Anti-inflammatory ointment with hypolipidemic effect

FIELD: medicine, pharmaceutical industry, pharmacy.

SUBSTANCE: invention relates to an anti-inflammatory ointment with hypolipidemic effect. Proposed ointment comprises ephthylline-base for ointment, a statin wherein lescol (fluvastatin) is used as statin, and ephthylline comprises 40% of ephthiderm. Invention provides enhancing the curative effect and hypolipidemic effect and effects on enzymatic systems of biological membranes that results to prolongation of curative effect of ointment.

EFFECT: valuable medicinal properties of ointment.

3 cl, 2 tbl

 

The invention relates to medicine, specifically to anti-inflammatory remedies for external use. The tool can be used in the treatment of hyperlipidemia any origin, including in combination with coronary heart disease (CHD) and hypertension (GB).

There are a large number of drugs anti-inflammatory action, for example - NSPs [Ivanova L.A., Kopteva EJ, 1991; Klyuev M.A. and others, 1990; Mashkovsky PPM, 1993; Nasonova V.A., Astapenko M.G., 1989; Nelyubov M.V. and others, 1998; Orlov, T.V., 1990; Ackerman, S.J. et al., 1983]. Unfortunately, they all have side effects. First of all, it ulceration of the mucous membrane of the stomach and duodenum, which may be accompanied by bleeding; damage and necrosis of the kidneys, delay delivery [Dale M.M. j shaped. To; Mashkovsky PPM, 1993; Adams D.O., Hamilton T.A., 1988].

Closest to the patent-pending tool is ointment anti-inflammatory eftimation containing etterlin (application No. 2003131288 from 28.10.2003 - prototype). This ointment has no lipid-lowering effect.

On the other hand, well-known drugs statins, which inhibit the synthesis of cholesterol and lower the levels of low density lipoprotein (LDL) in the blood, eliminating hyperlipidemia. It is recommended to use these drugs in the form of tablets or capsules constantly throughout life. Unfortunately, the due to their high cost they are not available for most patients. In addition, the daily dose of statins variable, as is the accumulation of the drug in the body and changes its activity [Avesco and others, 2001, Mhglte, Kaabeli, Lgeria, 1999; W.J.Patrick, .Serruys, 2002].

The technical challenge is to improve therapeutic effect of the ointment on the basis of afterline with achievement of the lipid-lowering effect.

The technical result is achieved by the fact that anti-inflammatory ointment containing afterin add a statin, such as lescol, in the following ratio, wt.%:

afterin80,000-99,890
statin (lescol)0,040-0,240

The invention is also characterized by the fact that the ointment (afterin) contains 40% epiderma.

The technical result is ensured by the ability of epiderma conduct biologically active substances through the skin and mucous membranes. It also has anti-inflammatory and high antioxidant activity; increases oxygenation (oxygen regime) tissues; increases cell viability; the effect on the enzymatic system of biological membranes, which leads to the enhancement and prolongation of therapeutic effect of all components of the ointment.

The obviousness and sverhsummarny effect of the proposed technical solutions SOS is the RTO is what afterin, preserving all properties epiderma, not only easily holds a statin in the tissue, but also extends it for 22-26 hours. This afterin significantly enhances the activity of the statin, which allows you to reduce the dose in the last fifty or more times (usual daily oral dose 10-160 mg statin, and 100 g of ointment contains 160 mg of a statin at a daily dose ointments for external use is 0.5-2 g, which contained only 0.8 to 3.2 mg statin).

The mechanism of action of statins: lovastatin (mevacor), simvastatin (zocor), pravastatin (lipostat), fluvastatin (lescol), atorvastatin (Liprimar), based on the fact that they have a chemical structure similar to HMG-COA reductase, which catalyzes the synthesis of cholesterol from acetic acid via the formation of avalonbay acid. Statins, superseding the true enzyme, interrupting the path of education avalonbay acid and thereby inhibit the synthesis of cholesterol in the liver, resulting in their level in the blood drops.

The feasibility of the present invention proves a specific example of obtaining ointments on the basis of afterline content 0,160% of the statin lescol (fluvastatin), called "Attestat". Instead of lescol in the proposed ointments you can use other known statins: mevacor (lovastatin), or zocor (simvastatin), or lipostat (pravastatin), or lindens who IMAR (atorvastatin). You get a ointment with similar therapeutic effect.

