U.S. patent application number 13/893626 was filed with the patent office on 2013-09-19 for gel containing pirfenidone.
This patent application is currently assigned to CELL THERAPY AND TECHNOLOGY, S.A. DE C.V.. The applicant listed for this patent is CELL THERAPY AND TECHNOLOGY, S.A. DE C.V.. Invention is credited to Juan Socorro ARMEND RIZ BORUNDA, Jose Agustin Rogelio MAGANA CASTRO, Laura V ZQUEZ CERVANTES.
Application Number | 20130245073 13/893626 |
Document ID | / |
Family ID | 40350871 |
Filed Date | 2013-09-19 |
United States Patent
Application |
20130245073 |
Kind Code |
A1 |
MAGANA CASTRO; Jose Agustin Rogelio
; et al. |
September 19, 2013 |
GEL CONTAINING PIRFENIDONE
Abstract
The invention relates to a gel composition containing
pirfenidone, which is advantageous over other cutaneously
administered pharmaceutical forms known in the prior art and which
can be used in treatment for the restoration of tissues with
fibrotic lesions and for the prevention of fibrotic lesions.
Inventors: |
MAGANA CASTRO; Jose Agustin
Rogelio; (Mexico, MX) ; V ZQUEZ CERVANTES; Laura;
(Mexico, MX) ; ARMEND RIZ BORUNDA; Juan Socorro;
(Mexico, MX) |
|
Applicant: |
Name |
City |
State |
Country |
Type |
CELL THERAPY AND TECHNOLOGY, S.A. DE C.V. |
Mexico |
|
MX |
|
|
Assignee: |
CELL THERAPY AND TECHNOLOGY, S.A.
DE C.V.
Mexico
MX
|
Family ID: |
40350871 |
Appl. No.: |
13/893626 |
Filed: |
May 14, 2013 |
Related U.S. Patent Documents
|
|
|
|
|
|
Application
Number |
Filing Date |
Patent Number |
|
|
12673304 |
Apr 28, 2010 |
8492412 |
|
|
PCT/MX2008/000107 |
Aug 14, 2008 |
|
|
|
13893626 |
|
|
|
|
Current U.S.
Class: |
514/345 |
Current CPC
Class: |
A61K 9/06 20130101; A61P
11/00 20180101; A61P 29/00 20180101; A61K 47/22 20130101; A61K
47/32 20130101; A61K 31/4418 20130101; A61K 9/0014 20130101; A61K
47/02 20130101; A61K 47/18 20130101; A61P 17/00 20180101 |
Class at
Publication: |
514/345 |
International
Class: |
A61K 31/4418 20060101
A61K031/4418; A61K 9/06 20060101 A61K009/06 |
Foreign Application Data
Date |
Code |
Application Number |
Aug 14, 2007 |
MX |
MX/A/2007/009796 |
Claims
1. A method of making a composition of a Pirfenidone gel,
comprising the following steps: a) mixing 50% of the total water to
be used with a viscous agent and allowing complete humectation of
the viscous agent; b) mixing Pirfenidone and a solubilizer agent
separately and with constant agitation; c) dissolving separately a
non ionic solubilizer agent in 25% of total water at 40.degree. C.
and once dissolved, adding 15% of total water; d) adding the
solution from part c) to the mix from part b), and agitating until
homogenous; e) diluting a neutralizer agent in 10% of total water
to be used, and agitating until homogenous; and f) combining the
solutions of subparts (a)-(e).
2. A method for treating fibrotic lesions in a patient by
administering to the patient a composition of Pirfenidone gel
consisting of 8% Pirfenidone, 0.5% of a viscous agent, 20% of a
solubilizer, 11.5% of a non ionic solubilizer, 0.5% of a conserving
agent, 0.5% of a neutralizer agent and 59% of purified water,
thereby treating the fibrotic lesions.
3. The method of claim 2, wherein (a) the viscous agent is selected
from the group consisting of a Carbomer 940 (MR), Carbomer
Homopolymer Type A, a cellulose derivative, a gum, and a poloxamer;
(b) the solubilizer is selected from the group consisting of
N-methylpyrrolidone, ethyl alcohol, and propylene glycol; (c) the
conserving agent is selected from the group consisting of
diazolidinyl urea, iodopropynyl butylcarbamate, methylparaben,
propylparaben, and mixes of these conserving agents; and (d) the
neutralizer agent is selected from the group consisting of primary,
secondary and tertiary mono-, bi-, and triethanolamine aliphatic
amines, and a hydroxide alkaline metal.
4. The method of claim 3, wherein the viscous agent is Carbomer 940
(MR), the solubilizer is N-methylpyrrolidone, the conserving agent
is diazolidinyl urea, and the neutralizer agent is
triethanolamine.
5. The method of claim 3, wherein the viscous agent is Carbomer 940
(MR), the solubilizer is N-methylpyrrolidone, the conserving agent
is iodopropynyl butylcarbamate, and the neutralizer agent is
triethanolamine.
6. The method of claim 3, wherein the hydroxide alkaline metal is
sodium hydroxide.
Description
RELATED APPLICATIONS
[0001] This application is a divisional application of U.S. patent
application Ser. No. 12/673,304, filed on Apr. 28, 2010, which
claims the benefit of and which is a national stage filing of
International Application Serial No. PCT/MX2008/000107, filed on
Aug. 14, 2008, which claims priority to, and the benefit of,
Mexican Patent Application Serial No. MX/a/2007/009796, filed on
Aug. 14, 2007, the entire contents of both of which are hereby
incorporated by reference.
