Ointments, analgesic, anti-inflammatory and antispasmodic action

 

(57) Abstract:

The invention relates to medicine, in particular to pharmacology, and can be applied in proctology for the treatment of hemorrhoids and fissures of the rectum. The invention lies in the fact that the ointment contains dry extract of oak bark extract, herb dense and optionally glycerin, preservative, emulsifier and purified water, polyethylene oxide of high molecular weight and low molecular weight with a specific ratio of components, the high molecular weight polyethylene oxide ointment contains polyethylene oxide mol.m. 1500, or 3000, or 4000, as well as low molecular weight polyethylene oxide - polyethylene oxide mol. m 400. The invention provides for an expansion of the range of medicines on the basis of available and non-deficient plant materials. The ointment has a high quality performance is stable during storage, it has a uniform consistency with a good light ability. 1 C.p. f-crystals, 1 table.

The proposed ointment relates to the field of medicine, in particular to pharmacology, medicinal plant-based raw materials and can be applied in proctology, namely for the treatment of hemorrhoids and fissures of the rectum.

Naracoorte interest in the use of medicinal plants, containing biologically active substances.

Compositions containing biologically active substances derived from plant materials, have broad-spectrum, non-toxic and when used there are fewer allergic reactions.

In modern medicine, extracts of plant materials used in various pharmaceutical forms such as tinctures, tablets, sprays, and ointments.

The closest composition together existing signs to the proposed ointment is an ointment that is described in the patent N 2095074 "drug "Philipopolis-drug and method thereof", which is selected as a prototype (1).

In accordance with example 2 of the enforcement of this invention ointment contains extracts of vegetable raw materials in an organic solvent, propolis and polietilenoksidnoy basis, including high and low molecular weight polyethylene oxides in the following ratio, wt. %:

The extract of plant materials in absolute Dimexidum - 5-15

Propolis - 5-15

The oxides of high-molecular - 10-30

The oxides of low-molecular - 100

As high-molecular-weight polim - the oxides mol. m 200-400.

The technology for this ointment consists of the following stages.

1. Extraction of plant materials Dimexidum in the ratio of 10:1, respectively, at a temperature of 100-90oC;

2. The resulting extract was dissolved propolis at 70-60oC;

3. In filtered dioxide extract plant materials and propolis dissolved polyethylene oxide grades 3000-4000 and polyethylene oxide 400 brand;

4. After mixing the product Packed in the packaging;

5. Ointment sterile steam method at a temperature of 90-95oC for 30 minutes

6. As a vegetable raw material for ointments use the herb St. John's wort.

Dimexide together with dissolved in it bioveschestv plants and propolis well penetrates through the skin and mucous membranes without damage to the latter, showing a therapeutic effect.

However, according to the "Instructions for use Dimexidum" (Approved by FC M3 USSR 16.06.72, its use is contraindicated in pregnancy, severe lesions in parenchymal organs (especially the liver), angina, comatose States, myocardial infarction, severe atherosclerosis, various forms of stroke.

In addition to these disadvantages of the known ointment, technology of its receipt is complicated by the fact that it is necessary to carry out the sterilization ointment steam method at high temperature. Exception this operation from the process will not allow you to get sterile and stable drug.

To eliminate the above disadvantages of the task was to create a new ointment on the basis of extracts of plant materials with high quality while expanding the range of ointments with a broad spectrum of action, and the possibility of its application to a wide range of patients for the treatment of proctologic diseases, including hemorrhoids and rectal fissures.

The problem is solved by the proposed ointment, analgesic, anti-inflammatory and antispasmodic effect, containing extracts of plant materials and polietilenoksidnoy basis, including high - and low-molecular-weight polyethylene oxides, according to the invention as extract vegetable cheese is alligator and purified water in the following ratio of components, wt. %:

Dry extract of oak bark - 3,0-5,5

The herb extracts thick - 3,0-5,0

Glycerin - 3,5-4,5

Preservative - 0,17-0,23

Emulsifier - 4,5-5,5

The high molecular weight polyethylene oxide - 27,0-32,0

The low molecular weight polyethylene oxide - 38,0-42,0

The optimal effect of the painkiller, anti-inflammatory and antispasmodic actions ointment is provided by the integrated action of active ingredients: oak bark extract and herb extracts dense in combination with polietilenoksidnoy basis (PEO).

