Liquisoft capsules

• US 10,555,901 B2
• Filed: 10/27/2017
• Issued: 02/11/2020
• Est. Priority Date: 03/26/2015
• Status: Active Grant

• Current Assignee: Patheon Softgels, Inc. (Thermo Fisher Scientific Incorporated)
• Original Assignee: Patheon Softgels, Inc. (Thermo Fisher Scientific Incorporated)
• Inventors: Zhao, YinYan, Hu, Yunhua, Williams, Jr., Mervin, Dyakonov, Tatyana, Gosangari, Saujanya, Yang, Chue, Van Duijnhoven, Henricus Marinus Gerardus Maria, Piest, Martin, Fatmi, Aqeel A
• Primary Examiner(s): Purdy, Kyle A
• Application Number:
  US15/795,814
• Publication Number:
  US 20180049979A1
• Time in Patent Office: 837 Days
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/045 Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/4825 Proteins, e.g. gelatin gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816
• CPC Class Codes: A61K 9/4833 Encapsulating processes; Filling of capsules mechanical aspects A61J3/07
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds

Abstract

Described herein are oral pharmaceutical compositions suitable for chewing, sucking, or buccal dissolution comprising soft gel capsules and liquid fills, methods for making the same, and methods for treating subjects in need thereof with such capsules. In particular, oral pharmaceutical compositions comprising chewable, suckable, or dissolvable soft gel capsules with various flowable fill compositions are described.

Claims

1. An oral pharmaceutical composition suitable for chewing, sucking, or buccal dissolution comprising a soft shell encapsulating a liquid matrix,

the shell comprising:

(a) about 20% gelatin, 150 Bloom;

(b) about 9% gelatin, 100 Bloom;

(c) about 5% hydrolyzed collagen;

(d) about 17% lycasin;

(e) about 25% glycerin;

(f) about 0.5% citric acid;

(g) about 2.5% about xylitol,

(h) about 0.2% sucralose; and

(i) about 21% water; and

the matrix comprising;

(j) about 21% polyethylene glycol 500,

(k) about 8% propylene glycol;

(l) about 1% polyvinylpyrrolidone K30;

(m) about 58% lycasin;

(n) about 1% citric acid;

(o) about 1% lactic acid;

(p) about 0.6% sucralose,

(q) about 0.6% acesulfame potassium;

(r) about 5% water;

(s) about 1% dextromethorphan hydrobromide; and

(t) about 0.1% menthol.

5. A kit for dispensing the oral pharmaceutical composition of claim 1, the kit comprising:

(a) at least one oral pharmaceutical composition;

(b) at least one moisture proof dispensing receptacle comprising blister or strip packs, an aluminum blister, a transparent or opaque polymer blister with pouch, polypropylene tubes, colored blister materials, tubes, bottles, and bottles optionally containing a child-resistant feature, optionally comprising a desiccant, such as a molecular sieve or silica gel; and

optionally

(c) at least one daily regimen for the oral pharmaceutical composition; and

(d) an insert comprising instructions or prescribing information for the oral pharmaceutical composition.

6. A pharmaceutical combination comprising the oral pharmaceutical composition of claim 1 and one or more additional therapeutic compounds selected from NSAIDS, diphenhydramine, or codeine.

7. A method for treating, retarding the progression of, prophylaxis of, delaying the onset of, ameliorating, reducing the symptoms of inflammation, cough, cold, chest congestion, nasal congestion, sinusitis, throat or bronchial irritation, flu, fever, or pain comprising administering to a subject in need thereof the oral pharmaceutical composition of claim 1.

2. An oral pharmaceutical composition suitable for chewing, sucking, or buccal dissolution comprising a soft shell encapsulating a liquid matrix,

the shell comprising:

(a) about 27% gelatin, 100 Bloom;

(b) about 5% hydrolyzed collagen;

(c) about 17% lycasin;

(e) about 21% glycerin;

(f) about 1% propylene glycol;

(g) about 0.5% citric acid;

(h) about 2.5% xylitol;

(i) about 0.8% sucralose;

(j) about 0.1% peppermint oil;

(k) about 24% water; and

the matrix comprising;

(l) about 42% glycerin;

(m) about 2% propylene glycol;

(n) about 3% polyvinylpyrrolidone K30;

(o) about 40% sorbitol;

(p) about 0.3% citric acid;

(q) about 0.5% sucralose;

(r) about 0.1% eucalyptol;

(s) about 0.3% peppermint oil;

(t) about 10% water;

(u) about 0.004% thymol; and

(v) about 0.2% menthol.

8. A kit for dispensing the oral pharmaceutical composition of claim 2, the kit comprising:

(a) at least one oral pharmaceutical composition;

(b) at least one moisture proof dispensing receptacle comprising blister or strip packs, an aluminum blister, a transparent or opaque polymer blister with pouch, polypropylene tubes, colored blister materials, tubes, bottles, and bottles optionally containing a child-resistant feature, optionally comprising a desiccant, such as a molecular sieve or silica gel; and

optionally

(c) at least one daily regimen for the oral pharmaceutical composition; and

(d) an insert comprising instructions or prescribing information for the oral pharmaceutical composition.

