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With the ongoing work of organ transplantation , the development of efficient , low toxicity immunosuppressant drug research has become one of the priorities . Sirolimus (Sirolimus, Rapamycin, SRL) is a novel, potent immunosuppressant , is becoming essential drugs for kidney transplant patients with long-term immunosuppressive therapy , immune to prevent organ transplant rejection . This product , developed by American Home Products , Inc. , in the United States for the first time in October 1999 , the trade name of Rapamune , first time in March 2000 are listed in the United Kingdom , Germany , Denmark , Norway , Sweden , Switzerland and other countries . Foreign listing of dosage forms for oral solution , containing the goods concentration of 1mg · mL -1 , specifications 60mL , 150mL two kinds . Sirolimus oral solution needs shading, sealed ,4-8 ℃ cold storage , valid for one year , patients taking quantitative also very inconvenient . 2001 developed by Elan Corporation sirolimus nano - crystal piece , the technology will sirolimus mixed with an aqueous solution of poloxamer and milled for 5 days under conditions of 50% of the critical speed by a ball mill to obtain a particle diameter of 400nm or less the nano- crystals. Compared with the oral solution , nanocrystals piece bioavailability increased almost doubled , indicating that the preparation of water- insoluble drugs preparations nanotechnology has broad application prospects . This subject was prepared by using high pressure homogenization techniques sirolimus nanoparticles through the screening of surfactant, the ratio of the organic phase and high pressure homogenization process parameters prepared to obtain the average particle diameter of 191.5nm , and the surface potential - 12.2mv nanoparticles. After adding suitable lyoprotectant by cryogenic freeze-drying technology prepared sirolimus nano powder , the powder in water was added after the dispersion can be quickly re - formed nanoparticle suspension . Prescription of preparations and the process of screening , the tablets prepared by direct compression sirolimus nanoparticles
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