Composition with sedative activity (options)

 

The invention relates to the field of medicine and concerns sedative medicinal composition of soft steps, including Pediatrics. The invention lies in the fact that the composition with sedative activity includes biologically active substances Valerian, sodium bromide, magnesium sulfate, the preparation of citral and glucose, as biologically active substances Valerian contains an effective amount of valepotriates comprising dry extract of Valerian, citral in the form of oil, and optionally includes the solvent to volume of 100 ml) at a certain ratio of components. The composition may be in the form of dry mixtures or water or alcohol 20%-aqueous solution. The invention provides the required quality of dry medicine that meets the requirements of the Pharmacopoeia, and the shelf life of not less than 2 years. 2 S. and 3 C.p. f-crystals, 2 tab.

Group of inventions relates to the field of pharmacy and suitable as a sedative medicinal composition of soft steps, the potential for use in medicine, including children.

Mixtures of complex composition, containing sodium chloride, magnesium sulfate, glucose, tincture of Valerian and alcohol solution of citral (razlichnykh age with increased excitability of the Central nervous system.

Sodium bromide and Valerian tincture known as sedatives. Magnesium sulfate along with soothing possesses anticonvulsant, antispasmodic, laxative and cholagogue action. These pharmacological effects of magnesium sulfate contribute to better bowel movements and eliminate constipation, which often occurs in children with increased nervous excitability. Alcoholic solution of citral is introduced into the composition as an analgesic and anti-inflammatory component, in addition, it is antiseptic (preservative) [Mashkovsky M. D. Medicines. - M.: Medicine, 1988]. In the classical literature additionally mentions its oral use in hypertension and signs of intracranial hypertension. Glucose, which is part of this composition, in the case of oral administration is corrigent taste of the drug.

Medicine with these components is often repeated words in the formulation of industrial pharmacy Russian Federation. We found a great variety of combinations and concentrations of incoming ingredients. Common to all analyzed compounds is that they all include ethyl alcohol in videocentral alcohol, not subject to long-term storage.

Drugs for children and certain categories of adults should be safe for the body, should not contain toxic and allergenic substances. From preparations for infants recommended the exception of ethyl alcohol and alcohol-containing ingredients [Spiridonov C. N., Obolentseva, Century Medicines for children // Technology and standardization of drugs. Sat. the scientific. proceedings / edited by George B. N. and F. A. Konev. - Kharkov: Publishing house LTD Puper, 1996].

In addition, mixtures are favorable environment for growth of microorganisms [Spiridonov C. N., Obolentseva, Century Medicines for children // Technology and standardization of drugs. Sat. the scientific. proceedings / edited by George B. N. and F. A. Konev. - Kharkov: Publishing house LTD Puper, 1996]. Mentioned liquid sedative medicine has a shelf life of one day [the Ministry of health of the Russian Federation from 16.07.97, 214 "On the control of drugs manufactured in the pharmacy"], so it cannot be made as store preparing procurement (WHA). Unification and standardization extemporally division reserves are improving the quality of medicines and medical care [Lobacheva L. A., Klimko So Century. the Development of a range of drug is. extemporally recipe needs a critical reappraisal // pharmacy. 1991. 4. S. 66-67].

At the same time to young children and some adults patients, oral administration, as a convenient, simple, painless, is the most preferred. Liquid medicines for internal use are characterized by good biopharmaceutical indicators related to the uniformity and rate of absorption of drugs.

Dry medicines have their advantages over liquid. They are more stable, compact, and less susceptible to microbial contamination during storage [Kelman, I. , Krylov, Y. F., Shub T. A. Questions and methods for determining microbial contamination of non-sterile medicines (review) // HFJ, 1985. 4. S. 477-485]. However, some medicinal substances, in particular bromides, the powders are irritating to mucous membranes, which is not observed in their use as medicines [ANCOVA A. I., Again I. C. Dosage form and therapeutic effectiveness of drugs (introduction to biopharmaceu). - M.: Medicine, 1974. S. 226-258].

Famous permitted for medical use "Medicine cough for use medications replaced by dry extracts of licorice and tempsize (for adults) or altejnogo root (for children). These dry mixtures are produced in S.-Petersburg and Moscow pharmaceutical factory. Known preparative form a dry mixture from cough for children. It is a waterproof bag with a single dose of a mixture of dry components subject to subsequent dissolution. Recipes include dry extracts of licorice and thermopsis or altejnogo root [Testimony RF 11710 utility model, And 61 To 9/52. Preparative form of medicine // PMPO. 1999. 11. C. 21].

Known dry substance of natural biologically active compounds from the aerial parts of the plant Valerian. It is obtained by extraction from herbs, crushed by rolling, and has a strong sedative effect. The extraction carried out 65-75% ethanol [RF Patent 2098115, IPC 6 a 61 K 35/78. The method of obtaining an extract of Valerian has sedative effect // PMPO. 1997. 12.10].

