Delivery of antidepressants through an inhalation route
First Claim
1. A condensation aerosol for delivery of bupropion formed by heating a composition containing bupropion coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of bupropion and less than 5 percent by weight of bupropion degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
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Abstract
The present invention relates to the delivery of antidepressants through an inhalation route. Specifically, it relates to aerosols containing an antidepressant that are used in inhalation therapy. In a method aspect of the present invention, an antidepressant is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of an antidepressant, on a solid support, form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% antidepressant degradation products. In a kit aspect of the present invention, a kit for delivering an antidepressant through an inhalation route to a mammal is provided which comprises: a) a thin coating of an antidepressant composition and b) a device for dispensing said thin coating as a condensation aerosol.
251 Citations
182 Claims
- 1. A condensation aerosol for delivery of bupropion formed by heating a composition containing bupropion coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of bupropion and less than 5 percent by weight of bupropion degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 4. A condensation aerosol for delivery of nefazodone formed by heating a composition containing nefazodone coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of nefazodone and less than 5 percent by weight of nefazodone degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 7. A condensation aerosol for delivery of perphenazine formed by heating a composition containing perphenazine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of perphenazine and less than 5 percent by weight of perphenazine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 10. A condensation aerosol for delivery of trazodone formed by heating a composition containing trazodone coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of trazodone and less than 5 percent by weight of trazodone degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 13. A condensation aerosol for delivery of trimipramine formed by heating a composition containing trimipramine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of trimipramine and less than 5 percent by weight of trimipramine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 16. A condensation aerosol for delivery of venlafaxine formed by heating a composition containing venlafaxine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of venlafaxine and less than 5 percent by weight of venlafaxine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 19. A condensation aerosol for delivery of tranylcypromine formed by heating a composition containing tranylcypromine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of tranylcypromine and less than 5 percent by weight of tranylcypromine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 22. A condensation aerosol for delivery of citalopram formed by heating a composition containing citalopram coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of citalopram and less than 5 percent by weight of citalopram degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 25. A condensation aerosol for delivery of fluoxetine formed by heating a composition containing fluoxetine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of fluoxetine and less than 5 percent by weight of fluoxetine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 28. A condensation aerosol for delivery of fluvoxamine formed by heating a composition containing fluvoxamine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of fluvoxamine and less than 5 percent by weight of fluvoxamine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 31. A condensation aerosol for delivery of mirtazepine formed by heating a composition containing mirtazepine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of mirtazepine and less than 5 percent by weight of mirtazepine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 34. A condensation aerosol for delivery of paroxetine formed by heating a composition containing paroxetine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of paroxetine and less than 5 percent by weight of paroxetine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 37. A condensation aerosol for delivery of sertraline formed by heating a composition containing sertraline coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of sertraline and less than 5 percent by weight of sertraline degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 40. A condensation aerosol for delivery of amoxapine formed by heating a composition containing amoxapine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of amoxapine and less than 5 percent by weight of amoxapine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 43. A condensation aerosol for delivery of clomipramine formed by heating a composition containing clomipramine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of clomipramine and less than 5 percent by weight of clomipramine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 46. A condensation aerosol for delivery of doxepin formed by heating a composition containing doxepin coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of doxepin and less than 5 percent by weight of doxepin degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 49. A condensation aerosol for delivery of imipramine formed by heating a composition containing imipramine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of imipramine and less than 5 percent by weight of imipramine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 52. A condensation aerosol for delivery of maprotiline formed by heating a composition containing maprotiline coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of maprotiline and less than 5 percent by weight of maprotiline degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 55. A condensation aerosol for delivery of nortriptyline formed by heating a composition containing nortriptyline coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of nortriptyline and less than 5 percent by weight of nortriptyline degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 58. A condensation aerosol for delivery of valproic acid formed by heating a composition containing valproic acid coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of valproic acid and less than 5 percent by weight of valproic acid degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 61. A condensation aerosol for delivery of protriptyline formed by heating a composition containing protriptyline coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of protriptyline and less than 5 percent by weight of protriptyline degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
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64. A method of forming a bupropion containing aerosol comprising:
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(a) heating a composition containing bupropion coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of bupropion degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (65, 66, 154)
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67. A method of forming a nefazodone containing aerosol comprising:
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(a) heating a composition containing nefazodone coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of nefazodone degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (68, 69, 155)
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70. A method of forming a perphenazine containing aerosol comprising:
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(a) heating a composition containing perphenazine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of perphenazine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (71, 72, 156)
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73. A method of forming a trazodone containing aerosol comprising:
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(a) heating a composition containing trazodone coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of trazodone degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (74, 75, 157)
