RU2088214C1 - Balsamic agent for local application with antimicrobial, antiinflammatory and analgetic action - Google Patents

Abstract

FIELD: medicine. SUBSTANCE: main ingredients of balsam are biologically active substances and gel-forming composition. As biologically active substances used are bornyl or isobornylacetate, α-pinene, camphor, salicylic acid or sodium salicylate, and benzyl alcohol and copper sulfate. Gel-forming base contains distilled water, glycerin, ethanol, or isopropanol and blockcopolymer of oxide of ethylene and propylene. EFFECT: higher ANTIMICROBIAL, antiinflammatory and analgetic efficiency. 1 tbl

Description

 The invention relates to medical pharmacy, namely to balsamic agents for local (external) use, affecting the sensitive nerve endings of the skin and subcutaneous tissues. The proposed tool also has antimicrobial, anti-inflammatory and analgesic effects.

 Known balms "Tiger" and its domestic substitute "Gevkamen", the Vietnamese "Golden Star" and others (Mashkovsky MD Medicines. M. Medicine, 1993, v. 1, p. 401 407). Foreign balms contain scarce essential oils of tropical and subtropical plants, and in the complex compositions of the latter, along with the main ingredients, there are a number of minor, whose therapeutic benefit is problematic. The easily oxidized Karen contained in some oils can irritate the skin ten times more strongly than other terpenes, which sometimes provokes allergies and dermatitis. The development of adverse reactions with the use of the Golden Star balm is described (Yarkov VV Yarkova RD Vestnik dermatologii, 1988, N 9, p. 60). Balsamic preparations are usually prepared on a greasy or paraffin base, it is difficult to rinse off, they can stain clothes and leave stains on the tissues.

 A hydrophilic-based agent is also known, but it is too exotic in the composition of essential oils, and karen are also present in the latter; gelling agents are polyoxyethylated esters of stearyl, palmitic, oleic, cetyl and lauric alcohols (Petraglia A.G. Swedish Pat. N 343759, publ. 20.03.72). The previously patented emulsion containing instead of essential oils separate, obviously useful ingredients, including isobornyl acetate (Klemm T. et al. Pat. GDR. N 75368, published 12.08.70), is prepared on a relatively toxic substance chloromethylene, the presence of which in air in an amount of 8 mg / l causes nausea (Lazarev N.V. Harmful substances in industry. M. L. Chemistry, 1965, v. 1, p. 177).

 Among the balsamic preparations obtained from monoterpenoids of taiga conifers, turpentine ointment and pichtanol are most known, having a limited scope, mainly as distractions.

Turpentine ointment, Unguentum Terebinthinae (Mashkovsky M.D. see above) contains 3-karen, it is present in the gum pine turpentine in an amount of 30 and even after purification by distillation of the fractions to 170 ^o C remains one of the components of the "purified" turpentine (GF X, s. 491). This ointment is prepared on a basis containing pork fat, or on a water-petrolatum base using a T-2 food emulsifier (FS 42-403-72), it is not resistant enough, if the storage rules are violated, it stratifies and contains the products of the emulsifier decomposition.

 The closest analogue of the invention is pichtanol, Pichtanolum (VFS 42-2110-92). But this tool is an easily spreading flammable liquid. In pihtanol, 80 consisting of fir oil, 3-karen is also present, the content of which in fir oil reaches 15 (Poltavchenko Yu.A. Chem. -Pharm. W, 1981, N 3, p. 52 55). The composition of pihtanol also includes camphor, salicylic and formic acids, ethyl alcohol. When using pihtanol allergic reactions, dermatitis were observed.

 The objective of the invention is the expansion of the range and scope of domestic balsamic products while reducing its toxicity and improving consumer properties.

The problem is solved by obtaining a balsamic agent consisting of a hydrophilic base and individual biologically active and auxiliary substances introduced into it, and the following are applied:
as biologically active monoterpenoids, the most important component of fir oil is bornyl acetate or the stereoisomeric ether replacing it - isobornyl acetate, α-pinene, camphor;
as other biologically active balsamic components - salicylic acid or sodium salicylate;
as excipients, copper sulfate and benzyl alcohol;
as a basis, a gelling composition comprising ethyl or isopropyl alcohol, glycerin, a block copolymer of ethylene oxide and propylene oxide (GDPE-107) and distilled water,
in the following ratio of components, wt.

Bornyl or isobornyl acetate 5.0 15.0
a-pinene 3.0 6.0
Camphor 3.0 5.0
Salicylic acid or sodium salicylate 1.0 2.0
Copper sulfate (pentahydrate) 0.1 0.2
Benzyl alcohol 2.0 4.0
Ethyl or isopropyl alcohol 5.0 8.0
Glycerin 2.0 3.0
Block copolymer (GDPE-107) 25.0 -30.0
Distilled water up to 100
The proposed tool, received the conventional name "Taiga Balm", is a non-fluid, transparent green gel with a balsamic odor, stable during storage. This gel does not contain, in contrast to pichtanol, such strong allergens as karen. Side effects in its application have not been established, and the possibilities of use have been more diverse.

 Unlike expensive and scarce fir oil obtained occasionally in semi-artisanal furnaces, isobornyl acetate can be produced as a semi-product of camphor production, on a factory scale, from more affordable wood-chemical raw materials. It is proved that, similarly to bornyl acetate, it has a pronounced bactericidal effect against staphylococci and streptococci.

 a-Pinene is an integral part of many essential oils, turpentine and balsamic drugs; The therapeutic role of camphor is also well known; these monoterpenoids have long been used along with salicylates in medical practice.

