Racecadotril lipid compositions

Patent metadata

Field	Value
Publication number	US-9636300-B2
Application number	US-201414205565-A
Country	US
Kind code	B2
Filing date	Mar 12, 2014
Priority date	Mar 15, 2013
Publication date	May 2, 2017
Grant date	May 2, 2017

Abstract

A composition comprising racecadotril, at least one surfactant and a lipid.

First claim

What is claimed:

1. A composition for oral administration, comprising:
about 4% to about 10% racecadotril, about 90% of at least one surfactant and about 1% to about 2% lipid,
wherein the at least one surfactant is a glyceride selected from the group consisting of Distearoylphosphatidylglycerol (DSPG), L-α-dimyristoylphosphatidylcholine (DMPC), L-α-dimyristoylphosphatidylglycerol (DMPG), Polyoxyl 35 castor oil, Polyoxyl 40 hydrogenated castor oil, Polyoxyl 60 hydrogenated castor oil, PEG 300 capryliecapric glycerides, PEG 400 caprylic/capric glycerides, PEG 300 oleic glycerides, PEG 300 linoleic glycerides, Glyceryl Caprylate, Glyceryl Caprylate Diglyceride medium chain partial glycerides, and mixtures thereof,
wherein the lipid is a triglyceride selected from the group consisting of Long-chain triglycerides, Medium-chain triglycerides, Caprylic/capric triglycerides and mixtures thereof;
wherein the composition is stable for about 3 months at 40° C.

2. The composition of claim 1 , wherein the at least one surfactant is present in an amount of from about 88 wt. % to about 91 wt. % in total per 100 ml of the composition.

3. The composition of claim 1 , further comprising an optional ingredient selected from the group consisting of buffers, preservatives, sweeteners, viscosity modifiers, colors, aromas, flavors, and mixtures thereof.

4. The composition of claim 1 , further comprising an optional ingredient selected from the group consisting of xanthan gum, citric acid, sodium benzoate, sucralose, flavors and mixtures thereof.

5. The composition of claim 1 , wherein the composition has a total water content of less than about 3.5 wt. % based on the total weight of the composition.

6. The composition of claim 1 , wherein the at least one surfactant is castor oil.

7. The composition of claim 1 , wherein the at least one surfactant is selected from a monoglyceride and a diglyceride.

8. The composition of claim 1 , further comprising a digestive health active ingredient.

9. The composition of claim 8 , wherein the digestive health active ingredient is selected from the group consisting of laxatives, antacids, proton pump inhibitors, anti-gas agents, antiemetics, H2 blockers, and antidiarrheal agents.

10. The composition of claim 8 , wherein the anti-gas agent is simethicone.

11. The composition of claim 8 , wherein the antidiarrheal agent is loperamide.

12. A soft shell dosage form comprising the composition of claim 1 .

13. A hard shell dosage form containing the composition of claim 1 .

14. A tablet dosage form containing the composition of claim 1 .

15. A method for treating a subject experiencing diarrhea comprising the step of orally administering to the subject the composition of claim 1 .

Assignees

• Johnson & Johnson Consumer Inc

Inventors

• Lee Der-Yang

Classifications

• A61K31/222

  with compounds having aromatic groups, e.g. dipivefrine, ibopamine · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K9/1075 Primary

  Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence) · CPC title

• A61K47/44

  Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14) · CPC title

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title