Pharmaceutical preparation comprising permethylated cyclodextrin
View Patent ↗The invention relates to a pharmaceutical preparation for applying a pharmaceutical agent. According to the invention, the preparation contains: a) a pharmaceutical agent which has an aromatic group or an aromatic part and the molecule of which has a maximum diameter of ≦2 nm; b) a permethylated cyclodextrin having a degree of substitution of 3 methyl groups per glucopyranose unit. The permethylated cyclodextrin and the pharmaceutical agent form a complex.
1. A pharmaceutical preparation for the application of midazolam, wherein said pharmaceutical preparation contains:
a) midazolam;
b) a permethylated β-cyclodextrin with a degree of substitution of 3 methyl groups per glucopyranose unit;
wherein the permethylated β-cyclodextrin and the midazolam form a complex.
2. The pharmaceutical preparation as claimed in claim 1 wherein said pharmaceutical preparation has a pH from 4 to 7.
3. The pharmaceutical preparation as claimed in claim 1 , wherein the complexing constant K of the complex of midazolam and permethylated β-cyclodextrin is between 10 and 70 l/M.
4. The pharmaceutical preparation as claimed in claim 1 , wherein the midazolam has a log P value of at least 3.
5. The pharmaceutical preparation as claimed in claim 1 , wherein said pharmaceutical preparation is formulated for transmucosal application.
6. The pharmaceutical preparation as claimed in claim 5 , wherein said pharmaceutical preparation is formulated for transnasal, intralingual, intestinal or orovestibular application.
7. The pharmaceutical preparation as claimed in claim 1 , wherein the content of the midazolam is 0.5 to 2 wt. %.
8. The pharmaceutical preparation as claimed in claim 1 , wherein said pharmaceutical preparation has a pH from 5.5 to 6.5.
9. The pharmaceutical preparation as claimed in claim 1 , wherein the complexing constant K of the complex of pharmaceutical active substance and cyclodextrin is between 15 and 65 l/M.
10. The pharmaceutical preparation as claimed in claim 1 , wherein the complexing constant K of the complex of midazolam and permethylated β-cyclodextrin is between 20 and 55 l/M.
11. The pharmaceutical preparation as claimed in claim 1 , wherein the complexing constant K of the complex of midazolam and permethylated β-cyclodextrin is between 30 and 40 l/M.