Pharmaceutical compositions comprising a fumaric acid ester and method for the preparation thereof
AssigneePharmathen S.A.
InventorsEvangelos KARAVAS, Efthymios KOUTRIS, Vasiliki SAMARA, Ioanna KOUTRI, Anastasia KALASKANI, Morfis ABATZIS, Manolis FOUSTERIS
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Abstract
The present invention relates to a delayed release pharmaceutical composition comprising a fumaric acid ester such as Dimethyl fumarate in the form of gastro-resistant tablets filled into hard gelation capsule.
Claims15
A delayed release pharmaceutical composition for oral administration comprising Dimethyl fumarate in a tablet core of diameter 5-10 mm wherein said core is coated with two gastro-resistant polymeric layers.
A delayed release pharmaceutical composition for oral administration comprising Dimethyl fumarate in a tablet core of diameter 5-10 mm wherein said core is coated with two gastro-resistant polymeric layers and exhibits the following in vitro release rate measured using Eu,Phar, paddles method at 100 rpm in buffer HCl 0.1N (for the 1st two hours) and change to phosphate buffer pH 6.8, at 37° C.:
- not more than 85 wt % Dimethyl fumarate released after 140 minutes;
- more than 90 wt % Dimethyl fumarate released after 150 minutes.
A process for the preparation of a delayed release pharmaceutical composition comprising Dimethyl fumarate in a tablet core of diameter 5- 10 mm wherein said core is coated with two gastro-resistant polymeric layers, which process comprises the steps of:
- Blending Dimethyl fumarate with croscarmellose sodium, microcrystalline cellulose colloidal silicon dioxide;
- Blending the above mixture with magnesium stearate;
- Direct tableting the powder mixture into round convex tablets;
- Spraying a solution of methacrylic acid methyl methacrylate, talc, triethyl citrate and ethanol onto the tablet cores up to the desired weight gain;
- Spraying a dispersion of methacrylic acid ethyl acrylate, talc, triethyl citrate and water onto the coated tablets up to the desired weight gain;
- The appropriate amount of enteric coated tablets are filled into hard gelatin capsules.
Dependencies are inferred from the claim text.