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Solid pharmaceutical formulations for slow, zero order release via controlled surface erosion: expanded range

Patent 4539198 Issued on September 3, 1985. Estimated Expiration Date: Icon_subject July 7, 2003. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

Pharmaceutical formulation for slow release via controlled surface erosion
Patent #: 4264573
Issued on: 04/28/1981
Inventor: Powell ,   et al.

Solid pharmaceutical formulations for slow, zero order release via controlled surface erosion Patent #: 4361545
Issued on: 11/30/1982
Inventor: Powell ,   et al.

Inventors

Assignee

Application

No. 06/511605 filed on 07/07/1983

US Classes:

424/464, Tablets, lozenges, or pills424/465, With claimed perfecting feature in contents (e.g., excipient, lubricant, etc.)514/161, With heterocyclic compound514/960SIGNIFICANT, TABLET FORMULATION (E.G., DESIGNATED EXCIPIENT, DISINTEGRANT, GLYDENT OR LUBRICANT, ETC.)

Examiners

Primary: Rose, Shep K.

Attorney, Agent or Firm

International Classes

A61K 31/60 (20060101)
A61K 9/20 (20060101)

Abstract

A new class of solid pharmaceutical formulations enables the attainment of slow, zero order in vivo release of a wide range of pharmaceutically active ingredients upon oral administration. A broad range of release rates can be preselected by suitable adjustments of tablet properties. The formulations are based upon control of active ingredient release from the surface of the tablet via a controlled surface erosion mechanism. These compositions comprise:(a) an effective amount in the range of 10-90 wt. % of a pharmacologically active compound having a water solubility (20° C.) of 1/5-1/1000 (w/w);(b) 1-40 wt. % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20° C.) of 1/1-1/40 (w/w);(c) 2-20 wt. % of a compound which is pharmaceutically acceptable in oral compositions and has a water solubility (20° C.) of 1/1-1/10 (w/w);(d) an amount in the range of 0.05-1.0 wt. % of a disintegrating agent for pharmaceutical compositions, at which amount the compound is ineffective as a disintegrating agent;(e) 0.1-2.0 wt. % of a surfactant which is pharmaceutically acceptable in oral compositions; and, as necessary for tablet manufacturing purposes;(f) 1-20 wt. % of a binder which is pharmaceutically acceptable in oral compositions; or(g) 0.5-5.0 wt. % of a die wall lubricant which is pharmaceutically acceptable in oral compositions.

Other References

  • Porter et al., "The Permeability of Enteric Coatings and the Dissolution Rates of Coated Tablets", Jun. 5, 1981, pp. 5-8
  • Remington's Pharmaceutical Sciences, 1970, pp. 1689-1691
  • Porter, "Tablet Coating," Jun. 1981, pp. 44, 46, 48, 50, 51, 86, 90, 92, 94
  • Luce, "Cellulose Acetate Phthalate: A Versatile Enteric Coating", Jun. 1977
  • Rasmussen, "5-Aminosalicylic Acid in a Slow-Release Preparation: Bioavailability, Plasma Level, and Excretion in Humans," 1982, pp. 1062-1070
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