9. A pharmaceutical combination comprising the oral pharmaceutical composition of claim 2 and one or more additional therapeutic compounds selected from chlorhexidine or ethanol.

10. A method for treating, retarding the progression of, prophylaxis of, delaying the onset of, ameliorating, reducing the symptoms of, or promoting health, including but not limited to of one or more of dry mouth, halitosis, stained teeth, oral pain, loss of enamel, refreshing breath, inhibiting onset of breath malodor, or freshening the oral cavity comprising administering to a subject in need thereof the oral pharmaceutical composition of claim 2.

3. An oral pharmaceutical composition suitable for chewing, sucking, or buccal dissolution comprising a soft shell encapsulating a liquid matrix:

the shell comprising;

(a) about 22% gelatin, 150 Bloom;

(b) about 10% gelatin, 100 Bloom;

(c) about 5% gelatin hydrolysate;

(d) about 20% glycerin;

(e) about 17% maltitol;

(f) about 0.5% citric acid;

(g) about 2.6% xylitol;

(h) about 0.2% sucralose;

(i) about 0.3% peppermint oil; and

(j) about 21% water; and

the matrix comprising;

(k) about 1% polyethylene glycol 400;

(l) about 19% glycerin;

(m) about 3% xylitol;

(n) about 37% maltitol;

(o) about 5% glycine;

(p) about 0.2% sucralose;

(q) about 0.04% menthol;

(r) about 0.04% peppermint oil;

(s) about 17% water; and

(t) about 2% nicotine polacrilex.

11. A kit for dispensing the oral pharmaceutical composition of claim 3, the kit comprising:

(a) at least one oral pharmaceutical composition;

(b) at least one moisture proof dispensing receptacle comprising blister or strip packs, an aluminum blister, a transparent or opaque polymer blister with pouch, polypropylene tubes, colored blister materials, tubes, bottles, and bottles optionally containing a child-resistant feature, optionally comprising a desiccant, such as a molecular sieve or silica gel; and

optionally

(c) at least one daily regimen for the oral pharmaceutical composition; and

(d) an insert comprising instructions or prescribing information for the oral pharmaceutical composition.

12. A pharmaceutical combination comprising the oral pharmaceutical composition of claim 3 and one or more additional therapeutic compounds selected from bupropion or varenicline.

13. A method for treating, retarding the progression of, prophylaxis of, delaying the onset of, ameliorating, or reducing the symptoms of, or promoting health, including but not limited to cessation of urge to smoke, satiating nicotine desire, nicotine-replacement therapy, or smoking cessation therapy comprising administering to a subject in need thereof the oral pharmaceutical composition of claim 3.

4. An oral pharmaceutical composition suitable for chewing, sucking, or buccal dissolution comprising a soft shell encapsulating a liquid matrix:

the shell comprising;

(a) about 19% gelatin, 150 Bloom;

(b) about 13% gelatin, 100 Bloom;

(c) about 2% gelatin hydrolysate;

(d) about 22% glycerin;

(e) about 14% maltitol;

(f) about 0.5% citric acid;

(g) about 2.5% xylitol;

(h) about 0.2% sucralose; and

(i) about 29% water; and

the matrix comprising;

(j) about 1% polyethylene glycol 400;

(k) about 2% glycerin;

(l) about 6% propylene glycol;

(m) about 27% sorbitol;

(n) about 3% xylitol;

(o) about 0.2% sucralose;

(p) about 0.04% menthol;

(q) about 0.04% peppermint oil;

(r) about 11% water; and

(s) about 47% bismuth subsalicylate.

14. A kit for dispensing the oral pharmaceutical composition of claim 4, the kit comprising:

(a) at least one oral pharmaceutical composition;

(b) at least one moisture proof dispensing receptacle comprising blister or strip packs, an aluminum blister, a transparent or opaque polymer blister with pouch, polypropylene tubes, colored blister materials, tubes, bottles, and bottles optionally containing a child-resistant feature, optionally comprising a desiccant, such as a molecular sieve or silica gel; and

optionally

(c) at least one daily regimen for the oral pharmaceutical composition; and

(d) an insert comprising instructions or prescribing information for the oral pharmaceutical composition.

15. A pharmaceutical combination comprising the oral pharmaceutical composition of claim 4 and one or more additional therapeutic compounds selected from cimetidine, ranitidine, famotidine, ondansetron, omeprazole, lansoprazole, rabeprazole, esomeprazole, pantoprazole, calcium supplements, calcium hydroxide, alluminum hydroxide, magnesium hydroxide, or combinations thereof.

16. A method for treating, retarding the progression of, prophylaxis of, delaying the onset of, ameliorating, or reducing the symptoms of, or promoting health, including but not limited to of one or more of inflammation of the gastrointestinal tract, neoplasia, hyperthyroidism, hypercalcemia, hyperparathyroidism, parathyroid carcinoma, indigestion, heartburn, nausea, flatulence, bloating, acid reflux, irritable bowels, constipation, diarrhea, comprising administering to a subject in need thereof comprising administering to a subject in need thereof the oral pharmaceutical composition of claim 4.