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Stable glassy state powder formulations

Patent 6258341 Issued on July 10, 2001. Estimated Expiration Date: Icon_subject October 17, 2016. 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

Porous microspheres for drug delivery and methods for making same
Patent #: 4818542
Issued on: 04/04/1989
Inventor: DeLuca ,   et al.

Protection of proteins and the like
Patent #: 4891319
Issued on: 01/02/1990
Inventor: Roser

Low fusing temperature toner powder of cross-linked crystalline and amorphous polyester blends
Patent #: 5057392
Issued on: 10/15/1991
Inventor: McCabe, et al.

Storage of materials
Patent #: 5098893
Issued on: 03/24/1992
Inventor: Franks, et al.

Powder coating composition low Tg and high Tg polymers with acid groups
Patent #: 5098955
Issued on: 03/24/1992
Inventor: Pettit, Jr.

Method of protecting biological materials from destructive reactions in the dry state
Patent #: 5200399
Issued on: 04/06/1993
Inventor: Wettlaufer, et al.

Method of protecting biological materials from destructive reactions in the dry state Patent #: 5290765
Issued on: 03/01/1994
Inventor: Wettlaufer, et al.

Inventors

Application

No. 733225 filed on 10/17/1996

US Classes:

424/45, Organic pressurized fluid128/203.15, Particulate treating agent carried by breathed gas424/484, Matrices424/486, Synthetic polymer424/488, Polysaccharides (e.g., cellulose, etc.)424/489Particulate form (e.g., powders, granules, beads, microcapsules, and pellets)

Examiners

Primary: Page, Thurman K.
Assistant: Fubara, B.

Attorney, Agent or Firm

Foreign Patent References

  • 0524748 A1 EP. 06/13/1992
  • 0 520 748 A1 EP. 12/13/1992
  • WO 95/05805 WO. 03/13/1995
  • WO 96/33744 WO. 10/13/1996
  • WO 97/41031 WO 11/13/1997
  • WO 97/41833 WO 11/13/1997

International Class

A61K 009/12

Abstract

A powdered, dispersible composition having stable dispersibility over time is provided. The composition exhibits a characteristic glass transition temperature (Tg) and a recommended storage temperature (Ts), wherein the difference between Tg and Ts is at least about 10° C. (i.e. Tg -Ts is greater than 10° C.). The composition comprises a mixture of a pharmaceutically-acceptable glassy matrix and at least one pharmacologically active material within the glassy matrix. It may be further mixed with a powdered, pharmaceutically-acceptable carrier.It is particularly valuable in unit dosage from having a moisture barrier, in combination with appropriate labelling instructions.A process for producing a powdered dispersible composition is also provided, wherein the process comprises removing the solvent from a solution comprising a solvent, a glass former and a pharmacologically active material under conditions sufficient to form a glassy matrix having the pharmacologically active material within the matrix.

Other References

  • Angell, (1995) "Formation of Glasses from Liquids and Biopolymers," Science 267:1924-1935
  • Clark, et al., (1996) "The Balance Between Biochemical and Physical Stability For Inhalation Protein Powders: rhDNASE As An Example," Respiratory Drug Delivery V 167-174
  • Faldt and Bergenstahl, (1994) "The Surface Composition of Spray-Dried Protein-Lactose Powders," Colloids and Surfaces A: Physiochemical and Engineering Aspects 90:183-190
  • Fox, (1995) "Putting Proteins Under Glass," Science 267:1922-1923
  • Franks, (1993) "Solid Aqueous Solutions," Pure & Appl. Chem. 65:2527-2537
  • Franks, et al. (1992) "Materials Science and the Production of Shelf-Stable Biologicals," Pharmaceutical Technology 32-50
  • Franks, (1989) "SEPARATION, Improved Freeze-Drying, An Analysis of the Basic Scientific Principles," Process Biochemistry 24:R3-R7
  • Franks and Murase, (1992) "Nucleation and Crystallization In Aqueous Systems During Drying: Theory and Practice," Pure & Appl. Chem. 64:1667-1672
  • Gibbs and DiMarzio, (1958) "Nature of the Glass Transition and the Glassy State," The Journal of Chemical Physics 28:373-383
  • Roos and Karel, (1990) "Differential Scanning Calorimetry Study of Phase Transitions Affecting the Quality of Dehydrated Materials," Biotechnol. Prog. 6:159-163
  • Slade and Levine, (1988) "Non-equilibrium Behavior of Small Carbohydrate-Water Systems," Pure & Appl. Chem. 60:1841-1864
  • Wolanczyk, (1989) "Differential Scanning Calorimetry Analysis of Glass Transitions," Cryo-Letters 10:73-7
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