Oral tablet for delivery of active ingredients to the gastrointestinal tract

Abstract

The invention relates to an oral tablet for delivery of active ingredients to the gastrointestinal tract comprising a population of particles and an active ingredient to be delivered to the gastrointestinal tract, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles providing the tablet with a plurality of discrete non-DC areas, and the non-DC areas resulting in induced saliva generation upon mastication of the tablet, wherein the tablet is designed to be masticated and designed to deliver the active ingredient to the gastrointestinal tract as part of the saliva generated upon mastication of the tablet.

1 - 95 . (canceled) 
     
     
         96 . An oral chewable tablet for delivery of active ingredients to the gastrointestinal tract comprising a population of particles and an active ingredient to be delivered to the gastrointestinal tract, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, the non-DC particles providing the tablet with a plurality of discrete non-DC areas, and the non-DC areas resulting in induced saliva generation upon mastication of the tablet, wherein the tablet is designed to be masticated directly after oral administration and designed to deliver the active ingredient to the gastrointestinal tract as part of the saliva generated upon mastication of the tablet. 
     
     
         97 . The oral chewable tablet according to  claim 96 , wherein the non-DC sugar alcohol particles have not been granulated prior to tableting. 
     
     
         98 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is absorbable in the gastrointestinal tract. 
     
     
         99 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is a gastrointestinal agent acting in the gastrointestinal tract. 
     
     
         100 . The oral chewable tablet according to  claim 96 , wherein at least 50% by weight of the active ingredient is absorbed in the gastrointestinal tract. 
     
     
         101 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is a gastrointestinal stimulant. 
     
     
         102 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is a gastrointestinal relaxant. 
     
     
         103 . The oral chewable tablet according to  claim 96 , wherein the tablet comprises means for sustained release. 
     
     
         104 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is at least partly encapsulated. 
     
     
         105 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is a prodrug. 
     
     
         106 . The oral chewable tablet according to  claim 96 , wherein the tablet is designed to release the active ingredient in the oral cavity for absorption through the oral mucosa of a part of the active ingredient, and wherein the tablet is designed to deliver another part of the active ingredient to the gastrointestinal tract as part of saliva generated upon mastication of the tablet. 
     
     
         107 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is an active pharmaceutical ingredient. 
     
     
         108 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is a nutraceutical. 
     
     
         109 . The oral chewable tablet according to  claim 96 , wherein said population of particles is tableted into a first module of the tablet and combined with a second population of particles that is tableted into a second module of the tablet. 
     
     
         110 . The oral chewable tablet according to  claim 96 , wherein a series of at least 10 of said tablets comprises said non-DC particles in an amount varying with a relative standard deviation (RSD) below 10%. 
     
     
         111 . (canceled) 
     
     
         112 . The oral chewable tablet according to  claim 96 , wherein the non-DC sugar alcohol particles are selected from the group consisting of non-DC particles of erythritol, non-DC particles of maltitol, non-DC particles of xylitol, and combinations thereof. 
     
     
         113 . The oral chewable tablet according to  claim 96 , wherein the non-DC sugar alcohol particles are non-DC erythritol particles. 
     
     
         114 . The oral chewable tablet according to  claim 96 , wherein the tablet comprises said non-DC sugar alcohol particles in an amount of at least 10% by weight of the tablet. 
     
     
         115 . The oral chewable tablet according to  claim 96 , wherein the tablet has a weight ratio between said non-DC sugar alcohol particles and said DC sugar alcohol particles, which is between 0.3 and 0.7. 
     
     
         116 . The oral chewable tablet according to  claim 96 , wherein saliva generation upon mastication of the tablet is induced compared to a tablet where the discrete areas are based on DC sugar alcohol particles. 
     
     
         117 . The oral chewable tablet according to  claim 96 , wherein the tablet generates more than 1.5 mL saliva within 30 seconds from onset of mastication. 
     
     
         118 . An oral chewable tablet for delivery of active ingredients to the gastrointestinal tract comprising a population of particles and an active ingredient to be delivered to the gastrointestinal tract, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, wherein the entire tablet is designed to be masticated and to turn into liquid within 20 seconds of mastication. 
     
     
         119 . An oral chewable tablet for delivery of active ingredients to the gastrointestinal tract comprising a population of particles and an active ingredient to be delivered to the gastrointestinal tract, the population of particles comprising directly compressible (DC) and non-directly compressible (non-DC) sugar alcohol particles, wherein the tablet is designed to be masticated, including any module of the tablet, and to dissolve within 20 seconds of mastication. 
     
     
         120 . The oral chewable tablet according to  claim 96 , wherein the active ingredient is selected from alginate, atenolol, aspirin (acetylsalicylic acid), ampicillin, aminosalicylates, anhydrous citric acid, bisacodyl, bismuth subsalicylate, bupropion, caffeine, calcium, calcium carbonate, cetirizine, cimetidine, cisapride, clarithromycin, desloratadine, dexlansoprazole, diphenhydramine HCl, diphenhydramine citrate, dimenhydrinate, docusate erythromycin, dopamine, esomeprazole, famotidine, fexofenadine HCl, guaifenesin, hydrotalcite, ibuprofen, ketoprofen, lactase enzyme, lansoprazole, loratadine, lorcaserin, loperamide, loperamide HCl, magnesium, magnesium carbonate, magnesium hydroxide, melatonin, methamphetamine HCl, metoclopramide, metronidazole, montelukast, mycostatin, naltrexone, naproxen, naproxen sodium, nizatidine, omeprazole, ondansetrone, orlistat, pantoprazole, paracetamol (acetaminophen), pectin, phentermine HCl, polypodium leucotomos, prednisolone, prednisone, progesterone, propranolol, propantheline Currently bromide, pseudoephedrine HCl, phentermine, rabeprazole, ranitidine, roflumilast, scopoloamine butyl hydroxide, simethicone, sodium, sodium bicarbonate, sodium docusate, sumatriptan, testosterone, tetracycline, topiramate, vitamin A, vitamin B, vitamin B12, vitamin C (ascorbic acid), vitamin D, and vitamin E, vitamin K, or any combination thereof. 
     
     
         121 . The oral chewable tablet according to  claim 96 , wherein at least 30% by weight of the non-DC sugar alcohol particles have a particle size above 500 μm.