FIELD OF INVENTION
[0002] The present invention is related to a gel formula that
contains Pirfenidone, which offers advantages over other
pharmaceutical forms of known cutaneous administration in the state
of the technique.
BACKGROUND OF THE INVENTION
[0003] The 5-methyl-1-phenyl-2(1H)-pyridone, formula;
##STR00001##
It is a drug that has been applied in the restoration of tissues
with lesions with fibrosis and the prevention of fibrotic lesions.
This compound, Pirfenidone, it is by itself a known compound and
its pharmacological effects has been described, for example, in
Japanese applications numbers 87677/1974 and 1284338/1976, as an
anti-inflammatory agent that includes antipyretic and analgesics.
The U.S. Pat. No. 3,839,346, published Oct. 1 of 1974; the U.S.
Pat. No. 3,974,281, published Aug. 10 of 1976; the U.S. Pat. No.
4,042,699 published August 16 of 1977, and the U.S. Pat. No.
4,052,509 published Oct. 4 of 1977, which described the methods for
the obtained Pirfenidone, as well as its use as an
anti-inflammatory agent. In the Mexican patent 182,266 the
antifibrotic activity of the 5-methyl-1-phenyl-2(1H)-pyridone is
described.
[0004] Different resources and treatments have been used to the
date and none of them have shown to be really effective.
Pirfenidone has shown its efficacy as an anti-fibrotic agent in
different pathologies and organs, and has been demonstrated in
previous works, where we have observed an effect on the fibroblasts
and the production of collagen and extracellular matrix, as well as
in experimental models and in clinical tests also.
[0005] Many substances could form gels when a gelificant agent is
added. This is use in many diverse products in the manufacturing
industry, from food to paint, passing through adhesives.
[0006] Gels are also important in the chemistry part related with
the processes SOL_GEL and in the synthesis of solid materials with
nanopores.
[0007] Gels are classified in: aqueous (hydrogels) or organic
(organogels), depending if the aqueous component is water or an
organic solvent; organic or inorganic in nature, colloidal or thick
grain, according to the size of the particles; and rigid gels,
elastic or tixothrophic, according to its mechanic properties.
[0008] The hydrocolloids are substances that are produced from
vegetable and animal proteins or multiple sugars. They have the
capacity to swell themselves and to bind to water. The
hydrocolloids are used to thicken, solidify and stabilize food.
OBJECT OF THE INVENTION
[0009] The object of the present invention is to provide a gel
composition for its cutaneous administration that contains
Pirfenidone, a viscous agent; a solubilizer; a non ionic
solubilizer; a conserving agent; a neutralizer agent and purified
water. [0010] Also, it is the object of the present invention to
provide a process of manufacture of a gel that contains pirfenidone
for its cutaneous application. [0011] Another objective of the
present invention is to provide a gel medicine to be used as an
anti-fibrotic and anti-inflammatory agent.
SPECIFICATION OF THE INVENTION
Composition of the Gel
[0012] The composition of the gel contains from 2 to 12% of
Pirfenidone is elaborated utilizing from 0.4 to 1.2% of a viscous
agent, from 10 to 30% of a solubilizer, from 5 to 15% of a non
ionic solubilizer, from 0.2 to 1% of a conserving agent, from 0.4
to 1.2% a neutralizer agent and the rest of purify water. The
viscous agent is selected from a carbomer 940 (MR); Ultrex 10(MR),
cellulose derivatives; gums; polioxameres; ethylic alcohol and
propylenglycol; the conserving agent is selected from a group that
consist of Diazolidinyl urea, iodopropinil-butilcarbamate;
methylparabene and a mix of these compounds; the neutralizer agent
is selected from a group of primary, secondary and tertiary
aliphatic amines of the mono- , bi- and triethanolamine type, and
of the hydroxide alkaline metals, such as sodium hydroxide.
An example of the composition of the gel is shown in the table
1:
TABLE-US-00001 Component Quantity (g) % Pirfenidone 8 8 Viscous
agent 0.5 0.5 Solubilizer 20 20 Non ionic solubilizer 11.5 11.5
Conserving agent 0.5 0.5 Neutralizer 0.5 0.5 Purified water up to
100 59
[0013] The gel containing Pirfenidone is manufactured as follows:
[0014] a) Mix 50% of the total water to be used with the viscous
agent, allowing the complete humectation of the viscous agent;
[0015] b) Mix separately and with constant agitation the
Pirfenidone with the solubilizer agent; [0016] c) Dissolve
separately the non ionic solubilizer agent in the 25% water to be
used at 40.degree. C., once dissolved, the 15% of the total water
is added; [0017] d) Add the solution from part c) to the mix from
part b), agitate until the mix is homogenate. [0018] e) Dilute the
neutralizer agent in 10% of the total water to use, agitate until
the mix is homogenate; and [0019] f) Add with constant agitation
and homogenate in each addition to the mix from part a) the
solution from part d); the conservative and the solution from part
e).
[0020] A prepared composition according to procedure describe is
shown in table 2.
TABLE-US-00002 Component Quantity (g) Pirfenidone 8 Carbomer 0.5
N-methylpirrolidone 20 Macrogolglycerol 11.5 Hidroxiestearate 40
Diazolidinilurea and 0.5 Iodopropinil-butilcarbamate
Triethanoalamine 0.5 Purified water up to 100
[0021] These compositions are shown in an example mode, but they
are not limited in any level of the reach of the description of the
present invention.
* * * * *