Latest medical literature on euglucon

Our library of drug research abstracts drawn from the medical literature is updated on a regular schedule, and you can be assured that new euglucon research articles will be listed here shortly after becoming available to us.

Medical research on euglucon

A new system for the prediction of drug absorption using a pH-controlled Caco-2 model: evaluation of pH-dependent soluble drug absorption and pH-related changes in absorption.

J Pharm Sci. 2004 Jan; 93(1): 71-7
He X, Kadomura S, Takekuma Y, Sugawara M, Miyazaki K
One purpose of this study was to develop a new system for the prediction of pH-dependent soluble drug absorption that takes into account the physiological condition of the gastrointestinal tract. Another purpose was to establish several models of different gastric acidities: a normal gastric acidity model, a low gastric acidity model (a model of achlorhydria), a temporarily elevated gastric acidity model (a model of a case in which an acidic drug was coadministered to temporarily elevate gastric acidity in the case of low gastric acidity), a weak antacid model (a model of a case in which a weak antacid drug, such as an H(2) receptor antagonist, was coadministered to temporarily elevate pH up to 6), and a strong antacid model (a model of a case in which a strong antacid drug, such as magnesium hydroxide, was coadministered to temporarily elevate pH up to 8.0). These models were used to evaluate variation in pH-related absorption in humans. Dipyridamole preparation (Persantin tablets) and glibenclamide preparation (Euglucon tablets), both poorly water-soluble and pH-dependent soluble drugs, were chosen as model drugs to determine whether absorption is altered by changes in levels of gastric acid. The extent of absorption of dipyridamole was remarkably lower when gastric pH was continuously elevated to 6.0, whereas it was increased when gastric pH temporarily decreased to 1.8. The extent of absorption of glibenclamide increased dramatically when gastric pH temporarily increased to 8.0, but did not change when gastric pH temporarily increased to 6.0. These results are consistent with reported results obtained in clinical studies. The results suggest that pH-related variations in absorption in humans can be accurately predicted using our new system.

Simultaneous analyses of hypoglycemic agents and C-peptide are essential in a homicide case with the combined dosing insulin and insulin-releasing drug.

Leg Med (Tokyo). 2002 Mar; 4(1): 34-6
Uezono T, Shiono H, Shimizu K, Ogawa K, Saito O, Yoshida M, Mizukami H, Matsubara K
A 5-year-old girl was given a sulfonylurea hypoglycemic agent, 25 mg of glibenclamide (ten tablets of Euglucon) with two benzodiazepine drugs, 2 mg of estazoram and 0.75 mg of triazolam (one tablet of Eurodin and three tablets of Halcion), by her 37-year-old pharmacist father and then injected with 70 units of insulin (NovoLet 40R). She died several hours after the injection of insulin. Autopsy was carried out 12 h after the death. A glibenclamide level of 103 ng/ml was detected in the serum collected from the heart at autopsy. The serum insulin and C-peptide concentrations were 295 microU/ml and 0.5 ng/ml, respectively. The high level of insulin and the low level of C-peptide indicated that most of the serum insulin was exogenous. The determination of the serum C-peptide concentration was useful to the diagnosis of hypoglycemia caused by exogenous insulin even in the case of co-administration with an endogenous-insulin-releasing agent.

TCM treatment of diabetic hearing loss--an audiological and rheological observation.

J Tradit Chin Med. 2000 Sep; 20(3): 176-9
Li R, Wu L, Song N, Li W
35 cases (48 ears) of diabetic hearing loss were randomly assigned to 2 groups: the treatment group of 19 cases (25 ears) treated with drugs for nourishing the kidney-yin, invigorating blood circulation and removing blood stasis based on differentiation of symptoms and signs, and the control group of 16 cases (23 ears) treated with euglucon and other routine drugs. The results showed that the total effective rate for audition elevation in the treatment group was 52.0%, and that in the control group, 26.1%. In the treatment group, the rheological indexes were improved after treatment, the difference being very significant in comparison with those before treatment (P < 0.05 and P < 0.01); while in the control group, except the whole blood low shearing specific viscosity, all the other 4 indexes were not statistically significant before and after treatment (P > 0.05).

[Fatal iatrogenically-induced hyperglycemia following accidental glibenclamide ingestion]

Klin Padiatr. 1990 Mar-Apr; 202(2): 103-5
Lemke R
A 2 9/12 years old girl had swallowed 8 to 9 tablets Euglucon N. By concatenation of unfortunatable facts the infant died of hyperglycaemia. The findings from this case should contribute to differentiate also in medical textbooks therapeutic recommendations.

