Stuffy nose deblocking composition having antiviral activity
Inventors
Grassauer, Andreas • Prieschl-Grassauer, Eva • Bodenteich, Angelika • Koller, Christiane • MOROKUTTI-KURZ, Martina
Assignees
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Publication Number
US-10660914-B2
Publication Date
2020-05-26
Expiration Date
Abstract
A pharmaceutical composition has a stuffy nose deblocking activity. The composition includes a hyperosmolar aqueous solution of a non-ionic osmolality adjusting agent, optionally in combination with an ionic osmolality adjusting agent, wherein the composition further includes iota-carrageenan and/or kappa-carrageenan as an active antiviral ingredient in an antivirally effective amount, with the proviso that the composition in its ready-for-use formulation contains no more than 0-1.5% w/v of the ionic osmolality adjusting agent. The composition is useful for deblocking a stuffy nose and for prophylactic or therapeutic intervention of a number of viral infections of the upper respiratory tract.
Core Innovation
The disclosed invention relates to a hyperosmolar aqueous solution having immediate stuffy nose deblocking activity and antiviral activity against viral infections of the respiratory tract. The hyperosmolar aqueous solution includes a carrageenan component as an active antiviral ingredient and is formulated with osmolality adjusting agents to reach a hyperosmolar osmolality value. The carrageenan component is described as iota-carrageenan, kappa-carrageenan, or a mixture of iota- and kappa-carrageenan, and is described as the sole antiviral active ingredient in the hyperosmolar aqueous solution.
The composition is formulated with a non-ionic osmolality adjusting agent in combination with an ionic osmolality adjusting agent, while including a nasally compatible buffer and having a pH value from 4.0 to 8.0. EDTA is included at a concentration of up to 2 mg/ml. The total concentration of non-ionic and ionic osmolality adjusting agents is defined such that the hyperosmolar osmolality is from 500 mOsm/kg to 1000 mOsm/kg, together with a proviso limiting ionic osmolality adjusting agent content in the formulation to no more than 1.5% w/v.
The description emphasizes that non-ionic osmolality adjusters are used in place of higher NaCl to preserve carrageenan antiviral activity, while also improving formulation properties such as viscosity and enabling sterile filtration with buffer and EDTA. The document reports antiviral inhibitory concentration data for viruses including human rhinovirus HRV1a and HRV8 and human coronavirus OC43, and includes patient evidence of rapid deblocking within minutes after nasal spray application.
Claims Coverage
The independent claim covers a hyperosmolar aqueous nasal formulation with immediate stuffy nose deblocking activity and antiviral activity against viral infections of the respiratory tract, comprising a carrageenan component as the sole antiviral active ingredient and specific combinations of non-ionic and ionic osmolality adjusting agents plus formulation constraints (buffer, pH, EDTA, hyperosmolar osmolality, and ionic proviso).
Hyperosmolar deblocking and respiratory-tract antiviral activity
A hyperosmolar aqueous solution having immediate stuffy nose deblocking activity and which is active against viral infections of the respiratory tract.
Carrageenan sole antiviral active ingredient
The hyperosmolar aqueous solution comprises a carrageenan component as an active antiviral ingredient, where the carrageenan component is the sole antiviral active ingredient and is selected from iota-carrageenan, kappa-carrageenan, and a mixture of iota- and kappa-carrageenan in an antivirally effective amount.
Non-ionic plus ionic osmolality adjusting agents under hyperosmolarity and ionic proviso
The hyperosmolar aqueous solution comprises a non-ionic osmolality adjusting agent in combination with an ionic osmolality adjusting agent, the hyperosmolar osmolality is from 500 mOsm/kg to 1000 mOsm/kg, the ionic osmolality adjusting agent is selected from sodium chloride, potassium chloride, and a mixture of sodium and potassium chloride, and the formulation contains no more than 1.5% w/v of the ionic osmolality adjusting agent.
Nasally compatible buffer and pH range
The hyperosmolar aqueous solution includes a nasally compatible buffer and has a pH value from 4.0 to 8.0.
EDTA up to defined maximum
The hyperosmolar aqueous solution includes EDTA at a concentration of up to 2 mg/ml.
Concentration of carrageenan in administered formulation
A concentration of the carrageenan component from 0.05% to 1% weight by volume (g/L) of a formulation of the hyperosmolar aqueous solution that is to be administered.
Overall, the claim coverage centers on a hyperosmolar aqueous nasal solution combining immediate stuffy nose deblocking with antiviral activity, where carrageenan (iota- and/or kappa-carrageenan) is the sole antiviral active ingredient and the antiviral effect is supported by formulation constraints involving non-ionic and ionic osmolality adjusting agents, a nasally compatible buffer with pH 4.0 to 8.0, EDTA up to 2 mg/ml, specified hyperosmolar osmolality, and a limit of no more than 1.5% w/v ionic osmolality adjusting agent.
Stated Advantages
Improves formulation properties such as viscosity.
Enables sterile filtration with buffer and EDTA.
Preserves carrageenan antiviral activity while using non-ionic osmolality adjusters instead of high NaCl.
Provides immediate stuffy-nose decongestion (patient evidence of rapid deblocking within 2–5 minutes after nasal spray application).
Documented Applications
Immediate stuffy-nose decongestion using a nasal spray, with simultaneous antiviral prophylactic/therapeutic intervention against respiratory-tract viral infections.
Antiviral activity against human rhinovirus (HRV1a and HRV8) and human coronavirus OC43.
Antiviral intervention for viral infections of the respiratory tract, including viruses associated with respiratory-tract conditions described in the dependent claims (e.g., parainfluenza virus, metapneumovirus, respiratory syncytial virus).
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