Symptomatic drug to relieve pain and fever (options)

 

(57) Abstract:

The tool is made in the form of rectal suppositories. The product contains the active substance with a pronounced analgesic, antipyretic and anti-inflammatory effect - analgin in the number of 0,09-0,11 or 0,225-0,275 g for one suppository and base. The basis is a confectionery fat solid based on plasticized hydrogenated fat or mixture of triglycerides of natural dietary fatty acids (C12-C18with mono - and diglyceride of these acids. New dosage form provides relief of various pains and fever with influenza, rheumatism, in the postoperative period and accelerates the healing effect due to the rapid receipt of medicinal substance in the blood. 2 S. p. f-crystals, 6 PL.

The invention relates to medicine, in particular, to medicines and can be used in the manufacture of rectal suppositories to relieve pain of different origin in children (headache, neuralgia, radiculitis, myositis), febrile States, influenza, rheumatism, in the postoperative period.

As analgesics, antipyretics and anti-inflammatory drugs for the treatment of the other substances derived pyrazolone - antipyrine and dipyrone.

Representative of this group, analy, has a pronounced analgesic, antipyretic and anti-inflammatory action.

Because symptomatic drug to relieve pain and fever containing analgin and auxiliary substances (sugar, potato starch, calcium stearate, talc), produced in the form of tablets with a dose of dipyrone of 0.05, 0.1 and 0.15 g for children, is the closest to the technical essence and the achieved effect to the proposed facility and taken as a prototype (1), (2).

Analgin is highly soluble in water; rapidly absorbed from the gastrointestinal tract, especially when taken before meals and with alkaline solutions. Full antipyretic and analgesic effect develops after 1-2 hours, anti - 1-3 hours. Thus, analgin suitable for use in those cases when you need to quickly create a high blood concentration of the drug.

With long-term same treatment perhaps oppression blood (granulocytopenia, agranulocytosis); in this case it is necessary to periodically study the blood. Allergic reactions are possible, although the frequency of their substantially lower the RNA for children, therefore, analgin, as a symptomatic remedy for the relief of pains of different origin and feverish condition, finds wide application in pediatric practice.

However, the use of tablets causes difficulty, especially in children with high fever and vomiting, are in an unconscious state, with diseases of the upper gastrointestinal tract. In addition, given that children in the younger age a process of oxidative deamination of proteins in the liver is slowed down and with frequent doses (more than 4 times a day) in children possible accumulation and the appearance of intoxication, it is preferable to rectal administration of drugs, which would also avoid impacts on food preparation and acidic environment of the stomach.

The objective of the proposed solution is the creation of a medicinal product for relief of pains of different origin and feverish condition, containing the active substance with a pronounced analgesic, antipyretic and anti-inflammatory properties (analgin) in the form of rectal suppositories with high biological availability and accelerating the healing effect, which is especially important in pediatric pane pain and fever of two compositions, containing the active substance with a pronounced analgesic, antipyretic and anti-inflammatory effect - analgin and excipients. According to the invention the tool is made in the form of rectal suppositories and as excipients contains the base - solid grease type a or Witepsol in the following ratio of components, g:

1 composition

Analgin - 0,09 - 0,11

The basis is Sufficient to obtain the suppository mass (1.18 to 1.32 to) g

II composition

Analgin - 0,225 - 0,275

The basis is Sufficient to obtain the suppository mass (1.18 to 1.32 to) g

Suppozitornyj form promising and preferable for many medicines, particularly in pediatric practice, due to the speed of onset of therapeutic effect due to the rapid return of therapeutic substance from the basics and very fast it enters the blood due to the high absorption ability of the mucosa of the rectum. Drugs, administered rectally, contribute to the rapid achievement of high concentrations in their blood, changing their circulation in the blood line and loss of the barrier function of the liver.

Given the above, the dose for rectal administration of dipyrone Ena form is preferable to the other from the point of view of simplicity and obespechennosti the introduction and reduction of allergenic effects on the body, that is very important for children.

As a result of experimental studies have been developed suppositories with different dipyrone (2) : 1 - (0,09 - 0,11) g and II - (0,225 - 0,275) , Specified dipyrone determine the appropriate dosage depending on the age of the child and the nature of the disease.

