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Entogastric lingering floating slow-release tablet for treating malignant tumor of gastrointestinal tract

A technology for gastric retention and malignant tumors, applied in the direction of antineoplastic drugs, sheet-like delivery, organic active ingredients, etc., can solve single problems, achieve the effects of reducing toxic and side effects, improving bioavailability, and improving safety

Active Publication Date: 2010-06-09
SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Both of the above-mentioned published documents are preparations with a single active ingredient, and there are no reports of gastric retention floating sustained-release tablets containing the three active ingredients of tegafur, gimeracil and oteracil potassium.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 Preparation of a gastric retention floating sustained-release tablet for the treatment of gastrointestinal malignant tumors

[0022] Components: (prescription quantity is 1000 tablets)

[0023] Tegafur 50g

[0024] Gimeracil 14.5g

[0025] Oteracil Potassium 49g

[0026] Hydroxypropyl Methyl Cellulose K100M 60g

[0027]PEG6000 10g

[0028] PVPK29 / 32 10g

[0029] Sodium bicarbonate 5g

[0030] Stearyl Alcohol 30g

[0031] Microcrystalline Cellulose 50g

[0032] 75% ethanol appropriate amount

[0033] Magnesium Stearate 3g

[0034] The tablets are prepared as described below:

[0035] Pass tegafur, gimeracil, oteracil potassium, hydroxypropyl methylcellulose K100M, PEG6000, PVPK29 / 32, sodium bicarbonate, stearyl alcohol, and microcrystalline cellulose through a 100-mesh sieve respectively; Weigh in a suitable container; add to a wet mixing granulator and mix evenly; add an appropriate amount of 75% ethanol to make soft materials; add to a swinging gra...

Embodiment 2

[0042] Example 2 A floating sustained-release tablet retained in the stomach for the treatment of malignant tumors of the gastrointestinal tract

[0043] Components: (prescription quantity is 1000 tablets)

[0044] Tegafur 50g

[0045] Gimeracil 10g

[0046] Oteracil Potassium 10g

[0047] Hydroxypropyl Methyl Cellulose K100M 100g

[0048] PEG6000 15g

[0049] PVPK29 / 32 15g

[0050] Sodium bicarbonate 10g

[0051] Octadecanol 40g

[0052] Microcrystalline Cellulose 20g

[0053] 75% ethanol appropriate amount

[0054] Magnesium Stearate 3g

[0055] The tablets are prepared as described below:

[0056] Pass tegafur, gimeracil, oteracil potassium, hydroxypropyl methylcellulose K100M, PEG6000, PVPK29 / 32, sodium bicarbonate, stearyl alcohol, and microcrystalline cellulose through a 100-mesh sieve respectively; Weigh in a suitable container; add to a wet mixing granulator and mix evenly; add an appropriate amount of 75% ethanol to make soft materials; add to a swinging gr...

Embodiment 3

[0063] Example 3 A floating sustained-release tablet retained in the stomach for the treatment of malignant tumors of the gastrointestinal tract

[0064] Components: (prescription quantity is 1000 tablets)

[0065] Tegafur 5g

[0066] Gimeracil 40g

[0067] Oteracil Potassium 40g

[0068] Hydroxypropyl Methyl Cellulose K100M 130g

[0069] PEG6000 20g

[0070] PVPK29 / 32 20g

[0071] Sodium bicarbonate 15g

[0072] Octadecanol 50g

[0073] Microcrystalline Cellulose 10g

[0074] 75% ethanol appropriate amount

[0075] Magnesium Stearate 3g

[0076] The tablets are prepared as described below:

[0077] Pass tegafur, gimeracil, oteracil potassium, hydroxypropyl methylcellulose K100M, PEG6000, PVPK29 / 32, sodium bicarbonate, stearyl alcohol, and microcrystalline cellulose through a 100-mesh sieve respectively; Weigh in a suitable container; add to a wet mixing granulator and mix evenly; add an appropriate amount of 75% ethanol to make soft materials; add to a swinging gra...

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Abstract

The invention relates to an entogastric lingering floating slow-release tablet for treating the malignant tumor of the gastrointestinal tract, which contains three active components: tegafur, gimeracil and oteracil potassium; the entogastric lingering floating slow-release tablet also contains a hydrophilic gel skeleton material, a medicine release regulation material, a foaming agent, a floating aid, a diluting agent and a lubricant; and the mole ratio of the three active components of the tegafur to the gimeracil to the oteracil potassium is 1:0.2-8:0.2-8, and the three active components account for 25-50% according to the weight percent of the tablet. The preparation can quickly float after oral administration and float above the gastric juice for a long time, and the medicines are stably, slowly and durably released, thereby generating a permanent killing function to the malignant tumor of the gastrointestinal tract. The preparation is a dosage form with the characteristics of high bioavailability, low toxic or side effect, targeting and slow release. The preparation can be applied to a patient suffering from the malignant tumor of the gastrointestinal tract.

Description

technical field [0001] The invention relates to a floating slow-release tablet retained in the stomach for treating malignant tumors of the gastrointestinal tract. In particular, the invention relates to a gastric retention floating sustained-release tablet containing three active ingredients of tegafur, gimeracil and oteracil potassium. Background technique [0002] Gastrointestinal cancer is one of the common malignant diseases in human body. According to national statistics, its incidence rate accounts for the first of all malignant tumors, accounting for about 1 / 3 of all tumors. Effective prevention and treatment of gastrointestinal malignant tumors has always been the focus of national medical and health policies. At present, the commonly used methods for the treatment of malignant tumors of the gastrointestinal tract include radical surgery, intravenous infusion of chemotherapy, and interventional therapy. [0003] Since the 1960s, 5-fluorouracil has been the basic ...

Claims

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Application Information

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IPC IPC(8): A61K31/53A61K31/506A61K31/44A61K9/70A61P35/00
Inventor 崔婧王志国朱丹吴筱昆冯汉林
Owner SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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