US 9,808,418 B2
Pharmaceutical dosage form
Viness Pillay, Gauteng (ZA); Rubina Perveen Shaikh, Gauteng (ZA); Yahya Essop Choonara, Gauteng (ZA); and Lisa Claire Du Toit, Gauteng (ZA)
Assigned to UNIVERSITY OF THE WITWATERSRAND, JOHANNESBURG, Johannesburg Gauteng (ZA)
Appl. No. 13/988,959
Filed by Viness Pillay, Gauteng (ZA); Rubina Perveen Shaikh, Gauteng (ZA); Yahya Essop Choonara, Gauteng (ZA); and Lisa Claire Du Toit, Gauteng (ZA)
PCT Filed Nov. 28, 2011, PCT No. PCT/IB2011/055331
§ 371(c)(1), (2), (4) Date Sep. 3, 2013,
PCT Pub. No. WO2012/070028, PCT Pub. Date May 31, 2012.
Claims priority of application No. 2010/03740 (ZA), filed on Nov. 26, 2010.
Prior Publication US 2013/0337022 A1, Dec. 19, 2013
Int. Cl. A61K 9/00 (2006.01); A61K 9/52 (2006.01)
CPC A61K 9/00 (2013.01) [A61K 9/006 (2013.01); A61K 9/0065 (2013.01)] 25 Claims
 
1. An oral pharmaceutical dosage form for the release of at least two pharmaceutically active agents to different regions of the gastro intestinal tract, the pharmaceutical dosage form consisting of:
(1) a first gastric pharmaceutical dosage component said gastric component consisting of:
(a) a mucoadhesive layer which is capable of adhering to the gastro intestinal tract or buccal mucosa of the human or animal body, wherein the mucoadhesive layer of the gastric component is configured to adhere to the wall of the stomach when in use;
(b) a water-insoluble outer layer; and
(c) an intermediate layer positioned between the mucoadhesive and water-insoluble outer layers, wherein the water-insoluble outer layer of the gastric component ensures unidirectional release of pharmaceutically active agent from the intermediate and/or the mucoahesive layer to the gastric region;
wherein the pharmaceutically active agent is incorporated into the intermediate and/or the mucoadhesive layer in the form of micro- and/or nano-fibers that are produced by electrospinning and crosslinking;
(2) a second intestinal pharmaceutical dosage component, said intestinal component consisting of:
(a) a mucoadhesive layer which is capable of adhering to the gastro intestinal tract or buccal mucosa of the human or animal body, wherein the mucoadhesive layer of the intestinal component is configured to adhere to the intestinal wall;
(b) a water-insoluble outer layer; and
(c) an intermediate layer positioned between the mucoadhesive and water-insoluble outer layers, wherein the water-insoluble outer layer of the intestinal component ensures unidirectional release of pharmaceutically active agent from the intermediate and/or the mucoadhesive layer to the intestine;
wherein the pharmaceutically active agent is incorporated into the intermediate and/or the mucoadhesive layer in the form of micro- and/or nano-fibers that are produced by electrospinning and crosslinking;
(3) a pH responsive polymeric layer connecting the first gastric pharmaceutical dosage component and the second intestinal pharmaceutical dosage component, said pH responsive layer located between the mucoadhesive layer of the intestinal component and the water-insoluble outer layer of the gastric component, said pH responsive polymeric layer causing the first gastric pharmaceutical dosage component and the second intestinal pharmaceutical dosage component to separate after ingestion from each other.