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PubMed2002

Application of time-dependent sessile drop contact angles on compacts to characterise the surface energetics of sulfathiazole crystals.

The time-dependent wetting of sulfathiazole compacts with sessile water drops was evaluated using video microscopy. The influence of sulfathiazole crystalline form, particle size, pre-saturation with water, humidity and compaction pressure on the droplet spreading kinetics and contact angles are reported. The rate and extent of droplet spreading decreased for compact surfaces of high microscopic roughness; this was determined by atomic force microscopy (AFM). Pre-saturation of powder compacts with water (pre-saturated with sulfathiazole) enhanced droplet spreading and enabled pseudo-equilibrium contact angles to be determined for up to 10 min. Sessile-drop contact angles on both sulfathiazole powder compacts and single crystals are compared with particle contact angles determined by liquid penetration. This study has led to an improved understanding of the influence of physical heterogeneities and the face-specific surface chemistry of individual crystals on the wetting characteristics of pharmaceutical compacts.

Algorithms↗

PubMed2001

Polymorph control of sulfathiazole in supercritical CO2.

PURPOSE: Sulfathiazole was used to investigate polymorph control in liquid and supercritical CO2. Conventional techniques require a variety of solvents and techniques to produce different polymorphs. The present approach involves precipitation from an organic solution with liquid or supercritical CO2 using the SEDS process. METHODS: Sulfathiazole was precipitated from methanol or acetone solutions. Experiments were carried out within a temperature range of 0-120 degrees C. Composition of the fluid phase was varied between x(CO2) = 0.27-0.99. Pressure was constant at 200 bar. Samples obtained were analyzed using SEM, DSC, and XRPD. RESULTS: Pure polymorphs were obtained at different temperatures and flow rate ratios of CO2/solvent. With methanol Form I, III, and IV and their mixtures could be crystallized. With acetone Form I or a mixture of Form I and amorphous sulfathiazole was obtained. The fluid composition was used as a control parameter to define the process areas (T-x diagram) where the pure forms or mixtures of different forms could be obtained. CONCLUSIONS: The experiments enabled the relationship between flow and temperature for each polymorph to be determined. The crystallization method developed proved to be a simple and efficient technique for reproducible and consistent isolation of sulfathiazole polymorphs.

Acetone↗

PubMed1995

Deposition kinetics, metabolism and urinary excretion of sulfathiazole following oral administration in sheep.

Deposition kinetics, metabolism and urinary excretion of sulfathiazole were investigated in German black head sheep following single oral administration (100 mg/kg). Kinetic evaluation of plasma levels was performed using a two-compartment best fit model. Sulfathiazole is significantly metabolized to N4-acetyl metabolite in the rumen fluid. The drug is very poorly absorbed since the minimum effective concentration in plasma was not attained at any time following oral administration. The prolonged elimination half-life in sheep may be due to a low rate of drug absorption from the rumen and gastro-intestinal tract. Sulfathiazole was mainly excreted in the urine as free drug and N4-acetyl metabolite.

Administration, Oral↗

PubMed1977

Disposition of sulfonamides in food-producing animals V: Disposition of sulfathiazole in tissue, urine, and plasma of sheep following intravenous administration.

The plasma, urine, and tissue sulfathiazole concentrations were determined at various times following intravenous administration to 12 sheep. The plasma and urine data were consistent with a one-compartment pharmacokinetic model, with an elimination half-life of 1.1 hr and a volume of distribution of 0.39 liter/kg. Sulfathiazole was eliminated by excretion of unchanged drug in urine (67%) and by formation of two metabolites. The data obtained from eight tissue sites were consistent with the one-compartment pharmacokinetic model presented and confirmed that tissue residues of sulfathiazole can be calculated from serum and urine drug concentration.

Animals↗

PubMedDate not supplied

The 1941 sulfathiazole disaster and the birth of good manufacturing practices.

The beginning of modern standards for good manufacturing practices can be traced to an incident that began in December 1940, when the Winthrop Chemical Company of New York put on the market sulfathiazole tablets contaminated with phenobarbital. Hundreds of deaths and injuries resulted. FDA's investigation into Winthrop's sulfathiazole production and the agency's efforts to retrieve the Winthrop drug remaining on the market revealed numerous control deficiencies in the plant and serious irregularities in the firm's attempt to recall the tainted tablets. The incident prompted FDA to require detailed controls in sulfathiazole production at Winthrop and throughout the industry, an approach that became the basis for production control standards for all pharmaceuticals.

