PHARMACEUTICAL COMBINATION CONTAINING AN ANALGESIC AGENT AND AN ANTISPASMODIC AGENT

Abstract

“PHARMACEUTICAL COMBINATION CONTAINING AN ANALGESIC AGENT AND AN ANTISPASMODIC AGENT”, whose analgesic agent is the Ketorolac Tromethamine, which is physically isolated from the antispasmodic agent and whose antispasmodic active ingredient, in combination with the analgesic agent Ketorolac Tromethamine, is Hyoscine, Pargeverine, Tolterodine, Mebeverine or Papaverine. Both the analgesic agent Ketorolac Tromethamine and the antispasmodic agent are combined in separate and immediate release form. The analgesic agent Ketorolac Tromethamine can also be found in the present combination in separate and immediate release form, while the combined antispasmodic agent is presented in equally separate, but programmed release form. The active ingredient Ketorolac Tromethamine is in a ratio between 2.5% and 20% by weight and the antispasmodic active ingredient is in a ratio between 2.5% and 20% by weight.

Claims

1. A pharmaceutical composition comprising an analgesic and an antispasmodic agent, wherein the analgesic agent contains Ketorolac Tromethamine and is present in said composition in a ratio of between 5% and 20% by weight and the antispasmodic active ingredient is in a ratio of between 5% and 20% by weight of said composition.

2. The pharmaceutical composition according to claim 1, wherein the analgesic agent Ketorolac Tromethamine is physically isolated from the antispasmodic agent.

3. The pharmaceutical composition according to claim 1, wherein the antispasmodic active ingredient in combination with the analgesic agent Ketorolac Tromethamine is Hyoscine.

4. The pharmaceutical composition according to claim 1, wherein the antispasmodic active ingredient in combination with the analgesic agent Ketorolac Tromethamine is Pargeverine.

5. The pharmaceutical composition according to claim 1, wherein the antispasmodic active ingredient in combination with the analgesic agent Ketorolac Tromethamine is Tolterodine.

6. The pharmaceutical composition according to claim 1, wherein the antispasmodic active ingredient in combination with the analgesic agent Ketorolac Tromethamine is Mebeverine.

7. The pharmaceutical composition according to claim 1, wherein the antispasmodic active ingredient in combination with the analgesic agent Ketorolac Tromethamine is Papaverine.

8. The pharmaceutical composition according to claim 1, wherein both the analgesic agent Ketorolac Tromethamine and the antispasmodic agent are combined in separate and immediate release form.

9. The pharmaceutical composition according to claim 1, wherein the analgesic agent Ketorolac Tromethamine is provided in a separate and immediate release form, while the antispasmodic agent is presented in an equally separate, but programmed release form.

10. The pharmaceutical composition according to claim 1, wherein the composition is provided in the form of granules containing the active ingredients, said granules having diameters between 0.2 mm and 1.8 mm, preferably between 0.4 mm and 1.5 mm.

11. The pharmaceutical composition according to claim 1, further comprising a binder polymer comprising polyvinylpyrrolidone.

12. The pharmaceutical composition according to claim 1, further comprising a binder polymer comprising polyethylene glycol.

13. The pharmaceutical composition according to claim 1, further comprising a binder polymer comprising methylcellulose.

14. The pharmaceutical composition according to claim 1, further comprising a binder polymer comprising an amide.

15. The pharmaceutical composition according to claim 1, further comprising a coating polymer for programmed release of antispasmodic agent, the coating polymer comprising ethyl cellulose in different proportions in acetone, alcoholic, aqueous solutions or mixtures thereof.

16. The pharmaceutical composition according to claim 1, further comprising a coating polymer for programmed release of the antispasmodic agent, the coating polymer comprising hydroxypropylmethylcellulose in different proportions in acetone, alcoholic, aqueous solutions or mixtures thereof.

17. The pharmaceutical composition according to claim 1, further comprising a coating polymer for programmed release of the antispasmodic agent, the coating polymer comprising acrylic polymers in different proportions in acetone, alcoholic, aqueous solutions or mixtures thereof.

