| According to World Cancer Report issued by World Health Organization (WHO) on April 3rd, 003, the incidence of cancer around the world will increase 50 percent, and cancer cases will amount to 15 million by 2020 from the tendency of present cancer incidence. At present, the highest incidence of disease is lung cancer, with which annual cases are 1.2 million, and breast carcinoma is in the second place with annual cases about 1 million; and then intestinal cancer (0.94 million), carcinoma ventriculi (0.87 million), liver cancer (0.56 million), cervical carcinoma (0.47 million), oesophagus cancer (0.41 million), etc. Of those mentioned above, lung cancer, carcinoma ventriculi, and liver cancer are of highest execution, which account for 17.8, 10.4, and 8.8 percent of the death toll. In addition, the developed countries such as the United States of America, Italy, Australia, Germany, Netherlands, Canada and France, etc. are among those countrieswith high incidence of cancer, whereas some developing countries in Northern Africa, Southern and Eastern Asia are among those with low incidence. Cancer is one of chronic and stubborn diseases. In China, the highest incidences of cancer are carcinoma ventriculi, lung cancer, intestinal cancer, liver cancer, and breast carcinoma, etc. Medication, as one of major means to cure cancer, develops rapidly in recent years.Vinorelbine, whose tartrate can be used as an anti-cancer drug, comes from vincaleuucoblastine with the change of its chemical strcture. It is produced by French Pieree Fabre Medicament Company with the name of Eunodes. Granted by FDA in 1995, it was produced and put onto market by Glaxowellcom Company with the name of Navelbine. It has a special effect in treating lung cancer, and can also be used in the treatment of breast cancer, ovarian cancer, and prostatic carcinoma, etc. Vinca, belong to dogbane family, is very common in SouthChina. Vincaleuucoblastine and vincristine from vinca have been widely applied in clinic antineoplastic treatment. Vinorelbine, a kind of semisynthesis alkaloid belonging to vinca, has changed its annulus from 9 to 18, its forms are intended for nutrient solution, and its specification is 10 mg/10 ml. Vinorelbine, as a broad-spectrum drug, has similar function on division canaliculus with vincaleuucoblastine and vincristine, but has less function on nerve axons microtubule. As a result, it is strongly antineoplastic. As for the treatment of no small cell lung cancer, this drug has similar or stronger effects with vinca alkaloid and other common drugs such as ifosfamide, cisplatin, mitomycin C, and adriamycin, etc. In addition, this drug also has good effects on indolent ovarian cancer and breast cancer at the advanced stage.According to clinic treatment, Vinorelbine is similar in antineoplastic activity with anthracene nucleus drugs. From An Analysis of Antineoplastic Drugs in 138 Hospitals inYangtze River Basin and the Tendency, the amount of Vinorelbine is in the 7th place with 7.72 million yuan in 1999, 8.59 million in 2000, and 15.09 million in 2001.Due to its unique production process, freeze drier provides a stable manufacturing means to many drugs, in particular, macromolecular drugs sensitive to temperature and those unstable in aqueous solution. Since its validity period is only one year, vinorelbine brings much inconvenience in the management and to users. As a result, this research changes its formulation to enable it more stable and convenient for clinic treatment. For sake of the proper and secure clinic application, an affecting factor experiment is conducted as to tartaric vinorelbine from various aspects such as .light, heat, humidity, acid, alkali, oxidation, reduction and degradation, etc. The experiment indicates that the samples are unstable in the environment of light and that degradation is obvious in heat. Tartaric vinorelbine requires keeping inlow temperature and in dark place. In the meantime, the production process also requires low temperature, dark place and control of PH. Through the affecting factor experiment, the impurity of the samples is analyzed to detect possible conditions, which provides necessary theoretical basis for such quality controls as production process control and sample preservation.Retartaric vinorelbine injection is produced with mannitol as excipient, controlling solution (PH value 3.0～4.5) and 0.03% charcoal injection by the means of freezing and drying in the approach of comparative experiment.After studying the its stability in high temperature and light, retartaric vinorelbine injection falls in content when it is put for 10 days at the temperature of 40℃, some related substances rise, in a light test of 4500Lx, the physical form of its samples changes from light white to light yellow, with the content falling and some related substances rising,degradation products larger than 2.5%, which means this solution should be stored in low temperature and dark place.After studying its stability in gluon and sodium chloride injections, the clarity of retartaric vinorelbine injection meets the requirements when it is in gluon and sodium chloride injections without iridescence, mud or precipitation, and its content has no obvious changes.After studying its stability under the condition of accelerated experiment and long-term sample test, the index of retartaric vinorelbine injection's physical form characters, content and some related substances have no obvious changes at the temperature of 25℃±2℃, the humidity of 60%±10% in a 6-month accelerated test; at 6℃±2℃in a 6-month long-term test, all indicators have no changes.Retartaric vinorelbine injection is stable, quality-controllable and effective.
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