To get proposed as the object of a patent anti-inflammatory ointment AFRISTAT use the following ingredients:

- attilly on FS 42-3809-99 in the form of ointment.

- Statin (lescol-fluvastatin) in the idea of a powder or granules

Per. No. in Russia: Novartis Pharma AG (Switzerland) 008833 from 16.12.1998 g Novartis Farmaceutica S.A. (Spain) 011859/01-2000, 17.04.2000,

For more ointment into the pot stirrer and homogenizer load 75% of the required number afterline.

Statin pounded into fine powder, sieved through sieve No. 38, weighed on an analytical balance in the right quantity, then carefully rubbed with epilinum in the ratio of at least 1:10 and fed into the boiler, followed by stirring for 5-7 minutes.

In the resulting mass is added to the desired amount afterin and mix thoroughly for 15 to 20 minutes to form a homogeneous mass of light-yellow or light yellow with a greenish tint, with low specific smell.

Ointment AFRISTAT applied to the skin in the area of the carotid arteries (lateral surface of the neck) 1 time per day in the amount of 0.5 to 2.0,

When the content of the statin in ointments less 0,080% specific action moderately expressed, and when its content is more 0.240% of the effect is not practically increase the W (the difference between false). The best is the concentration 0,160%.

The composition of the studied compositions shown in table 1.

Previously conducted experimental tests on animals, which allowed to determine the optimal composition of the ointment, which was named "Attestat". It was found that the proposed anti-inflammatory ointment does not have acute and chronic toxicity, local irritant effect, not cumulated, not a potential allergen. Confirmed anti-inflammatory ointments, especially in animals 2 and 5 groups. In addition, it should be noted their high anti-edema effect.

0,080
Table 1
Studied composition ointment
No.

p/p
ComponentsComposition, wt.%Control
Lescol - fluvastatinLipostat - pravastatin
1234567
1Afterin99,92099,84099,76099,92099,84099,760-
2Statin0,1600,2400,0800,1600,240-
3Vaseline------100

The study was conducted on 70 Mature white rats with severe experimental hyperlipidemia, distributed into 7 groups of 5 males and 5 females in each. Animals within 30 days applied the ointment, according to the group 2 area of the skin in the area of the carotid arteries in size 2×2 cm once a day. Before the beginning of the experiment and the next day after it investigated the peripheral blood, and performed biochemical analysis of blood serum. Below are some data obtained in animals 2, 5 and control (7) groups (see table 2).

From these data suggest that statins concentration 0,160% significantly reduce hyperlipidemia, including total lipids 8.7 to 12.2%, β-lipoproteins on 17,74-22,56%. At the same time cholesterol is reduced by 12,95-16,07%, and the viscosity of the serum 17,44-22,05%.

Table 2
The parameters of blood serum of rats in the dynamics
№ p/pImpactTerm studies. Blood lipids, mg %β-lipoprotein, mg %Cholesterol, mg %Viscosity
1Controlto229±3,8362±1,8467,2±0,861,95±0,03
after226±3,2761±1,3565±0,791,89±0,06
Lescol 0,160%to229±3,8362±1,8467,2±0,861,95±0,03
after209±2,52*51±0,69*58,5±0,94*1,61±0,08*
Lipostat 0,160%to229±3,8362±1,8467,2±0,8b1,95±0,03
after201±3,06*48±1,63*of 56.4±1,02*1,52±0,07*
Note. Significant values at p≤0.05 is marked with *.

The comparison is carried out with the parameters of the control group.

To research all figures are based on 70 animals.

On the basis of the obtained data was prepared in a pharmacy by way ointment AFRISTAT for klinicheskoj the application.

Here are clinical examples of the use of the ointment AFRISTAT for local treatment.

