SMANCS (Styrene Maleic Acid Neocarzinostatin) oily preparation, preparation method and application
A preparation and oil-based technology, applied in the field of chemical drugs, can solve the problems of fluctuation of treatment results, standardization of unfavorable treatment, prolongation of operation preparation time, etc., and achieve the effect of convenient and standardized clinical use, increased indications for treatment, and simplified treatment application.
Inactive Publication Date: 2013-05-22
GCA MEDICAL
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[0003] [3] In terms of chemical structure, SMANCS is a high-molecular anticancer agent composed of protein anticancer drug New Carcinogen (NCS) and styrene maleic acid polymer (SMA). The compound connects two amino groups on NCS through an amide to form the following macromolecular structure: (SMA)--(NCS)--(SMA), which has a molecular weight of 15,000 and is a macromolecular drug that is usually stable. Poor sex
[0005] [5] This method has the following problems in clinical treatment: 1) the drug may be inactivated when stored in cold storage and at room temperature; 2) the drug needs to be prepared in two preparations (SMANCS and iodinated Oil), ultrasonic treatment and mixing at the medical site, this method of operation results in prolonged operation preparation time; 3) Due to the temporary preparation on site, the doctor cannot effectively adjust the drug dose during the operation, such as increasing or decreasing the dose; 4) Because different doctors or assistant doctors have different proficiency in on-site mixing and preparation, the mixing of drugs is prone to individual deviations due to differences in implementers, resulting in fluctuations in treatment results, which is not conducive to the standardization of treatment
[0006] [6] In recent studies, those skilled in the art have tried to make SMANCS into oral preparations to increase the convenience of use. However, considering the biological characteristics and large molecular weight of SMANCS, it is not easy for the protein and polypeptide digestive juice in the human body. Absorbed, the body's utilization is low
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Embodiment 2
[0043] [43] SMANCS and iodized oil were respectively added with cholesterol to make the cholesterol content 1%, 2%, 4%, 5%, 6%, and 8%, to make 1.5mg / ml oily preparations.
[0044] [44] Example 3
[0045] [45] SMANCS and iodized oil were added with palmitic acid to make the content of palmitic acid 5% and 10%, respectively, to make 1.5mg / ml oily preparation.
[0046] [46] Example 4
[0047] [47] SMANCS and iodized oil were added with nitroglycerin to a concentration of 10 μg / ml to prepare two 1.5 mg / ml tumor-selective enhanced oily preparations.
[0048] [48] Example 5
[0049] [49] SMANCS and iodized oil were added with palmitic acid to a concentration of 5% and 10%, and nitroglycerin to a concentration of 10 μg / ml to prepare two 1.5 mg / ml tumor-selective enhanced oily preparations.
[0050] [50] Example 6
[0051] [51] SMANCS and iodized oil were added with cholesterol to a concentration of 5% and 8%, and nitroglycerin was added to a concentration of 10 μg / ml to prepar...
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The invention discloses an SMANCS (Styrene Maleic Acid Neocarzinostatin) oily preparation. The SMANCS oily preparation is a single preparation and comprises active ingredients listed in (1): SMANCS, namely styrene maleic acid neocarzinostatin, is a chemically combined body of a neocarzinostatin NCS and a copolymer of styrene and maleic acid SMA; and (2) oily materials with good biocompatibility, comprising iodized oil. The oily preparation disclosed by the invention overcome the defects of complex storage conditions and inconvenient clinical application of the traditional SMANCS and has the effects of being convenient to use and flexible in medicine concentration regulation.
Description
technical field [0001] [1] The utility model relates to an oily preparation of a macromolecular anticancer drug SMANCS, which has the characteristics of high stability in biological activity and convenient clinical application, and belongs to the field of chemical drugs. Background technique [0002] [2] SMANCS was developed by Maeda Hiroshi et al., the world's earliest macromolecular anticancer drug (references: Maeda H, Ueda M, Morinaga T, Matsumoto T, Conjugation of poly(styrene-co-maleic acid) Derivatives to the antitumor protein neocarzinostatin: pronounced improvements in pharmacological properties, J Med Chem.28 (4): 455-61, 1985), can be applied to the treatment of various tumors, as a therapeutic drug for primary liver cancer (hepatocellular carcinoma) In 1993, the method of arterial injection with iodized oil (lipiodol) as the carrier was approved by the Ministry of Health, Labor and Welfare of Japan. [0003] [3] In terms of chemical structure, SMANCS is a high-m...
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IPC IPC(8): A61K9/10A61K38/16A61K45/00A61K47/44A61P35/00
Inventor 前田浩方军
Owner GCA MEDICAL
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