Menthol-containing preparation

• US 20060121067A1
• Filed: 06/28/2004
• Published: 06/08/2006
• Est. Priority Date: 06/30/2003
• Status: Abandoned Application

• Current Assignee: Nihon Pharmaceutical Company Limited (Takeda Pharmaceutical Company Limited)
• Original Assignee: Nihon Pharmaceutical Company Limited (Takeda Pharmaceutical Company Limited)
• Inventors: Hamawaki, Tomonori, Kataoka, Yosuke, Isoda, Takako
• Application Number:
  US10/559,731
• Publication Number:
  US 20060121067A1
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61B 1/2736 Gastroscopes
• CPC Class Codes: A61B 1/31 for the rectum, e.g. proctoscopes, sigmoidoscopes , colonoscopes
• CPC Class Codes: A61K 31/045 Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/44 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 Class Codes: A61K 49/00 Preparations for testing in vivo
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

It is known that L-menthol controls smooth muscle contraction. In order to use L-menthol in practice as a digestive tract contraction inhibiting agent in digestive tract endoscopy, it is required to devise means of giving a formulation in which an L-menthol-containing formulation remains stable and transparent or little cloudy over a long time after the production and which shows little foaming at the administration. In the present invention, an antifoaming agent is further added to a formulation for inhibiting smooth muscle contraction or a peristaltic contraction in a digestive tract containing a L-menthol emulsion having an average particle size of less than 100 nm. Thus, it is possible to obtain a formulation that remains stable over a long time, has a high light transmittance, and produces little foam when filled into a container and sprayed at a target area to inhibit contraction to facilitate observation of the area in endoscopic examination of the digestive tract etc.

Claims

1. An L-menthol-containing formulation for inhibiting smooth muscle contraction, which comprises L-menthol, a surfactant, and an antifoaming agent and which is an emulsion with an average particle size of less than 100 nm.

2. The L-menthol-containing formulation according to claim 1, which further comprises a fat or oil.

3. The L-menthol-containing formulation according to claim 1, which has a light transmittance of 50% or more.

4. The L-menthol-containing formulation according to claim 1, which comprises 0.01 to 5.0% by weight of L-menthol, 0.1 to 10% by weight of a surfactant, and 0.0001 to 0.01% by weight of an antifoaming agent based on the weight of the whole formulation.

5. The L-menthol-containing formulation according to claim 4, wherein a content of the fat or oil is far from 0.1 to 10% by weight.

6. The L-menthol-containing formulation according to claim 1, wherein the antifoaming agent is at least one agent selected from silicone antifoaming agents.

7. The L-menthol-containing formulation according to claim 1, wherein the surfactant is at least one member selected from polyoxyethylene hydrogenated caster oils and sucrose fatty acid esters.

8. The L-menthol-containing formulation according to claim 2, which has a light transmittance of 50% or more.

9. The L-menthol-containing formulation according to claim 2, which comprises 0.01 to 5.0% by weight of L-menthol, 0.1 to 10% by weight of a surfactant, and 0.0001 to 0.01% by weight of an antifoaming agent based on the weight of the whole formulation.

10. The L-menthol-containing formulation according to claim 3, which comprises 0.01 to 5.0% by weight of L-menthol, 0.1 to 10% by weight of a surfactant, and 0.0001 to 0.01% by weight of an antifoaming agent based on the weight of the whole formulation.

11. The L-menthol-containing formulation according to claim 2, wherein the antifoaming agent is at least one agent selected from silicone antifoaming agents.

12. The L-menthol-containing formulation according to claim 3, wherein the antifoaming agent is at least one agent selected from silicone antifoaming agents.

13. The L-menthol-containing formulation according to claim 4, wherein the antifoaming agent is at least one agent selected from silicone antifoaming agents.

14. The L-menthol-containing formulation according to claim 5, wherein the antifoaming agent is at least one agent selected from silicone antifoaming agents.

15. The L-menthol-containing formulation according to claim 2, wherein the surfactant is at least one member selected from polyoxyethylene hydrogenated caster oils and sucrose fatty acid esters.

16. The L-menthol-containing formulation according to claim 3, wherein the surfactant is at least one member selected from polyoxyethylene hydrogenated caster oils and sucrose fatty acid esters.

17. The L-menthol-containing formulation according to claim 4, wherein the surfactant is at least one member selected from polyoxyethylene hydrogenated caster oils and sucrose fatty acid esters.

18. The L-menthol-containing formulation according to claim 5, wherein the surfactant is at least one member selected from polyoxyethylene hydrogenated caster oils and sucrose fatty acid esters.

19. The L-menthol-containing formulation according to claim 6, wherein the surfactant is at least one member selected from polyoxyethylene hydrogenated caster oils and sucrose fatty acid esters.