Pharmaceutical composition with anaesthetic effect

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ether doai

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Details

514626, 514772, 514817, 514818, 514900, A61K 906

Patent

active

060310073

DESCRIPTION:

BRIEF SUMMARY
THE FIELD OF THE INVENTION

The present invention is directed to a new pharmaceutical composition and its use in therapy, particularly as an anaesthetic for use on mucous membranes and particularly within the oral cavity.


BACKGROUND AND PRIOR ART

It is estimated that approximately 10-13% of the population suffers from periodontal diseases with pathological periodontal pockets. In order to eliminate or control the disease and arrest further periodontal tissue destruction, periodontal pockets need repeated subgingival mechanical debridement/cleansing. The number of periodontal pockets in a patient may vary as can the pocket depth measurement. Approximately 40% of all periodontal scaling procedures performed involve some kind of anaesthesia.
Accumulation of bacterial plaque on teeth and in the gingival sulcus elicits an inflammatory response in the marginal gingiva which may spread in an apical direction and result in loss of tooth support with the formation of periodontal pockets. The object of mechanical debridement of periodontal pockets is to control and arrest further destruction of tooth support by removal of plaque and calculus from within the pockets.
The majority of the scaling procedures are performed by hygienists. The main use of anaesthesia techniques used in conjunction with periodontal scaling is either a nerve block or infiltration. Infiltration anaesthesia is either carried out alone or in combination with topical anaesthesia, mainly jelly, ointment or spray. However, the problem with existing topical products are lack of efficacy due to inadequate depth of penetration, too short duration and difficulties in administration due to spread, taste etc. EP 244 118 discloses a controlled release drug delivery system for placement in the periodontal pocket, having a plurality of discrete microparticles consisting of a rate-controlling polymer matrix having a drug dispersed therein, said microparticles being in the range of 10-500 .mu.m. EP 241 178 also discloses a controlled release drug delivery system for placement in the periodontal pocket, which composition comprises solid particles having an average size of 1-500 .mu.m. However, the drug delivery systems disclosed in both these prior art patents are deviced for administration of a medicament for a longer period of time. Thus the drug delivery systems of EP 244 118 and EP 241 178 are not suitable for use in pain management in conjunction with minor surgical procedures, where a fast onset of action and relatively short duration is required.
Thus, the problem underlying the present invention is to provide a pharmaceutical composition which would provide effective pain relief in conjunction with periodontal scaling and root planing following local administration. In other words, the object of the invention is to provide a local anaesthetic that can be applied in a facile manner in the oral cavity, and more precisely within periodontal pockets. A further object of the invention is to provide a pharmaceutical composition having a short onset time and an adequate duration for the intended procedure, with no inconvenient anaesthesia.


OUTLINE OF THE INVENTION

The problem identified above has now been solved by providing a new pharmaceutical composition which preferably is in form of an emulsion, more preferably in form of a microemulsion, comprising the following ingredients: produce a homogenous formulation; and composition.
The local anaesthetic in the final composition is one or more local anaesthetics in oil form as such, or a eutectic mixture formed by two or more local anaesthetics. The amount of the local anaesthetic in the oil phase depends on the pH-value of the formulation.
In a particularly preferred embodiment of the invention the local anaesthetic is a eutectic mixture of lidocaine base and prilocaine base.
In a further embodiment of the invention a eutectic mixture may also be formed by two or more substances, where at least one of these substances is a local anaesthetic.
The amount of the local anaesthetic or mixture of local anaest

REFERENCES:
patent: 4188373 (1980-02-01), Krezanoski
patent: 4478822 (1984-10-01), Haslam et al.
patent: 4780320 (1988-10-01), Baker
patent: 5114719 (1992-05-01), Sabel et al.
patent: 5288497 (1994-02-01), Stanley et al.
patent: 5288498 (1994-02-01), Stanley et al.
patent: 5292516 (1994-03-01), Veigas et al.
patent: 5589180 (1996-12-01), Hind
patent: 5612052 (1997-03-01), Shalaby
patent: 5635540 (1997-06-01), Edlich et al.
CA 123:152960, Shike et al, Jun. 20, 1995.
WPIDS AN 94-351141 Balard et al, Nov. 4, 1994.
CA 105:11993, Nyqvist-Mayer et al, 1986.
Nyqvist-Mayer et al, J Pharmaceutical Sciences, 75(4) pp. 365-373, Apr. 1986.

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