Method of producing debricine

专利摘要:
1512604 Compositions containing debrycin CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA RT 18 June 1976 [20 June 1975] 25407/76 Heading A5B A pharmaceutical composition comprises debrycin and a pharmaceutically acceptable carrier or diluent wherein (a) at least a portion of the debrycin is in the form of particles of colloidal size, and/or (b) the composition is a solution in aqueous ethanol formulated to precipitate debrycin in colloidal form on contact with body fluids. In example 1 lidocaine is also present.
公开号:SU1338778A3
申请号:SU762374703
申请日:1976-06-18
公开日:1987-09-15
发明作者:Надь Габор；Вираг Шандор；Давид Агоштон；Зилань Тибор；Бартфай Йюдит
申请人:Хиноин Дьедьсер Еш Ведьесети Термекек Дьяра Р.Т. (Инопредприятие)；
IPC主号:

专利说明:

1 13387782
This invention relates to the pharmacist-percentage of active
ticking industry, namely the ingredient in the gel was determined on
to methods for producing antibiotics. Based on microbiological activity.
The aim of the invention is to increase the time. The content of the activity of the target product. Reverse processing method is carried out as follows, h, at dient,%
at once.
Debricin is dissolved in 60-65% -1,213
ethanol solution, from the obtained 3 0,224
its solution is precipitated with ice water5 0,221
in the presence of high molecular weight, the data refer to the original
Limers, or polyethylene glycols, iderbicin mass as 100%.
ethers, or agar-agar, the pitch theoretical value is
tina or methylcellulose. 15 0,200%. Biological definition
Example 1. Debricin gel was carried out in accordance with the method, contains, g: house of a square when used in ca-ethanol 96% of the 50.0 quality of the tested organism, Carbopol-940 1, 2Bacillus subtilis ATCC-6633. The indicated chlorophyll 0.01 gel, which does not contain debricin, was used as the fat-soluble 20 control, it did not debricin 0.2 detect any antibacterial activity in solutions, and Lidocaine 1, used in the tests. Menthol 0.225 Thus, the resulting debris-Triethanolamine 1, 5new gel contains active Ingredient 20 Tween 1.5 debris in the partially dissolved-Distilled and partially colloidal form, to water Up to 100 having a particle size of 0.5 μm, and 0.2 g of debricin is dissolved in 30 ml of 30 the active ingredient is very thin; 62.5% (by volume) of ethanol is determined.
temperature not exceeding 40 ° SP2. Prepare ras- (solution 1). I, 2 g carbopol-940 soluble tablets, having the following
pendiruyut in 4 g of isoadipate and sub-composition, g: debricin 4; urea 96.
are exposed to vacuum for half-35 debricin dissolved in the mixture
hours dp in order to remove air ethanol and water containing 62.5% (according to
(solution 2). Lidocaine is dissolved in a volume of ethanol. Drink a solution
the residual amount of ethanol and water in small portions to urea. Next (solution 3). Chlorophyll, the soluble portion of the solution is poured out only in fats, and menthol is dissolved in Twi-40 K after the preceding 20 (solution 4). The solutions and solution solution evaporate. Granules
The readers, if necessary, are filtered. Compressed into tablets in the usual way.
Solutions 1 and 3 are mixed. After this, the resulting tablets are easily soluble.
solution 2 is poured at constant water, the solution of the colloidal debi is vigorously stirred, the specified ricin is 45, is stable,
the mixture and this mixture is vacuum. The percentage of active
clearing for half an hour for the ingredient soluble tablets, podaerating. After standing for the amount thus obtained, it is determined.
24 hours solution 4 is added with stirring after heating the tablets at 100 ° C.
pshvanii. At the time of addition, 50 microbial-based for 5 hours should avoid the presence of air. Mixed activity (example 1).
neutralize with triethanolamine while using the term content of permutational stirring. The resulting reverse Inglegel is stored in sealed vessels, h, dienta,%
dah at 100 ° C for 5 h and then55 at the SO with
still for a month at -5 C.1 98.1
No organolep-3 was observed 95.1
tic changes.5 92.6
These data indicate that the tablets obtained in this way are resistant to thermal effects.
PRI me R 3. Prepare an aerosol solution suitable for treating wounds, having the following composition, g Debricin 0.10
Film-forming
agent 1.50
Aqueous ethanol
(62.5% by volume) 48.40 Propellent50.0
0.10 g of debricin is dissolved in 40 ml of a mixture of ethanol and water containing 62.5% (by volume) of ethanol upon heating. The temperature of the solution should not exceed 40 ° C. After cooling, the film-forming suspension (e.g., polyvinylpyrrolidone, polyvinyl alcohol) is dissolved at 20-25 ° C and the solution is added to 50.0 g with 62.5% (by volume) aqueous ethanol. The solution is filled into aerosol vessels equipped with valves with a propellant, and each vessel is compressed in the usual way.
