Steroid tetrol solid state forms
Inventors
Frincke, James • Lewbart, Marvin • Reading, Christopher
Assignees
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Publication Number
US-8486926-B2
Publication Date
2013-07-16
Expiration Date
Abstract
The invention relates to solid state forms of androst-5-ene-3β,7β,16α,17β-triol, formulations containing or prepared from such solid state forms and use of such materials for modulating acute and chronic non-productive inflammation. The formulations can be used to prevent, treat or slow the progression of conditions related to autoimmunity such as arthritis, multiple sclerosis, ulcerative colitis or Type 1 diabetes. The formulations can also be used to prevent, treat or slow the progression of conditions related to metabolic disorders such as Type 2 diabetes.
Core Innovation
The invention relates to solid state forms of androst-5-ene-3β,7β,16α,17β-tetrol (Compound 1) as a product obtained by obtaining purified androst-5-ene-3β,7β,16α,17β-tetrol and recovering androst-5-ene-3β,7β,16α,17β-tetrol from aqueous acetonitrile. The solid state forms are intended to be identifiable and controllable as substantially pure forms based on analytical signatures.
The invention further includes characterization of the solid state form using solid-state Raman and X-ray powder diffraction (XRPD), together with DTA/thermogravimetric traces for identifying a desired substantially pure or controlled solid form. The document provides measured solid-state characterization signatures using XRPD 2-theta peak positions and solid-state infrared Raman peak wavenumbers, and in some embodiments additionally includes differential thermal analysis transition and onset temperatures.
In addition, the invention describes compositions and liquid formulations that incorporate the solid state form of androst-5-ene-3β,7β,16α,17β-tetrol, including excipient-containing compositions and liquid formulations prepared by admixing the solid state form with a liquid excipient. The document also describes treating inflammation conditions or diseases by administering an effective amount of a solid formulation comprising the solid state form.
Claims Coverage
The partial content provides four independent claims that cover: a solid state form product defined by purification and recovery from aqueous acetonitrile; an excipient-containing composition; a liquid formulation preparation method; and a treatment method for inflammation-related conditions. The independent claim set includes distinct inventive features focused on the solid-state product obtained via a specified recovery step and its use in compositions, liquid formulations, and therapeutic treatment.
Solid-state form product obtained by recovery from aqueous acetonitrile
A product wherein the product is a solid state form of androst-5-ene-3β,7β,16α,17β-tetrol obtained by obtaining purified androst-5-ene-3β,7β,16α,17β-tetrol and recovering androst-5-ene-3β,7β,16α,17β-tetrol from aqueous acetonitrile.
Excipient-containing composition of a recovered solid state form
A composition comprising one or more excipients and a solid state form of androst-5-ene-3β,7β,16α,17β-tetrol obtained by obtaining purified androst-5-ene-3β,7β,16α,17β-tetrol and recovering androst-5-ene-3β,7β,16α,17β-tetrol from aqueous acetonitrile.
Liquid formulation by admixing a recovered solid state form with a liquid excipient
A method of preparing a liquid formulation comprising admixing a solid state form of androst-5-ene-3β,7β,16α,17β-tetrol obtained by obtaining purified androst-5-ene-3β,7β,16α,17β-tetrol and recovering androst-5-ene-3β,7β,16α,17β-tetrol from aqueous acetonitrile, with a liquid excipient.
Treating inflammation by administering a solid formulation of the recovered solid state form
A method of treating an inflammation condition or disease comprising administering an effective amount of a solid formulation to a subject in need thereof wherein the formulation comprises a solid state form of androst-5-ene-3β,7β,16α,17β-tetrol obtained by obtaining purified androst-5-ene-3β,7β,16α,17β-tetrol and recovering androst-5-ene-3β,7β,16α,17β-tetrol from aqueous acetonitrile.
Across the independent claims, the shared inventive foundation is the solid state form of androst-5-ene-3β,7β,16α,17β-tetrol obtained by purification and recovery from aqueous acetonitrile. Claim coverage then extends this solid state form to an excipient-containing composition, a liquid formulation prepared by admixing with a liquid excipient, and a method of treating inflammation conditions or diseases via administration of an effective amount of a solid formulation.
Stated Advantages
Allows identification of a desired substantially pure/controlled solid form using analytical signatures including solid-state Raman and XRPD, and DTA/thermogravimetric traces.
Documented Applications
Treating inflammation conditions or diseases by administering an effective amount of a solid formulation comprising the solid state form of androst-5-ene-3β,7β,16α,17β-tetrol.
Treating autoimmune conditions or diseases, including Type 1 diabetes.
Treating metabolic conditions or diseases, including hyperglycemia.
Use in chronic, non-production inflammation conditions or diseases.
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