Diclofenac formulations and methods of use
DCFirst Claim
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1. A method of treating migraine associated with phonophobia and photophobia in a human patient within two hours of administration comprising:
- a) providing a liquid formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein said formulation;
i) is provided as a powder formulation and dissolved or suspended in water immediately before administration, or as a liquid formulation that is ingested with or without further mixing;
ii) optionally has been found to achieve a maximum plasma concentration (Cmax) (arithmetic mean) of from about 1500 to about 2500 ng/ml; and
iii) has been found to achieve a time to maximum plasma concentration (tmax) (arithmetic mean) in from about 10 to about 25 minutes;
b) orally administering said formulation to a patient suffering from migraine associated with photophobia and phonophobia, andc) thereby relieving said photophobia and said phonophobia in said patient within two hours of administration.
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Abstract
Methods and formulations are provided for treating migraine and other acute pain episodes using diclofenac, and formulations of diclofenac that provide both rapid and sustained relief from acute pain. Methods and formulations are also provided for treating symptoms that often accompany migraine and acute pain such as photophobia, phonophobia, nausea and vomiting.
18 Citations
25 Claims
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1. A method of treating migraine associated with phonophobia and photophobia in a human patient within two hours of administration comprising:
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a) providing a liquid formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein said formulation; i) is provided as a powder formulation and dissolved or suspended in water immediately before administration, or as a liquid formulation that is ingested with or without further mixing; ii) optionally has been found to achieve a maximum plasma concentration (Cmax) (arithmetic mean) of from about 1500 to about 2500 ng/ml; and iii) has been found to achieve a time to maximum plasma concentration (tmax) (arithmetic mean) in from about 10 to about 25 minutes; b) orally administering said formulation to a patient suffering from migraine associated with photophobia and phonophobia, and c) thereby relieving said photophobia and said phonophobia in said patient within two hours of administration. - View Dependent Claims (2, 3, 4, 5)
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6. A method of treating recurrent migraine requiring 24 hour treatment in a human patient suffering from migraine comprising:
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a) providing a liquid formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein said formulation; i) is provided as a powder formulation and dissolved or suspended in water immediately before administration, or as a liquid formulation that is ingested with or without further mixing; ii) optionally has been found to achieve a maximum plasma concentration (Cmax) (arithmetic mean)of from about 1500 to about 2500 ng/ml; and iii) has been found to achieve time to maximum plasma concentration (tmax) (arithmetic mean) in from about 10 to about 25 minutes; b) orally administering said formulation to said patient; and c) thereby providing sustained migraine relief to said patient for at least 24 hours. - View Dependent Claims (7, 8, 9, 10, 11, 12)
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13. A method of treating migraine in a human patient, including headache pain, nausea, photophobia and phonophobia, within two hours after administration, comprising:
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a) providing a liquid formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein said formulation; i) is provided as a powder formulation and dissolved or suspended in water immediately before administration, or as a liquid formulation that is ingested with or without further mixing; ii) optionally has been found to achieve a maximum plasma concentration (Cmax) (arithmetic mean) of from about 1500 to about 2500 ng/ml; and iii) has been found to achieve time to maximum plasma concentration (tmax) (arithmetic mean) in from about 10 to about 20 minutes; b) orally administering said formulation to a patient suffering from migraine, including headache pain, nausea, photophobia and phonophobia; and c) thereby treating said migraine, headache pain, nausea, photophobia and phonophobia in said patient within two hours of administration, wherein said migraine is defined as a disease manifested in a population of patients by periodic attacks of headache pain, nausea, photophobia and phonophobia. - View Dependent Claims (14, 15, 16, 17, 18, 19)
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20. A method of treating headache pain, nausea, phonophobia and photophobia in a human patient within two hours of administration comprising:
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a) providing a pharmaceutical formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein said formulation; i) has been found to achieve an average maximum plasma concentration (Cmax) (arithmetic mean) of from about 1400 to about 2500 ng/ml; and ii) has been found to achieve an average time to maximum plasma concentration tmax (arithmetic mean) in from about 10 to about 35 minutes; and b) orally administering said formulation to a patient suffering from photophobia and Phonophobia; thereby treating said headache pain, nausea, photophobia and phonophobia within two hours of administration. - View Dependent Claims (21)
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22. A method of treating recurrent migraine requiring 24 hour treatment in a human patient suffering from migraine, and providing relief from said migraine for at least 24 hours without rebound, comprising:
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a) providing a pharmaceutical formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein said formulation; i) has been found to achieve an average maximum plasma concentration (Cmax) (arithmetic mean) of from about 1400 to about 2500 ng/ml; and ii) has been found to achieve an average time to maximum plasma concentration tmax (arithmetic mean) in from about 10 to about 35 minutes; and b) orally administering said formulation to said patient; thereby treating said recurrent migraine and providing relief from said migraine for at least 24 hours without rebound. - View Dependent Claims (23)
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24. A method of treating headache pain, nausea, phonophobia and photophobia in a human patient within two hours of administration comprising:
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a) providing a pharmaceutical formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein greater than 90% of said diclofenac dissolves completely in 50 ml. of water at 25°
C. under continuous stirring for fifteen minutes at pH 6.8; andb) orally administering said formulation to a patient suffering from photophobia and phonophobia, and thereby relieving said photophobia and phonophobia within two hours of administration.
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25. A method of treating recurrent migraine requiring 24 hour treatment in a human patient suffering from migraine comprising:
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a) providing a pharmaceutical formulation comprising about 50 mg. of diclofenac or a pharmaceutically acceptable salt thereof in combination with an alkali metal carbonate or bicarbonate, wherein greater than 90% of said diclofenac dissolves completely in 50 ml. of water at 25°
C. under continuous stirring for fifteen minutes at pH 6.8;b) orally administering said formulation to said patient; thereby treating said recurrent migraine for at least twenty four hours after administration.
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Specification