Oral formulation of A-nor-5α androstane compound

An oral formulation, wherein said oral formulation comprises an A-nor-5α androstane compound as an active ingredient, a filling agent, a disintegrant, a binder, a lubricant, and a glidant, each of which has the following parts by weight:

• active ingredient
• 1-50 parts by weight
• filling agent
• 30-95 parts by weight
• disintegrant
• 0-20 parts by weight
• binder
• 0.1-10 parts by weight
• lubricant
• 0.1-5 parts by weight
• glidant
• 0.1-5 parts by weight
• wherein said A-nor-5α-androstane compound is selected from the group consisting of:
• 2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-dihydroxy compound (Ia),
• 2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-dihydroxy diacetate compound (Ib),
• 2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-dihydroxydipropionate compound (Ic),
• 2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-dihydroxy-2β-mono succinate compound (Id),
• 2α, 17α-diethynyl-A-nor-5α-androstane-20, 17β-di succinate compound (Ie),
• 2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-dibutyrate compound (If),
• 2α, 17α-dihydroxypropynyl-A-nor-5α-androstane-2β, 17β-dihydroxy compound (Ig),
• 2α, 17α-dicyano-A-nor-5α-androstane-2β, 17β-dihydroxy compound (Ih),
• 2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-dihydroxy-di-(trichloroacetate) compound (Ii),
• 2α, 17α-diethynyl-A-nor-5α-androstane-2β, 17β-dihydroxy-2β-propionate-17β succinate compound (Ij),
• 2α, 17α-dipropynyl-A-nor-5α-androstane-2β, 17β-dihydroxy compound (Ik), and
• 2α, 17α-dipropynyl-A-nor-5α-androstane-2β, 17β-dihydroxy bipropionate compound (Il);
• said filling agent is one or more selected from the group consisting of lactose, sorbitol, mannitol, xylitol, starch and inorganic salts;
• said disintegrant is one or more selected from the group consisting of crospovidone (PVPP), croscarmellose sodium (CC Na), sodium carboxymethyl starch (CMS-Na), and low-substituted hydroxypropylcellulose (L-HPC);
• said lubricant is one or more selected from the group consisting of stearic acid, sodium stearate, magnesium stearate, calcium stearate, and polyethylene glycol;
• said binder is one or more selected from the group consisting of starch slurry, hydroxypropylmethylcellulose (HPMC), povidone (PVP) and copovidone (Kollidon);
• said glidant is one or more selected from the group consisting of aerosil and talcum powder;
• a microcrystalline cellulose in the oral formulation is present in an amount of ≤1 wt %;
• and
• said oral formulation has one or more characteristics selected from a group consisting of:
• (i) under pH5.0-8.0, the dissolution rate Y30 of A-nor-5α androstane compound in said formulation within 30 minutes is ≥80%,
• (c) X3≥85%, wherein X3=Y3/Y30;
• Y3 is a dissolution rate of the A-nor-5α-androstane compound in said oral formulation within 30 minutes under pH 5.0-8.0 after stored for 180 days at a temperature of 40° C.±2° C. and a relative humidity of 75%±5%, and
• (d) X4≥85%, wherein X4=Y4/Y30;
• Y4 is a dissolution rate of the A-nor-5α-androstane compound in said oral formulation within 30 minutes under pH 5.0-8.0 after stored for 365 days at a temperature of 25° C.±2° C. and a relative humidity of 60%±10%.