Polymorphs of 6-Beta-Naltrexol
AssigneeMallinckrodt Inc.
InventorsJian Bao, Gary A. Nichols
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Abstract
The present invention provides polymorphs of 6-beta-naltrexol and process for their preparation. In particular, the present invention provides crystalline forms of the free base of 6-beta-naltrexol and processes for their preparation. The present invention also provides crystalline and amorphous forms of the hydrochloride salt of 6-beta-naltrexol and processes for their preparation.
Claims12
A crystalline form of 6-beta-naltrexol base, morphinan-3,6,14-triol,17-(cyclopropylmethyl)-4,5-epoxy chosen from Form IB and Form IIB.
A polymorph of 6-beta-naltrexol hydrochloride, morphinan-3,6,14-triol,17-(cyclopropylmethyl)-4,5-epoxy chosen from crystalline Form IS, crystalline Form IIS, crystalline Form IIIS, crystalline Form IVS, crystalline Form VS, crystalline Form VIS, crystalline Form VIIS, crystalline Form VIIIS, crystalline Form IXS, crystalline Form XS, crystalline Form XIS is, and an amorphous form.
A pharmaceutical composition, the composition comprising at least one crystalline form of 6-beta-naltrexol base, morphinan-3,6,14-triol,17-(cyclopropylmethyl)-4,5-epoxy, and at least one pharmaceutically acceptable excipient, wherein the crystalline form of 6-beta-naltrexol base is chosen from Form IB, Form IIB, and combinations thereof.
A pharmaceutical composition, the composition comprising at least one polymorph of 6-beta-naltrexol hydrochloride, morphinan-3,6,14-triol,17-(cyclopropylmethyl)-4,5-epoxy, and at least one pharmaceutically acceptable excipient, wherein the polymorph of 6-beta-naltrexol hydrochloride is chosen from crystalline Form IS, crystalline Form IIS, crystalline Form IIIS, crystalline Form IVS, crystalline Form VS, crystalline Form VIS, crystalline Form VIIS, crystalline Form VIIIS, crystalline Form IXS, crystalline Form XS, crystalline Form XIS, an amorphous form, and combinations thereof.
A process for preparing a substantially pure crystalline form of 6-beta-naltrexol base, morphinan-3,6,14-triol,17-(cyclopropylmethyl)-4,5-epoxy, the process comprising:
- i. contacting 6-beta-naltrexol base with a solvent to form a saturated or a near saturated solution;
- and
- ii. forming crystals of the substantially pure crystalline form of 6-beta-naltrexol base.
Dependencies are inferred from the claim text.