Oral liquid compositions containing paroxetine resinate

Details Oral liquid compositions containing paroxetine resinate Oral liquid compositions containing paroxetine resinate

1996-08-01

1998-09-22

MacMillan, Keith

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

424267, A61K 918

Patent

active

058114360

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/EP95/00319, filed Jan. 30, 1995, which claims priority to GB 9402029.4 filed Feb. 3, 1994.
The present invention relates to novel formulations and to the use of such a formulation in the treatment and/or prevention of certain disorders.
U.S. Pat. No. 4,007,196 describes certain compounds which possess anti-depressant activity. One specific compound mentioned in this patent is known as paroxetine and which has the following formula: ##STR1##
This compound has been approved for human use and is being sold in many countries around the world as an anti-depressant agent
All paroxetine sold to date has been in the form of oral swallow tablets.
Many physicians have expressed a desire to be able to prescribe an oral liquid containing paroxetine and some have even made their own oral liquid by crushing conventional swallow tablets and mixing them with water. There are however, a number of draw-backs to this oral liquid, firstly paroxetine has a very bitter taste which is highly noticeable when administered as an oral liquid, secondly such oral liquids have poor stability qualities and have a shelf-life of only a few days.
WO 91/13612 relates to the sustained release of pharmaceuticals using compositions in which the drug is completed with an ion-exchange resin. The specific ion-exchange resin described in this published patent application is AMBERLITE IRP 69, a sodium polystyrene sulphonate resin.
When AMBERLITE IRP-69 is used to complex with paroxetine it was found that whilst the taste was effectively masked the composition had an unacceptably low bioavailability when compared to a swallow tablet.
It has now been found that AMBERLITE IRP 88, an acrilin potassium resin can be used to form a stable taste masted complex with paroxetine and which complex has acceptable bioavailability when compared to the conventional swallow tablet.
Accordingly, the present invention provides an oral liquid pharmaceutical composition comprising a paroxetine-AMBERLITE IRP-88 complex.
AMBERLITE IRP-88 is commercially available from Rohm & Haas in a pharmaceutically acceptable grade.
The oral liquid pharmaceutical composition is prepared in conventional manner such as by mixing paroxetine and AMBERLITE IRP-88 together in an aqueous medium. Suitably the IRP-88 and paroxetine are present in a ratio of 1:1 to 2:1. It should be appreciated that superior taste masking properties are obtained with a 2:1 ratio.
Other pharmaceutically acceptable excipients may also be added such as thickeners such as Keltrol and/or Avicel (in particular Avicel CL 611); dispersants such as propylene glycol; moisture retaining agents such as glycerol; sweetners such as sorbitol and sodium saccharin buffering agents such as citric acid and sodium citrate; preservatives such as sodium benzoate and mixtures of methyl and and propyl parabens (parahydroxybenzoates), artificial colours such as F D and C Yellow No. 6 Sunset Yellow; flavouring such as Givaudan Natural Orange and/or Lemon; and antifoaming agents such as silicone anti-foam.
Preferably the amounts of buffering agents are controlled to give a pH of 4 to 6. Most preferably a pH of 4.5 to 6.0.
The amount of paroxetine used is adjusted such that in a single unit dose there is a therapeutically effective amount of paroxetine. Preferably the unit dose contains from 10 to 100 mg paroxetine (as measured in terms of the free base). More preferable the amount of paroxetine in a unit dose is 10 mg, 20 mg, 30 mg, 40 mg or 50 mg. The most preferred amount of paroxetine in a unit dose is 20 mg of paroxetine.
Preferably the volume of liquid in a unit dose is in the range 5 to 20 ml most preferably 10 ml.
Preferably paroxetine used in the formulation is in the form of the hydrocholide hemi-hydrate which may be prepared according to the procedures outlined in U.S. Pat. No. 4,721,723.
Suitable procedures for preparing paroxetine include those mentioned in U.S. Pat. Nos. 4,009,196, 4,902,801, 4,861,893 and 5,039,803 and PCT/GB 93/00721.
It has been mentioned that paroxetine has particular uti

REFERENCES:
patent: 4007196 (1977-02-01), Christensen et al.
patent: 5476654 (1995-12-01), Conte et al.

Affiliated with

Also associated with

Rating

Oral liquid compositions containing paroxetine resinate does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Oral liquid compositions containing paroxetine resinate, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Oral liquid compositions containing paroxetine resinate will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-1622053