In the nomenclature of medicines no dry drug underground organs of Valerian, which could be replaced Valerian tincture (rhizomes with roots) in the preparation of dry medicine. However, an integral part of all elements of technological methods of obtaining extracts and dry extracts from growing drugs. -M.: Medicine, 1971. S. 196, 198, 202].

We received dry extracts of Valerian for several options technology, including maceration and repercolation. Phytochemical studies confirmed the adequacy of the set of biologically active substances Valerian, thick extract and the resulting dry extracts.

The content of valepotriates in the dry extracts obtained by different technological methods, ranging from 0.11 to 10.2 wt.% It is established that the specific process parameters and characteristics of the individual technological operations can be selected from well-known and widely used in practice, techniques and methods.

There still remains the search for compounds sedative action that combines the advantages of liquid and solid preparations and, if possible, eliminating the disadvantages of each.

Closest to the proposed formulations is a prescription drug with sedative action of a solution. The drug is recommended for adults by the Ministry of health of the Russian Federation [the unified Collection of medicinal formulations. - M.: Publishing house of JSC "Pharmimpex", 1995. - C. 14] and include: 1% Solution of citral alcohol - 3.0 Magnesium sulfate infusion of Valerian - AA 4,0 N is and with sedative activity as able to the subsequent dissolving the dry dosage forms, meet the requirements of OST 91500.05.001-00 "standards for the quality of medicines. General provisions", suitable for long-term storage, it is convenient to implement.

This is achieved by the fact that the proposed compounds with sedative activity contain compatible ingredients that do not violate the flowability of the mixture, soluble in purified water or water-alcohol solutions, and have a shelf life of not less than 1 year.

When this composition with sedative activity, including biologically active substances (BAS) from the rhizomes with roots of Valerian, sodium bromide, magnesium sulfate, the preparation of citral and glucose, as BAS Valerian contains an effective amount of valepotriates comprising dry extract of Valerian obtained from underground organs, citral - in the form of oil, and optionally includes a solvent (water or 20% spirtually solution to 100 ml) in the following ratio of components, g: Sodium bromide and 0.5-2.0 Magnesium sulfate 0.5 to 2.0 Glucose - 5,0-20,0
Valepotriates comprising dry extract of Valerian - 0,0009-0,0051
Citral - 0,005-0,01
Composition for infant dosage form has the following primary content of the dry components in a single dose, g:
Sodium bromide - 0,05
Magnesium sulfate - 0,05
Glucose - 0,5
wow Valerian extract depends on the content of valepotriates and determined the age of therapeutic dose.

The composition may be in the form of powder or water or 20% alcohol solution.

Failure to comply with the ratio of ingredients of the composition or technology medicine does not allow to obtain the necessary quality dry medicine in the acquisition and storage.

The dry mixture is layered introduction the stated ingredients. The method allows know-how, which is not a subject invention and belongs to SPFA.

Replacement solution of citral in 95% alcohol for citral oil does not violate the main technological properties of the dry drug - flowability.

Example 1.

In a mortar consistently mix the ingredients until smooth and tightly Packed in measured doses by several techniques (angro) or as separate doses of the composition (dry medicine, if the application is assumed dilution in water).

Examples of practical implementation of the compositions shown in table.1.

The observation of dry mixtures described in the examples of the compositions, more than one and a half years. The stability of the qualitative and quantitative characteristics of the ingredients are preserved.

Dry extracts are loose powders from light brown (extract 1) to brown (estorach.

Extract 1 is produced by the method of fractional maceration with further evaporation. As extractant use purified water. This variant of the technology used in order to obtain a dry extract, similar to the complex of biologically active substances of the extract of rhizomes with roots of Valerian [State Pharmacopoeia of the USSR: In 2 vol.11th ed. (GF XI). Vol.2. M.: Medicine, 1990.- S. 369 (article 77); EXT. 5 dated 27.10.99 to Art. 77 GF XI. Vol.2]. The possibility of obtaining a dry extract of water is important for plants that do not have licenses to work with alcohol.

Extract 2 produced by the method of fast repercolation with subsequent distillation of the solvent. As extractant using a 20% ethyl alcohol. This technology leads to the production of dry extract, which is close to the complex BAS thick Valerian extract [FS 42-3685-98].

Dry extracts, approaching on the content of biologically active substances to the complex Valerian [FS 42-3865-99], is obtained using the alcohol strength above 40%.

Phytochemical study of dry extracts of Valerian
Phytochemical analysis was carried out by the main groups of biologically active substances contained in the rhizomes with roots of Valerian [GF XI. Vol.2, Art. 77; MEAs. 5 dated 27.10.99 to Art. 77 GF XI. Vol.2], in comparison with tincture of Valerian [FS 42-3865-99] or HUS is].

To assess the quality of the obtained dry extracts of Valerian have been used methodology to determine the presence of valepotriates and such groups of biologically active substances like tannins, amino acids, saponins, flavonoids and alkaloids. The results of the evaluation of drugs presents table.2.

As valepotriates are a group of biologically active substances, which causes the main therapeutic effect of Valerian preparations [Fursa N. S., Rzezinski C. D. Valepotriates some species of the family Valeriano-o and create drugs based on them // pharmacy. 1992. 5. S. 69-73], valepotriates were identified by us. Chromatographic analysis of valepotriates carried out in the solvent system: n-hexane - methylisobutyl ketone (8:2). The Rf value and color spots compounds obtained by chromatographicaliy dry extracts were compared with those thick extract and tincture of Valerian.

Quantifying the amount of valepotriates was conducted based on the methodology developed VNIIR [Konovalov O. A., Konon N. G., Rybalko K. S., Sablinski A. N. Quantitative determination of the amount of valepotriates in rhizomes with roots of Valeriana officinalis L. // HFG. 1983. 7. S. 831-836], the amount of tannins - method GF XI [GF XI. Vol.2. S. 160-161, 369-371], su is dative tool. As extractant in it regulated the use of ethyl alcohol 40%.

When poluchenii dry extract 2 we reduced the concentration of extractant (ethyl alcohol) from 40 to 20%, and in the case of extract 1 as the extractant used purified water.

The number of valepotriates dry extract depends on the amount of dry extract in the inventive composition.

Evaluation of the pharmacological action of dry extracts of Valerian
Pharmacological studies on the evaluation of the sedative dry extracts were carried out in experiments on laboratory animals according to the generally accepted test "open field" and "mink reflex" [Balykin E. C., Berezovskaya I. C. Comparative evaluation of methods approximate the response of rats in a Toxicological experiment // Pharmacology and toxicologia. 1976. 5. S. 636-638; Markel, A. A. , Chugainov R. A. Method of complex registration behavioral and autonomic responses in rats during the test "open field" // Higher nervous activity. 1976. 6. C. 1314-1318]. The experiments were carried out on outbred white rats-males. The tests were filmed before the introduction of the drug after a single weekly injection as freshly prepared and kept for more than a year dry exsto standard drug Valerian tincture, the second group - extract 1, the third - extract 2, the fourth group of control.

During the experiment evaluated the change in aggression (AG) and estimated (OA), search (PA) and motor (YES) activity of animals.

It is established that AG is reduced by 40-50% when administered infusions, and both extracts.

OA with the introduction of infusions reduced to 50-55%, whereas in animals treated with the extracts of OA has not changed.

PA animals treated with the tincture and extract 2 were reduced by 30%, and in rats treated with extract 1, it decreased by 40%.

YES treated as a tincture and extracts reduced twice.

Thus, the dry extracts to the same extent as the tincture of Valerian, reduce hypertension, and YES. It is positive that extracts, in contrast tinctures, does not have a significant impact on OA, which contributes to the preservation of orientation in space. In General, the dry extract of Valerian as its tincture, has a sedative effect.

The claimed variants of the composition with a dry extract of Valerian are the best found experimentally, provide the necessary quality of dry medicine, compliance OST 91500.05-00 and have a number of advantages over ready the containing alcohol, reducing the time and improving the quality of public service.

The technology is traditionally performed in the conditions of pharmacy operations: poroshkovaya, sieving, mixing powders and adding citral, filling, corking.

In the manufacturing pharmacies S. Petersburg dry mixture according to the formulations can be produced as store preparing the workpiece (WHA).


Claims

1. The composition of the sedative activity, including biologically active substances Valerian, sodium bromide, magnesium sulfate, the preparation of citral and glucose, characterized in that the biologically active substances of Valerian contains an effective amount of valepotriates comprising dry extract of Valerian, citral - in the form of oil, and optionally includes water or ethyl alcohol 20% (up to a volume of 100 ml) in the following ratio of components, g:

Sodium bromide 0.5 to 2.0

Magnesium sulfate 0.5 to 2.0

Glucose 5,0 - 20,0

Valepotriates in the composition of dry

Valerian extract 0,0009 - 0,0051

Citral 0,005 - 0,01

2. The composition of the sedative activity, including biologically active substances Valerian, sodium bromide, magnesium sulfate, the preparation of citral and glucose, characterized in that before the>/p>Sodium bromide 0,05

Magnesium sulfate 0.05

Glucose 0,5

Dry extract of Valerian (when the content of valepotriates 1,8%) 0,005

Citral 0,0005

3. Composition under item 1 or 2, characterized in that it is made in the form of dry mixtures.

4. Composition under item 1 or 2, characterized in that it is made in the form of an aqueous or alcohol 20% solution.

 

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