ST-246 (tecovirimat monohydrate) suspension formulations
Inventors
Tyavanagimatt, Shanthakumar R. • Holt, Kris • Tan, Ying • Anderson, Melialani A. C. L. S. • Hruby, Dennis E.
Assignees
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Publication Number
US-11433051-B2
Publication Date
2022-09-06
Expiration Date
Abstract
The present invention is directed to a dry suspension for reconstitution containing Tecovirimat (ST-246) powder and simethicone. The dry suspension is dispersed in water to provide an aqueous pharmaceutical suspension formulation for oral administration for treating orthopoxvirus infections and/or eczema vaccinatum. The suspension formulation exhibits excellent stability and good dissolution and has an improved taste and texture.
Core Innovation
The invention provides a dry suspension formulation comprising polymorph Form I of Tecovirimat (ST-246) and simethicone. The dry suspension is intended to be reconstituted to form an oral aqueous suspension. The formulation addresses poor aqueous solubility of Tecovirimat (ST-246) by enabling oral suspension delivery using simethicone together with dry suspension components.
The problem being solved is related to achieving suitable liquid/suspension stability upon reconstitution and during storage, including preventing particle growth, foaming, and sedimentation while enabling rapid and easy redispersion without dosage error. The described dry suspension system aims to support reconstitution that yields an aqueous suspension with improved physical behavior and consistent handling, including appropriate pH stability.
The invention further addresses sensory attributes by providing simethicone-containing suspensions, including flavored and flavor-masked embodiments, to mitigate off-notes such as bitterness and undesirable taste/texture. The described approach includes selecting suspending agents and simethicone form, and controlling formulation characteristics including polymer concentration, anti-foaming effect, viscosity, and particle-size effects to improve dissolution and off-taste intensity relative to other material forms.
Claims Coverage
The independent claim coverage centers on a dry suspension composition of polymorph Form I Tecovirimat (ST-246) with simethicone, with the main inventive concept further narrowed by independent claim dependencies that specify quantitative formulation characteristics, aqueous reconstitution/pH constraints, and a defined reconstitution step.
Dry suspension comprising polymorph Form I Tecovirimat (ST-246) and simethicone
A dry suspension comprising polymorph Form I of Tecovirimat (ST-246) and simethicone.
Dry suspension with defined Tecovirimat particle size
The dry suspension is characterized by a particle size of ST-246 ranging from 0.5 to 10 μm.
Dry suspension with specific lubricant/excipient exemplars
The dry suspension specifies that the lubricant is magnesium stearate and/or that the excipient is lactose monohydrate.
Aqueous formulation pH constraint
The formulation has a pH between 4 and 7.
Reconstitution by dispersing in water
The formulation is made by dispersing a dry suspension in water, where the water optionally includes a suspending agent.
Across the independent-claim-driven coverage, the core inventive concept is the dry suspension of polymorph Form I Tecovirimat (ST-246) with simethicone, further refined by particle-size constraints, selection of specific lubricant/excipient exemplars, an aqueous pH range, and dispersing the dry suspension in water, optionally with a suspending agent.
Stated Advantages
Improves oral aqueous suspension handling by enabling rapid and easy redispersion without dosage error.
Improves physical stability on reconstitution and during storage by preventing particle growth, foaming, and sedimentation.
Improves sensory attributes by mitigating bitterness and off-notes, including undesirable taste and texture, using flavored and flavor-masked suspensions.
Supports improved dissolution behavior relative to other material forms, including micronized API having lower off-taste intensity than granules.
Provides pH stability for the aqueous formulation within a specified pH range.
Documented Applications
Treatment of orthopoxvirus infections and/or eczema vaccinatum using an oral aqueous suspension derived from the dry suspension formulation.
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