BE902226R - Analgesic and antiinflammatory ointments - contg. indomethacine and neutralised with ammonia - Google Patents

Abstract

Ointment comprises (a) an effective quantity of indomethacine; (b) a medium comprising 15-85% hydroxyl cpd., 30-55% water and a gelling agent that is a cellulosic cpd. or a carboxyvinyl polymer neutralised with ammonia or an amine (c) 0.5-5% of an adjuvant that is an ester formed from 1-5C alcohol and a 4-14C monocarboxylic, acid, or a diester formed from a 1-3C alcohol and a 4-10C dicarboxylic acid, and (d) water. The pH of the mixt. is slightly acid to slightly basic, pref. pH 4.8-7.5. - This is an addn. to BE868348 which describes neutralisation of the mixture used in (b) only with an amine.

Description

       

  "Analgesic and anti-inflammatory gelled ointment" The main patent describes and puts under protection an analgesic and anti-inflammatory ointment comprising indomethacin, a medium consisting of a glycol, an alcohol and water, a chosen gelling agent

  
 <EMI ID = 1.1>

  
was neutralized with an amine, and enough water to balance.

  
Analgesic and anti-inflammatory gel ointment conforming to the main patent can be produced

  
(1) by swelling a gelling agent in water (2), by dissolving indomethacin and an adjuvant in a mixture of a glycol and an alcohol and

  
(3) by adding (2) to (1), then adding an amine to the resulting mixture to form the desired gelled ointment.

  
The present improvement is based on the discovery that equivalent results are obtained when ammonia is added instead of an amine to the above mixture obtained by the addition of (2) to (1).

  
The present improvement therefore relates to an anti-inflammatory and analgesic ointment comprising
(a) an anti-inflammatory and analgesic amount of indomethacin (b) a medium consisting of a hydroxylated compound at a rate of 15 to 85% by weight, of water at a rate <EMI ID = 2.1>

  
sufficient to gel the ointment, this gelling agent being chosen from cellulosic compounds and carboxyvinyl polymers which have been neutralized with ammonia (ammonia in aqueous solution) or an amine; (c) an adjuvant at a rate of

  
0.5 to 5% by weight, chosen from esters of Ci - Cs alcohols of C4 - C14 monocarboxylic acids and diesters of Ci - C3 alcohols of dicarboxylic acids

  
This*. - Cloet (d) water in sufficient quantity to constitute the rest of the ointment whose pH is from an acid level to slightly basic, enough to dissolve the indomethacin in the composition without however being too basic not to cause the breakdown of indomethacin.

  
The details of the invention are in substance as described in the main patent.

  
The final pH of the ointment should be 4.8 to 7.5, preferably 6.2 to 7.2. A pH below 4.8 causes indomethacin to crystallize during the preparation of the ointment. A pH higher than 7.5 causes the breakdown of indomethacin and therefore gives rise to harmful instability in the human body.

  
The following examples are given to illustrate the invention in addition to those given in the main patent.

  
The percentages given in this specification are by weight unless otherwise noted

Example I

  

 <EMI ID = 3.1>


  
A. Dissolve 2) in 3) and 4)

  
B. Disperse 1) in A)

  
C. Add 6) to B) and swell the mixture thus obtained D. Add 5) to C) and stir the composition until

  
what it becomes homogeneous.

CLAIMS

  
1. An anti-inflammatory analgesic ointment comprising (a) an anti-inflammatory and analgesic amount of indomethacin; (b) a medium consisting of a hydroxylated compound in an amount of 15 to 85% by weight,

  
of water at a rate of 30 to 55% by weight and of a gelling agent in an amount sufficient to gelling the ointment, this gelling agent being chosen from cellulose compounds and carboxyvinyl polymers which have been neutralized by ammonia or a amine; (c) an adjuvant in an amount of 0.5 to 5% by weight,

  
 <EMI ID = 4.1>

  
sufficient amount to constitute the rest of the ointment whose pH is from an acid level to slightly basic, enough to dissolve the indomethacin in the composition without being too basic, so as not to cause the decomposition of the indomethacin.

  
2. Anti-inflammatory analgesic ointment


    

Claims (1)

before the claim, characterized in that its pH is 4.8 to 7.5. 3. Ointment according to any one of claims 1 and 2, characterized in that its pH is 5.5 to 7.5. 4. Ointment according to any one of claims 1 to 3, characterized in that the hydroxylated compound is chosen from propylene glycol, butylene glycol, polyethylene glycol, ethanol and isopropanol. 5. Qnguent according to any one of claims 1 to 4, characterized in that the cellulosic compound is chosen from hydroxyethylcellulo- se, methylcellulose, carboxymethylcellulose, <EMI ID = 5.1> lulosë. 6. Ointment according to any one of claims 1 to 5, characterized in that indomethacin is present in an amount of 0.5 to 1.5% by weight. Example II  <EMI ID = 6.1> A) Dissolve 1) in 2) B) Swell 3) in 40 g of 5) C) add B) to A). Add the rest of 5) and 4) to C) and stir the composition until it becomes homogeneous. Of course, the invention is not limited to the details described in this specification.