Intranasal pharmaceutical compositions with improved pharmacokinetcs
AssigneeShin Nippon Biomedical Laboratories, Ltd.
InventorsRyoichi Nagata, Shunji Haruta
Life of this patent
Estimating the term…
Abstract
Methods are provided for the engineering of inhalable dry powder pharmaceutical formulations with desired pharmacokinetic profiles and parameters. Compositions with improved pharmacokinetics are disclosed.
Claims39
An inhalable dry powder pharmaceutical formulation comprising a therapeutic agent wherein at least some of the therapeutic agent is present in a freebase form, wherein, therapeutic agent comprises particles having a particle size distribution between about 5 μm to about 250 μm.
The pharmaceutical formulation of claim 25, wherein the crystalline cellulose has a particle diameter range from about 5 to 250 μm.
The pharmaceutical formulation of claim 24, wherein the additional therapeutic agent is a salt of the additional therapeutic agent, a freebase of the additional therapeutic agent, or a mixture thereof.
An inhalable dry powder pharmaceutical formulation comprising a therapeutic agent wherein at least some of which is present in a freebase form, and wherein said formulation has a water-octanol Log D 7.4 of between about 0 and about 5.
An inhalable dry powder pharmaceutical formulation comprising a therapeutic agent wherein at least some of which is present in a freebase form, and wherein said formulation has a water-octanol Log P of between about 0 and about 5.
A pharmaceutical formulation comprising a therapeutic agent wherein at least some of therapeutic agent is present in a freebase form, and wherein following intranasal administration to a human, the taste profile is substantially less bitter or objectionable than the taste profile of an identical pharmaceutical formulation wherein the therapeutic agent is present as a salt form at the same molar quantity.
An inhalable dry powder pharmaceutical formulation comprising a therapeutic agent wherein at least some of the therapeutic agent is present in a freebase form, wherein the maximal blood therapeutic concentration (Cmax) of the therapeutic agent in the pharmaceutical formulation is at least 60% of the Cmax compared to the therapeutic agent when present at 100% salt form at the same molar quantity in an otherwise identical pharmaceutical formulation when administered to a primate.
An inhalable dry powder pharmaceutical formulation comprising a therapeutic agent wherein at least some of the therapeutic agent is present in a freebase form, wherein the time to reach a blood concentration of ½ of Cmax(T1/2) of to the therapeutic agent in the pharmaceutical formulation is at least 60% of the T1/2 compared to the therapeutic agent when present at 100% salt form at the same molar quantity in an otherwise identical pharmaceutical formulation when administered to a primate.
An inhalable dry powder pharmaceutical formulation comprising a therapeutic agent wherein at least some of therapeutic agent is present in a freebase form, wherein the time to reach a blood concentration Cmax (Tmax) of the therapeutic agent in the pharmaceutical formulation is at least 60% of the Tmax compared to the therapeutic agent when present at 100% salt form at the same molar quantity in an otherwise identical pharmaceutical formulation when administered to a primate.
An inhalable dry powder pharmaceutical formulation comprising a therapeutic agent wherein at least some of the therapeutic agent is present in a freebase form, wherein the bioavailability (BA) of the therapeutic agent in the pharmaceutical formulation is at least 60% of the BA compared to the therapeutic agent when present at 100% salt form at the same molar quantity in an otherwise identical pharmaceutical formulation when administered to a primate.
The pharmaceutical formulation of claim 74, wherein the formulation has a BA that at least 110% compared to the BA of the therapeutic agent when present at 100% salt form at the same molar quantity in an otherwise identical pharmaceutical formulation when administered to a primate.
Dependencies are inferred from the claim text.