Absorption promoter and use for same

Patent metadata

Field	Value
Publication number	US-11219688-B2
Application number	US-201816489181-A
Country	US
Kind code	B2
Filing date	Mar 2, 2018
Priority date	Mar 3, 2017
Publication date	Jan 11, 2022
Grant date	Jan 11, 2022

Abstract

To provide an absorption promotor that is capable of improving the efficiency in absorption of a pharmaceutical drug and that is highly stable, an absorption promotor includes an oxa acid having a structure represented by the formula (1) below,where R1 represents a linear or branched hydrocarbon group having 1 to 40 carbon atoms, one or more but not all carbon atoms of which hydrocarbon group have optionally been substituted by an oxygen atom, a nitrogen atom, or a sulfur atom, the hydrocarbon group being saturated or unsaturated; m represents a real number of 0 to 50; n represents an integer of 1 to 5; and —C(═O)—X represents a functional group capable of chemical reaction.

First claim

The invention claimed is:

1. An oral preparation comprising:
an absorption promotor containing an oxa acid having a structure represented by formula (A) below,
n -CH 3 (CH 2 ) 7 —CH═CH(CH 2 ) 8 —(OCH 2 CH 2 ) p —O—(CH 2 ) n —COOH  (A)

where p on average is a real number of 1 to 9, and n is an integer of 1 to 5;

soybean oil; and
a drug,
wherein the oral preparation is a capsule, a powder, a granule, a syrup, or a liquid drug for internal use.

2. The oral preparation according to claim 1 , further comprising water.

3. The oral preparation according to claim 1 , further comprising a surfactant.

4. The oral preparation according to claim 1 ,
wherein
the absorption promotor, together with the soybean oil, form micelles; and
the micelles have an average particle diameter of not more than 1000 nm.

5. The oral preparation according to claim 4 , wherein not less than 5% of the micelles each have a particle diameter of not more than 100 nm.

6. The oral preparation according to claim 1 , further comprising water, wherein
the absorption promotor is present in an amount of 5% by weight to 20% by weight;
the soybean oil is present in an amount of 5% by weight to 30% by weight; and
the water is present an amount of 50% by weight to 90% by weight.

7. The oral preparation according to claim 1 , wherein in the formula (A), n is 1.

Assignees

• Moresco Corp

Inventors

• Sugawara Mitsuru
• Sato Yuki
• Takekuma Yoh
• Maruyama Shingo

Classifications

• A61K31/122 Primary

  having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin · CPC title

• A61K31/121

  acyclic · 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

• A61K47/12 Primary

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61K9/1075

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