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Suppositories for treating proctologic and gynecologic diseases

IPC classes for russian patent Suppositories for treating proctologic and gynecologic diseases (RU 2421210):
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FIELD: medicine.

SUBSTANCE: invention refers to suppositories for treating proctologic and gynaecologic diseases. Said suppositories contain a drug in the form of the dehydrated preparation 'Baliz' or a power-predried form of the preparation 'Baliz', or an active substance pre-recovered from the preparation 'Baliz' in the form of comenic acid or its salts, and also a base representing fatty substances, and a food or medicinal emulsifier.

EFFECT: higher therapeutic clinical effectiveness in gynecologic and proctologic diseases by reducing tissue inflammatory processes, hypostasis events, itching, burning and providing longer remission period.

4 cl, 3 ex

 

The invention relates to medicine and the pharmaceutical industry and the development of a medicinal product in the form of rectal and vaginal suppositories for the treatment of proctologic diseases, such as external and internal hemorrhoids, rectal fissures, chronic anal fissures, shinkaryov, erosions on the surface of internal hemorrhoids, chronic hemorrhoids, thrombosis of hemorrhoids, hemorrhoidectomy, acute paraproctitis, and various gynecological diseases, such as inflammatory diseases of the vagina, acute vaginitis, bacterial vaginosis.

Known suppositories "Basis" for the treatment of proctologic diseases containing drug Beliz-2, representing a multicomponent mixture of carbohydrate ketoacids, in particular a mixture of katalogowy acids, lactones of these acids, and acid number of gamma-pyrone, and Superin-M as the basis.

(EN 2076696 C1, A61K 9/02, AK 31/71, 1997)

The disadvantages of the known suppositories are not high enough quality, leading to kashimashi suppositories and, ultimately, to their disintegration, not a high therapeutic effect and a narrow spectrum of activity, namely the use only for the treatment of hemorrhoids.

The closest essential prize is akov to the proposed suppositories are rectal suppositories "Basis" for the treatment of proctologic diseases, containing the drug Bales and a mixture of confectionery fat, frying fat and emulsifier of Apol taken as the basis.

(EN 2337666 C1, AC 9/02, AK 31/191, AR 9/14, 10.11.2008.)

These suppositories have not sufficiently high anti-inflammatory activity, not allowing to arrest the inflammatory processes in tissues, low remission in cases of chronic diseases and narrow spectrum of activity, namely only for the treatment of proctologic diseases.

The present invention is the development of suppositories broad-spectrum with enhanced anti-inflammatory activity, allowing to arrest the inflammatory processes in tissues, the phenomenon of swelling, itching, burning in anal and female genital area, and to increase the period of remission for up to 6 months in cases of chronic gynecological and proctological diseases.

The technical result is reflected in increased therapeutic efficacy of the treatment of gynecological and proctological diseases through the reduction of inflammatory processes in tissues, the phenomena of swelling, itching, burning, and increase remission of chronic diseases to 6 months.

The problem is solved in that the suppositories for the treatment of proctologic and gynecological diseases, including prep the rat "Basis" and the basis according to the invention, they contain dehydrated form in the concentrated form of the drug "Basis" in the amount of 0.14 g or dried powdered form of the drug "Basis" in the amount of 0.9 grams, or isolated from drug Beliz" Kamenovo acid or a salt thereof in the amount of 0,0084 g suppository mass of 2.0,

In addition, as the basis suppositories contain fatty substances and food or medical emulsifier.

Fatty substances selected from the group: witepsol, supportin, hydrogenated fats, animal fats, solid fats type a, b, C.

Food emulsifier selected from the group of Apol, lecithins, mono - and diglycerides of fatty acids, esters of glycerol and fatty organic acids, Palsgaard 0093.

Medical emulsifier selected from the group T-2, saponin, anionic surfactants (Soaps), nonionic surfactants (tween-80), calcium stearate, pentol, sorbifolia.

Suppositories prepared as follows.

Take in a given quantity of a fatty substance selected from the group: witepsol, supportin, hydrogenated fats, animal fats, solid fats type a, b, C, and food emulsifier, selected from the group of Apol, lecithins, mono - and diglycerides of fatty acids, esters of glycerol and fatty organic acids, Palsgaard 0093, or medical emulsifier selected from the group: T-2, saponins, Ani is by surfactants (Soaps), nonionic surfactants (tween-80), calcium stearate, pentol, sorbifolia. Download these main components in a container, heated to 65-70°C. to obtain a molten mass. The molten mass is stirred for 10 min to obtain a homogeneous mass. Add to the melt in terms of one suppository: pre-dehydrated form of the drug Basis" in the form of a concentrate in the amount of 0.14 g, or pre-dried form of the drug Basis" to a powder in the amount of 0.9 grams, or pre-selected active substance of the medicinal product "Basis" in the form of Kamenovo acid or a salt thereof in the amount of 0,0084, Mix these components for 20 min to obtain a homogeneous mass.

