Pharmaceutical composition

 

(57) Abstract:

Pharmaceutical composition for treating and alleviating symptoms of weliwita and vulvovaginitis in accordance with the invention contains, wt%: 0,05 - 0,5 folic acid, 0.25 to 2.5 panthenol and/or 0.15 - 1.5 allantoin, 0.75 to 7.5 hydrolyzed protein or hydrolyzed casein, 3,0 - 15,0 lactose or dextrose, 0,25 - 2,5 lactic acid, 0.25 to 2.5 magnesium sulfate and 0.75 - 7.5 sodium chloride or ammonium chloride. Provides quick absorption. 1 C.p. f-crystals, 7 PL.

The present invention relates to new biologically active pharmaceutical composition, its preparation and use for the treatment of symptoms of weliwita and candidiasis genital Beli).

The mentioned symptoms and their treatment raises a number of problems since the restoration of damage to health caused by disruption of the vagina, due to the rapid reconstruction of or ability to quickly recreate epithelial tissues, not just treating the symptoms of the disease. The nature of the treatment of genital whiter discussed by Dr. S. Gardo two article entitled: "The Causes and Treatment of Genital Fluor" (Causes and treatment of genital whiter) /Magyar Noorvosok Lapja (Journal of Hungarian Gynecologists) 54, pp. 7-12 (1991)/ and theatment of G is the corresponding normal microflora lactobacilli in the vagina contributes to the suppression of symptoms, however, there are various possibilities and ways to restore the normal state, and their effectiveness cannot equally be guaranteed in every case.

In the patent Hungary N 190732 describes about a hundred ingredients, about thirty combinations which are expected to prepare to restore the normal microflora of the vagina. These combinations are aimed at achieving this result, as the increase in its infancy, the number of lactobacilli or limitation of pathogenic or pseudophoenix microorganisms, respectively, when testing some combinations in some cases the suppression of symptoms sometimes was long or the combination did not show sufficient activity.

Ensure suction is also an important factor in the use of therapeutic products. According to experience, traditional ointments and emulsions of the type water-in-oil and oil-in-water and water or alcohol (ethanol) solutions do not help or even hinder obtaining the necessary results in treating symptoms of velvita.

The objective of the invention is the manufacture of a pharmaceutical composition, which is used to palliate symptoms vulvadynia and/or irritated.

In addition, the object of the invention is to achieve stabilization, as well as providing rapid absorption of the composition.

The task is solved by providing a pharmaceutical composition for the treatment of symptoms of weliwita and vulvovaginitis, containing a mixture of active ingredient and pharmaceutically acceptable carriers and/or auxiliary substances, which according to the invention as a mixture of active ingredients contains folic acid, panthenol and/or allantoin, hydrolyzed protein or hydrolyzed casein, lactose or dextrose, lactic acid, magnesium sulfate and sodium chloride or ammonium chloride in the following ratio, wt.%:

Folic acid - 0,05-0,5

Panthenol - 0,25-2,5

and/or Allantoin - 0,15-1,5

Hydrolyzed protein or hydrolyzed casein - 0,75-7,5

Lactose or dextrose - 3,0-15,0

Lactic acid - 0,25-2,5

Magnesium sulfate - 0,25-2,5

Sodium chloride or ammonium chloride - 0,75-7,5

Pharmaceutically acceptable carriers and/or excipients - Rest

Preferred as pharmaceutically acceptable carriers it contains polyoxyethyleneglycol and an ester of fatty acid and polyoxyethylenesorbitan.

Suppositories containing 0.05-0.5. % folic acid, 0.8 to 1.5 wt.% protein hydrolysate, 8-14 wt.% lactose, 1.0 to 2.0 wt.% lactic acid, 1.0 to 2.1 wt.% magnesium sulfate, 2.0 to 4.0 wt.% sodium chloride or ammonium chloride, 60,0-to 68.0 wt.% polyoxyethyleneglycol 1540 and 10-15 wt.% carboxihemoglobin. Almost suppositories weigh 3.5 to 4.0 g each.

