RU2146920C1 - Complex natural preparation as suppository for treatment of patient with urological, proctological and gynecological diseases and method of its preparing - Google Patents

Abstract

FIELD: medicine, chemical-pharmaceutical industry. SUBSTANCE: invention relates to the complex natural preparation "Prostopin" and method of its preparing. Preparation "Prostopin" has the following components: natural polyflower honey, mother bee milk, propolis (native and concentrate), bee bread, flower pollen (pollen load) taken by bees from different species of plants, bee wax, anhydrous lanolin (sheep fat), cacao butter or any of other fatty bases (solid fat, supporin-M, massupol, vitepsol). Technological process of preparing the complex preparation involves 3 main stages: preparing stage of initial components, preparing stage of initial components with suppository base and preparing stage of suppository mass and its packing. Invention provides the high effectiveness of the preparation in treatment of patients with urological (acute and chronic prostatitis, benign hyperthrophy of prostate, adenoma), gynecological (inflammation of vagina and uterus cervix) and proctological (anal fissures, hemorrhoid) diseases. EFFECT: enhanced effectiveness of treatment, improved method of preparing. 2 cl, 1 ex

Description

 The invention relates to the pharmaceutical industry, medicine, and relates to the composition, preparation and use of the original complex preparation "Prostopin" based on biologically active beekeeping products.

 The inventive preparation is rectal, vaginal suppositories and includes natural polyfler honey, royal jelly, propolis (native and concentrate), dried bee bread, flower pollen (pollen) collected by bees from certain types of plants, beeswax, lanolin (sheep fat ) anhydrous, cocoa butter or other fatty bases.

 All the components that make up Prostopin have a rich chemical composition and have versatile biological properties described in the literature.

 Polyfler honey (collected by bees from the flowers of various plants) includes more than 300 substances and consists mainly of carbohydrates glucose and fructose, sucrose, protein compounds (enzymes), non-protein nitrogen compounds (amino acids), vitamins, aromatic and mineral acids, neutral triglyceride fats, free fatty acids, sterols, phospholipids, flavonoids, minerals and trace elements. The rich chemical composition of honey determines the diversity of its biological properties: immunostimulating, anti-inflammatory, wound healing, anesthetic, antibacterial, antifungal, antiprotozoal, anti-radiation, anti-allergic, antitoxic and others (Apitherapy today. Rybnoe, 1997).

 Royal jelly (royal jelly) is the secret of the pharyngeal and mandibular glands of young working bees secreted for feeding uterine larvae consists of dry substances (34%): protein substances - albumin, globulins, lipoproteins, enzymes, glycoproteins, non-protein - glutamic amino acids, asparagine, lysine, proline, cysteine, histidine, etc., carbohydrates - glucose, fructose, sucrose, etc., vitamins A, B, D, pantothenic and ascorbic acids, hormones - estradiol, testosterone, progesterone, lipids - saturated and unsaturated mono - and dicarbon hydro acids, sterols, phospholipids, minerals, organic acids and other biologically active substances. Royal jelly is a highly active biogenic stimulator, normalizes and activates metabolic processes in tissues, improves their nutrition, stimulates a number of biochemical processes, including the immune and endocrine systems, regulates the level of sex and other hormones, has anti-aging, bacteriostatic, antiviral, antitoxic, radioprotective, antimutagenic and other types of pharmacological actions (T.V. Vakhonina. "Bee Pharmacy", 1992).

 Propolis ("bee balm") includes phenolic compounds (flavonoids, hydroxybenzoic, hydroxycinnamic acids and alcohols, coumarins, etc., polymeric phenolic compounds, tannins, essential oils, resins, lipids, aliphatic, organic acids, carbohydrates, volatile compounds , minerals, vitamins, azo-containing compounds, etc. Propolis surpasses many synthetic antibiotics in its activity, having a wider spectrum of antibacterial, antiviral, antifungal, antiprotozoal ystviya and characterized by immunostimulant, anesthetic, anti-oxidant, wound healing, anti-inflammatory, radioprotective and other valuable biological properties ( "Valuable product bee propolis" Apimondia, Bucharest, 1988).

