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CN-122003230-A - Quick release soft gel formulation

CN122003230ACN 122003230 ACN122003230 ACN 122003230ACN-122003230-A

Abstract

A fast-release soft gel capsule formulation comprising 15 to 60 mass% of one or more film-forming polymers, 1 to 30 mass% of one or more disintegrants, 5 to 30 mass% of one or more plasticizers or co-solvents, and 10 to 45 mass% of one or more solvents. A process for making a fast-release soft gel capsule includes (a) preparing a gel block composition comprising one or more film-forming polymers, one or more disintegrants, one or more plasticizers or co-solvents, and one or more solvents to form a gel block, (b) heating the gel block to form a uniform and degassed gel block, (c) aging the uniform and degassed gel block to form an aged gel block, (d) casting the aged gel block into a film or tape using a thermally controlled drum or surface, (e) transferring the homogenized fill solution to a packaging line, (f) encapsulating the homogenized fill solution within the gel block film or tape using rotary die encapsulation to form a capsule, (g) drying and trimming the capsule, (h) optionally coating and drying the capsule with a coating, and (i) post-treating and packaging.

Inventors

  • R. Perry
  • L. Fankovei
  • G. Vam Vakus
  • S. Batalai

Assignees

  • 帕西恩软胶公司

Dates

Publication Date
20260508
Application Date
20240816
Priority Date
20230818

Claims (20)

  1. 1. A rapid release soft gel capsule formulation, the formulation comprising: About 15 to 60 mass% of one or more film forming polymers; about 1 to 30 mass% of one or more disintegrants; About 5 to 30 mass% of one or more plasticizers or co-solvents, and About 10 to 45 mass% of one or more solvents.
  2. 2. The formulation of claim 1, wherein the one or more film-forming polymers comprise gelatin, gelatin hydrolysate, collagen, carrageenan, or agar.
  3. 3. The formulation of claim 1 or 2, wherein the one or more film-forming polymers comprises gelatin having a Bloom value of about 50 Bloom to about 200 Bloom.
  4. 4. The formulation of claim 3, wherein the gelatin has a Bloom value of about 150 Bloom.
  5. 5. The formulation of any preceding claim, wherein the formulation comprises from about 20 to 40 mass% of the one or more film-forming polymers.
  6. 6. A formulation according to any preceding claim, wherein the one or more disintegrants comprise sodium carboxymethyl starch, croscarmellose sodium, crospovidone, calcium silicate, magnesium aluminium silicate or cross-linked alginic acid.
  7. 7. The formulation of any preceding claim, wherein the formulation comprises from about 5 to 25 mass% of the one or more disintegrants.
  8. 8. The formulation of claim 7, wherein the formulation comprises about 8 to 12 mass% of the one or more disintegrants.
  9. 9. The formulation of claim 7, wherein the formulation comprises about 15 to 25 mass% of the one or more disintegrants.
  10. 10. The formulation of any preceding claim, wherein the one or more plasticizers or co-solvents comprise a solution of a polyol, a monosaccharide, a disaccharide, an oligosaccharide, a blended hydrophilic molecule, glycerol, sorbitol, polyethylene glycol, or maltitol.
  11. 11. The formulation of any preceding claim, wherein the formulation comprises from about 10 to 20 mass% of the one or more plasticizers or co-solvents.
  12. 12. The formulation of any preceding claim, wherein the one or more solvents comprise water.
  13. 13. The formulation of any preceding claim, further comprising one or more of a colorant, opacifier, flavor or sweetener, humectant, preservative, coating, viscosity modifying agent, filler or extender, active pharmaceutical ingredient, viscosity modifying polymer or buffer salt, and acid.
  14. 14. The formulation of claim 13, wherein the formulation comprises from about 0.01 mass% to 10 mass% of one or more colorants, the one or more colorants comprising synthetic dyes, natural dyes, or combinations thereof.
  15. 15. The formulation of claim 13, wherein the formulation comprises from about 0.01 to 1 mass% of one or more opacifying agents comprising titanium dioxide, zinc oxide, calcium carbonate, or a combination thereof.
  16. 16. The formulation of claim 13, wherein the formulation comprises about 0.01 to 1 mass% of one or more flavoring or sweetening agents.
  17. 17. The formulation of any preceding claim, further comprising from 1 to 20 mass% of one or more viscosity modifying polymers.
  18. 18. The formulation of claim 17, wherein the formulation comprises about 5 to 15 mass% of the one or more viscosity modifying polymers.
  19. 19. The formulation of claim 17, wherein the formulation comprises about 10 mass% of the one or more viscosity modifiers.
  20. 20. The formulation of claims 17-19, wherein the one or more viscosity modifying polymers comprise hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinyl alcohol, and dextran.

