Pharmaceutically Acceptable Salts and Polymorphic Forms of Hydrocodone Benzoic Acid Enol Ester and Processes for Making Same
US-2016039837-A1 · Feb 11, 2016 · US
US10351574B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10351574-B2 |
| Application number | US-201715730885-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 12, 2017 |
| Priority date | Mar 8, 2013 |
| Publication date | Jul 16, 2019 |
| Grant date | Jul 16, 2019 |
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Compositions comprising hydrocodone benzoic acid enol ester to form novel prodrugs including hydrocodone benzoic acid enol ester salts, and various polymorphs. Also provided are processes for the preparation of hydrocodone benzoic acid enol ester salts, and various polymorphs.
Opening claim text (preview).
The invention claimed is: 1. A compound comprising a polymorphic form of hydrocodone benzoic acid enol ester hydrochloride, wherein the polymorphic form is Form I, wherein Form I has an x-ray powder diffraction pattern comprising peaks at about the following 2θ values: 9.05, 12.32, 13.16, 14.94, and 18.57. 2. The compound of claim 1 , wherein Form I has an x-ray powder diffraction pattern further comprising peaks at about the following 2θ values: 6.16, 10.95, 11.91, 14.60, 17.04, 17.23, 17.80, 19.18, 20.66, 21.10, 22.15, 23.50, 26.07, and 28.39. 3. A solid pharmaceutical composition comprising a therapeutically effective amount of a polymorphic form of hydrocodone benzoic acid enol ester hydrochloride and a pharmaceutically acceptable excipient in a formulation for oral administration, wherein the polymorphic form is Form I, wherein Form I has an x-ray powder diffraction pattern comprising peaks at about the following 2θ values: 9.05, 12.32, 13.16, 14.94, and 18.57. 4. The solid pharmaceutical composition of claim 3 , wherein Form I has an x-ray powder diffraction pattern further comprising peaks at about the following 2θ values: 6.16, 10.95, 11.91, 14.60, 17.04, 17.23, 17.80, 19.18, 20.66, 21.10, 22.15, 23.50, 26.07, and 28.39. 5. A method for treating pain in a patient comprising the step of selecting a patient that is in need of pain treatment, administering to said patient a pharmaceutical composition comprising a therapeutically effective amount of one or more polymorphic forms of hydrocodone benzoic acid enol ester hydrochloride the compound of claim 1 . 6. A method for treating pain in a patient comprising the step of selecting a patient that is in need of pain treatment, administering to said patient a pharmaceutical composition comprising a therapeutically effective amount of one or more polymorphic forms of hydrocodone benzoic acid enol ester hydrochloride the compound of claim 3 .
Morphinan derivatives, e.g. morphine, codeine · CPC title
Crystalline forms, e.g. polymorphs · CPC title
with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone · CPC title
Salts; Organic complexes · CPC title
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