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US 7,582,284 B2Granted
Particulate materials
AssigneeNektar Therapeutics
InventorsAndreas Kordikowski, Stephen Ernest Walker, Peter York
Life of this patent
Estimating the term…
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.
Claims62
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 μm, 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).
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 μm, 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).
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 μm;
- and
- a 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).
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 μm;
- and
- a 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).
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 μm, 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).
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 μm, 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).
Dependencies are inferred from the claim text.