Mercaptopurine composition freeze-drying tablet and preparation method thereof
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The technology of mercaptopurine and composition is applied in the field of mercaptopurine composition freeze-dried tablet and preparation thereof, and achieves the effects of large dissolution rate, high bioavailability, and guaranteeing curative effect and safety.
Inactive Publication Date: 2015-04-29
HAINAN WEI KANG PHARMA QIANSHAN
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[0007] Starch is the basic excipient of oral solid preparations. It is formed by the polymerization of glucose molecules. It is often used as a binder, diluent and disintegrating agent in tablets. It is cheap and easy to obtain, and is safe for the human body. However, starch is used alone as an excipient There is no report on producing mercaptopurine freeze-dried tablets by freeze-drying process
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Embodiment 1
[0026]
[0027] A. Weigh 100g of cornstarch, add 900ml of purified water and stir, use a pH regulator to control the pH of the solution at 5-7.5, then heat to 72°C and keep for 120 minutes to make 9% (W / V) cornstarch solution.
[0028] B. Measure 45ml of purified water, boil, add 85g of sucrose, stir, after dissolving, continue heating to 100°C, filter with refined cotton, wash the filter with an appropriate amount of hot distilled water, combine the lotion and filtrate, let cool, add Add appropriate amount of distilled water to make the whole volume into 100mL, stir well to obtain B solution.
[0029] C. Mix the solution obtained in step A with the solution obtained in step B, fully stir for 30 minutes, and then lower the solution to normal temperature to obtain a corn-sucrose solution.
[0030] D. Weigh 2.5 g of mercaptopurine, add it into 1 L of corn-sucrose solution, and stir for 30 minutes.
[0031] E. After measuring the content of mercaptopurine in the medicinal so...
Embodiment 2
[0034]
[0035] A. Weigh 130g of cornstarch, add 900ml of purified water and stir, use a pH regulator to control the pH of the solution at 5-7.5, then heat to 72°C and keep for 120 minutes to make 13% (W / V) cornstarch solution.
[0036] B. Measure 45ml of purified water, boil, add 85g of sucrose, stir, after dissolving, continue heating to 100°C, filter with refined cotton, wash the filter with an appropriate amount of hot distilled water, combine the lotion and filtrate, let cool, add Add appropriate amount of distilled water to make the whole volume into 100mL, stir well to obtain B solution.
[0037] C. Mix the solution obtained in step A with the solution obtained in step B, fully stir for 30 minutes, and then lower the solution to normal temperature to obtain a corn-sucrose solution.
[0038] D, take by weighing 2.5 grams of mercaptopurine (calculated as 1000 tablets), add 1L of corn-sucrose solution, and stir for 30 minutes.
[0039] E. After measuring the content o...
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Abstract
The invention provides a mercaptopurine composition freeze-drying tablet and a preparation method thereof, and relates to the technical fields of medicines and medicine production. The mercaptopurine composition freeze-drying tablet contains mercaptopurine, starch and cane sugar, wherein the starch and the cane sugar are used as auxiliary materials, and after heating technology processing is performed on common corn starch, the bonding and disintegrating functions of the starch in the tablet can be improved, and the formability of the tablet is improved; the mercaptopurine composition freeze-drying tablet only needs the starch and the cane sugar as the auxiliary materials. The mercaptopurine composition freeze-drying tablet adopts a two-drop two-rise free-drying technology, twice temperature drop and twice temperature rise can enable the tablet to be better formed, and the dissolution rate of the tablet can be increased, so that the biological availability of the tablet is improved; the tablet disclosed by the invention overcomes the defects of a common mercaptopurine tablet, and has the characteristics that the kinds and the dosage of the auxiliary materials in the mercaptopurine tablet are reduced, and the tablet has a high dissolution rate and high biological availability, so that the curative effect and the safety of clinical medication are guaranteed.
Description
technical field [0001] The invention relates to the technical field of medicine and medicine production, in particular to a mercaptopurine composition freeze-dried tablet and a preparation method thereof. Background technique [0002] Mercaptopurine is a lineage-specific drug that inhibits the purine synthesis pathway. Its chemical structure is similar to hypoxanthine, so it can competitively inhibit the conversion process of hypoxanthine. When this product enters the body, it must be produced by phosphoribosyl transferase in the cell. It is only active after conversion to 6-mercaptopurine ribonucleotide. The use of mercaptopurine to treat leukemia often produces drug resistance, which may be due to the emergence of mutated leukemia cell lines in vivo, thus losing the ability of mercaptopurine to convert mercaptopurine ribonucleotides. [0003] Molecular weight 170.19 [0004] Ordinary mercaptopurine tablets contain many types and quantities of excipients. Generally, fil...
Claims
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Application Information
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