Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ketone doai
Patent
1993-02-22
1996-07-23
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ketone doai
A61K 3112
Patent
active
055390005
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/GB93/00145 filed Jan. 22, 1993.
BACKGROUND OF THE INVENTION
The present invention relates to spray-chilled nabumetone and a process for its manufacture.
GB 1,474,377 describes a non-steroidal anti-inflammatory drug 4-(6-methoxy-2-naphthyl)-butan-2-one which is Commonly known as nabumetone. This patent also describes a process for the manufacture of nabumetone.
Nabumetone is most commonly prescribed as 500 mg or 1000 mg swallow tablets. The resulting tablets containing nabumetone and conventional excipients are fairly large in size and can be a problem to swallow for some patients.
Conventionally isolated and milled nabumetone has a poured density range of 0.35 to 0.39 gcm.sup.-3 and a tapped density range of 0.44 to 0.48 gcm.sup.-3 and when mixed with conventional excipients produces a tablet volume of 0.485 cm.sup.3 for a 500 mg nabumetone tablet and a volume of 0.970 cm.sup.3 for a 1000 mg nabumetone tablet.
Conventionally isolated and milled nabumetone is formulated into conventional swallow tablets by admixing with conventional fillers, surfactants and disintegrants. It has been found that the maximum amount of drug that can be mixed with excipients, especially fillers, is 82%. Increasing the percentage of drug further (i.e. reducing the percentage of excipients, especially fillers) causes the tablet to be prone to breaking up on manufacture, storage and transportation, which is obviously a disadvantage.
Spray-chilling is a technique that has been in existence for approximately 30 years, and has been applied to the production of food-stuffs such as coffee as well as pharmaceuticals.
Spray-chilling is usually chosen because it is a process which produces uniform product qualifies such as particle size, moisture content and bulk density.
In pharmaceutical production, spray-chilling is used because it can provide products which have improved flow characteristics.
SUMMARY OF THE INVENTION
It has now been found that spray chilled nabumetone has excellent formulation properties, is cheaper to produce and can be surprisingly formulated into viable tablets using fewer excipients than were previously needed. Furthermore, spray-chilled nabumetone has the unexpected advantage of being more dense than conventionally isolated and milled nabumetone and can therefore be formulated into smaller tablets which are easier to swallow.
DESCRIPTION OF THE PREFERRED EMBODIMENTS
Accordingly, the present invention provides spray-chilled nabumetone.
The present invention further provides spray-chilled nabumetone having a poured density range of 0.40 to 0.65 gcm.sup.-3.
In particular, the poured density range of spray-chilled nabumetone is suitably between 0.45 and 0.60 gcm.sup.-3 or more preferably 0.5 to 0.55 gcm.sup.-3 Most preferably the poured density of spray-chilled nabumetone is about 0.5 gcm.sup.-3.
The present invention also provides spray-chilled nabumetone having a tapped density range of 0.50 to 0.65 gcm.sup.-3.
In particular, the tapped density range of spray-chilled nabumetone is suitably between 0.54 to 0.62 gcm.sup.-3 or more preferably between 0.58 to 0.62 gcm.sup.-3. Most preferably the tapped density of spray-chilled nabumetone is about 0.60 gcm.sup.-3.
The present invention also provides a pharmaceutical composition containing spray-chilled nabumetone admixed with a pharmaceutically acceptable carrier.
It should be appreciated that the term excipient hereinafter used means a pharmaceutically acceptable carrier.
Another aspect of the present invention provides spray-chilled nabumetone in unit dose form. Suitable unit dose forms include tablets, sachets, suspensions and suppositories containing nabumetone, which are formed using conventional techniques known in the art of formulation science.
The invention yet further provides a swallow tablet containing 500 mg of spray-chilled nabumetone admixed with conventional excipients which tablet has a volume of 0.429 cm.sup.3. Thus, the present invention provides swallow tablets containing 500 mg of spray-chilled nabumetone ha
REFERENCES:
patent: 4086346 (1978-04-01), Bocker et al.
patent: 4420639 (1983-12-01), Lake et al.
Chemical Abstracts, vol. 108, No. 12, 21 Mar. 1988, Columbus, Ohio, US; abstract No. 101197y, E. A. Daigneault et al. 'bioeqiuvalence study of nabumetone: tablet versus suspension' p. 436; column 2; see abstract & Am. J. Med. 1987, 83(4B).
Cintins Marianne M.
Lentz Edward T.
MacMillan Keith
SmithKline Beecham p.l.c.
Venetianer Stephen
LandOfFree
Spray-chilled nabumetone does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Spray-chilled nabumetone, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Spray-chilled nabumetone will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-713411