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At least 19 recordsLinked to original sources
PubMed1976

[The kinetics of sulfamerazine (Mebacid) and the effect of sulfamerazine therapy on p-aminohippuric acid clearance in pregnancy].

Elimination half-life of Sulfamerazin (Mebacid) was not different in pregnant and non-pregnant women after a single oral dose and after 11 days repeated administration in therapeutic dosis. The initial concentrations of Sulfamerazin are lower in pregnants than in non-pregnants. Elimination half-life of p-aminohippurate (PAH) is shortened by Sulfamerazin-pretreatment, renal excretion of PAH is increased respectively.

Adult↗
PubMed1980

[Pharmacokinetic model studies of sulfamerazine in domestic mammals. 3. Acetylation, protein binding, and minimal inhibitory concentration of sulfamerazine].

Acetylation and protein fixation were established for the purpose of elucidating the chemotherapeutically effective part of sulphamerazine when applied to cattle, swine, horse, sheep, dog, and cat. The highest degree of acetylation and lowest protein fixation in all species tested, were recorded from swine. A reciprocal correlation was found to exist between the two above parameters, and it was statistically secured, except for horse. A mathematical description of the functional relationship between sulphamerazine fixed to serum protein and free sulphamerazine was possible by means of the Freundlich isothermia which had been recommended by SCHOLTAN (1962) in the following form: cgeb = K+ . cfreim The problem of minimum inhibitory concentration is discussed and explained in greater detail by computational examples with Escherichia coli.

Acetylation↗
PubMed1984

Pectin-gelatin complex coacervates II: Effect of microencapsulated sulfamerazine on size, morphology, recovery, and extraction of water-dispersible microglobules.

Spherical medicated microglobules were prepared by complex coacervation of Type A gelatin with pectin, having nominal diameters of 5, 10, and 25 micron and containing 37.3, 44.9, and 45.2% (w/w) sulfamerazine, respectively. They were recovered as water-insoluble powders and were spontaneously revertible to highly disperse systems when reconstituted in water or physiological electrolyte solution. The conditions affecting microglobule formation were studied. For complete formation, the crystals must be dispersed at greater than or equal to pH 5. The effect of the sulfamerazine mass added on microglobule morphology, yield, and contents were investigated. As much as 37.3, 44.5, and 69.1% (w/w) sulfamerazine in 5-, 10- and 25-micron microglobules could be formed without loss of spherical shape. The microglobule yield versus drug-to-colloid ratio curves were nonlinear below the critical drug-to-colloid ratio for loss of sphericity. Addition of sulfamerazine suppressed coacervation by 10-15% but it had no significant effect on microglobule size. The extraction of medicated microglobules in various media demonstrated the existence of a porous matrix that required hydration to facilitate extraction of the microglobular drug. Fifteen percent of the encapsulated sulfamerazine was extracted from 25-micron microglobules as opposed to 9% from 10-micron microglobules after equilibration for 24 h in replacement electrolyte solution.

Capsules↗
PubMed1988

Pharmacokinetics, metabolism, and renal clearance of sulfadiazine, sulfamerazine, and sulfamethazine and of their N4-acetyl and hydroxy metabolites in calves and cows.

The effect of molecular structure on the drug disposition and protein binding in plasma and milk, the urinary recovery, and the renal clearance of sulfadiazine, sulfamerazine, and sulfamethazine and of their N4-acetyl and hydroxy derivatives were studied in calves and cows. Sulfadiazine was highly acetylated and was slightly hydroxylated. Sulfamerazine and sulfamethazine were hydroxylated predominantly at the methyl group of the pyrimidine side chain; hydroxylation of the pyrimidine ring itself was more extensive for sulfamethazine than for sulfamerazine. At dosages between 100 and 200 mg/kg of body weight, sulfamethazine had a capacity-limited elimination pattern, which was not observed for sulfadiazine or sulfamerazine. The concentrations of the parent sulfonamide and its metabolites in plasma and milk were parallel, the latter being lower. Metabolite concentrations in milk were at least 8 times lower than those of the parent drug. Metabolism speeds drug elimination, producing compounds with renal clearance values higher than those of the parent drug. The effect on the metabolism and renal clearance of methyl substitution in the pyrimidine side chain is discussed.

Animals↗
PubMed1978

Effect of sulfamerazine and exercise on life span of rats and hamsters.

Rats and hamsters of both sexes were divided into exercise and non-exercise groups with and without small amounts of sulfamerazine in the diet. In every case rats on exercise lived longer than their controls. The females outlived the males while hamster males lived slightly longer than females. Sulfamerazine had a significantly beneficial effect on life span of rats and apparently increased that of male hamsters. All rats fed sulfamerazine attained higher maximum weights than their controls. There was no consistent change in bone densities.

Animals↗
PubMed1975

[Effect of increased diuresis on the renal excretion of sulfamerazine].

The excretion velocity of sulfamerazine is very slow, caused by a high reabsortion rate in renal tubuli. An increased diuresis by i.p. administration of saline or p.o. load with water has no effect on the sulfamerazine excretion velocity. The enhanced diuresis is accompanied by a decrease of the urine pH-value and consequently by a decreased dissociation rate of sulfamerazine.

Animals↗
PubMed1979

Disposition of sulfonamides in food-producing animals: pharmacokinetics of sulfamerazine in ewe lambs.

Date from plasma and urine samples from four ewe lambs were analyzed after administration of sulfamerazine as single IV and oral doses. A two-compartment pharmacokinetic model was developed to describe the disposition of sulfamerazine. The drug was eliminated, primarily by renal excretion of (i) unchanged sulfamerazine and metabolism to an acetyl metabolite, (ii) polar conjugates, and (iii) a third metabolite. The biological half-life of the drug was 6.6 hours. The average value of the absorption rate constant was 0.433 hour-1 (half-life 1.60 hours). Sulfarmerazine was relatively completely absorbed (approx 81% of dose) after oral administration in solution.

Administration, Oral↗
PubMed1978

The distribution of sulfamerazin between plasma, cerebrospinal fluid, and bile in humans.

The concentration-time curves of sulfamerazin were determined in plasma, cerebrospinal fluid (c.s.f.) and bile in two groups of patients (ventricle drainage and Kerr's T-tube drain). In plasma, a half-life of 13.6 hours as well as an invasion and evasion constant of 0.145 hours -1 and 0.051 hours -1, resepectively, were observed. The distribution of half-life times showed a bimodal behavior in these patients. The unbound part of sulfamerazin was 12% and the acetylated products 14%. Unlike plasma in c.s.f. and bile the influx is delayed up to steady state. The decreases of concentration in all three compartments are the same. The concentration ratio of sulfamerazin between C.S.F. and bile and plasma water amounted to 1 and 2.5, respectively. Of the given dose of sulfamerzin, 0.87% was eliminated by bile within 24 hours. The therapeutic conclusions are discussed with regard to the bimodal distribution of half-lives, the minimal inhibition concentrations and the unbound part in the plasma.

Acetylation↗
PubMed1993

[Pharmacokinetics of sulfamerazine after a single intravenous dose in healthy calves and calves with diarrhea of different severity with consideration of the influence of an existing kidney function restriction].

Blood levels of Sulfamerazine were examined in 16 calves with different severity of diarrhoea in consideration of kidney function and compared with the values of 5 clinically intact animals. Urea and creatinine levels in plasma as well as urea and creatine clearance were tested to check kidney function. A single dose of 60 mg Sulfamerazine/kg body weight was administered to all animals via catheter into the vena jugularis. Blood samples were collected for 48 hours. The mean concentration of Sulfamerazine in calves with severe diarrhoea was significantly higher 24 hours post application than in the healthy control group and in animals with low and middle intensive diarrhoea (healthy animals: 37.61 +/- 7.18 micrograms/ml; animals with severe diarrhoea: 57.3 +/- 7.5 micrograms/ml). Animals with severe diarrhoea showed significantly higher values of half life time of elimination t1/2 (healthy animals: 7.08 +/- 1.25 h; animals with severe diarrhoea: 11.39 +/- 2.11 h) and of area under the curve AUC (healthy animals: 2023.4 +/- 397.21 micrograms*h/ml; animals with severe diarrhoea: 2990.6 +/- 594.9 micrograms*h/ml) than the others. Low and middle intensive diarrhoea has no important influence on the pharmacokinetics of Sulfamerazine.

Animals↗
PubMed1977

Pharmacokinetics of sulfaclomide and sulfamerazine in patients with impaired renal function after first and after repeated application.

