Candles for the treatment of proctologic diseases

 

(57) Abstract:

The invention relates to medicine, namely to the pharmaceutical industry, and for candles, which can find use for the treatment of external and internal hemorrhoids and rectal fissures. The invention lies in the fact that the candles for the treatment of proctologic diseases contain herb extracts dense, excipient antiseptic and polietilenoksidnoy basis, according to the invention additionally contain dry oak bark extract, preservative and water clean, and as excipients - dimethylsulfoxide at a certain ratio of components, as polietilenoksidnoy basis candles contain preferably a polyethylene oxide m m 1500, or 3000, or 4000, or 6000, or mixtures thereof, or a mixture of these high molecular weight polyethylene oxides with a low molecular weight polyethylene oxide m 400 m. The invention provides a high therapeutic effectiveness of the proposed candles, while significantly (2-fold) decreased time to onset of therapeutic effect. 1 C.p. f-crystals, 2 tab.

The invention relates to medicine, in particular, to the manufacture of candles based on vegetable raw materials, which can find the growing interest in the use of medicinal plants, contain biologically active substances, in different dosage forms: in the form of tinctures, tablets, aerosols, ointments, and suppositories.

The use of medicinal plant raw material in the manufacture of drugs is associated with such properties as a broad spectrum of action, lack of toxicity, it is not scarce.

Known suppositories based on an extract of plant material for the Dimexidum and propolis, is described in the patent of Russian Federation N 2095074, "drug "Philipopolis-drug" and how to obtain it" (1).

According to the example of execution of the invention suppository contains: extract of yarrow in Dimexidum, propolis and polietilenoksidnoy basis, including high and low molecular weight polyethylene oxides (PEO) in the following ratio, wt. %:

An extract of the herb yarrow in Dimexidum - 15

Propolis - 15

The polyethylene oxide of high molecular weight 5000-7000 - 30

The low molecular weight polyethylene oxide 400 - 40

The process of obtaining a suppository in accordance with the above example is as follows.

The extraction is carried out rastitelnogo is racte dissolve propolis at 70-60oSince, then, it is filtered and dissolved PEO with molecular weight of 5000-7000 and polyethylene oxide with a molecular weight of 400. The resulting mass is mixed and Packed in containers. Suppozitornyj mass sterilized steam method at 90-95oC for 30 minutes

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. When this drug is in the form of a suppository get sterile and stable.

However, the use of suppositories is limited by the presence of bioveschestv propolis, which is associated with increased individual sensitivity of some patients to propolis and allergies to bee products.

In addition, the use of an organic solvent, in particular Dimexidum, to extract plant materials complicates the process of obtaining a medicinal product in the form of suppositories. For the extraction process requires special equipment, and installation of vapour recovery of organic solvent.

The closest similar Takasaki (2).

Known candle contains: extract of belladonna thick, phenol and the base - solid grease type C or Witepsol" with emulsifier T-2 or a mixture of oxides of molecular weight 1500 and 400 in the following ratio of components, g on one candle:

Option I.

The herb extracts thick - 0,01 - 0,02

Phenol - 0,0009 - 0,0019

Base - solid grease type C or Witepsol with emulsifier - 0,819 - 1,648

Option II.

The herb extracts thick - 0,01 - 0,02

Phenol - 0,0009 - 0,0019

The basis is a mixture of oxides of molecular weight 1500 and 400 - 1,049 - 2,108

The mixture of oxides contains PEO mol. mass 1500 in amount of about 80 to 98% and ROA mol. mass 400 in the amount of 2-10%.

Technology of production of candles on polietilenoksidnoy basis is as follows.

In molten at a temperature of 55-60oC PEO mol. m 1500 pour PEO mol. m 400, stirred until a homogeneous mass and injected molten phenol. The resulting mixture is stirred and enter prepared aqueous extract of the herb (ratio herb extracts: water 1:3). Suppozitornyj mass is thoroughly mixed and Packed candles.

Through the use of this technology aqueous extract of the herb, not the pain, anti-inflammatory and antispasmodic properties. However through the use of polietilenoksidnoy basis accelerates the release and absorption of biologically active substances herb.

The main therapeutic effect is known candles with herb extracts dense, in particular anti-inflammatory and antispasmodic, is determined by the presence of belladonna troyanovich alkaloids - giostsiamina and scopolamine. The main alkaloid - active giostsiamin selecting it from plants herb enters atropine, which has a pronounced anticholinergic (antispasmodic action.

However, the exacerbation of the inflammatory process in haemorrhoidal nodes and heavy bleeding known candles with herb extracts do not provide quick vasoconstrictor and hemostatic effect, which leads to longer time required for removal of the inflammatory process.

