RU2605271C1 - Granules with extracts of cranberries, red bilberry madder antidiuretic, antispasmodic and litholytic action - Google Patents

Abstract

FIELD: pharmaceutics.

SUBSTANCE: invention refers to pharmaceutical industry, namely to an agent in the form of granules, possessing diuretic, antispasmodic and litholytic action. Agent in the form of granules possessing diuretic, antispasmodic and litholytic action, contains dry extract of rhaponticum madder, dry extract of cranberry and dry extract of bilberry, potato starch, aerosil A-380, glucose, 0.25 % aqueous solution of hydroxyethyl cellulose (HEC), in certain proportions.

EFFECT: proposed agent in form of granules has a pronounced diuretic, antispasmodic and litholytic action, possesses fast solubility within 30 seconds, easy and hygienic in use.

1 cl, 1 dwg, 3 tbl, 5 ex

Description

The present invention relates to medicine, namely to pharmacy, and relates to the development of a phytopreparation in the form of granules containing plant extracts, and can be used for the prevention and complex treatment of urolithiasis.

Known biologically active food supplement "Monurel PreviCyst", containing in 1 tablet: dry extract of cranberry fruit in maltodextrin 120 mg; ascorbic acid 60 mg and excipients: MCC; dicalcium phosphate; glyceryl behenate; croscarmellose sodium; polyvinyl polypyrrolidone; hydroxypropyl methylcellulose; magnesium stearate; silica; dye titanium dioxide (E171); shellac; stearic acid; fatty acid mono- and diglycerides (E472); polyvinylpyrrolidone; dyes: Ponceau 4R (E124) and indigo carmine (E132). Cranberry berries contain a high concentration of proanthocyanidins (PACs). These are natural substances that cause damage to the bacterial membrane, prevent the growth of bacteria on the epithelium of the urinary tract. One Monurel PreviCyst tablet contains 36 mg of PAC, which is a sufficient daily dosage to obtain the effect, and 60 mg of vitamin C, which increases the protective properties of the body [Monurel PreviCyst: description and price [Electronic resource] Access mode: http: //www.rlsnet. com / baa_tn_id_46045.htm. Date of appeal: 06/26/2015].

The closest analogue of the invention is an antispasmodic of plant origin. The main active ingredient of the preparation is the dry extract of madder madder obtained from the rhizomes and roots of madder madder - Rubia tinctorum L. and its Georgian variety Rubia tinctorum L. var.iberica Fisch. Ex DC. (R.iberica Fisch. Ex DC.) Koch Sem. madder - Rubiaceae. The product is available in the form of tablets containing a dry extract of rhizomes with roots of madder dye 250 mg, containing excipients: lactose (milk sugar), potato starch, colloidal silicon dioxide (Aerosil A-380), calcium stearate, croscarmellose sodium [Maren dye extract: instructions for use and reviews. [Electronic resource] Access mode: https://health.mail.ru/drug/mareny_krasilnoy_ekstrakt/. Date of appeal: 06/26/2015].

Dry extract of madder madder has a diuretic and antispasmodic effect, contributes to loosening of urinary calculi containing calcium and magnesium phosphates, and their excretion from the kidneys and urinary tract.

The objective of the invention is to expand the arsenal of herbal medicines for the prevention of stone formation and complex treatment of urolithiasis.

EFFECT: obtaining a new domestic product in the form of granules containing plant extracts, having a diuretic, antispasmodic and litholytic effect, which is convenient and hygienic in use.

The specified technical result is achieved in that the agent in the form of granules, having a diuretic, antispasmodic and litholytic effect, containing as an active substance a dry extract of rhizomes with roots of madder dye, as auxiliary substances potato starch and aerosil A-380, according to the invention additionally contains as active substances, dry extract of cranberry berries and dry extract of lingonberry, and additionally contains glucose and 0.25% aqueous solution as auxiliary substances Op hydroxyethylcellulose (HEC) in the following ratio, wt. %:

Madder extract tinting 12.0 Cranberry extract 12.0 Lingonberry extract 12.0 Potato starch 31,0 Glucose 31,0 Aerosil A-380 1,0 0.25% solution of SCE in purified water 1,0

The invention is illustrated by the following materials: table 1 presents excipients in the experimental formulations of granules containing dry extracts of madder dye, cranberries and lingonberries; table 2 - determination of the solubility time of the granules in water; table 3 - the results of the quantitative determination of the main biologically active substances of the dosage form according to example 1; the figure shows the quantitative content of arbutin (%) in granules according to examples 1-5.

All components that make up the granules are approved for medical use.

Dry extract of madder madder (No. PR 58171769-43-2011) has a diuretic and antispasmodic effect, contributes to loosening of urinary calculi containing calcium and magnesium phosphates, and their excretion from the kidneys and urinary tract.

