Microparticulate form of a Tetrahydropyridine derivative
The invention relates to a microparticulate form of 1-[2-(2-naphthyl)-ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride consisting of particles for which at least 55% of the population have a diameter below 50 micrometers, and to pharmaceutical compositions in which it is present.
1 . An oral dosage unit comprising a microparticulate form of 1-[2-(2-naphthyl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride consisting of particles wherein at least 55% of said particles have a diameter below 50 micrometers, wherein said microparticles exhibit a better absorption which is not influenced by the intake of food and wherein absorption of said microparticles is at least two times more than the non-micronized form of 1-[2-(2-naphthyl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride.
2 . The dosage unit according to claim 1 wherein the particle diameter is below 25 micrometers.
3 . The dosage unit according to claim 2 wherein the particle diameter is below 15 micrometers.
4 . The dosage unit according to claim 3 wherein the diameter of 80-85% of the population of particles is below 10 micrometers.
5 . The dosage unit according to claim 1 wherein the particles are microspheres.
6 . The dosage unit according to claim 5 wherein the microparticles consist of 1-[2-(2-naphthyl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine hydrochloride in an essentially amorphous form.
7 . The dosage unit according to claim 1 wherein the particles are micronized crystals.
8 . A pharmaceutical composition containing a microparticulate form according to claim 1 as the active principle.
9 . A composition according to claim 8 wherein it is in the form of a tablet.
10 . A composition according to claim 9 wherein each tablet contains from 0.1 to 5 mg of active principle (calculated as the free base).
11 . A composition according to claim 10 wherein each tablet contains from 0.5 to 3 mg of active principle (calculated as the free base).
12 . A composition according to claim 11 wherein each tablet contains 2 mg of active principle (calculated as the free base).
13 . A pharmaceutical composition containing a microparticulate form according to claim 2 as the active principle.
14 . A pharmaceutical composition containing a microparticulate form according to claim 3 as the active principle.
15 . A pharmaceutical composition containing a microparticulate form according to claim 4 as the active principle.
16 . A pharmaceutical composition containing a microparticulate form according to claim 5 as the active principle.
17 . A pharmaceutical composition containing a microparticulate form according to claim 6 as the active principle.
18 . A pharmaceutical composition containing a microparticulate form according to claim 7 as the active principle.