Anti-constipation composition

a composition and anti-constipation technology, applied in the field of anti-constipation composition, can solve the problems of poor intra-pooling effect, inability to use pges or pgfs as cathartic agents, and unknown activity of bi-cyclic tautomers as anti-constipation treatment and prevention agents,

Inactive Publication Date: 2012-01-26
SUCAMPO
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The bi-cyclic-halogenated compounds provide effective constipation relief with minimal side effects, promoting normal bowel movements and bowel cleansing, suitable for various conditions including constipation associated with hernia or cardiovascular diseases, and are useful for preparing the bowel for procedures.

Problems solved by technology

PGEs or PGFs are found to possess contraction of intestines caused by intestinal stimulation is great, while enteropooling effect is poor.
Accordingly, it is impossible to use PGEs or PGFs as cathartics because of side effects such as stomachache caused by the intestinal contraction.
However, the pronounced activity as anti-constipation treatment and prevention agents of the bi-cyclic tautomers has not been heretofore known.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0116]The biological activity of compositions due to the ratios of mono-cyclic / bi-cyclic structures when Z of general formula (I) is an oxygen atom, and a ketone is present at the C-9 position of the present invention can be seen from the following examples. The number of fluorine atoms at the C-16 position and the ratio of mono-cyclic / bi-cyclic structures are shown in Table 1.

[0117]Enteropooling tests and diarrhea tests were conducted. The results are set forth in Table 1. The dose that raise the intraintestinal content by 50% was referred to as ED50.

TABLE 1Example AExample BComparative Example ANumber of F atoms210at C-16 positionRatio of mono-4:961:1No signal derived fromcyclic / bi-cyclicbi-cyclic structure wasstructure*detected.Enteropooling0.6 μg / kg2 μg / kg320 μg / kgactivity, ED50Diarrhea in mice+: at 3 mg / kg (PO1)±: at 0.3 mg / kg (SC)−: at 10 mg / kg (PO)+: at 0.3 mg / kg (SC2)−: at 1 mg / kg (SC)*Determined by NMR measurement, in CDCl3 solution.1PO is by mouth (oral administration)2SC ...

example 2

[0118]The biological activity of the composition due to the ratios of mono-cyclic / bi-cyclic structures when Z in Formula (I) is an oxygen, a ketone is present at the C-9 position, and there is a double bond between the 5,6-carbons is shown below.

Enteropooling tests and diarrhea tests were conducted. The results are set forth below in Table 2. The dose that raise the intraintestinal content by 50% was referred to as ED50.

TABLE 2Example CExample DComparative Example CNumber of F atoms210at C-16 positionRatio of mono-4:961:1no signal derived fromcyclic / bi-cyclicbi-cyclic structure wasstructure*detected.Enteropooling0.3 μg / kg3 μg / kg220 μg / kgactivity, ED50Diarrhea in mice+: at 1 mg / kg (PO)1−: at 1 mg / kg (PO)−: at 10 mg / kg (PO)+: at 5 mg / kg (PO)*Determined by NMR measurement in CDCl3 solution.1PO is by mouth (oral administration)

Effect of the Present Invention Dissolved in Medium Chain Fatty Acid Triglyceride on Bowel Movement after Single Oral Administration to Healthy Male Volunteers

[01...

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Abstract

An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in ratio of bi-cyclic / mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I):where X1 and X2 are preferably both fluorine atoms. The composition can be used to treat constipation with out substantive side-effects, such as stomachache.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This is a request for a Continuation Application of U.S. application Ser. No. 11 / 142,251 filed Jun. 2, 2005, which is a divisional of U.S. application Ser. No. 10 / 443,046 filed May 22, 2003, now abandoned, which is a divisional of U.S. application Ser. No. 10 / 138,650 filed May 6, 2002, now U.S. Pat. No. 6,610,732, which is a divisional of U.S. application Ser. No. 09 / 655,760 filed Sep. 5, 2000, now U.S. Pat. No. 6,414,016, the disclosures of all of which are incorporated herein by reference.BACKGROUND OF THE INVENTION[0002]Prostaglandins (hereinafter referred to as PGs) is the name of the group of fatty acids which possess various physiological activities and are contained in human and animal tissues and organs. PGs basically contain the prostanoic acid skeleton of the following formula:[0003]and some synthetic products may contain the above skeleton with some modification. PGs are classified into several types according to the structure ...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/352A61P1/10C07D311/94A61K31/23A61K31/335A61K31/35A61K31/4741A61K31/557A61K31/5575A61K31/558
CPCA61K31/335C07D335/04A61K31/352A61K31/4741A61K31/557A61K31/35C07D221/04C07C405/00A61K31/559A61K31/5575Y10S514/892A61K2300/00A61P1/00A61P1/10A61P1/12
InventorUENO, RYUJI
OwnerSUCAMPO