Diuretic and hypotensive agent of prolonged effect

FIELD: chemical-pharmaceutical industry, medicine, pharmacy.

SUBSTANCE: invention relates to medicinal agents of prolonged effect used in treatment of arterial hypertension. Medicinal agent of prolonged effect used in treatment of arterial hypertension comprises indapamide, accessory substance represented by interpolymeric complex of polymethacrylic acid with polyethylene glycol or polypropylene glycol. The claimed invention provides preparing a stable and easily dosed medicinal formulation of prolonged effect.

EFFECT: improved and valuable medicinal properties of agent.

1 tbl, 3 ex

 

The invention relates to the field of pharmacy, in particular to medicines prolonged action for the treatment of arterial hypertension.

For the treatment of arterial hypertension is widely used medicines, which has diuretic activity. Often use indapamide. Indapamide is part of drugs such as "Indep", "Pamid" [1].

These medicines have little therapeutic activity.

The objective of the invention is the creation of medicines for the treatment of hypertension, ensure the maintenance of therapeutic level of the drug concentration in the blood and the optimal duration.

The problem is solved by a composition comprising indapamide, excipients - interpolymer complex of poly (methacrylic acid) and poly (ethylene glycol) (CPN-1) [2] and the interpolymer complex of poly (methacrylic acid) and polypropylenglycol (CPN-2) [3], or a mixture thereof.

We offer drug get traditional for the art methods: direct pressing, granulation, followed by pressing. Received a drug covered by a shell of CPN-1.

Presents examples reflect the receipt of the offer medicines.

Example 1.

10.0 g indapamide mixed with 10.0 g CPN-1. The resulting mixture is pressed into tablets. For applying enteric film coating solution prepared CPN-1 in ethanol. Add titanium dioxide, suspended before the formation of uniformly colored film-forming composition. Shell tablet put in abductor.

Example 2.

10.0 g indapamide mixed with 10.0 g of the CPN-2. The resulting mixture is pressed into tablets. For applying enteric film coating solution prepared CPN-1 in ethanol. Add titanium dioxide, which is suspended to the formation of the colored film-forming composition. Shell tablet put in abductor.

Example 3.

10.0 g indapamide mixed with 5.0 g CPN-1 and 2.0 g of lactose. The mixture is pressed, crushed to granules with a particle diameter of 1 mm, the granulate is mixed with calcium stearinovokisly. The obtained granulate is pressed into tablets which are covered with a shell of CPN-1.

Example 4.

10.0 g indapamide mixed with 5.0 g of the CPN-2 and 2.0 g of lactose. The mixture is pressed, crushed to granules with a particle diameter of 1 mm, the granulate is mixed with calcium stearinovokisly. The obtained granulate is pressed into tablets which are covered with a shell of CPN-1.

Example 5.

10.0 g indapamide hydrate solution CPN-1 in ethanol. Granularit, dried at a temperature of n is above 40° C to a residual moisture content of not more than 3% and re-granularit through a sieve with the hole diameter of 1 mm Obtained granules are mixed with calcium stearinovokisly and pressed tablets that cover the shell of the CPN-1.

Received medicines tested on the release of indapamide (Wednesday phosphate buffer, pH 6.8) for 8 hours. The results of the study are presented in table 1.

Table 1.
The release of indapamide.
ExampleRelease, %
158
257
360
459
556

As shown, the drug has a pronounced and prolonged effect.

Literature.

1. Register of medicines of Russia 2002, radar, Moscow (2002).

2. FS 42-3011-94. Composite polymeric carrier.

3. THE 6-02-121-90, process regulation No. 28-90.

Drug for the treatment of arterial hypertension, containing indapamide and excipients, made in the form of slow release tablets, characterized in that it additionally contains in Apolinary complex of poly (methacrylic acid with polyethylene glycol (CPN-1) or polypropylenglycol (CPN-2), or a mixture of the active substance is mixed with a polymer complex CIT-1 or CIT-2 and auxiliary substances.