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76. A method of forming a trimipramine containing aerosol comprising:
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(a) heating a composition containing trimipramine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of trimipramine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (77, 78, 158)
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79. A method of forming a venlafaxine containing aerosol comprising:
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(a) heating a composition containing venlafaxine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of venlafaxine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (80, 81, 159)
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82. A method of forming a tranylcypromine containing aerosol comprising:
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(a) heating a composition containing tranylcypromine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of tranylcypromine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (83, 84, 160)
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85. A method of forming a citalopram containing aerosol comprising:
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(a) heating a composition containing citalopram coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of citalopram degradation product, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (86, 87, 161)
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88. A method of forming a fluoxetine containing aerosol comprising:
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(a) heating a composition containing fluoxetine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of fluoxetine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (89, 90, 162)
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91. A method of forming a fluvoxamine containing aerosol comprising:
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(a) heating a composition containing fluvoxamine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of fluvoxamine degradation product, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (92, 93, 163)
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94. A method of forming a mirtazepine containing aerosol comprising:
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(a) heating a composition containing mirtazepine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of mirtazepine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (95, 96, 164)
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97. A method of forming a paroxetine containing aerosol comprising:
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(a) heating a composition containing paroxetine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of paroxetine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (98, 99, 165)
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100. A method of forming a sertraline containing aerosol comprising:
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(a) heating a composition containing sertraline coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of sertraline degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (101, 102, 166)
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103. A method of forming an amoxapine containing aerosol comprising:
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(a) heating a composition containing amoxapine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of amoxapine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (104, 105, 167)
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106. A method of forming a clomipramine containing aerosol comprising:
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(a) heating a composition containing clomipramine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of clomipramine degradation product, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (107, 108, 168)
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109. A method of forming a doxepin containing aerosol comprising:
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(a) heating a composition containing doxepin coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of doxepin degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (110, 111, 169)
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112. A method of forming an imipramine containing aerosol comprising:
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(a) heating a composition containing imipramine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of imipramine degradation product, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (113, 114, 170)
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115. A method of forming a maprotiline containing aerosol comprising:
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(a) heating a composition containing maprotiline coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of maprotiline degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (116, 117, 171)
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118. A method of forming a nortriptyline containing aerosol comprising:
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(a) heating a composition containing nortriptyline coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of nortriptyline degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (119, 120, 172)
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121. A method of forming a valproic acid containing aerosol comprising:
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(a) heating a composition containing valproic acid coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of valproic acid degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (122, 123, 173)
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124. A method of forming a protriptyline containing aerosol comprising:
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(a) heating a composition containing protriptyline coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of protriptyline degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (125, 126, 174)
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127. A method of forming a drug containing aerosol comprising:
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(a) heating a composition containing the drug and a pharmaceutically acceptable excipient coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of bupropion, nefazodone, perphenazine, trazodone, trimipramine, venlafaxine, tranylcypromine, citalopram, fluoxetine, fluvoxamine, mirtazepine, paroxetine, sertraline, amoxapine, clomipramine, doxepin, imipramine, maprotiline, nortriptyline, valproic acid, and protriptyline, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (128, 129, 175)
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130. A method of forming a drug containing aerosol comprising:
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(a) heating a composition containing a salt form of the drug coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of bupropion, nefazodone, perphenazine, trazodone, trimipramine, venlafaxine, tranylcypromine, citalopram, fluoxetine, fluvoxamine, mirtazepine, paroxetine, sertraline, amoxapine, clomipramine, doxepin, imipramine, maprotiline, nortriptyline, valproic acid, and protriptyline, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (131, 132, 176)
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177. A method of forming a drug containing aerosol comprising:
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(a) heating a composition containing the drug coated on a solid support to form a vapor, and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of bupropion, nefazodone, perphenazine, trazodone, trimipramine, venlafaxine, tranylcypromine, citalopram, fluoxetine, fluvoxamine, mirtazepine, paroxetine, sertraline, amoxapine, clomipramine, doxepin, imipramine, maprotiline, nortriptyline, valproic acid, and protriptyline, wherein the condensation aerosol is formed at a rate greater than 0.5 mg/second, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (178, 179, 180, 181, 182)
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Specification