Sample records for dibekacin
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Namiki, N; Yokoyama, H; Moriya, K; Fukuda, M; Takashima, T; Uchida, Y; Yuasa, H; Kanaya, Y
1986-11-01
For the purpose of preventing suppuration of wounds of the oral cavity and throat, we attempted to develop a viscous solution of dibekacin sulfate (DKB) as a suitable medication. Solutions of different viscosity and antibacterial potency were prepared by mixing DKB, sodium carboxymethyl cellulose (CMC-Na), and water in varying proportions. Studies were then performed to ascertain relationships between the concentration of CMC-Na pH and viscosity, and between the viscosity and diffusion of DKB. The concentration of CMC-Na giving rise to optimal clinical efficacy was determined, and the concentration of DKB necessary for clinical treatment was estimated on the basis of the ionic binding constant between DKB and CMC-Na. As a result, the optimum CMC-Na concentration was found to be 2%, while the optimum DKB concentration was estimated to be 100 micrograms/ml.
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Effect of ophthalmic solution components on acrylic intraocular lenses.
Ayaki, Masahiko; Nishihara, Hitoshi; Yaguchi, Shigeo; Koide, Ryohei
2007-01-01
To investigate the effect of ophthalmic solution components on the surface of acrylic intraocular lenses (IOLs). Department of Opthalmology, Showa University School of Medicine. Measurement of the contact angles of ophthalmic solutions on 3 acrylic IOLs was performed. The solutions were diclofenac sodium (Diclod), bromfenac sodium (Bronuck), betamethasone phosphate (Rinderon), dibekacin sulfate (Panimycin), polysorbate 80 (Tween 20), benzalkonium chloride, chlorobutanol, methylparahydroxybenzoate, and propylparahydroxybenzoate. The IOLs were incubated at 35 degrees C for 2 weeks in undiluted ophthalmic solutions and in 1:10 dilutions of ophthalmic solution components. The IOLs were sectioned and observed by scanning electron microscopy. The contact angle of Diclod and Bronuck solutions was the smallest. The contact angle of Rinderon and Panimycin was similar to that of distilled water. Scanning electron microscopy examination of IOLs incubated in ophthalmic solution components showed intralenticular changes. The IOLs immersed in ophthalmic solutions did not show any change, even after extended incubation. The chemical components of ophthalmic solutions, such as surfactants and solvents, permeate acrylic IOLs, suggesting the potential for long-term adverse effects of eyedrops in pseudophakic eyes.
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Kondo, S
1994-06-01
Our studies on the resistance mechanisms and chemical modifications of aminoglycoside antibiotics led to the synthesis of arbekacin (ABK), which was refractory to most aminoglycoside-modifying enzymes in resistant bacteria. In 1990, ABK was launched into clinical uses in Japan as a chemotherapeutic agent for the treatment of infections caused by methicillin-resistant Staphylococcus aureus (MRSA). By 1993 only a few MRSA strains moderately resistant to ABK (MIC, 6.25-12.5 micrograms/ml) had clinically been isolated. ABK was modified by the reaction with an excess of an enzyme preparation extracted from an ABK-resistant strain (12.5 micrograms/ml) and three inactivated products were produced, consisting mainly of ABK 2''-phosphate along with small amounts of 6'-N-acetyl-ABK and the doubly modified ABK. Based on these results, replacement of the 2''-hydroxyl by amino group in dibekacin (DKB) or in ABK was designed to obtain potent active derivatives against MRSA. Conversion of the 2''-hydroxyl group by DMSO-DCC oxidation followed by reductive amination with NH4OAc-NaBH3CN gave 2''-amino-2''-deoxy-DKB (D1) and -ABK (A1). Their 5-deoxy (D2 and A2), 5-epifluoro (D3 and A3) and 5-epiamino (D4 and A4) derivatives were also synthesized. All 2''-amino-2''-deoxy-ABK derivatives (A1, A2, A3 and A4) showed excellent activities against MRSA and Gram-negative bacteria, as expected. Among them, A4 having low acute toxicity and nephrotoxicity was selected as a new candidate for anti-MRSA agent.