The dipyrone less than 0.09 g (1 part) and 0,225 g (II) does not provide the desired therapeutic effect, i.e. reduce pain is not increased sweating, which is an important component in the mechanism of action of antipyretics (especially in children under 7 years old), does not decrease the inflammatory process. The dipyrone more than 0.11 g (1) and 0,275 (II) is unreasonably high, as therapeutic effect has been achieved; especially in case of prolonged use of excessive dosages of aspirin may cause adverse reactions.

The basis was chosen also experimentally in the process of identifying compatibility of dipyrone with different bases and exploring the impact of his basis in order to identify the best basis for its use in pediatric practice.

According to these criteria best are solid grease type and Witepsol.

Tallow the basis plasticized hydrogenated fat (without added emulsifiers).

Witepsol is a mixture of triglycerides of natural dietary fatty acids with C12- C18with a small amount of mono - and diglycerides of the same acids.

Data bases do not have irritating and absolutely harmless to the body, which is especially important for their application in Pediatrics, in addition, they are adaptable to production and are widely used as suppozitornoj bases.

The quantitative content of the framework was determined to create suppositories normal consistency, based on the required GF XI mass suppositories.

Due to different number of lay analgin weight suppositories corrigiola quantitative content basis.

Thus, for suppositories 1 structure content framework (1,09-1,21) g, II composition - (0,955-1,045) ,

Contents the basics beyond the specified ranges, violates the percentage compositions of the claimed suppositories and does not allow to achieve a therapeutic effect.

Contents fundamentals of less 1,09 g (1 part) and 0,955 g (II) contributes to the excess of the required therapeutic dose of dipyrone and difficulty of the technological process of manufacturing supposito the t is not reached.

Thus, the new symptomatic medication in the form of rectal suppositories, successful, combining in its structure a therapeutic substance with a pronounced analgesic, antipyretic and anti-inflammatory effect and the basis for the rapid flow of therapeutic substance into the blood, is the necessary drugs to control the pain of different origin (headache, neuralgia, radiculitis, myositis), febrile States, influenza, rheumatism, in the postoperative period, especially in pediatric practice.

Analysis of scientific-technical and patent information allows us to conclude that the proposed composition of the suppositories is new and meets the criterion of "inventive step".

Manufacturing technology claimed suppositories with dipyrone solid fat type And fat confectionery firm based on plasticized hydrogenated fat) or Witepsol (a mixture of witepsol grades N-15 and W-35 is as follows.

To prepare the concentrate analgin thoroughly mixed with a part of the pre-melted base and fray on three-wheel rubbing machine to obtain a product with dispersed temperature 38-40oC, under continuous stirring for 50-60 minutes until a homogeneous mass which is formed into suppositories by the method of pouring. In the molding process suppositories constantly maintain the temperature of 36-38oC. Packaging film PVC brand EP-73C.

To study the quality of the proposed suppositories and therapeutic effect were prepared 4 mixture components (table. 1).

Match the quality of the proposed suppositories requirements of the project VFS reflected in table 2.

Data storage suppositories the applicant is not currently available.

The test results of the proposed suppositories for microbiological purity in accordance with the global Fund XI, vol. 2, S. 193 reflected in table 3; declare suppositories have microbiological purity according GF XI, vol.2, S. 193.

The task of the pre-clinical study suppositories with dipyrone conducted by UNIATES, was to study the specific activity and safety in acute and chronic experiments.

On specific activity of suppositories judged by indicators analgesic and antipyretic actions. Analgesic activity was determined on the model to adscam cramps were 15 minutes after injection of acetic acid for 30 minutes. Suppositories with dipyrone (I-IV examples) at a dose of 1.4 g/kg (dose of aspirin 100 mg/kg) and 0.7 g/kg (dose of aspirin 50 mg/kg) was administered into the rectum for an hour before the injection of acetic acid. For comparison, were examined in the same doses analgesic activity of a solution of aspirin in the stomach and rectum.

The results of the analysis showed that the use of rectal suppositories (I-IV examples) is a clear analgesic effect, there is a strong dependence of the effect of the doses.

