Gastric retention dosage form having multiple layers

a dosage form and active agent technology, applied in the direction of pharmaceutical active ingredients, pill delivery, medical preparations, etc., can solve the problems of inability to generally leave the stomach of non-digested material, inconvenient use for users, and short window for absorption of active agents in the small intestine to provide a desired therapeutic effect, etc., to achieve the effect of prolonging the delivery of active agents

Inactive Publication Date: 2005-01-27
ENCINAL PHARMA INVESTMENTS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

As can be observed in the above-referenced patents and publications, devices have been described that provide for prolonged delivery of an active agent and retention in the gastric environment. Howe...

Problems solved by technology

For active agents that are not easily absorbed by the small intestine or that do not dissolve readily, the window for active agent absorption in the small intestine may be too short to provide a desired therapeutic effect.
The need for frequent dosing presents compliance problems and is often inconvenient for the user as well.
In the fed state, non-digested material is not generally able to leave the stomach.
However, it is not practical to regularly maintain the fed state over a long period ...

Method used

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  • Gastric retention dosage form having multiple layers
  • Gastric retention dosage form having multiple layers
  • Gastric retention dosage form having multiple layers

Examples

Experimental program
Comparison scheme
Effect test

preparation 1

An example of a active agent which requires frequent dosing is acyclovir. A typical dosing regimen for this antiviral active agent is five doses per day administered every four hours. A dosage form in accordance with this invention for twice daily dosing of acyclovir is formulated according to the following procedures. The dosage form is retained in the stomach and releases acyclovir over a prolonged period of time.

22.5 Grams of acyclovir and 3.6 grams of the gel-forming polymer polyethylene oxide, having a number average molecular weight of approximately 200,000 grams per mole, are separately screened through a mesh having 40 wires per inch. The polyethylene oxide is supplied under the trade name Polyox® grade WSR N80 as manufactured by Union Carbide Corporation, Danbury, Conn. The sized active agent and polymer are dry mixed. Then, 3.75 grams of a hydroattractant water-insoluble polymer, hydroxypropyl cellulose having a hydroxypropyl content of 10-13 weight percent and an avera...

example 1 (

ASSAY)

Banded devices fabricated in Preparation 1 are assayed for dimensional changes and release of active agent as follows:

A banded dosage form is placed in a beaker of simulated gastric fluid, as specified in U.S. Pharmacopedia / National Formulary 23 / 18, having a pH of approximately 1.4 and a maintained temperature of 37° C. After one hour, the device is removed and measured for dimensional change in length and diameter. The swollen device will have the general appearance of the dosage form shown in FIG. 4.

Samples of the dosage form are tested for release of active agent by shaking at prescribed conditions in an aqueous media simulating the media in the upper gastrointestinal tract. Each dosage form is first placed in a cylindrical, slotted basket having inside diameter of 15 mm and inside length of 52 mm. Each basket has eight slots and each slot is 1-2 mm wide and 52 mm long and positioned lengthwise along the length of the basket. The basket containing the dosage form is th...

example 2

Dosage forms of this invention containing the antiviral drug ganciclovir are prepared in accordance with the procedures of Preparation 1. The dosage forms prepared are retained in the stomach and release ganciclovir over a prolonged period of time.

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PUM

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Abstract

The present invention is directed to a multilayered dosage form which is adapted for retention in the stomach and useful for the prolonged delivery of an active agent to a fluid environment of use. The active agent dosage form is a multilayer core, often bilayer, formed of polymer matrices that swell upon contact with the fluids of the stomach. At least one layer of the multilayered dosage form includes an active agent. A portion of the polymer matrices are surrounded by a band of insoluble material that prevents the covered portion of the polymer matrices from swelling and provides a segment of the dosage form that is of sufficient rigidity to withstand the contractions of the stomach and delay expulsion of the dosage form from the stomach until substantially all of the active agent has been dispensed.

Description

FIELD OF THE INVENTION The present invention is related to the prolonged release of an active agent from a dosage form. More particularly, it relates to a multilayered active agent dosage form having a highly swellable layer and a drug layer, the dosage form being adapted for retention in the stomach for a prolonged period. BACKGROUND OF THE INVENTION Controlled release dosage forms that provide for prolonged delivery of active agent formulations to the environment of use have found application for increasing numbers of active agents. However, with respect to pharmaceutical and veterinary active agent formulations, there has been a need not only to provide for prolonged delivery of the active agent over time, but also to provide prolonged delivery of the active agent at a particular location or locations in the environment of use, such as in the stomach. Certain active agents are absorbed primarily from the small intestine. Generally, the time of passage of different particles th...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/22A61K9/24A61K31/00A61K47/00
CPCA61K9/0065Y10S514/866Y10S514/836Y10S514/884Y10S514/909Y10S424/06Y10S514/961Y10S514/965Y10S514/96
Inventor EDGREN, DAVID E.JAO, FRANCISCOWONG, PATRICK S.L.
Owner ENCINAL PHARMA INVESTMENTS
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