Pharmaceutical preparation comprising an active dispersed on a matrix
View Patent ↗The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation, an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohols, triglycerides, partial triglycerides and fatty acid esters.
1. A preparation in which an active ingredient selected from the group of PDE4 inhibitors is essentially uniformly dispersed or dissolved in an excipient matrix comprising one or more excipients selected from the group consisting of a fatty alcohol, a triglyceride, a partial glyceride and a fatty acid ester, wherein the preparation is in the form of microspheres.
2. The preparation according to claim 1 , further comprising one or more additional other pharmaceutically suitable excipients in the excipient matrix.
3. The preparation according to claim 2 , further comprising one or more other excipients selected from the group consisting of polymers and sterols in the excipient matrix.
4. The preparation according to claim 1 , wherein the excipient matrix comprises one or more excipients selected from the group consisting of a fatty alcohol, a triglyceride and a partial glyceride.
5. The preparation according to claim 1 , wherein the excipient matrix is composed of at least one solid paraffin together with one or more excipients selected from the group consisting of a fatty alcohol, a triglyceride, a partial glyceride and a fatty acid ester.
6. The preparation according to claim 5 in which the active ingredient is i) present in a matrix composed of a mixture comprising at least one fatty alcohol and at least one solid paraffin, ii) present in a matrix composed of a mixture comprising at least one triglyceride and at least one solid paraffin, iii) present in a matrix composed of a mixture comprising at least one partial glyceride and at least one solid paraffin or iv) present in a matrix composed of a mixture comprising at least one fatty acid ester and at least one solid paraffin.
7. The preparation according to claim 1 , wherein the microspheres have a particle size in the range of 50-500 μm.
8. The preparation according to claim 1 , wherein the microspheres have a particle size in the range of 50-400 μm.
9. The preparation according to claim 1 , wherein the partial glyceride is selected from the group consisting of glycerol monostearate, glycerol distearate, glycerol monopalmitate, glycerol dipalmitate and mixtures thereof.
10. The preparation according to claim 9 , wherein the partial glyceride is glycerol monostearate.
11. The preparation according to claim 1 , wherein the fatty alcohol is selected from the group consisting of cetyl alcohol, myristyl alcohol, lauryl alcohol, stearyl alcohol and mixtures thereof.
12. The preparation according to claim 11 , wherein the fatty alcohol is cetyl alcohol.
13. The preparation according to claim 1 , obtainable by prilling a solution or dispersion of the active ingredient in the melt of the excipients using a vibrating nozzle.
14. A method of manufacturing a preparation according to claim 1 , comprising the step of prilling a solution or dispersion of the active ingredient in the melt of the excipients using a vibrating nozzle.
15. A pharmaceutical dosage form comprising a preparation as claimed in claim 1 and further comprising one or more pharmaceutical excipients.
16. The pharmaceutical dosage form according to claim 15 , which is selected from the group consisting of suspensions, gels, tablets, coated tablets, multi-component tablets, effervescent tablets, rapidly disintegrating tablets, powders in sachets, coated tablets, capsules, solutions and suppositories.
17. The pharmaceutical dosage form as claimed in claim 16 in the form of a rapidly disintegrating tablet, wherein the excipients are excipients which bring about rapid disintegration of said tablet.
18. The tablet as claimed in claim 17 , further comprising one or more excipients selected from the group consisting of lubricants, flavors, flavoring substances and surface-active substances.
19. The pharmaceutical dosage form according to claim 16 , which is a suspension or solution.
20. A suspension or solution according to claim 19 , comprising one thickener or a mixture of two or more thickeners.