Cocrystalline DHEA formulations
AssigneesThe Methodist Hospital, University of Houston System
InventorsAnders Berkenstam, Edward Kuczynski, Alf S. Andersson, Jan-Ake Gustafsson, Carly Sue Filgueira
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Abstract
A cocrystalline DHEA composition with at least one additional coformer is disclosed for therapeutic formulations. The cocrystalline DHEA/coformer formulation including at least one coformer chosen from the group consisting of glutaric acid, maleic acid, tartaric acid, fructose, and wherein the L-isomer of tartaric acid and the D-isomer of fructose are utilized. The cocrystalline DHEA/coformer formulations include certain excipients as a solubilizer or inhibitor.
Claims15
A composition formulated to produce a supersaturated intestinal solution, said composition comprising:
- dehydroepiandrosterone (DHEA), wherein the DHEA is a polymorph form I (FI) or polymorph form II (FII);
- and
- a crystalline coformer selected from the group consisting of fructose and maleic acid, wherein the DHEA and the coformer are in an approximately 1:1 molar stoichiometric ratio;
- and wherein said supersaturated intestinal solution is maintained at between 50 micrograms/ml and 236 micrograms/ml for between 60 minutes and 240 minutes.
A cocrystalline composition comprising
- dehydroepiandrosterone (DHEA);
- wherein the DHEA is a polymorph form I (FI) or polymorph form II (FII);
- and
- a coformer selected from the group consisting of fructose and maleic acid, wherein the DHEA and the coformer are in an approximately 1:1 molar stoichiometric ratio;
- and
- an excipient, wherein said cocrystalline composition is about three times more soluble in an intestinal fluid than DHEA itself.
A method for treating a neurological disease in a patient comprising:
- identifying a neurological disease symptom in the patient;
- determining the patient's tolerance to at least one crystalline coformer, wherein the coformer is selected from the group consisting of fructose and maleic acid;
- providing the patient a cocrystalline formulation comprising DHEA, and the at least one coformer,
- wherein said cocrystalline formulation forms a supersaturated intestinal solution;
- wherein the supersaturated solution contains DHEA at between 50 and 236 micrograms/ml for between 60 and 240 minutes;
- analyzing a response by the patient to the formulation;
- and
- adjusting the cocrystalline formulation according to the patient's response.
A composition comprising:
- a cocrystal, wherein the cocrystal comprises:
- dehydroepiandrosterone (DHEA), wherein the DHEA is a polymorph form I (FI) or polymorph form II (FII);
- and
- a coformer, wherein the coformer is selected from the group consisting of fructose and maleic acid, wherein the DHEA and the coformer are in an approximately 1:1 molar stoichiometric ratio;
- and wherein said cocrystal is about three times more intestinal soluble than DHEA itself.
A composition formulated to delay recrystallization of dehydroepiandrosterone (DHEA) from an aqueous intestinal solution, wherein said composition comprises:
- dehydroepiandrosterone (DHEA) polymorph form I (FI);
- and a maleic acid cocrystal, wherein the DHEA and the maleic acid cocrystal are in approximately a 1:1 molar stoichiometric ratio, and wherein said aqueous intestinal solution is at a concentration of between 50 and 148 micrograms/ml for about 60 minutes prior to recrystallization.
A composition formulated to delay recrystallization of dehydroepiandrosterone (DHEA) polymorph form I (FI) from an aqueous intestinal solution wherein said composition comprises:
- dehydroepiandrosterone (DHEA) polymorph form I (FI);
- and a crystalline coformer, wherein the coformer is fructose, and said conformer and the DHEA are in approximately a 1:1 molar stoichiometric ratio, and wherein said aqueous intestinal solution is at a concentration of between 50 and 236 micrograms/ml for about 60 minutes prior to recrystallization.
Dependencies are inferred from the claim text.