Stable 40-O-(2-ethoxyl)-rapamycin tablet and preparation method thereof

The technology of rapamycin tablets and rapamycin, which is applied in the field of medicine, can solve problems such as hidden safety hazards, multiple impurities, and poor stability, and achieve the effects of reducing equipment requirements, simplifying process steps, and reducing hygroscopicity.

Pending Publication Date: 2022-07-22
杭州华东医药集团康润制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its disadvantage is that the micronization of 40-O-(2-hydroxyethyl)-rapamycin requires an increase in equipment performance, and causes 40-O-(2-hydroxyethyl)-rapamycin loss, which increases the Production cost; 40-O-(2-hydroxyethyl)-rapamycin has reproductive toxicity, which brings safety hazards to personnel when micronized, and requires corresponding protective measures; During storage, its stability will be deteriorated and more impurities will be produced

Method used

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  • Stable 40-O-(2-ethoxyl)-rapamycin tablet and preparation method thereof
  • Stable 40-O-(2-ethoxyl)-rapamycin tablet and preparation method thereof
  • Stable 40-O-(2-ethoxyl)-rapamycin tablet and preparation method thereof

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Effect test

Embodiment 1

[0038] Table 1

[0039] composition batch / g 40-O-(2-hydroxyethyl)-rapamycin 15 2,6-Di-tert-butyl-4-methylphenol 0.3 Hypromellose 60 Hypromellose 75 anhydrous lactose 595.95 Magnesium stearate 3.75 Acetone, absolute ethanol mixture (1:1) 750

[0040] Preparation Process:

[0041] Add 40-O-(2-hydroxyethyl)-rapamycin, 2,6-di-tert-butyl-4-methylphenol and part of hypromellose into absolute ethanol and acetone to dissolve, spray Add the remaining amount of hypromellose and part of the anhydrous lactose into the fluidized bed granulation to obtain dry granules for granulation, and uniformly mix with the remaining amount of anhydrous lactose and magnesium stearate, and then tableting can be obtained.

Embodiment 2

[0043] Table 2

[0044] composition batch / g 40-O-(2-hydroxyethyl)-rapamycin 15 2,6-Di-tert-butyl-4-methylphenol 0.3 Hypromellose 30 Hypromellose 105 anhydrous lactose 595.95 Magnesium stearate 3.75 Acetone, absolute ethanol mixture (1:1) 1200

[0045] Preparation Process:

[0046]Add 40-O-(2-hydroxyethyl)-rapamycin, 2,6-di-tert-butyl-4-methylphenol, and hypromellose into absolute ethanol and acetone to dissolve, spray into The hypromellose is subjected to fluidized bed granulation, and the obtained dry granules are granulated, mixed with anhydrous lactose and magnesium stearate, and pressed into tablets.

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Abstract

The invention provides a stable 40-O-(2-ethoxyl)-rapamycin tablet and a preparation method thereof, and relates to the technical field of medicines, the 40-O-(2-ethoxyl)-rapamycin tablet specifically comprises the following raw materials: 40-O-(2-ethoxyl)-rapamycin, an antioxidant, an adhesive, an organic solvent and auxiliary materials; the antioxidant is 2, 6-di-tert-butyl-4-methylphenol, and the solvent is a solvent; the adhesive comprises one or more of hydroxy propyl cellulose, hydroxypropyl methylcellulose and povidone; the organic solvent comprises one or more of absolute methanol, absolute ethyl alcohol, acetone and dichloromethane; the auxiliary material comprises one or more of a carrier, a filling agent and a lubricating agent. The prepared tablet is good in dissolution rate and high in stability.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a stable 40-O-(2-hydroxyethyl)-rapamycin tablet and a preparation method thereof. Background technique [0002] 40-O-(2-hydroxyethyl)-rapamycin is an inhibitor of mTOR (mammalian target of rapamycin), a serine-threonine kinase downstream of the PI3K / AKT pathway. 40-O-(2-hydroxyethyl)-rapamycin was first developed by Novartis in Switzerland under the trade name certican. [0003] In 2010, 40-O-(2-hydroxyethyl)-rapamycin was approved to prevent organ rejection in heart and kidney transplant patients. In addition, in addition to renal cell carcinoma and post-transplant rejection, 40-O-(2-hydroxyethyl)-rapamycin is being tested for neuroendocrine tumors, lymphomas, other cancers, and tuberous sclerosis complex. Study how it can be used as a single agent or with existing cancer treatments. [0004] 40-O-(2-hydroxyethyl)-rapamycin is a derivative of sirolimus (also known as rapamyc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/436A61K47/38A61K47/32A61K47/10A61K47/08A61P37/06
CPCA61K9/2054A61K9/2027A61K9/2013A61K31/436A61P37/06
Inventor 马雯霞唐建飞余龙赵福斌朱颖谢红瑜戚兰君周璐
Owner 杭州华东医药集团康润制药有限公司
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