 

Same patents:

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition comprising enalapril maleate, lactose, potato starch, polyvinylpyrrolidone and magnesium stearate wherein a medium-molecular polyvinylpyrrolidone aqueous solution is used as polyvinylpyrrolidone, and the pharmaceutical composition comprises indapamide and aerosil additionally. The pharmaceutical composition is made as an enveloped-covered core in the following ratio of the core components, wt.-%: enalapril maleate is taken in the therapeutically effective dose; indapamide, 1.1-2.6; aerosil, 0.2-0.4; potato starch, 20.0-40.0; medium-molecular polyvinylpyrrolidone aqueous solution with the concentration 12%, 1.7-2.3; magnesium stearate, 0.8-1.0, and lactose, the balance. The claimed composition provides enhancing the hypotensive effect based on design of the composition comprising enalapril maleate and indapamide. The selected qualitative and quantitative composition excludes sticking tablet mass on equipment in tablets making process, loss of active substance and change of the ratio mass of components in ready tablets as compared to the measured one. Invention provides high strength and stability of tablets in storage.

EFFECT: improved and valuable properties of pharmaceutical composition, improved preparing method.

2 tbl

FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes an agent comprising the following components, mg: 2-ethyl-6-methyl-oxypyridine succinate, 25-1500; nicotinamide adenine dinucleotide, 0.5-100, and inositol, 100-1200. Agent can comprise additionally L-carnitine in the amount 10-100 mg. Also, agent can comprise additionally choline alphoscerate in the amount 50-1000 mg. Agent can be prepared in injection or tabletted medicinal formulation or as suppository. Agent provides effective delaying apoptosis and arresting transformation of apoptotic alterations to necrotic alterations in pathological processes of different etiology.

EFFECT: valuable properties and enhanced effectiveness of agent.

4 cl, 2 dwg, 2 tbl, 9 ex

FIELD: medicine, therapy.

SUBSTANCE: the present innovation deals with complex therapy in patients with arterial hypertension. Additionally to the conventional hypertensive therapy one should introduce daily in the first part of the daytime per 50 ml 0.9%-sodium chloride physiological solution pre-treated for 5 min with ozone-oxygen mixture at ozone concentration being 1000-1200 mcg/l and the rate of gas flow being 500 ml/min, therapeutic course consists of about 7-10 procedures. The innovation provides rapid and efficient normalization of hemodynamics and lipid exchange, decreases side effects due to optimal combination of the volume and the concentration of ozone in the introduced solution for such group of patients.

EFFECT: higher efficiency of therapy.

1 cl, 2 ex, 2 tbl

FIELD: pharmaceutical industry.

SUBSTANCE: invention relates to application of 2-hydroxyoleic acid and analogs thereof in production of drugs useful in diseases associated with G-proteins and mediated by membrane structure transition from lamellar structure to hexagonal one. Discribed is application of compounds of general formula I: COOH-CHR-(CH2)m-CH=-CH-(CH2)n-CH3, wherein R represents OH or NH2; m and n = 1-6 in production of drugs useful in treatment of cancer; as well as compounds of formula I, wherein R represents H, OH, NH2 or CH3, useful in treatment of hypertension and obesity.

EFFECT: drugs with increased effectiveness.

8 cl, 11 dwg, 3 tbl, 11 ex

FIELD: medicine, pharmacology.

SUBSTANCE: endothelial dysfunction is modulated in Wistar-line rats by daily intraperitoneal administering of L-nitro-arginine-methyl ester in dose of 25 mg/kg for 7 days and simultaneously combination of indapamide and L-arginine is administered one time per day, wherein indapamide is administered intragastrically in dose of 2 mg/kg and L-arginine is administered intraperitoneally in dose of 200 mg/kg.

EFFECT: method for correction of endothelial dysfunction due to synergistic action of indapamide and L-arginine.

2 tbl, 1 ex

FIELD: medicine, cardiology.

SUBSTANCE: after a dosed physical loading it is necessary to add a sudorific plant species. The innovation provides efficient decrease of pressure due to abundant diaphoresis accompanied by the release of chlorides.

EFFECT: higher efficiency of therapy.

FIELD: organic chemistry, medicine.

