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Metoclopramide composition freeze-dried tablet and preparation method thereof

A technique of metoclopramide and a composition is applied in the field of metoclopramide composition freeze-dried tablet and preparation thereof, and achieves the effects of improving adhesion, high bioavailability and improving bioavailability

Inactive Publication Date: 2015-05-13
HAINAN WEI KANG PHARMA QIANSHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] 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 the production of metoclopramide freeze-dried tablets by freeze-drying process

Method used

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  • Metoclopramide composition freeze-dried tablet and preparation method thereof
  • Metoclopramide composition freeze-dried tablet and preparation method thereof
  • Metoclopramide composition freeze-dried tablet and preparation method thereof

Examples

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Effect test

Embodiment 1

[0029]

[0030] A. Weigh 100g of cornstarch, add 900ml of purified water and stir, use a pH regulator to control the pH of the solution at 2.5-4.5, then heat to 72°C and keep for 120 minutes to make 9% (W / V) cornstarch solution.

[0031] B. Measure 45ml of purified water, boil it, 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.

[0032] 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.

[0033] D. Weigh 5 g of metoclopramide, add it into 1 L of corn-sucrose solution, and stir for 30 minutes.

[0034] E. After measuring the content of metoclopramide in the medicinal...

Embodiment 2

[0037]

[0038]

[0039] A. Weigh 130g of corn starch, add 900ml of purified water and stir, use a pH regulator to control the pH of the solution at 2.5-4.5, then heat to 72°C and keep for 120 minutes to make 13% (W / V) cornstarch solution.

[0040] B. Measure 45ml of purified water, boil it, 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.

[0041] 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.

[0042] D, take by weighing 5 grams of metoclopramide (calculated as 1000 tablets), add 1L corn-sucrose solution, and stir for 30 minutes.

[0043] E. After measuring ...

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Abstract

The invention provides a metoclopramide composition freeze-dried tablet and a preparation method thereof, and relates to the technical field of medicines and medicine production. The metoclopramide composition freeze-dried tablet comprises metoclopramide, starch and cane sugar, wherein the starch and the cane sugar are taken as auxiliary materials. Common corn starch is treated by a heating technique, so that the bonding and disintegration functions of the starch in the tablet can be improved, and the formability of the tablet is improved. The metoclopramide composition freeze-dried tablet only needs two auxiliary materials namely the starch and the cane sugar. The metoclopramide composition freeze-dried tablet adopts a twice-temperature-reduction and twice-temperature-rise freeze-drying technique, and due to twice temperature reduction and twice temperature rise, the formability of the tablet is better, and the dissolution rate of the tablet is improved, so that the bioavailability of the tablet is improved; the tablet overcomes the defects of a common metoclopramide tablet, the types and the quantities of the auxiliary materials in the metoclopramide tablet are reduced, the dissolution rate of the tablet is large, the bioavailability of the tablet is high, and the curative effect and the safety of clinical medication are ensured.

Description

technical field [0001] The invention relates to the technical field of medicine and medicine production, in particular to a freeze-dried tablet of a metoclopramide composition and a preparation method thereof. Background technique [0002] Metoclopramide is prepared from p-aminosalicylic acid through esterification, acylation and methylation to obtain methyl p-acetamido-o-methoxybenzoate, and then through chlorination, amination and hydrolysis. [0003] This product is a dopamine 2 (D2) receptor antagonist, and also has a serotonin 4 (5-HT4) receptor agonist effect, and has a mild inhibitory effect on 5-HT3 receptors. It can act on dopamine receptors in the medullary emetic chemoreceptor zone (CTZ) to increase the threshold of CTZ, and has a strong central antiemetic effect. This product can also block dopamine receptors in the hypothalamus, inhibit prolactin inhibitory factor, and promote the secretion of prolactin, so it has a certain prolactin effect. It has less inhibi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/166A61K47/36A61K47/26A61P1/08
Inventor 王丹石金友汪金灿郝结兵吴函峰
Owner HAINAN WEI KANG PHARMA QIANSHAN
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