• Journal of Pharmaceutical Investigation
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• 제7권1_4호
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• pp.22-27
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• 1977

Absorption of sulfisoxazole after oral administration was significantly increased by small dose(60mg/kg) of alloxan but not increased significantly by large dose (160mg/kg) of alloxan from that of normal rabbits. Pretreatment with alloxan did not give any effect on clearance of sulfisoxazole. As the results, It could come to conclusion that in creased absorption of the sulfisoxazole administered small dose of the alloxan was influenced by transport of intestinal membrane or intestinal enzyme activation or increase of intestinal absorption function.

• Journal of Pharmaceutical Investigation
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• 제17권3호
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• pp.127-133
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• 1987

Dissolution characteristics and urinary excreted amount of commercially available three brands of sulfisoxazole tablets were investigated in order to elucidate the in vitro-in vivo correlations and relative bioavailability in humans. All the tablets tested met the K.P. IV and the USP XXI specifications for tablet weight variation, content uniformity, disintegration and dissolution. The disintegration and dissolution rate constants of sulfisoxazole tablets in pH 2.0 HCl-KCl buffer were reduced more significantly (p<0.05) than those in diluted HCl $(1{\rightarrow}12.5)$ and pH 6.5 phosphate buffer. It seemed to be attributed to the pH dependent solubility of sulfisoxazole. We could see that the relative bioavailability of brand B to sulfisoxazole powder was about 90% and that its value was higher than those of other two brands from the urinary excretion data obtained from eight healthy male volunteers by means of Latin square cross over design. No useful correlation was observed between the in vitro and in vivo studies in this experiment.

• Journal of Pharmaceutical Investigation
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• 제19권1호
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• pp.15-20
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• 1989

The displacement of protein bound sulfonamides (sulfisoxazole, sulfamethoxazole, sulfisomidine) by furosemide was investigated in bovine serum albumin by equilibrium dialysis method. Furosemide $(2{\times}10^{-4}M)$ in bovine serum albumin ($7.24{\times}10^{-5}$, $1.45{\times}10^{-4}$, $2.89{\times}10^{-4}M$). Sulfisoxa캐1e and furosemide were bound reversibly to bovine serum albumin and competitive for the same binding sites when administered together. Consequently, dosage regimen of sulfisoxazole should be adjusted carefully when sulfisoxazole is administered along with furosemide.

• Archives of Pharmacal Research
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• 제5권2호
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• pp.61-70
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• 1982

Sulfisoxazole, a chemotherapeutic agent, was microencapsulated with ethylcellulose by means of phase separation form cyclohexane by temperatture change. The size distribution was determined by use of standard sieves and the effect of core to wall ratio was noted. To examine their shapes and usrface characteristics, the microcapsules were observed with a scanning electron microscope. Release of the drug from microcapsules into pH 7.5 buffer medium was studied. The release pattern was found to have similar properties to the release of a drug from an insoluble porous matrix reported. The apparent diffusion coefficient of sulfisoxazole was measured for the transport of the drug from the core of microcapsules into the surronding sink condition. The apparent diffusion coefficient increased with increasing capsule size.

• 대한수의학회지
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• 제15권1호
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• pp.101-108
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• 1975

The susceptibility of 536 isolates of Staphylococcus and 313 isolates of Streptococcus to a number of chemotherapeutics were studied. These organisms were isolated from bovine mastitis during 1973 and 1974. In addition to this, the rate of multiple resistance of 425 isolates of Staphylococcus and 164 isolates of Streptococcus, isolated in 1974, to the chemotherapeutics was analysed. The results obtained in this work were summerized as follows: 1. Staphylococcus and Streptococcus isolated in 1974 showed a higher resistance, with 3 exceptions of chemotherapeutics, than the isolates of 1973. 2. Staphylococcus isolated in 1973 and 1974 showed a higher susceptibility than Streptococcus. 3. The strains of Staphylococcus resistant to colistin were 39 strains (9.2%), to colistin and sulfisoxazole 33 (7.8%), to streptomycin, kanamycin, colistin and sulfisoxazole 20 (4.7%), and to penicillin, colistin and sulfisoxazole 18 (4.2%). 4. The strains of Streptococcus resistant to colistin were 17 strains (10.4%), to streptomycin, kanamycin, colistin and sulfisoxazole 13 (7.9%), to colistin and sulfisoxazole 11 (6.7%) and to penicillin, colistin and sulfisoxazole 11 (6.7%).

• Archives of Pharmacal Research
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• 제5권2호
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• pp.79-86
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• 1982

Sulfisoxazole, $C-{11}H_{13}N_{3}S$, crystallized in the orthohombic system, space group Pbca, with a = 14.492(1), b = 11.563(1), c = 14.900(2) $\AA$ and Z = 8. Intensities for 1867(1360 observed) unique reflections were measured on a four-circle diffractometer wirh CuKa radiation ($\lambda$ = 1.5418$\AA$). The structure was solved by heavy atom methods and refined by full-matrix least-squares procedures to a final R of 0.094. The benzene ring plane makes an angle of $68^{\circ}C$ with the plane of the isoxazole ring, which is plannar. The conformational angle formed by the torsional angle C(4)-S-N(2)-C(7) is $54^{\circ}C$. There are two intermolecular hydrogen bonds in the structure. One of them is of the type N-H...H with the length 2.915$\AA$. Thus two dimensional networks of hydrogen bonds form infinite moelcular sheets parallel to the (001) plane. Adjacent sheets are bound together by van der Waals forces.

