Method for the production of a dosage form

Patent metadata

Field	Value
Publication number	US-11369571-B2
Application number	US-201716310491-A
Country	US
Kind code	B2
Filing date	Jun 14, 2017
Priority date	Jun 21, 2016
Publication date	Jun 28, 2022
Grant date	Jun 28, 2022

Abstract

A method is described for producing a dosage form and granules including surface-reacted calcium carbonate. Also described, are tablets and/or capsules obtained by the method. Methods using such a surface-reacted calcium carbonate, and a dosage form comprising the granules are also described. Further, methods of using the granules, or the tablets and/or capsules, or the dosage form in a pharmaceutical product, a nutraceutical product, an agricultural product, a cosmetic product, a home product, a food product, a packaging product and a personal care product are also described. A pharmaceutical product, a nutraceutical product, an agricultural product, a cosmetic product, a home product, a food product, a packaging product and a personal care product including the granules, or the tablets and/or capsules, or the dosage form are also described.

First claim

The invention claimed is:

1. A method of producing granules comprising surface-reacted calcium carbonate, the method comprising the steps of:
a) providing the surface-reacted calcium carbonate, wherein the surface-reacted calcium carbonate is a reaction product of: (1) natural ground or precipitated calcium carbonate with (2) carbon dioxide and (3) one or more H 3 O + ion donors in an aqueous medium, wherein the carbon dioxide is formed in-situ by the H 3 O + ion donor treatment and/or is supplied from an external source;
b) compacting the surface-reacted calcium carbonate of step a) by means of a roller compactor at a compaction pressure in the range from 1 kN/cm to 30 kN/cm into a compacted form;
c) milling the compacted form of step b) into granules; and
d) optionally, sieving the granules of step c) with at least one mesh size to obtain granules having a median grain size of from 180 μm to 710 μm;
wherein the method further comprises loading the compacted form obtained in step b) or the granules obtained in step c) with at least one active ingredient and/or inactive precursor thereof, to obtain loaded granules, wherein the loading is carried out by spraying or dropping the at least one active ingredient and/or inactive precursor thereof onto the compacted form obtained in step b) or the granules obtained in step c), and mixing in a device selected from the group consisting of a fluidized bed dryer/granulator, a ploughshare mixer, a vertical mixer, a horizontal mixer, a high shear mixer, a low shear mixer and a high speed blender, wherein the at least one active ingredient and/or inactive precursor thereof is in liquid form;
wherein the compacted form obtained in step b) comprises the surface-reacted calcium carbonate of step a); and
wherein the method further comprises mixing the granules with at least one formulating aid selected from the group consisting of a lubricant, an impact modifier, a plasticizer, a wax, a stabilizer, a pigment, a coloring agent, a scenting agent, a taste masking agent, a flavoring agent, a sweetener, a mouth-feel improver, a diluent, a film forming agent, an adhesive, a buffer, an adsorbent, an odor-masking agent and mixtures thereof.

2. The method according to claim 1 , wherein the natural ground calcium carbonate comprises a calcium carbonate containing mineral selected from the group consisting of marble, chalk, dolomite, limestone and mixtures thereof; and
wherein the precipitated calcium carbonate comprises a precipitated calcium carbonate having aragonitic, vateritic or calcitic mineralogical crystal forms and mixtures thereof.

3. The method according to claim 1 , wherein the surface-reacted calcium carbonate
i) has a BET specific surface area of from 20 m 2 /g to 450 m 2 /g measured using the nitrogen and BET method according to ISO 9277; and/or
ii) comprises particles having a volume median grain diameter d 50 of from 1 μm to 50 μm; and/or
iii) has an intra-particle intruded specific pore volume within the range of 0.15 cm 3 /g to 1.35 cm 3 /g calculated from a mercury intrusion porosimetry measurement.

4. The method according to claim 1 , wherein roller compacting step b) is carried out at a roller compaction pressure in the range from 1 kN/cm to 28 kN/cm.

5. The method according to claim 1 , wherein sieving step d) is carried out by sieving with a mesh having a size selected from the group consisting of 180 μm, 250 μm, 355 μm, 500 μm and 710 μm.

6. The method according to claim 1 , wherein the granules are mixed with a disintegrant.

7. The method according to claim 1 , wherein the at least one active ingredient and/or inactive precursor thereof is selected from the group consisting of a fragrance, a flavour, a herbal extract a fruit extract, a nutrient, a trace mineral, a repellent, food, a cosmetic, a flame retardant, an enzyme, a macromolecule, a pesticide, a fertilizer, a preserving agent, an antioxidant, a reactive chemical, a pharmaceutically active agent, a pharmaceutically inactive precursor of synthetic origin, a pharmaceutically inactive precursor of semi-synthetic origin, a pharmaceutically inactive precursor of natural origin thereof, and mixtures thereof.

8. The method according to claim 1 , further comprising a final step of tableting or filling the loaded granules into capsules.

9. The method according to claim 1 , wherein the at least one active ingredient and/or inactive precursor thereof is provided in a solvent selected from the group consisting of water, methanol, ethanol, n-butanol, isopropanol, n-propanol, n-octanol, acetone, dimethylsulphoxide, dimethylformamide, tetrahydrofurane, a vegetable oil, a derivative of a vegetable oil, an animal oil, a derivative of an animal oil, a molten fat, a wax, and mixtures thereof.

10. The method of claim 1 , wherein the compacted form obtained in step b) consists essentially of the surface-reacted calcium carbonate of step a).

11. The method according to claim 1 , wherein sieving step d) is carried out.

12. The method according to claim 1 , wherein the compacted form obtained in step b) does not comprise a formulating aid.

13. The method according to claim 1 , wherein the compacted form obtained in step b) does not comprise a binder or disintegrant.

14. The method according to claim 1 , wherein the compacted form obtained in step b) does not comprise an active ingredient and/or inactive precursor thereof.

Assignees

• Omya Int Ag

Inventors

• Diaz Quijano Carolina
• De Miguel Laura
• Schölkopf Joachim

Classifications

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• A61K2800/92

  Oral administration · CPC title

• A23K40/10

  by agglomeration; by granulation, e.g. making powders · CPC title

• A23V2002/00

  Food compositions, function of food ingredients or processes for food or foodstuffs · CPC title

• A61K2800/10

  General cosmetic use · CPC title