Pharmaceutical compositions comprising cyclosporins
DCFirst Claim
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1. An oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a propylene glycol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
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Abstract
Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or Nva!2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.
124 Citations
198 Claims
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1. An oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a propylene glycol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12)
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13. An oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a propylene glycol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24)
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25. An oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of an ethanol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36)
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37. An oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of an ethanol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48)
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49. An oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant other than the hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (50, 51, 52, 53, 54)
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55. An oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant other than the hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (56, 57, 58, 59, 60)
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61. A method of orally administering a composition, said method comprising orally administering to a patient in need of cyclosporin therapy an oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant other than the hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (62, 63, 64, 65, 66)
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67. A method of orally administering a composition, said method comprising orally administering to a patient in need of cyclosporin therapy an oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant other than the hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (68, 69, 70, 71, 72)
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73. A method of reducing the variability of bioavailability levels of cyclosporin A for patients during cyclosporin therapy, said method comprising orally administering an oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant other than the hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (74, 75, 76, 77, 78)
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79. A method of reducing the variability of bioavailability levels of cyclosporin A for patients during cyclosporin therapy, said method comprising orally administering an oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant other than the hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (80, 81, 82, 83, 84)
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85. An oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component, about 0.5 to about 90% by weight of a hydrophilic surfactant selected from the group consisting of polyoxyethylene glycolated natural vegetable oil, polyoxyethylene glycolated hydrogenated vegetable oil, polyoxyethylene-sorbitan-fatty acid ester and polyoxyethylene fatty acid ester wherein said surfactant is other than said hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (86, 87, 88, 89, 90, 91, 92, 93, 94, 95)
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96. An oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component, about 0.5 to about 90% by weight of a hydrophilic surfactant selected from the group consisting of polyoxyethylene glycolated natural vegetable oil, polyoxyethylene glycolated hydrogenated vegetable oil, polyoxyethylene-sorbitan-fatty acid ester and polyoxyethylene fatty acid ester wherein said surfactant is other than said hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (97, 98, 99, 100, 101, 102, 103, 104, 105, 106)
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107. A method of orally administering a pharmaceutical composition, said method comprising orally administering to a patient in need of cyclosporin therapy an oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component, about 0.5 to about 90% by weight of a hydrophilic surfactant selected from the group consisting of polyoxyethylene glycolated natural vegetable oil, polyoxyethylene glycolated hydrogenated vegetable oil, polyoxyethylene-sorbitan-fatty acid ester and polyoxyethylene fatty acid ester wherein said surfactant is other than said hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (108, 109, 110, 111, 112, 113, 114, 115, 116, 117)
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118. A method of orally administering a pharmaceutical composition, said method comprising orally administering to a patient in need of cyclosporin therapy an oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component, about 0.5 to about 90% by weight of a hydrophilic surfactant selected from the group consisting of polyoxyethylene glycolated natural vegetable oil, polyoxyethylene glycolated hydrogenated vegetable oil, polyoxyethylene-sorbitan-fatty acid ester and polyoxyethylene fatty acid ester wherein said surfactant is other than said hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (119, 120, 121, 122, 123, 124, 125, 126, 127, 128)
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129. A method of reducing the variability of bioavailability levels of cyclosporin A for patients during cyclosporin therapy, said method comprising orally administering an oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component, about 0.5 to about 90% by weight of a hydrophilic surfactant selected from the group consisting of polyoxyethylene glycolated natural vegetable oil, polyoxyethylene glycolated hydrogenated vegetable oil, polyoxyethylene-sorbitan-fatty acid ester and polyoxyethylene fatty acid ester wherein said surfactant is other than said hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (130, 131, 132, 133, 134, 135, 136, 137, 138, 139)
- 140. A method of reducing the variability of bioavailability levels of cyclosporin A for patients during cyclosporin therapy, said method comprising orally administering an oil-in-water microemulsion composition having an average particle size of less than about 1,500 A comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90t by weight of a hydrophilic component, about 0.5 to about 90t by weight of a lipophilic component, about 0.5 to about 90% by weight of a hydrophilic surfactant selected from the group consisting of polyoxyethylene glycolated natural vegetable oil, polyoxyethylene glycolated hydrogenated vegetable oil, polyoxyethylene-sorbitan-fatty acid ester and polyoxyethylene fatty acid ester wherein said surfactant is other than said hydrophilic component, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
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151. A method of orally administering a pharmaceutical composition, said method comprising orally administering to a patient in need of cyclosporin therapy an oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a propylene glycol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162)
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163. A method of orally administering a pharmaceutical composition, said method comprising orally administering to a patient in need of cyclosporin therapy an oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a propylene glycol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174)
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175. A method of reducing the variability of bioavailability levels of cyclosporin A for patients during cyclosporin therapy, said method comprising orally administering an oil-in water microemulsion composition having particles of less than 2,000 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a propylene glycol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186)
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187. A method of reducing the variability of bioavailability levels of cyclosporin A for patients during cyclosporin therapy, said method comprising orally administering an oil-in-water microemulsion composition having an average particle size of less than about 1,500 Å
- comprising water, about 5 to about 25% by weight of cyclosporin A, about 0.5 to about 90% by weight of a propylene glycol hydrophilic component, about 0.5 to about 90% by weight of a lipophilic component and about 0.5 to about 90% by weight of a hydrophilic surfactant, all weight percents being based on the total weight of the cyclosporin A, hydrophilic component, lipophilic component and hydrophilic surfactant.
- View Dependent Claims (188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198)
Specification