1. Patient P., 52, within 10 years, suffering from essential hypertension stage 3, coronary heart disease (CHD) in the form of strokes voltage 1-2 F.K. Despite intensive treatment and compliance hypocholesterolemia diet, identified elevated levels of total cholesterol to 6.8 mmol/l, low density lipoprotein - cholesterol of 4 mmol/l, triglycerides - to 3.36 mmol/l, decreased high density lipoprotein - HDL to 0,684 mol/L. When performing duplex scanning of the carotid arteries detected seal intima in the proximal internal carotid artery local atherosclerotic plaques, stenocereus the lumen of the vessel to 20%. On the background diet compliance hypocholesterolic the patient was prescribed a course of local therapy AFRISTAT (lescol 160 mg per 100 g of ointment). It is recommended to apply 2 g ointment on the night of the carotid arteries. After 4 weeks the biochemical analysis of blood: total cholesterol - 4,94 mmol/l, triglycerides - to 2.42 mmol/l, LDL - 3.1 mmol/l, HDL - 0,76 mmol/L. Duplex scanning of the carotid arteries: the thickness of the intima-media of the common carotid arteries less than 0.9 mm in the proximal internal carotid artery atherosclerotic plaques, stenocereus clearance to 11.9%.

2. Patient S., 71,, for m is ogic years, suffering from essential hypertension stage 3, risk group 4, CHD, painless form of ischemia in type 2, dyslipidemia 2A type. Admission: total cholesterol was 7.3 mmol/l, LDL - 5.7 mmol/l, HDL - 1.05 mmol/l Duplex scanning of the carotid arteries: the intima-media of the common carotid arteries thickened to 1.4 mm, at the mouth of the right subclavian artery, atheromatous plaque, stenoziruyuschaya the lumen of the vessel up to 35%, in the region of the carotid bifurcation - the atherosclerotic plaque with stenosis of up to 40%.

Were assigned to the treatment: hypocholesterolemia diet, Renitec 10 mg bisoprolol 5 mg, aspirin 0,125. When re-examination after 4 weeks of positive changes in the lipid spectrum of blood did not happen. Further appointed local therapy AFRISTAT (lescol 160 mg per 100 g of ointment). It is recommended to apply 2 g ointment on the night of the carotid arteries. After 1 month of local therapy studies: total cholesterol 5,61 mmol/l, LDL a 3.87 mmol/l, HDL-C increased 1.58 mmol/l After 12 weeks of treatment: total cholesterol - 3.9 mmol/n, LDL - 2.2 mmol/l, HDL - 1.6 mmol/l, duplex scanning of the carotid arteries: the reduction of the thickness of the intima-media to 0.9-1.0 mm, stenosis atherosclerotic plaque decreased, the lumen of the right subclavian artery is 98% of normal.

3. Patient A., 55 years. For a long time suffers from high blood pressure, coronary artery disease. In 2002 he suffered acute infer the t of the myocardium, in the same year is an acute disorder of cerebral circulation, within 3 years diagnosed dyslipidemia 2-b type. Takes treatment, observes hypocholesterolemia diet. Repeatedly cardiologist recommended taking statins. However, due to their high cost, the patient was unable to buy them. The hospital was assigned the rate of local therapy attestator (lescol 160 mg per 100 g of ointment). It is recommended to apply 2 g ointment on the night of the carotid arteries. Before treatment total cholesterol was 5,61 mmol/l, triglycerides - to 3.02 mmol/l, LDL - 3,59 mmol/l, HDL - 0,656 mmol/l, haemoglobin rate - 7,6; ultrasonic examination of the intracranial arteries revealed thickening of the intima-media of up to 2 mm, in the course of the carotid arteries lazerous single atherosclerotic plaques, stenocereus the lumen of a vessel of up to 15%.

After 4 weeks of treatment, total cholesterol was 4,48 mmol/l, triglyceride is 1.91 mmol/l, LDL - 2,85 mmol/l, HDL - 0,755 mmol/l After 12 weeks of treatment: total cholesterol was - 3.54 mmol/l, triglycerides - is 1.81 mmol/l, LDL - of 1.93 mmol/l, HDL - 0.78 mmol/l, haemoglobin rate - 3,53; duplex scanning of the carotid arteries-the thickness of the intima-media of 0.9-1.0 mm, plaques not lazerous.

So, experimental animal testing allowed us to determine the Optima is capacity composition of anti-inflammatory ointment AFRISTAT. It is established that the ointment does not have acute and chronic toxicity, local irritant effect, does not accumulate in the body, is not a potential allergen.

