JPWO2020201515A5 - - Google Patents

Claims (16)

A solid pharmaceutical composition suitable for vaginal administration comprising:
a. 5-30 wt% glucono-delta-lactone (GDL); and b. 10-40 wt% hypromellose (HPMC)
A solid pharmaceutical composition comprising: 2. The pharmaceutical composition according to claim 1, wherein said pharmaceutical composition is a tablet. Up to 60% of the pharmaceutical composition dissolves within 2 hours using the United States Pharmacopeia (USP) dissolution apparatus 2-paddle method at 37° C. and 50 rpm in 500 mL of 50 mM acetate buffer (pH 4.0). The pharmaceutical composition according to claim 1 or 2 , wherein 4. Any one of claims 1-3, wherein the GDL is released in vivo for at least 6 hours, such as at least 12 hours, such as at least 18 hours, such as at least 24 hours, such as at least 36 hours, such as at least 42 hours. The pharmaceutical composition according to the paragraph. The pharmaceutical composition according to any one of claims 1-4, wherein the amount of GDL is 50-500 mg, such as about 150 mg or about 300 mg, such as 100-400 mg. A pharmaceutical composition according to any one of the preceding claims, wherein said composition comprises 10-25 wt% GDL, such as about 20 wt% or about 15 wt%. The pharmaceutical composition according to any one of claims 1-6, further comprising a gluconate salt, such as sodium gluconate (NaG). 8. The pharmaceutical composition of claim 7, wherein the composition comprises NaG in the range of 10-30 wt%, such as 15-25 wt%, such as 18-19 wt% or such as 24-25 wt%. A pharmaceutical composition according to claim 7 or 8 , wherein the molar ratio of GDL and gluconate is from 2:1 to 1:2, such as from 3 :2 to 2:3, such as about 1:1 . A pharmaceutical composition according to any one of the preceding claims, wherein said composition comprises HPMC in the range of 10-20 wt%, such as 20-35 wt%, or HPMC in the range of 15-40 wt%. of claims 1-10, wherein the viscosity of the HPMC is in the range of 50-200 mPas, such as 100 mPas, or the viscosity of the HPMC is in the range of 50.000-200.000 mPas, such as 100.000 mPas. A pharmaceutical composition according to any one of claims. Pharmaceutical composition according to any one of claims 1 to 11 , wherein said composition further comprises starch, silica , lubricants and/or cellulose such as microcrystalline cellulose (MCC) . Provided that the composition does not exceed 100 wt% in total of the ingredients,
a. 10-25 wt% GDL; 15-30 wt% NaG; 10-40 wt% HPMC; 10-25 wt% starch; 0.25-1.25 wt% silica; magnesium acid ,
b. 15 wt% HPMC; 36 wt% MCC; 14.25 wt% starch; 0.38 wt% silica; and 1.0 wt% magnesium stearate, or 10-30 wt% NaG; 5-40 wt% HPMC; 10-45 wt% MCC; 10-20 wt% starch; 25 wt% silica; and 0.5-1.5 wt% magnesium stearate, or
c. 24.5 wt% NaG; 35 wt% HPMC; 19 wt% starch; 0.5 wt% silica; and 1 wt% magnesium stearate. 15-30 wt% NaG; 30-40 wt% HPMC; 15-45 wt% starch; 0.25-1.25 wt% silica; and 0.5-1.5 wt% stearin. magnesium acid
2. The pharmaceutical composition of claim 1, comprising or consisting of: A pharmaceutical composition according to any one of claims 1 to 13 for use as a medicament. A pharmaceutical composition according to any one of claims 1 to 14 for use in the treatment of microbial infections , such as vaginal microbial infections. Use of a pharmaceutical composition according to any one of claims 1-15 in the manufacture of a medicament for the treatment of microbial infections such as vaginal microbial infections.