Lingonberry extract (TU 9199-075-13179897-04) contains a large amount of vitamin C, increases the protective properties of the body as a whole, reduces irritation of the mucous membrane of the urinary system, has an astringent and diuretic effect, affects the crystal-colloidal ratio of stones, causing their destruction and dissolution, has antimicrobial activity.

Cranberry extract (TU 9168-004-31474708-2007) prevents the entry of pathogenic bacteria into the human bladder. Natural cranberry extract destroys the cell of the bacterium E. coli, as soon as it enters the body, and damages the synthesis of fibria, has antimicrobial activity.

Potato starch (GOST 7699).

Glucose crystalline hydrate (GOST 975-88).

Hydroxyethyl cellulose (HEC) is a cellulose derivative, a non-ionic water-soluble polymer used in cosmetic formulas to achieve viscosity and durability of emulsions. Hydroxyethyl cellulose is a white or yellowish-white substance that is readily soluble in cold or hot water to form solutions with a wide range of viscosity. It can thicken, suspend, bind, emulsify, form films, stabilize, disperse, retain water or provide a protective colloidal effect. Due to its non-ionic nature, it has a wide range of compatibility with other products, such as emulsion polymers, natural and synthetic resins, emulsifiers and anti-foaming agents [http://forum.academy-miracles.ru/lofiversion/index.php/t7973.html].

Aerosil A-380 (GOST 14922-77) mixes well with water and organic liquids, is used as a thickener, is hygroscopic and easily absorbs (absorbs) moisture during storage, is used as a carrier of active substances in medicine and perfumery.

- 1 чайной ложки гранул (0,35-0,7 г) в 100 мл воды горячей или комнатной - по желанию пациента (раствор готов к употреблению внутрь через

минуты). Перечисленные компоненты состава фитопрепарата в виде гранул в заявляемых соотношениях позволяют получить качественно новый состав и новую лекарственную форму сочетания трех растительных экстрактов в виде гранул, обладающих стабильностью, быстрой растворимостью (30 секунд), диуретическим, спазмолитическим и литолитическим действием, сроком годности 2 года, а также удобством и гигиеничностью применения.As a result of experimental studies, it was found that a solution of 0.25% HEC moisturizes a mixture of plant extracts taken at a ratio of 1: 1: 1 and excipients: potato starch, glucose and Aerosil A-380, which subsequently breaks through a sieve with a size then 2 mm, and takes the form of granules. Giving the drug the form of granules provides storage stability, convenience and hygiene of use by dissolution

- 1 teaspoon of granules (0.35-0.7 g) in 100 ml of hot or room water - at the request of the patient (the solution is ready for use inside through

minutes). The listed components of the composition of the herbal preparation in the form of granules in the claimed ratios allow to obtain a qualitatively new composition and a new dosage form of a combination of three plant extracts in the form of granules with stability, fast solubility (30 seconds), diuretic, antispasmodic and litholytic action, shelf life 2 years, and also convenience and hygiene of use.

- 1 чайной ложки - масса 0,35-0,7 г растворить в 100 мл воды.Get granules as follows. Pre-prepared 0.25% aqueous solution of hydroxyethyl cellulose based on: SCE 0.25; purified water to 100 ml. The crushed dry extracts of cranberries, lingonberries, madder dye in a ratio of 1: 1: 1 and a mixture of auxiliary dry substances: potato starch, glucose, Aerosil A-380, are uniformly moistened with a prepared 0.25% solution of HEC - binder using a spray gun. Triturated to a homogeneous moistened mixture for the preparation of granules, the mixture is punched through a sieve to obtain granules with a pore size of 2 mm and dried in an oven at a temperature of 50 ° C. The resulting herbal remedy consists of granules of irregular spherical shape, 2 mm in diameter, containing plant extracts of a heterogeneous red-brown color interspersed. At one time recommended

- 1 teaspoon - the mass of 0.35-0.7 g is dissolved in 100 ml of water.

The proposed granules are applied as follows.

Granules are taken orally before meals or between meals, in dissolved form - 0.35 g of granules (1/2 teaspoon) or 0.7 g of granules (1 teaspoon) dissolved in 100 ml of boiled water at hot or room temperature. Granules dissolve quickly (30 seconds). The solution is ready for use inside.

Example 1. Composition per 100.0 g of granules, wt. %: dry cranberry extract 12.0; dry cowberry extract 12.0; dry extract of madder madder 12.0 and excipients: potato starch 31.0; glucose 31.0; Aerosil A-380 1.0; a solution of HEC in purified water 0.25% - 1.0 (table 1, composition 7).

