Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1996-12-19
2000-04-18
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424465, 424474, 424475, 424480, 514770, 5147723, 514778, 514781, A61K 930, A61K 932, A61K 936
Patent
active
060512555
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to medicaments for oral administration in the treatment of bacterial infections, comprising amoxycillin and salts of clavulanic acid.
Amoxycillin and its derivatives, e.g. amoxycillin trihydrate, are known (e.g. GB 1241844) as antibacterial agents useful in the treatment of gram-negative and gram-positive bacterial infections. Clavulanic acid and its derivatives, e.g. its salts such as potassium clavulanate, are known (e.g. GB 1508977) as .beta.-lactamase inhibitors which inhibit the activity of .beta.-lactamase enzymes produced by bacteria and which confer antibiotic resistance by destroying .beta.-lactam antibiotics such as amoxycillin. The terms "amoxycillin" and "clavulanate" used herein unless otherwise specified include both the free parent acids and derivatives such as salts thereof. The use of clavulanate in combination with amoxycillin consequently enhances the effectiveness of amoxycillin.
The use of potassium clavulanate in combination with amoxycillin trihydrate within the ratios amoxycillin:clavulanic acid 1:1 to 6:1, (expressed in terms of the weight of parent compound amoxycillin or clavulanic acid, this terminology being used throughout this description unless otherwise stated) is described in GB 2005538. Potassium clavulanate is an exceptionally difficult material to formulate, being extremely hygroscopic and moisture sensitive. Degradation readily occurs in the presence of water and aqueous media.
Known formulations of amoxycillin and clavulanate are provided for administration three times daily (i.e. "tid" dosing). It is desirable for inter alia patient convenience and compliance that such formulations be provided for administration twice daily (i.e. "bid" dosing). It is also highly desirable that such formulations should have a consistent bioavailability of the active ingredients clavulanate and amoxycillin.
An amoxycillin/clavulanate formulation has been produced which enables bid dosage, and also has the unexpected benefit of a particularly consistent bioavailability, particularly of clavulanate. In some instances the formulation may also show a increased bioavailability.
Accordingly the present invention provides a tablet formulation, being a medicament for oral administration for the treatment of bacterial infections, the tablet comprising a compacted mixture of 750-950 mg of amoxycillin and a quantity of clavulanate, in a weight ratio amoxycillin:clavulanate between 6:1 to 8:1 inclusive, and having a film coating of polymers which can be applied by aqueous film coating techniques.
Suitable derivatives of amoxycillin are amoxycillin trihydrate, anhydrous amoxycillin and alkali metal salts of amoxycillin such as sodium amoxycillin. Suitable derivatives of clavulanic acid are alkali metal salts of clavulanic acid such as potassium clavulanate. It is preferred to use amoxycillin trihydrate and potassium clavulanate in combination in a tablet formulation of this invention containing the two, this combination having met with regulatory approval, and being particularly advantageous.
Suitably the tablet contains nominally 875 mg of amoxycillin .+-.10% and 125 mg of clavulanate .+-.10%, i.e. in a ratio amoxycillin:clavulanate of nominally 7:1. The tablet of the invention may suitably contain 50 wt. % or more, for example around 65-75 wt. % of the combination of amoxycillin and clavulanate, e.g. typically 70 wt. % +2 wt %.
The tablet formulation of this invention may be provided for treatment of bacterial infections generally, for example one or more of inter alia upper respiratory tract infections, lower respiratory tract infections, genito-urinary tract infections and skin and soft tissue infections. The tablet formulation of this invention is generally suitable for treatment of infections by microorganisms which are susceptible to .beta.-lactam antibiotics, and may also have efficacy for some penicillin-resistant microorganisms.
The tablet formulation of the invention may include one or more other additional excipients etc. generally conventional to the dosag
REFERENCES:
patent: 4232005 (1980-11-01), Howarth
patent: 4441609 (1984-04-01), Crowley
patent: 4537887 (1985-08-01), Rooke et al.
Repertoria Farmaceutico Italiano (1989) pp. A105-A108 and English Translation.
Pharmaceutical Dosage Forms, vol. 3, (1990), pp. 93-97.
Drug Development and Industrial Pharmacy, 3(3), 227-240 (1977).
Repertoria Farmaceutico Italiano(1992) pp. A-75.
Repertoria Farmaceutico Italiano (1993) pp. A79-80.
Repertoria Farmaceutico Italiano (1994) pp. A72.
Conley Creighton Pierce
Davidson Nigel Philip McCreath
Rivett Ernest Lionel Gilbert
Yeates Kenneth Trevor
Dinner Dara L.
Kinzig Charles M.
SmithKline Beecham Plc
Spear James M.
Venetianer Stephen
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