Nanosuspension containing progerinin, and preparation method therefor
AssigneePrg S&Tech Inc.
InventorMin Ju KIM
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Abstract
The present invention relates to a nanosuspension formulation suitable for a progerinin drug, which is insoluble, and a preparation method therefor, wherein the progerinin nanosuspension is a vehicle composition for improving dispersive stability of a progerinin drug(a), which is insoluble, and employs hydroxypropylmethyl cellulose (HPMC)(b) or hydroxypropyl cellulose (HPC)(b′), TPGS(c) or sodium dioctyl succinate (DOSS)(c′), and potassium sorbate(d), and a mixture thereof was subjected to wet-type ball milling in a Dyno-Mill chamber to prepare a white nanosuspension containing a progerinin drug with an average particle diameter of 100 nm to 300 nm.
Claims16
A nanosuspension comprising progerinin, the nanosuspension comprising:
- (a) 1 to 10 wt % of a progerinin compound represented by the following Chemical Formula 1;
- (b) 0.5 to 5 wt % of hydroxypropyl methylcellulose (HPMC) which is a polymeric suspension;
- (c) 0.5 to 5 wt % of D-α-tocopherol polyethylene glycol succinate (TPGS) which is a solubility enhancer;
- and
- (d) 0.1 to 0.5 wt % of potassium sorbate which is a preservative:
- wherein the progerinin compound is drug particles formed via wet type ball milling in an average particle diameter (D50) of 100 nm to 300 nm.
A nanosuspension comprising progerinin, the nanosuspension comprising:
- (a) 1 to 10 wt % of a progerinin compound represented by the following Chemical Formula 1;
- (b′) 0.5 to 5 wt % of hydroxypropyl cellulose (HPC) which is a polymeric suspension;
- (c′) 0.1 to 0.5 wt % of dioctyl sodium sulfosuccinate (DOSS) which is a surfactant;
- and
- (d) 0.1 to 0.5 wt % of potassium sorbate which is a preservative:
- wherein the progerinin compound is drug particles formed via wet type ball milling in an average particle diameter (D50) of 100 nm to 300 nm.
A method of preparing a nanosuspension comprising progerinin, the method comprising:
- (i) mixing purified water with hydroxypropyl methylcellulose (HPMC) (b) and D-α-tocopherol polyethylene glycol succinate (TPGS) (c) to prepare a vehicle solution and then adding and mixing progerinin (a) represented by the following Chemical Formula 1 so as to prepare a suspension;
- (ii) subjecting the suspension to wet type ball milling to prepare a nanosuspension;
- and
- (iii) mixing the nanosuspension with potassium sorbate (d) to finally prepare a nanosuspension with enhanced stability:
- wherein the progerinin compound in the nanosuspension of (iii) is in the form of drug particles with an average particle diameter (D50) of 100 nm to 300 nm.
A method of preparing a nanosuspension comprising progerinin, the method comprising:
- (i) mixing purified water with hydroxypropyl cellulose (HPC) (b′);
- and dioctyl sodium sulfosuccinate (DOSS) (c′) to prepare a vehicle solution and then adding and mixing progerinin (a) represented by the following Chemical Formula 1 so as to prepare a suspension;
- (ii) subjecting the suspension to wet type ball milling to prepare a nanosuspension;
- and
- (iii) mixing the nanosuspension with potassium sorbate (d) to finally prepare a nanosuspension with enhanced stability:
- wherein the progerinin compound in the nanosuspension of (iii) is in the form of drug particles with an average particle diameter (D50) of 100 nm to 300 nm.
Dependencies are inferred from the claim text.