At the beginning of the therapy with sulfaclomide resp. sulfamerazine elimination half-life of sulfaclomide was prolonged significantly in patients with impaired renal function (creatinine in serum greater than 2 mg/100 ml) on 119.6+/-6.9 h in comparison to control group (83.6+/-14.5 h). Half-life of sulfamerazine (23.6+/-4.1 h) did not differ from that of the control group (20.3+/-2.8 h). Renal excretion of both sulfonamides was sharply diminished. After treatment for 11 days with sulfaclomide resp. sulfamerazine in patients with impaired renal function, half-lives were prolonged to 117.3+/-6.1% resp. 119.3+/-3.9% of the initial value. In patients with impaired renal function elimination half-life of PAH as a measure of tubular function is three times that of control group. It is not statistically significantly influenced by repeated administration of the sulfonamides. In the control group there is a shortening of the PAH-half-life under the same conditions.

Adolescent↗
PubMed2002

Crystallization and transitions of sulfamerazine polymorphs.

A bulk powder of sulfamerazine polymorph II in a narrow distribution of particle size was prepared for the first time. The two known sulfamerazine polymorphs, I and II, were physically characterized by optical microscopy, powder X-ray diffractometry, differential scanning calorimetry, carbon-13 solid-state nuclear magnetic resonance spectroscopy, and measurements of aqueous solubility and density. The thermodynamics and kinetics of the transition between the polymorphs was examined under various pharmaceutically relevant conditions, such as heating, cooling, milling, compaction, and contact with solvents. The two polymorphs were found to be enantiotropes with slow kinetics of interconversion. The thermodynamic transition temperature lies between 51 and 54 degrees C, with polymorph II stable at lower temperatures. Ostwald's Rule of Stages explains the crystallization of the polymorphs from various solvents and may account for the delay in the discovery of polymorph II.

Anti-Infective Agents↗
PubMed2003

Characterization of physical mixtures and directly compressed tablets of sulfamerazine polymorphs: implications on in vitro release characteristics.

The present study evaluates the effects of excipients, compression pressure, and relative humidity (RH) on the stability of sulfamerazine polymorphs (referred here as SMZ I and SMZ II) and their release from directly compressed tablets using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and dissolution analysis. SMZ I and SMZ II tablets were compressed with magnesium stearate (MGST), and microcrystalline cellulose (MCC) at 5000, 7500, and 10,000 lbs. pressures and stored at 40, 75, 95, and 100% RH conditions for 5 weeks. There were indications of possible drug-excipient interaction in the binary mixtures under different relative humidity conditions from the DSC data, but they could not be confirmed by PXRD because the crystal structures of the drug and excipients remained unaltered. The crystal structures of the polymorphs in the tablet also remained unaltered under the above conditions. There were, however, significant differences observed in the drug release properties of the two polymorphs. SMZ II was found in general to have a higher rate of drug release than SMZ I. Extensive gelation of MCC under higher moisture conditions, compression pressure during tableting, and inherent tabletability of the sulfamerazine crystals were factors that affected drug release. All these factors contributed towards prolonging the disintegration and deaggregation of the tablet particles and were therefore concluded to be the rate limiting steps for the dissolution process.

Anti-Infective Agents↗
PubMed1986

Reversal of sulfamerazine inhibition of rat hepatic uroporphyrinogen synthesis by folic acid.

The ability of rat hepatic uroporphyrinogen cosynthase to direct formation of uroporphyrinogen III and the synthesis of uroporphyrinogen in vitro was impaired by sulfamerazine. Inhibition was reversed by the addition of folic acid. Administration of a single, oral dose (1 g/kg) of sulfamerazine to rats was associated with elevated levels of hepatic uroporphyrin I isomer. These results suggest that sulfonamides may interfere with the biosynthesis of uroporphyrinogen III.

Ammonia-Lyases↗
PubMed2001

Influence of crystal structure on the tableting properties of sulfamerazine polymorphs.

