Particulate materials
First Claim
Patent Images
1. A composition of an aerosol formulation, comprising:
- a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 μ
m, suspended in a nonsolvent hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v, which formulation exhibits a flocculation volume of about 85% or greater, about 1 minute after mixing the particulate active substance and the vehicle, wherein the particulate active substance comprises a compound selected from the group consisting of salmeterol xinafoate, budesonide, salbutamol sulfate, dihydroergotamine mesylate, risperidone-(9-hydroxy)-palmitate, bromocriptine mesylate, and derivatives thereof and the nonsolvent hydrofluorocarbon fluid vehicle comprises 1,1,1,2-tetrafluoroethane (HFA 134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFA 227ea).
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Abstract
The present invention relates to active substances in particulate form, to methods for preparing them, to formulations containing them and to uses of such substances and formulations. A preferred embodiment is directed to particulate suspensions having improved flocculation behavior in a suspension vehicle, such as a hydrofluoroalkane propellant used in metered dose inhalers.
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Citations
62 Claims
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1. A composition of an aerosol formulation, comprising:
a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 μ
m, suspended in a nonsolvent hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v, which formulation exhibits a flocculation volume of about 85% or greater, about 1 minute after mixing the particulate active substance and the vehicle, wherein the particulate active substance comprises a compound selected from the group consisting of salmeterol xinafoate, budesonide, salbutamol sulfate, dihydroergotamine mesylate, risperidone-(9-hydroxy)-palmitate, bromocriptine mesylate, and derivatives thereof and the nonsolvent hydrofluorocarbon fluid vehicle comprises 1,1,1,2-tetrafluoroethane (HFA 134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFA 227ea).- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 33, 34)
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26. A composition of an aerosol formulation, comprising:
a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 5 μ
m, suspended in a nonsolvent hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v, which formulation exhibits a flocculation volume of greater than 85%, about 60 seconds after mixing the particulate active substance and the vehicle, wherein the particulate active substance comprises a compound selected from the group consisting of salmeterol xinafoate, budesonide, salbutamol sulfate, dihydroergotamine mesylate, risperidone-(9-hydroxy)-palmitate, bromocriptine mesylate, and derivatives thereof and the nonsolvent hydrofluorocarbon fluid vehicle comprises 1,1,1,2-tetrafluoroethane (HFA 134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFA 227ea).- View Dependent Claims (27, 28, 35, 36)
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29. A composition of an aerosol formulation, comprising:
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a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 μ
m; anda suspension containing the particulate active substance suspended in a nonsolvent hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 3% w/v, wherein the suspension exhibits a flocculation volume of about 35% or greater, 5 minutes after mixing the particulate active substance and the vehicle, wherein the particulate active substance comprises a compound selected from the group consisting of salmeterol xinafoate, budesonide, salbutamol sulfate, dihydroergotamine mesylate, risperidone-(9-hvdroxv)-palmitate, bromocriptine mesylate, and derivatives thereof and the nonsolvent hydrofluorocarbon fluid vehicle comprises 1,1,1,2-tetrafluoroethane (HFA 134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFA 227ea). - View Dependent Claims (37, 38)
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30. A composition of an aerosol formulation, comprising:
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a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 10 μ
m; anda suspension containing the particulate active substance suspended in a nonsolvent hydrofluorocarbon fluid vehicle and having a flocculation volume of about 85% or greater, about 1 minute after mixing the particulate active substance and the vehicle, wherein the particulate active substance comprises a compound selected from the group consisting of salmeterol xinafoate, budesonide, salbutamol sulfate, dihydroergotamine mesylate, risperidone-(9-hydroxv)-palmitate, bromocriptine mesylate, and derivatives thereof and the nonsolvent hydrofluorocarbon fluid vehicle comprises 1,1,1,2-tetrafluoroethane (HFA 134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFA 227ea). - View Dependent Claims (31, 32)
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39. A composition of an aerosol formulation, comprising:
a particulate active substance of non-micronized, solid particles having a mass median diameter of less than 15 μ
m, suspended in a nonsolvent hydrofluorocarbon fluid vehicle at a concentration within a range from about 0.2% w/v to about 5% w/v, wherein the formulation exhibits a flocculation volume of 35% or greater, about 1 minute after mixing the particulate active substance and the vehicle, wherein the particulate active substance comprises a compound selected from the group consisting of salmeterol xinafoate. budesonide. salbutamol sulfate. dihydroergotamine mesylate, risperidone-(9-hydroxy)-palmitate, bromocriptine mesylate, and derivatives thereof and the nonsolvent hydrofluorocarbon fluid vehicle comprises 1,1,1,2-tetrafluoroethane (HFA 134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFA 227ea).- View Dependent Claims (40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59)
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60. A composition of an aerosol formulation, comprising:
a particulate active substance of non-micronized, solid particles having a mass median aerodynamic diameter of less than 5 μ
m, suspended in a nonsolvent hydrofluorocarbon fluid vehicle, wherein the formulation exhibits a flocculation volume of 50% or greater, 1 minute after mixing the particulate active substance and the vehicle, wherein the particulate active substance comprises a compound selected from the group consisting of salmeterol xinafoate, budesonide, salbutamol sulfate, dihydroergotamine mesylate, risperidone-(9-hydroxy)-palmitate, bromocriptine mesylate, and derivatives thereof and the nonsolvent hydrofluorocarbon fluid vehicle comprises 1,1,1,2-tetrafluoroethane (HFA 134a) or 1,1,1,2,3,3,3-heptafluoropropane (HFA 227ea).- View Dependent Claims (61, 62)
Specification