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AssigneeContera Pharma Aps
InventorsJohn Bondo Hansen, Mikael S. Thomsen, Jens D. Mikkelsen, Peter Gudmund Nielsen, Mads Kreilgaard
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The present invention provides a pharmaceutical formulation for oral administration comprising an agonist of two or more of the 5-HT1B, 5-HT1D and 5-HT1F receptors, such as a triptan, e.g. zolmitriptan, in a matrix constituent with extended release characteristics, and further comprising a 5-HT1A-R agonist, such as buspirone, in a constituent with immediate-release characteristics. The special formulation is particularly well-suited for use in the treatment of movement disorders by combining the two active ingredients in a manner that achieves synergy from both the combination per se and the special release parameters of the pharmaceutical formulation, allowing for ease of administration and reducing the risk of adverse effects of each of the two active ingredients.
A pharmaceutical formulation comprising
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation is a solid dosage form, such as a tablet.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation comprises matrix constituent a. providing for extended release of an agonist of two or more of the 5-HT1B, 5-HT1D and 5-HT1F receptors, and constituent b. providing for immediate release of an agonist of the 5-HT1A receptor, in separate compartments or layers.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation comprises
The pharmaceutical formulation according to any of the preceding claims, wherein each of said constituents a. and b. are provided together in a capsule, wherein said capsule comprises constituents a. and b. as separate granules or pellets.
The pharmaceutical formulation according to any of the preceding claims, wherein said matrix constituent a. and matrix constituent b. each comprises one or more excipients.
The pharmaceutical formulation according to any of the preceding claims, wherein said matrix constituent a. comprises one or more excipients, such as one or more release-controlling excipients.
The pharmaceutical formulation according to any of the preceding claims, wherein said matrix constituent a. further comprises talc.
The pharmaceutical formulation according to any of the preceding claims, wherein said matrix constituent a. is compressed to a hardness of from 50-70N.
The pharmaceutical formulation according to any of the preceding claims, wherein said matrix constituent a. provides for at least 80% release of the agonist of two or more of the 5-HT1B, 5-HT1D and 5-HT1F receptors after 12 hours.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation comprises said agonist of two or more of the 5-HT1B, 5-HT1D and 5-HT1F receptors in an amount of from 0.1 to 10 mg, such as from 0.5 to 5 mg, for example about 1 mg.
The pharmaceutical formulation according to any of the preceding claims, wherein said matrix constituent a. consists of one or more HPMCs, one or more MCCs, talc, and an agonist of two or more of the 5-HT1B, 5-HT1D and 5-HT1F receptors.
The pharmaceutical formulation according to any of the preceding claims, wherein said matrix constituent a. comprises or consists essentially of
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation comprises said agonist of the 5-HT1A receptor in an amount of from 1 to 20 mg, such as from 5 to 15 mg, for example about 10 mg.
The pharmaceutical formulation according to any of the preceding claims, wherein said constituent b. comprises an excipient.
The pharmaceutical formulation according to any of the preceding claims, wherein said constituent b. comprises a film-forming excipient.
The pharmaceutical formulation according to any of the preceding claims, wherein said constituent b. comprises or consists of at least one HPMC and an agonist of the 5-HT1A receptor.
The pharmaceutical formulation according to any of the preceding claims, wherein said constituent b. comprises or consists of
The pharmaceutical formulation according to any of the preceding claims, wherein the formulation consisting of constituents a. and b. comprises or consists essentially of
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation comprises one or more further active ingredients.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation is for oral administration.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation is for use in the treatment of a movement disorder.
The pharmaceutical formulation according to any of the preceding claims, wherein said agonist of two or more the 5-HT1B, 5-HT1D and 5-HT1F receptors is to be administered in a dosage of from 0.001 to 10 mg/kg bodyweight, such as 0.001 to 5 mg/kg bodyweight, such as 0.01 to 1 mg/kg bodyweight.
The pharmaceutical formulation according to any of the preceding claims, wherein said 5-HT1A agonist is to be administered in a dosage of from 0.01 to 10 mg/kg bodyweight, such as 0.01 to 5 mg/kg bodyweight, such as 0.1 to 1 mg/kg bodyweight.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation is to be administered once daily.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation is to be administered in combination with a separate dopamine prodrug, such as L-DOPA, sequentially or simultaneously.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation is to be administered as long as a movement disorder or an increased risk of developing a movement disorder is present.
The pharmaceutical formulation according to any of the preceding claims, wherein said formulation is manufactured by 1) preparing granules by mixing (MCC and HPMC) with (HPMC and the agonist of two or more of the 5-HT1B, 5-HT1D and 5-HT1F receptors, such as zolmitriptan),
Dependencies are inferred from the claim text.