SACCHARIDE PROTECTIVE COATING FOR PHARMACEUTICAL PACKAGE

• US 20150126941A1
• Filed: 05/09/2013
• Published: 05/07/2015
• Est. Priority Date: 05/13/2009
• Status: Active Grant

• Current Assignee: SiO2 Medical products Inc.
• Original Assignee: SiO2 Medical products Inc.
• Inventors: Felts, John T., Fisk, Thomas E., Abrams, Robert S., Ferguson, John, Freedman, Jonathan R., Pangborn, Robert J., Sagona, Peter, Weikart, Christopher, Israelachvili, Jacob
• Granted Patent: US 9,545,360 B2
• Time in Patent Office: Days
• US Class Current: 604/230
• CPC Class Codes: A61J 1/00 Containers specially adapted for medical or pharmaceutical purposes capsules or the like for oral use A61J3/07; specially adapted for surgical or diagnostic appliances or instruments A61B50/30; containers for radioactive substances G21F5/00
• CPC Class Codes: A61J 1/05 for collecting, storing or administering blood, plasma or medical fluids multiple bags systems for separating or storing blood components A61M1/0209; Infusion or perfusion containers
• CPC Class Codes: A61J 1/1468 Containers characterised by specific material properties
• CPC Class Codes: A61J 1/2096 Combination of a vial and a syringe for transferring or mixing their contents
• CPC Class Codes: A61J 2200/50 Insulating means
• CPC Class Codes: A61L 2400/10 Materials for lubricating medical devices
• CPC Class Codes: A61L 2420/08 Coatings comprising two or more layers
• CPC Class Codes: A61L 31/10 Macromolecular materials
• CPC Class Codes: A61M 3/0262 manually, e.g. by squeezing a bulb
• CPC Class Codes: Y10T 428/1383 Vapor or gas barrier, polymer derived from vinyl chloride or vinylidene chloride, or polymer containing a vinyl alcohol unit is sandwiched between layers [continuous layer]

Abstract

A method for providing a saccharide based lubricating or protective coating or layer on a substrate surface is provided. In particular, a lubricity and/or protective coating or layer made by said method is provided. Pharmaceutical packages or other vessels coated by said method and the use of such pharmaceutical packages or other vessels protecting a compound or composition contained or received in said vessel with a protective coating against mechanical and/or chemical effects of the surface of the vessel without a protective coating material are also provided.

Claims

1. A filled package comprising:

a vessel having a lumen defined at least in part by a wall, the wall having an interior surface facing the lumen and an outer surface;

a barrier coating of SiO_x, wherein x is from 1.5 to 2.9, from 2 to 1000 nm thick, the barrier coating of SiO_x having an interior surface facing the lumen and an outer surface facing the wall interior surface, the barrier coating being effective to reduce the ingress of atmospheric gas into the lumen compared to an vessel without a barrier coating;

a protective coating or layer of a saccharide, the protective coating or layer having an interior surface facing the lumen and an outer surface facing the interior surface of the barrier coating, the protective coating or layer being effective to increase the calculated shelf life of the package (total Si/Si dissolution rate); and

a fluid composition contained in the lumen and having a pH between 5 and 9;

wherein the calculated shelf life of the package is more than six months at a storage temperature of 4°

C.

5. The filled package of claim 1, in which at least a portion of the wall of the vessel comprises:

a polyolefin,

a polyester or

a combination of a polyolefin and a polyester.

8. The filled package of claim 1, in which at least a portion of the wall of the vessel comprises or consists essentially of a member selected from the group consisting of:

a cyclic olefin polymer, a cyclic olefin copolymer, polypropylene, a polyester and polyethylene terephthalate.

18. The filled package of claim 1, in which the vessel comprises a syringe barrel or a vial.

31. The filled package of claim 1 in which the protective coating further comprises a coupling agent linking the saccharide to the SiO_x barrier coating.

32. The filled package of claim 31, in which the saccharide is a sugar that is a sorbitan or comprises hyaluronic acid.

35. The filled package of claim 31, in which the coupling agent has a functionality reactive with a saccharide hydroxyl functional group.

37. The filled package of claim 31, in which the coupling agent comprises a member selected from the group consisting of:

a silane functional group that interacts with an SiO_x barrier layer, trimethoxysilylpropyl isocyanate, and 3-Aminopropyltriethoxysilane (APTES).

41. The filled package of claim 1, in which the protective coating or layer contacting the fluid composition is between 10 and 1000 nm thick two years after the invention is assembled.

46. The filled package of claim 1, in which the rate of erosion of the protective coating or layer, if directly contacted by a fluid composition having a pH of 8, is less than 20% of the rate of erosion of the barrier coating, if directly contacted by the same fluid composition under the same conditions.

50. The filled package of claim 1, in which the rate of erosion of the protective coating or layer, if directly contacted by a fluid composition having a pH of 8, is from 5% to 20% of the rate of erosion of the barrier coating, if directly contacted by the same fluid composition under the same conditions.

54. The filled package of claim 1, in which the protective coating or layer is at least coextensive with the barrier coating.

56. The filled package of claim 1, having a shelf life, after the invention is assembled, of at least two years, in which the shelf life is determined at 4°

C.

67. The filled package of claim 1, having a shelf life, after the invention is assembled, of at least two years, in which the shelf life is determined at 20°

C.

78. The filled package of claim 1, in which the fluid composition removes the protective coating or layer at a rate of 1 nm or less of protective coating or layer thickness per 44 hours of contact with the fluid composition.

83. The filled package of claim 1, in which the protective coating or layer is effective to provide a lower frictional resistance than the uncoated interior surface, wherein the frictional resistance is reduced by at least 25% in comparison to the uncoated interior surface.

88. The invention filled package of claim 83 in which the invention is a syringe comprising a syringe barrel and a plunger and the wall defines at least a portion of the syringe barrel, in which the protective coating or layer is effective to reduce the frictional resistance between the wall and the plunger at least two years after the filled package is assembled.

97. The filled package of claim 1, in which the silicon dissolution rate by a 50 mM potassium phosphate buffer diluted in water for injection, adjusted to pH 8 with concentrated nitric acid, and containing 0.2 wt. % polysorbate-80 surfactant from the vessel is less than 170 ppb/day.

104. The filled package of claim 1, in which the total silicon content of the protective coating and barrier coating, upon dissolution into 0.1 N potassium hydroxide aqueous solution at 40°

C. from the vessel, is less than 66 ppm.

112. The filled package of claim 1, in which the calculated shelf life (total Si/Si dissolution rate) is more than 2 years.

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