Controlled release delivery coating formulation for bioactive substances

• US 4,891,223 A
• Filed: 09/03/1987
• Issued: 01/02/1990
• Est. Priority Date: 09/03/1987
• Status: Expired due to Term

• Current Assignee: aaiPharma, Inc.
• Original Assignee: Air Products and Chemicals Incorporated (Linde Plc)
• Inventors: Ambegaonkar, Anil S., Howells, Roger A.
• Primary Examiner(s): Dixon, Jr., William R.
• Assistant Examiner(s): Griffin, Andrew
• Application Number:
  US07/092,743
• Time in Patent Office: 852 Days
• Field of Search: 424/471, 424/473, 424/408
• US Class Current: 424/408
• CPC Class Codes: A01N 25/26 in coated particulate form
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61K 9/5073 having two or more different coatings optionally including drug-containing subcoatings

Abstract

The present invention relates to a bioactive composition having a controlled, sustained release delivery pattern when contacted with a suitable surrounding media. The composition comprises a pharmaceutically, insecticidally, herbicidally or fertilizing bioactive material core, soluble in a given surrounding media, the core present in an amount at least sufficient for a total dosage during a specified treatment period; a first coating enveloping the bioactive material core comprising a polymer or a blend of polymers, said polymer or blend of polymers being swellable upon penetration by the surrounding media; and a second coating enveloping the first coating, the second coating comprising a polymer or a blend of polymers being water-insoluble and forming a semi-permeable barrier to the inward diffusion of the surrounding media and the outward diffusion of the bioactive material dissolved in the surrounding media.

Claims

1. A bioactive composition having a controlled, sustained release delivery pattern when contacted with a suitable surrounding media comprising:

(a) a pharmaceutically, insecticidally, herbicidally or fertilizing bioactive material core, soluble in the surrounding media, the core present in an amount at least sufficient for a total dosage during a specified treatment period;

(b) a first coating enveloping the bioactive material core comprising a polymer or a blend of polymers, said polymer or blend of polymers being water-soluble and swellable upon penetration by the surrounding media; and

(c) a second coating enveloping the first coating, the second coating comprising a polymer or a blend of polymers;

said polymer or blend of polymers being water-insoluble and forming a semi-permeable barrier permitting inward diffusion of the surrounding media and outward diffusion of the bioactive material dissolved in the surrouding media;

whereby when the composition is exposed to the surrounding media, the exposure will result in the controlled release of the bioactive material.

2. The composition of claim 1 wherein the first coating further comprises a plasticizing agent.

3. The composition of claim 1 wherein the controlled, sustained release delivery pattern is a zero-order pattern and wherein the first coating is present in an effective thickness and wherein the second coating is present in an effective thickness and permeability so as to cause the diffusion of penetrants through the first coating to be the rate controlling step and wherein the second coating has the requisite stretchability to prevent rupture of the second coating due to the swelling of the first coating.

4. The composition of claim 1 wherein the controlled, sustained release delivery pattern is a bi-phasic pattern and wherein the first coating is present in an effective thickness and wherein the second coating is present in efffective thickness and permeability so as to cause the diffusion of penetrants through the first coating to be the rate controlling step and wherein the second coating has the requisite stretchability to prevent rupture of second coating due to the swelling of the first coating until a specific time in the release pattern.

5. The composition of claim 1 wherein the first coating polymer or blend of polymers, which are water-soluble and swellable, is selected from the group consisting of hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyvinyl alcohol, polyvinyl pyrrolidone and mixtures thereof.

6. The composition of claim 1 wherein the second coating polymer or blend of polymers is selected from the group consisting of ethyl cellulose, ethyl cellulose and hydroxypropyl cellulose, ethyl cellulose and methyl cellulose, and ethyl cellulose and hydroxypropyl cellulose hydroxypropyl methyl cellulose and rosin.