Anthropogeny complex drug


(57) Abstract:

The invention relates to the field of medicine and pharmaceutics and concerns anthropologi of the integrated product that includes ascorbic acid, acetylsalicylic acid, rutin, diphenhydramine, calcium supplements, aspirin and a filler, in which the active components are grouped according to chemical compatibility in two capsules or tablets: acetylsalicylic acid, ascorbic acid, rutin, the filler is one capsule or tablet, aspirin, diphenhydramine, calcium supplements, the filler is another tablet or capsule. The drug has a high stability. 2 C.p. f-crystals, 8 PL.

The invention relates to medicine, namely to oral means for treatment of influenza. The invention relates to a pharmaceutical, a pharmaceutical form of long term storage, stable, suitable for industrial production.

Influenza is one of the most common respiratory infections. In the epidemic period on the territory of the Russian Federation is sick with influenza and other viral respiratory diseases from 10 to 20 million people. The popularity of this infection is often combined with high frequency complicated is by acute onset, a short course with the phenomena of intoxication, lesions of the mucous membrane of the respiratory tract, fever, damage to the nervous and cardiovascular systems, accompanied by leukopenia with lymphopenia, muscle and joint pain, the phenomenon of weakness.

The incubation period for influenza type a, from several hours to 2 days, when influenza type b is up to 3 days [1].

Flu treatment includes symptomatic and causal treatment. Medical treatment depending on the severity of the disease, its course, from the presence of those or other complications. Used to treat fever, anti-inflammatory, antiviral, antiallergic, tonic medicines.

Etiotropic therapy of influenza is the use of antiviral drugs that block the reproduction of the virus at different stages of the replicative cycle. One of the most effective drugs in etiotropic therapy is rimantadine [2]. However, in the process of treatment with rimantadine, unfortunately, did not immediately disappear, the symptoms associated with intoxication and catarrhal phenomena.

Symptomatic drugs common flu approx, Algin [4] and other antipyretic and analgesic drugs.

The need for treatment of influenza a comprehensive drugs acting on different clinical manifestations of the disease at the same time, led to the emergence of various anthropogenic compositions.

Known drug “Coldrex”. It includes: paracetamol, phenylephrine, caffeine, terpyridyl and ascorbic acid [5]. The disadvantages of the drug should include the fact that it contains a psycho stimulant caffeine, which can interfere with sleep (insomnia is typical of influenza, so the caffeine exacerbates this symptom). “Coldrex contains paracetamol, coursework which contributes to the development of hepatotoxic effects. Phenylephrin amid capillaroscopy causes abnormalities in blood flow in vital organs (lungs, brain).

Called “Antigrippin” in Handbook Vidal given medication

- in the form of effervescent tablets containing paracetamol, ascorbic acid, chlorphenesin [6]. Paracetamol is recommended to relieve fever in this composition, as in “Goldrake”, can lead to the development of hepatotoxic effects.

The prototype offers the holding of acetylsalicylic acid, ascorbic acid, rutin, diphenhydramine and calcium salts (calcium lactate or calcium gluconate) in a weight ratio 53:32:2:2:11 [7]. The disadvantage of this drug is a weak analgesic activity, which is important in the symptomatic treatment of influenza. This extemporally mixture was tested on patients with influenza A(H3N2) A(H1N1) and Century. It had no significant effect on either the degree or the duration of the reaction temperature. This composition was slightly improved the well-being of patients, has led to less pronounced catarrhal phenomena [7]. The amount of acetylsalicylic acid in the mixture is 0.5,

The use of this composition in some cases due to the high concentration of powder (crystalline) acetylsalicylic acid can cause ulcers of the stomach or duodenum.

Pharmacy prescription is stable.

The aim of the invention is the creation of such a combined tool for the treatment of influenza, which simultaneously acts on the main symptoms of flu: fever, headache, pain in the eyeballs, muscle pain, aching joints, gemot causal therapeutic effect, you have to have a higher clinical efficacy and broader spectrum of activity compared to the prototype.

The aim of the invention is also to create a combined means for the treatment of influenza with high stability, suitable for industrial production.

