼠胃肠道的吸收情况。方法：采用大鼠在体灌流技术，对阿昔洛韦在大鼠胃部及不同肠段的吸收进行了研究。结果：3h后胃中吸收平均值为9．46％，在小肠上部、中部、下部和结肠段的吸收百分率分别为20．22％，15．70％，9．15％和4．59％。结论：阿昔洛韦主要在胃肠道上部吸收，但吸收亦较差。     

Lectin-mediated mucosal delivery of drugs and microparticles

Absorption of drugs and vaccines at mucosal surfaces may be enhanced by conjugation to appropriate bioadhesins which bind to mucosal epithelia. Bioadhesins might also permit cell- and site-selective targeting. One approach is to exploit surface carbohydrates on mucosal epithelial cells for lectin-mediated delivery. We review work supporting the use of lectins as mucosal bioadhesins in the gastrointestinal and respiratory tracts, the oral cavity and the eye. The gastrointestinal tract is particularly favoured for mucosal delivery. Many studies have demonstrated that the antigen sampling intestinal M cells offer a portal for absorption of colloidal delivery vehicles. Evidence is presented that M cell targeting may be achieved using M cell-specific lectins, microbial adhesins or immunoglobulins. While many hurdles must be overcome before mucosal bioadhesins can guarantee consistent, safe, effective mucosal delivery, this is an exciting area of research that has important implications for future drug and vaccine formulation.     

藿香正气滴丸对正常及乙酰胆碱刺激下动物胃肠道功能的影响

目的:观察藿香正气滴丸对正常及乙酰胆碱刺激下动物胃肠功能的影响。方法:观察藿香正气滴丸对正常小鼠胃排空和肠推进运动、乙酰胆碱所致大鼠离体胃底条平滑肌收缩、家兔离体肠平滑肌收缩作用以及家兔在体肠平滑肌收缩作用的影响。结果:藿香正气滴丸对正常状态胃肠运动无明显影响;可不同程度抑制乙酰胆碱引起的家兔在体回肠平滑肌收缩幅度以及乙酰胆碱所致大鼠离体胃底平滑肌以及家兔离体十二指肠平滑肌的收缩。结论:藿香正气滴丸对不同状态的胃肠道具有不同影响,对过度兴奋的胃肠道平滑肌收缩具有抑制作用,而对正常状态的胃肠道无明显影响。     

Gastrointestinal absorption of nitrofurantoin: evaluation of a newly developed method for determination of the gastrointestinal transit time in dogs]

The relationship between the oral absorption and gastrointestinal transit time of nitrofurantoin was investigated in dogs by the double-marker method using acetaminophen and salicylazosulfapyridine as markers. The extent of bioavailability of nitrofurantoin gave correlations with both gastric emptying time and small intestinal transit time. The results indicate that the slower the passage from the stomach into the small intestine and/or the longer the residence time in the small intestine, the oral absorption efficiency of nitrofurantoin increases. These observations were consistent with the reported findings from in situ absorption study in rats and intestinal intubation study in humans, respectively. Moreover, it was clarified that small intestinal transit time is the most important determinant of absorption of nitrofurantoin, since the good correlation was observed between the small intestinal transit time and the extent of bioavailability. The double-marker method appears consequently to be useful tool for the determination of the gastrointestinal transit time in dogs.     

基于案例的药物相互作用住吸收环节的影响（一）

目的：了解药物在吸收阶段发生的相互作用的机制。方法：通过文献检索和案例分析，对吸收阶段药物相互作用对药物疗效的影响进行探讨。结果：4例患者使用的药物因在吸收阶段发生的相互作用．一种药物可增加或减少另一种药物的吸收，致使后一种药物血药浓度增高或降低，影响治疗效果。结论：两种药物在吸收阶段可因改变肠道菌群．胃肠动力及络合作用等机制而影响药物的吸收。     

The effect of dinoprost on transport of water and imipramine through rat small intestinal membranes.

