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• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K31/00—Medicinal preparations containing organic active ingredients
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P35/00—Antineoplastic agents
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P9/00—Drugs for disorders of the cardiovascular system
  • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Definitions

• the ethyleneimines and methylmelamines include the compounds triethylenemelamine, thiotepa (triethylene thiophosphoramide) and altretamine (hexamethylmelamine).
• Thiotepa and its primary metabolite, triethylenephosphoramide are capable of fo ⁇ ning DNA cross-links, as the aziridine rings open after protonation of the ring-nitrogen, leading to a reactive molecule.
• the alkyl sulfonates include busulfan.
• the nitrosoureas include carmustine and lomustine, semustine and streptozocin.
• the triazenes include dacarbazine.
• the alkylating agent melphalan was incorporated into polymer stents and implanted into pig coronary arteries, and this study will now be discussed.
• stents as depicted in Fig. 3C were prepared and loaded with melphalan and then placed in the coronary arteries of pigs. Preparation of the melphalan-loaded stents is described in Example 3.
• the stents, which carried a total drug load of 546 ⁇ g, were deployed into the pig coronary artery using a balloon catheter and positioned distally in the right coronary artery and approximately in the middle of the left circumflex artery.
• a commercially available metal stent not carrying a polymer member was also deployed into the left anterior descending artery.
• Stents carrying four polymer sleeve segments were prepared as described in Example 2.
• a solution of melphalan in methanol was prepared by dissolving 0.0293 g melphalan in 1.5 mL methanol to give a solution concentration of 19.5 ⁇ g/ ⁇ L.
• Each of the four segments was loaded with 136.5 ⁇ g of melphalan from the stock solution by pipetting 1 ⁇ L of the solution on each segment 7 times.
• the total drug loading in the polymer stent was 546 ⁇ g.
• the pig was euthanized and the heart and coronary arteries explanted.
• the arteries were pressure fixed for mo ⁇ hometric analysis to determine the percent diameter stenosis and percent intimal growth.
• the percent diameter stenosis was taken as l-[(stented vessel's minimum lumenal diameter)/(diameter of unstented reference vessel)]*100.
• the percent intimal growth was taken as l-[(stented vessel's minimum lumenal diameter)/(diameter of stented portion prior to stent placement)]* 100.
• the balloon to artery ratio was also determined as a measure of the degree of distension of the vessel by the balloon. The results are shown in Table 1.
• a solution of busulfan in dimethylsulfoxide was prepared by dissolving 0.0243 g busulfan in 300 ⁇ L dimethylsulfoxide to give a solution concentration of 81 ⁇ g/ ⁇ L.
• Each of the four segments was loaded with 81 ⁇ g of busulfan from the stock solution by pipetting 1 ⁇ L of the solution on each segment.
• the total drug loading in the polymer stent was 162 ⁇ g-

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• Health & Medical Sciences (AREA)
• Public Health (AREA)
• Medicinal Chemistry (AREA)
• Life Sciences & Earth Sciences (AREA)
• Pharmacology & Pharmacy (AREA)
• Chemical & Material Sciences (AREA)
• General Health & Medical Sciences (AREA)
• Veterinary Medicine (AREA)
• Animal Behavior & Ethology (AREA)
• Engineering & Computer Science (AREA)
• Organic Chemistry (AREA)
• General Chemical & Material Sciences (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Cardiology (AREA)
• Heart & Thoracic Surgery (AREA)
• Urology & Nephrology (AREA)
• Vascular Medicine (AREA)
• Epidemiology (AREA)
• Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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• 2000
  • 2000-02-10 EP EP00914574A patent/EP1150670A2/de not_active Withdrawn
  • 2000-02-10 CA CA002362883A patent/CA2362883A1/en not_active Abandoned
  • 2000-02-10 JP JP2000598150A patent/JP2002536406A/ja active Pending
  • 2000-02-10 WO PCT/US2000/003667 patent/WO2000047197A2/en not_active Application Discontinuation
  • 2000-02-10 AU AU35947/00A patent/AU3594700A/en not_active Abandoned

Non-Patent Citations (1)

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