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Method for preparing tablet of hydroxy camptothecin and application of oral application

A technology of hydroxycamptothecin and hydroxycamptothecin, which is applied in the field of preparation of antineoplastic drug hydroxycamptothecin tablets, can solve the problems of low blood drug concentration, drug difficulty, and low bioavailability, so as to extend the validity period and prevent Good oxidation and stability

Inactive Publication Date: 2008-04-02
黄石燕舞药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Because hydroxycamptothecin is insoluble in water and has poor ester solubility, the direct compression of unopened hydroxycamptothecin (C-HCPT) makes it difficult for the drug to enter the blood after oral administration by the human body. Therefore, hydroxycamptothecin (C-HCPT) HCPT) Tablets prepared by conventional methods have extremely low blood drug concentration after oral administration to the human body, that is, their bioavailability is on the low side when the bioavailability test is carried out
Difficult to achieve clinical efficacy

Method used

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  • Method for preparing tablet of hydroxy camptothecin and application of oral application
  • Method for preparing tablet of hydroxy camptothecin and application of oral application

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Experimental program
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Effect test

Embodiment 1

[0029] Hydroxycamptothecin 2%

[0030] 2% Sodium Carbonate Appropriate amount

[0031] Starch 35%

[0032] Microcrystalline Cellulose 35%

[0033] Glycine 22%

[0034] Sodium Carboxymethyl Starch 5.7%

[0035] Magnesium Stearate 0.3%

[0036] The preparation method of hydroxycamptothecin tablet, the steps are as follows:

[0037] (1) 350 grams of starch, 350 grams of microcrystalline cellulose, and 57 grams of sodium carboxymethyl starch in the prescription were respectively passed through an 80-mesh sieve, and 4% starch slurry was prepared for subsequent use.

[0038] (2) Mix the excipients (except magnesium stearate) in the prescription evenly and set aside.

[0039] (3) Add an appropriate amount of 2% sodium carbonate solution to hydroxycamptothecin to dissolve it, add aminoacetic acid to adjust the pH value to 9-9.5, put it in a freeze dryer, and put it in a vacuum of 0.01mbar at -55°C , freeze-dried for 36 hours, and collected the dried product to obtain ring-opene...

Embodiment 2

[0044] Hydroxycamptothecin 5%

[0045] 0.8% sodium hydroxide appropriate amount

[0046] Starch 34.5%

[0047] Microcrystalline Cellulose 34.5%

[0048] Glycine 20%

[0049] Sodium Carboxymethyl Starch 5.7%

[0050] Magnesium Stearate 0.3%

[0051] The preparation method of hydroxycamptothecin tablet, the steps are as follows:

[0052] (1) Pass 414 grams of starch, 414 grams of microcrystalline cellulose, and 68.4 grams of sodium carboxymethyl starch in the prescription respectively through an 80-mesh sieve, and prepare 4% starch slurry for subsequent use.

[0053] (2) Mix the above-mentioned auxiliary materials (except magnesium stearate) evenly for subsequent use respectively.

[0054] (3) Add 60 grams of hydroxycamptothecin to an appropriate amount of 0.8% sodium hydroxide solution to dissolve it, add aminoacetic acid to adjust the pH value to 9-9.5, put it in a freeze dryer, and put it in a vacuum of 0.01mbar at -55°C Under certain conditions, freeze-dry for 36 hour...

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Abstract

An orally-taken tablet of hydroxycamptothecin for treating cancer is prepared from using the pharmacologically acceptable alkali solution to open the lactone ring in hydrocamptothecin, and conventional steps.

Description

1. Technical field [0001] The invention belongs to a preparation method of an antineoplastic drug hydroxycamptothecin tablet, in particular to a preparation method and an oral application of a human body-absorbable hydroxycamptothecin tablet. 2. Background technology [0002] Hydroxycamptothecin is a natural plant alkaloid extracted from the fruit of the unique plant Camptotheca acuminate Decsne in my country. It is the only anticancer drug that acts on topoisomerase I (TOPO I) so far. It can inhibit Topoisomerase I (TOPO I), causes DNA single-strand breaks, inhibits DNA replication, acts on the S phase of cells, and at the same time inhibits the formation of new blood vessels around tumor cells, induces cancer cell apoptosis, and eventually leads to cancer cells death. [0003] Hydroxycamptothecin has the characteristics of broad anti-cancer spectrum and definite curative effect. At present, there are injections and freeze-dried powder injections used clinically in China, w...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/475A61K9/20A61P35/00
Inventor 陈秀珍肖文辉王群
Owner 黄石燕舞药业有限公司
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