The solution thus obtained is subjected to heat treatment at. The content of the active ingredient in the solution is determined by the microbiological method (Example 1). Thermal treatment was carried out in the absence of a propellant. Time of thermal treatment content, h, dient,% at 100 s
1 0,203
30,203
50,201
PRI me R 4. Prepare eye drops of the following composition, g: Debricin0.02
Carbonate
rub 18,0
Aqueous solvent510, 0 Oh, 1% phenomer solution 15, 0 Distilled
water suitable
for injection purposes up to 1000.0
Freshly distilled and still warm
4.0 g of methylcellulose and 3.5 g of sodium chloride are dissolved in water, respectively, and both solutions are combined. The solution thus obtained is made up to 510 g with distilled water, after which it is filtered through a glass filter WG-3. To 510 g of the solution was added 15.1 g of a 0.1% phenomer solution as a preservative agent. The solution is heated at the boiling point of water for one hour, after which it is cooled to the temperature of melting ice. Debricin is added to boiling distilled water. The debricin solution is heated to boiling for 5-10 minutes, after which the still hot solution is cooled, poured into a viscous solvent and cooled to ambient temperature. The acidic sodium carbonate is dissolved in the resulting solution, which is then brought to the desired volume with sterilized distilled water. The solution is filtered through a glass filter WG-3 and the thus-obtained eye drops are filled with fibers free from the flask. The composition is sterilized
at 100 ° C for an hour.
I
PRI me R 5. Prepare a heterocolloidal solution having the following composition:
Debricin1,0
Aqueous ethanol 62.5%
(by volume) 20.0
Water100.0
1 g of debricin is dissolved in 20 g of 62.5% (by volume) aqueous ethanol under heating until boiling, after which the solution is quickly mixed with 79.0 g of ice water. A dispersion is obtained that includes debricin in a state of extremely fine distribution. Such a dispersion can also be obtained by preparing a hot saturated solution with ethanol having a concentration of 60 or 65% (by volume).
PRI me R 6. Prepare an ointment of the following composition: Heterocolloidal Debritsinovy solution prepared according to example 5, ml 10.0 Stearic Sor-box3,6
ten
15
25
Liquid Paraffin 3,6 Cetylstearin alcohol10,80
White petrolatum 18.0 Propyl-p-hydroxybenzoate0.054
Methyl-p-hydroxybenzoate 0, 1 26
Highly concentrated alcohol 2.93 Lidocaine hydrochloride1, 00 Distilled water Up to 100.00 The ointment is prepared in a known manner from sorbobethene-stearate, liquid paraffin, cetylstearic alcohol, white petrolatum, propyl-p-hydroxybenzoate, methyl-p- hydroxybenzoate, concentrated stirred alcohol and distilled water. To this ointment is added in small portions a solution of lidocaine hydrochloride dissolved in a heterocolloidal debricin solution. The ointment is introduced into the mill with three rollers, spread on a mitral plate or injected into tubes. The ointment thus obtained may be reduced by water.
Example. Prepare a composition for spray (spray) of the following composition:
Heterocolloidal debricin solution prepared in accordance with Example 5 2.0 Foaming agent 3.0
Propylene glycol 85, O Propellant10.0
The foaming agent, preferably Pollavax, is dissolved in propylene glycol, when heated, the solution is allowed to cool and a heterrcolloidal debricin solution is added. The spray solution is filled with aerosol cans. Debricin is dissolved in propylene glycol at 80-90 ° C, the foaming agent, for example Pollavax, is dissolved at 40-50 ° C. The resulting solution is filled into aerosol cans according to methods known in aerosol technology.
Example 8. Preparing eye drops of the following composition, g: Heterocolloidal debris again
1338778
the solution obtained in accordance with example 52,0
Cholesterol25,0
Sterile castor oil Up to 1000.0 Cholesterol is added to castor oil filtered through a fiber-free WG-3 glass filter and the system is heated at
constant stirring at 140 ° C
thirty
40
45
50
all cholesterol is not
until
dissolved, heating is carried out for 3 hours. To the cooled solution with vigorous stirring is added a heterocolloidal debricin solution. The eye drops thus obtained fill the glass vessels.
PRI me R 9. Prepare eye ointment of the following composition, g: Heterocolloidal debrichin solution prepared in accordance with example 52.0
Beeswax 300.0 Cholesterol25.0