Anti-Infective Agents↗

PubMed2004

[Effect of cerium nitrate supplementation to silver sulfathiazole preparations on survival of planctonic and attached to the dermis Staphylococcus aureus cells].

The purpose of this study was to evaluate the influence of preparations containing silver sulfathiazole, with or without cerium nitrate, on survival of Staphylococcus aureus. In the first step, sensitivity of the planctonic bacteria to the tested compounds was determined. Addition of cerium nitrate enhanced the antibacterial activity of silver sulfathiazole by 4 times, as evidenced by MIC and MBC values. For the estimation of antibacterial activity of the mentioned chemotherapeutic on attached bacteria in vitro model of an "infected wound" was applied. Sensitivity of bacteria attached to the dermis was lower than sensitivity of planctonic bacteria. Kinetics of the release of chemotherapeutic compounds incorporated into a collagen dressing was the most effective for the combination of silver sulfathiazole with cerium nitrate.

Anti-Infective Agents, Local↗

PubMed1978

Disposition of sulfonamides in food-producing animals: pharmacokinetics of sulfathiazole in swine.

Disposition of sulfathiazole in plasma and urine of swine was determined following single intravenous and oral doses. Pharmacokinetics of the drug were described by a 1-compartment open model. The drug was rapidly eliminated, mainly by renal excretion of unchanged sulfathiazole and metabolism to acetylsulfathiazole, with a biological half-life of 1.4 hours. Sulfathiazole (in solution) was absorbed rapidly (half-life 0.8 hour) and relatively completely (73%) following oral administration.

Animals↗

PubMed2006

Characterization of temperature-induced phase transitions in five polymorphic forms of sulfathiazole by terahertz pulsed spectroscopy and differential scanning calorimetry.

The far-infrared properties of all five known polymorphic forms of the drug sulfathiazole have been studied by terahertz pulsed spectroscopy and low-frequency Raman spectroscopy. The observed spectra of the different polymorphs are distinctly different. Terahertz pulsed spectroscopy proves to be a rapid and complementary alternative to other physical characterization techniques reported in the literature for distinguishing between the five forms. Variable-temperature measurements (293-473 K) of all polymorphic forms have been performed. The phase transitions observed have been related to thermal analysis data. Form I is the form stable at high temperature of sulfathiazole with a melting point of about 475 K. Form II melts at around 470 K and recrystallizes at higher temperatures to form I. Forms III, IV, and V all convert to form I via a solid-solid phase transition at temperatures below 450 K. The phase transitions can be monitored by terahertz pulsed spectroscopy. Polymorphic impurities of the samples can be detected in the room temperature spectra and their effect on the phase transition behavior can be studied.

Calorimetry, Differential Scanning↗

PubMed2001

Determination of the onset of crystallization of N1-2-(thiazolyl)sulfanilamide (sulfathiazole) by UV-Vis and calorimetry using an automated reaction platform; subsequent characterization of polymorphic forms using dispersive Raman spectroscopy.

This work describes the use of UV/visible spectroscopy and calorimetry to follow the onset of crystallization of a commercially available compound, N(1)-2-(thiazolyl)sulfanilamide (sulfathiazole), during crystallization reactions performed using an automated reaction platform. Sulfathiazole has been the subject of numerous publications through which considerable confusion about the morphic form is apparent. This work does not attempt to investigate exhaustively the polymorph issue, but rather to exploit the use of the HEL auto-MATE for monitoring the onset of crystal formation. Real-time calorimetry and UV-Vis spectroscopy are compared as tools for determining the onset of crystallization. Subsequently, differential scanning calorimetry, dispersive Raman, and infrared spectroscopy analysis serve to identify the crystal forms generated by the HEL auto-MATE. A solvent-anti-solvent matrix and several bench-top crystallization experiments were performed to supplement the investigation in terms of generating the desired polymorphs.

Ammonia↗

PubMedDate not supplied

Rapid quantitative thin layer chromatographic screening procedure for sulfathiazole residues in honey.

