Calcifediol soft capsules

Claims

PATENT REQUESTS 1. Soft capsule containing: a) soft capsule shell, where the soft capsule shell contains: 40 to 80% by weight of gelatin, 10 to 50 wt.% of a plasticizer selected from the group consisting of glycerol, sorbitol, propylene glycol, polyethylene glycol, dibutyl sebacate, diethyl phthalate, dimethyl phthalate, triacetin, tributyl citrate, triethyl citrate, and mixtures thereof, quantities by mass are expressed in relation to the total mass of the soft capsule shell; and b) pharmaceutical composition containing: calcifediol, an oil component selected from the group consisting of medium chain triglycerides, isopropyl myristate, C14-C18 alkyl alcohols, C14-C18 alkenyl alcohols, lanolin alcohols and mixtures thereof, and a pharmaceutically acceptable organic solvent selected from the group consisting of ethanol, isopropanol, propylene glycol, polyethylene glycol, benzyl alcohol and mixtures thereof, wherein the soft capsule shell encapsulates the pharmaceutical composition and wherein said pharmaceutical composition is wax-free.

2. The soft capsule according to claim 1, wherein the pharmaceutical formulation comprises: 0.001 to 0.2 wt.% calcifediol, 80 to 99.9 wt.% oil component, and 0.3 to 6 wt.% of a pharmaceutically acceptable organic solvent; The amounts by weight are expressed relative to the total weight of calcifediol, oil component and pharmaceutically acceptable organic solvent present in the pharmaceutical composition.

3. A soft capsule according to any one of the preceding claims, wherein the oil component is selected from the group consisting of medium chain triglycerides, isopropyl myristate, C14-C18 alkenyl alcohols, and mixtures thereof.

4. A soft capsule according to any one of the preceding claims, wherein the oil component is a medium chain triglyceride, preferably caprylic / capric triglyceride, and / or wherein the pharmaceutically acceptable organic solvent is selected from the group consisting of ethanol, isopropanol, propylene glycol, polyethylene glycol and mixtures thereof, preferably ethanol.

5. A soft capsule according to any one of the preceding claims, which is free of surfactants.

6. A soft capsule according to any one of the preceding claims, wherein the pharmaceutical composition further comprises calcium or a pharmaceutically acceptable derivative thereof.

7. A soft capsule according to any one of the preceding claims, wherein the pharmaceutical composition further comprises iron or a pharmaceutically acceptable derivative thereof, vitamin B12, vitamin B9, levomefolic acid or a pharmaceutically acceptable salt thereof, and / or an essential unsaturated fatty acid, or mixtures thereof.

8. A soft capsule according to any preceding claim, wherein the pharmaceutical composition further comprises a bisphosphonate.

9. A soft capsule according to any one of the preceding claims, wherein the soft capsule shell further comprises a pharmaceutically acceptable opacifying agent and / or a pharmaceutically acceptable coloring agent.

10. A soft capsule according to any one of the preceding claims containing from 200 to 180,000 IU of calcifediol.

11. A soft capsule as defined in any of the preceding claims for use in medicine.

12. A soft capsule as defined in any one of claims 1 to 10 for use in the treatment and / or prevention of a disease selected from the group consisting of vitamin D deficiency, demineralization such as hypocalcemia and hypophosphatemia, renal osteodystrophy, rickets, osteoporosis, osteopenia, osteoarthritis, osteoarthrosis, osteomalacia, hypoparathyroidism, and inflammatory bowel disease.

13. The soft capsule for use according to claim 12, wherein the soft capsule is for administration once every three months, once every two months, once a month, once every three weeks, once every two weeks, once a week, or once a day.

14. A process for preparing a soft capsule as defined in any one of claims 1 to 10, said process comprising: a) preparing a mixture comprising calcifediol; an oil component; and a pharmaceutically acceptable organic solvent; and optionally calcium or a pharmaceutically acceptable derivative thereof, iron or a pharmaceutically acceptable derivative thereof, vitamin B12, vitamin B9, levomefolic acid or a pharmaceutically acceptable salt thereof, an essential unsaturated fatty acid and / or a bisphosphonate; b) preparing a mixture comprising gelatin; a plasticizer; water; and an optional pharmaceutically acceptable opacifying agent and / or a pharmaceutically acceptable coloring agent; c) forming a coating from the mixture of step b); d) filling the casing with the mixture from step a), and e) drying the capsule obtained in step d).