Claims
- 1. An inhalable pharmaceutical composition for the treatment of a patient in need of bronchodilating therapy, said composition comprising an amount of micronized formoterol containing at least 90% by weight of (R,R)-formoterol and 10% or less by weight of (S,S)-formoterol, or a pharmaceutically acceptable salt thereof, and a propellant.
- 2. An inhalable pharmaceutical composition according to claim 1, wherein the amount of micronized formoterol containing at least 90% by weight of (R,R)-formoterol and 10% or less by weight of (S,S)-formoterol, or a pharmaceutically acceptable salt thereof, is sufficient to elicit a bronchodilator effect, but insufficient to cause adverse effects associated with racemic formoterol.
- 3. An inhalable pharmaceutical composition according to claim 1, wherein the amount of micronized formoterol containing at least 90% by weight of (R,R)-formoterol and 10% or less by weight of (S,S)-formoterol, or a pharmaceutically acceptable salt thereof, is about 1 μg to about 100 μg.
- 4. An inhalable pharmaceutical composition according to claim 3, wherein the amount of micronized formoterol containing at least 90% by weight of (R,R)-formoterol and 10% or less by weight of (S,S)-formoterol, or a pharmaceutically acceptable salt thereof, is about 6 μg to about 25 μg per day.
- 5. An inhalable pharmaceutical composition according to claim 1, comprising (R,R)-formoterol fumarate dihydrate and a propellant.
- 6. An inhalable pharmaceutical composition according to claim 1, further comprising a pharmaceutically acceptable carrier.
- 7. A kit for the treatment of a patient in need of bronchodilating therapy, said kit comprising a metered dose inhaler and an inhalable pharmaceutical composition comprising micronized formoterol containing at least 90% by weight of (R,R)-formoterol and 10% or less by weight of (S,S)-formoterol, or a pharmaceutically acceptable salt thereof, and a propellant.
- 8. A kit according to claim 7, wherein said micronized formoterol contains at least 99% by weight of (R,R)-formoterol and 1% or less by weight of (S,S)-formoterol.
- 9. A kit according to claim 8, wherein said micronized formoterol contains greater than 99% by weight of (R,R)-formoterol and less than 1% of (S,S)-formoterol.
- 10. A kit according to claim 7, wherein the formoterol containing at least 90% by weight of (R,R)-formoterol and 10% or less by weight of (S,S)-formoterol, or a pharmaceutically acceptable salt thereof, comprises formoterol fumarate dihydrate.
- 11. A kit for the treatment of a patient in need of bronchodilating therapy, said kit comprising (1) an inhalable pharmaceutical composition comprising micronized formoterol containing at least 90% by weight of (R,R)-formoterol and 10% or less by weight of (S,S)-formoterol, or pharmaceutically acceptable salt thereof, and a propellant; and (2) instructions for administering said composition to cause bronchodilation while reducing the concomitant liability of adverse effects.
CROSS REFERENCE TO RELATED APPLICATIONS
This application is a continuation of U.S. Ser. No. 09/136,109 (now U.S. Pat. No. 6,068,833), filed Aug. 18, 1998 as a continuation of U.S. Ser. No. 08/613,382 (now U.S. Pat. No. 5,795,564), filed Mar. 7, 1996 as a continuation-in-part of U.S. Ser. No. 08/373,515 (now abandoned), filed Jan. 12, 1995 as a continuation-in-part of U.S. Ser. No. 08/222,319 (now abandoned), filed Apr. 4, 1994 as a continuation of U.S. Ser. No. 07/927,458 (now abandoned), filed Aug. 10, 1992, and is a continuation-in-part of U.S. Ser. No. 08/382,744 (now abandoned), filed Feb. 2, 1995 as a continuation of U.S. Ser. No. 08/223,798 (now abandoned) filed Apr. 6, 1994 as a continuation of U.S. Ser. No. 07/862,907 (now abandoned), filed Apr. 3, 1992.
US Referenced Citations (5)
Foreign Referenced Citations (2)
Number |
Date |
Country |
2255503 |
Nov 1992 |
GB |
9205147 |
Nov 1992 |
WO |
Non-Patent Literature Citations (12)
Entry |
Trofact et al. (1991). Chirality 3(6): 443-450.* |
Dellamary et al. (2000). Pharmaceutical Research 17(2): 168-174.* |
“Comparison of the Action of BD 40 A and some Other β-Adrenoceptor Stimulants of the Isolated Trachea and Atria of the Guinea Pig” H. Ida, Arzneim.—-Forsch. 26, 839-842 (1976). |
“Cardiorespiratory Activities of 3-Formylamino-4-hydroxy α-(N-1-methyl-2-methoxyphenethylaminomethyl)-benzylalcohol-bemifumarate (BD 40A) and some other β-Adrenoceptor Stimulants in Conscious Guinea Pigs” H. Ida, Arzneim. -Forsch. 26, 1337-1340 (1976). |
“New β-Adrenoreceptor Stimulants. Studies on 3-Acylamino-4-hydroxy-α-(N-substituted aminomethyl)benzyl Alcohols” Murase et al., Chem. Pharm. Bull. 25(6) 1368-1377 (1977). |
“Steric Aspects of Agonism and Antagonism at β-Adrenoceptors: Synthesis of and Pharmacological Experiments With the Enantiomers of Formoterol and Their Diasteromers” Trofast et al., Chirality 3 443-450 (1991). |
“A Three-Month Comparison of Twice Daily Inhaled Formoterol Versus Four Times Daily Inhaled Albuterol in the Management of Stable Asthma 1-3” Kesten et al., Am. Rev. Respir. Dis. 144 622-625 (1991). |
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“Racemic therapeutics-ethical and regulatory aspects” Ariëns, Eur. J. Clin. Pharmacol 41, 89-93 (1991). |
“Absolute Configurations of four Isomers of 3-Formamido-4-hydroxy-α[[N-(p-methoxy-α-methylphenethyl)amino]methyl]benzyl Alcohol, a Potent β-Adrenoreceptor Stimulant,” Murase et al., Chem. Pharm. Bull, 26:1123-29 (1978). |
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Continuations (5)
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Number |
Date |
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Parent |
09/136109 |
Aug 1998 |
US |
Child |
09/535200 |
|
US |
Parent |
08/613382 |
Mar 1996 |
US |
Child |
09/136109 |
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US |
Parent |
07/927458 |
Aug 1992 |
US |
Child |
08/222319 |
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US |
Parent |
08/223798 |
Apr 1994 |
US |
Child |
08/382744 |
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US |
Parent |
07/862907 |
Apr 1992 |
US |
Child |
08/223798 |
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US |
Continuation in Parts (3)
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Parent |
08/373515 |
Jan 1995 |
US |
Child |
08/613382 |
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US |
Parent |
08/222319 |
Apr 1994 |
US |
Child |
08/373515 |
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US |
Parent |
08/382744 |
Feb 1995 |
US |
Child |
07/927458 |
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US |