A procedure is presented for the quantitative determination of sulfathiazole residues in honey. Induced fluorescence of sulfathiazole is measured by fluorescent scanning densitometry; sulfaquinoxaline is added as an internal standard for quantitation. Recovery is greater than 98% and results are linear over the range 0.05-0.60 mg/kg. The detection limit, CL (k = 3), is 0.02. The procedure allows a single analyst to process 50-60 samples/day.

Chromatography, Thin Layer↗

PubMed1982

Screening test for sulfamethazine and sulfathiazole in swine liver.

A screening method is described for estimation of sulfamethazine and sulfathiazole residues in swine livers. Tissues are homogenized with CHCl3-ethyl acetate (1 + 1). The drugs are extracted from the organic solvent with pH 10 carbonate buffer and back-extracted into dichloromethane, as an ion-pair with tetrabutylammonium hydroxide, without pH adjustment. Following evaporation of the solvent, the residue is dissolved in methanol, subjected to thin layer chromatography, and detected by the Bratton-Marshall reaction. Recoveries of sulfamethazine and sulfathiazole, determined by high pressure liquid chromatography, were 50.8 and 42%, respectively, with coefficients of variation of 4.2 and 4.7%.

Animals↗

PubMed1976

Binding of salicylate and sulfathiazole by whole blood constituents.

The binding of salicylic acid and sulfathiazole to bovine whole blood, plasma proteins, and purified albumin fraction was investigated using a dynamic dialysis system. The binding profiles for salicylic acid were quite similar in bovine plasma and 4% bovine serum albumin. In contrast, the binding of sulfathiazole was significantly greater in the plasma than in solutions of fraction V bovine serum albumin. Data from dynamic dialysis binding studies of the compounds, conducted in whole blood and suspended erythrocyte systems, did not lend themselves to analysis by classical methods. Hemolysis and alteration in the nature of the protein binding sites during the binding studies were shown to be factors that could explain the unusual binding observed in the whole blood system.

Animals↗

PubMed1999

Sulfathiazole polymorphism studied by magic-angle spinning NMR.

The literature on sulfathiazole polymorphs has many confusions and inconsistencies. These are largely resolved by the distinctive appearance of (13)C magic-angle spinning NMR spectra, which immediately show the number of molecules in the crystallographic asymmetric unit. The spectra presented include those of a newly-recognized form. The assignments of the spectra are established and discussed in relation to such factors as electronic structure of the aromatic ring, second-order quadrupolar effects originating from the nitrogen nuclei, and hydrogen bonding. The results are compared to literature information on the crystal structures. When the amino group acts as a hydrogen bond acceptor, there is a shielding effect on C-4 to the extent of ca. 8 ppm (which should be compared to a further shielding by ca. 10 ppm for sulfathiazole sulfate). The fact that the spectrum of form III is similar to the sum of those of forms IV and V is rationalized in relation to the crystal structures. Some surprising variability of spectra with temperature and with specific sample is reported.

Carbon Isotopes↗

PubMed1984

Physiological model for distribution of sulfathiazole in swine.

A physiological flow model was developed for the distribution of sulfathiazole residues in various tissues in swine. The approach was compartmental, in which the compartments and equilibrium constants had physiological meaning. Differential equations were developed, and appropriate parameter values and initial conditions were substituted and solved by a fourth-order Runga-Kutta technique. Simulation values corresponded with the experimentally determined concentration values in plasma and kidney, liver, muscle, fat, and heart tissues.

Animals↗

PubMed1989

Polymorphism of sulfathiazole.

The polymorphism of sulfathiazole has been reexamined. The issue of the separate existence of two of the forms, forms III and IV, has now been definitively resolved: both forms exist. Single crystals were used to generate X-ray diffraction patterns, equivalent to those normally obtained from polycrystalline samples, using the ingenious Gandolfi camera. The patterns obtained were distinct and in agreement with the theoretical powder patterns calculated from the reported structures of the two forms, thus confirming the separate existence. Disagreement between the results of previous workers has been traced to two main causes: characterization techniques are not very discriminating for the two forms (III and IV), and the samples examined have invariably been mixtures of III and IV, since the two forms usually crystallize together. Furthermore, crystals of form III exhibit marked preferred orientation, which complicates powder X-ray diffraction (PXRD) analysis. The IR, Raman, and 13C NMR spectra, and PXRD patterns are reported for all four forms. These distinct fingerprints should now enable one to isolate pure samples and to study the properties and the relationships between these forms with full confidence.

