PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL COMPOSITION CONTAINING PIRFENIDONE IN SUSTAINED-RELEASE TABLET FORM AND ITS APPLICATION IN THE REGRESSION OF HUMAN CHRONIC RENAL FAILURE, BREAST CAPSULAR CONTRACTURE AND HEPATIC FIBROSIS

摘要

The instant invention relates to a process for the preparation of a pharmaceutical composition in sustained-release tablet form comprising from 600 milligrams to 2400 milligrams of Pirfenidone (PFD), in such a way that the drug is bioavailable during an extended period of time of 12 hours from its administration. In this way, the anti-fibrotic and anti-inflammatory action of the drug Pirfenidone is optimized. Moreover, the instant invention offers advantages and a higher therapeutic efficacy compared to other pharmaceutical forms of Pirfenidone for oral administration and its therapeutic application in the regression of chronic renal failure secondary to primary glomerulosclerosis; it shows a better activity with regard to the reduction and/or regression of deleterious effects in breast capsular contracture observed after the surgical implantation of breast implants in humans and has an important anti-TNF-α and anti-TGF-β1 action for the treatment of hepatic fibrosis.

主权项

1. A process for preparing a composition in sustained-release tablet form comprising 600 mg of Pirfenidone, wherein said process comprises the following steps:
A) screening Pirfenidone and silicium dioxide through a mesh 30 screen in an oscillating granulator and mixing the screened Pirfenidone and silicium dioxide in a ribbon blender for 5 minutes; B) screening microcrystalline cellulose, low viscosity hydroxypropylmethylcellulose (HPMC) and high viscosity hydroxypropylmethylcellulose (HPMC) through a mesh 30 screen in the oscillating granulator and mixing the screened low viscosity HPMC and high viscosity HPMC the ribbon blender for 15 minutes; C) screening sodium stearyl fumarate through a mesh 30 screen in the oscillating granulator and mixing the screened sodium stearyl fumarate in the ribbon blender for 3 minutes; and D) forming a tablet in a Stokes tablet machine, wherein the Stokes tablet machine is equipped with elongated punches having the following compression parameters: average weight: 850 mg+5%; hardness: maximum 10 kgF; and brittleness: lower than 1%.