The objective of the invention is the creation of a new candle on the basis of extracts of plant materials having a high therapeutic effect with a broad spectrum of action while expanding Arsenal of suppositories used to treat proctological task is solved by as the candles containing herb extracts dense, excipient antiseptic and polietilenoksidnoy basis, additionally contain dry oak bark extract, preservative and water clean, and as excipients - sulfoxide in the following, wt. %:

The herb extracts thick - 2,3-3,0

The oak bark extract - 4,0-4,8

Dimethyl sulfoxide - 4,0-4,8

Preservative - 0,15-0,22

Purified water - 8,0-9,0

Polietilenoksidnoy basis Up to 100

As polietilenoksidnoy framework can be used high molecular weight PEO, selected from oxides (mol. m 1500, 3000, 4000, 6000, or mixtures thereof, or mixtures of these high molecular weight PEO with PEO mol. m 400. Given this property of oxides, as unlimited Miscibility of polymeranalogous of various molecular weights, their quantitative content was determined experimentally, taking into account its density and create a spark of good consistency.

Studies on selection of optimal variants polietilenoksidnoy basis showed that the best results by indicators such as the appearance of the candle, the stability, uniformity and consistency were the PEO molecular mol. m 4000 - 98% and low molecular weight PEO mol. m 400 - 2% or a mixture of high molecular weight PEO mol. m 6000 - 90%, 4000 - 20% and 1500% to 20%.

Taking into account that one of the components of the composition of the candles is purified water in the amount of 8.0, and 9.0 wt.%, which is necessary to dissolve the extracts of oak bark and herb.

The additional introduction of the candles of oak bark extract, containing tannic compounds, provides hemostatic and sosudosuzhayushcheye action, thereby amplifies the inflammatory and analgesic effect. Biological activity of tannins is that they penetrate into the intercellular spaces and associated proteins, enzymes, causing a local inflammatory reaction. This results in the dense film aluminates, relieves inflammation, and pain (3).

It is the presence of biologically active substances of oak bark extract and herb extracts dense together with dimethylsulfoxide provides amplification therapeutic effects: anti-inflammatory, analgesic and antispasmodic.

Experimental studies on optimal quantitative content of extracts of plant sys.% leads to a decrease in therapeutic effect. The increase in the content of herb extracts thick more than 3.0 wt.% leads to an increase in the concentration of atropine is the main biologically active substances herb. The high content of the active component may cause side effects: increased heart (tachycardia), pupillary constriction, dizziness.

The content of the extract of oak bark more than 4.8 wt.% leads to uneven distribution of this component in the candle mass. The mass becomes more dense, which violates the technological process of manufacturing of candles.

The additional introduction of the spark dimethyl sulfoxide has anti-inflammatory, local anesthetic and antiseptic.

Unlike phenol (in the prototype is used as an antiseptic), which when injected into the blood have General toxic action, dimethylsulfoxide non-toxic, highly penetrating (penetrating) capacity, accelerating the absorption of mucous biologically active substances-extracts of oak bark and herb.

The decrease in the content of dimethyl sulfoxide below 4.0 wt.% leads to deterioration of therapeutic effect and the increase of more than 4.8 wt.% impractical because therapeutic effect of the way. The water content within the specified limits provides a good dissolution of the dry extract of oak bark and herb extracts dense and contributes to their uniform distribution in the candle mass and simultaneously supports a certain density.

Change the content of purified water (less than 8.0 wt.%) leads to incomplete dissolution of the dry extract of oak bark, which violates the manufacturability of candles. High water content (more of 9.0 wt.%) may cause deterioration of the stability of candles during storage. In addition, candles soften and lose their marketability.

As preservative can be used nipagin, nipazol or a mixture thereof, sorbic acid and other permitted for use in medicine. The introduction of the proposed candles preservative in the amount of 0.15-0.22 wt.% is sufficient to prevent the growth of microorganisms and achieve microbiological purity in accordance with the requirements of EOF on microbial purity.

Effective selection of the ratios of components allowed us to obtain new candle on the basis of extracts of oak bark and herb, with a high therapeutic effect is anti-inflammatory, local anesthetic, spasma the ECCA get spark when used as the basis of high molecular weight polyethylene oxides are melting and at a temperature of 55-60oWith stirred until a homogeneous polietilenoksidnoy basis.

When using as the basis of a mixture of high molecular weight polyethylene oxide, PEO mol. weight of 400 first melt of high molecular weight PEO, and then injected liquid polyethylene oxide mol. m 400. The further process is carried out on the total of the developed technology.

In the resulting polietilenoksidnoy mass bred calculated the amount of preservative and dimethyl sulfoxide.

Then, the resulting mixture was added pre-dissolved in purified water extract of the herb dense and dry extract of oak bark. The ratio of water and extract of plant materials is 1:3, respectively. The resulting mass is stirred at a temperature of 50-60oC to obtain a homogeneous structure.

The resulting mass is fed to the formation of the candles by the method of pouring. Candles are packaged in blister packaging made of PVC film.

Examples of specific performance of the proposed candles for the treatment of proctologic diseases are presented in table 1.