Antipyretic and anti-inflammatory suppositories radiated on the model of experimental fever, caused by injection under the skin of rats with 1.0 ml of 20% freshly prepared mixture of baking yeast. The maximum temperature rise was determined after 4-5 hours after administration of the yeast. Suppositories were studied at doses of 0.7-1.4 g/kg, which corresponds to the dose of the substance of 0.05-0.1 g/kg, respectively, was injected 3 hours after injection of yeast. From the presented data table 4 shows that the suppositories with dipyrone (I-IV) has antipyretic effect, causing a decrease in temperature (40,7-73,0)% and reduce the inflammatory process.

Establishing the safety of the proposed suppositories for children about>/P>Acute toxicity was studied on rats of both sexes weighing 70, Used suppositories (III-IV examples) at a dose of 11.2 g/kg, which corresponds to the dose of the substance of 2.0 g/kg Suppositories were administered in three doses with an interval of 45-60 minutes. Observation of animals were conducted within two weeks.

The results of the study showed that the proposed suppositories did not cause death.

The toxicity of the proposed suppositories investigated in rats of both sexes weighing 100-110, Suppositories (III, IV examples) was applied to the maximum dose of 1.4 g/kg for 4 weeks.

As control was used the solid confectionery fat dose of 1.15 g/kg

During the observation period, all animals remained alive. Their appearance, behavior, rats treated with suppositories with dipyrone, did not differ from the control group who received basis. Body weight also did not differ.

The influence of the proposed suppositories (III, IV examples) on the morphological composition of blood is presented in table 5.

When analyzing the indices of peripheral blood found that the hemoglobin level and the levels of leukocytes remained unchanged as in experienced, tavoy normal physiological limits changes in rats.

When examining the condition of the Central nervous system was observed a significant reduction of locomotor activity in rats treated with suppositories with dipyrone. Occurred statistically significant variations in the level of estimated and reflex reactions were observed both in the experimental and control groups. (see table 6).

Microscopic examination were taken out of the experiment by decapitation of the rats, which for months has introduced suppositories with dipyrone (I,IV examples), and control animals to them, which was introduced only solid confectionery fat, showed no visible deviations in the condition of the mucous membranes, woolen cover and internal organs.

Microscopic examination was exposed areas of the myocardium, lung, liver, kidney, adrenal, pancreas, gonads, spleen, rectum.

Conducted functional analysis of histostructure internal organs and tissues of rats experimental and control groups revealed no pathological changes in the research bodies.

Input rectal claimed suppositories have no irritant action on the mucous membrane of the rectum, a condition slizeobrazujushchej elements inflammatory action, are the most preferred form for children of different ages in the relief of pains of different origin and feverish condition.

Sources of information

1. VFS 42-3188-95 Tablets analgin

2. Mashkovsky M. D. Medicines. So 1. M.: Medicine, 1994, S. 200-201.

1. Symptomatic drug to relieve pain and fever that contains the active substance with a pronounced analgesic, antipyretic and anti-inflammatory effects - analgin and excipients, characterized in that it is made in the form of rectal suppositories and as excipients contains the confectionery fat solid based on plasticized hydrogenated fat or mixture of triglycerides of natural dietary fatty acids12-C18with mono - and diglycerides of these acids in the following ratio of components, g on one suppository:

Analgin - 0,09-0,11

This basis is Sufficient to obtain the suppository mass (1.18 to 1.32 to) g

2. Symptomatic drug to relieve pain and fever that contains the active substance with pronounced analgesic, antipyretic and anti-inflammatory effects of analg the ve auxiliary substances provides the basis of - confectionery fat solid based on plasticized hydrogenated fat or mixture of triglycerides of natural dietary fatty acids12-C18with mono - and diglycerides of these acids in the following ratio of components, g on one suppository:

Analgin - 0,225-0,275

This basis is Sufficient to obtain the suppository mass (1.18 to 1.32 to) g

 

Same patents:

The invention relates to pharmaceutical industry and relates to the establishment of the dosage form in the form of suppositories containing erythromycin

The invention relates to medicine, namely to pharmaceutical production, and for the creation of new dosage forms

The invention relates to medicine, namely to pharmaceutical production and for the creation of new dosage forms

The invention relates to medicine, namely to the pharmaceutical industry and relates to the creation of new dosage forms
Candles // 2119330
The invention relates to pharmaceutical industry and relates to candles containing human leukocyte interferon (CLI)

The invention relates to medicine, in particular to drugs, and can be used in the manufacture of suppositories for the treatment of purulent-inflammatory diseases in gynecology (Trichomonas colpitis, gonorrhea, purulent infection)

The invention relates to medicine and relates, in particular, pharmacology, namely rectally local anesthetic candles

The invention relates to medicine, in particular to drugs, and can be used in the manufacture of candles broad-spectrum

FIELD: chemical and pharmaceutical industry.

