Formula comprising a hypolipidemic agent

Patent metadata

Field	Value
Publication number	US-2016136131-A1
Application number	US-201414899912-A
Country	US
Kind code	A1
Filing date	Jul 24, 2014
Priority date	Jul 25, 2013
Publication date	May 19, 2016
Grant date	—

Abstract

The present invention relates to the stable pharmaceutical composition of a suitable hypolipidemic agent. Preferably, the present invention discloses novel formulations of the compound of formula (I), or pharmaceutically acceptable salts of compounds of formula (I). More particularly the present invention relates to the stable pharmaceutical composition of compounds of formula (I) comprising compounds of formula (I) or its pharmaceutically acceptable salts, wherein the pH of the formulation is maintained above 7.

First claim

1 . A stable pharmaceutical composition of compounds of formula (I),

where ‘R’ is selected from hydroxy, hydroxyalkyl, acyl, alkoxy, alkylthio, thioalkyl, aryloxy, arylthio and M + represents suitable metal cations such as Na + , K + , Ca +2 , Mg +2 wherein the pH of the composition is maintained above 7 which comprises
i) suitable alkalinizers or suitable pH modifying agents which maintain the pH of the formulation above 7, and optionally
ii) a suitable stabilizer; and
iii) one or more other pharmaceutically acceptable excepients.

2 . The pharmaceutical composition as claimed in claim 1 wherein R is selected from alkylthio or thioalkyl and M + represents Mg +2 .

3 . The pharmaceutical composition as claimed in claim 1 wherein R is SCH 3 .

4 . The pharmaceutical composition as claimed in claim 1 wherein the alkalinizers or pH modifying agents is selected from attapulgite, bentonite, calcium carbonate, calcium phosphate, calcium sulphate, mono ethanolamine, tri ethanolamine, potassium bicarbonate, potassium citrate, potassium hydroxide, sodium benzoate, sodium hydroxide, sodium sulfite, sodium bicorbonate, sodium carbonate, Disodium hydrogen phosphate, mono basic potassium phosphate, Dicalcium phosphate, meglumine, light or heavy magnesium oxide.

5 . The pharmaceutical composition as claimed in claim 4 wherein the alkalinizers or pH modifying agent is Disodium hydrogen phosphate or magnesium oxide.

6 . The pharmaceutical composition as claimed in claim 1 wherein the stabilizers are selected from the classes of suitable antioxidants or chelating agents.

7 . The pharmaceutical composition as claimed in claim 6 , wherein the antioxidants are selected from citric acid, alpha tocopherol, sodium sulphite, sodium metabisulphite, butylated hydroxy anisole (BHA), BHT (2,6-di-tert-butyl-4-methylphenol), monothioglycerol, Vitamin C (ascorbic acid), propyl gallate or suitable combinations thereof.

8 . The pharmaceutical composition as claimed in claim 6 wherein the chelating agent is selected from Disodium EDTA, citric acid and or its salts, maleic acid, chlorambutol, chlorhexidine or its salts, chlorocresol or their suitable combinations.

9 . The pharmaceutical composition as claimed in claim 1 where in the other pharmaceutical excepients are selected from suitable diluents, fillers, disintegrants, binder, lubricants, glidants, wetting agents and solvent(s).

10 . The pharmaceutical composition as claimed in claim 9 wherein the binder is selected from acacia alginic acid, tragacanth, carboxymethylcellulose sodium, poly(vinylpyrrolidone), compressible sugar (e.g., NuTab), ethyl cellulose, gelatin, liquid glucose, methyl cellulose, povidone and pregelatinized starch or suitable combinations thereof.

11 . The pharmaceutical composition as claimed in claim 9 wherein the diluent or filler is selected from dibasic calcium phosphate, kaolin, sucrose, mannitol, microcrystalline cellulose, powdered cellulose, precipitated calcium carbonate, sorbitol, starch or suitable combinations thereof.

12 . The pharmaceutical composition as claimed in claim 9 wherein the lubricant is selected from calcium stearate, magnesium stearate, mineral oil, stearic acid, zinc stearate or suitable combinations thereof.

13 . The pharmaceutical composition as claimed in claim 9 wherein the disintegrant is selected from corn starch, potato starch, pre-gelatinized and modified starched thereof, sweeteners, clays, microcrystalline cellulose (e.g. Avicel™), carsium (e.g. Amberlite™), alginates, sodium starch glycolate, gums selected from agar, guar, locust bean, karaya, pectin, tragacanth or combinations thereof.

14 . The pharmaceutical composition as claimed in claim 9 wherein glidants is selected from colloidal silica, calcium silicate, magnesium silicate, silicon hydrogel, cornstarch, talc or suitable combinations thereof.

15 . The pharmaceutical composition as claimed in claim 1 is in the form of a tablet or a caplet or a capsule or a powder or a suspension in a liquid or an aerosol formulation or solutions, preferably in the form of a tablet or capsule.

16 . The pharmaceutical composition as claimed in claim 1 prepared by direct compression, wet granulation or dry granulation.

17 . The pharmaceutical composition as claimed in claim 16 wherein the formulation is prepared by direct compression comprising mixing the drug with all the pharmaceutical excepients required and then either compressing into tablets or filled in capsules.

Assignees

• Cadila Healthcare Ltd

Inventors

• Patel Jitendre D
• Davadra Prakash
• Patel Snehal
• Sheikh Shafiq

Classifications

• A61P3/06

  Antihyperlipidemics · CPC title

• A61K9/2009

  Inorganic compounds · CPC title

• A61K31/40 Primary

  having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil · CPC title

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title