Solid controlled release bioadherent emulsions

• US 5,055,303 A
• Filed: 01/31/1989
• Issued: 10/08/1991
• Est. Priority Date: 01/31/1989
• Status: Expired due to Term

• Current Assignee: DrugTech Corporation (PD International Holdings LLC)
• Original Assignee: KV Pharmaceutical Company (Apollo Global Management, Inc.)
• Inventors: Riley, Thomas C. Jr.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Hulina, Amy
• Application Number:
  US07/304,124
• Time in Patent Office: 980 Days
• Field of Search: 424/436, 514/966, 514/967
• US Class Current: 424/436
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/02 Suppositories; Bougies; Bases therefor; Ovulesapparatus for making A61J3/08; devices for introducing into the body A61M31/00

Abstract

Solid delivery systems which at body temperature exhibit controlled release and bioadherence characteristics. These systems are emulsions which are water in oil in nature and whose internal phase is greater than that of the external phase. That is, the internal phase comprises at least 60% of the system.

Claims

1. A bioadherent controlled release drug delivery system which is a solid at room temperature and a cream at body temperature, which comprises:

a solid emulsion system containing a continuous lipoidal external phase, an active agent, and a nonlipoidal internal phase that is at least 60% by volume of the emulsion, wherein said internal phase is selected from the group consisting of water, glycerine, and mixtures thereof.

2. The delivery system of claim 1 wherein said system contains plasticizers.

3. The delivery system of claim 1 wherein said internal phase is at least 70% by volume of the system.

4. The delivery system of claim 1 wherein said system is a suppository.

5. The delivery system of claim 1 wherein said system is orally administered.

6. The delivery system of claim 1 wherein the external phase melts to form the cream.

7. A method for preparing a bioadherent controlled release drug delivery system, which comprises:

a) mixing an active pharmaceutical agent with a non-lipoidal internal phase selected from the group consisting of water, glycerine, and mixtures thereof until a homogeneous mixture is obtained;

b) mixing the homogeneous mixture with a continuous lipoidal external phase at low shear to obtain a uniform emulsion system, wherein the temperatures of the internal phase and external phase are about 5 degrees to about 10 degrees above the melting point of the highest melting point component in the system and the nonlipoidal internal phase is at least 60% by volume of the emulsion system; and

c) inserting the product into preformed molds and recovering a bioadherent controlled release drug delivery system which is a solid at room temperature and a cream at body temperature.

8. The process of claim 7 wherein the internal phase is slowly added to the external phase while mixing the system.

9. The process of claim 7 wherein the nonlipoidal internal phase is at least 70% by volume of the internal phase.

10. The process of claim 7 wherein the preformed mold is a preformed package.