Rectal suppositories containing vitamin complex

 

(57) Abstract:

The invention relates to medicine, more specifically to a drug in a form representing a suppository containing vitamin complex. The invention consists in that the composition contains kokarboksilazu hydrochloride, Riboflavin, lipoic acid and suppozitornyj based on one candle mass of 1.27-1,41, the Invention provides for obtaining a medicinal product in the form of suppositories, which has high biological activity, the ease of use, and has no side effects. table 1.

The invention relates to the field of medicine, but rather a drug in a form representing a suppository containing vitamin complex.

The invention can most effectively be used as a medicine in the form of a suppository (candles) for the treatment of diseases, leading to the decrease of redox processes in tissues of internal organs (chronic tissue hypoxia) - low immunity, chronic bacterial and viral infections, chronic somatic diseases as a means of influencing tissue metabolism.

Action regulirovaniya two most important stages of the Krebs cycle: the inclusion of pyruvic acid oxidation her to acetyl COA and oxidative decarboxylation of a-Ketoglutarate acid.

Known medicinal composition - pills "Decemeber" [1] , coated, containing, g:

Retinol - 0,00227 (ME) (Vit. A)

Thiamine chloride - 0,02 (Vit. B1)

Riboflavin - 0,01 (Vit. B2)

Pyridoxine hydrochloride - 0,02 (Vit. B6)

Cyanocobalamin Is 0.0001 (Vit. B12)

Folic acid - 0,005 (Vit. Sun)

Rutin - 0,02 (Vit. P)

Tocopherol acetate - 0,01 (Vit. E)

Methionine - 0,2

Ascorbic acid is 0.2 (Vit. C)

Nicotinamide - 0,05

However, this composition is not suitable for children neonatal period, infancy and early age, for patients with impaired function of the gastrointestinal tract (intestinal dysbiosis, gastritis). In addition, advanced ingredients of this composition are capable of causing allergic reactions in immunocompromised patient population.

Known medicinal composition [2] , used in children "Unicap" (syrup: 100 ml in vials). 100 ml of syrup contains:

The thiamine hydrochloride 10 mg

Riboflavin 5 mg

Pyridoxine hydrochloride 5 mg

Nicotinamide 100 mg

Calcium Pantothenate 5 mg

Para-aminobenzoic acid 2.5 mg

Inot the g glycerol 15 g of condensed milk.

This composition is applied under conditions involving increased need for b vitamins (the period of intensive growth, pre-and postoperative period, chronic infectious diseases, diseases of the digestive tract and nervous system, and so on ). However, due to the large set of components, possible allergic reactions, which is especially important for newborns and infants, and can not be used with nausea and vomiting.

Known medicinal composition "Bioplex" [3] (solution for injection), the closest composition and intensity of absorption of the drug for the claimed composition, which we have chosen as a prototype, as the closest to the technical nature of the claimed object. Composition "Bioplex" contains mg:

Thiamine chloride - 40

Riboflavin - 4

Pyridoxine hydrochloride - 8

Calcium Pantothenate - 10

Cyanocobalamin - 4

Nicotinamide - 100

The effect of the drug is determined by the effects of the vitamins included in its composition. This song is also used in conditions involving an increased need for vitamins of group C. However, this arrangement is not convenient for independent use, is TRASTA the use of this composition is undesirable, because it is accompanied by pain effect, which reduces the effect of the treatment.

The present invention is the creation of medicines in the form of a suppository, affecting tissue metabolism, contributing to the improvement of redox processes in tissues of internal organs, convenient to use, no side effects.

The problem is solved in that the inventive composition contains kokarboksilazu hydrochloride, Riboflavin, lipoic acid and suppozitornyj based on one candle mass of 1.27-of 1.41 g (g):

Cocarboxylase hydrochloride - 0,0225-0,0275

Riboflavin - 0,0018-0,0022

The lipoic acid - 0,011-0,013

Suppozitornyj basis - Rest

As a medicinal components use the following vitamin preparations.

Cocarboxylase hydrochloride (FS-2381-98) is diphosphorus ester of thiamine (vitamin B1)-freeze dry hygroscopic porous mass of white, with low specific smell. In terms of their biological action approaching vitamins and enzymes. Is the coenzyme of enzymes involved in carbohydrate metabolism. Two main reactions in the body - cocarboxylase is usually well tolerated, low-toxic. For medical use kokarboksilaza applied in the form of cocarboxylase hydrochloride.

