New dosage forms of demoliton in the treatment of leprosy, itching, and allergic, dermatitis herpetiformis during the

 

(57) Abstract:

The invention relates to the field of medicine and for new dosage forms of demoliton. The invention lies in the fact that the proposed demoliton in the form of capsules and ointment in the amount of active substance, respectively, 0.05-0.2 g and 2-5 wt. %. The invention provides a reduction in the number of medication to 1-2 times a week due to a longer therapeutic effect, and leads to a significant reduction of effects: nausea, reflux, dyspepsia, hepatitis. 2 C. p. F.-ly, 3 tables.

The invention relates to medicine, specifically to dosage forms containing drug demoliton capsules and ointments.

Known developed by the present authors medication demoliton (and.with. 611326), representing colpotomy complex of 1 mole of diaminodiphenylsulfone with 2 moles of methyluracil, previously used to treat leprosy, itching, and allergic, dermatitis herpetiformis during the drug in the form of "powder". Along with the inconvenience of using powder demoliton (bitter taste, need 3-5 times of admission to the day, the inability of local application in the centers of poraj the same.

The aim of the invention is the creation of new dosage forms of demoliton devoid of these shortcomings. All these years the authors have continued to develop new legform. Were created and studied in the experiment different legform demoliton: tablets, capsules, ointment, rectagel, aerosol. Of them were selected optimal legform by the greatest therapeutic effect and minimum side effects. Pharmacological Committee by its decision 5 from 24.06.99, has allowed clinical trials demoliton capsules as leprosy and anti-inflammatory agents.

The purpose of the invention is achieved by placing demoliton in gelatin capsules and the creation of 2% of dimaternovoi ointment. Experimental animal studies and clinical trials have shown the advantages of these dosage forms according to the duration and effectiveness of anti-allergic and anti-inflammatory action.

The use of a new dosage form of demoliton in the form of capsules allowed that appeared for authors obvious, to reduce the number of doses of the drug to 1-2 times a week due to a longer therapeutic effect, and led to a significant drop the capsules reduced the toxicity of the drug in rats test on LD60with 2100 (1500-2255) mg/kg up to 2500 (2232-2800)mg/kg, and does not cause undesirable changes in the blood with a long introduction of demoliton. Application of 2% of dimaternovoi ointment promotes the rapid onset antipruritic, anti-inflammatory and antiallergic effect.

The invention is illustrated by the following examples:

Example 1. The action of demoliton in various lekforma on hematological parameters in the experiment.

The impact of demoliton in powder and capsules with dimocifonum on indicators of formula blood was studied in experiments on white rats-females weighing 250 grams contained in laboratory vivarium for 10 animals in each group. Animals received demoliton in the study lekforma in subtoxic doses within 30 days. Special attention is paid to indicators of red blood, which is subject to change under the influence of diaminodiphenylsulfone. The results are shown in table.1.

As seen from the obtained results, demoliton capsules in subconsiously doses in continuous introduction virtually no effect on the level of red blood cells and hemoglobin, while demoliton again the type in "powder" CH is>/P>Anti-inflammatory effect of dimaternovoi ointment demonstrated in experiments on creating inflammation caused by thermal burn.

In experiments on outbred mice (weight 18,0-24,0 g) after thermal activity on one of the rear paws after 10 min and 2 h was applied in the same group depositnow ointment, and the other with ointment base. A day later, animals were scored, amputated both hind paws (healthy and swollen) and weighed them. Anti-inflammatory activity of the ointment was determined by its ability to reduce the development of termotek. The results of the experiment considered according to the following formula:

< / BR>
where a is antiexudative activity;

Mo is the mass of swollen paws in the experience;

MH is the mass of healthy paws in control;

The IOC is the mass of swollen paws in control;

ILC - weight healthy paws in control.

Anti-inflammatory activity of dimaternovoi ointment was determined by the ability to reduce the development of termotek. The results are presented in table.2.

Thus, gimazitdinova ointment reduces inflammation caused by thermal burn.