The oak bark extract with a high content of tannins, has astringent, anti-inflammatory and hemostatic effect. The best results of therapeutic action of the extract of oak bark is achieved when its content in the ointment, is 3.0 to 5.5 wt.%; when the content below 3.0% reduced healing effect, and it increased more than 5.5% violates technology for the production of ointments due to insufficient amount of water needed for complete dissolution of oak bark extract, thus improve therapeutic effect is not observed.

The major biologically active substances belladonna (belladonna) are Troyanova alkaloids - giostsiamin and scopolamine. Of them perehodit in atropine, which is the main representative of anticholinergic substances (2).

Therefore, the herb extracts dense along with analgesic and anti-inflammatory effect and has a pronounced anticholinergic (antispasmodic action.

It is the presence of these biologically active compounds in the herb extracts and determines its pharmacological action: decreases spasm of smooth muscles, namely the rectum.

As a result of studies on the optimal quantities of herb extracts thick, it was found that its content is less than 3 wt. % leads to deterioration of therapeutic effect, and the content of more than 5.0 wt. % leads to an increase in the concentration of atropine is the main biologically active substances herb extracts. An overdose of this active component can cause side effects: increased heart (tachycardia), pupillary constriction, dizziness.

Thus, the presence in the composition of ointments herb extracts possessing analgesic and antispasmodic effect, and oak bark extract, has good hemostatic and strong tanning action, the result of which is summarized Oia, as hemorrhoids.

Use as part of the proposed as the basis of water-soluble polyethylene oxides with molecular weights of 400, 1500, 3000, and 4000 promotes the penetration of active component of biologically active substances in extracts of oak bark and herb through the cell membrane, because the basis has a high osmotic activity and provides sulemaniyah effect on tissue inflammation.

In addition, the high solubility of PEO in water and its ability to dissolve hydrophilic drugs promotes uniform distribution of the extracts in the basis.

The quantitative content of the high - and low-molecular-weight PEO was determined experimentally based on their density and the creation of ointments good consistency.

Introduction PEO m m 400 less 38,0 wt.% reduces the degree of dissolution of biologically active substances in extracts of oak bark and herb extracts dense, resulting in reduced therapeutic effect, and more than 42 wt.% - affects the consistency of the ointment. The ointment becomes "fluid" and badly kept in inflammation.

Optimal quantitative content of PEO m m 1500, or 3000, or 4000 allows you to get may in the composition of ointments glycerin improves elasticity and protects against drying, because of its high hygroscopicity. This property of glycerol can be used as a moisturizing component.

The change of the proportion of the amount of glycerin in the direction of increase or decrease from the optimal value leads to deterioration of quality indicators ointments, namely deteriorating its light ability and the uneven distribution of herb extracts in basis.

The best results are achieved when the content is equal to 3.5 to 4.5 wt. %.

As the emulsifier can be used such well-known emulsifiers as tween-80 (Polysorbate-80), span-80 (product of esterification of sorbitol with oleic acid), natrocarbonatite cellulose, etc. used to obtain ointments.

Laboratory studies have shown that the best results by indicators such as stability, consistency, uniformity of distribution of active ingredients were obtained when the content of the emulsifier in the amount of 0.17-0.23 wt. %.

The introduction of emulsifier in combination with glycerin allows obtaining ointment with a high stability and a uniform distribution of biological active substances exmatriculated sodium, salicylic acid and other permitted for use in medicine.

The introduction of the proposed ointment preservatives in the amount of 0.17-0.23 wt. % is sufficient to prevent the growth of microorganisms and achieve microbiological purity.

Thus, the use of an extract of plant materials dry oak bark extract and herb extracts dense in combination with polietilenoksidnoy basis, glycerine, emulsifier and preservative allowed to obtain a new composition of ointments, analgesic, anti-inflammatory and antispasmodic effect, which can find application in proctology, in particular for the treatment of hemorrhoids and fissures of the rectum.

The selected ratio of the components of the ointment are the best and provide effective therapeutic effect and high quality indicators - ointment stable during storage, it has a uniform consistency with a good light ability.

The technology of obtaining the proposed ointment is as follows.

