Suspension methyluracil


(57) Abstract:

The invention relates to medicine and the pharmaceutical industry, concerns the creation of new dosage forms. The proposed suspension methyluracil containing form methyluracil and water. The suspension has a high wound-healing activity, prolonging effect and can be used for healing burns and wounds of different origin. table 1.

The invention relates to medicine and pharmaceutical industry and for the creation of new dosage forms of the derivatives of uracil.

Preparation of pyrimidine series - methyluracil belongs to the group of stimulants metabolic processes and is widely used in medical practice to improve the resistance of the organism to infection, accelerate the regeneration of tissues damaged by the disease process, as well as immunostimulant. Pharmacopoeial methyluracil comes in the form of powders, tablets (0.5), candles (0.5) and 5-10% ointment.

Known-form 2,4-dioxo-6-methyl-1,2,3,4-tetrahydropyrimidine (methyluracil), which is assigned to N state of registration 7382186 September 12, 1986 , is used as a wound healing agent.

However, lanolin base interferes with the normal gas exchange, which has a negative effect on the healing process, especially for slow processes. The lack of prolonging effect necessitates frequent introduction of eye ointment (up to 6 times per day), which creates discomfort during treatment, and may also lead to additional trauma burn.

The purpose of the invention is the creation of a new dosage form methyluracil with prolonging effect, high wound healing activity in the absence of side effects.

The essence of the invention is that first proposed suspension methyluracil, containing, by weight. % :

The powder-form methyluracil 1,0-2,5


solution or water for injection to 100.0

Because the proposed dosage form methyluracil previously was not known, you should consider the claimed solution as a pioneer.

Unlike eye ointments containing form methyluracil, suspension-shaped methyluracil in the proposed combination of components reveals unexpected, not previously known effect of prolonged action, which allows 3 times to reduce the share of the acyl due to the fact, only in the specified concentration range shows high therapeutic effect is not accompanied by side effects.

When the concentration-shaped methyluracil below 1.0% therapeutic effect decreased significantly with an increase in concentration up to 3.0% was observed signs of irritation of the wound surface.

Use as a pharmaceutical diluent water for injection or saline due to the fact that only a combination-form methyluracil with one of these diluents contributes to prolonging effect of the active substance.

Preparation of suspension shall be in accordance with the standards of GF X by mixing the ingredients with the creation of the dispersion-heterogeneous system in which the dispersed phase is a powder-form methyluracil, and the dispersion medium is water for injection or saline.

The authors found that the form of methyluracil manifests in suspension prolonged effect.

For evidence of extension was determined by the rate of dissolution form methyluracil in the device "rotating basket" type DT-D6 firm "Erweka (Germany) when the mode mixing at 50 rpm Medium is predelli spectrophotometric method with spectrophotometer firm "Perkin-Elmer" N 75 at a wavelength of 259 nm. As a comparison used pharmacopoeial methyluracil under identical conditions. Parameter comparison served as a constant dissolution rate based on the average results of the transition of the drug in the solution is taken from the amount (0.25 g) from 0 to 45 minutes In the quality control used water for injection.

Data analysis showed a high rate constant of dissolution pharmacopoeial methyluracil K = 0,18 min-1and expressed prolonged dissolution-shaped methyluracil with a rate constant K = 0,025 min-1.

Sedimentation stability of the claimed suspension was studied photoelectrocolorimetry method. In a comparative perspective has been studied 2% aqueous suspension pharmacopoeial methyluracil. Analysis of the obtained curves sedimentation suggests that 2% suspension form methyluracil has good stability and preserves the homogeneity within 2 hours the Suspension pharmacopoeial methyluracil, practically, has no sedimentation stability, within 5 min the optical density at her sharply.

The optimality of the selected number of powder methyluracil in the composition of the suspension was confirmed by experimental IIT reduce therapeutic effect in eye burns and complications. In the group of animals treated with a 0.5% suspension of methyluracil, in 8% of cases occurred perforation of the cornea, and in some cases have formed intense cornea. The increase in the concentration of the suspension to 3% does not lead to increased therapeutic effect, but at the same time causes irritation of the eyeball in 78% of rabbits.

Thus, found that the greatest therapeutic effect without side effects is achieved by using a suspension with a content-form methyluracil from 1.0 to 2.5% .

Selected pharmaceutical diluent saline or water for injection can achieve the effect of prolongation of the active substance - -form methyluracil.

Assessment of clinical effectiveness suspension methyluracil was held in biomedical studies on models of chemical burns to the eyes of rabbits.