Example 3. Comparative clinical data the results of treatment of patients with leprosy, dermatitis herpetiformis dur the clinical trials of demoliton capsules (minutes of the pharmacological Committee 5 from 24.06.99,) examined 50 patients: 20 patients with leprosy, 15 patients with dermatitis herpetiformis during the, 14 patients with atopic dermatitis, of which 50% of patients took demoliton powder (25 people) and 50% of patients took demoliton capsules (25 people).

As a result of treatment and examination, the following conclusions were made:

1. When using capsules demoliton therapeutic effect (reduction, and then the disappearance of itching, inflammation, swelling lesions) occurred 30-50 min later than in the application pharmaceutical form "powder", but the duration of therapeutic effect was much longer. For example, if you use powder demoliton therapeutic effect lasted for 8-12 h, applying capsules demoliton therapeutic effect lasted 24-48 hours, sometimes up to 72 hours This allowed the authors to propose a new application of demoliton capsules, reducing the intake of the drug demoliton to 1 capsule in 24 to 48 hours In some cases, therapeutic effect was evident even when taking 1-2 capsules demoliton during the week. Clinical and laboratory indicators of inflammation (erythrocyte sedimentation rate, C-reactive protein) normalized already on 5-7 day reception demoliton capsules.

Treatment in the period of exacerbation (recidi is 7-12 days (average of 9.4 days), while in the treatment dimocifonum powder this period amounted 18-24 days (21 days).

The above has allowed not only to obtain significant economic results due to the sparse reception demoliton, but also to offer new ways of treating dimocifonum.

2. When taking demoliton capsules unexpectedly for authors showed no side effect in the form of hypochromic anemia, toxic hepatitis, immunosuppression. The study results side effects are presented in table. 3.

Example 4. Comparative data of the results of treatment of dermatitis herpetiformis during neurodermatitis drug in the form of "ointment".

Use dimaternovoi ointment had a fast and stable antipruritic and anti-inflammatory effect. Compared with her boric-Naftalan ointment so pronounced therapeutic effect did not possess.

The study included 60 patients (Centre for research dermatovenerologic Institute, Moscow, Centre of clinical immunology and Allergology, Vladivostok, Department of skin and venereal diseases of the Moscow medical Academy), including atopic dermatitis - 39 blinies on lesions 2-3 times a day until the disappearance of clinical manifestations.

The performance was full or partial (80%) devolution rash on 5-7 days of treatment, the disappearance of itching, burning.

Positive effect (clinical recovery) was observed in 34 patients (17 patients with atopic dermatitis during the 10 - neurodermatitis, a significant improvement was observed in 22 patients with atopic dermatitis and dermatitis herpetiformis during the. Itching was gone within the first hour after application of the ointment. Side effects and complications are marked intensification of itching in three patients with atopic dermatitis and increased itching with the appearance of redness and irritation in one patient with dermatitis herpetiformis during the. This may be due to individually intolerance Dimexidum.

For comparison, the 30 patients, among which 18 people with atopic dermatitis, 6 - with dermatitis herpetiformis during the 6 - with neurodermatitis, was appointed boric-Naftalan ointment, which is only 5 patients with atopic dermatitis and three patients with neurodermatitis caused clinical improvement. The remaining patients not only had a positive effect, but the continued progression of the pathological process.

Based on the foregoing, we can conclude that the new drug form of demoliton, which is our invention, virtually created the conditions for new ways to apply demoliton with the elimination of side effects and a significant economic effect (treatment dimocifonum capsules allows to obtain a therapeutic effect at a dose of 2-4 smaller than dimocifonum in powder form).

Sources of information

Grenuk ie - "New domestic drug demoliton and its combination with rifadin and lamproom in the treatment of patients lepromatous leprosy". - PhD thesis, Moscow, 1984

Copyright certificate 611326. "Antipruritic and anti-allergic agent democide".

1. Drug, possess anti-allergic, anti-inflammatory, antipruritic, leprosy effect, characterized by the fact that it is made in the form of a capsule and contains as active substance demoliton in the amount of 0,05-0,2 g

2. Drug createresource fact, it is made in the form of ointments and contains as active substance demoliton in the amount of 2-5 wt. %.

 

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