Use of Polymeric Materials with Other Substances for Improved Performance

Abstract

Methods of enabling or improving the ability of a hydrogel to swell in the stomach of an animal and/or increasing the amount of time said hydrogel remains swollen in the stomach are described herein. In one embodiment, a polymer is administered in combination with one or more pH modifying agents which raise and maintain the pH of the micro environment of the polymer and/or the stomach in order inducing swelling in the polymer. The polymer can be a homopolymer, a copolymer, or a polymer blend or composite. In one embodiment, the polymer is a superabsorbent polymer (“SAP”). The polymers can also be administered with one or more active agents, such as appetite suppressants. The pH modifying agent and/or the active agent can be administered simultaneously with the polymer in the same dosage form, simultaneously with the polymer in separate dosage forms, or sequentially. The compositions are formulated for oral administration. The formulation can include drugs for delivery to the stomach, such as antibiotics, or the hydrogel can be used as a filler, for example, for obesity control. The formulation an also be used to enhance gastric retention, for example, for controlled drug delivery. Methods of delivering a drug are also described herein, along with medicaments for carrying out the methods of the present invention.

1 . A method of enabling or improving the ability of a hydrogel to swell in the stomach of an animal and/or increasing the amount of time said hydrogel remains swollen in the stomach comprising administering to the animal a water-swellable polymer in combination with one or more substances which raise and maintain the pH of the microenvironment of the polymer and/or the stomach. 
   
   
       2 . The method of  claim 1 , wherein the polymer is a superabsorbent polymer. 
   
   
       3 . The method of  claim 1 , wherein the polymer is selected from the group consisting of homopolymers, copolymers, polymer blends, cross-linked polymers, polymer composites, and combinations thereof. 
   
   
       4 . (canceled) 
   
   
       5 . The method of  claim 1 , wherein the one or more substances which alter the pH are selected from the group consisting of buffers, H 2  blockers, proton pump inhibitors, antacids, proteins, nutritional shakes, and combinations thereof. 
   
   
       6 . The method of  claim 5 , wherein the buffer is selected from the group consisting of ammonium bicarbonate, ammonium carbonate, ammonium hydroxide, sodium bicarbonate, calcium carbonate, calcium hydroxide, magnesium carbonate, potassium bicarbonate, potassium carbonate, potassium hydroxide, sodium carbonate, sodium hydroxide, and combinations thereof. 
   
   
       7 . The method of  claim 5 , wherein the H 2  blocker is selected from the group consisting of cimetidine, ranitidine, famotidine, nizatidine, and combinations hereof. 
   
   
       8 . The method of  claim 5 , wherein the proton pump inhibitor is selected from the group consisting of omeprazole, lansoprazole, esomeprazole, pantoprazole, abeprazole, and combinations thereof. 
   
   
       9 . The method of  claim 5 , wherein the antacid is selected from the group consisting of aluminum hydroxide, magnesium hydroxide, aluminum carbonate, calcium carbonate, and hydrotalcite. 
   
   
       10 . (canceled) 
   
   
       11 . (canceled) 
   
   
       12 . The method of  claim 1 , wherein the polymer is administered with one or more therapeutically active, diagnostic or prophylactically active agents. 
   
   
       13 . The method of  claim 12 , wherein the agent is selected from the group consisting of analgesics, anti-inflammatory drugs, antipyretics, antidepressants, altiepileptics, antihistamines, antimigraine drugs, antimuscarinics, anxioltyics, sedatives, hypnotics, antipsychotics, bronchodilators, anti asthma drugs, cardiovascular drugs, corticosteroids, dopaminergics, electrolytes, gastro-intestinal drugs, muscle relaxants, nutritional agents, vitamins, parasympathomimetics, stimulants, anorectics, appetite suppressants, antiobesity agent, anti-narcoleptics, and combinations thereof. 
   
   
       14 . (canceled) 
   
   
       15 . The method of  claim 13 , wherein the agent is an appetite suppressant or antiobesity agent is selected from the group consisting of sibutramine hydrochloride, orlistat, rimonabant, benzphetamine, diethylpropion, mazindol phendimetrazine, phentermine, amphetamine, fenfluramine, nalmetrene, and combinations thereof. 
   
   
       16 . The method of  claim 1 , wherein the polymer is formulated for oral administration in the form of a tablet a caplet, a capsules, a syrup, a solution, a suspension, a powder, a bar or a shake. 
   
   
       17 . (canceled) 
   
   
       18 . The method of  claim 1 , wherein the substance which raises the pH of the microenvironment of the polymer and/or the stomach is administered simultaneously with the polymer in the same dosage form. 
   
   
       19 . The method of  claim 1 , wherein the substance which raises the pH of the microenvironment of the polymer and/or the stomach is administered before, after or simultaneously with the polymer in different dosage forms. 
   
   
       20 . (canceled) 
   
   
       21 . The method of  claim 19 , wherein the substance which raises the pH of the microenvironment of the polymer and/or the stomach is administered within 2, 6 or 24 hours of administration of the polymer. 
   
   
       22 . (canceled) 
   
   
       23 . (canceled) 
   
   
       24 . The method of  claim 1  further comprising administering a substance which causes the hydrogel to degrade, disperse, and/or shrink after the hydrogel has resided in the stomach for a time. 
   
