Preparation and administration form comprising an acid-labile active compound
View Patent ↗Novel administration forms and preparations for acid-labile active compounds are described. The novel administration forms contain individual active compound units, the active compound being present in the active compound units in a matrix made of a mixture comprising at least one fatty alcohol and at least one solid paraffin, in a matrix made of a mixture of a triglyceride and at least one solid paraffin or in a matrix made of a mixture comprising at least one fatty acid ester and at least one solid paraffin. In particular, the active compound units are microspheres which can be produced by prilling.
1. An oral solid active compound unit comprising a solidified drop, the solidified drop comprising:
a matrix comprising a mixture of at least one fatty alcohol that is a linear, saturated or unsaturated primary alcohol having 10-30 carbon atoms and at least one solid paraffin; and pantoprazole sodium sesquihydrate,
wherein said pantoprazole sodium sesquihydrate is present in said matrix, and
wherein the solidified drop does not comprise an enteric coating.
2. The oral solid active compound unit as claimed in claim 1 , wherein the matrix further comprises one or more excipients selected from the group consisting of polymers, sterols and basic compounds.
3. A process for the production of an oral solid active compound unit in the form of a solidified drop comprising pantoprazole sodium sesquihydrate which is present in the solidified drop in a matrix made of a mixture comprising at least one fatty alcohol that is a linear, saturated or unsaturated primary alcohol having 10-30 carbon atoms and at least one solid paraffin, comprising the following steps:
a. preparing a solution or dispersion of the pantoprazole sodium sesquihydrate in the fatty alcohol that is a linear, saturated or unsaturated primary alcohol having 10-30 carbon atoms and paraffin;
b. prilling the solution or dispersion prepared in step (a) and obtaining drops of the solution or dispersion; and
c. solidifying the drops obtained in step (b) in a suitable medium,
wherein the solidified drop microsphere does not comprise an enteric coating.
4. The process as claimed in claim 3 , where the prilling is carried out by means of vibrating nozzles, wherein the solution or dispersion which flows to the nozzle is kept at a constant temperature, and wherein the solidification of the drops takes place in a suitable cooling medium after stabilization thereof by sudden quenching.
5. An oral solidified drop prepared by the process as claimed in claim 3 .
6. The oral solid active compound unit as claimed in claim 1 , wherein the solidified drop has a particle size range of 50-800 μm.
7. The oral solid active compound unit as claimed in claim 1 , wherein the solidified drop has a particle size range of 50-400 μm.
8. The oral solid active compound unit as claimed in claim 1 , wherein the solidified drop has a particle size range of 50-200 μm.
9. The oral solid active compound unit as claimed in claim 1 , wherein the fatty alcohol that is a linear, saturated or unsaturated primary alcohol having 10-30 carbon atoms is selected from the group consisting of cetyl alcohol, myristyl alcohol, lauryl alcohol, stearyl alcohol and mixtures thereof.
10. The oral solid active compound unit as claimed in claim 1 , wherein the solid paraffin is paraffinum solidum or ozocerite.
11. The oral solid active compound unit as claimed in claim 1 , wherein the pantoprazole sodium sesquihydrate is 1-90% by weight of the oral solid active compound unit.
12. The oral solid active compound unit as claimed in claim 11 , wherein the pantoprazole sodium sesquihydrate is 2-70% by weight of the oral solid active compound unit.
13. The oral solid active compound unit as claimed in claim 11 , wherein the pantoprazole sodium sesquihydrate is 5-40% by weight of the oral solid active compound unit.
14. The oral solid active compound unit as claimed in claim 11 , wherein the pantoprazole sodium sesquihydrate is 10-20% by weight of the oral solid active compound unit.
15. The oral solid active compound unit as claimed in claim 1 , wherein the fatty alcohol that is a linear, saturated or unsaturated primary alcohol having 10-30 carbon atoms is 10-70% by weight of the oral solid active compound unit.
16. The oral solid active compound unit as claimed in claim 15 , wherein the fatty alcohol that is a linear, saturated or unsaturated primary alcohol having 10-30 carbon atoms is 20-70% by weight of the oral solid active compound unit.
17. The oral solid active compound unit as claimed in claim 15 , wherein the fatty alcohol that is a linear, saturated or unsaturated primary alcohol having 10-30 carbon atoms is 30-60% by weight of the oral solid active compound unit.
18. The oral solid active compound unit as claimed in claim 1 , wherein the solid paraffin is 10-70% by weight of the oral solid active compound unit.
19. The oral solid active compound unit as claimed in claim 18 , wherein the solid paraffin is 30-60% by weight of the oral solid active compound unit.