Pre-prepared 0.25% aqueous solution of hydroxyethyl cellulose based on: SCE 0.25; purified water to 100 ml. The crushed dry extracts of cranberries, lingonberries, madder dye in a ratio of 1: 1: 1 and a mixture of auxiliary dry substances: potato starch, glucose, Aerosil A-380, are uniformly moistened with a prepared 0.25% solution of hydroxyethyl cellulose - a binder using a spray gun. Triturated to a homogeneous moistened mixture for the preparation of granules, the mixture is punched through a sieve to obtain granules with a pore size of 2 mm and dried in an oven at a temperature of 50 ° C. The resulting herbal remedy is a granule of irregular spherical shape, 2 mm in diameter, containing plant extracts of a heterogeneous red-brown color interspersed.

The obtained granules dissolve after 30 seconds (table 2, composition 7); quantitative content of arbutin in granules 12.3% (figure, composition 7). Table 3 presents the results of the quantitative determination of the main biologically active substances of the dosage form.

Example 2. Composition per 100.0 g of granules, wt. %: dry cranberry extract 12.0; dry cowberry extract 12.0; dry extract of madder madder 12.0 and excipients: potato starch 15.5; glucose 46.5; a solution of hydroxycellulose in purified water 0.25% - 1.0 (table 1, composition 1). Granules are made in a similar manner. The obtained granules of a rounded shape dissolve after 1.21 minutes (table 2, composition 1); the quantitative content of arbutin in granules of 5.4% (figure, composition 1).

Example 3. Composition per 100.0 g of granules, wt. %: dry cranberry extract 12.0; dry cowberry extract 12.0; dry extract of madder dye 12.0 and excipients: potato starch 21.0; talcum powder 41.0; a solution of polyvinylpyrrolidone (PVP) in purified water 1% - 1.0 (table 1, composition 33).

Pre-prepared 1% aqueous solution of PVP at the rate of: PVP 1.0; purified water to 100 ml.

Granules are made in a similar manner. The obtained round-shaped granules dissolve after 1.50 minutes (table 2, composition 33); quantitative content of arbutin in granules 6.9% (figure, composition 33).

Example 4. Composition per 100.0 g of granules, wt. %: dry cranberry extract 12.0; dry cowberry extract 12.0; dry extract of madder madder 12.0 and excipients: potato starch 41.0; talc 21.0; a solution of PVP in purified water 1% -1.0 (table 1, composition 51).

Pre-prepared 1% aqueous solution of PVP at the rate of: PVP 1.0; purified water to 100 ml.

Granules are made in a similar manner. The obtained granules of a rounded shape dissolve after 1.30 minutes (table 2, composition 51); the quantitative content of arbutin in granules is 8.7% (figure, composition 51).

Example 5. Composition per 100.0 g of granules, wt. %: dry cranberry extract 12.0; dry cowberry extract 12.0; dry extract of madder madder 12.0 and excipients: potato starch 51.50; gelatin 10.50; a solution of hydroxycellulose in purified water 0.25% - 1.0 (table 1, composition 61).

Pre-prepared 0.25% aqueous solution of hydroxyethyl cellulose based on: SCE 0.25; purified water to 100 ml. The crushed dry extracts of cranberries, lingonberries, madder dye in a ratio of 1: 1: 1 and a mixture of auxiliary dry substances: potato starch and gelatin are evenly moistened with a prepared 0.25% solution of hydroxyethyl cellulose - a binder using a spray gun. Triturated to a homogeneous moistened mixture for the preparation of granules, the mixture is punched through a sieve to obtain granules with a pore size of 2 mm and dried in an oven at a temperature of 50 ° C. The obtained granules of a rounded shape dissolve after 1.32 minutes (table 2, composition 61); the quantitative content of arbutin in granules of 8.2% (figure, composition 61).

From the above examples it is seen that the optimal composition in terms of solubility and content of the active substance is described in example 1.

After conducting full-scale clinical trials and developing quality control methods for the developed granules, a pharmacopeia article is planned.

Claims (1)

The product in the form of granules, with a diuretic, antispasmodic and litholytic effect, containing as an active substance a dry extract of rhizomes with roots of madder dye, potato starch and aerosil A-380 as auxiliary substances, characterized in that it additionally contains dry extract as active substances cranberry berries and a dry extract of lingonberry berries, and as auxiliary substances it additionally contains glucose and 0.25% aqueous solution of hydroxyethyl cellulose (SCE) in the following ratio research component, wt.%:
Madder extract tinting 12.0 Cranberry extract 12.0 Lingonberry extract 12.0 Potato starch 31,0 Glucose 31,0 Aerosil A-380 1,0 0.25% solution of SCE in purified water 1,0

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