18. The pharmaceutical composition according to claim 1, wherein the composition has incorporated plasticizers of the type of diethyl phthalates, dibutyl phthalates, polyethylene glicols, triethylcitrates, triacetin and triglycerides of fatty acids.

19. The pharmaceutical composition according to claim 1, wherein, for presentation in the form of granules containing the active ingredients, these have diameters between 0.4 mm and 1.5 mm.

Description

DESCRIPTION

[0018] In the following, it will be demonstrated, by way of no-limiting illustration, how the present application can be put into practice.

[0019] The granules containing the active ingredient Ketorolac Tromethamine are designed to be immediate release, being elaborated with cores composed of sugar and starch, which are incorporated to the micronized active ingredient, through the binder polymers.

[0020] The granules containing the antispasmodic active ingredient (Hyoscine, Pargeverine, Tolterodine, Mebeverine, Papaverine, among others), are designed to be immediate release, to which it is added to the microgranules, coating polymers in such a manner, to achieve the appropriate release profile.

[0021] Said granules present diameters between 0.2 mm and 1.8 mm, preferably, between 0.4 mm and 1.5 mm and add to these dyes o differentiate each containing the active ingredient.

[0022] The solvents used for the preparation of the substantially spherical granules can be acetone, isopropyl alcohol, ethyl alcohol, chloroform, methylene chloride, water or a mixture thereof.

[0023] As binder polymers, polyvinylpyrrolidones, polyethylene glicols, methylcellulose, sucrose, gelatin, starch and mixtures thereof are preferably used. As coating polymers or film formers, different types of methylcelluloses, hydroxypropylmethylcelluloses, hydroxypropylmethylcellulose phtalates, acrylic polymers (Eudragit L, S, RL, RS or combinations thereof), shellac and ethyl-celluloses, combined in different ratios in acetone, alcoholic, aqueous solutions or mixtures thereof can be used. These solutions can have incorporated plasticizers of type of diethyl phthalate, dibutyl phthalate, polyethylene glycol, triethylcitrate, triacetin, triglycerides of fatty acids or others. As lubricant, talc is used. [0024] Formula of the granules of Ketorolac Tromethamine. [0025] Formula of the granules of antispasmodic.

TABLE-US-00001 PRODUCT FORMULA KETOROLAC TROMETHAMINE    5-30% POVIDONE (PVP K 30)     1-5% WHITE TALC    5-30% Tartrazine yellow DYE  0.03-0.06% CORES N° 1 88.97-34.94%   100.00%

[0026] Composition as preferred mode of carrying out the

TABLE-US-00002 PRODUCT FORMULA ANTISPASMODIC    5-30% POVIDONE (PVP K 30)     1-5% WHITE TALC    5-30% Green DYE  0.03-0.06% CORES N° 1 88.97-34.94%   100.00%
contents of each capsule with separate microgranules, according to the active ingredient of immediate release both the analgesic and the antispasmodic.

TABLE-US-00003 PRODUTO FINAL CÁPSULA FÓRMULA CETOROLACO DE TROMETAMINA    2.5-20% ANTIESPASMÓDICO    2.5-20% POVIDONA (PVP K 30)     1-5% TALCO BRANCO    5-30% CORANTES (A + V)  0.03-0.06% NÚCLEOS 88.97-34.94%   100.00%

[0027] Composition as preferred mode of carrying out the contents of each capsule with separate microgranules, according to the active ingredient of programmed release for the antispasmodic case.

TABLE-US-00004 FINAL PRODUCT CAPSULE FORMULA KETOROLAC TROMETHAMINE    2.5-20% ANTISPASMODIC    2.5-20% POVIDONE (PVP K 30)     1-5% WHITE TALC    5-30% DYES (A + V)  0.03-0.06% CORES 87.97-29.94% COATING POLYMERS     1-5%   100.00%

[0028] There is no doubt that when the present application is put into practice, modifications may be made to certain construction details and form without departing from the fundamental principles which are clearly demonstrated in the following claims: