Protective Effects of Norursodeoxycholic Acid Versus Ursodeoxycholic Acid on Thioacetamide-induced Rat Liver Fibrosis.

Background/objectives: Effects of norursodeoxycholic acid (norUDCA) and ursodeoxycholic acid (UDCA) on liver fibrosis progression and liver fibrosis reversal in thioacetamide (TAA)-treated rats were studied.

Methods: Advanced liver fibrosis was induced by TAA treatment (200 mg/kg, i.p.

Ursodeoxycholic acid dose-dependently improves liver injury in rats fed a methionine- and choline-deficient diet.

Aim:   The data on the beneficial effect of ursodeoxycholic acid (UDCA) in non-alcoholic steatohepatitis (NASH) are controversial. The difference of opinion is connected with UDCA dosage to be used. Therefore, we evaluated the dose-dependent efficacy of UDCA in experimental NASH.

Ursodeoxycholic acid treatment in preterm infants: a pilot study for the prevention of cholestasis associated with total parenteral nutrition.

In a prospective, double-blind, placebo-controlled trial, the efficacy and safety of ursodeoxycholic acid (UDCA) was evaluated in preterm infants, in terms of its potential impact on fat absorption, advancement of enteral feeding, development of cholestasis, growth, nutritional status, and metabolic status. Although fecal fat excretion slightly decreased and achievement of full enteral feeding was earlier in the UDCA group, these differences were not significant. Interestingly, whereas serum gamma-glutamyl transferase activity increased during the parenteral nutrition period in the placebo group, we observed a constant and significant decrease in the UDCA group.

Predictors of premature delivery in patients with intrahepatic cholestasis of pregnancy.

Aim: To evaluate the predictive value of clinical symptoms and biochemical parameters for prematurity in intrahepatic cholestasis of pregnancy (ICP).

Methods: Sixty symptomatic patients with ICP were included in this retrospective analysis. Preterm delivery was defined as delivery before 37 wk gestation.

Ursodeoxycholic acid differentially affects three types of sphingomyelinase in human colon cancer Caco 2 cells.

We investigated the effects of UDCA on sphingomyelinase (SMase) in Caco 2 cells cultured in monolayer and polarized conditions. Alkaline SMase activity was high in polarized cells whereas, acid and neutral SMase activities were high in monolayer cells. In polarized cells, UDCA increased alkaline SMase expression and caspase 3 activity but had no effect on acid and neutral SMases.

Bioequivalence of a new liquid formulation of ursodeoxycholic acid (Ursofalk suspension) and Ursofalk capsules measured by plasma pharmacokinetics and biliary enrichment.

Background: Ursodeoxycholic acid is an approved therapy for hepatobiliary disorders but in infants and children compliance is compromised because it is formulated exclusively as capsules, or tablets.

Aim: To determine the pharmacokinetics and bioequivalence of a new liquid formulation of ursodeoxycholic acid (Ursofalk suspension) with a standard capsule (Ursofalk) in a randomized, unblinded, crossover designed study of 24 healthy adults.

Methods: Equivalence was based on single bolus oral plasma pharmacokinetics and biliary ursodeoxycholic acid enrichments after repeat doses.

Evaluation of oral budesonide in the treatment of active distal ulcerative colitis.

Budesonide, a topical corticosteroid, has proven useful for the management of Crohn's disease. Its efficacy is similar to prednisone but it has fewer side effects. A new pH-modified release capsule (Budenofalk) is probably efficacious in distal ulcerative colitis.

Ursodeoxycholic acid does not affect ethinylestradiol bioavailability in women taking oral contraceptives.

Objective: Contraception is recommended for female patients during ursodeoxycholic acid (UDCA) treatment for the potential teratogenic effect of this bile acid, and the aim of our study was to determine whether this treatment affects the bioavailability of ethinylestradiol (EE2).

Methods: In this double-blind, randomised study, we measured EE2 pharmacokinetics in eight healthy volunteers randomly allocated to receive oral contraceptive (30 microg EE2 and 75 microg gestodene) plus either UDCA (8-10 mg/kg per day) or placebo for 21 days during the first of three consecutive menstrual cycles. After a washout period during the second cycle, the subjects received the alternative treatment during the third menstrual cycle.

The protective effect of ursodeoxycholic acid in alloxan-induced diabetes.

The purpose of this work was to study the effect of ursodeoxycholic acid (UDCA) on the morphological and functional alterations in pancreatic islet beta-cells in rats with diabetes induced by alloxan (150 mg kg(-1), i.p.).

Ursodeoxycholic acid complexation with 2-hydroxypropyl-beta-cyclodextrin increases ursodeoxycholic acid biliary excretion after single oral administration in rats.