SUBSTANCE: the present innovation deals with creating medicinal preparations of plant origin and could be applied for treating functional constipations and affected biorhythm of defecation. It is suggested to apply either dry aqueous or aqueous-alcoholic extract of horse chestnut seeds of Aesculus species to prepare curative-prophylactic preparation in case of constipation and affected biorhythm of defecation. The suggested preparation should be applied in the form of powder, tablets or suppositories. Pharmaceutical composition for preventing and treating constipation and affected biorhythm of defecation contains an active substance out of medicinal plant and a pharmaceutically acceptable filling agent, moreover, this preparation is designed as suppositories and contains either dry aqueous or aqueous-alcoholic extract of horse chestnut seeds of Aesculus species and suppository hydrophobic foundation at certain content of ingredients. Dry aqueous or aqueous-alcoholic extract contains 1-50% active substance as escin. As foundation it could contain either cacao oil or vitepsol. The method for preventing and treating constipations and affected biorhythm of defecation deals with introducing the suggested pharmaceutical composition into patient's anus 5-15 min before planned act of defecation. Application of "Rectum-activ" preparation provides positive result at treating functional psychogenic constipation: in 5-15 min after introducing a suppository into anus pronounced urgency for defecation. In case of course therapy for 4 wk one should observe restoration of natural urgency for intestinal evacuation. Moreover, purgative preparation causes no unfavorable pain feelings.

EFFECT: higher efficiency.

10 cl, 6 ex

FIELD: pharmaceutical industry.

SUBSTANCE: rectal- and vaginal-administration suppositories contain 1,3-diethylbenzimidazolium triiodide as active principal, polyvinylpyrrolidone as solubilizer and stabilizer, and lipophilic base with specified proportions of components.

EFFECT: extended therapeutical activity and reduced occurrence of side effects.

4 cl, 2 ex

FIELD: medicine, gynecology, pharmacology, pharmaceutical industry.

SUBSTANCE: invention proposes a preparation that comprises bacterial mass of live microorganisms as an active component, protecting medium and fat base. The preparation comprises lactobacilli as bacterial mass and one or some eubiotic microorganisms taken among the following group: bifidobacteria, streptococci and lactococci taken in the amount per a single dose. Also, the preparation comprises additionally an acceptable sorbent and a biologically active supplement. Also, invention relates to a method for preparing this preparation that involves preparing firstly lactobacilli bacterial mass and one or some genus of eubiotic microorganisms taken among the following group: bifidobacteria, streptococci and lactococci. Then the prepared bacterial mass of microorganisms is immobilized on sorbent used in medicine in its ratio to bacterial mass of microorganisms = (9-1):(1-9) followed by addition of the protecting medium and biologically active supplement to formed mass in the necessary amount. Also, invention describes a method for prophylaxis and treatment of bacterial vaginitis that involves intravaginal administration of the preparation described above in the amount 1-3 doses, 1-3 times per 24 h. The treatment course is prescribed individually. Invention provides expanding assortment of agents used for treatment of bacterial vaginitis. Invention can be used in obstetric-gynecological practice.

EFFECT: improved method for vaginitis treatment, valuable medicinal properties of preparation.

13 cl, 4 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: means has dibunol, 15% oil extraction of propolis, gelatin, glycerol and treated water taken in known component proportion.

EFFECT: enhanced effectiveness of treatment; prolonged regenerating and antibacterial action.

2 cl

FIELD: medicine and immunology, in particular treatment and prevention immunodeficiency conditions and diseases associated with bacterial or viral aggression.

