Succinyl-sulfathiazole

Spiropiperone I, 306 Spirorenone 3, 91, 92 Spi rothiobarbital 1, 276 Stanazole 174 Stenbolone acetate 155 Styramate 2. 219 Succinyl sulfathiazole U 132 Sudoxicam 2, 394 Sulazepam , 403 Sulconazole 3, 133 Sulfabenzamide 112... 

Interference with transport characteristics can serve many purposes. The introduction of a hydrophilic disposable moiety can restrict a drug to the gastrointestinal tract and prevent its absorption. Such a type of drug is represented by the intestinal disinfectant succinyl-sulfathiazole (3.27). On the other hand, lipophilic groups can ensure peroral activity, as in the case of the penicillin derivative pivampicillin (3.28), which enters the circulation and then slowly releases the antibiotic in its free acid form, producing high blood levels of the latter. 

The major class of compounds used as growth promotants in non-ruminant (single stomached) animals, such as pig and poultry, is that of the antimicrobials. Growth responses to antimicrobials were reported as early as 1946 but these findings were overlooked at the time. However, several years later, when growth responses were obtained with chlor-tetracycline, streptomycin (29), succinyl sulfathiazole and 3-nitro-4-hydroxyphenylarsonic acid, the practical aspects of growth responses to antimicrobials became clear. Since then, hundreds of antimicrobial compounds that promote growth have been reported in the scientific literature and in patents and many have been approved for use commercially. 

Simultaneous diaveridine, phthalyl sulfathiazole, pyrimethamine, succinyl sulfathiazole, sulfabenzamide, sulfacetamide, sulfachloropyrideizine, sulfadiazine, sulfadimethoxine, sulfaguanidine, sulfamerazine, sulfameter, sulfamethazine, sulfamethizole, sulfamethox-yp3Tidazine, sulfamoxole, sulfanilamide, sulfaniUc acid, sulfapjnidine, sulfaquinoxaline, sulfathiazole, sulfisomidine, sulfisoxazole, trimethoprim... 

The instability of many anhydrate phases with respect to water has been long known. For instance, it was shown by Shefter and Higuchi that hydrate phases of cholesterol, theophylline, caffeine, glutethimide, and succinyl sulfathiazole would spontaneously form during dissolution studies [32]. Similar behavior has been reported for metronidazole benzoate [33] and carbamazepine [34]. In each of these systems, the integrity of the anhydrous phases can be maintained only as... 

Sayed HA, Price JC. Tablet properties and dissolution characteristics of compressed cellulose acetate butyrate microcapsules containing succinyl sulfathiazole. Drug Development and Industrial Pharmacy. 1986 12 577-587. 

Sulfaguanidine, sulfadiazine, and succinyl sulfathiazole from a pharmaceutical powder were baseline resolved on a C,g column (A = 270nm) using a 20/80 methanol/water (50 mM ammonium acetate) mobile phase [508]. Elution was complete in 5 min and peak shapes were excellent. Twelve sulfonamides were well resolved on a C,g colunm (A = 254 nm) using an isocratic 6/94 IPA/water (20 mM sodium dodecylsullate [SDS] with phosphate buffer at pH 3.0) mobile phase. Elution was complete in 15 min. The effects of changing % IPA and SDS concentration on Id and a values were presented [509]. This study provides excellent background information for method development. Detection limits of 1 pg/mL were reported. 

Several other hydrates also exist in different polymorphic modifications. For example, fiuprednisolone monohy-drate, succinyl sulfathiazole monohydrate, nedocromil... 

Substitution of the p-amino group leads to loss of antibacterial activity. However, substituents on the p-amino group, which readily degrade in vivo to release the free amino group, have been employed with success. For example, succinyl sulfathiazole undergoes enzymatic degradation in vivo to yield the active sulfathiazole with a free primary amine moiety. 

The sulphonamides have been used in the treatment of intestinal infections. Substitution of the aniline N with a succinyl group produces an acidic compound which is fully ionised at intestinal pH and is therefore not appreciably absorbed into the bloodstream. Slow enzjmatic hydrolysis of the product in the intestine releases the free primary amine group which is essential for activity. This concept of prodmg design has been exploited in the sjmthesis of succinyl-sulfathiazole (p/Gt 4.5) from sulfathiazole (p/Gt 7.1) (Fig. 22.42). 

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