RU2225213C2 - Suppository "apiprost" eliciting wound-healing effect - Google Patents

Abstract

FIELD: medicine, proctology, pharmacy. SUBSTANCE: invention relates to method for making suppository "Apiprost" recommended for complex therapy in inflammatory processes in rectum intestine, prostatitis, hemorrhoid, for treatment of anal fissures. Proposed suppository contains homogenate or lyophilizate of drone breeding, mother milk, bee breed, natural honey, propolis, pot-marigold tincture, bee wax, anhydrous lanoline, solid fat or vitepsol or butyrum-cacao. Invention provides the complete release of active substances, shows the expressed curative effect and minimal risk for development of adverse effects. EFFECT: enhanced effectiveness and valuable medicinal properties of suppository. 3 ex

Description

 The invention relates to the field of pharmacy and medicine and relates to the technology of soft dosage forms, namely the Apiprost suppository.

In Russia, a small number of rectal suppositories with wound healing and anti-inflammatory effects are registered. So, in medical practice, domestic suppositories with ichthyol are used (M.D. Mashkovsky, 1997), suppositories with tincture of calendula (VFS 42-2622-95), candles "Prostopin" (VFS 42-3453-99), which have anti-inflammatory effects. Candles "Prostopin" containing beekeeping products can be taken as a prototype (VFS 42-3453-99). The composition of these suppositories is as follows, g:
Native royal jelly (apilak) - 0.1
Pollen - 0.08
Perga - 0.15
Natural honey - 0.12
Propolis - 0.31
Beeswax - 0.06
Anhydrous lanolin - 0.12
Cocoa Butter - 1.97
Suppositories "Prostopin" are prepared on a lipophilic basis (cocoa butter), have anti-inflammatory, antihemorrhoidal effects.

 The disadvantage of this drug is that it uses an expensive imported base.

 The aim of this invention is the creation of Apiprost suppositories with anti-inflammatory and wound healing effects, for the preparation of which, in addition to cocoa butter, they use relatively cheap and affordable domestic raw materials: solid fat, witepsol. The active components of Apiprost candles are bee products and calendula tincture. The composition of the components is selected for suppositories weighing 2.2-2.5 g.

 Solid fat and vitepsol are registered in Russia as the basis for the preparation of suppositories (FS 42-8991-98, type A and VTU 3-78), are cheap substitutes for cocoa butter. The physicochemical properties of these substrates allow them to be used to produce Apiprost candles.

This goal is achieved by introducing into the basis of beekeeping products and tinctures of calendula containing a complex of biologically active substances, in the following ratio of components, g:
Example 1
Drone brood homogenate - 0.05-0.06
/ or drone brood lyophilisate - 0.03-0.04
Royal jelly - 0.05-0.06
Perga - 0.11-0.13
Natural honey - 0.09-0.11
Propolis - 0.23-0.25
Calendula tincture - 0.6 ml
Beeswax - 0.05-0.07
Anhydrous lanolin - 0.09-0.11
Solid fat - enough to prepare a suppository weighing 2.2-2.5 g
Example 2
Drone brood homogenate - 0.05-0.06
/ or drone brood lyophilisate - 0.03-0.04
Royal jelly - 0.05-0.06
Perga - 0.11-0.13
Natural honey - 0.09-0.11
Propolis - 0.23-0.25
Calendula tincture - 0.6 ml
Beeswax - 0.05-0.07
Anhydrous lanolin - 0.09-0.11
Vitepsol is sufficient for the preparation of a suppository weighing 2.2-2.5 g
Example 3
Drone brood homogenate - 0.05-0.06
/ or drone brood lyophilisate - 0.03-0.04
Royal jelly - 0.05-0.06
Perga - 0.11-0.13
Natural honey - 0.09-0.11
Propolis - 0.23-0.25
Calendula tincture - 0.6 ml
Beeswax - 0.05-0.07
Anhydrous lanolin - 0.09-0.11
Cocoa butter - a sufficient amount for the preparation of a suppository weighing 2.2-2.5 g
The base (cocoa butter, or vitepsol, or solid fat) is manually fed into the stirred reactor and melted at a temperature of 40-45 ^° C. After that, molten wax is fed into the reactor and mixed. The molten base is then filtered through a double gauze colatura. The entire mass of the base is divided into two approximately equal parts by overflowing it into existing reactors.

