Nebulizer formulations of dehydroepiandrosterone and methods of treating asthma or chronic obstructive pulmonary disease using compositions thereof
AssigneeEpigenesis Pharmaceuticals, Inc.
InventorsSherry A. Leonard, Keith A. Johnson
Life of this patent
Estimating the term…
Abstract
This invention relates to a sealed container containing a powder formulation comprising a dehydroepiandrosterone, its analogue(s) or salt(s) by itself or with a pharmaceutically or veterinarily acceptable carrier or diluent, and having a particle size of about 0.1 μm to about 100 μm. The formulation can be used to treat or prevent asthma, chronic obstructive pulmonary disease, lung inflammation, and other respiratory diseases or conditions. The formulation may be prepared by jet milling, and may be delivered through the respiratory tract or other routes using a nebulizer. The sealed container is provided in a device and/or a therapeutic kit.
Claims21
A pharmaceutical composition comprising an agent, wherein the agent comprises a compound as described by chemical formula (I), (II), (III), (IV) or (V), or a pharmaceutically or veterinarily acceptable salt thereof, in an anhydrous form thereof;
- wherein the broken line represents a single or a double bond;
- wherein R is hydrogen or a halogen;
- the H at position 5 is present in the alpha or beta configuration or the compound of formula (I) comprises either isomer or a racemic mixture of both configurations;
- and R1 is hydrogen or a multivalent inorganic or organic dicarboxylate acid covalent bound to the compound of chemical formula (I);
- wherein R1, R2, R3, R4, R6, R7, R8, R9, R10, R11, R12, R13, R14 and R19 are independently H, OH, halogen, C1-10 alkyl or C1-10 alkoxy;
- R5 is H, OH, halogen, C1-10 alkyl, C1-10 alkoxy or OSO2R20;
- R15 is (1) H, halogen, C1-10 alkyl or C1-10 alkoxy when R16 is C(O)OR21 or (2) H, halogen, OH or C1-10 alkyl when R16 is H, halogen, OH or C1-10 alkyl or (3) H, halogen, C1-10 alkyl, C1-10 alkenyl, C1-10 alkynyl, formyl, C1-10 alkanoyl or epoxy when R16 is OH;
- or R15 and R16 taken together are ═O;
- R17 and R18 are independently (1) H, OH, halogen, C1-10 alkyl or C1-10 alkoxy when R16 is H, OH, halogen, C1-10 alkyl or —C(O)OR21 or (2) H, (C1-10 alkyl)n amino, (C1-10 alkyl)n amino-C1-10 alkyl, C1-10 alkoxy, hydroxy-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, (halogen)m-C1-10 alkyl, C1-10 alkanoyl, formyl, C1-10 carbalkoxy or C1-10 alkanoyloxy when R15 and R16 taken together are ═O;
- or R17 and R18 taken together are ═O or taken together with the carbon to which they are attached form a 3-6 member ring containing 0 or 1 oxygen atoms;
- or R15 and R17 taken together with the carbons to which they are attached form an epoxide ring;
- [R20 is OH, pharmaceutically acceptable ester or pharmaceutically acceptable ether;
- R21 is H, (halogen)m -C1-10 alkyl or C1-10 alkyl];
- n is 0, 1 or 2;
- and m is 1, 2 or 3, with the proviso that (a) R3 is not H, OH or halogen when R1, R2, R4, R6, R7, R9, R10, R12, R13, R14, R17 and R19 are H and R5 is OH or C1-10 alkoxy and R8 is H, OH or halogen and R11 is H or OH and R18 is H, halogen or methyl and R15 is H and R16 is OH;
- (b) R3 is not H, OH or halogen when R1, R2, R4, R6, R7, R9, R10, R12, R13, and R14 [and R19 ] are H and R5 is OH or C1-10 alkoxy and R8 is H, OH or halogen and R11 is H or OH and R18 is H, halogen or methyl and R15 and R16 taken together are ═O;
- (c) R5 is not H, halogen, C1-10 alkoxy or OSO2R20 when R1, R2, R3, R4, R6, R7, R8, R9, R10, R12, R13, R14 and R17 are H and R11 is H, halogen, OH or C1-10 alkoxy and R18 is H or halogen and R15 and R16 taken together are ═O;
- and (d) R5 is not H, halogen, C1-10 alkoxy or OSO2R20 when R1, R2, R3, R4, R6, R7, R8, R9, R10, R12, R13, R14 and R17 are H and R11 is H, halogen, OH or C1-10 alkoxy and R18 is H or halogen and R15 is H and R16 is H, OH or halogen;
- wherein R is A —CH(OH)—C(O)— and A is hydrogen or a C1-C22 alkyl or alkenyl group wherein the C1-C22 alkyl or alkenyl group is not subsitutued or substituted with one or more C1-C4 alkyl groups, phenyls, halogens or hydroxyl groups, said phenyl is not substituted or substituted with one or more halogen HO or CH3O;
- wherein said dry powder pharmaceutical composition is particles of respirable or inhalable size.
Dependencies are inferred from the claim text.