Then the temperature suppozitornoj mass is brought to 42-45°C and stirred for 30 minutes Take samples for analysis. The resulting mass is fed to the molding in special for suppositories forms, pre-cooled and washed with a soap solution or spirtovm solution of glycerol. Filled forms cool for 15-20 minutes, remove from moulds and Packed.

Received suppositories have a high therapeutic efficacy in the treatment of gynecological and proctological diseases by inflammatory edema is x processes in tissues, phenomena of swelling, itching, burning, and increase remission of chronic diseases to 6 months.

The invention is illustrated in the following examples.

Example 1. For manufacturing fundamentals take a fatty substance selected from the group: witepsol, supportin, hydrogenated fats, animal fats, solid fats type a, b, C, and food emulsifier, selected from the group of Apol, lecithins, mono - and diglycerides of fatty acids, esters of glycerol and fatty organic acids, Palsgaard 0093. Download these main components in a container, heated to 65°C. to obtain a molten mass. The molten mass is stirred for 10 min to obtain a homogeneous mass. Added to the molten fatty substance the active substance of the drug Beliz - Kamenovo acid or its salts, previously isolated from a medicinal product "Bales". Mix these components within 20 minutes

These components take in the city in terms of one suppository mass of 2.0 g:

kamenova acid
or
salt Kamenovo acid 0,0084
base 1,8216

Then the temperature suppozitornoj mass was adjusted to 42°C and stirred for 30 min to obtain a homogeneous mass. Take samples for analysis. The resulting mass is fed to the molding in special for suppositories forms, pre-cooled and washed with a soap solution or alcohol solution of glycerol. The filled form is cooled for 15 minutes, remove suppositories form and Packed.

Example 2. For manufacturing fundamentals take a fatty substance selected from the group: witepsol, supportin, hydrogenated fats, animal fats, solid fats type a, b, C, and food emulsifier, selected from the group of Apol, lecithins, mono - and diglycerides of fatty acids, esters of glycerol and fatty organic acids, Palsgaard 0093. Download these main components in a container, heated to 70°C. to obtain a molten mass. The molten mass is stirred for 10 min to obtain a homogeneous mass. Added to the molten fatty substance and an emulsifier dehydrated form of the drug Basis" in the form of a concentrate. Mix these components within 20 minutes

These components take in the city in terms of one suppository mass of 2.0 g:

dehydrated form of the drug Beliz" 0,14
base 1,69

Mix these components for 30 min to obtain a homogeneous mass. Then the temperature suppozitornoj mass is brought to 45°C and stirred for 20 minutes Take samples for analysis. The resulting mass is fed to the molding in special for suppositories forms, pre-cooled and washed with a soap solution or alcohol solution of glycerol. The filled form is cooled for 15 minutes, remove suppositories form and Packed.

Example 3. For manufacturing fundamentals take a fatty substance selected from the group: witepsol, supportin, hydrogenated fats, animal fats, solid fats type a, b, C, and medical emulsifier selected from the group: T-2, saponin, anionic surfactants (Soaps), nonionic surfactants (tween-80), calcium stearate, pentol, sorbifolia.

Download these main components in a container, heated to 70°C. to obtain a molten mass. The molten mass is stirred for 10 min to obtain a homogeneous mass. Added to the molten fatty substance and an emulsifier powder form of the drug Basis". Mix these components within 20 minutes

These components take in the city in terms of one suppose the oriy weight of 2.0 g:

the powdered form of the drug Beliz" 0,9
base 0,93

Mix these components for 30 min to obtain a homogeneous mass. Then the temperature suppozitornoj mass is brought to 45°C and stirred for 20 minutes Take samples for analysis. The resulting mass is fed to the molding in special for suppositories forms, pre-cooled and washed with a soap solution or alcohol solution of glycerol. The filled form is cooled to 20 minutes, remove the suppositories form and Packed.

The comparative analysis of suppositories obtained in examples 1, 2, 3, with a unique selection of component framework with suppozitornyj mass obtained on the prototype showed that suppozitornaja the weight of the claimed method, homogeneous, elastic, compact, does not crumble or disintegrate during use.

The effectiveness of the treatment by suppositories made on the presented examples, was investigated in 3 groups of patients suffering from anal and gynecological diseases, 10 people each. The first group of patients (control prototype)suffering from proctologic diseases, the definition is about the daily introduction 1 suppository, made the prototype, 2 times a day morning and evening course 5 days. And the second group of patients with proctological diseases (such as external and internal hemorrhoids, fissures of the rectum, chronic anal fissure, sincerity, erosion on the surface of internal hemorrhoids, chronic hemorrhoids, thrombosis of hemorrhoids, hemorrhoidectomy, acute paraproctitis), and the third group of patients suffering from gynecological diseases (such as inflammatory diseases of the vagina, acute vaginitis, bacterial vaginosis), assigned to the introduction of suppositories which are manufactured according to examples 1, 2, 3, 1 suppository 2 times a day morning and evening course 5 days. As a result of treatment, there was statistically significant decrease in inflammatory processes in tissues, the phenomenon of swelling, itching, burning, reducing the number of pathological whiter, increasing the number of lactobacilli, improving the microflora of the vagina.