Calendula tincture is poured into propolis powder, the mixture is thoroughly mixed for 30 minutes, then the ground beef is added and mixed again until smooth. The resulting mixture is introduced into part of the base in a separate reactor and stirred for 30-45 min at a temperature of 40-45 ^o C. Pre-thawed royal jelly and homogenate (lyophilisate) of drone brood are introduced into the mixer with lanolin and mixed with a mixer to a homogeneous mass. Then, the resulting mass is introduced in portions into the reactor with the required amount of decrystallized honey and the mixture is stirred for 25 minutes at 35-38 ^o C. The resulting mass is introduced into the second part of the molten base and stirred for 30 minutes at a temperature of 35-40 ^o C. Then combine the resulting mixture from two reactors and mix them for 30 minutes, after which the suppository mass is used for pouring.

 The essential distinguishing features of the claimed compositions are the use of solid fat, or vitepsol, or cocoa butter as the basis, and the following complex as the active ingredient: royal jelly, drone brood homogenate, honey, propolis, wax, perga, calendula tincture.

The advantages of the proposed compositions are:
- low cost of production, as developed candles are prepared on domestic raw materials;
- the optimal combination of compatible, mutually potentiating pharmacologically active substances;
- minimal risk of side effects;
- the use of a new relatively cheap active component - homogenate or lyophilisate of the drone brood, having a composition similar to royal jelly.

 Suppositories "Prostopin" are prepared on a lipophilic basis (cocoa butter), have anti-inflammatory, antihemorrhoidal effects.

 The disadvantage of this drug is that it uses an expensive imported base.

 The aim of this invention is the creation of Apiprost suppositories with anti-inflammatory and wound healing effects, for the preparation of which, in addition to cocoa butter, relatively cheap and affordable domestic raw materials are used: solid fat, witepsol. The active components of Apiprost candles are bee products and calendula tincture. The composition of the components is selected for suppositories weighing 2.2-2.5 g.

 Solid fat and vitepsol are registered in Russia as the basis for the preparation of suppositories (FS 42-8991-98, type A and VTU 3-78), are cheap substitutes for cocoa butter. The physicochemical properties of these substrates allow them to be used to produce Apiprost candles.

This goal is achieved by introducing into the basis of beekeeping products and tinctures of calendula containing a complex of biologically active substances, in the following ratio of components, g:
Example 1
Drone brood homogenate - 0.05-0.06
/ or drone brood lyophilisate - 0.03-0.04
Royal jelly - 0.05-0.06
The therapeutic and prophylactic effects of the Apiprost suppository are due to the complex of active components that make up their composition.

 Royal jelly contains a complex of biologically active substances: proteins necessary for the construction and restoration of tissues; amino acids that contribute to the formation of collagen and elastin, wound healing; saturated and unsaturated fatty acids that activate metabolic processes; steroids that contribute to cell renewal, thickening of the epidermis, phospholipids, glycolipids that improve the delivery of active substances to the cells of the body and participate in the restoration of the lipid composition of cell membranes. Steroid hormones are characterized by anti-inflammatory activity.

 Drone brood homogenate or lyophilisate is an affordable and relatively inexpensive substitute for royal jelly with a similar composition. The drone brood contains proteins, amino acids, carbohydrates, vitamins, enzymes, minerals, nucleic acids, hormones, lipids and other compounds. The complex of biologically active components causes a pronounced anti-inflammatory and wound healing action.

 Propolis contains 55% resins and balsams, a large amount of wax, aromatic essential oils and pollen. The composition of vegetable resins and balms, which are the main component of propolis, include acids, alcohols, phenols, tannins and hydrocarbons. Propolis defines amino acids, terpenoids, ketones, flavones, flavonones, aliphatic and aromatic hydrocarbons, mineral compounds, etc. The complex of these biologically active substances causes pronounced pharmacological effects. Propolis has antibacterial and anti-inflammatory properties, it is used as a strong anesthetic, against itching. Active propolis compounds cleanse the cell membranes in the body, affecting lipoproteins, promote the removal of cholesterol from the body, normalize the respiration of cells, and suppress the pathological cell. In addition, propolis is effective in the treatment of burns and wounds of various etiologies, has preservative properties.