Riboflavin (vitamin B2) (HFH, senior 585)-6,7-dimethyl-9-(ribitil)-isoalloxazine, yellow-orange crystalline powder with low specific smell, bitter taste. The light is not sustainable. When entering the body interacts with Riboflavin ATP acid and forms playmonopolyonline and flavine adenine dinucleotide. The latter are coenzymes of flavoproteins and participate in the transfer of hydrogen and regulation of redox processes. Riboflavin is involved in carbohydrate, protein and fat metabolism. He also played an important role in maintaining normal long eye function and hemoglobin synthesis. Riboflavin low toxicity.

The lipoic acid (PS-1918-94)-6,8-cityoklahoma acid, crystalline powder light yellow color, bitter taste, with a specific smell. The lipoic acid is a coenzyme involved in the oxidative decarboxylation of pyruvic acid and a-ketoacids, and plays an important role in the formation of energy in the body. The nature of the biochemical steps lipoa the underwater exchange, has a lipotropic effect, affects the metabolism of cholesterol, improves liver function, has a detoxifying effect in case of poisoning by salts of heavy metals and other intoxication.

As suppozitornoj bases use cocoa butter, tallow, type a, Witepsol.

Cocoa butter (the State Pharmacopoeia - GFH St) - fatty oil obtained by pressing roasted and released from the peel of cacao seeds. Dense homogeneous mass of yellowish color, sabarmathi smell of cocoa and a pleasant taste, brittle at room temperature, melts at 30-34oS, becoming transparent liquid, an acid number of not more than 2.25, iodine 32-38.

Tallow, type a (VFS 42-W-97), this confectionery fat, firm-based plasticized hydrogenated fat, from white to white with a creamy tinge, homogeneous, solid at room temperature, odorless, melts at a temperature of 34-36oS, becoming transparent liquid, density 0,920-0,950. The pour point of not lower than 30oWith, an acid number of not more than 0.3.

Witepsol (ND 9584-98) is a mixture of triglycerides of natural dietary fatty acids C12-C18 with a small amount of mono - and diglyceride the second transparent state. The melting point of 33.5-35,5oWith the solidification temperature of 27-30oWith, iodine number not greater than 3, the acid is not more than 0.3.

Doses of drugs were chosen on the basis of doses in injectable dosage forms. The spacing of the components is selected according to the Order of the RF Ministry of health 305 dated 16.10.97 "On the norms of tolerance in the manufacture of pharmaceuticals and packaging of industrial products at the drugstore."

Reducing the number of cocarboxylase hydrochloride does not lead to the desired therapeutic effect. The increase, in some cases, can lead to allergic reactions.

Reducing the number of Riboflavin does not lead to the desired therapeutic effect, the increase may lead to hyperinflation where there decrease appetite, a drop in body weight, weakness, headache, burning skin, pain in the eyes, pain in the corners of the mouth and lower lip.

Dose reduction of lipoic acid does not give the desired therapeutic effect. Increasing the dose possible dyspeptic symptoms (pain in the epigastric region, heartburn), allergic skin rashes.

Number basis for the medicinal product featur what the active ingredients of suppositories and therefore may slow down the healing effect. Decrease the basis of less than 1.27 g leads to an increase in the concentration of the medicinal substance in the medicinal product, which can have a toxic effect.

The composition is prepared as follows: the required number of medicinal substances in the form of powders are mixed, following the rules of mixing powders (GFH 1, vol. 2, S. 150). The resulting mixture was triturated with a small amount of molten basics and introducing the remaining portion of the fused bases of the fractional portions and stirred to obtain a homogeneous mass. Received suppozitornyj mass is filtered and fed to the machine for the manufacture of suppositories. The masses poured into the cell from a film of polyvinyl chloride (type EP-73S) at 32-34oC and cooled at a temperature of 5-10oC.

For preparing suppositories on Witepsol W 35 received suppozitornyj was poured at a temperature of 36-38oC, with continuous stirring in a pre-chilled suppozitornoj forms that leave at room temperature. After 15-20 minutes release molded suppositories.

