Preparation including vaccine adjuvant
AssigneeSumitomo Dainippon Pharma Co., Ltd.
InventorMaiko Onita
Life of this patent
Estimating the term…
Abstract
Provided is a composition that is useful as a vaccine adjuvant and has excellent storage stability and immunostimulatory activity. Specifically provided is a freeze-dried preparation that has high storage stability, said preparation containing a (4E,8E,12E,16E,20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexan-3-yl]amino}-6-methylpyrimidin-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaenamide, squalane, a hydrophilic surfactant, and an oleophilic surfactant, and being characterized by containing an ascorbic acid-based antioxidant and an excipient.
Claims28
A lyophilized formulation of an emulsion comprising:
- i) (4E,8E,12E,16E,20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexan-3-yl]amino}-6-methylpyrimidin-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaenamide (Compound A), or a pharmaceutically acceptable salt thereof;
- ii) squalane;
- iii) an antioxidant A selected from the group consisting of an ascorbate ester, an inorganic salt of ascorbic acid, and ascorbic acid;
- and
- iv) an excipient A selected from the group consisting of a non-reducing sugar and a sugar alcohol, provided that mannitol is excluded;
- wherein the D90 value of particle sizes of an emulsion reconstituted after 6-month storage at 5° C. as the lyophilized formulation is 1000 nm or less;
- wherein the amount of squalane in the formulation is 200 to 300 times the weight of Compound A in the formulation;
- wherein the amount of the antioxidant A in the formulation is 5 to 100 times the weight of Compound A in the formulation, in terms of the weight of sodium ascorbate;
- and
- wherein the amount of the excipient A in the formulation is 200 to 625 times the weight of Compound A in the formulation.
Dependencies are inferred from the claim text.