Sterile castor oil. Up to 1000.0 A mixture of melted beeswax and cholesterol is added to castor oil, filtered through a fiber-free WG-3 glass filter, with constant stirring. The mixture is heated at 140 ° C with constant stirring for at least 3 hours. To the cooled ointment, the heterocolloidal debricin solution is added while stirring the mixture is filled with sterile tubes.
Example 10. Stock solution for making liniment.
1.0 g of debricin is dissolved in 500 ml of ethanol (60% by volume). The dissolution was promoted by heating the mixture to 50 ° C. After cooling, the solution was brought to its original volume.
10 ml of this stock solution was diluted to 500 ml with a 30-40% (by volume) ethanol solution.
Raw cotton or sterile cotton fabric impregnated with this
solution and used as liniment in the treatment of fresh burns or as
55
constant stirring at 140 ° C
five
0
0
0
five
0
all cholesterol is not
until
dissolved, heating is carried out for 3 hours. To the cooled solution with vigorous stirring is added a heterocolloidal debricin solution. The eye drops thus obtained fill the glass vessels.
PRI me R 9. Prepare eye ointment of the following composition, g: Heterocolloidal debrichin solution prepared in accordance with example 52.0
Beeswax 300.0 Cholesterol25.0
Sterile castor oil. Up to 1000.0 A mixture of melted beeswax and cholesterol is added to castor oil, filtered through a fiber-free WG-3 glass filter, with constant stirring. The mixture is heated at 140 ° C with constant stirring for at least 3 hours. To the cooled ointment, the heterocolloidal debricin solution is added while stirring the mixture is filled with sterile tubes.
Example 10. Stock solution for making liniment.
1.0 g of debricin is dissolved in 500 ml of ethanol (60% by volume). The dissolution was promoted by heating the mixture to 50 ° C. After cooling, the solution was brought to its original volume.
10 ml of this stock solution was diluted to 500 ml with a 30-40% (by volume) ethanol solution.
Raw cotton or sterile cotton fabric impregnated with this
solution and used as liniment in the treatment of fresh burns or as
five
24-hour wet dressing.
Example II Anesthesia solution for epithelial lesions.
0.025 g of debricin is dissolved in 500 ml of 65% (by volume) ethanol solution at a temperature below, after cooling it is brought to its original volume; or 10.0 g of polyvinyl jirromidone is dissolved in 500 ml of a 65% by volume ethanol solution at a temperature below 50 ° C, after cooling the solution is brought to its original volume.
The method for producing debricin is based on the fact that debricin is capable of exhibiting suitable activity in tissue fluids on the skin surface at a concentration of 10-20 µg / ml, and during treatment, a smaller amount of the active ingredient is capable of providing a higher level of local concentration.
five
0
therefore, the therapeutic efficacy of the composition of the street is common.
The concentration of the active ingredient in the proposed compositions is lower than the concentration of the previously known formulations, but its therapeutic activity is higher.

权利要求:
Claims (1)
[1]
Invention Formula
The method of producing Debricin by dissolving it, which is different from that, in order to increase the activity of the target product, the debricin is dissolved in a 60-65% ethanol solution, precipitated from the resulting solution with ice water in the presence of high molecular weight polymers, or polyethylene glycols, or ethers, or agar-agar, pectin, or methylcellulose.

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引用文献:

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US4404189A|1981-01-21|1983-09-13|Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.|Synergistic antimicrobial compositions|

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JPH0140809B2|1981-02-02|1989-08-31|Kinoin Giogisuzeru Esu Begiesuzechi Terumekeku Giara Ruto|

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US5217707A|1988-06-16|1993-06-08|Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.|Pharmaceutical composition and process for the preparation thereof|

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HU203476B|1988-06-16|1991-08-28|Chinoin Gyogyszer Es Vegyeszet|Process for producing stabile, aquous suspoemulsion containing primicin and suspoemulsionic pharmaceutical composition containing them as active component|

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HU207222B|1990-02-15|1993-03-29|Chinoin Gyogyszer Es Vegyeszet|Process for producing eyedrops containing primycin|

法律状态:

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