Experimentally in animals and clinically confirmed the positive effect of the ointment, the anti-inflammatory activity. Performed posed technological challenges, i.e. achieved a pronounced hypolipidemic effect of the proposed anti-inflammatory ointment.

It is proved that the statin drug in the form of ointment, much cheaper than tablets or capsules. Thus, when the maximum local application of ointments (2 grams per day, containing 3.2 mg statin), its consumption is only 60 grams per month, i.e. the consumption of statins decreases in comparison with oral way (depending on dosage) in 3-750 times while maintaining therapeutic effect. It makes available a wide statin drug in the form of ointment for the treatment of patients both in the inpatient and outpatient settings.

Given the above, we can conclude that the proposed anti-inflammatory ointment meets the criteria of novelty, non-obviousness and industrial applicability.

Thus, the obtained anti-inflammatory ointment with hypolipidemic effect called AFRISTAT, which is offered to the legal protection of a patent for an invention.

Sources of information

1. Ivanova L.A., Kopteva TRIGGER the Selection of the optimal acid concentration mefenamovoy and benzoflavone in ointments. - Pharmacy. 1991, 40. No. 3. - P.15-17.

2. Cleaner I. age related and degenerative changes in the joints and spine. // M - Medgiz. - 1962.

3. Mashkovsky PPM Medicines. // M - Medicine. - 1993. - part 1, 2.

4. Nasonova V.A., Astapenko MG Clinical rheumatology. // M - Medicine. - 1989, - 592 S.

5. Medicines used in medical practice in the USSR. Ed. Klyuyev M.A., M. - Medicine. - 1990, - 512 S.

6. Nelyubov M.V., Bashtanka A.F., Kuncheva M.M. and other Application calavita in the treatment of urological diseases. // Scientific and practical use. Conf.: Galavit in experiment and clinic. - M - 1998. - P.26-28.

7. Orlova T. Development of composition and technology of ophthalmic suspensions of non-steroidal anti-inflammatory drugs. // Autoreponders. - M - 1990.

8. Manual immunopharmacology. / Ed Dale M.M., Formen JK, M - Medicine. - 1998, - 332 S.

9. Ackerman, S.J., G. Kephart, T. Habermann et all. Localization of eosinophil granule major basic protein in human basophils.//J. exp. Med. - 1983. - V.158.-N3. - R-961.

10. Ackerman, S.J., Loegering D.A., P. Velge et al. Distinctive cationic proteins of the human eosinophil granule major basic protein, eosinophil cationic protein, and eosinophil-derived neurotoxin. // J. Immunol. - 1983. - V.131, N6. - R - 2982.

11. Adams D.O., Hamilton T.A. Phagocitic Cells: Cytotoxyc Activities of Macrophages // Inflammation: Basic Principles and clinical cjrrelates. // Eds. By J.I. Gallin et al. - New York, 1988. - .471-492.

12. The money A.V. and other Lescol and coronary atherosclerosis: results of three controlled trials //proc. the honey. the magazine, so 4, M, 2001, p.1-7.

13. Glaser MG, Sobolev KE, Sorin G. // Lipid-lowering effect of fluvastatin (lescol) in patients with ischemic heart disease old age. Moscow honey. Acad. them. Sechenov. The clinically. pharmacology and therapeutics, 1999, vol 8 (3), p.29-31.

14. Patrick W.J.C. Serruys. //The use of fluvastatin for prevention of cardiac events following successful first percutaneous intervention. A randomized controlled trial (reprinted) JAMA, June 26, 2002 - V287. No. 24.

1. Anti-inflammatory ointment with hypolipidemic effect, containing afterin, characterized in that it contains afterin basis for ointments and statin in the following ratio, wt.%:

Afterin basis for ointments99,76-99,920
Statin0,08-0,240

2. Anti-inflammatory ointment according to claim 1, characterized in that statin use lescol (fluvastatin).

3. Anti-inflammatory ointment according to claim 1, characterized in that afterin contains 40% epiderma.



 

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22 cl, 2 tbl, 1 ex

FIELD: medicine, endocrinology, pharmaceutical technology, pharmacy.