 The pollen collected from the flowers by the bees is processed by secretions of the pharyngeal glands and nectar and a pollen is formed, which is folded into cells, rammed and filled with honey. Due to the enzymes of saliva of bees and honey, without access to air, pollen undergoes fermentation and turns into a new product - bee bread ("bee bread"). As a result of this process, the amount of protein and lipid in bee bread is reduced, but the content of lactic acid and carbohydrates increases. Pollen and perge contain 28 mineral macro- and microelements (salts of potassium, phosphorus, calcium, iron, copper, zinc, etc.), nitrogenous compounds of protein (proteins, enzymes, nucleoproteins) and non-protein nature (free amino acids and peptides), carbohydrates (glucose, fructose, maltose, sucrose, starch, fiber, etc.), neutral fats and fat-like substances (phosphatides, sterols, sterols), essential fatty acids (linoleic, linolenic, arachidonic, etc.), vitamins A, C, B, P, E, inosine, flavonoids, phenolic acids, triterpenoids, saponins and other ve of society. Pollen and perge are characterized by antimicrobial, immunostimulating, anabolic, tonic, antispastic, trophic, adaptogenic, hepatoprotective, antianemic, anti-inflammatory, hormone-regulating and other biological properties (AF Sinyakov. "Bee pharmacy". - M., 1995).

 Wax is a complex composition of more than 300 substances that make up its composition. 70-75% consists of esters (mainly esters of ceryl and melisinic alcohols and the corresponding acids), 12-15% of free fatty acids (lignoceric, cerotinic, etc.), 11.9% of hydroxy and keto acids and paraffin hydrocarbons, monohydroxy and dihydric alcohols, minerals, resins, plant pigments, aromatics, vitamins, cholesterol, triterpenes and other substances (Apitherapy today. Rybnoe, 1997).

 Cocoa butter and anhydrous lanolin form the suppository base. Wax performs plastic and stabilizing functions.

 On the basis of beekeeping products abroad and in Russia, a whole series of medicines and biologically active food additives have been created, including dragees with royal jelly, vitadone (tablets with lyophilized royal jelly), melcacin (granular preparation with royal jelly, calcium and honey), apilak, granular pollen, polenapine, log wood (pollen and royal jelly tablets), energine (pollen and honey concentrate), polenolecithin (a product based on pollen, honey and vegetable lecithin), melprosept (propolis me ), Vitas (a complex preparation from honey, pollen, beef and royal jelly), proposept (tablets with propolis), apiren (ointment and liniment with bee venom), proderm (solution of propolis in alcohol), ointment with propolis, apisartron, propoceum and a number of other drugs (Apitherapy today, Bucharest, p. 50).

In our country, V.F.Orkin developed suppositories from a thick extract of propolis for the treatment of chronic prostatitis (Vakhonina, p. 181). To do this, 20 g of crushed propolis for 3 days, insist in 100 g of 96% ethanol at a temperature of 20-25 ^o C (without access to light), followed by removal of the solvent by distillation under vacuum or gradual evaporation. The composition of the suppository: 0.1 g of a thick extract of propolis and 2 g of cocoa butter. Abroad, for the treatment of prostate diseases, candles were tested, which included 24 g of cocoa butter, 2.5 g of lanolin, 7.5 g of thick propolis extract, 0.5 g of royal jelly and 2 g of honey. N. Mihailescu (Romania, 1976) obtained good, stable results with benign prostatic hypertrophy and prostatitis (T.V. Vakhonina. "Bee Pharmacy", 1992, p. 181).

 The closest in composition (prototype) to the claimed drug "Prostopin" is "Mipropol" (Romania), which is a suppository containing 0.4 g of polyfler honey, 0.25 g of propolis extract (thick extract), 0.15 g of pollen , 0.15 g of royal jelly and cocoa butter (T. V. Vakhonina. "Bee Pharmacy", 1992, p. 180), tested and successfully used today for the treatment of acute and chronic prostatitis, benign prostatic hypertrophy, prostate adenoma (Apitherapy today, Bucharest, 1988, p.66). Treatment of prostate adenoma (stage I and II) led to a decrease in the frequency of urination, a decrease in the amount of residual urine, and a pressure sensation in the lower abdomen decreased in 45-50% of cases, the act of defecation was facilitated ("Beekeeping Products - Food, Health, Beauty," Apimondia Bucharest, 1988). Such a course of treatment delayed the duration of the operation and the general condition of the patients improved so much that it further facilitated its implementation (M. M. Frenkel. "Unique Healer", 1991, p. 54).

