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Transmucosal administration of agents

A technology for mucosal drug administration and medicine, which is applied in the direction of antipyretics, anesthetics, anti-inflammatory agents, etc., can solve the problems related to the mucosal absorption of podocalyxin, and achieve the goal of improving absorption efficiency, convenience or effectiveness Effect

Pending Publication Date: 2022-03-18
DENKA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, podocalyxin is not at all known to be involved in the mucosal absorption of drugs

Method used

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  • Transmucosal administration of agents

Examples

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Embodiment

[0048] The present invention will be specifically described below, but the present invention is not limited by them.

reference example 1

[0049] Reference Example 1 Confirmation of the expression of podocalyxin in M-like cells in vitro

[0050] For example in literature (Kai H, Motomura Y, Saito S, Hashimoto K, Tatefuji T, Takamune N, Misumi S. Royal jelly enhances antigen-specific mucosal IgAresponse. Food SciNutr. 2013 Mar 6; 1(3): 222-227.) As described, 3×10 cells were inoculated on the membrane of a permeable cell culture chamber (Transwell) (Corning, pore size: 3 μm, 24 holes). 5 Caco-2 cells were left to stand overnight, and then the membrane of the permeable cell culture chamber was immersed in Eagle's MEM (20% FBS) containing 20% ​​fetal bovine serum and 0.1 mM non-essential amino acids. , 0.1 mM NEAAEMEM) in a 24-well plate. The permeable cell culture chamber was moved to a 24-well plate added with new 20% FBS and 0.1 mM NEAAEMEM approximately every 3 days and cultured for 21 days to form a Caco-2 monolayer. After 21 days of culture, add 1 × 10 to the upper chamber of the permeable cell culture chamb...

reference example 2

[0053] Reference Example 2 Confirmation of the expression of podocalyxin in intestinal M cells of cynomolgus monkeys

[0054] A portion of the cynomolgus monkey from the ileum side 30 cm from the cecum to the cecum was excised, embedded with an OCT embedding medium (Sakura Finetek), and frozen sections were prepared. The frozen sections containing Peyer's patches were fixed by immersion in cold acetone, and then masked by immersion in D-PBS containing 5% skim milk for 3 hours. After masking, use skim milk in D-PBS containing anti-podocalyxin antibody (R&D Systems), Alexa488-labeled donkey anti-goat IgG antibody, Alexa555-labeled anti-GP2 antibody, and diamino-phenyliodide (DAPI) To stain. The stained tissue sections were observed with a laser microscope (Keyence).

[0055] figure 2 3 shows an image observed by a laser microscope, and the expression of GP2, which is an M cell marker, was confirmed in the portion indicated by the arrow in the figure, and the expression of po...

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Abstract

Provided is a drug which improves the absorption efficiency of a drug from the mucosal epithelium. This transmucosal administration agent contains, as an active ingredient, an agent compound to which a podocalyxin target molecule is bound.

Description

technical field [0001] The present invention relates to a drug for transmucosal administration having excellent drug delivery performance. Background technique [0002] Transmucosal administration preparations are used for the treatment and prevention of various diseases, especially oral administration preparations account for most of the medicines due to the convenience of administration and low invasiveness. However, in transmucosal administration preparations, since the mucosal epithelial cell layer acts as a fat-soluble barrier, a drug with a small molecular size and high fat solubility can be efficiently absorbed from the mucosa. Drugs with large molecular size or very water-soluble drugs cannot pass through the mucosal epithelial layer and cannot be absorbed into the body. Therefore, no matter how excellent the pharmacological activity of the compound is, if it is a drug whose absorption from the mucosa is insufficient, it cannot be used in transmucosal administration...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/68A61P9/12A61P25/02A61P25/20A61P37/04A61P37/08A61P1/04A61P3/06A61P3/10A61P5/00A61P11/08A61P25/08A61P31/12A61P33/00A61P9/00A61P25/04A61P25/22A61P25/24A61P11/10A61P11/14A61P13/02A61P29/00A61P9/06A61P21/02A61P31/04A61P19/10A61P25/06A61P25/16A61P25/28A61P23/00A61P25/18A61P37/06A61P3/00A61P9/10A61P11/06A61P29/02
CPCA61K47/6803A61K9/0043A61K9/007A61K9/0048A61P9/12A61P25/02A61P25/20A61P37/04A61P37/08A61P1/04A61P3/06A61P3/10A61P5/00A61P11/08A61P25/08A61P31/12A61P33/00A61P9/00A61P25/04A61P25/22A61P25/24A61P11/10A61P11/14A61P13/02A61P29/00A61P9/06A61P21/02A61P31/04A61P19/10A61P25/06A61P25/16A61P25/28A61P23/00A61P25/18A61P37/06A61P3/00A61P9/10A61P11/06A61P29/02A61K47/6849C07K16/28A61K2039/541A61K9/0073A61K47/6927A61K9/006
Inventor 三隅将吾岸本直树三股亮大郎
Owner DENKA CO LTD
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