SUBSTANCE: invention relates to a novel salt possessing hypotensive activity, namely, to N-(2-methylphenoxyethyl)-N-cyclohexylamine hydrochloride of the general formula: .

EFFECT: valuable medicinal property of compound.

1 tbl, 2 dwg

FIELD: medicine, experimental cardiopharmacology.

SUBSTANCE: method involves modeling the endothelial dysfunction by every day intraperitoneal administration of L-nitroarginine methyl ester in rats (Wistar strain) in the dose 25 mg/kg for 7 days. On background of dysfunction modeling its correction is carried out by simultaneous intragastric administration of enalapril in the dose 0.5 mg/kg and by intraperitoneal administration of resveratrol in a single dose 2 mg/kg per 24 h. Degree of dysfunction development and activation of its correction are evaluated by the ratio endothelium-independent and endothelium-dependent vasodilation. Method provides possibility for study of endothelium-protective effects of resveratrol and activation of endothelial NO-synthase at stage of modeling endothelial dysfunction and their evaluation by the above given ratio endothelium-independent and endothelium-dependent vasodilation. Invention can be used in correction of endothelial dysfunction.

EFFECT: improved method of correction.

2 tbl, 1 ex

FIELD: medicine.

SUBSTANCE: method involves +placing patient into closed space like mini-sauna manufactured mainly from wood. Saturated vapor concentrate is produced in vapor generator by making air pass through a concentrate volume. Compressor is used as means for feeding vapor generator with air. Human skin is treated with the produced velvet antlers concentrate supporting concentrate temperature equal to 50-98°C in the vapor generator and closed space temperature equal to 30-70°C during 5-25 min.

EFFECT: enhanced effectiveness of treatment.

3 cl, 1 dwg

FIELD: medicine, ophthalmology, chemical-pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to a combination of agents used in treatment or prophylaxis of glaucoma. The combination comprises angiotensin II antagonist of the formula (Ia): and prostaglandin representing isopropylunoprostone or latanoprost as active components for simultaneous or successive using the indicated active components. The combination shows high effectiveness and bioavailability and has no toxicity.

EFFECT: improved and valuable medicinal properties of combination.

5 cl, 3 tbl, 7 ex

FIELD: medicine.

SUBSTANCE: invention relates to system for controlling oral or anal administering of biological component and method for prolonged bacteria administering into living body. Claimed system contains hydrophilic agent and bacterium; or viscosity modifier, hydrophilic agent and bacterium; or viscosity modifier, electrolytic agent, hydrophilic agent and bacterium. Hydrophilic agent provides viscosity from 4000 mPa to 15000 mPa and is selected from at least one group comprising: a) gum, such as tragacant gum, locust gum, acacia gum, guar gum, xantan gum, etc.; b) polysaccharide such as pectin and maltodextrin; c) cellulose derivative such as methylcellulose, carboxymethyl cellulose, methylcellulose hydroxyethyl, methylcellulose hydroxypropyl, etc.; d) polypeptide such as gelatin, collagen, casein of heterogeneous protein mixture. Claimed systems are obtained by component drying, blending and pressing. Bacterium/hydrophilic agent ratio is from 1:0.33 to 1:1.33.

EFFECT: system for controlling administering of biological component in desired regions of gastrointestinal tract.

32 cl, 13 ex, 13 tbl, 13 dwg

FIELD: medicine.

SUBSTANCE: claimed composition contains core including Rabeprasol or pharmaceutically acceptable salt thereof as acid secretion inhibitor in stomach and basic compound, intermediate coat coating the core, and overcoat applied on intermediate layer and containing water insoluble polymer and enterosoluble polymer. Also described is method for production of composition containing said preparation.

EFFECT: composition of prolonged storage time providing effective concentration of Rabeprasol in blood for long period of time.

16 cl, 5 dwg, 14 ex

FIELD: medicine.

SUBSTANCE: the present innovation deals with applying ambroxol and its acceptable salts for obtaining the medicinal preparation indicated for treating pains in oral cavity and pharynx.

EFFECT: higher efficiency of therapy.