For preparing suppositories solid fat, the type And received suppozitornyj was poured at a temperature of 34-38oFrom philadelhia. After 10-15 minutes, the forms are removed to free the molded suppositories.

Received suppositories light yellow, odorless, torpedo-shaped form, has the following physico-chemical characteristics.

The basis of cocoa butter

The full deformation 5 min

The melting temperature of 30-31oWITH

The solidification temperature of 25oWITH

Hardness "ERWEKA" 3.2 kg/cm2< / BR>
The content of active substances Kokarboksilaza hydrochloride 0,0251 g

Riboflavin 0,0021 g

Lipoic acid 0,0119 g

The basis of solid fat type AND

The full deformation 7 min

The melting temperature of 34-35oWITH

The solidification temperature of the 31oWITH

Hardness "ERWEKA" 2.4 kg/cm2< / BR>
Potency

Kokarboksilaza hydrochloride 0,0249 g

Riboflavin 0,0021 g

Lipoic acid 0,0118 g

The basis of Witepsol

The full deformation 9 min

The melting temperature of 34.5oWITH

The solidification temperature of 28-29oWITH

Hardness "ERWEKA" 5.0 kg/cm2< / BR>
Potency

Kokarboksilaza hydrochloride 0.025 g

Riboflavin 0,0018 g

Lipoic acid 0,012 g

Studies consistently is sitories not change for 2.5 years (observation period) during storage at a temperature of 3-5oC (refrigerator). Using chromatography in thin layer of sorbent (TLC) and high performance liquid chromatography (HPLC) identified the lack of interaction between vitamins a and suppozitornyj the basics. Histological study of the internal organs of rats and rabbits treated with suppositories with a complex of vitamins and coenzymes, irritant and toxic effects not found.

Cytochemical studies and clinical observations on the comparative evaluation of the bioavailability and efficacy of different dosage forms cocarboxylase hydrochloride, Riboflavin, and lipoic acid (injections, powders, tablets, pills and suppositories) showed the greatest efficacy of these drugs in a rectal in the form of suppositories prepared on the fundamentals of cocoa butter or tallow type a or Witepsol.

Contraindications and side effects of suppositories is not revealed.

Newborns and infants suppositories rectally 1 pc. through the day, older children, 1 pc. each day for 10 days adults: 1 PCs 2 times a day for 10 days. After the introduction of the candle preferably the patient's stay in bed the repeat within 2-6 months.

The table lists examples of specific compounds of the proposed suppositories.

The use of the claimed composition allows to obtain a dosage form is a suppository, with medicinal properties in the following conditions: low immunity, chronic bacterial and viral infections, chronic somatic diseases as a means of improving tissue metabolism.

The proposed dosage form is a suppository containing kokarboksilazu, Riboflavin, lipoic acid, in the country and abroad are missing. In comparison with existing analogues - coated tablets, syrup, suppositories possess high biological availability, ease of use, can be applied with increased gag reflex when malabsorption in the gastrointestinal tract. Moreover, with the introduction of rectal able to eliminate or significantly reduce the presystemic clearance of vitamins and avoid inactivation of the enzymes of the digestive tract.

Compared to the injectable form (prototype) application of suppositories painless, does not cause degeneration of the endothelium of blood vessels, necrosis, fusion of tissues, severe allergic reactions of all incoming ingredients the mixture menuitemindex injection before their introduction may lead to undesirable consequences.

The proposed dosage form in the form of suppositories can be used as a standalone treatment and as an adjunct to standard treatment.

Sources of information

1. Mashkovsky, M. D. "Drug" 1998 , ed. 13, T. 2, S. 107.

2. Mashkovsky, M. D. "Drug" 1998 , ed. 13, T. 2, S. 108.

3. Drugs in Russia. Reference Vidal, 1998 , section C. , S. 4.

Rectal suppositories containing vitamin complex and suppozitornyj base, characterized in that as vitamins supposely contains cocarboxylase hydrochloride, Riboflavin, lipoic acid in the following ratio of components on one candle mass of 1.27-of 1.41 g, g:

Cocarboxylase hydrochloride - 0,0225 - 0,0275

Riboflavin - 0,0018 - 0,0022

The lipoic acid - 0,011 - 0,013

Suppozitornyj basis - the Rest

 

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