 Benzyl alcohol serves as an auxiliary hydrotropic additive that improves the solobilization of terpenoids and stabilizes the gel. It expands the antimicrobial spectrum of the balm and at the same time enhances its analgesic properties (in Western European medicine, benzyl alcohol was used along with novocaine for local, surface anesthesia).

 The auxiliary role of copper sulfate supplementation is to enhance the antiseptic and “astringent” properties of the balsam and to give it, as a result of a color reaction, a characteristic color. As a trace element, copper is part of the skin of humans and animals and is involved in the most important enzymatic reactions of tissue metabolism.

 The developed composition relieves suffering from neuralgic pains, arthritis, radiculitis, lumbago and rheumatoid ailments, but is also applicable as a massage agent for muscle and ligament sprains, colds, external staphylococcal skin lesions, boils, minor burns, minor household injuries, bites insects, headaches. It is well distributed on the skin, unlike adhesive or oily, balsamic products staining clothes, it can be applied, for example, under dressings and stockings, and if necessary can be easily washed off with water, since the block copolymer has surface-active properties. The healing qualities and ease of use of the proposed gel are its undeniable advantages over such a relatively toxic caustic liquid like Pichtonolum.

 The anti-inflammatory and therapeutic efficacy of an indifferent balsamic agent turns out to be the highest within the range of terpenoids of approximately 15 to 20, probably due to the fact that toxicity increases with their higher content (the gel stability also worsens). A lower content of terpenoids leads to a weakening of the healing and rheological properties of the gel.

 Examples of composition are given in the table.

 The variant of example 1 is more suitable in the treatment of rheumatoid ailments (since in this case the balm contains slightly more irritants, pinene and camphor), and the variant of example 3 for the treatment of boils (since in this case the balm contains more terpenoid esters that exhibit a bactericidal effect in against staphylococci). Optimal for balsamic products with a wide profile is the variant according to example 2.

 An example of obtaining a balsamic remedy.

 Suppose you want to cook 1 kg of "Taiga Balm" according to the best option (example 2 composition).

 A portion of the HDPE-107 block copolymer 280.0 g is melted in a beaker in a water bath and mutually dissolved monoterpenoids and benzyl alcohol are introduced into the melt: 30.0 g of camphor, 52.4 ml of α-pinene (density 0.858), 101.5 ml of isobornyl acetate (density 0.985), 33.6 ml of benzyl alcohol (density 1.042), and then pour it with stirring with a previously prepared alcohol-water solution containing also salicylic acid (or sodium salicylate) and copper sulfate (salicylates 15.0 g, copper pentasulfate 2.0 g, ethyl alcohol 76.0 ml (density 0.789), glycerol with a density of 1.260, 18.3 ml, distilled water 410.0 ml). When mixed, glass transition occurs and a gel forms.

 In the same way, in the case of using bornyl acetate and, for example, instead of ethyl alcohol, isopropyl alcohol, the densities of which differ only in the third digit, in this case, when preparing small amounts of balsamic remedy, the measured volumes of its ingredients are almost equal. So, for example, when using 99.6 chromatographic purity bornyl acetate, whose density is 0.986, its volume for preparing 1 kg of the product will be 101.4 ml, and the volume of isopropyl alcohol with a density of 0.785 will be 76.4 ml. In the preparation of large quantities of balsamic funds in the calculations are made appropriate refinements.

 Similarly to the above, but taking into account other ratios of the ingredients, receive funds according to examples 1 (5.0 terpenoid ethers) and 2 (15.0 terpenoid ethers).

 Examples of therapeutic use of "Taiga Balm".

 Suppose, there was a need to apply a balm to alleviate suffering in arthrosis or osteochondrosis. To do this, it is better to use the compositions according to examples 1 or 2, which are applied in a thin layer in the area of pain (joints of the limbs, various parts of the spine) and rubbed into the skin for 3-5 minutes with massage movements. Then it is advisable to insulate the places for applying the balm with bandages. The course of treatment is 10 days.

 In the treatment of furunculosis, it is better to use the compositions according to examples 2 or 3, lubricating them with the affected areas until complete healing. The same compounds are suitable as disinfectants and itching, for example, for mosquito bites.

 For colds (cough, runny nose, headache), the compositions of examples 2 or 3 are used, lubricating them in the nose, rubbing temples, chest, back, with repeating procedures 3-4 times a day. It is also recommended to lubricate the feet and do hot foot baths at night.

 For small wounds, burns, use the compositions of examples 2 to 3, applying them to previously cleaned and washed damaged areas with a thin layer, followed by a dressing. The course of treatment is about 15 days.

 "Taiga Balm" is a persistent, convenient remedy for storage and transportation. Under appropriate conditions (room temperature, a place protected from light), it is guaranteed to remain for at least 12 months from the date of manufacture.

 As follows from the foregoing, the proposed balsamic product is characterized by accessibility, ease of manufacture, durability, relatively low toxicity, a variety of possibilities for effective therapeutic use, ease of storage and use.

Claims (1)

 Topical balsamic drug with antimicrobial, anti-inflammatory and analgesic effects, including monoterpinoids, camphor, salicylates, excipients and a base, characterized in that it contains boron or isobornyl acetate and α-pinene, salicylic acid or salicylates sodium, as auxiliary substances, benzyl alcohol and copper sulfate pentahydrate, as a base a gel-forming base from a block copolymer of ethylene oxide and ilena (GDPE-107) and water-ethanol-glycerol mixture at a ratio of components, wt. Bornyl or isobornyl acetate 5.0 15.0
α - Penene 3.0 6.0
Camphor 3.0 5.0
Salicylic acid or sodium salicylate 1.0 2.0
Benzyl alcohol 2.0 4.0
Copper sulfate pentahydrate 0.1 0.2
Gelling base

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