[Clinical study comparing the effectiveness and tolerance of 2 current and one new glibenclamide formulation]

Wien Med Wochenschr. 1989 Jun 30; 139(12): 281-4
Lingg G, Haushofer A
In a clinical study efficacy and tolerance of Neogluconin (2.5 mg) a new galenical form of glibenclamide were compared with a conventional preparation (Euglucon 5). Neogluconin showed an improved absorption and comparable blood sugar levels at a dosage reduced by 25%. 25 outpatients suffering from Type II diabetes in a well balanced metabolic state and previously under Euglucon therapy for at least one year were changed to the new product. After 2 months of Neogluconin therapy blood sugar profiles, HbA1, C-peptide and cholesterin levels were unchanged in comparison to values determined during the previous Euglucon treatment. This confirms that Neogluconin produces a comparable favorable blood glucose lowering effect despite a 25% reduction in dosage.

[Effectiveness of combined treatment with glibenclamide and insulin in secondary sulfonylurea failure. A controlled multicenter double-blind clinical trial]

Dtsch Med Wochenschr. 1988 Apr 22; 113(16): 631-6
Bachmann W, Lotz N, Mehnert H, Rosak C, Schöffling K
The effectiveness of combined insulin and glibenclamide was compared with that of insulin alone in a multicenter double-blind trial of secondary sulphonylurea failures. Protocols of 176 patients at 26 centers were available, but only 68 could ultimately be included in the analysis. Combined insulin and glibenclamide (Euglucon N) had been taken by 37 patients, combined insulin and placebo by 31. The final criterion, postprandial one-hour blood sugar level of less than or equal to 220 mg/100 ml after 24 weeks, was attained by nearly 75% of patients in both groups. Fasting blood sugar and postprandial one-hour blood sugar as well as HbA1 did not differ during the entire test period of 24 weeks. Mean daily insulin dose was 20 IU in the insulin/glibenclamide group, 35 IU in the insulin/placebo group. This increased the number of second evening insulin injections by 50% in the insulin/placebo group compared with the insulin/glibenclamide group. The frequency of mild hypoglycemia was similar in the two groups. The results indicate that combined insulin/glibenclamide, given over a period of six months to patients with secondary sulphonylurea failure, provided metabolic results as good as those with insulin alone. The required insulin dosage was thus reduced by more than a third.

[Mechanism of action of combined administration of glibenclamide and insulin in type II diabetics with secondary failure of oral treatment]

Klin Wochenschr. 1986 Oct 15; 64(20): 1021-3
Schmidt FH, Klujko J, Kühnle HF, Reiter J
In a double-blind placebo-controlled cross-over study eight type II diabetics (three men, five women), of whom six were at the point of late failure to oral treatment, were given an insulin infusion of 22 U human insulin/patient for 45 min (approximately 7 microU/kg X min); 30 min before infusion either glibenclamide (1 tablet Euglucon N) or placebo was administered. Glucose in venous blood, C-peptide, insulin, and glibenclamide concentrations in the blood plasma were simultaneously determined over a period of 210 min. The monitoring of glucose was handled using a Biostator. The insulin level reached a mean maximum of 400 to 500 microU/ml and was in a behavior of 100 microU/ml for 60 min. The areas under the concentration-time curves (AUCs) were practically identical in the two regimes. The blood glucose fell (in mean) from 260 mg/dl to 135 mg/dl and at the end of the experiment was in the range of 155 mg/dl. The glibenclamide concentrations reached maximal concentrations of 185 ng/ml 90 min after administration. The C-peptide concentrations fell in the placebo phase by more than 40%. In contrast, in the glibenclamide period there was at first a slight rise and later a slight marginal fall (initial, 2.0 ng/ml vs 1.9 ng/ml; 60 min, 1.3 ng/ml vs 1.8 ng/ml; 180 min, 1.2 ng/ml vs 1.8 ng/ml). Values after 90, 120, and 180 min were statistically different. The AUCs (0-180 min) were different (329 ng X min/ml vs 251 ng X min/ml). The inhibition of insulin secretion (measured by C-peptide) caused by exogenous insulin administration is largely abolished by glibenclamide.(ABSTRACT TRUNCATED AT 250 WORDS)

The pharmacokinetics of glibenclamide: a single dose comparison of four preparations in human volunteers.