• 대한화학회지
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• 제20권1호
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• pp.19-34
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• 1976

Sodium sulfisoxazole hexahydrate, $C_{11}H_{12}N_3O_3SNa{\cdot}6H_2O$의 결정 및 분자구조를 X-선 회절법으로 해명하였다. 이 화합물의 결정은 공간군 $P2_1/c$에 속하는 단사형으로 a = 15.68(3), b = 7.70(2), c = $17.94(4){\AA}$, ${\beta}$ = $118(2)^{\circ}$ and Z = 4이다. Weissenberg 사진 촬영으로 얻은 회절반점의 총수는 1717개이며 중원자법을 적용하여 구조해명을 한 후 최소 자승법으로 정밀화하였으며 최종 R값은 0.14이다. Benzene ring과 isoxazole ring은 평면구조를 가지며 서로 $60^{\circ}$의 각을 이루고 있다. 나트륨 원자는 다섯개의 물의 산소 원자들과 N(1)으로 만들어진 찌그러진 팔면체로 배위되어 있다. 분자들은 결정내에서 14개의 서로 다른 종류의 수소결합으로 결합되어 있다. 여섯종류의 $O-H{\cdots}O-H$, 세종류의 $O-H{\cdots}O,$ 두종류의 $O-H{\cdots}N$및 각각 한종류의 $N-H{\cdots}O,$ $O-H{\cdots}N$, $N-H{\cdots}O-H$ 수소결합들이며 그 길이는 2.71에서 $3.04{\AA}$까지이다.

• 미생물학회지
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• 제12권2호
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• pp.77-84
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• 1974

In order to study 5-nitro-2-furaldehyde derivatives having more effective antibacterial activity, four new $N^4$-(5-nitro-2-furfurylidene)-$N^1$-substituted sulfanilamides$N^1$-3,4-dimethyl-5-isoxazoyl-$N^4$-5-nitro-2-furfurylidene sulfanilamide, $N^1$-4,6-dimethyl-2-pyrimidyl-$N^4$-5-isoxazoyl-$N^4$-5-nitro-2-furfurylidene sulfanilamide, $N^1$-6-methoxy-3-pyridazinyl-$N^4$-5-nitro-2-furaldehyde with sulfa drugs such as sulfisoxazole, sulfamethazine, sulfamethoxypyridazine, and sulfadimethoxine. All compounds were tested for antibacterial activity in vitro on the following micro-organisms : Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Proteus vulgaris. Each compound exhibited a fair bacteriostatic activity against each microorganism. Above all, sulfisoxazole derivatives showed higher activity than the others. Each compound was most active against Staphylococcus aureus, whereas least active against proteus vulgaris.

• Journal of Pharmaceutical Investigation
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• 제6권2호
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• pp.88-94
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• 1976

This paper attempted to investigate the effect of pretreatment with carbon tetrachloride on absorption, excretion, protein binding, and biological half-life of sulfisoxazol from rats and rabbits. Absorption of sulfisoxazol was found to decrease in severe damage rats, compared with that of normal rats, but in mild rats, absorption of sulfisoxazol was similar to that of nomal rats. Absorption of sulfisoxazol was decreased significantly in severe damage rabbit pretreated with carbon tetrachloride but in mild damage rabbit, absorption of sulfisoxazol was not influenced significantly. Pretreatment with carbon tetrachloride gave the effect on clearance of sulfisoxazol in part but protein binding percent of sulfisoxazol was not influenced by concentration of carbon tetrachloride.

• 미생물학회지
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• 제22권1호
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• pp.41-48
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• 1984

아산 양어장에서 양식되고 있는 뱀장어 (Anguilla japonica)로부터 22주의 병원성 세균을 분리하여 그 생화학적 성질, 혈청학적 관계, 금붕어에 대한 감염성 및 여러 항생물질에 대한 감수성을 시험하였다. 22균주중 14주 (64%)는 Edwardsiella tarda 5주 (23%)는 Aeromonas hydrophila, 기타 3균주(14%)는 Vibrio anguillarum으로 동정되었다. 3가지 분리균중에서 E. tarda는 동일한 혈청형으로 그 분리율 및 금붕어에 대한 감염성이 가장 높았다. 이에 따라 E. tarda가 조사된 양어장의 뱀장어에서 발생하는 세균성 질병의 주 병원체로 판명되었다. 세 분리균주의 균액을 수조에 풀어 금붕어에 접촉시켰을 때 그 감염율은 세 균주 모두 상대적으로 낮았다. 10주의 분리균을 택해 12가지 항생물질에 대해 감수성 검사를 한 결과 하나에서 여섯가지 약제에 대해 저항성을 나타냈으며, 그 중 tetracycline 유도체와 sulfisoxazole에 대한 저항성이 현저하였다.