At the control examination after 10 days it is established that in 2 and 3 groups of patients positive therapeutic result, which is manifested in the inflammation process, removing edema, itching, burning, subsidence of the pain, stop bleeding, occurred in 20-30 minutes after administration of suppositories, and full recovery occurred after stock in contrast to the control group, where therapeutic effect occurred on the 14th day. Observations have shown that anti-inflammatory activity of the claimed suppositories reduces to twice the duration of treatment of inflammatory proctologic diseases and pelvic inflammatory disease (up to 7 days) compared to the prototype (up to 14 days).

At the control examination after 6 months of complaints from patients suffering from chronic inflammatory proctologic and gynecological diseases, have been reported. During the survey it was noted achieve a positive result in all treated patients. Ultrasound examination confirmed the removal of inflammation.

When assessing the toxicity of the drug was conducted an experiment on rats clean Wistar daily rectal 200 mg suppozitornoj mass while simultaneously placebo-control group of 50 and 10 animals, respectively). Evaluation of the effects of the drug were conducted over the course of the introduction on the General condition of the animals, immediately after completion of the course introduction, and after 2 weeks on the biochemical parameters of blood, peripheral blood and blood coagulability and conduct morphometric analysis and histopathological studies of the internal organs of animals. The experiments were conducted on four experimental the of the other groups of 10 females and 10 males in each group. The excess of the injected dose up to 5 times does not lead to pathological changes in the body. Within 9 days (treatment) there were no reported deaths or acute poisoning. Biochemical parameters remained within the normal range (total protein, the ratio of protein fractions and total serum cholesterol, glucose, urea, creatinine, the activity of alanine and aspartate transaminases, alkaline phosphatase). Histological examination of the organs did not reveal any deviations in their structure.

Thus, the proposed suppositories for the treatment of proctologic and gynecological diseases eliminate the disadvantages associated with the use of known suppositories, and to improve therapeutic efficacy of treatment due to edema in the short term inflammatory processes in tissues, the phenomenon of swelling, itching, tingling, painless insertion of suppositories, which helps to prolong the remission period up to 6 months in cases of chronic diseases.

Clinical studies have allowed us to draw the following conclusions.

The use of declared suppositories achieve a high therapeutic effect in the treatment of a wide spectrum of proctologic diseases, such as external and internal hemorrhoids, rectal fissures, chronic the x anal fissures, sphincteric, erosions on the surface of internal hemorrhoids, chronic hemorrhoids, thrombosis of hemorrhoids, hemorrhoidectomy, acute paraproctitis, and various gynecological diseases, such as inflammatory diseases of the vagina, acute vaginitis, bacterial vaginosis.

The choice of components and their quantitative values gives an opportunity to gain new technical result, which is manifested in the reduction of inflammatory processes in tissues as in proctology, and in the female genital area, and the increase of remission in cases of chronic gynecological and proctological diseases.

The tool is well tolerated and does not cause allergies and other side effects during treatment. In addition, suppositories stable during storage, resist the action of air, light and high temperatures, which gives an opportunity to choose the optimum conditions of the technological process of their production.

Thus, the claimed rectal and vaginal suppositories comply with the requirements of normative-technical documentation as suppositories are effective and safe drug and can be recommended for clinical use in patients with proctological and gynecological diseases.

1. Soup is sicarii for the treatment of proctologic and gynecological diseases, containing the drug and a base, characterized in that they contain as a medicinal product previously dehydrated form of the drug Basis" in the form of a concentrate in the amount of 0.14 g in terms of one suppository or pre-dried to a powder form of the drug Basis" in the amount of 0.9 g in terms of one suppository, or pre-allocated out of the drug Beliz active substance in the form of Kamenovo acid or its salts in the number 0,0084 g in terms of one suppository, and as the basis they contain fatty substances and food or medical emulsifier.

2. Suppositories according to claim 1, characterized in that as fatty substances they contain components selected from the group: witepsol, supportin, hydrogenated fats, animal fats, solid fats type a, b, C.

3. Suppositories according to claim 1, characterized in that as a food emulsifier they contain components selected from the group: Apol, lecithins, mono - and diglycerides of fatty acids, esters of glycerol and fatty organic acids, Palsgaard 0093.

4. Suppositories according to claim 1, characterized in that the quality of medical emulsifier they contain substances selected from the group T-2, saponin, anionic surfactants (Soaps), nei is ngenye surfactants (tween-80), calcium stearate, pentol, sorbifolia.

 

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