前苏联专利SU976837A3 Method of producing substance having antibiotic action

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优先权

专利摘要:
This invention relates to color-stabilized aqueous parenteral antibiotic compositions of a parenterally acceptable salt of an aminoglycoside antibacterial agent, having a pyranose ring which is unsaturated between the 4' and 5' positions and which contains an aminoalkyl substituent at the 5' position and to a process for their preparation. Such stable compositions have an initial pH of 5.0 - 7.0. The preferred pH range is 5.8 - 6.8 and the most preferred range is 6.2 - 6.5. The pH may be adjusted either by adding NaOh to the solution or, preferably, by including certain sulfite salts as antioxidants in such quantities that the desired pH is achieved.
公开号:SU976837A3
申请号:SU792709256
申请日:1979-01-15
公开日:1982-11-23
发明作者:Эли Розенкрантц Бернард；Исаак Стюпэк Эллиот
申请人:Шерико Лтд (Фирма)；
IPC主号:

专利说明:

397 glycerin, thiosorbitol, thioglycolic acid and cysteine hydrochloride. The pH of the substance is adjusted to the required limits by the addition of a suitable base, for example sodium hydroxide, or a suitable acid, for example, hydrochloric acid. Substances with an antibiotic effect may contain 1050 mg / ml sisomycin sulfate or 10100 mg / ml netilmicin sulfate or 10-50 mg / ml 5 episizomycin. As usual additives, soder. Contaminating agents can be: servant agents - parabens, zilic alcohol, electrolytes - sodium chloride and sodium sulfate, chelating agent - disodium salt with ethylenediamine of tetraacetic acid. The stability of the drug, having a pH of 6.2-6.5, consider an example. Two solutions are prepared by mixing which contain 250 mg of netilmicin sulphate in 5 ml of water each and the pH of the preparation is adjusted to 6.5 with sodium hydroxide. The solutions are fed into ampoules, and one ampoule is sealed in the nitrogen atmosphere (ampoule 1), and the other in the presence of air (ampoule). After storing the ampoules at 75 ° C for one week, the pH of the preparations is measured. At the same time, it is found that the pH of the substance in ampoule 1 was 6.5, while the pH of the preparation in ampoule 2 decreased to 6.2. The commercial preparation of syzomycin sulfate, intended for injection, has the following composition, mg / ml: Sisomycin sulfate 50 , 0 sodium metabisulfate. 3) Sodium chloride Netilparaben Disodium salt of ethylenediaminetetraacetic acid Distilled water, Up to 1 ml of p11 of this preparation is 3.7-3.9, and the storage stability is. , 18 months at 30 ° C. R | RIMER 1-5. the preparation, the composition of the substance is presented in the table, is prepared in the amount of 50 liters as follows. In a stainless steel boiler; With a casing, 35 liters of distilled water is supplied, which is heated to stirring vigorously, methylparaben and propylparaben are added. After complete dissolution of the parabens, the solution is cooled to 25-30 ° C, washed with nitrogen and the subsequent operations are carried out in a nitrogen atmosphere. Ethylenediaminetetraacetic acid disodium salt and / or sodium chloride, and / or sodium sulfite, -and / or sodium sulfonate and sisomycin or netilmicin sulfate are successively dissolved in quantities in amounts consistent with the content indicated in the table. The resulting solution is mixed with distilled water to obtain 50 liters and stirred until homogeneous, after which the pH of the solution is measured. The solution of each example has the pH indicated by IB Table, with the exception of the preparation of Example 1, whose pH is increased by adding sodium hydroxide solution from 3.9 to, the solution is passed through a bacteria-retaining filter under sterile conditions and the filtrate is fed into the reservoir. The preparation is then supplied to sterile pyrogen-free containers, such as ampoules under aseptic conditions, which are sealed. Examples 6-10, 1, and 19. Examples 1-5 are repeated, with the difference that, after being supplied with distilled water to the boiler 35, they are heated to .5-30 ° C, washed with nitrogen and, with stirring, the additives are dissolved in the specified sequence in a nitrogen atmosphere. The composition of the prepared preparations is presented in the table.
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权利要求:
Claims (1)
[1]
vD Example 20. Example 1 is repeated with the difference that the pH of the preparation is increased from 3.9 to 5.0 and 7.0 by addition of sodium liquor Example 21. Example 5 is used with the difference that the pH of the preparation is increased from 6.8 to 7.0 by the addition of sodium hydroxide and lower the pH from 6.8 to 5.0 by the addition of hydrochloric acid. The proposed method allows to maintain high stability during storage of 8 for up to 3 months at 30 ° C. The invention of the method of obtaining a substance having an antibiotic effect, pu97 7 mixing the amino glucoside derivative with distilled water, preserving and chelating agents, characterized in that, in order to preserve the stability of the target product during storage, salt 10 -50 mg / ml or netilmicin sulfate at a concentration of 10-100 mg / ml, or 5 episizomycin at a concentration of 10-50 mg / ml and mixed with sulfite salt at a concentration of 2.0, 0 mg / ml with a mixture of sulfite salts in to ntsent-. radios 3.2-3.8 mg / ml and further the target product is adjusted to pH 5.0-7.0. Sources of information taken into account in the examination 1. US patent fP 3832286, cl. 195/80, 1971..