   
       25 . The method of  claim 24 , wherein the substance is administered after the administration of the polymer. 
   
   
       26 . The method of  claim 24 , wherein the substance acts to lower the pH of the microenvironment of the polymer and/or the stomach. 
   
   
       27 . The method of  claim 26 , wherein the substance is an organic acid, an acidic drink, or a protein. 
   
   
       28 - 30 . (canceled) 
   
   
       31 . The method of  claim 27 , wherein the protein is an enzyme selected from the group consisting of pepsin, pancreatin, and combinations thereof. 
   
   
       32 . (canceled) 
   
   
       33 . (canceled) 
   
   
       34 . The method of  claim 18 , wherein the water-swellable formulation is in the form of a shake, optionally including vitamins, mineral, or nutraceuticals, which is effective to increase stomach pH to enhance swelling of the polymer, to supplement dietary nutrients, or induce satiation and weight loss. 
   
   
       35 . (canceled) 
   
   
       36 . The method of  claim 1 , wherein the animal is a human. 
   
   
       37 - 74 . (canceled) 
   
   
       75 . A medicament for enabling or improving the ability of a hydrogel to swell in the stomach of an animal and/or to increase the amount of time said hydrogel remains swollen in the stomach comprising a water-swellable polymer in combination with one or more substances which raise and maintain the pH of the microenvironment of the polymer and/or the stomach. 
   
   
       76 . The medicament of  claim 75 , wherein the polymer is a superabsorbent polymer. 
   
   
       77 . The medicament of  claim 75 , wherein the polymer is selected from the group consisting of homopolymers, copolymers, polymer blends, polymer composites, and combinations thereof. 
   
   
       78 . (canceled) 
   
   
       79 . The medicament of  claim 75 , wherein the one or more substances which alter the pH are selected from the group consisting of buffers, H 2  blockers, proton pump inhibitors, antacids, proteins, nutritional shakes, and combinations thereof. 
   
   
       80 . The medicament of  claim 79 , wherein the buffer is selected from the group consisting of ammonium bicarbonate, ammonium carbonate, ammonium hydroxide, sodium bicarbonate, calcium carbonate, calcium hydroxide, magnesium carbonate, potassium bicarbonate, potassium carbonate, potassium hydroxide, sodium carbonate, sodium hydroxide, and combinations thereof. 
   
   
       81 . The medicament of  claim 79 , wherein the H 2  blocker is selected from the group consisting of cimetidine, ranitidine, famotidine, nizatidine, and combinations hereof. 
   
   
       82 . The medicament of  claim 79 , wherein the proton pump inhibitor is selected from the group consisting of omeprazole, lansoprazole, esomeprazole, pantoprazole, abeprazole, and combinations thereof. 
   
   
       83 . The medicament of  claim 79 , wherein the antacid is selected from the group consisting of aluminum hydroxide, magnesium hydroxide, aluminum carbonate, calcium carbonate, and hydrotalcite. 
   
   
       84 . (canceled) 
   
   
       85 . (canceled) 
   
   
       86 . The medicament of  claim 75 , wherein the medicament further comprises one or more therapeutically active, diagnostic or prophylactically active agents. 
   
   
       87 . The medicament of  claim 86 , wherein the agent is selected from the group consisting of analgesics, anti-inflammatory drugs, antipyretics, antidepressants, altiepileptics, antihistamines, antimigraine drugs, antimuscarinics, anxioltyics, sedatives, hypnotics, antipsychotics, bronchodilators, anti asthma drugs, cardiovascular drugs, corticosteroids, dopaminergics, electrolytes, gastro-intestinal drugs, muscle relaxants, nutritional agents, vitamins, parasympathomimetics, stimulants, anorectics, appetite suppressants, antiobesity agent, anti-narcoleptics, and combinations thereof. 
   
   
       88 . (canceled) 
   
   
       89 . The medicament of  claim 87 , wherein the agent is an appetite suppressant or antiobesity agent selected from the group consisting of sibutramine hydrochloride, orlistat, rimonabant, benzphetamine, diethylpropion, mazindol phendimetrazine, phentermine, amphetamine, fenfluramine, nalmetrene, and combinations thereof. 
   
   
       90 . The medicament of  claim 75 , wherein the medicament is formulated for oral administration in the form of a tablet, a caplet, a capsules, a syrup, a solution, a suspension, a powder, a bar or a shake. 
   
   
       91 - 93 . (canceled) 
   
   
       94 . The medicament of  claim 75  further comprising a substance which causes the polymer to degrade, disperse, and/or shrink after the polymer has resided in the stomach for a time. 
   
   
       95 . The medicament of  claim 75  wherein substance acts to lower the pH of the microenvironment or the polymer and/or the stomach. 
   
   
       96 . The medicament of  claim 95 , wherein the substance is an organic acid, an acid drink or a protein. 
   
   
       97 . (canceled) 
   
   
       98 . (canceled) 
   
   
       99 . The medicament of  claim 75 , wherein the medicament is in the form of a shake, optionally including vitamins, mineral, or nutraceuticals, which is effective to increase stomach pH to enhance swelling of the polymer, to supplement dietary nutrients, or induce satiation and weight loss. 
   
   
       100 - 136 . (canceled)