Method for the production of a dosage form

Patent metadata

Field	Value
Publication number	US-11400050-B2
Application number	US-201716309148-A
Country	US
Kind code	B2
Filing date	Jun 19, 2017
Priority date	Jun 21, 2016
Publication date	Aug 2, 2022
Grant date	Aug 2, 2022

Abstract

A method is described for producing a dosage form. Also described, are granules and tablets obtained by the method. The use of a surface-reacted calcium carbonate in such a method, a dosage form comprising the granules, the use of 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 as well as 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 such 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 a dosage form, the method comprising the steps of:
a) providing a 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) providing at least one active ingredient and/or inactive precursor thereof;
c) loading the surface-reacted calcium carbonate of step a) with the at least one active ingredient and/or inactive precursor thereof of step b);
wherein loading step c) is carried out by spraying or dropping the at least one active ingredient and/or inactive precursor thereof onto the surface-reacted calcium carbonate and mixing it 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 precursor thereof is in liquid form or is in a melted state;

d) compacting the loaded surface-reacted calcium carbonate obtained in step c) 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 comprising the surface-reacted calcium carbonate of step a) and the at least one active ingredient and/or inactive precursor thereof of step b);
e) milling the compacted form of step d) into granules; and
f) sieving the granules of step e) to obtain granules having a median grain size of from 180 μm to 710 μm, wherein the sieving step f) is carried out by sieving with at least two meshes having different sizes selected from the group consisting of 180 μm, 250 μm, 355 μm, 500 μm and 710 μm.

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; or the precipitated calcium carbonate is selected from the group consisting of a precipitated calcium carbonate having an aragonitic, vateritic or calcitic mineralogical crystal form and mixtures thereof.

3. The method according to claim 1 , wherein the surface-reacted calcium carbonate
a) 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
b) comprises particles having a volume median grain diameter d 50 of from 1 μm to 50 μm; and/or
c) 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 the at least one active ingredient and/or inactive precursor thereof is selected from the group consisting of a fragrance, a flavor, a herbal extract, 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 or 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.

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

6. The method according to claim 1 , wherein at least one formulating aid is provided at step b), step c), or step e), and
wherein the at least one formulating aid is selected from the group consisting of a disintegrant, 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.

7. The method according to claim 1 , further comprising a step g) of tableting the granules obtained in step e) or step f) or filling the granules obtained in step e) or step f) into capsules.

8. The method according to claim 1 , wherein the at least one active ingredient and/or inactive precursor 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 and a derivative thereof, an animal oil and a derivative thereof, a molten fat and wax, and a mixture thereof.

9. The method according to claim 1 , wherein loading step c) is carried out at a temperature range from 5° C. to 180° C. and under vacuum.

10. The method according to claim 1 , wherein the compacted form of step d) consists essentially of the surface-reacted calcium carbonate of step a) and the at least one active ingredient and/or inactive precursor thereof of step b).

11. The method according to claim 1 , wherein loading step c) is carried out at the melting temperature of the at least one active ingredient and/or inactive precursor thereof.

12. The method according to claim 1 , wherein the compacted form of the loaded surface-reacted calcium carbonate obtained in step d) consists essentially of the surface-reacted calcium carbonate and the at least one active ingredient and/or inactive precursor thereof.

13. The method according to claim 1 , wherein the compacted form of the loaded surface-reacted calcium carbonate obtained in step d) does not comprise a formulating aid.

14. The method according to claim 1 , wherein the compacted form of the loaded surface-reacted calcium carbonate obtained in step d) does not comprise a binder or disintegrant.

15. The method according to claim 1 , wherein loading step c) is carried out by spraying the at least one active ingredient and/or inactive precursor thereof onto the surface-reacted calcium carbonate.

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

• A61K9/2009

  Inorganic compounds · CPC title

• A61K8/00

  Cosmetics or similar toiletry preparations · CPC title

• A61K31/085

  having an ether linkage to aromatic ring nuclear carbon · CPC title

• A61K9/1611 Primary

  Inorganic compounds · CPC title