Complexation of ursodeoxycholic acid (UDCA) with 2-hydroxypropyl-beta-cyclodextrin (HPbetaCD) improves the water solubility and the dissolution rate of UDCA and may therefore increase its bioavailability. We compared the amount and the rate of biliary excretion of UDCA and biliary lipid secretion after a single oral administration of UDCA in 3 different pharmaceutical formulations [UDCA-HPbetaCD ('urso-beta-cyclodextrin'), UDCA suspension and UDCA capsule] at 3 different dosages each, in 11 groups (2 control groups) of bile fistula rats. UDCA excretion increased with an increase in dose, biliary UDCA recovery and peak secretion were significantly higher after administration of UDCA-HPbetaCD than after UDCA in suspension or capsule.

Ursodeoxycholic acid increases the activities of alkaline sphingomyelinase and caspase-3 in the rat colon.

Background: Ursodeoxycholic acid (UDCA) has been found to inhibit the development of colon carcinoma induced by chemical carcinogens with unidentified mechanisms. Sphingomyelin metabolism has emerged as a novel signal transduction pathway closely related to cell proliferation and apoptosis. We recently found that alkaline sphingomyelinase (SMase) activity was decreased in human colon cancer.

Effects of ursodeoxycholate and other bile salts on levels of rat intestinal alkaline sphingomyelinase: a potential implication in tumorigenesis.

Previous studies showed that bile salts had a promoting effect on colon cancer development and this effect was inhibited by ursodeoxycholate (UDC). We recently found that both human colorectal adenomas and carcinomas were associated with a specific decrease in alkaline sphingomyelinase activity. In this work, we compared the effects of ursodeoxycholate and other bile salts on the levels of rat intestinal alkaline sphingomyelinase both in the intestinal loops and after oral administration.

ATPase and cytochrome oxidase activities at the polar organelle in swarm cells of Sphaerotilus natans: an ultrastructural study.

The polar organelle of bacteria presumably is part of the flagellar apparatus. In order to characterize this structure, cytochemical studies on Sphaerotilus natans have been performed. Marked ATPase activity is associated with the inner boundary layer and central layer of this organelle.

[The percutaneous action of a heparin-allantoin-dexpanthenol combination in a specific ointment base. Thrombolytic action on the rabbit ear].

Experimentally induced thrombi of ear veins in albino rabbits have been treated locally with heparin-containing ointments in presence or absence of allantoin and dexpanthenol, the heparin concentration varying. While the ointments, containing heparin only, induce no or only minor thrombolytic activity, the combination ointments Hepathrombin Adenylchemie containing heparin, allantoin and dexpanthenol show significant thrombolytic activity. This effect is dependent upon the heparin concentration, yet, heparin doses above 50 000 IU per 100 g of ointment do not enhance the thrombolysis furthermore.

[The percutaneous effect of a heparin-allantoin-dexpanthenol combination in a specific ointment base. Anti-allergic, anti-inflammatory effect in the PCA test in the rat].

Local application of a heparin-allantoin-dexpanthenol (Hepathrombin-Adenylchemie) ointment to rats 15 min prior to induction of a passive cutaneous anaphylaxis (PCA) reaction inhibits the anaphylactic reaction as compared to the ointment base. Also, the Evans Blue content as a measure for vascular permeability and the oedema weights are reduced under the heparin containing ointment. The antiallergic/antiinflammatory effect is probably due to heparin.

[Investigations on the percutaneous activity of a combination of heparin, allantoin and dexpanthenol in a specific ointment base, Antiinflammatory effect on UV-erythema in the guinea pig].

Compared to the ointment base, the application of a heparin-allantoin-dexpanthenol combination ointment (Hepathrombin ointment) to guinea pigs immediately after as well as 30 and 120 min prior to UV-irradiation effects more rapid regression of the erythema along with a reduction in erythema formation. After a pretreatment of 30 min, the temperature of the erythematous skin is also significantly lower. At a pretreatment of 120 min, no temperature differences can be observed between the ointment groups.

[Pharmacological effect of piprozoline on the exocrine pancreas of dogs (author's transl)].

Ethyl (Z)-(3-ethyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)-acetate (piprozoline, Gö 919, Probilin) and its main metabolite Gö 3284 cause a long-acting stimulation of the ecbolic function of the exocrine pancreas in the dog after intraduodenal administration or after i.v. injection.

[Pharmacological effects of piprozoline on bile secretion in dogs (author's transl)].

Ethyl (Z)-(3-ethyl-4-oxo-5-piperidino-thiazolidin-2-ylidene)-acetate (piprozoline, Gö 919, Probilin) and its main metabolite Gö 3284 induce a strong choleretic effect in dogs after i.v. and i.

[Method for direct measurement of choleresis and secretory function of the exocrine pancreaas demonstrated by sodium dehydrocholate and secretin (author's transl)].

A method has been described that enables to check secretory processes in animals directly. This has been demonstrated in dog exocrine pancreas stimulated by secretin and on bile secretion induced by sodium dehydrocholate. The design of this method permits to run experiments on pancreas and choleresis separately as well as simultaneously.