 The aim of this invention is to develop the composition of the new complex drug "Prostopina" in the form of rectal, vaginal suppositories based on biologically active beekeeping products and a method for its preparation.

 The inventive drug "Prostopin" differs from the prototype "Mipropol" in its qualitative and quantitative composition, and also has an original production technology and a wider range of applications.

 The composition of Prostopin components per one candle weighing 2.9 g: natural polyfler honey 0.12 g (4.0%); royal jelly royal jelly 0.10 g (3.5%) or royal jelly royal jelly freeze-dried 0.033 g (1.14%); propolis (native and concentrate) 0.31 g (10.5%); dried salmon 0.15 g (5.2%); flower pollen (pollen) collected by bees from certain plant species 0.08 g (2.8%); beeswax 0.06 g (2.0%); lanolin (sheep fat) anhydrous 0.12 g (4.0%); cocoa butter 1.97 g (68.0%) or any other of the following fatty bases: solid fat, supporin-M, massupol, witepsol.

 The technological process consists of three main stages: the stage of preparation of the starting components; the stage of preparation of the mixture of the starting components with a suppository base and the stage of preparation of the suppository mass and its packaging. For the preparation of Prostopin suppositories, the raw materials and materials specified in the temporary technical conditions (VTU) for this type of product are used.

1. The technological scheme and the description of the technological process:
decrystallization of honey or heating liquid honey to a temperature of +35 ^o C.

preparation of native propolis
preparation of propolis concentrate
preparation of a mixture of honey with royal jelly
preparation of a mixture of pollen and pollen
preparation of suppository base with the addition of colloidal wax
preparation of mixtures of native propolis, propolis concentrate, pollen, bee bread, honey and royal jelly
mixing suppository components
molding rectal, vaginal suppositories
suppository packaging
packaging, labeling
Example 1

1.1. Honey decrystallization
Decrystallization of honey is carried out by incubation at 35-40 ^o C for 48 hours.

1.2. Propolis Preparation
1.2.1. Propolis is crushed into pieces no larger than 2-3 cm.

1.2.2. Preparation of Powdered Propolis
Propolis in the form of lumps is placed evenly on a pallet, placed in a refrigerator and cooled to a temperature of from -5 to -15 ^o C. The cooled propolis is subjected to grinding in M-8-M mills or other closed type grinders.

 1.2.3. Screening of powdered propolis.

 The ground propolis is sieved through a sieve with a hole size of 0.5 mm. Screenings are returned for re-cooling, grinding and sieving.

 1.2.4. Preparation of propolis concentrate.

Powdered propolis is placed in a container and filled with 96% ethyl alcohol in a ratio of 4: 1. Infusion is carried out at a temperature of 36-40 ^o C for 48 hours with constant and periodic stirring without access to light. The resulting concentrate is a thick creamy mass of dark brown.

1.3. Preparation of a mixture of honey with royal jelly
Royal jelly is introduced into the prepared honey in parts with constant stirring until a homogeneous mass is obtained.

1.4. Preparation of a mixture of pollen and pollen
Pre-ground bee bread and pollen collected by bees from certain plant species are mixed with each other and homogenized for 5 minutes in a “drunk barrel”.

 1.5. Preparation of suppository mass.

 1.5.1. Preparation of suppository base.

Cocoa butter with lanolin is melted at a temperature of 40-45 ^o C, add pre-melted wax there to stabilize the drug with constant stirring.

 1.5.2. Mixing components with a suppository base.

 1.5.3. Preparation of a mixture of propolis with a base.

To 1/2 of the base, having a temperature of 40-45 ^o C, is added with constant stirring powder of native propolis (40% of the total mass of propolis). The mixture is heated to a temperature of 60-65 ^o C and maintained at this temperature with constant stirring for 20 minutes. Then the mixture is cooled to 40-45 ^o C and make the rest of the propolis powder (30% of the total mass of propolis) and propolis concentrate (30% of the total mass of propolis). The mixture is kept at 40-45 ^o C with constant stirring for 20 minutes.