Calorimetry, Differential Scanning↗

PubMed2004

Specific polyclonal-based immunoassays for sulfathiazole.

A highly sensitive and specific enzyme-linked immunosorbent assay has been developed for detection of sulfathiazole (STZ, 4-amino- N-thiazol-2-yl-benzenesulfonamide). A set of haptens was synthesized in order to produce polyclonal antibodies against sulfonamides. Two ELISA formats (antibody-coated and conjugate-coated) were also investigated using all the serum/coating conjugate combinations that showed specific recognition. The developed ELISA succeeded in detection of STZ at concentrations as low as 0.03 ng mL(-1) over a measurable range of 0.12-6.71 ng mL(-1). Selectivity studies have demonstrated that other sulfonamides do not interfere significantly (<10%) with analysis of STZ by this immunochemical technique. Analysis of spiked bee honey samples by the developed ELISA method showed recoveries were good. The selectivity and sensitivity (IC(50)=1.6 ng mL(-1)) make it a suitable screening method for determination of low levels of STZ in food samples.

Antibodies↗

PubMed2006

A comparison of morphology and surface energy characteristics of sulfathiazole polymorphs based upon single particle studies.

The morphological, adhesion and surface energetic properties of three sulfathiazole polymorphs (III, IV and polymorph I prepared from both acetone and methanol, designated I-ace and I-met, respectively) produced using Nektar supercritical fluid (SCF) technology have been characterized using scanning electron microscopy (SEM) and atomic force microscopy (AFM). Surface roughness values for each polymorph were determined at different length scales. At sample sizes less than 1micromx1microm the polymorphs rank in terms of roughness as follows: I-met>I-ace approximately equal to IV>III. At the larger scales the polymorphs rank in terms of roughness as follows: I-met>III>I-ace approximately equal to IV. The surface energies for polymorphs determined against graphite (HOPG) and particles of the same polymorph were, respectively, I-met: 0.99mJm(-2) (S.D. 1.25mJm(-2)), 3.09mJm(-2) (S.D. 2.67mJm(-2)); I-ace: 309mJm(-2) (S.D. 329mJm(-2)), 16mJm(-2) (S.D. 11mJm(-2)); III: 1.17mJm(-2) (S.D. 1.5mJm(-2)), 5.4mJm(-2) (S.D. 3.6mJm(-2)); IV: 20.35mJm(-2) (S.D. 28.5mJm(-2)), 16.8mJm(-2) (S.D. 9.6mJm(-2)). In terms of surface energies the polymorphs hence rank I-ace>IV>III approximately equal to I-met (HOPG adhesion measurements) and IV approximately equal to I-ace>III>I-met (particle cohesion measurements). Consideration of contacting asperities and surface roughness was shown to have limited effect on the surface energies, and instead the differences were ascribed to variations in the surface chemistry as a result of changes in crystallization mechanisms.

Acetone↗

PubMed1990

Selective removal of anti-acetylcholine receptor antibodies and IgG in vitro with an immunoadsorbent containing immobilized sulfathiazole.

Adsorption therapy, which treats the autoimmune disease by the selective removal of pathogenic substances from the blood, is an active subject. In this therapy, bioactive molecules such as antigen, antibodies and protein A are usually used as affinity-ligands. The disadvantages of using these substances as affinity-ligands are the availability, sterilizability, and ability to cause antigenic reactions. After surveying hundreds of synthetic compounds, it was found that polyacrylic beads [Eupergit C (EC)] immobilized covalently with sulfathiazole (ST) are an ideal biomimetic ligand for the selective adsorption of IgG (24.3 +/- 0.4 mg IgG/g wet beads). In an in vitro study, this adsorbent selectively removed the antiacetylcholine (AChR) receptor antibody of myasthenia gravis (MG) patients. Further experiments demonstrated that the Fab fragment was adsorbed three times more efficiently than the Fc fragment of IgG.

Animals↗