Extended release pharmaceutical formulations of s-adenosylmethionine

A technology of delayed release and preparation, which is applied in the directions of drug combination, animal repellent, plant growth regulator, etc., can solve the problems such as the application of delayed release SAMe has not been reported, and the application of delayed release SAMe has not been reported yet.

Inactive Publication Date: 2010-03-24
METILEJSHN SAJENSIS INT SRL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the application of delayed-release SAMe has not been reported so far, nor has the application of delayed-release SAMe in the treatment of diseases been reported.

Method used

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  • Extended release pharmaceutical formulations of s-adenosylmethionine
  • Extended release pharmaceutical formulations of s-adenosylmethionine
  • Extended release pharmaceutical formulations of s-adenosylmethionine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0214] Example 1: Delayed release monolithic matrix tablet

[0215] A formulation containing SAMe, magnesium aluminosilicate, light liquid paraffin and magnesium stearate is prepared by mixing the ingredients and compressing with a semi-automatic tablet machine. During the entire manufacturing process, the humidity is kept below 30% and the temperature is kept at 20-25°C. Table 1-1 below lists the proportions of each component.

[0216] Table 1-1: SAMe formulations containing liquid paraffin

[0217] excipient

[0218] The formulations in Table 1-1 enable the manufacture of SAMe tablets with a total excipient content of less than 30%. The granules used in this formulation have good fluidity and no sticking picking during compression.

Embodiment 2

[0219] Example 2: Slugging method

[0220] To improve the compressibility of the SAMe formulation of Example 1, a granulation step (impact) was employed. SAMe was mixed with liquid paraffin and magnesium aluminosilicate. The resulting powdered mixture was loaded into a V-blender and mixed at 50 RPM for 10 minutes. Half the amount of magnesium stearate (see Table 2-1 below) 2.97 g was added to the V-blender and mixed for another 10 minutes.

[0221] The resulting powder was passed through a 20# sieve. The mixture was compressed into 400-500 mg of small pieces having a hardness of approximately 8-9 kp. The small pieces were then ground, passed through a 30# sieve, and blended with the rest of the magnesium stearate (2.97 g). The resulting mixture was then pressed to a hardness of 12-15 kp.

[0222] Table 2-1: Recipe for making SAMe cores with liquid paraffin

[0223] excipient

mg / tablet

% (wt)

Excipient mass of 110 tablets

SAMe

800

...

Embodiment 3

[0228] Embodiment 3: coating test

[0229] with different amounts of pore formers ( A combination of pore forming agent, sodium alginate and purified stearic acid) was coated with an ethylcellulose coating of matrix core SAMe tablets as described in Example 2 above. The ethylcellulose portion of the coating is a combination of purified water, Ethyocel 20cP standard premium ethylcellulose and 28% ammonium hydroxide. The coatings were tested at weight ratios of 100:0 (ethylcellulose:pore former), 80:20 and 70:30. Tablets were either uncoated or coated with a 2.5% 70:30 or 80:20 ethylcellulose composition. Dissolution was tested in pH 6.8 PBS buffer. The results are summarized in Table 3-1.

[0230] Table 3-1: Dissolution Results of Uncoated and Coated Tablets at pH 6.8

[0231] time (hours)

uncoated core

With ethylcellulose 70:30*,

2.5%** coated tablet

Ethyl cellulose

80:20*, 2.0%** coating

the tablet

2

...

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PUM

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Abstract

Extended release formulations of S-methyladenosylmethionine (SAMe) are provided, as are methods of treating various disorders using extended release SAMe formulations. The extended release formulations may be used to treat a variety of disorders, including liver disorders, psychiatric disorders and joint disorders. Thus, extended release SAMe formulations may be used to treat alcoholic liver disease, fatty liver disease, hepatitis, generalized anxiety disorder, obsessive compulsive disorder, post traumatic stress disorder, panic disorder, and depressive disorders such as depression (e.g. majorclinical depression) and dysthymia.

Description

[0001] Cross-references and priority claims to related applications [0002] This application claims priority to US Provisional Patent Application Serial No. 60 / 887,565, filed January 31, 2007, which is hereby incorporated by reference in its entirety. Background of the invention [0003] S-adenosyl-L-methionine ("SAMe") is a naturally occurring compound found throughout the tissues of the body. At the molecular level, SAMe is involved in various metabolic pathways including transmethylation, transsulfuration and aminopropylation (eg in the production of polyamines such as spermidine and spermine from putrescine). Thus, SAMe is involved in the biosynthesis of various hormones and neurotransmitters. Although SAMe is involved in metabolic processes throughout the body, the majority of SAMe is produced in the liver. [0004] [0005] S-adenosyl-L-methionine [0006] (SAMe) [0007] In vivo, SAMe is synthesized from the amino acid methionine and the nucleotide triphosphate ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N43/04A61K31/70
CPCA61K9/2013A61K9/2009A61K9/2095A61K9/2866A61K31/519A61K31/7076A61K31/714A61K9/286A61K31/70A61P1/14A61P1/16A61P19/02A61P25/00A61P25/04A61P25/24A61P25/30A61P25/32A61P25/36A61P29/00A61P3/04A61P43/00A61K2300/00
Inventor M·弗里德曼
Owner METILEJSHN SAJENSIS INT SRL
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