Anti-misuse microparticulate oral pharmaceutical form
First Claim
1. A method of preparing a pharmaceutical formulation for combating the misuse of active principle (AP), the method comprising:
- providing inert cores;
coating the inert cores with at least one layer comprising the active principle;
coating the at least one layer comprising the active principle with at least one coating layer (Ra) to create modified release coated microparticles resistant to crushing;
wherein said at least one coating layer (Ra) represents a fraction by weight (Tp) greater than 30%, expressed in % by dry weight, based on the total weight of the coated microparticles,whereby said at least one coating layer (Ra) comprises;
at least one film-forming (co)polymer (A1) insoluble in the gastrointestinal juices present in a proportion of 60% to 90% by weight on a dry basis, relative to the total mass of the coating composition;
at least one (co)polymer soluble in the gastrointestinal juices (A2) present in a proportion of 5% to 40% by weight on a dry basis, relative to the total mass of the coating composition; and
at least one plasticizer (A3) present in a proportion of 1% to 30% by weight on a dry basis, relative to the total mass of the coating composition; and
wherein said formulation further comprises at least one viscosifier (Vb) whereby said formulation further comprises at least one AP sequestering agent Q, whereby a complex with the AP is formed in solution.
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Accused Products
Abstract
The present invention relates to solid microparticulate oral pharmaceutical forms whose composition and structure make it possible to avoid misuse of the pharmaceutical active principle (AP) they contain.
The object of the present invention is to prevent solid oral drugs from being misappropriated for any use other than the therapeutic use(s) officially approved by the competent public health authorities. In other words, the object is to avoid the voluntary or involuntary misuse of solid oral drugs.
The invention relates to a solid oral pharmaceutical form which is characterized in that it contains anti-misuse means, in that at least part of the AP it comprises is contained in coated microparticles for modified release of the AP, and in that the coated microparticles of AP have a coating layer (Ra) which assures the modified release of the AP and simultaneously imparts crushing resistance to the coated microparticles of AP so as to avoid misuse.
103 Citations
31 Claims
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1. A method of preparing a pharmaceutical formulation for combating the misuse of active principle (AP), the method comprising:
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providing inert cores; coating the inert cores with at least one layer comprising the active principle; coating the at least one layer comprising the active principle with at least one coating layer (Ra) to create modified release coated microparticles resistant to crushing; wherein said at least one coating layer (Ra) represents a fraction by weight (Tp) greater than 30%, expressed in % by dry weight, based on the total weight of the coated microparticles, whereby said at least one coating layer (Ra) comprises; at least one film-forming (co)polymer (A1) insoluble in the gastrointestinal juices present in a proportion of 60% to 90% by weight on a dry basis, relative to the total mass of the coating composition; at least one (co)polymer soluble in the gastrointestinal juices (A2) present in a proportion of 5% to 40% by weight on a dry basis, relative to the total mass of the coating composition; and at least one plasticizer (A3) present in a proportion of 1% to 30% by weight on a dry basis, relative to the total mass of the coating composition; and wherein said formulation further comprises at least one viscosifier (Vb) whereby said formulation further comprises at least one AP sequestering agent Q, whereby a complex with the AP is formed in solution. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31)
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Specification