Description

Quick release soft gel formulation Background Soft gel capsules are popular and accepted for their aesthetic and transparent gelatin shells. In addition, soft gel capsules are homogeneous, stable, dissolve relatively quickly, allow for liquid formulations, and are easier for most subjects to swallow. Soft gel capsules are typically formed from a capsule shell that encapsulates a liquid matrix fill. The matrix fill may be aqueous or oil-based, depending on the solubility of the Active Pharmaceutical Ingredient (API). There is an increasing interest in developing fast dissolving soft gel capsules. What is needed is a soft gel capsule that readily dissolves or ruptures and rapidly releases the API. Disclosure of Invention One embodiment described herein is a fast-release soft gel capsule formulation comprising about 15 to 60 mass% of one or more film forming polymers, about 1 to 30 mass% of one or more disintegrants, about 5 to 30 mass% of one or more plasticizers or co-solvents, and about 10 to 45 mass% of one or more solvents. Optionally, the formulation further comprises about 1 to 20 mass% of one or more viscosity modifying polymers. In one aspect, the one or more film-forming polymers include gelatin, gelatin hydrolysate, collagen, carrageenan, or agar. In another aspect, the one or more film-forming polymers include gelatin having a Bloom value of about 50 Bloom to about 200 Bloom. In another aspect, the gelatin has a Bloom value of about 150 Bloom. In another aspect, the formulation comprises from about 20% to 40% by mass of one or more film-forming polymers. In another aspect, the one or more disintegrants include sodium carboxymethyl starch, croscarmellose sodium, crospovidone, calcium silicate, magnesium aluminum silicate, or cross-linked alginic acid. In another aspect, the formulation comprises from about 5 to 25 mass% of one or more disintegrants. In another aspect, the formulation comprises about 8 to 12 mass% of one or more disintegrants. In another aspect, the formulation comprises about 15 to 25 mass% of one or more disintegrants. in another aspect, the one or more plasticizers or co-solvents include solutions of polyols, monosaccharides, disaccharides, oligosaccharides, blended hydrophilic molecules, glycerol, sorbitol, polyethylene glycol, or maltitol. In another aspect, the formulation comprises from about 10 to 20 mass% of one or more plasticizers or co-solvents. In another aspect, the one or more solvents include water. The formulation of claim 1, further comprising one or more of a colorant, opacifier, flavor or sweetener, humectant, preservative, coating, viscosity modifying agent, filler or extender, active pharmaceutical ingredient, viscosity modifying polymer or buffer salt, and acid. In another aspect, the formulation comprises from about 0.01 to 10 mass% of one or more colorants, including synthetic dyes, natural dyes, or combinations thereof. In another aspect, the formulation comprises from about 0.01 to 1 mass% of one or more opacifying agents comprising titanium dioxide, zinc oxide, calcium carbonate, or a combination thereof. In another aspect, the formulation comprises from about 0.01% to 1% by mass of one or more flavoring or sweetening agents. In another aspect, the formulation comprises from about 1% to 20% by mass of one or more viscosity modifying polymers. In another aspect, the formulation comprises 5 to 15 mass% of one or more viscosity modifying polymers, or about 10 mass% of one or more viscosity modifying agents. In another aspect, the formulation comprises one or more viscosity modifying polymers comprising hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinyl alcohol, and dextran. In another aspect, the capsule breaks in USP apparatus II at 37 ℃ within about 3 minutes to 9 minutes. In another aspect, the capsule breaks in USP apparatus II at 37 ℃ within about 5 minutes. Another embodiment described herein is a method for making a fast-release soft gel capsule comprising preparing a gel block composition comprising one or more film-forming polymers, one or more disintegrants, one or more plasticizers or co-solvents, and one or more solvents to form a gel block, and optionally one or more viscosity modifying polymers, heating the gel block to form a uniform and degassed gel block, aging the uniform and degassed gel block to form an aged gel block, casting the aged gel block into a film or tape using a thermally controlled drum or surface, transferring the homogenized fill solution to an encapsulation line, encapsulating the homogenized fill solution within the gel block film or tape using a rotary die encapsulation to form a capsule, drying and trimming the capsule, optionally coating and drying the capsule with a coating, and post-treating and packaging. In one aspect, the gel block comprises about 15 to 60 mass% of one or more film forming polymers, about 1 to 30 mass% of one or more disintegrants, about 5 to 30 mass% of one or more plasticizers