Film-coated tablet for improved upper gastrointestinal tract safety

• US 6,165,513 A
• Filed: 06/10/1998
• Issued: 12/26/2000
• Est. Priority Date: 06/11/1997
• Status: Expired due to Term

• Current Assignee: Allergan Pharmaceuticals International Ltd. (Abbvie Incorporated)
• Original Assignee: The Procter & Gamble Company
• Inventors: Dansereau, Richard John, Bekker, Petrus Jakobus
• Primary Examiner(s): CELSA, BENNETT M
• Application Number:
  US09/095,322
• Time in Patent Office: 930 Days
• Field of Search: 424/451, 424/456, 424/457, 424/461, 424/464, 424/468, 424/474, 424/475, 424/486, 424/489, 424/490, 514/108, 514/960-964
• US Class Current: 424/490
• CPC Class Codes: A61K 31/138 Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377
• CPC Class Codes: A61K 31/375 Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/401 Proline; Derivatives thereof, e.g. captopril
• CPC Class Codes: A61K 31/49 Cinchonan derivatives, e.g. quinine
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 31/65 Tetracyclines
• CPC Class Codes: A61K 31/663 Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
• CPC Class Codes: A61K 31/675 having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• CPC Class Codes: A61K 31/7072 having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/04 for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
• CPC Class Codes: A61P 19/08 for bone diseases, e.g. rachitism, Paget's disease

Abstract

A novel oral dosage to be delivered to the stomach comprising a safe and effective amount of an active ingredient selected from the group consisting of emepronium bromidebromide, doxycycline, and other tetracyclines/antibiotics, iron preparations, quinidine, nonsteroidal anti-inflammatory drugs, alprenolol, ascorbic acid, captopril, theophylline, zidovoudine (AZT), bisphosphonates and mixtures thereof and pharmaceutically-acceptable excipients, wherein said oral dosage form is a generally oval form and film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus.

Claims

1. An oral dosage form comprising a safe and effective amount of a bisphosphonate wherein said oral dosage form is oval shaped, about 0.23 to about 0.85 inches in length, about 0.11 to about 0.4 inches in width, and about 0.075 to about 0.3 inches in thickness and said oral dosage form is film coated to facilitate rapid esophageal transit and avoid irritation in the mouth, buccal cavity, pharynx, and esophagus wherein said film coating allows for delivery of said bisphosphonate to the stomach.

2. A dosage form according to claim 1 wherein the film coating is a polymer that is soluble at pH from about 1.2 to about 5.

3. A dosage form according to claim 2 wherein said film coating is selected from the group consisting of hydroxypropylmethylcellulose, hydroxypropylcellulose, carboxymethylcellulose, methylcellulose, ethylcellulose, acrylic resins, polyvinylpyrrolidone, gelatin, and mixtures thereof.

4. A dosage form according to claim 2 wherein said film coating is selected from the group consisting of hydroxypropylmethylcellulose and hydroxypropylcellulose.

5. A dosage form according to claim 4 wherein said active ingredient is selected from the group consisting of risedronate, alendronate, and pamidronate.

6. A dosage form according to claim 5 wherein said active ingredient is risedronate.

7. A dosage form according to claim 6 wherein said risedronate is from about 0.25% to about 40% of the composition.

8. A dosage form according to claim 1 wherein said dosage form is a compressed tablet comprising particles of the active ingredient and pharmaceutically-acceptable excipients.

9. A dosage form according to claim 1 wherein said active ingredient is selected from the group consisting of risedronate, alendronate and pamidronate.

10. A dosage form according to claim 9 wherein said dosage form is a compressed tablet comprising particles of the active ingredient and pharmaceutically-acceptable excipients.