Entity created of the invention is that the composition additionally introduced dipyrone, and the quantity of acetylsalicylic acid reduced in 1,5-2 times. The high stability of the proposed composition is provided that incompatible substances are posted in two separate capsules or tablets. The use of aspirin in the treatment of influenza is known [4]. It is prescribed for fevers, neuralgia, headache. Analgin quickly creates high blood concentration of the drug when administered orally. These properties of the drug used, including in the prescription pharmacy Antigrippin instead of acetylsalicylic acid [8]. Composition: proteins, ascorbic acid, calcium glycerol, diphenhydramine and rutin in terms of weight (mg) 500:300:100:20:10 recommended flu with contraindications to take acetylsalicylic acid. Such a comprehensive drug is AI analgin with amidopirina [4] and not meeting assignments simultaneously analgin with acetylsalicylic acid, the authors in pharmacy prescription (prototype) introduced acetylsalicylic acid and dipyrone in half (compared to the usually used when a separate application) dosages, i.e., the effective doses were reduced in 1,5-2 times.

Analysis of the mechanisms of action of the components of such compositions have started to do after was obtained an unexpected result in the treatment of influenza. The use of such integrated product, on average, 2-3 days reduced the duration of febrile period of SARS, and with the rise of the symptoms and the severity of the disease, the efficacy of the drug was increased.

In patients observed no complications from the lining of the stomach or duodenum (dyspeptic symptoms and pain in the stomach).

Clinical trials are proposed according to the invention medicines were conducted in the research Institute of influenza, Russian Academy of medical Sciences in the group of patients with acute respiratory viral infections. Results characterizing the subjective and objective evaluation of its effectiveness, are presented in tables 1, 2, 3.

The test results confirmed the clinical efficacy of the integrated product. It has a therapeutic effect and as a means of symptomatic terpenene with the results of treatment of influenza a mixture of drugs for pharmacy recipes [7], when it is used or one acetylsalicylic acid, or one analgin while maintaining all other components in the composition, showed a significant advantage for the joint use of acetylsalicylic acid and dipyrone in the composition, and acetylsalicylic acid and proteins used in half doses.

Laboratory and clinical tests of components of the proposed compositions are given below. To understand the mechanism of action were tested for efficacy in the symptomatic treatment of influenza and viral reproduction.

The antiviral effect of acetylsalicylic acid and rutin were studied by influenza viruses a and B. the Results of studies of direct antiviral activity are presented in table 4.

As a benchmark we used the drug rimantadine, which at a concentration of 25 μg/ml inhibited the reproduction of influenza viruses And up to 85% of control.

During testing it was found that rutin has direct antiviral activity, although previously [7] read indifferent with the flu.

The effectiveness of joint use in the compositions of acetylsalicylic acid and dipyrone can be explained on the basis of their resultant sodium. The structure of the drug, including phenyl radical, makes it partially hydrophobic, and the presence of N-methanesulfonate group strongly balances the polarity of the 4-aminopyrazole radical that leads to the manifestation of membranotropic properties of the drug. Membranotropic properties of the drug make it an effective blocker of K+/Na+ion channels that simultaneously provides analgesic and anti-inflammatory effects.

It is known that pyrolidinone and pyrazolone derivatives of adamantanes exhibit antiviral activity [10].

Presumably, the influenza viruses type a analgin effect on the function of the protein M2. Effect on influenza viruses In is probably through the influence on the reproduction of influenza viruses indirectly through the blockade of Pro-inflammatory response of infected cells. For dipyrone is also possible for a wider range of targets among viral proteins.

It is noted that dipyrone in certain conditions begins to have a distinct effect on the replication of influenza viruses types a and B. It inhibits the reproduction of viruses influenza A(H3N2) by 60%, and influenza viruses In 68% at a concentration of from 40 to 60 µg/ml apparently, the combination of acetylsalicylic to the antiviral effect with symptomatic treatment.

Thus, typing is additionally known in the composition of proteins, has been reduced by 1.5-2 times the quantity of acetylsalicylic acid and at the same time to obtain a complex drug with high activity for the treatment of influenza. The total dose for a single application is usually 0.8 to 1.0, the Ratio of components in the composition: acetylsalicylic acid, aspirin, ascorbic acid, rutin, diphenhydramine, calcium supplements and filler wt.%: 20-35:20-35:20-35:1-4:1-4:5-15:the rest of it.

Example: composition for treatment of influenza consists of acetylsalicylic acid, aspirin, ascorbic acid, rutin, Dimedrol, calcium gluconate, calcium stearate, talc wt.%: 21,5:32,5:26:1,7:2,6:13:0,5:2,2. The components of the total weight of 0.96 g are mixed in a given proportion and used as a complex dosed powders.