 1.5.4. Preparation of a mixture of pollen and pollen with the base.

To 1/4 of the base, having a temperature of 40-45 ^o C, add a crushed mixture of bee bread with pollen collected by bees from certain types of plants. At this temperature and with constant stirring can withstand 30 minutes.

 1.5.5. Preparation of a mixture of honey and royal jelly with a base.

To 1/4 of the base, having a temperature of 40-45 ^o C, add a mixture of honey and royal jelly. Stir until a homogeneous mass.

 1.5.6. Mixing the components of suppository mass.

All components of the suppository mass (paragraphs 1.5.3., 1.5.4., 1.5.5.) Must, before mixing, have a temperature in the range of 35-45 ^o C. The order of their mixing does not matter. The resulting suppository mass is mixed until a homogeneous mass.

 1.6. Formation of rectal, vaginal suppositories.

 The suppositories are poured on machines with separate casting and packaging operations (Franco-Crespi, Italy) or on a fully automated line (Hefliger and Karg Servac200S, Germany) or other similar machines.

1.4.4. When molding suppositories manually, the molten suppository mass is cooled to a temperature of 26-30 ^o C and poured into demountable molds. Pre-empty molds are lubricated with an alcoholic solution of calcium stearate, cooled using a refrigeration device (automatic mode) or a freezer for 10-20 minutes. The poured forms are placed in the freezer for 30-40 minutes. After hardening, the suppositories are removed and transferred to a pallet covered with parchment paper. Finished suppositories are rejected in appearance and subjected to analysis.

 Studies of the clinical effectiveness of Prostopin suppositories were carried out in three main areas: urological diseases (acute and chronic prostatitis, benign prostatic hypertrophy, prostate adenoma), gynecological diseases (inflammation of the vagina and cervix), proctologic (anal fissures, hemorrhoids).

 In urology, all patients were divided into three groups: the 1st group included 36 patients with acute and chronic prostatitis, the 2nd group included 24 patients with benign prostatic hypertrophy, and the 3rd group included 18 patients with periurethral prostate adenoma. The age of the patients was from 18 to 42 years for prostatitis, from 28 to 66 years for total benign prostatic hypertrophy, and from 46 to 77 years for prostate adenoma. The main symptoms of acute and chronic prostatitis were pain in the urogenital organs of the pelvis, the presence of palpation changes (size and consistency) on the part of the gland and the cytological composition of its secretion (increased number of leukocytes and red blood cells with a decrease in the number of lecithin grains). To establish the diagnosis and stage of adenoma evolution, we used the following criteria: the frequency of urination, the presence of dysuretic disorders, the increase in prostate volume, established by rectal palpation, the presence of prostatic amprenta during an urographic examination, with the determination of the remainder in the bladder and in some cases by measuring the remainder in the bladder. All patients were given 1 Prostopin suppository overnight in the rectum after preliminary bowel movement. The course of treatment lasted 30 days. As a result of treatment, 32 patients (89%) with acute and chronic prostatitis showed a significant improvement in all indicators, pain quickly disappeared, discharge from the urethra ceased, the general condition of the patients, prostate functions, clinical blood tests, urine and gland secretions returned to normal. When cytological examination of the secretion of the prostate, the absence or persistent decrease in leukocytes (not more than 1100-1700 in 1 mm cubic) was noted. In 16 patients (67%) with benign prostatic hypertrophy, the size of the gland significantly decreased, urination improved, pain lumbago disappeared. In the group of patients with prostate adenoma, 13 patients (72%) decreased urination frequency, residual urine volume, size and consistency of periurethral adenoma, general condition improved, and neuropsychiatric disorders decreased.

