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Methods of treatment using cadotril compositions

A composition, the technology of racecadotril, which is applied in the directions of drug combination, pharmaceutical formula, medical preparation of non-active ingredients, etc., can solve the problems of poor water solubility and dissolution rate, limited absorption, etc. Rapid onset of action and improved bioavailability

Inactive Publication Date: 2018-04-17
JOHNSON & JOHNSON CONSUMER COPANIES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0024] Racecadotril is a class II drug (according to the Biopharmaceutical Classification System) with poor water solubility and rate of dissolution and therefore limited absorption

Method used

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  • Methods of treatment using cadotril compositions
  • Methods of treatment using cadotril compositions
  • Methods of treatment using cadotril compositions

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0135] Concentrated racecadotril lipid composition: for use in liquid-filled gelatin capsules

[0136] Table 1: Compositions based on racecadotril lipids as percentage of compositions: Class 1 triglycerides

[0137]

[0138] 1: yes 35 USP / NF, EP, JP are commercially available from CRODA Healthcare

[0139] 2: yes 988 USP / NF, EP, JP commercially available from CREMER

[0140] 3: yes 810N (caprylic / capric triglyceride; 70:30 / C8:C10) USP / NF, EP, JP Commercially available from CREMER

[0141] Table 2: Compositions based on racecadotril lipids as a percentage of compositions: Class 2 triglycerides

[0142]

[0143] 1: yes 35 USP / NF, EP, JP Commercially available from CRODA Healthcare

[0144] 2: yes 988 USP / NF, EP, JP commercially available from CREMER

[0145] 3: yes 812N (caprylic / capric triglyceride; 60:40 / C8:C10) USP / NF, EP, JP Commercially available from CREMER

[0146] Using the materials in Table 1 and Table 2, the following mixing steps were tak...

Embodiment 2

[0196] Concentrated racecadotril lipid composition: for use in liquid-filled gelatin capsules

[0197] Table 4 :

[0198]

[0199] 1: Can IMWITOR USP / NF, EP, JP are commercially available from CREMER

[0200] 2: yes 810N (caprylic / capric triglyceride; 70:30 / C8:C10) USP / NF, EP, JP Commercially available from CREMER

[0201] 3: yes 812N (caprylic / capric triglyceride; 60:40 / C8:C10) USP / NF, EP, JP Commercially available from CREMER

[0202] table 5 :

[0203]

[0204] 1: Can IMWITOR USP / NF, EP, JP are commercially available from CREMER

[0205] 2: yes 810N (caprylic / capric triglyceride; 70:30 / C8:C10) USP / NF, EP, JP Commercially available from CREMER

[0206] 3: yes 812N (caprylic / capric triglyceride; 60:40 / C8:C10) USP / NF, EP, JP Commercially available from CREMER

[0207] testing method :

[0208] Sample preparation: (in acetonitrile)

[0209] 1. Pipette 1ml of racecadotril lipid solution into a 100ml volumetric flask (V.F.)

[0210] 2. Dilute t...

Embodiment 3

[0222] Racecadotril Lipid Composition: Droplet Size

[0223] process

[0224] Droplet size was measured by dynamic light scattering (DLS) at a scattering angle of 90 degrees on a Horiba SZ-100 nanoparticle size analyzer. The samples were kept in a temperature controlled room at 25°C during the measurement. Instrument performance was checked with a nominal 100 nm polystyrene latex (PSL) particle size standard in 10 mM NaCl solution immediately prior to the measurement. Count rates for these measurements range from 1 million to 3 million counts per second. Each measurement is performed for one minute. Data were analyzed using cumulative techniques.

[0225] Solubility and droplet size of lipid-based formulations

[0226] ** Formulation 1, Formulation 3, Formulation 5

[0227]

[0228] ** Formulation 2, Formulation 4, Formulation 6

[0229]

[0230] *Using Horiba SZ-100 nano particle size analyzer, measured by dynamic light scattering (DLS), the average value o...

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Abstract

Methods of treatment using cadotril compositions are disclosed.

Description

[0001] Cross References to Related Applications [0002] This patent application is a continuation-in-part of US Patent Application Serial No. 14 / 138,309; and claims the benefit of 14 / 138,309; 14 / 205,565; 13 / 929,996; 61,787,597; and 61 / 665,470, which are incorporated herein by reference. technical field [0003] The present invention relates to methods of treatment using cadotril compositions. Background technique [0004] The World Health Organization defines diarrhea or dysentery as a condition characterized by at least three loose or liquid bowel movements per day, or a greater volume than is normal for the individual 1 . The condition often lasts for several days and can lead to dehydration due to fluid loss. [0005] The most common cause of diarrhea is an intestinal infection caused by a virus, bacteria, or parasite, a condition called gastroenteritis. These infections usually originate from food or water contaminated with feces, or directly from another infected p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/265A61P1/12
CPCA61K9/107A61K9/1075A61K9/2009A61K9/2018A61K9/2031A61K9/2054A61K9/2059A61K9/2077A61K9/4858A61K9/4866A61K31/216A61K31/265A61K47/14A61K47/44A61P1/12
Inventor D-Y·李
Owner JOHNSON & JOHNSON CONSUMER COPANIES