A stable soluble methotrexate granule

A methotrexate and soluble technology, applied in the direction of non-central analgesics, anti-inflammatory agents, organic active ingredients, etc., can solve the problems of inaccurate dosage division of active ingredients, low oral bioavailability, difficult storage and transportation, etc. , to achieve the effect of solving inaccurate dose division, good stability and high bioavailability

Active Publication Date: 2022-01-28
济南新科医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Soluble granules can well solve the problems of inaccurate dosage division of active ingredients, poor product stability, difficult storage and transportation, etc.
However, because methotrexate is almost insoluble in water, ethanol, chloroform and ether, the oral bioavailability is very low, so far there has been no report of using methotrexate as a raw material to prepare soluble granules

Method used

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  • A stable soluble methotrexate granule
  • A stable soluble methotrexate granule

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: Preparation of soluble methotrexate granules

[0039] 1. Raw material prescription:

[0040] Methotrexate 120 grams, disodium hydrogen phosphate 68.64 grams, citric acid 75.24 grams, sodium hydroxide 60 grams, hydroxypropyl cellulose 48 grams, mannitol 150 grams, sucralose 60 grams, flavoring agent 6 grams.

[0041] 2. Preparation process:

[0042] (1) adding water to the hydroxypropyl cellulose of prescription quantity is mixed with the aqueous solution of 4wt%, for subsequent use;

[0043] (2) Weigh the methotrexate, disodium hydrogen phosphate, citric acid, sodium hydroxide, sucralose and flavoring agent in the prescribed amount, add them to the aqueous solution of step (1), and stir until fully dissolved;

[0044] (3) Preheat the prescribed amount of mannitol in a fluidized bed for 5 minutes, add the top spray into the solution in step (2) and stir until it is completely dissolved, the air temperature at the spray inlet is 70°C, the atomization press...

Embodiment 2

[0045] Embodiment 2: Preparation of soluble methotrexate granules

[0046] 1. Raw material prescription:

[0047] Methotrexate 100g, disodium hydrogen phosphate 80g, citric acid 70g, sodium hydroxide 100g, hydroxypropyl cellulose 30g, mannitol 160g, sucralose 40g, flavoring agent 10g.

[0048] The preparation process is the same as in Example 1.

Embodiment 3

[0049] Embodiment 3: Preparation of soluble methotrexate granules

[0050] 1. Raw material prescription:

[0051] Methotrexate 140 grams, disodium hydrogen phosphate 60 grams, citric acid 80 grams, sodium hydroxide 8.5 grams, hydroxypropyl cellulose 60 grams, mannitol 140 grams, sucralose 80 grams, flavoring agent 5 grams.

[0052] The preparation process is the same as in Example 1.

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Abstract

The invention discloses a stable soluble methotrexate granule, which is prepared from the following raw materials in parts by weight: 100-140 parts of methotrexate, 60-80 parts of disodium hydrogen phosphate, and 70-80 parts of citric acid , 8.5-100 parts of sodium hydroxide, 30-60 parts of hypromellose, 140-160 parts of mannitol, 40-80 parts of sucralose, and 5-10 parts of flavoring agent. In the present invention, soluble methotrexate granules are prepared directly from methotrexate for the first time. The problem of inaccurate dose division of tablets; and the soluble granules have good stability. Under normal storage conditions, the drug has a validity period of at least 2 years and high bioavailability; it is especially suitable for children or the elderly to swallow. It is difficult for patients to take it, which provides a broad prospect for the clinical application of methotrexate.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a stable soluble methotrexate granule. Background technique [0002] Methotrexate is an antiproliferative agent and immunosuppressant, since its introduction in the 1950s, it has been widely used in the treatment of cancer and immune and inflammatory diseases, such as adult rheumatoid arthritis, juvenile idiopathic Arthritis, psoriasis, etc. Especially in the clinical treatment of childhood acute lymphoblastic leukemia and juvenile idiopathic arthritis, methotrexate as a classic drug plays a key role. [0003] Methotrexate is cytotoxic, and its therapeutic window is relatively narrow. Small doses of methotrexate are less effective, or even ineffective, while large doses of methotrexate can cause severe myelosuppression, gastrointestinal reactions, renal failure, etc. Toxic side effects such as dysfunction. Therefore, strict dose control must be carried out ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/519A61K47/12A61K47/02A61K47/38A61P35/02A61P29/00A61P19/02A61P17/06
CPCA61K9/1611A61K9/1617A61K9/1623A61K9/1652A61K9/1682A61K31/519
Inventor 宋永亮马广磊李顺王宁
Owner 济南新科医药科技有限公司
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