Fexofenadine microcapsules and compositions containing them
The present invention provides a pharmaceutical composition comprising taste-masked immediate release microcapsules which comprise fexofenadine and a water-insoluble polymer coating. These microcapsules and the pharmaceutical compositions comprising them have suitable drug content and desirable pharmaceutical properties, including a quick dissolution rate of fexofenadine combined with a taste masking effect.
1. A water-suspendable pharmaceutical composition comprising
(a) a co-granulate of at least one inactive ingredient and taste-masked immediate release microcapsules comprising fexofenadine and a water-insoluble polymer coating; and
(b) at least one granulated inactive ingredient;
wherein the co-granulate (a) and the at least one granulated inactive ingredient (b) have a fine fraction below 125 μm of <5%, and a fraction over 600 μm of <10%.
2. The pharmaceutical composition of claim 1 , wherein the ratio of the co-granulate (a) to the at least one granulated inactive ingredient (b) is 1:1.
3. The pharmaceutical composition of claim 1 , wherein said fexofenadine is crystalline fexofenadine.
4. The pharmaceutical composition of claim 1 , wherein said fexofenadine is fexofenadine hydrochloride.
5. The pharmaceutical composition of claim 1 , wherein said water-insoluble polymer is selected from the group consisting of ethylcellulose, polyvinyl acetate, cellulose acetate, cellulose acetate butyrate, polyvinyl acetate, ammonio-methacrylate copolymers and mixtures thereof.
6. The pharmaceutical composition of claim 5 , wherein said water-insoluble polymer is ethylcellulose.
7. The pharmaceutical composition of claim 1 , wherein the weight of the water-insoluble polymer of said microcapsules is from about 2% to about 40%.
8. The pharmaceutical composition of claim 7 , wherein the weight of the water insoluble-polymer of said microcapsules is from about 10% to about 20%.
9. The pharmaceutical composition of claim 8 , wherein the weight of the water-insoluble polymer of said microcapsules is from about 13% to about 18%.
10. The pharmaceutical composition of claim 4 , wherein said composition releases at least about 60% of said fexofenadine hydrochloride within 15 minutes in pH 6.8 JP 2° nd fluid.
11. The pharmaceutical composition of claim 10 , wherein said composition releases at least about 80% of said fexofenadine hydrochloride within 15 minutes in pH 6.8 JP 2° nd fluid.
12. The pharmaceutical composition of claim 11 , wherein said composition releases at least about 95% of said fexofenadine hydrochloride within 15 minutes in pH 6.8 JP 2° nd fluid.
13. The pharmaceutical composition of claim 1 , wherein said microcapsules further comprise a surfactant, glidant or an antisticking agent.
14. The pharmaceutical composition of claim 13 , wherein said surfactant is sodium docusate.
15. The pharmaceutical composition of claim 1 , wherein said at least one granulated inactive ingredient (b) is selected from the group consisting of a granulated sugar alcohol, and a granulated saccharide.
16. The composition of claim 1 , wherein the at least one granulated inactive ingredient (b) is a mixture of sucrose and xanthan gum.
17. The pharmaceutical composition of claim 1 , wherein said composition is in the form of a tablet, capsule or sachet.
18. The pharmaceutical composition of claim 1 , wherein the co-granulate (a) and the at least one granulated inactive ingredient (b) have a fine fraction below 125 μm of <5.0%, and a fraction over 600 μm of <5.0%.
19. The pharmaceutical composition of claim 1 , wherein the co-granulate (a) consists of taste masked immediate release microcapsules, xanthan gum, and sucrose, wherein the weight ratio of the microcapsules to the (xanthan gum+sucrose) is between 1:6 and 1:7.
20. The pharmaceutical composition of claim 19 , wherein said composition is in the form of a sachet.