PURPOSE: To understand the influence of polymorphic structure on the tableting properties of sulfamerazine. METHODS: Bulk powders of sulfamerazine polymorph I and of two batches. II(A) and II(B) of different particle size, of polymorph II were crystallized. The powders were compressed to form tablets whose porosity and tensile strength were measured. The relationships between tensile strength, porosity and compaction pressure were analyzed by the method developed by Joiris. E., et al. Pharm. Res. 15:1122-1130 (1998). RESULTS: The sensitivity of tensile strength to compaction pressure, known as the tabletability, follows the order. I >> II(A) > II(B) and the porosity at the same compaction pressure, which measures the compressibility, follows the order, I << II(A) < II(B). Therefore. the superior tabletability of I over II(A) or II(B) is attributed to its greater compressibility. Molecular simulation reveals slip planes in crystals of I but not in II. Slip planes provide I crystals greater plasticity and therefore greater compressibility and tabletability. Larger crystal size of II(B) than of II(A) leads to fewer contact points between crystals in the tablets and results in a slightly lower tabletability. CONCLUSIONS: Slip planes confer greater plasticity to crystals of I than II and therefore greater tabletability.

Anti-Infective Agents↗
PubMed1982

Pharmacokinetics of sulfamerazine and antipyrine in neonatal and young lambs.

The disposition of sulfamerazine after oral and after IV administrations was studied in lambs at different times after birth. There was a gradual increase in systemic clearance and plasma binding until the 9th week. After sulfamerazine was given orally, there was a marked evolution in the shape of the concentration-time curves in function of age, strongly suggesting a defective absorption rate in the first weeks after birth. For antipyrine, too, the clearance increased gradually during the period of study, but absorption seemed to be rapid in the very young animals.

Administration, Oral↗
PubMed2005

A study of sulfamerazine single crystals using atomic force microscopy, transmission light microscopy, and Raman spectroscopy.

Sulfamerazine (SMZ) Form I and II single crystals were prepared from aqueous dispersions of SMZ bulk samples and studied using several microscopic and spectroscopic techniques. Transmission light microscopy and Raman spectroscopy were used to observe and identify single crystals. The results indicated that Form I single crystals tended to be rectangular laths while Form II ones tended to be hexagonal laths. Surface morphology of individual single crystals was further investigated by atomic force microscopy (AFM). AFM images revealed a smooth top surface, a uniform height, and sharp edges for both forms of single crystals. Both height and phase images showed crystalline terraces with different step heights for the top surface of Form I. Surface properties of single crystals were evaluated using AFM force measurements. Experimental results indicated that the top surface of Form I single crystals was more hydrophilic than that of Form II. Theoretical calculations predicted a dominant crystal face of (020) for the Form I single crystals and (002) for the Form II ones. The correlations between calculation predictions and experimental results were discussed.

Anti-Infective Agents↗
PubMed1977

Direct spectrophotometric determination of sulfathiazole in presence of sulfadiazine and sulfamerazine.

A direct spectrophotometric method for the quantitative determination of sulfathiazole and the total pyrimidyl sulfonamide content in a mixture containing sulfadiazine and sulfamerazine is reported. This three-component system was readily reduced to the problem of a simple two-component system analysis. Based on dual isoabsorptive wavelength spectroscopy, simultaneous equations were developed that required absorbance measurements at only two selected wavelengths both isoabsorptive. The location of the isoabsorptive wavelengths was dependent on the pH of the solvent medium, and 0.1 M HCl gave the best results. The validity of the derived equations was demonstrated in a recovery study involving synthetic mixtures containing varying quantities of the three sulfonamides. The recovery was linear over a wide concentration range, and the precision of the method was about 1%.

Methods↗
PubMed1979

Flocculation of sulfamerazine suspensions by a cationic polymer.

Flocculation by a cationic polymer of sulfamerazine suspensions containing a wetting agent was evaluated. Suspensions with sufficient surfactant concentrations to ensure complete wetting were deflocculated. When the anionic surfactant, dioctyl sodium sulfosuccinate, was used as a wetting agent, the suspensions were flocculated over a limited polymer concentration range. Flocculation was attributed to simultaneous interaction of a polymer molecule with more than one particle. At higher polymer concentrations, the particles were covered completely with polymer, leading to repulsion between the particles and deflocculation of the suspensions. The polymer concentration required for flocculation provided evidence for interaction between the anionic surfactant and the cationic polymer. Suspensions containing a nonionic surfactant also were flocculated using various polymer concentrations. When a surfactant mixture was employed in the suspensions, the peak sedimentation volume of flocculated systems and the concentration of polymer at the peak depended on the surfactant mixture composition.

Cations↗