In the reactor melt the calculated amount of high molecular weight polyethylene oxide selected from PEO mol. m 1500, 3000, or 4000, enter PEO mol. m 400, d mixture of oxides bred calculated the amount of preservative. At a temperature of 50-60oC mix glycerin and emulsifier, and the resulting mixture was added dissolved in purified water extract of the herb and oak bark extract. When the ratio of water and extract is 1:3, respectively. The resulting mixture was mixed and injected into the previously prepared polietilenoksidnoy base at a temperature of 50-60oC. the Mass is stirred, while controlling its homogeneity. Then the weight with the help of the pump serves for filling in tubes.

The resulting ointment has a very low odor and color from light brown to dark brown.

The table below shows examples of the implementation of the claimed invention.

To study the quality of the claimed ointment were conducted laboratory tests during storage at a temperature of 16 - 22oC. the results of the analysis showed that all samples retain their original properties within 1 year (ointment stable, not stratified, homogeneous, organoleptic parameters unchanged). This term is not limiting, monitoring is ongoing.

Clinical study designed ointment was held at the city hospital N 40, Nizhny Novgorod.

All were treated 30 patients ranging in age from 23 to 56 years, with an acute form of hemorrhoids 1-3 degrees were 7 patients, the postoperative period is 13 and with chronic hemorrhoids, accompanied by pain and bleeding - 10.

The ointment was applied by the method of application on external hemorrhoids and introducing into the lumen of the rectum chronic period special tip-cannula, developed in the laboratory LLC pharmcomplect" (application for invention N 97118926/14, a positive decision from 16.02.99 year). This cannula allows painless to enter the ointment into the rectum internal hemorrhoids.

In acute and chronic forms of hemorrhoids ointment was applied 3 times daily at a dose of not more than 2 grams per day, in the postoperative period, 2 times a day.

Evaluation of effectiveness was based on subjective data and the clinical picture in the dynamics on the following parameters: analgesic, anti-inflammatory and spasmolytic effect, the tolerability of the drug, allergic reactions, toxicity.

The comparison was conducted with a control group of patients whose treatment was conducted imported ointment "Proctosedyl", which is produced by the firm "P is positive therapeutic effect of the application of the ointment on the basis of extracts of oak bark and herb dense acute and chronic forms of hemorrhoids, manifested in the subsidence of the pain syndrome in 5-10 minutes, and the withdrawal of acute inflammatory process in 2-3 days faster than when applying the ointment "Proctosedyl".

The application of the proposed ointment in the postoperative period also confirmed a positive therapeutic effect on clinical recovery occurred on the 5 - 6th day, when using the ointment "Proctosedyl" - 7 - 9 day. None of the 13 cases there was no suppuration of postoperative seams, sharp paraproctitis, swelling of the perianal skin.

When combined chronic hemorrhoids application of the proposed ointment in 1-2 days stopped the bleeding and discomfort in the anus.

The ointment is well tolerated, non-toxic, does not cause General and local allergic reactions that will allow her to apply for the treatment of proctologic diseases, including hemorrhoids, a wider range of patients.

Thus, the proposed ointment can be used in medical practice, extending the range of ointments based on vegetable raw materials.

It should be noted that the proposed composition of the ointment includes such ingredients as dry extract cor> Furthermore, the method of obtaining the claimed ointment is quite simple and requires no special equipment compared to the prototype, where it is necessary to carry out the sterilization ointment steam method.

Industrial production of low-cost, but highly effective ointment on vegetable raw materials makes it accessible to a wide network of medical institutions.

Sources of information:

1. EN 2095074 C1, 10.11.97.

2. Kuznetsova, M. A. Medicinal plant raw materials and products. M: "High school", 1987, S. 138 - 140.

3. Convoluta ointment "Proctosedyl" manufactured by "Russell India limited, India, 1997.

1. Ointments, analgesic, anti-inflammatory and antispasmodic action, containing the extract of plant materials and polietilenoksidnoy basis, including high - and low-molecular-weight polyethylene oxides, characterized in that the extract as plant materials, it contains dry extract of oak bark and herb extracts thick and optionally glycerin, preservative, emulsifier and water purified in the following ratio, wt.%:

Dry extract of oak bark - 3,0 - 5,5

The herb extracts thick - 3,0 - 5,0

Glycerin - 3,5 - 4,5

Emulsifier - 4,5 - 5,5
regular - 38,0 - 42,0

Purified water - the Rest

2. Ointment under item 1, characterized in that as high molecular weight polyethylene oxide it contains polyethylene oxide mol.m. 15000, or 3000, or 4000, as well as low molecular weight polyethylene oxide - polyethylene oxide mol.m. 400.

 

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