Ointment containing 0.2 wt.% d-panthenol, 0.75 to 1.5 wt.% hydrolyzed protein, 7-12,0 wt. % lactose, 0.5 to 2.0 wt.% lactic acid, 0.1 to 0.5 wt.% magnesium sulfate, the 6.0-10.0 wt.% carboxihemoglobin, 25-70,0 wt.% of polyoxyethylene 400 and 0.5 of 51.0 wt.% polio is olidata protein of 5.0-10.0 wt.% lactose, 0.5 to 1.0 wt.% lactic acid, 0.3 to 0.5 wt.% magnesium sulfate, 2.0 to 3.0 wt.% sodium chloride, 44,5-to 50.0 wt. % of polyoxyethylene 400, 7.5 to 12.0 wt.% carboxihemoglobin, optional polyoxyethylene 4000 or 1540, as well as 19,0-33% by weight of distilled water.

These compositions are stable. As evidenced by biological experiments, they alleviate the symptoms of most of the different types of vaginitis and weliwita and contribute to the restoration or suppression of symptoms. An important advantage of the compositions is that their use does not require any research, depending on the condition of the patient, as they can usually be used in the above formulations.

Thus, the compositions containing the ingredients corresponding to the invention, useful for normalization of the vaginal flora to restore damaged microflora, to restore and training of epithelial tissues, and to provide preventive (prophylactic) protection against vaginal infections.

Among the types of vitamin B folic acid was the most effective, but the determination of their appropriate doses (0.001 to 0.1 g for each dose) or concentrations (0,03-0,3%), respectively t">

According to the conclusions of the authors, hydrolyzed protein and hydrolyzed casein are equally suitable nitrogen sources, as in all cases be ensured stability. Suitable sources of carbon are lactose and in some cases dextrose.

The presence of certain ions and trace elements in the "composition" is also significant. Among the cations Na+, NH+4and Hg2+and among anions Cl-and SO2-were the most important. Accordingly, we used the sodium chloride and/or ammonium chloride, and magnesium sulfate. A very important adjustment of the pH (2-3,5) and the optimal concentrations (0.1 to 0.5%) products. First of all, d-panthenol, allantoin and folic acid are suitable for the treatment of symptoms of irritation occurring as a result of diseases and epithelial damage of various degrees: they can recover the water balance of sugars and human tissue. Lactic acid is convenient to obtain the tightening action.

Activity composition largely depends on the composition and selection of the preferred pharmaceutical forms. The preferred form is a suppository, a gel, a solution, or Aer is civali physico-chemical and microbiological stability of combinations of active ingredients more than expected.

According to experimental data of the authors, the advantage suppozitornyj mass (base) containing polyoxyethylene and polyoxyethylene esters(s) fatty acids, consisted of the following:

- greater absorption of water and powdered substances,

- creating a desired consistency by mixing combinations with different molecular weights, and

- improved stability weight (base) of the suppository and the active ingredients included in them.

As examples of esters of polyoxyethylene we can mention polyoxyethylenated (MirjR), esters sorbitan, for example, sorbitanoleat (Span 20Ror esters aroxetine, such as carboxitherapy (Tween 20R), as well as carbocationic (Tween 90R).

The most effective was the combination listed in the table. 1.

Weight (base) suppository increased the activity of biologically active substances, as hygroscopicity mass (Foundation) is a factor that increases the action, thanks to which assistance is provided to the complete dissolution of the active ingredients through increased vaginal discharge. In addition, the other advantage of mass (Foundation) of the suppository is that it makes it possible to maintain a stable microbiologically unstable system.

The gel form provides advantages similar to the advantages of suppositories. One sample from two different gels contains about 50% of polyoxyethyleneglycol 1540 and 30-35% of polyoxyethyleneglycol 400, while the other sample contains polyoxyethyleneglycol 400 in its main part, and only 1-2% of polyoxyethyleneglycol 1540 (Macrogel).

