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# c12) United States Patent 

# Gramatte et al. 

# (54) ORAL DOSAGE FORM FOR PROPIVERINE OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS WITH AN EXTENDED RELEASE OF THE ACTIVE INGREDIENT 

(75) Inventors: Thomas Gramatte, Dresden (DE); Peter Gruber, Merzhausen (DE); Michael Heschel, Pima (DE); Dirk Pamperin, Dresden (DE); Jan Ploen, Dresden (DE); Steffen Scheithauser, Dresden (DE); Wolfgang Wehner, Barthen (DE); Peter Guldner, Dresden (DE) 

(73) Assignee: Apogepha Arzneimittel GmbH, Dresden (DE) 

( *) Notice: Subject to any disclaimer, the term ofthis patent is extended or adjusted under 35 U.S.C. 154(b) by 1151 days. 

(21) Appl. No.: 10/492,270 

(22) PCT Filed: Oct. 8, 2002 

(86) PCT No.: PCT /EP02/11253 § 371 (c)(l), (2), ( 4) Date: Apr. 8, 2004 

(87) PCT Pub. No.: WO03/030869 

PCT Pub. Date: Apr. 17, 2003 

## (65) Prior Publication Data 

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## (30) Foreign Application Priority Data 

Oct. 9, 2001 (DE) .................................. 101 49 674 

(51) Int. Cl. A61K 9/14 (2006.01) 

(52) U.S. Cl. ........ 424/489; 424/490; 424/494; 424/451; 424/457; 424/461; 514/317 

(58) Field of Classification Search ........................ None See application file for complete search history. 

## (56) References Cited 

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## U.S. PATENT DOCUMENTS 

## FOREIGN PATENT DOCUMENTS 

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# (IO) Patent No.: US 7,943,176 B2 

# May 17, 2011 (45) Date of Patent: 

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Laicher et al.-Theophyllin, "Die Pellet-Technologie", Arzneim› Forsch./Drug Res. 48(1), Nr. 5a (1998), pp. 540-547. 

Grunenberg et al.-Theophyllin, "Erfahrungen bei der Ubertragung des Filmcoating-Prozessess fur Theophyllin-Retardpellets in den ProduktionsmaBstab", Arzneim-Forsch./Drug Res. 48(1), Nr. 5a (1998), pp. 547-551. 

Fuchs et al.-Theophyllin, "EinfluB verschiedener Variablen auf die ln-vitro-Freisetzung eines Theophyllin-Retardpraparates", Arzneim› Forsch./Drug Res. 48(1), Nr. 5a (1998), pp. 552-556. 

Fuchs et al.-Theophyllin, Anforderungen an die Produktqualitat von Theophyllin-Retardpraparaten, Arzneim-Forsch./Drug Res. 48(1), Nr. 5a ( 1998), pp. 556-561. 

Wilson et al.-Theophyllin, "Wirkung der Vorbenhandlung mit Ranitidin auf Pharmakokinetik und gastrointestinale Passage eines Theophyllin Retard-Praparates", Arzneim-Forsch./Drug Res. 48(1), Nr. 5a (1998), pp. 561-568. 

Primary Examiner - Robert A. Wax 

Assistant Examiner - Hasan S Ahmed 

(74) Attorney, Agent, or Firm - Vidas, Arrett & Steinkraus 

## (57) ABSTRACT 

By suitable retardation oral pharmaceutical compositions containing propiverine or one or several pharmaceutically acceptable salts thereof in an amount of 4 mg to 60 mg propiverine and having a prolonged release of the active agent are produced. Preferably a blend of active agent and option› ally one or more acidic substances having a pKa value ofless than 6.65 are provided with a retarding coating or are embed› ded in a matrix which is then optionally coated with further retarding layers. 

US007943176B2 

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## OTHER PUBLICATIONS 

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## 19 Claims, 6 Drawing Sheets 

