Agent with antimicrobial and regenerating action

 

(57) Abstract:

The invention relates to medicine and concerns the establishment of a drug for the treatment of purulent skin infections. The invention lies in the fact that the product contains fuzidin sodium, methyluracil, sodium, peruserdictionary, polyvinylpyrrolidone 126002700, lanolin, vaseline, distilled water at a certain ratio of components. The invention provides a drug with a high therapeutic effect without side effects. 3 tab., 1 Il.

The invention relates to medicine, can be used in the production of pharmaceuticals and concerns the establishment of a drug for the treatment of purulent skin infections.

Well-known domestic preparations for the treatment of suppurative skin infections - gel "Fuzidin" 2% containing acid guideway and gel "Prefusion" containing acid guideway, prednisolone and zinc oxide.

However, this form of medicinal product - a gel in the application forms on the skin thin film, which has a protective effect for minor wounds, at the same time painfully pulls tissue impedes the outflow of pus in the case of serious skin lesions, increasing the duration of treatment.

what is burns III-IV degree, bedsores, ulcers.

For this group of diseases the effect of the ointment should be directed to the upper layers of the skin and soft tissues, i.e., the ointment should not have a high resorption. Developed the drug has antibacterial and regenerating effect and contains as active substance fuzidin sodium, as a wound healing agent contains methyluracil. Fat basis are petrolatum and lanolin, in addition, the product contains sodium, peruserdictionary, polyvinylpyrrolidone and distilled water in the following ratio, wt.%:

Fuzidin-sodium - 2,0

Methyluracil - 1,0

Sodium, peruserdictionary - 0,05

Polyvinylpyrrolidone 126002700 - 0,5

Lanolin - 40,0

Vaseline medical - 56,25

Distilled water - Up to 100.0

Clinical results of external application of fuzidinu described in the literature [3-8] , it exhibits high specific activity against staphylococci, meningococci, gonococci, and more effective in the treatment of purulent infections [1-2].

Antimicrobial activity of fuzidinu depends on pH, the optimum antimicrobial effect is observed at pH 6. To a much lesser stepne more than 2-3 times. Fuzidin shows high activity in the presence of a large number of pus, it has low toxicity [2], when applied externally, rarely gives a negative reaction.

The optimum concentration of the active ingredient in the drug is determined experimentally in terms of delay zones of growth the culture test You. Mykoides HB and is 2 g per 100 g of ointment. Further increase in concentration does not enhance the antibacterial effect [drawing].

Methyluracil entered in the drug as a wound-healing component for slow-healing skin lesions (e.g., burn wounds).

PVP is an agent that increases the stability of the active substance and enhancing the transdermal absorption.

Sodium, peruserdictionary used as antioxidant, preventing the oxidation of organic substances.

The technological process of preparation of ointments as follows.

Fat basis, consisting of lanolin and vaseline, is divided into 4 parts, three parts, in the molten state, separately prepare suspensions methyluracil, PVP, fuzidin-sodium with a sodium philosemitism and gradually introduce them to the rest of chastity agitators.

Example 3 (table. 1)

Prepare a melt of 40 g of lanolin and 56,25 g vaseline, divide it into 4 parts.

In an enamelled vessel 0.2 g PVP mixed with 0.2 g distilled water (602)oC and maintained at this temperature for 2 hours with periodic mixing. Then under stirring download solution of PVP in part molten at a temperature (602)oWith ointment bases and stirred for 10 min.

2 g of fuzidinu sodium, 1 g methyluracil, 0.05 sodium preservestacktrace sift and alternately at a temperature of (452)oC is mixed with parts of molten fat phase. The resulting suspension shredded in a dispersion mill to obtain particles less than 60 microns.

In the apparatus loads the remaining portion of the fatty basis, stirred for 5-10 min and the temperature (602)oC and stirring gradually introducing her first suspension PVP, then at a temperature of (452)oWith load suspension methyluracil and fuzidin-sodium with a sodium philosemitism, cooled with stirring to room temperature.

The resulting ointment is a homogeneous mass of yellowish color, pleasant and easy superimposed on the affected areas of your skin.

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The effectiveness of the claimed drug was studied in the treatment of purulent wounds in animals. The experiment was performed at 80 outbred rats-males, who were divided into 5 groups of 16 animals each.

In the first group (control) effects on the wound had been made, in 2-5 groups once daily applied the ointment composition is shown in table. 1, examples 1-4 at a dose of 0.5 g/cm2.

Daily were measured area of the wound was observed the terms of its purification, reduction and disappearance otolaryngolo infiltrate, the appearance of granulation and epithelialization to complete healing.

The results presented in table. 3 gives a comparative description of wound healing depending on the concentration of methyluracil.

Significantly marked acceleration of epithelialization in effect on the wound variants ointments containing methyluracil. The optimal concentration of methyluracil 1% (example 3), a lower concentration (examples 1, 2) increases the period of epithelialization, increased concentration (example 4) does not lead to significant improvements in the efficiency of ointment.

The results of pharmacological studies proved the high healing efficiency is thus the invention makes it possible to organize the production of stable highly effective drug for the treatment of purulent skin infections.

Sources of information

1. Fuzidin and its properties. "Antibiotics", 1967, 6, S. 451-454. Auth. N. M Vihrova, M. A. Petrova, I. P. Fomin, S. M. Navashin.

2. Bochkov, M. L., Storozhev I. A., Berezin, E. K. the pharmacology of fuzidinu. "Antibiotics", 1971, 3, S. 216-217.

3. Queen Of The Century, Navashin S. M., Semagina N. G. Absorption, distribution and excretion of fuzidinu in animals. "Antibiotics", 1971, 10, c.926-928.

4. Saxe, E. F. , Queen of the Century, Navashin S. M. Effectiveness of fuzidinu in surgical patients. "Antibiotics", 1972, 12, S. 1094-1098.

5. Ritchie, I. C: Clin. Trials J. 1966 3:529-531.

6. Sobye, P.: Ugeskr. Lager 1966 128:204-207.

7. Vickers, C. F. H.: Brit. J. Derm 1969 81:902-908.

8. Coodwin F. W. et al. Fusidic acid in staphyloccocal intection. - "Lancet, 1973, 2, p.1504-1505.

Drug for the treatment of purulent skin infections, containing fuzidin-sodium based and fillers, characterized in that it is made in the form of ointment with a base of lanolin and vaseline, as filler contains sodium, peruserdictionary and polyvinylpyrrolidone 126002700 and further comprises methyluracil in the following ratio, wt. %:

Fuzidin-sodium - 2

Methyluracil - 1

Sodium, peruserdictionary - 0,05

Polyvinylpyrrolidone 126002700 - 0,5

Lanolin - 40



 

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