For preparation of compositions of the specified composition in the form of solutions, which can be in the form of a mechanical aerosol ingredients taken in quantities that depend on the total mass dissolved in the aqueous phase, i.e. polyoxyethyleneglycol 400 and water, followed by the addition of polyoxyethyleneglycol 1540 and 4000.

The invention is illustrated in detail by the following examples.

Example 1. Suppository (see tab. 2)

Suppositories prepared as follows.

After mixing folic acid with an adequate amount of lactose remaining lactose, magnesium sulfate and sodium chloride successively added with stirring. Hydrolyzed protein is immediately mixed with the powder mixture to prepare a suspension. At the same time after melting the floor/SUP>C in the melt is stirred into lactic acid, the powder mixture is suspended in the liquid base of the suppository containing lactic acid, then the mass is homogenized in a mill to form colloid. At a temperature of approximately 55oC mass is poured into a chilled form.

Example 2. Ointment (see tab. 3)

After cooling to about 50oC melt polyoxyethyleneglycol and polyoxyethyleneglycol esters of fatty acids, optional condensate hydrogenated castor oil with ethylene oxide can first be dissolved in the melt, panthenol, and after cooling, the mass is still up to 40-45oC suspended in her powder substance, respectively milled (to a size smaller than the sieve mesh VI) and pre-mixed with each other. Finally there stirred into lactic acid and the system is stirred until complete cooling.

Example 3. The solution or aerosol (see tab. 4)

Powder the ingredients and panthenol consistently portions add in distilled water, heated to a temperature of about 60oC. Simultaneously melt the ingredients of the fatty phase. The two phases are mixed at a temperature of about 60oC and then stirred until cooling of the mixture.

A comprehensive study was extended to the so-called investigation of the purity of the vagina, the cultivation of bacteria and fungi, as well as on colposcopic and cytological samples, bimanual pelvic examination, determination of pH values and the assessment of subjective complaints. It was found a significant change under the effect of the treatment in the pH values of the studied persons Changes in the cervix, vagina and vulva were estimated on the basis of research SOTE before and after treatment. The results are shown in table. 5.

From the results it is clear that in all three areas of research pH shifted the suppository according to the invention in the negative direction.

In the evaluation it is necessary to consider that the conduct of (standard) treatment known in the SZOTE were aimed at the control of the vagina. These results are summarized in table. 6. The results of the validation studies, performed one month after treatment, also shown in column 3 of table. 6.

The effectiveness of the suppository is also proven by the results of table 6. The duration of this effect shows significant differences from the (standard) treatment method known in this field.

The development of subjective complaints is illustrated in the table. 7 research-based SOTE. Four of the syndrome, i.e., irritation, pain, redness and discharge, were evaluated and patients, and dealing with their doctors.

The severity of symptoms expressed by the following estimates:

0 = no complaints, 1 = light complaints, 2 = moderate complaints, 3 = severe complaints.

In relation to subjective complaints, you can specify that the improvement in all four syndromes, especially in cases of irritation, pain, and discharge was not significant. Significant mitigation of complaints was observed at the joint assessment of complaints.

1. Pharmaceutical composition for the treatment of symptoms of weliwita and vulvovaginitis, containing a mixture of active ingredient and pharmaceutically acceptable carriers and/or excipients, characterized in that a mixture of the active ingredient is at or dextrose, lactic acid, magnesium sulfate and sodium chloride or ammonium chloride, in the following ratio, wt.%:

Folic acid - 0,05 - 0,5

Panthenol - 0,25 - 2,5

and/or Allantoin - 0,15 - 1,5

Hydrolyzed protein or hydrolyzed casein - 0,75 - 7,5

Lactose or dextrose - 3,0 - 15,0

Lactic acid - 0,25 - 2,5

Magnesium sulfate - 0,25 - 2,5

Sodium chloride, or

Ammonium chloride - 0,75 - 7,5

Pharmaceutically acceptable carriers and/or excipients - Rest

2. The composition according to p. 1, characterized in that as pharmaceutically acceptable carriers it contains polyoxyethyleneglycol and an ester of a fatty acid polyoxyethylenesorbitan.

 

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