Taken as a prototype of the composition relates to pharmaceutical medicine [7]. Its composition during storage is unstable. Reducing network pharmacy with prescription departments designed to prepare medications to the copies, makes the search for the transition of the production of medicinal preparations on industrial way in which medicines should have stabiles is made in a single powder or in one capsule, stable drug. The composition of the claimed invention offers a more efficient therapeutic effect than the prototype. However, it is the same as the prototype, in powder form or in the form of capsules, for long-term storage is not suitable. It is not stable. Its characteristics of stability are absolutely identical to the prototype (in the tables, the object comparison Tool 2”).

The essence of the invention is that incompatible during storage between a medicinal substance exploded in two separate capsules or tablets. Reception at the same time these two tablets or capsules gives a therapeutic effect, as it completely saved the claimed composition.

Finished pharmaceutical products (FPPs) are subject to long-term storage. They should not occur chemical interaction of the individual components, leading to violation of the medicinal properties of the drug.

To obtain voice mixed pharmaceutical compositions for industrial production using different techniques: granulation, capsulate, obtaining multilayer tablets, etc. Often technological methods significantly increases the cost of the drug.

These studies showed that the most optimal is a result obtained binary preparation: each capsules or tablets for simultaneous reception contains chemically compatible substance. The weight of each tablet or the contents of capsules 0,30-0,70 g

The composition of each of the capsules or tablets are presented in table 5.

Comparative tests of the claimed medicinal product conducted with the simultaneous study of the stability of pharmacy recipe without dipyrone, i.e. the prototype. In pharmacy recipe all the components of the mixture were put up in one capsule, identified in tables test “Tool 2”.

Stability evaluation of the proposed drug in comparison with vehicle 2 was conducted in a climatic chamber at a temperature of 30 ° C and a relative humidity of 70% under the condition of storage of the drugs for 24 months. Analysis of samples was performed every three months. When detecting in the sample deviations from the specified level indicators of the quality of the drugs they further tests were seized. Below are presented in tables 6-8 systematized the results of the testing of the proposed drug during storage in comparison with the prototype.

As can be seen from the data presented in tables 6-8, the inventive tool when stored in a climate chamber practically did not change indicators Soichi the appearance of the contents of the capsules, and in the emergence of a large number (>4%) salicylic acid is a breakdown product of acetylsalicylic acid on acetic and salicylic acid.

In the industrial production of capsules of different filling colored food dyes in different colors, which makes them convenient when you receive the flu. Various colors and tablets have claimed composition.

The example run. Prepared capsules a and B with a mass content of 0.58 g and 0.38 g, respectively.

Test composition in capsules, conducted in the clinic for patients with influenza and acute respiratory viral infections, have yielded results completely coincide with the results presented in tables 1, 2, 3.

Complex drug had stability and high clinical efficacy. Its use has reduced the febrile period and duration of illness for 2-3 days.

Sources of information

1. The influenza. Ed. by G. I. Naruhina. - Lenizdat: Medicine, 1986.

2. Mashkovsky M. D. Medicines. H 2, Moscow, 1994, S. 395.

3. On The Main Page. Drugs in Russia. 1999. The e-5.

4. Mashkovsky M. D. Medicines. H 1, Moscow, 1987, S. 184-185.

8. Smorodintsev A. A. Influenza and its prevention. Moscow. 1984.

9. Isakov Century A. Modern tools symptomatic treatment of influenza and acute respiratory infections. - Terra Medica: 1999, №1(14), S. 3-5.

10. Kolocouris, N., A. Kolocouris, Foscolos G. B. et al. J. Med. Chem., 1996. V. 39, No. 17, R. 3307-3318.

1. Anthropogeny complex preparation for oral products, including ascorbic acid, acetylsalicylic acid, rutin, diphenhydramine, calcium supplements, analgin and filler, while active components are grouped according to chemical compatibility of two tablets or capsules, together constitute a single dose, in the following ratio, wt.% each capsule or tablet:

capsule or tablet:

Acetylsalicylic acid 35-50

Ascorbic acid 35-60

Rutin 1-5

Filler Rest

capsule or tablet B:

Analgin 40-70

Diphenhydramine 1-6

Calcium supplements 15-30

Filler Rest

2. Anthropogeny complex drug under item 1, comprising as calcium lactate and/or calcium gluconate.

3. Anthropogeny comprehensive drug


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