 In gynecological practice, treatment was applied to 54 patients aged 19 to 64 years with a diagnosis of inflammation of the vagina and cervix. Patients were divided into three groups. The first group consisted of 17 patients in whom the inflammation was caused by Trichomonas vaginalis. The second group (15 people) included patients in whom the disease was caused by pathogenic fungi. The third group included 22 patients whose inflammation was caused by infection of mixed bacterial origin. The cause of the inflammatory processes was the presence of pathogenic staphylococci and streptococci. Suppositories "Prostopin" were administered intravaginally daily, one at night for 15 days. As a result of treatment, the best results were obtained in the third group (mixed infection caused by at least two groups of bacteria) - in 18 patients (82%), the inflammatory process was eliminated while improving the condition of the cervix. The treatment of the 1st group (trichomoniasis) ended successfully, in which a significant improvement was achieved in 10 (59%) of 17 cases. In cases where the inflammatory process was induced by pathogenic fungi (group 2), the effect of the drug was found only in 47% of cases (7 patients). In all patients with vaginal inflammation and cervical erosion receiving suppositories, the inflammatory process was inhibited, pathogenic was suppressed, and normal microflora and epithelium were restored.

 In proctological practice, the treatment of anal fissures, hemorrhoids without loss of hemorrhoidal nodes using suppositories was performed in 32 patients. 15 of them had concomitant anal itching, all patients had pains after defecation from 30 minutes to 4-5 hours, 17 - discharge of red blood during defecation. "Prostopin" was administered 1 suppository at night after bowel movement for 30 days. 2-3 days after the start of treatment, 28 patients (88%) showed a significant improvement, pain and discomfort, itching in the anus decreased, and after 2-3 weeks the cracks completely disappeared, bleeding was eliminated, and hemorrhoids decreased in size.

 Thus, the preliminary clinical studies of Prostopin suppositories in urological, gynecological and proctological practice confirm the effectiveness of the new complex preparation based on biologically active beekeeping products in the treatment of a number of infectious and inflammatory diseases, including acute and chronic prostatitis, benign prostatic hypertrophy, adenoma prostate gland, vaginal inflammation and cervical erosion, anal fissures and hemorrhoids. The high biological activity of the drug is due to its rich chemical composition and a wide range of pharmacological effects of its constituents.

LITERATURE
1. "Apitherapy today." Apimondia, International Institute of Technology and Economics of Beekeeping. - Second ed., Bucharest, 1988.

 2. T.V. Vakhonina. "Bee Pharmacy". - St. Petersburg, Lenizdat, 1992.

 3. A.F. Sinyakov. "Bee Pharmacy". - M., Physical education and sport, 1995.

 4. M.M. Frenkel. "A unique healer." - M., Erus, 1991.

 5. "Apitherapy today." Materials of the V scientific-practical conference on apitherapy "Bees and your health", Sochi, October 9-12, 1996, Rybnoe, 1997. - Collection V.

 6. "A valuable beekeeping product is propolis." Ed. Fourth, Apimondia, Bucharest, 1988.

 7. "Beekeeping products - food, health, beauty." - Ed. Second, Apimondia, Bucharest, 1988.5

Claims (1)

1. A complex natural preparation in the form of suppositories, containing natural polyfler honey, royal jelly, propolis, flower pollen (dressing), a base characterized in that it additionally contains dried bee bread, beeswax, anhydrous lanolin, and flower pollen (dressing) collected by bees from different species of plants, propolis native and concentrate and the base contains anhydrous lanolin, beeswax and cocoa butter, or solid fat, or supporin-M, or massupol, or vitepsol in the following ratio of components in the calculation 1 suppository weight 2.9 g, g:
Polyfler natural honey - 0.12 (4.0%)
Royal jelly milk - 0.10 (3.5%)
Propolis native and concentrate - 0.31 (10.5%)
Dried salmon - 0.15 (5.2%)
Flower pollen (pollen) - 0.08 (2.8%)
Beeswax - 0.06 (2.0%)
Anhydrous lanolin - 0.12 (4.0%)
Cocoa butter, or solid fat, or supporin-M, or massupol, or vitepsol - 1.97 (68.0%)
2. A method of producing suppositories by mixing natural polyfler honey, royal jelly milk, propolis, flower pollen (mushrooms), a base, molding a suppository mass, packaging, packaging, characterized in that the honey is decrystallized at 35-40 ^° for 48 hours, prepared native propolis and a concentrate on 96% ethanol in a 4: 1 ratio, get a mixture of honey with royal jelly, mix the bee bread with pollen, prepare a suppository base consisting of molten cocoa butter and lanolin with the addition of beeswax, and then, in stages, mixtures of these fractions with a suppository base are obtained, mixed until a homogeneous suppository mass is obtained, formed by cooling and marked after packaging.