This invention concerns a new pharmaceutical combination which can be used for the treatment of muscular pain and acute lombalgia. It consists of a topical vehicle containing a combination of a non-steroid anti-inflammatory drug (NSAID) and a commonly used therapeutical substance that can act synergically in order to achieve a relatively high level of efficacy . Treatment with NSAIDs is extremely effective and is able to improve the quality of life in the majority of subjects affected by acute or chronic disorders. In clinical practice NSAIDs are frequently used as anti-inflammatory drugs and pain killers, but their use is often limited due to their potential adverse effects at gastric level, such as dyspepsia, abdominal pain, mucosal lesions, etc. This invention concerns a topical formulation that makes it possible to overcome the potential adverse effects of NSAIDs (irritation and ulceration of the gastric mucosa) and to increase their anti-inflammatory and analgesic effects, also adding a myorelaxant activity while maintaining plasma levels within the normal range for a long period of time after a single administration. From a technological point of view, an emulgel, i.e. an oil-in-water emulsion in which the external phase is gelified, was chosen as the final pharmaceutical form. Advantages The particular formulation provides the topical system with properties such as: Improved application properties with respect to the traditional formulations like creams and ointments; More rapid and complete transfer of the active ingredient from the vehicle to the skin and consequent greater efficacy; The product is easy to spread, favouring application on large areas of skin; The product is not greasy and does not leave traces after application; Excellent skin-feel; Easier penetration of the drugs through the skin due to the presence of absorption promoters; In vitro and in vivo tests have demonstrated that the active ingredients are quickly absorbed; In vivo tests, on healthy consenting volunteers, have confirmed the surprising anti-inflammatory and analgesic activity of the emulgels produced according to this invention. The onset of beneficial effects is rapid and effective almost to the same extent as an injectable administration. The various emulgels according to this invention are of interest from a formulation and functional point of view as they improve the parameters of permeation and increase the characteristics of absorption of the active ingredients in question with respect to commercial formulations that contain the same drugs. The production costs of these emulgels, containing substances commonly used in pharmaceutical production, are presumably comparable to those of similar medicinal preparations already present on the market.

Pharmaceutical preparations for transdermal use

CAVALLARI, CRISTINA;LUPPI, BARBARA;DI PIETRA, ANNA MARIA;RODRIGUEZ, LORENZO
2014

Abstract

This invention concerns a new pharmaceutical combination which can be used for the treatment of muscular pain and acute lombalgia. It consists of a topical vehicle containing a combination of a non-steroid anti-inflammatory drug (NSAID) and a commonly used therapeutical substance that can act synergically in order to achieve a relatively high level of efficacy . Treatment with NSAIDs is extremely effective and is able to improve the quality of life in the majority of subjects affected by acute or chronic disorders. In clinical practice NSAIDs are frequently used as anti-inflammatory drugs and pain killers, but their use is often limited due to their potential adverse effects at gastric level, such as dyspepsia, abdominal pain, mucosal lesions, etc. This invention concerns a topical formulation that makes it possible to overcome the potential adverse effects of NSAIDs (irritation and ulceration of the gastric mucosa) and to increase their anti-inflammatory and analgesic effects, also adding a myorelaxant activity while maintaining plasma levels within the normal range for a long period of time after a single administration. From a technological point of view, an emulgel, i.e. an oil-in-water emulsion in which the external phase is gelified, was chosen as the final pharmaceutical form. Advantages The particular formulation provides the topical system with properties such as: Improved application properties with respect to the traditional formulations like creams and ointments; More rapid and complete transfer of the active ingredient from the vehicle to the skin and consequent greater efficacy; The product is easy to spread, favouring application on large areas of skin; The product is not greasy and does not leave traces after application; Excellent skin-feel; Easier penetration of the drugs through the skin due to the presence of absorption promoters; In vitro and in vivo tests have demonstrated that the active ingredients are quickly absorbed; In vivo tests, on healthy consenting volunteers, have confirmed the surprising anti-inflammatory and analgesic activity of the emulgels produced according to this invention. The onset of beneficial effects is rapid and effective almost to the same extent as an injectable administration. The various emulgels according to this invention are of interest from a formulation and functional point of view as they improve the parameters of permeation and increase the characteristics of absorption of the active ingredients in question with respect to commercial formulations that contain the same drugs. The production costs of these emulgels, containing substances commonly used in pharmaceutical production, are presumably comparable to those of similar medicinal preparations already present on the market.
2014
EP2019666 B1
Cavallari C.;Luppi B.;Di Pietra AM; Rodriguez L.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11585/299132
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