SUBSTANCE: invention relates to nateglynide-containing preparation used in treatment of diabetes mellitus that comprises nateglynide as an active component and a carrier wherein nateglynide in amorphous form and indicated carrier represents hydrophilic material. Amorphous property of crystalline nateglynide is provided by the following methods: 1) by dissolving nateglynide crystals in pharmacologically acceptable solvent in common with hydrophilic materials taken among the group consisting of water-soluble polymers, water-swelling polymers, sugar alcohols and salts followed by granulation in fluidized layer, granulation by stirring at high rate, drying by spraying and process for coat applying for granulation of amorphous nateglynide; 2) by mixing nateglynide crystals with hydrophilic materials taken among the group of water-soluble polymers, water-swelling polymers, sugar alcohols and salts and the following application of the high shift force to the prepared mixture; 3) by mixing nateglynide crystals with hydrophilic materials taken among the group of water-soluble polymers, water-swelling polymers, sugar alcohols and salts and the following plasticizing the prepared mixture in melt by heating and milling at cooling; 4) by dissolving nateglynide crystals in pharmacologically acceptable liquid additives wherein liquid additives represent water-soluble polymers that are liquid at 37°C. Using amorphous nateglynide allows preparing the nateglynide preparation with immediate release wherein the dissolving rate of medicinal agents is high and without crystalline transition during preparing or preserving preparations.

EFFECT: valuable pharmaceutical properties of preparation.

6 cl, 3 tbl, 9 dwg

FIELD: medicine, pharmacy.

SUBSTANCE: invention proposes using xenogenous oligo-and/or polyribonucleotides, namely total RNA and tRNA, as an active component of external anhydrous medicinal agent for a single treatment of skin tumor relapse (for example, basalioma) or infections caused by herpes virus and the corresponding method for treatment. The claimed external anhydrous medicinal agents decline effectively relapses of indicated diseases after a single intake.

EFFECT: enhanced effectiveness and valuable medicinal properties of agents.

5 cl, 2 ex

FIELD: veterinary science.

SUBSTANCE: the suggested preparation contains dense propolis, vegetable oil, extract out of dead bees based upon glycerol, lanolin, honeycombs' cutting off, moreover, all the components should be taken at certain quantitative ratio, weight%: honeycombs' cutting off 15-20, dense propolis 20-25, extract out of dead bees upon glycerol 7.5 -10, lanolin 20-25, vegetable oil - the rest, moreover, honeycombs' cutting off includes honey residues. The preparation in question is of high biological activity, provides shortened terms for recovery in animals and excludes allergic reactions.

EFFECT: higher efficiency for therapy.

1 cl, 8 ex

FIELD: medicine, phytotherapy, infectious diseases, pharmaceutical industry.

SUBSTANCE: invention relates to a method for preparing ointment used in erysipelas treatment. Method for preparing ointment used in erysipelas treatment involves milling washed and dried viper's-bugloss roots (Echium rubrum, Jacg, family Boraginaceae) and their extraction with melted butter under the definite conditions. Then extract is infused at stirring for a definite time, macerate is filtered off at cooling to a definite temperature and poured off. Extraction is carried out twice, vegetable raw residues are squeezed out, and prepared sap is combined with first two extracts, settled for a definite time and bottled. Method provides preparing ointment that promotes to effective treatment of erysipelas and reducing treatment period.

EFFECT: improved preparing method, valuable medicinal properties of ointment.

5 ex

FIELD: medicine, oncology.

SUBSTANCE: one should intravenously irradiate blood with low-energy He-Ne laser including recanalization and venous catheterization at installing a quartz light guide into venous lumen through the catheter. At initial stage of surgical therapy on should introduce a light guide into the lumen of V.portae to irradiate blood in the basin of portal circulation during the main stages of operation conducted. Before operation, one should intramuscularly inject halavit at the dosage of 100 mg. The innovation enables to increase efficiency of laser therapy due to affecting "a target organ" directly, that is a liver, with photomodified blood with the purpose to achieve antimutagenic and antimetastatic effect, normalize the processes of antioxidant protection, stimulate the mechanisms of anti-cancer immunity and improve local microcirculation.

EFFECT: higher efficiency of prophylaxis.

1 ex

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