SUBSTANCE: claimed method includes administration to a patient immunoglobulin drug (e.g., pharmaceutical composition containing 6-12 % of specific heterologous secreted immunoglobulin A, isolated from milk or foremilk of immunized ungulates). Administration is performed parenterally wherein single dose is at least 10 IU/kg of patient weight for treatment or at least 5 IU/kg for prophylaxis; or perorally in dose of 0.2-0.5 g and/or topically one-two times per day for 1-5 days. Method of present invention makes it possible to decrease dose of administrating immunoglobulin due to prolonged retention of its high titers in body fluids.

EFFECT: enlarged range of application and assortment of immunoglobulin drugs.

4 cl, 5 ex

FIELD: medicine, proctology, pharmaceutics.

SUBSTANCE: the present innovation deals with obtaining medicinal forms as suppositories applied for treating proctological diseases. Medicinal preparation as suppositories containing active substance, anesthetic, purified water and foundation could additionally contain antiseptic and local irritating substance, as an active substance - glucocorticoid at the following ratio of components, weight%: glucocorticoid 0.0277-0.0368, anesthetic 1.8-2.2, antiseptic 2.8-3.52, local irritating substance 0.288-0.352, purified water 1.8-2.2, foundation - the rest. As glucocorticoid that inhibits the release of inflammation mediators and causes pronounced antiphlogistic and antiallergic action one should apply, for example, hydrocortisone or synaflane. As anesthetic one should apply, for example, anesthesin, lidocaine or trimecaine. As antiseptic being of astringent, drying off and analgesic actions one should apply, for example, dermatol or xeroform. As local irritating substance being of reflector, venotonic, analgesic and antiphlogistic and, also, antimicrobial actions one should apply, for example, racemic menthol or essential oils.

EFFECT: higher therapeutic efficiency.

5 cl, 3 ex, 4 tbl

FIELD: pharmaceutical industry.

SUBSTANCE: new urogenital drug contains 50-250 g antibacterially efficient antibiotic erythromycin, 50-250 g antifungally efficient antibiotic nistatin, antiprotozoal preparation metronidazole, and 1.5-3.5 g (to complete weight of suppository) A type solid fat as filler. Drug can be used to treat mixed urogenital infections.

EFFECT: reduced treatment time, lowered recurrence of diseases, lack of adverse effects, and lowered cost.

FIELD: medicine, chemical-pharmaceutical industry.

SUBSTANCE: invention relates to the development of new homeopathic suppository that can be used for treatment of prostatitis, hemorrhoid, uterus cervix erosion, endometritis. Invention proposes two variants. By the first variant agent represents suppository comprising the following components, g: propolis, 0.1; sea-buckthorn, 0.2; chestnut homeopathic essences, 0.1; Ginkgo biloba homeopathic essences, 0.1; aloe homeopathic essences, 0.1; milfoil, 0.1; wax, 0.1 and a base. The second variant represents suppository comprising the following components, g: sea-buckthorn, 0.2; propolis, 0.1; rue homeopathic essences, 0.05; Hypericum (Saint-John's-wort), 0.05; Symphytum (comfrey), 0.05; Tambukan curative muddy extract, 0.2; lanolin, 0.15; wax, 0.1, and a base. Proposed suppository elicits an anti-inflammatory regenerating effect and without toxic effect.

EFFECT: valuable medicinal properties of suppository.

15 cl, 4 ex

FIELD: medicine, gynecology, contraceptives, pharmaceutical chemistry.

SUBSTANCE: invention proposes vaginal suppository comprising benzalconium chloride, benzoic acid, purified water and the preparation vitespol taken in the definite content of components. Invention provides the reliable inhibition of fungal microflora being especially against fungus Candida albicans and the absence of irritation and symptoms in vagina drying. Invention can be used as an individual agent for prophylaxis of undesirable pregnancy.

EFFECT: valuable properties of suppository.

5 tbl

FIELD: veterinary pharmacology, veterinary science.

SUBSTANCE: the suggested method deals with mixing formalin with components followed by heating with subsequent cooling at the following ratio of components including: 0.8%-formalin 5 ml, analgin 1 g, Veratrum tincture 1.0 ml, glycerol 5 ml, citric acid 0.2 g, gelatin 3 g.

EFFECT: enhanced curative result, more convenient medicinal form.

1 ex, 2 tbl

Up!