To study the quality of the candles on the basis of extracts of oak bark and herb thick during storage is their quality. It was found that they retain their original properties within 1 year 5 months (on the date 10.12.99 further observations are made).

Clinical trials offer candles were conducted on samples in accordance with table 2.

Candles containing extracts of oak bark and dense herb, has been used to treat acute and chronic hemorrhoids, as well as in the postoperative period after hemorrhoidectomy.

Declare candles were used in 15 patients for the treatment of acute hemorrhoids in age from 30 to 55 years and in 15 patients with chronic hemorrhoids. The control group comprised 20 patients (12 chronic hemorrhoids and 8 sharp) at the age from 31 to 60 years, the treatment of which was made of known candles with herb extracts thick (polietilenoksidnoy basis).

Candles were applied 3 times a day for 7 days. Evaluation of effectiveness was based on subjective data and the clinical picture in the dynamics on the following parameters: the subsidence of the pain, cease the discomfort, itching, burning sensation in the anal area and bleeding.

The results of treatment are presented in table 2.

Analysis of the results of treatment offered candles the t after the introduction of candles and continuing up to 3 hours and relieve the discomfort, itching and burning after 10-15 minutes. In acute hemorrhoids cessation of bleeding occurred after 2 days in contrast to the control group, where therapeutic effect occurred at 4-5 days. The remaining patients of these groups have survived the effects of the inflammatory process, although significantly reduced itching and burning sensation in the anal area.

Patients from the control group were further used candles on the basis of extracts of oak bark and herb dense, with a positive effect came in 2 days, 7 patients out of 9 patients.

Clinical trials allowed us to draw the following conclusions:

- offer candles can be used in medical practice and are effective in the treatment of proctologic diseases, in particular acute and chronic hemorrhoids;

candles are well tolerated by patients and non-toxic;

- allergies and other side effects in the treatment of candles is not marked.

In addition, the use of non-deficient plant materials for the manufacture of candles makes them the best production in an industrial environment and provides an opportunity to expand the range of medicines for use in proctology.

Sources informaltable Prof. N. N. Maximinoi. Kiev "Health", 1985, S. 106-107.

1. Candles for the treatment of proctologic diseases containing herb extracts dense, excipient antiseptic and polietilenoksidnoy base, characterized in that they additionally contain dry oak bark extract, preservative and water clean, and as excipients - sulfoxide in the following ratio, wt.%:

The herb extracts thick - 2,3 - 3,0

Dry extract of oak bark - 4,0 - 4,8

Dimethyl sulfoxide - 4,0 - 4,8

Preservative - 0,15 - 0,22

Purified water - 8,0 - 9,0

Polietilenoksidnoy basis Up to 100

2. Candles under item 1, characterized in that as polietilenoksidnoy bases they contain polyethylene oxide m m 1500, or 3000, or 4000, or 6000, or mixtures thereof, or mixtures of these high molecular weight polyethylene oxides with a low molecular weight polyethylene oxide m 400 m.

 

Same patents:

The invention relates to the field of medicine and relates to biologically active agents tonic action

The invention relates to pharmacology, namely the radioprotective tonic, anti-inflammatory and bio-stimulant drug increases the immunological reactivity

The invention relates to medicine, namely to methods of treatment of vibration disease, in particular from the effects of local vibration

The invention relates to medicine, namely to methods of transplantation of fetal liver cells in the experiment

The invention relates to medicine, namely the pharmaceutical industry and relates to a medicinal product for the treatment of proctologic diseases

The invention relates to medicine, specifically to conservative methods of treatment of trophic ulcers of venous origin
The invention relates to chemical-pharmaceutical industry, medicine and relates to integrated natural drug "Postopen and method of its production

The invention relates to an external preparation for topical application, in particular to the outer local drug use, containing as activitiesthese substance 2-amino-2-(2-(4-octylphenyl)ethyl)propane-1,3-diol or its pharmaceutically acceptable acid salt additive

Rectal tool // 2152204
The invention relates to medicine and pharmaceutical industry and for the creation of new drugs used for the treatment of acute and chronic prostatitis

The invention relates to medicine, namely the pharmaceutical industry and relates to a medicinal product for the treatment of proctologic diseases
The invention relates to medicine, technology of medicinal forms with bacterial drugs
The invention relates to the pharmacy, the pharmaceutical form of human recombinant interferon Alfa-2 - rectal and vaginal suppositories

The invention relates to medicine, namely to Virology, immunology, gynecology and pharmacology
The invention relates to medicine
The invention relates to chemical-pharmaceutical industry, medicine and relates to integrated natural drug "Postopen and method of its production

The invention relates to the formulation of new drugs and methods of treatment of bacterial and viral infections and can be used in pharmacology and medicine

The invention relates to the perfume industry, namely the production of biologically active and flavors from vegetable raw materials and cosmetic products
The invention relates to medicine, in particular to neuralgia, and for the treatment of multiple sclerosis
Up!