U.S. patents available from 1976 to present.
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Pharmaceutical compositions with constant erosion volume for zero order controlled release

Patent 5393765 Issued on February 28, 1995. Estimated Expiration Date: Icon_subject December 13, 2013. 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

3870790

Sustained release therapeutic compositions
Patent #: 4226849
Issued on: 10/07/1980
Inventor: Schor

Method and composition for the preparation of controlled long-acting pharmaceuticals
Patent #: 4259314
Issued on: 03/31/1981
Inventor: Lowey

Sustained release therapeutic compositions based on high molecular weight hydroxypropylmethylcellulose
Patent #: 4389393
Issued on: 06/21/1983
Inventor: Schor ,   et al.

Prolonged release drug dosage forms based on modified low viscosity grade hydroxypropylmethylcellulose
Patent #: 4540566
Issued on: 09/10/1985
Inventor: Davis ,   et al.

Sustained release propranolol tablet
Patent #: 4556678
Issued on: 12/03/1985
Inventor: Hsiao

Pharmaceutical composition, in particular dermatological or cosmetic, comprising hydrous lipidic lamellar phases or liposomes containing a retinoid or a structural analogue thereof such as a carotenoid
Patent #: 5034228
Issued on: 07/23/1991
Inventor: Meybeck, et al.

Controlled release tablet containing water soluble medicament
Patent #: 5126145
Issued on: 06/30/1992
Inventor: Evenstad, et al.

Controlled release article with pulsatile release
Patent #: 5213808
Issued on: 05/25/1993
Inventor: Bar-Shalom, et al.

Oral osmotic system for slightly soluble active agents Patent #: 5284662
Issued on: 02/08/1994
Inventor: Koparkar, et al.

Inventors

Assignee

Application

No. 166123 filed on 12/13/1993

US Classes:

514/365, 1,3-thiazoles (including hydrogenated)424/464, Tablets, lozenges, or pills514/781Cellulose or derivative

Examiners

Primary: Henley, III, Raymond
Assistant: MacMillan, Keith D.

Attorney, Agent or Firm

Foreign Patent References

  • 0111144 EP. 06/21/1994

International Classes

A61K 031/425
A61K 047/00
A61K 009/20

Abstract

An erodible pharmaceutical composition providing a unique zero order controlled release profile is herein described. The erodible composition contains a therapeutically active substance having a solubility not greater than 80 mg/mL, a hydroxypropyl methylcellulose derivative and erosion modifiers depending on drug solubility and drug loading, such as lactose and polyoxyalkylene derivatives of propylene glycol, as well as other inert materials such as binders and lubricants. The hydroxypropyl methylcellulose derivative is most preferably a hydroxy-propylmethyl having a methoxy content of about 19-30% and hydroxypropyl content of 7-12%, a methoxy degree of substitution from 1.1 to 2.0, a molecular weight of approximately 20,000 to 26,000 daltons and a viscosity of a 2% w/w polymer solution at 25° C. ranging from 50 to 100 cps. The composition erodes with a constant erosion volume for a desired time period. When ingested, the matrix forms two layers, an outer layer of hydrated matrix which is eroding and an inner core of unchanged matrix. The composition provides a zero order release profile in part because the diffusion rate of the drug from the matrix is either negligible or is comparable to the erosion rate of the matrix and the drug concentration in the hydrated layer remains constant.

Other References

  • Theeuwes, Journal of Pharm. Sci. vol 64, No. 12, Elementary Osmotic Pump (1975)
  • Higuchi, Journal of Pharm. Sci. vol 52, No. 12, Mechanism of Sustained-Action Medication (1963)
  • Kallstrand, et al, Journal of Pharm. Sci. vol 72, No. 7, Membrane-Coated Tablets: A System for the Controlled Release of Drugs (1983
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