JP2009504616A5 - - Google Patents

Claims (13)

A pharmaceutical composition comprising at least one surface stabilizer by fine particles and the desired 7-t-butoxyiminomethylcamptothecin in a vehicle, the pharmaceutical composition fine particles is up to about 15 microns.   2. The pharmaceutical composition according to claim 1, wherein the vehicle is selected from an oil vehicle, a hydrophilic non-aqueous vehicle or a self-microemulsifying vehicle.   2. The pharmaceutical composition according to claim 1, wherein the at least one surface stabilizer is selected from hydroxymethylpropylcellulose, polyvinylpyrrolidone, Pluronic F68®, sodium dodecyl sulfate or colloidal silica.   The oil vehicle is selected from one or more of corn oil, sesame oil, olive oil, paraffin oil, soybean oil, cottonseed oil, long chain, medium chain and short chain mono, di, triglycerides and other suitable lipophilic components; The pharmaceutical composition according to claim 2. Hydrophilic non-aqueous vehicle, one or more of the following excipients polyethylene glycol glyceryl C ₆ -C 10 _- fatty acid esters, N- alkylpyrrolidones, benzyl alcohol or triethyl citrate, medicament according to claim 2 Composition. Self Micro-emulsifying vehicle of one or more lipophilic components, one or more surfactants, and optionally including one or more hydrophilic components, pharmaceutical composition according to claim 2 object.   7. A pharmaceutical composition according to claim 6 wherein the self-microemulsifying vehicle comprises corn oil mono, di and triglycerides, polyethylene glycol polyoxyl 40 hydrogenated castor oil, propylene glycol and optionally ethanol.   The pharmaceutical composition according to claim 1, further comprising a precipitation inhibitor.   The pharmaceutical composition according to claim 7, wherein the precipitation inhibitor is colloidal silica.   7-t-Butoxyiminomethylcamptothecin microparticles that are about 1 micron to about 5 microns.   11. Microparticles according to claim 10, produced by milling, high pressure homogenization or precipitation techniques. Use of the pharmaceutical composition according to claim 1 for treating a proliferative disease in a patient in need of treatment comprising administering the pharmaceutical composition according to claim 1 . Breast cancer, lung cancer, gastrointestinal cancer, colon and colorectal cancer, glioma, sarcoma, ovarian cancer, myeloma, cervical cancer, endometrial cancer, head and neck cancer, mesothelioma, renal cancer, prostate cancer, Use of a pharmaceutical composition in the manufacture of a medicament for the treatment of uterine, bladder and urethral cancer, skin cancer and melanoma.