5 cl, 2 dwg, 6 ex

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to a solid medicinal composition providing pH-independent release of active substance and comprising (2R)-1-{[4-chloro-2-(ureido)phenoxy]methyl}carbonyl-2-methyl-4-(4-fluorobenzyl)piperazine or one of its salts, polymeric matrix, pharmaceutically acceptable organic acid, lubricating additive and one or some accessory substances and wherein size of 90% of particles in powdery mixtures is from 0.1 to 750 mcm. Except for, invention relates to methods for preparing and using this medicinal composition.

EFFECT: valuable pharmaceutical properties of composition, improved preparing method.

22 cl, 11 dwg, 22 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes a pharmaceutical system for oral delivery of antioxidants, vitamin C and vitamin E. The delivery system comprises vitamin C in the amount providing delivery of the daily dose corresponding to 60 mg - 2 g of vitamin C, and comprises vitamin E in the amount providing delivery of the daily dose corresponding to 50 mg - 500 mg of α-tocopherol. Also, this delivery system provides the ratio of concentrations vitamin C and vitamin E in blood plasma in the range from 1:1 to 3:1, and wherein the solubility of vitamin E provides dissolving 90% of vitamin E for less in 30 min. The dissolving index is measured by heating at 37°C in 15 ml of water in the prescribed time intervals followed by decantation of the dissolving medium, washing out with 25 ml of 25% ethanol, combining the dissolving medium and decanted ethanol and measurement of the content of vitamin E in combined media for dissolving in ethanol, and wherein the solubility of vitamin C is so under conditions of the Test A that its dissolving after 1 h is less then 40% of vitamin C and wherein this test for solubility satisfies the order for the European Pharmacopoeia 711, and wherein administration of the indicated delivery system enhances the concentration of blood plasma vitamin E up to at least 20 mcmole/l, and the concentration of vitamin C to at least 40 mcmole/l. Also, invention represents methods for treatment including administration the claimed pharmaceutical system to a patient. The concentration and the ratio of these antioxidants corresponding to the stationary state of these antioxidants as was found are to be essential for prophylaxis and treatment of disorders associated with oxidative loading, such as arteriosclerosis, diabetes mellitus and damages of the nervous dystrophy type as Alzheimer disease.

EFFECT: improved and enhanced properties of pharmaceutical delivery system.

33 cl, 9 tbl, 3 dwg, 5 ex

FIELD: organic chemistry, medicine, pharmacology, pharmacy.

SUBSTANCE: invention relates to novel compounds possessing properties of EP4 agonist and their using as EP4 agonist for preparing a pharmaceutical composition used in treatment of disorders associated with reducing the osseous mass. Invention provides the enhanced effectiveness of treatment.

EFFECT: valuable medicinal properties of pharmaceutical compositions.

13 cl, 125 tbl, 32 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes a sustained-release composition comprising the following components: (1) a derivative of LH-RH of the formula: 5-oxo-Pro-His-Trp-Ser-Tyr-D-Leu-Leu-Arg-Pro-NH-C2H5 or its acetate, or its salt taken in the amount from 14% (mas./mas.) to about 24% (mas./mas.) of the total composition mass; (2) 3-hydroxy-2-naphthoic acid or its salt, and (3) polymer of lactic acid or its salt with average-mass molecular mass from 15000 to 50000 Da wherein the content of polymers with molecular mass from 5000 Da or below is 5% by mass or below and wherein the molar ratio of 3-hydroxy-2-naphthoic acid or its salt to derivative of LH-RH or its salt = from 3:4 to 4:3. Also, invention describes a method for preparing the composition and a medicinal preparation comprising the regulated composition. Proposed composition provides the constant release rate for the prolonged time based on inhibition of the parent intensive release of a pharmaceutically active compound.

EFFECT: improved and valuable properties of composition.

17 cl, 8 tbl, 22 ex

FIELD: medicine.

