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MTOR inhibitor and pharmaceutical composition, and application thereof

A technology of inhibitors and compositions, applied in the field of pharmaceutical compositions, mTOR inhibitors, capable of solving problems such as complex interactions

Inactive Publication Date: 2019-07-26
SHENYANG FUYANG PHARM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] What is more noteworthy is that there are multiple crosstalk phenomena between PI3K / AKT / mTOR and ERK / MAPKs signaling pathways to form complex interactions

Method used

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  • MTOR inhibitor and pharmaceutical composition, and application thereof
  • MTOR inhibitor and pharmaceutical composition, and application thereof
  • MTOR inhibitor and pharmaceutical composition, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Embodiment 1, isovalerylspiramycin I or isovalerylspiramycin II or isovalerylspiramycin III tablet

[0108] Specification: 200mg / 350mg

[0109] Tablet prescription:

[0110]

[0111] Coating Solution Prescription:

[0112]

[0113] Preparation Process:

[0114] Preparation of the tablet core: the main drug and auxiliary materials are respectively passed through a 100-mesh sieve, and the prescription amount of isovalerylspiramycin I or isovalerylspiramycin II or isovalerylspiramycin III, microcrystalline cellulose and 1 / 2 The prescription amount of sodium starch glycolate is mixed evenly, then add 5% povidone K 30 The soft material made from aqueous solution is granulated with a 18 mesh sieve, and the wet granules are dried at 60°C under ventilated conditions for 2 hours; after drying, the granules are sieved with an 18 mesh sieve, and then add 1 / 2 of the prescription amount of sodium carboxymethyl starch and stearic acid After the magnesium was evenly mixed, t...

Embodiment 2

[0117] Embodiment 2, isovalerylspiramycin I or isovalerylspiramycin II or isovalerylspiramycin III plain sheet (calculated by 10000 pieces)

[0118] prescription:

[0119] Isovalerylspiramycin I or Isovalerylspiramycin II or Isovalerylspiramycin III powder 1000g

[0120] Low-substituted hydroxypropyl cellulose (5%) 92.5g

[0121] Sodium carboxymethyl starch (3%) 55.5g

[0122] Magnesium stearate (1%) 18.5g

[0123] Total weight of starch - weight of other raw and auxiliary materials

[0124] Total weight 1850g

[0125] Preparation process: Weigh an appropriate amount of starch, dilute to 15% concentration, heat to a paste, and make an adhesive; the main ingredient isovalerylspiramycin I or isovalerylspiramycin II or isovalerylspiramycin III , auxiliary material starch, low-substituted hydroxypropyl cellulose, sodium carboxymethyl starch, and magnesium stearate were passed through a 100-mesh sieve respectively, and the required main materials and auxiliary materials were w...

Embodiment 3

[0126] Embodiment 3, isovalerylspiramycin I or isovalerylspiramycin II or isovalerylspiramycin III capsules (calculated by 10000 grains)

[0127] prescription:

[0128] Isovalerylspiramycin I or Isovalerylspiramycin II or Isovalerylspiramycin III powder 1000g

[0129] Starch 1080-isovalerylspiramycin I powder weight

[0130] Medicinal Capsule No. 3 1000 capsules

[0131] Liquid paraffin 50ml

[0132] Preparation process: Weigh the main material isovalerylspiramycin I or isovalerylspiramycin II or isovalerylspiramycin III, and the excipient medical starch according to the process formula, put them into a mixer and mix thoroughly 1.5-2 hours; the data obtained by sampling and testing the content should be basically consistent with the theoretical data (the weight of each capsule is about 0.105g), and the qualified medicinal No. According to the operation requirements of the machine, fill them into the feeder respectively, and conduct a difference test (within ±10%, <0.3g) fo...

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Abstract

The invention belongs to the field of drug application. Specifically, the invention discloses an mTOR inhibitor and a pharmaceutical composition, and an application thereof. The mTOR inhibitor includes one of carrimycin, isovaleryl spiramycin I, isovaleryl spiramycin II and isovaleryl spiramycin III, or a combination of two or three of isovaleryl spiramycin I, isovaleryl spiramycin II and isovaleryl spiramycin III. The mTOR inhibitor has obvious inhibitory effect on cells of mTOR pathway-related diseases, a theoretical basis is provided for application and clinical popularization of the mTOR inhibitor in preparation of drugs for treating and / or preventing mTOR pathway-related diseases, and the mTOR inhibitor has important economic and social benefits.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to an mTOR inhibitor, a pharmaceutical composition and applications thereof. Background technique [0002] Tumor is a kind of common and frequently-occurring disease. It is a new organism formed by the abnormal growth and differentiation of clonal abnormal proliferation and differentiation due to gene mutation and loss of normal regulation of its growth and differentiation under the long-term action of various internal and external tumorigenic factors. or vegetation. Tumors are divided into benign tumors and malignant tumors, and malignant tumors are subdivided into three types: carcinoma derived from epithelial tissue, sarcoma derived from mesenchymal tissue, and carcinosarcoma. Usually people say "cancer" refers to all malignant tumors. [0003] Malignant tumor is one of the most important malignant diseases threatening human health, and it is the first cause of death of the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/7048A61P1/16A61P3/04A61P3/10A61P7/04A61P7/06A61P9/10A61P9/12A61P13/12A61P21/00A61P25/16A61P25/28A61P27/12A61P29/00A61P35/00A61P37/06A61P39/00A61P35/02
CPCA61K45/06A61K31/7048A61P3/10A61P25/28A61P35/00A61P39/00A61P37/06A61P29/00A61P7/06A61P7/04A61P13/12A61P3/04A61P1/16A61P25/16A61P21/00A61P9/10A61P9/12A61P27/12A61P35/02A61K2300/00A61P43/00A61P31/00A61P9/00A61P11/00
Inventor 夏明钰赵小峰姜勋雷姜勋东
Owner SHENYANG FUYANG PHARM TECH CO LTD
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