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同族专利:

公开号 | 公开日

CA1129344A|1982-08-10|

FI790086A|1979-07-17|

EP0003150B1|1981-11-25|

DK14579A|1979-07-17|

AR223967A1|1981-10-15|

ZA7962B|1979-12-27|

FI64287B|1983-07-29|

PH18571A|1985-08-12|

IL56409D0|1979-03-12|

AT364715B|1981-11-10|

JPS54100346A|1979-08-08|

ATA20479A|1981-04-15|

IE790045L|1979-07-16|

IE48254B1|1984-11-14|

AU4332079A|1979-07-26|

PL119296B1|1981-12-31|

PT69063A|1979-02-01|

DK155306C|1989-08-28|

DD141410A5|1980-04-30|

NZ189363A|1984-07-06|

ES476754A1|1979-12-16|

NO790085L|1979-07-17|

GR73655B|1984-03-27|

NO153876C|1989-08-22|

AU524288B2|1982-09-09|

MY8500050A|1985-12-31|

US4223022A|1980-09-16|

JPS5914447B2|1984-04-04|

IL56409A|1981-09-13|

EP0003150A1|1979-07-25|

PL212809A1|1980-02-11|

DK155306B|1989-03-28|

NO153876B|1986-03-03|

DE2961370D1|1982-01-28|

BG32560A3|1982-08-16|

引用文献:

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JPS4911403B1|1970-12-29|1974-03-16|

US3832286A|1971-02-03|1974-08-27|Schering Corp|Sisomicin and methods for its production|

US3995635A|1971-09-09|1976-12-07|Alza Corporation|Ocular insert|

US3956068A|1972-07-14|1976-05-11|Schering Corporation|Antibiotic G-52 and method for the production thereof|

GB1405283A|1972-08-17|1975-09-10|Scherico Ltd|Antibiotics and processes for their preparation|

US3880828A|1973-02-23|1975-04-29|Schering Corp|Antibiotics 66-40B and 66-40D from micromonospora inyoensis|

US3898330A|1973-08-01|1975-08-05|Squibb & Sons Inc|Corticosteroid phosphate salts/neomycin sulfate ophthalmic|

US3962429A|1973-08-01|1976-06-08|Chugai Seiyaku Kabushiki Kaisha|Method for reducing side effects of aminoglycoside antibiotics and composition therefor|

US3944064A|1973-10-26|1976-03-16|Alza Corporation|Self-monitored device for releasing agent at functional rate|

US4011390A|1974-02-15|1977-03-08|Schering-Plough Corporation|Semi-synthetic aminocyclitol aminoglycoside antibiotics and methods for the preparation thereof|

US4002742A|1974-03-19|1977-01-11|Schering Corporation|1-N-alkyl-4,6-di--1,3-diaminocyclitols, methods for their manufacture, methods for their use as antibacterial agents, and compositions useful therefor|

US4009328A|1975-05-02|1977-02-22|Schering Corporation|Aminoglycoside 66-40C, method for its manufacture, method for its use as an intermediate in the preparation of known antibiotics and novel antibacterials|

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法律状态:

优先权:

申请号 | 申请日 | 专利标题

US05/869,741|US4223022A|1978-01-16|1978-01-16|Stabilized aminoglycoside antibiotic formulations|

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