SUBSTANCE: claimed composition contains pharmaceutical agent, carrier for retarded releasing of drug and accelerator of gel hydration. Carrier represents mixture of sodium alginate and xanthan gum in weight ratio of 1:0.1-10. Accelerator of gel hydration represents mixture of hydroxypropylmethyl cellulose and propylene glycol alginate in weight ratio of 1:0.05-20. Weight ratio of pharmaceutical agent, abovementioned carrier and abovementioned accelerator of gel hydration is 1:3-45:1-0.1-15. Said composition is capable of supporting stable levels of pharmaceutical agent in blood for 24 hours or more.

EFFECT: effective composition of retarded releasing for peroral drug administration.

5 cl, 8 dwg, 3 tbl, 21 ex

FIELD: medical engineering.

SUBSTANCE: pill taken per os comprises pharmaceutically active agent selectable from (S,S)-Reboxetin or its salt and Pramipexol or its salt. The pharmaceutically active agent is taken in the amount of 0.01% by mass to 25% by mass of composition. It is dispersed in matrix composed of hydrophilic polymer and starch having rupture strength of at least approximately 0.15 kN·cm-2, at least approximately 0.175 kN·cm-2 or at least approximately 0.2 kN·cm-2, when having solid substance usable for producing pills where hydrophilic polymer takes approximately 20-70% by mass and starch is available in the amount of approximately 25-75% by mass. Method involves determining starch usability and composition applicability for treating the cases of disorders and states selected from depressive psychosis, neuropathic pains and Parkinson disease. Starch of specified rupture strength allows pill to withstand high speed pelletization operation and to provide prolonged drug release and to take a pill once a day.

EFFECT: controlled and prolonged drug action; enhanced effectiveness of treatment.

21 cl, 9 tbl

FIELD: medicine, pharmacy.

SUBSTANCE: invention relates to a pharmaceutical composition for controlled release that comprises a medicinal agent, polyethylene oxide with molecular mass 2000000 Da or above and a special size-regulating agent for indicated polyethylene oxide and wherein indicated medicinal agent and size-regulating agent are dispersed uniformly in polyethylene oxide. Also, invention relates to a method for preparing indicated pharmaceutical composition for controlled release and a pharmaceutical preparation for controlled release comprising indicated pharmaceutical composition for controlled release. The pharmaceutical composition with controlled release possesses good uniformity of the content and can be prepared using polyethylene oxide powder particles showing properties suitable for making tablets that is prepared by uniform dispersing a size-regulating agent for polyethylene oxide.

EFFECT: improved and valuable pharmaceutical properties of composition.

32 cl, 1 tbl, 16 ex

FIELD: medicine, pharmacy.

SUBSTANCE: invention describes a pharmaceutical composition for its using in treatment of symptoms of catarrhal diseases and influenza, or as an analgesic drug. Composition represents a single dose as an aqueous medicinal formula of the total volume less 100 ml and containing paracetamol and a masking component that attenuates or masks its bitter taste and consisting of at least two components chosen from the following groups (i)-(vi): (i) magnesium chloride, gluconate, hydroxide, carbonate or hydrocarbonate, and/or a mixture of magnesium chloride and magnesium sulfate in the molar ratio from 0.0001:1 to 0.01:1 measured as the ratio magnesium atoms : paracetamol; (ii) gingerin and/or ginger oil in the weight ratio from 1:20000 to 1:10000 with respect to paracetamol; (iii) sweetening agent of the sustained onset effect and prolonged effect chosen from taumatin, neohesperidin DC and/or glycyrrhizin taken in the weight ratio from 1:20000 to 1:100 with respect to paracetamol; (iv) soluble starch taken in the weight ratio from 1:10 to 1:1 with respect to paracetamol; (v) sucrose ester having value of hydrophilic-lipophilic balance (HLB) above 10 and taken in the weight ratio from 1:10 to 2:1 with respect to paracetamol, and (vi) glycine taken in the molar ratio from 1:4 to 2:1 with respect to paracetamol. Proposed composition provides effective taste masking or bitterness of paracetamol being especially in liquid preparations containing less 100 ml of water, and in using the combination of different masking agents also.

EFFECT: improved and valuable properties of composition.

10 cl, 3 tbl, 3 ex

Up!