RU2196569C1 - Method of preparing ointment "apilar-g" eliciting anti-inflammatory effect - Google Patents

Abstract

FIELD: medicine, dermatology. SUBSTANCE: invention proposes method of preparing ointment comprising drone bee larvae as active component and polyethylene oxide 1500 gel as a base taken in the definite ratio of components: para-hydroxybenzoic acid methyl ester, para-hydroxybenzoic acid propyl ester, drone bee larvae (as measured for dry matter) and polyethylene oxide 1500. Invention provides deep penetration of biologically active substances in skin, easily application being without fatty glare and shows the expressed curative effect. Invention can be used for preparing ointment recommended in skin inflammatory sicknesses. EFFECT: improved method of preparing, enhanced effectiveness of ointment and treatment. 1 tbl, 2 ex

Description

 The invention relates to the field of pharmacy and medicine and relates to the technology of soft dosage forms, namely, Apilar-G ointment.

 Not a single medicinal product containing homogenate or lyophilisate of drone larvae was registered. As a cosmetic product, the cream "Lichinol" / Pat. RF 96104088/14 05/27/98. Bull. fifteen/.

A number of soft drugs with anti-inflammatory and reparative effects have been registered in Russia: 10% methyluracil ointment, Dolgit-cream, Butadion and others (MD Mashkovsky, 1996). Widely used in medicine, ointment "Butadion" can be taken as a prototype / Pat. 2128501. The composition of this ointment is as follows, wt.%:
Butadion - 5.0
Glycerin - 10.0
Trilon B - 0.1
Sodium metabisulfite - 0.1
PEO-1500 gel - Up to 100.0
Butadion ointment 5% is prepared on a washable hydrophilic basis, has a therapeutic effect in dermatitis of various etiologies, burns I and II degree of a small skin surface.

 The disadvantage of this ointment is that the active substance - a synthetic compound (a derivative of pyrazolidinedione), causes agranulocytosis with prolonged use.

 The aim of this invention is the creation of an ointment "Apilar-G", which has a pronounced anti-inflammatory effect, prepared on the basis of domestic raw materials - polyethylene oxide-1500 gel (PEO-1500) with the addition of a natural pharmacologically active component (drone larvae).

 PEO-1500 gel is registered in Russia as the basis for the preparation of ointments (reg. 58.5.9), and is currently widely used for various cosmetics (Patent 2110984 Russia, Patent 2124350 Russia). PEO-1500 gel is a colorless gel-like mass containing 94-95% water.

 The physicochemical and rheological properties of the PEO-1500 gel make it possible to use it to obtain Apilar-G ointment.

This goal is achieved by introducing into the basis of the homogenate or lyophilisate of drone larvae containing a complex of biologically active substances, preservatives (methyl and propyl esters of para-hydroxybenzoic acid) in the following ratio of components, wt.%:
Example 1
Ointment is prepared as follows:
Paraoxybenzoic acid methyl ester - 0.30-0.50
Paraoxybenzoic acid propyl ester - 0.15-0.50
Lyophilisate of drone larvae (in terms of dry matter) - 9.95-10.05
PEO-1500 - Else
Example 2
Paraoxybenzoic acid methyl ester - 0.30-0.50
Paraoxybenzoic acid propyl ester - 0.15-0.50
Homogenate of drone larvae (in terms of dry matter) - 9.95-10.05
Sodium hydrogen phosphate - 0.5-1.0
PEO-1500 - Else
A polyethylene oxide gel and preservatives are loaded into a stirred reactor at room temperature. The mass is homogenized for 20-30 minutes. The biologically active substance, drone larvae (homogenate or lyophilisate) is added to the resulting mixture with stirring. Mixing of all components is carried out for 20-30 minutes, after which the drug is Packed in containers.

An essential distinguishing feature of the claimed composition is the use of PEO-1500 gel as an ointment base, and a practically non-toxic natural component (drone larvae) as an active complex. The advantages of the proposed composition are:
- simplicity of the production process, because the stage of emulsification is excluded;
- low cost of production, because ointment is prepared on domestic raw materials;
- minimal risk of side effects.

 The drone larvae homogenate or lyophilisate contains a complex of biologically active substances that determine the therapeutic and prophylactic effect of the developed cream. These include proteins necessary for the construction and restoration of tissues; amino acids, of which significant quantities contain proline, lysine, threonine and glutamic acid, which contribute to the formation of collagen and elastin, healing of wounds; saturated and unsaturated fatty acids that activate metabolic processes; steroids that contribute to cell renewal, epidermis thickening, pore cleansing.

 Nucleic acids contained in drone larvae stimulate skin regeneration. In addition, phospholipids, glycolipids improve the delivery of active substances to the cells of the body, participate in the restoration of the lipid composition of cell membranes, changes that occur when metabolic processes are disturbed. The presence of steroid hormones in drone larvae determines the anti-inflammatory activity of the proposed ointment.

 Experimentally established pronounced anti-inflammatory effect of the proposed ointment.

 The anti-inflammatory activity of this ointment was studied using rat kaolin edema model. The experiments were carried out on white outbred rats obtained from vivarium Pyatpha, where they were kept under stationary conditions on a standard diet. Each group of animals in the experiment consisted of 6 rats weighing 170 ± 20.0. Inflammation was caused by the administration of 0.1 ml of a 10% kaolin suspension under the hind paw aponeurosis. The effect of the ointment on the second stage of inflammation was determined - exudation. Edema was evaluated oncometrically, its value was determined by the change in the volume of the legs, which was measured before the introduction of the flagogen, as well as 5, 24, and 48 hours after the introduction of a suspension of kaolin. The effectiveness of the developed composition was compared with the effectiveness of a 5% butadione ointment manufactured by Gendion Richter (Hungary).

 The first group of animals did not receive treatment, the second group was applied with Butadion ointment, the third with base, the fourth with Apilar-G ointment. The results are presented in the table. As follows from the results, Apilar-G ointment exceeds the biological activity of the prototype.

 The use of the claimed composition of the ointment will allow to organize the mass production of an inexpensive and effective therapeutic agent.

Claims (1)

A method of obtaining an ointment with anti-inflammatory effect, characterized in that it contains drone larvae as an active component, and polyethylene oxide-1500 gel as a base in a ratio of components, wt. %:
Paraoxybenzoic acid methyl ester - 0.30-0.50
Paraoxybenzoic acid propyl ester - 0.15-0.50
Drone larvae (in terms of dry matter) - 9.95-10.05
PEO-1500 - Up to 100.0

Images