Tizanidine therapy system
An object of the present invention is to provide a method for the treatment of a patient suffering from spasticity comprising administering to said patient a modified release dosage form comprising tizanidine or a pharmaceutically acceptable salt thereof. The present invention relates to a method of administering a transdermal patch preparation comprising tizanidine or a pharmaceutically acceptable salt thereof to a subject in need thereof, wherein the transdermal patch preparation releases about 4 mg to about 36 mg of tizanidine or a pharmaceutically acceptable salt thereof for at least about 24 hours.
1. A method of systemically delivering tizanidine to treat a musculoskeletal disease or disorder, comprising:
administering a transdermal patch preparation comprising tizanidine or a pharmaceutically acceptable salt thereof to a subject in need thereof, and
releasing about 4 mg to about 36 mg of tizanidine or a pharmaceutically acceptable salt thereof for at least about 24 hours.
2. The method of claim 1 , wherein an elimination rate constant of tizanidine is about 0.01 to about 0.2 h −1 .
3. The method of claim 1 , wherein the transdermal patch preparation has an AUC 0-inf of at least 1.0 ng*h/mL per mg of tizanidine.
4. The method of claim 1 for treating spasticity.
5. The method of claim 1 , wherein the transdermal patch preparation further comprises a sorbate component selected from the group consisting of sorbic acid, sodium sorbate, potassium sorbate, calcium sorbate, and a combination thereof.
6. The method of claim 1 , wherein the transdermal patch preparation provides a single dose T max of about 12 to about 48 hours.
7. The method of claim 1 , wherein the multiple-dose administration to a human subject provides a plasma concentration profile in steady state satisfying the following formula:
(
Css
,
max
-
Css
,
min
)
Css
,
max
<
0
.
9
.
8. The method of claim 1 , wherein the transdermal patch preparation provides a C ss,max of about 0.01 ng/mL to about 0.5 ng/mL per mg of tizanidine a day.
9. The method of claim 1 , wherein the transdermal patch preparation provides an elimination rate constant of tizanidine of about 0.01 to about 0.2 h −1 , calculated from the elimination time of the transdermal patch preparation.
10. The method of claim 1 , wherein the subject is suffering from a musculoskeletal disease or disorder ameliorated with tizanidine or a pharmaceutically acceptable salt thereof.
11. The method of claim 1 , wherein the transdermal patch preparation is applied to the subject once a day.
12. The method of claim 1 , wherein the transdermal patch preparation has a surface area of about 10 cm 2 to about 200 cm 2 .
13. The method of claim 1 , wherein the transdermal patch preparation further comprises a sorbate component selected from sorbic acid and/or a metal salt of sorbic acid.
14. The method of claim 1 , wherein the transdermal patch preparation comprises a support and a drug adhesive matrix on one surface of the support, and wherein the drug adhesive matrix comprises the tizanidine or the pharmaceutically acceptable salt thereof and has a thickness of about 600 μm in a wet state and/or a thickness of about 300 μm in a dry state.
15. The method of claim 1 , wherein the transdermal patch preparation comprises a support and a drug adhesive matrix on one surface of the support, and wherein the drug adhesive matrix comprises tizanidine or a pharmaceutically acceptable salt thereof and has a thickness of about 100 to about 400 μm.