Intranasal olanzapine formulations and methods of their use
Inventors
Assignees
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Publication Number
US-12171868-B2
Publication Date
2024-12-24
Expiration Date
Abstract
Compositions for intranasal delivery of olanzapine and methods for their use to treat various symptoms of schizophrenia, schizoaffective disorder, and bipolar disorder, such as acute agitation, mania, and mixed episodes. Intranasal olanzapine compositions comprise dodecyl maltoside to improve bioavailability of olanzapine and is administered via nasal mucosa to avoid direct systemic administration.
Core Innovation
The invention relates to a non-aqueous intranasal olanzapine formulation for intranasal delivery to a nasal mucosal membrane. The composition comprises about 1% w/v to about 15% w/v of olanzapine or a pharmaceutically acceptable salt thereof, about 0.1% w/v to about 1% w/v of dodecyl maltoside, about 30% w/v to about 40% w/v of N,N-dimethylacetamide, and about 40% w/v to about 70% w/v of polyethylene glycol, wherein the composition comprises less than about 3% w/v of water.
The disclosure is directed to treating acute agitation associated with schizophrenia, schizoaffective disorder, and bipolar disorder by intranasal administration of the specified non-aqueous olanzapine composition. The formulation is delivered to the nasal mucosal membrane, with dependent embodiments further refining the composition parameters and/or delivery format.
In addition to the composition and method, the disclosure includes device-oriented embodiments for intranasal administration. A single-use spray device can discharge an amount equivalent to 2.5 mg to 15 mg of olanzapine when actuated, and a pre-primed single use dosing device can provide the composition in a defined volume range.
Claims Coverage
The document includes two independent claims: one directed to a specific non-aqueous olanzapine composition and one directed to a method for treating acute agitation by intranasal administration. Across these claims, the inventive subject matter is defined by tightly constrained quantitative formulation ranges with low water content and by intranasal delivery to the nasal mucosal membrane, optionally coupled to time-to-effect and device/delivery constraints.
Non-aqueous intranasal olanzapine composition with specified low-water content
A non-aqueous solution composition comprising about 1% w/v to about 15% w/v of olanzapine or a pharmaceutically acceptable salt thereof, about 0.1% w/v to about 1% w/v of dodecyl maltoside, about 30% w/v to about 40% w/v of N,N-dimethylacetamide, and about 40% w/v to about 70% w/v of polyethylene glycol, wherein the composition is a non-aqueous solution comprising less than about 3% w/v of water.
Intranasal treatment of acute agitation using the specified non-aqueous olanzapine composition
A method of treating acute agitation associated with one or more of schizophrenia, schizoaffective disorder, and bipolar disorder in a subject in need thereof comprising intranasally administering a composition comprising about 1% w/v to about 15% w/v of olanzapine or a pharmaceutically acceptable salt thereof, about 0.1% w/v to about 1% w/v dodecyl maltoside, about 30% w/v to about 40% w/v N,N-dimethylacetamide, and about 40% w/v to about 70% w/v of polyethylene glycol to a nasal mucosal membrane of the subject, wherein the composition is a non-aqueous solution comprising less than about 3% w/v of water.
Claim coverage is anchored in a defined non-aqueous olanzapine composition using dodecyl maltoside, N,N-dimethylacetamide, and polyethylene glycol with less than about 3% w/v water. The method claim extends this composition to intranasal administration to the nasal mucosal membrane for treating acute agitation associated with schizophrenia, schizoaffective disorder, and bipolar disorder.
Stated Advantages
Reduction in the severity of acute agitation within about 20 minutes after administration.
Documented Applications
Treatment of acute agitation associated with one or more of schizophrenia, schizoaffective disorder, and bipolar disorder via intranasal administration of the specified non-aqueous olanzapine composition.
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