Int J Clin Pharmacol Ther Toxicol. 1985 Dec; 23(12): 642-6
Karttunen P, Uusitupa M, Nykänen S, Robinson JD, Sipilä J
The pharmacokinetic properties of two new HB 420 glibenclamide preparations, Semi-Euglucon N 1.75 mg and Daonil N 1.75 mg, and of two older HB 419 glibenclamide preparations, Semi-Euglucon 2.5 mg and Daonil 2.5 mg, were compared in a randomized cross-over study in eight healthy volunteers. The HB 420 glibenclamide preparations induced peak plasma glibenclamide concentrations up to about 90 ng/ml at 1.3 to 1.4 hours after ingestion. Administration of the HB 419 preparations induced significantly lower peak plasma glibenclamide concentrations at 1.8 to 2.3 hours after ingestion. Glibenclamide was absorbed and eliminated more rapidly after administration of both HB 420 preparations than after administration of the HB 419 preparations. The mean elimination half-life of glibenclamide was 1.3 +/- 0.1 hours in the case of both HB 420 preparations and 2.0 to 2.5 +/- 0.2 hours in the case of HB 419 preparations. Although the HB 420 preparations contained lower doses of glibenclamide than the HB 419 preparations, the AUC values after administration of the former were similar to the AUC value obtained after administration of one of the HB 419 preparations, indicating improved absorption of glibenclamide from the newly developed preparations. However, the other HB 419 preparation was associated with the greatest AUC value of all, suggesting that glibenclamide was absorbed from this preparation almost as completely as from the HB 420 preparations.

Absolute bioavailability and bioequivalence of glibenclamide (Semi-Euglucon N).

Int J Clin Pharmacol Ther Toxicol. 1985 Sep; 23(9): 453-60
Neugebauer G, Betzien G, Hrstka V, Kaufmann B, von Möllendorff E, Abshagen U
The absolute bioavailability of HB 420 (a new pharmaceutical form of glibenclamide) was investigated in comparison with an i.v. infusion of glibenclamide and also in comparison with HB 419 (Semi-Euglucon) on a group of 10 healthy volunteers with the aid of a highly specific bioanalytical detection method. A comparison of the dose-corrected areas under the concentration-time curves yielded an absolute bioavailability of 102% for HB 420. The relative bioavailability of HB 419 to HB 420 was 73%. This resulted in a bioequivalent dosage relationship of 2.5 mg HB 419 to 1.75 mg HB 420. It could be experimentally confirmed on further 10 healthy volunteers that 1.75 mg HB 420 (identical with Semi-Euglucon N) and Semi-Euglucon (containing 2.5 mg HB 419) are bioequivalent with respect to the absorbed quantity of active agents. The differences in absorption rate between the new and the old form did not lead to relevant differences in the glucose profile and the release of insulin, so that the two forms can be regarded as being pharmacodynamically equivalent. The median for the terminal elimination half-life for glibenclamide was 1.38 hours (min. 0.65, max. 4.64 hours), the total clearance was 100 ml/min and the steady-state distribution volume was 7.3 l (0.1 l/kg). On the basis of half-life, it can be expected that the elimination of the unchanged substance will be virtually complete within 10-12 hours. During long-term therapy, however, it cannot be ruled out that in some diabetics cumulation could occur, the cause of which cannot be explained by the data presented.

[Pharmacodynamics and pharmacokinetics of 2 glibenclamide preparations in type 2 diabetes. Intraindividual double-blind comparison of Euglucon 5 (HB 419) and Euglucon N (HB 420)]

Dtsch Med Wochenschr. 1984 Feb 10; 109(6): 210-3
Haupt E, Putschky F, Zoltobrocki M, Schöffling K
A new galenic form of glibenclamide (with a higher specific surface area for better absorption) was compared with the conventional form in 12 insulin-dependent and glibenclamide-treated diabetics (three women, nine men; aged 37-60 years) in a double-blind controlled crossover study. There was more rapid absorption, with a maximal serum concentration after 1 1/2 hours, compared with the usual preparation which gave a lower longer-sustained maximum of serum-glibenclamide level between 1 1/2 and 4 hours. In addition, there was more complete absorption so that the needed daily dose was decreased: 3.5 mg of the new form was bio-equivalent to 5 mg of the ordinary form. Duration of effect of the new form was not shorter despite different pharmacokinetics. Response of serum insulin and C-peptide level was the same in the two forms. On the other hand, the blood-glucose profile was significantly better with the new form.