CS267494B1 - Loose medicamentous form - Google Patents

Abstract

The solution concerns bulk drug active ingredients and conventional formulations excipients, characterized in that as vehicle contains 10 to 100%. wt. calcium salts chemically oxidized and radiation degraded pulp pulp carboxyl-containing form at least 10 ¢ - wt. and ion content Calcium 4.5 to 7.5 5? wt. Vehicle in the bulk dosage form of the invention cannot stand in the wound breeding ground for microorganisms and therefore does not occur during its use to wet and purge wounds, but vice versa wound healing is considerably accelerated because of the bulk formulation with the vehicle according to the invention has hemostatic effects.

Description

The invention relates to bulk dosage forms containing active ingredients and customary excipients, characterized in that the vehicle used is either wholly or at least in part the calcium salt of chemically oxidized and radiation-degraded cellulose.

Preferably, it is used here that said calcium salt is absorbable and has hemostyptic effects.

Oxidized cellulose is the product of oxidative (nitro- or otherwise) and radiation degradation degradation of cellulose at a dose of e.g. 75 kGy, which is characterized by free carboxyl groups converted to calcium salts. It is sterilized by radiation. Must contain min. 10 wt., Car _w 2+ boxyl groups and 4.5 to 7.5 wt. Ca,

Various vehicles have always been and still are used in bulk dosage forms (backfill) / Czechoslovak Pharmacopoeia, ed. IV., Pp. 3O2 / III, 94 / II, 478/11, 871/11; Melichar et al., Galician and Drug Technology, pp. 25, 46, 364, 368; Starkenstein, Lehrbuch d. Pharmakol., Toxicologie u. Arzneiverordnung, pp. 659, 666 /, such as talc, white clay, zinc oxide, sucrose, lactose and the like, which are indifferent or have only a small supportive therapeutic effect. The importance of a suitable vehicle is particularly true for wound dressings, where lactose is often used, the main advantage of which lies in its absorbability. A significant disadvantage of lactose or other carbohydrates used is the solubility in water, resp. in body fluids, the resulting solutions being an excellent breeding ground for microorganisms, so that after treatment with such a powder with a less suitable vehicle, such as lactose, wetting and festering of the wound can occur. This prolongs the healing of the wound and it is often necessary to remove the bandage prematurely and treat the wound in another way. Other vehicles, hitherto commonly used, such as the above-mentioned talc, white clay, are not always the most suitable, are not absorbed and have little or no supportive therapeutic effect and are not suitable for wound healing fillings.

These disadvantages are eliminated by a bulk dosage form containing active ingredients and customary excipients, characterized in that it contains 10 to 100% by weight of calcium, chemically oxidized calcium and radiation-degraded celluloses in powder form with a carboxyl group content of at least 10% by weight, and calcium ion content 4.5 to 7.5 / wt.

The method of preparation of powdered oxidized cellulose protects Czechoslovakia. AO No. 221 227/11 / / B1 /, where the cellulose is oxidized with nitric acid or a mixture of nitric acid and sodium nitrite and, after partial removal of the acid, converted to the calcium salt by dispersion in a solution of calcium chloride and acetate in the presence of isopropyl alcohol. The size of the resulting particles suitable for bulk dosage forms in the described processes is less than 40 31m to 50 31m.

The bulk dosage forms according to the invention have been successfully tested in veterinary medicine and the corresponding tests have also begun in human medicine.

ofactors and veterinary drugs (VUBVL) performed a preclinical verification of the composition according to the invention.

66,000 IU base 5,000 IU base oxidized and radiation degraded cellulose ad 20.0 g

66,000 IU base 5,000 IU base 9.9 g of oxidized and radiation-degraded cellulose 9.9 g of skin irritation in 6 rabbits with the result that both tested preparations showed very good tolerability and can therefore be released for medical use without limitations.

Research institute for beating two medicinal backfills

Tested preparations:

a / Xeomycin sulfate

Zn-bacitracin Calcium salt chemically b / Neomycin sulphate Zn-bacitracin Zinc oxide Calcium salt chemically

VUBVL carried out the provisions

CS 267 494 Bl

Furthermore, the therapeutic effect was monitored in both preparations on 6 rabbits, 6 pigs and 150 ends with a very good result. Experimental wounds were healed with both products without complications and without signs of inflammation. Capillary bleeding stopped within 30 seconds. Furthermore, the antimicrobial activity was determined on 4 calves and 12 rabbits with used strains of Escherichia coli and Staphylococcus epidermidis, when in infected calves the con7 3-2 concentration of Escherichia coli microbes decreased from 8.1.10 to 9.15.10 cfu.cm in 4 hours and rabbits kle6 ⁹ -2 sla initial concentration of Staphalococci from 1.5.10 to 5.4.10 "microbes.cm in 24 hours.

The products were clinically tested at 16 veterinary workplaces and the hemostatic and antimicrobial efficacy, tolerability and application form were evaluated. A total of 2,243 animals were treated with the product for b / b, of which 60 horses, 158 cows, 3 sheep, 1,508 pigs, 438 dogs, 54 cats and 12 animals kept in the zoo. '

The combination of hemostatic and antimicrobial components has proved very successful not only in covering surgical and traumatic wounds, but also in the treatment of superficial skin inflammations, excoriations and wetting eczemas. The efficacy of the preparation was generally evaluated as very good in 61 treatments and good in others. The local tolerability of the product was good, no side effects were observed.

The following examples illustrate, but do not limit, the bulk dosage form with the vehicle of the invention in various types of powders. ·

Example 1

Neomycin sulfate 6,600 IU base

Bacitracin zinc complex 500 IU base

Calcium salt of chemically oxidized and radiation degraded cellulose ad 2.0 g

After mixing finely powdery ingredients, a backfill was prepared, which was the axes surface walls early. The wounds were sealed with a patch with a pad after treatment and unusually quickly healed without any wetting and without signs of inflammation or even purulence. Example 2 Neomycin sulfate 6 600 j. Base Bacitracin zinc complex Calcium salt chemically oxidized and radiation degraded cellulose, 500 J. base Zinc oxide aa ad 2.0 g Example 3 Carbaethopendecinium bromide Hexachlophen Calcium salt chemically oxidized and radiation degraded cellulose 0.100 g 0.090 g 8.0 g Talc They were treated with the resulting backfill 11.810 g small purulent affections with a very good effect. Example 4 Buklosamide 3.0 g Salicylic acid Calcium salt chemically oxidized and radiation degraded cellulose 3.0 g 10.0 g Zinc oxide The powder worked well on the surface Example 5 Benzylpenicillin-K dermatomycoses. 1 250 16.7 g 000 j. Collagen 1.75 g

CS 267 494 Bl

-3Calcium salt of chemically oxidized and radiation degraded cellulose

2.00 g

Sulfacetamide

Sulfathiazole

Sulfadimidine aa ad

50.0 g

The backfill worked well for healing surface wounds and for festering wounds.

Claims (1)

Bulk dosage form containing active substances and customary excipients, characterized in that it contains as vehicle 10 to 100 wt.%, Calcium salts of chemically oxidized and radiation-degraded cellulose in powder form with a carboxyl group content of at least 10 wt.% And a calcium ion content 4.5 to 7.5 / wt.