Medical implants containing fk506 (tacrolimus) methods of making and methods of use thereof

a technology of tacrolimus and implants, which is applied in the field of implants, can solve the problems of affecting affecting the quality of the implant, and affecting the quality of the implant, and none of the active agents have been able to reduce the restnosis significantly, and agents delay the healing of the vessel wall injury

Inactive Publication Date: 2012-09-20
ASTELLAS PHARMA INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0146]The release of FK506 were determined by HPLC determination of the amount of FK506 in the blood of the rabbits after 1 hr, 8 hr, 24 hr and 48 hr. FIG. 6 is a graph showing the release of FK506 over time. The rabbits were sacrificed after 28 days, and the implanted stents were examined. The area of newly grown intima (neointima) within the stent was quantified under the optical microscope, and is reported in FIG. 7. There is a reduction of 53% in the formation of neointima for stents loaded with 60 μg of FK506 compared with bare stents. This reduction in neointima formation was accompanied by a detectable decrease in the foci of inflammation. The formation of macrophages and lymphocytes is shown in FIG. 8. The use of stents with a ceramic coating onto which FK506 is applied thus leads to a distinct reduction in neointima and in foci of inflammation after the implantation.

Problems solved by technology

These operations are moreover relatively complicated and costly and involve the risk of serious complications.
Unfortunately, to date none of these active agents have been able to reduce restenosis significantly (Gruberg et al., Exp. Opin. Invest. Active agents 9 (2000) 2555-2578).
On the other hand, this agent delays healing of vessel wall injury caused by balloon angioplasty and stent implantation.

Method used

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  • Medical implants containing fk506 (tacrolimus) methods of making and methods of use thereof
  • Medical implants containing fk506 (tacrolimus) methods of making and methods of use thereof
  • Medical implants containing fk506 (tacrolimus) methods of making and methods of use thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0105]Loading of Selected Active Agents onto Stent Grafts

[0106]All values are stated in μg.

TABLE 1Active agentFK 506Pac-type of(tacro-Vin-litaxelCis-Mitoxan-stentlimus)blastine(Taxol)platintroneA1382412815*116167112515514*142162523814814*113Average155914614414 124B181621Average18C194165Average180*measured by AASA: Experiments with dissolved solids in which stent grafts with a PTFE polymer layer were immersed in the solution.B: Experiments with i.v. solutions in which stent grafts with a PTFE polymer layer were immersed in the solution.C: Experiments with i.v. solutions in which polyurethane-coated stents were immersed in the solution.

example 2

Release Patterns of Various Stent Grafts and Stents Having Polymeric Coating of the Present Invention:

[0107]All values are stated in μg.

[0108]To analyze the active agent release, a stent was incubated at 37° C. in 10 ml of PBS buffer (stabilized with Na azide) at 37° C. After defined periods of time had elapsed, 2×1 ml of the solution were removed and analyzed. These 2 ml were replaced by fresh PBS buffer (stabilized with Na azide).

[0109]The tables reflect the total released content of active agent in the solution., ie., the amounts of active agent in the buffer volume removed for the analysis are accumulated with amounts detected in subsequent samples.

TABLE 2ActiveVinblastineagent / after 96 hrTypeafter 1 hrafter 3 hrafter 8 hrafter 24 hrafter 72 hrA73 and108 and121 and106 and132 and75114126120140Average:Average:Average:Average:(96 hr)74109124113Average:13637 and48 and47 and57 and56 and4151586257Average:Average:Average:Average:(72 hr)39504260Average:5780 and99 and108 and117 and113 an...

example 3

Production Process (1) for FK506-Coated Stents:

[0110]10 mg of FK506 are dissolved in 3 ml of ethanol.[0111]Uncoated stainless steel stents are immersed in the solution at room temperature under vacuum overnight.[0112]Wash three times with saline for 1 minute.[0113]Dry overnight.

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Abstract

Implants and methods of making same are provided for treatment or prophylaxis of coronary or peripheral vascular constrictions or vascular occlusions, and particularly, stenoses or restenoses, that comprise FK506 in chemically covalently bound, non-covalently bound or physically immobilized form.

Description

FIELD OF THE INVENTION[0001]The present invention relates to implants for the treatment or prophylaxis of coronary or peripheral vascular occlusions or vascular constrictions that comprise FK506 (Tacrolimus) in chemically covalently bound or non-covalently bound or physically immobilized form, processes for the production thereof and to the use thereof.BACKGROUND OF THE INVENTION[0002]The formation of arteriosclerotic lesions in arterial blood vessels is the underlying disease for a large range of clinical symptoms which extend from angina pectoris via intermittent claudication to myocardial infarction and ischemic stroke; all based on atheroma formation and / or stenotic lesions. The term stenotic lesions refers to the local reduction of the vascular lumen to less than 60-70% of its normal diameter, which in turn leads to a marked reduction in the supply of oxygen and nutrients to the particular tissue. Although pharmacotherapy (statins, ACE inhibitors, gpIIa / IIIb blockers and plasmi...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61F2/82B05D3/10A61L33/00A61F2/06A61L27/04A61L27/14A61L31/16A61M25/12
CPCA61L31/16A61L2300/606A61L2300/416A61F2/06A61F2/82A61L27/04A61L27/14
Inventor WNENDT, STEPHANVON OEPEN, RANDOLFKUTTLER, BERNDLANG, GERHARDLORENZ, GUENTERGRANDT, AXEL
Owner ASTELLAS PHARMA INC
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