Orodispersible tablets obtained by compression molding
Inventors
DECORTE, Isabelle • Gendrot, Edouard • Prevost, Yann
Assignees
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Publication Number
US-10111832-B2
Publication Date
2018-10-30
Expiration Date
Abstract
Embodiments of the present invention provide an orodispersible tablet having a hardness of 30 to 80 N, and preferably 40 to 75 N, a brittleness less than 1% and preferably less than 0.5%, disintegrating in the mouth within 60 seconds and preferably within 40 seconds, comprising an active ingredient in the form of coated microcrystals or microgranules and a mixture of excipients chosen from a group comprising a diluent, a disintegrant, a sweetener, a binder, a levelling agent, a humectant or wetting agent, a lubricant, a flavoring agent, a dye, and mixtures thereof, said mixture of excipients preferably coming in the form of grains.
Core Innovation
The invention concerns a compression molding process for preparing an orodispersible tablet. It addresses obtaining an orodispersible tablet with target mouth disintegration while maintaining friability and controlling brittleness/core effect and mouthfeel/taste.
The described approach uses excipients present as grains and a humidification-based preparation of a wet excipient mixture, followed by mixing coated microcrystals or microgranules of active principle and compressing the mixture to obtain a tablet. The wet mixture is prepared using a humidification method, and the humidification parameters and humectant/wetting solution selection are linked to improved performance.
In the described formulations and comparisons, humidification-based compression molding is contrasted with direct compression. The document reports examples in which the approach improves mouthfeel/taste masking and reduces core effect while keeping friability and disintegration time within targeted ranges.
Claims Coverage
The document includes two independent claims. The independent claims specify inventive features related to excipient composition in grain form, residual humidity or water content of the wet excipient mixture, selection and constraints of humectant or wetting solution, and mixing coated microcrystals or microgranules with the wet excipient mixture before compression.
Humidified wet excipient mixture with specified residual humidity and macrogol glyceride humectant
Preparing using a humidification method a wet mixture of excipients consisting of from 65 wt % to 90 wt % diluent, a disintegrant, a sweetener, a binder, and less than 3 wt % of a humectant in the form of grains, wherein the humectant is macrogol glyceride and wherein the wet mixture has a residual humidity or water content of from 2% to 3%.
Mixing coated active microcrystals or microgranules with the humidified wet excipient mixture and compressing
Preparing coated microcrystals or microgranules of active principle; mixing the coated microcrystals or microgranules with the wet mixture of excipients to obtain a mixture for compression; and compressing the mixture for compression to obtain a tablet.
Wet excipient mixture via humectant-class wetting solution reaching specified residual humidity
Incorporating a wetting solution into a grain-form mixture of excipients to obtain a wet mixture having a residual humidity or water content of from 0.5% to 7%, wherein the wetting solution comprises a humectant chosen from poloxamers, macrogols, macrogol glycerides, and polysorbates.
Mixing coated active microcrystals or microgranules with the wet excipient mixture and compressing
Preparing coated microcrystals or microgranules of active principle; mixing the coated microcrystals or microgranules with the wet mixture of excipients to obtain a mixture for compression; and compressing the mixture for compression to obtain a tablet.
Across the independent claims, the core claim coverage centers on a compression molding process in which a wet excipient mixture in grain form is prepared by humidification, then mixed with coated microcrystals or microgranules of active principle and compressed to obtain an orodispersible tablet.
Stated Advantages
Improved mouthfeel/taste masking.
Reduced core effect.
Maintaining friability while providing controlled mouth disintegration time.
Documented Applications
Preparation of an orodispersible tablet using a compression molding process.
Comparative examples contrasting humidification-based compression molding with direct compression for orodispersible tablets.
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