 Honey. The main components of honey are carbohydrates represented by monosaccharides and oligosaccharides. This product contains glucose, fructose, enzymes (diastase, invertase, catalase, peroxidase, lipase), organic acids (malic, tartaric, citric, oxalic, lactic acids), micro and macrocells. According to the chemical composition of minerals, honey is close to human blood plasma. In addition, bee honey contains vitamins, proteins, amino acids (proline, phenylalanine, tyrosine, aspartic and glutamic acids), lipids, free fatty acids (palmitic, stearic, oleic, lauric, arachidonic) and lipoids (sterols, phospholipids) hormonal, antibiotic, phytoncidal and other valuable substances. Various biological properties are characteristic of honey: it has immunotropic, anti-allergic, anti-radiation, anesthetic, anti-inflammatory and wound healing effects, and has preservative, antibiotic effects. It stimulates tissue growth in the body, restores the metabolic processes of withered skin cells. Honey is widely used for dietetic and medicinal purposes. It is used to treat wounds, gastrointestinal, cardiovascular and other diseases.

 Wax. The main component of beeswax are esters of ceryl, myricyl and melissinovoy alcohol and fatty acids (palmitic and oleic), as well as hydroxy and keto acids. Wax contains sterols (B-sitosterol, cholesterol and cholesterol esters), alcohols, saturated and unsaturated hydrocarbons, vitamin A. This product is used in dermatology to treat skin inflammations, burns, wounds as a bactericidal and tissue growth stimulating agent.

 Perga - a combination of nutrient and biologically active components of plant and animal (bee) origin, contains a number of substances: minerals, amino acids, carbohydrates, essential oils, vitamins, lipids, fatty acids, etc. Perga has a pronounced biological effect on the human body, contributes to normalization of all types of metabolism, has stimulating properties, accelerates the growth and development of organs and tissues. Its biologically active components have a positive effect on the mucous membrane of the gastrointestinal tract, on the excretory function of the glands, the functioning of the liver, thyroid gland and other organs. Perga is a biological stimulant, increases appetite, improves tissue tone and turgor, and stimulates the body's defenses. Perga has many phenolic compounds characterized by capillary-strengthening, antioxidant, choleretic, diuretic, anti-inflammatory, anti-sclerotic, anti-tumor and anti-radiation effects. This product is indicated for the treatment of atherosclerosis, inflammation of the meninges, diseases of the prostate gland.

 Calendula officinalis (Calendula officinalis). Flower baskets contain carotenoids: carotene, rubixanthin, lycopene, citroxanthin, violoxanthin, flavochrome, flavoxanthin, hydrocarbons (sitosterol, etc.), resins, triterpene glycosides, mucous and bitter substances, organic acids (malic, pentadecicylic acid) and other compounds. A wide range of pharmacological activity (anti-inflammatory, wound healing, bactericidal, antispasmodic and choleretic action) is due to the high content of biologically active compounds such as carotenoids, flavonoids, vitamins.

 Thus, the Apiprost suppository contains pharmacologically active and affordable components.

 Using the proposed composition of the suppository will allow you to organize the mass production of inexpensive and effective therapeutic and prophylactic agents.

Claims (1)

Suppositories with a wound healing effect containing beekeeping products - royal jelly, perga, natural honey, propolis, beeswax, base, anhydrous lanolin, characterized in that they additionally contain drone brood homogenate, calendula tincture, as a base solid fat or witepsol, or cocoa butter in the following ratio, g: Drone brood homogenate 0.05-0.06 (or drone brood lyophilisate) 0.03-0.04 Royal jelly 0.05-0.06 Perga 0.11-0.13 Natural honey 0.09-0.11 Propolis 0.23-0.25 Calendula tincture 0.6 ml Beeswax 0.05-0.07 Anhydrous lanolin 0.09-0.11 Solid fat or vitepsol or oil Cocoa Enough   for cooking   suppository mass   2.2-2.5 g