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.
Claims10
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 first and second pH-dependent gastro-resistant polymeric coating layers, and wherein the weight gain of the first polymeric coating layer is 4-8% w/w, and the weight gain of the second polymeric coating layer is 5-15% w/w.
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 first and second gastro-resistant coating layers, wherein the weight gain of the first polymeric coating layer is 4-8% w/w, and the weight gain of the second polymeric coating layer is 5-15% w/w and wherein the core exhibits an in vitro release rate of
- not more than 85 wt % Dimethyl fumarate released after 140 minutes;
- and
- 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 first and second gastro-resistant coating layers, which process comprises the steps of:
- Blending Dimethyl fumarate with croscarmellose sodium, microcrystalline cellulose and 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;
- wherein the weight gain of the first polymeric coating layer is 4-8% w/w, and that of the second polymeric coating layer is 5-15% w/w;
- and
- wherein the Dimethyl fumarate comprises particle size D90 value of less than 300 microns.
Dependencies are inferred from the claim text.