Alkaline burns to both eyes of 3 degrees caused by the introduction of 3 drops of 5% aqueous solution of sodium hydroxide in the conjunctival SAC with exposure 17 and followed by washing with water. The degree burn was determined after 3 h, then started treatment. The treatment included subconjunctival introduction 2 times a day sterile suspension containing-foas under the control of the 1% aqueous solution of methylene blue. The treatment efficiency was evaluated according to histological studies. To this end, the cornea tissue were fixed in 10% neutral formalin, followed by pouring in the wax. Sections were stained with hematoxylin-eosin.

P R I m m e R. (claimed composition - maximum contents-shaped methyluracil in suspension).

For treatment group I animals used a 2.5% suspension of methyluracil physiological solution and water for injection, which was administered subconjuctival 2 times a day. Each group consisted of 24 rabbit (48 eyes).

The animals were killed by an air embolism on 1,3,5,7,10,14,21 and 28 days after starting treatment. Evaluation of the effectiveness of the treatment was carried out by painting the clinical course of the burn eye and the histological and histochemical studies. The results showed that by 3 days in the studied groups of animals occurred epithelization of the greater part of the cornea. However, the epithelium is very thin (1-2 layers of epithelial cells). In the underlying tissue with a core of fibrous connective tissue with many macrophages, eosinophilic leukocytes, neutrophils, lymphocytes and sprouting emocapella. The main substance of the cornea disorganized, there are areas of thinning the sooma kapitalizirovana multilayered epithelium. Part of the epithelial cells vacuolization. Own the substance of the cornea of the burn injected small blood vessels and infiltrated by mononuclear and polynuclear by leukocytes. On day 7 areas of epithelium longer, mainly multi-layered, uneven. In the underlying connective tissue infiltrated by mononuclear leukocytes, sprout blood vessels of larger caliber. After 2 weeks the epithelial defects were minor, infiltration by mononuclear leukocytes, proliferation of fibrous connective tissue and germination vessels decreased significantly. Regenerating epithelium 2-3 layers. To 18 days epithelization of the cornea ended. The epithelium covering the surface of burns, sharply layered, penetrated by blood vessels.

P R I m m e R 2 (claimed composition - minimum maintenance-shaped methyluracil in suspension).

For treatment group II animals used a 1.0% suspension of methyluracil physiological solution and water for injection.

Each group consisted of 24 rabbit (48 eyes).

Experiment similar to example 1.

The results showed that by 3 days in the study gruppovenetobanca, there are lots thinning of their own substance. In the anterior chamber of the eye accumulation of leukocytes.

At 7 days the burn mainly kapitalizirovana a multilayered epithelium that is part of the epithelial cells vacuolization. Own the substance of the cornea of the burn injected small blood vessels and infiltrated by mononuclear and polynuclear by leukocytes.

At 18 days the epithelial defects were minor. Regenerating epithelium 2-3 layer.

To 21 days epithelization of the cornea ended.

P R I m e R 3 (0.5% suspension-shaped methyluracil, the comparison group).

For the treatment group III animals used a 0.5% suspension form methyluracil.

Experiment and number of animals were similar to those of example 1. In the studied series is already on the 3rd day of observation discharge was moderate, slimy; the defect of the corneal epithelium was shallow, appeared the areas of newly formed epithelium. In subsequent follow-up period detachable remained moderate, slimy, necrotic lesions of the conjunctiva reduced in size, the formation of newly formed epithelium increased. To 10 days on the periphery of the cornea appeared single novobrdo is I. Detachable wore Muco-purulent character, was observed infiltration of the cornea, appeared purulent exudation in the anterior chamber. To 10 days at these eyes happened perforation of the cornea. On the other eyes during the process was favorable. The defect of the corneal epithelium was further reduced to 21 days was practically absent; in its place was formed cornea of varying intensity. For 28 days at 5 eyes observed the enlightenment of the cornea at the periphery and intense turbidity in the center.

The experimental results presented in the table. Analysis of experimental data showed that two-day introduction of the proposed suspension with burns of the eyes leads to full recovery of the epithelium already in 18-20 days. No side effects and complications. The peculiarity of the pharmacological action of the suspension is early vascularization of the lesion, which has a positive impact on the dynamics of wound healing and enhances the anti-inflammatory effect of the drug. At the same time, compared with the eye ointment suspension methyluracil preferred mode of administration (2 times a day, eye ointment to 6 times per day), which is associated with prolonged healing on the Sabbath., characterized in that the active substance it contains form methyluracil, and as a diluent saline or water for injection in the following ratio, wt. % :

form methyluracil 1,0 - 2,5

Saline or water for injection Up to 100.0


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