The relation between transmucosal fluid movement and its effect on absorption and exsorption of imipramine was studied with the in-situ single-pass perfusion technique in rats. Dinoprost (prostaglandin F2 alpha, PGF2 alpha) caused a dose-related inhibition of both absorption and secretion of water across the intestinal membrane. When PGF2 alpha was infused at a rate of 5 mumols kg-1 h-1, the absorption rate of water decreased from 51.7 to 21.5 mL h-1 and the secretion rate decreased from 48.9 to 26.8 mL h-1. Net water flux changed from net water absorption (0.9 mL h-1) to net water secretion (5.33 mL h-1) by infusion of PGF2 alpha. However, absorption and exsorption of imipramine were little affected by infusion of PGF2 alpha. The absorption rates of imipramine were 3.03 and 2.36 mg h-1 in the absence and presence of PGF2 alpha, respectively. Furthermore, the average amounts of imipramine exsorbed into the intestinal lumen in 2 h were 7.82 and 8.10% in the absence and presence of PGF2 alpha, respectively. Infusion of PGF2 alpha also enhanced motility of the small intestine compared with the control. From these results, it appears that PGF2 alpha has no effect on the absorption and exsorption of imipramine across the intestinal membrane although it is reasonable to use PGF2 alpha in the case of patients with overdoses of drugs which decrease gastrointestinal motility.     

Effects of three proteins on absorption of cadmium in rats

The effects of 3 proteins on the gastrointestinal absorption of cadmium were studied. Glycinin and ovalbumin significantly decreased cadmium in liver and the total cadmium in the tissues of rats following a single oral administration of cadmium. In addition, in rats fed continuously with the experimental diets containing cadmium together with proteins, glycinin and ovalbumin significantly decreased the contents of cadmium in the tissues. These results show that the proteins depressed the gastrointestinal absorption of cadmium. Moreover, the effects of cadmium on various digestive enzymes for proteins and the pepsin or pepsin-pancreatin digestion of the proteins were examined. As a result it is likely that the inhibitory effect of cadmium on the intestinal digestion of these proteins is one of the causes of the inhibitory effects of the proteins on the intestinal absorption of cadmium in rats. The undigested oligopeptides may decrease the amount of free cadmium available to be absorbed from the intestine by binding cadmium itself, resulting in decreased intestinal absorption of cadmium.     

Baicalin, the predominant flavone glucuronide of scutellariae radix, is absorbed from the rat gastrointestinal tract as the aglycone and restored to its original form

When baicalin was orally administered to conventional rats, it was detected in their plasma for 24 h after administration, but baicalein, the aglycone of baicalin, was not detected. However, when baicalin was given to germ-free rats, only a small amount of baicalin was detected in their plasma within 2 h after the administration, its AUC0-lim (the area under the concentration-time curve from 0 to last determination time) being 12.0% of that in conventional rats. Subsequently, a considerable amount (55.1 +/- 6.2%) of baicalin was recovered from the gastrointestinal tract even 4 h after administration. When baicalein was orally administered to conventional rats, however, baicalin appeared rapidly in their plasma at an AUC0-lim value similar to that obtained after oral administration of baicalin, despite the absence of baicalein in plasma. When intestinal absorption was evaluated by the rat jejunal loop method, baicalein was absorbed readily, but only traces of baicalin were absorbed. Moreover, in conventional rats a small amount (13.4 +/- 3.1%) of baicalin and an appreciable amount (21.9 +/- 3.4%) of baicalein were recovered from the gastrointestinal tract even 4 h after oral administration of baicalin, but only a small amount (3.93 +/- 1.43%) of baicalein was detected in the intestinal tract 1 h after administration of baicalein. Baicalin was transformed to baicalein readily by the rat gastric and caecal contents. When baicalin was administered orally to conventional rats, an appreciable amount of baicalein was recovered in their gastrointestinal tracts. Moreover, baicalein was efficiently conjugated to baicalin in rat intestinal and hepatic microsomes. These results indicate that baicalin itself is poorly absorbed from the rat gut, but is hydrolysed to baicalein by intestinal bacteria and then restored to its original form from the absorbed baicalein in the body.