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A kind of pharmaceutical composition containing idebenone and its preparation method

A technology of idebenone and its composition, which is applied in the field of pharmaceutical preparations, can solve the problem of low percentage of related substances in grinding, and achieve the effects of good redispersibility, high drug loading, and low content of related substances

Active Publication Date: 2021-07-23
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In order to overcome the defects of the prior art, the present invention mainly solves three main problems: First, a pharmaceutical composition with a uniform particle size distribution and a low percentage of grinding related substances is proposed to improve its water solubility, increase dissolution rate, and bioavailability. degree, in vivo and in vitro antioxidant capacity, and cognitive ability; secondly, a simple and easy-to-operate method for preparing the pharmaceutical composition with high drug loading, less related substances, and good absorption is proposed, which can be used in industrial production 3. Provide the application of the pharmaceutical composition in the preparation of medicines for improving cognitive ability

Method used

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  • A kind of pharmaceutical composition containing idebenone and its preparation method
  • A kind of pharmaceutical composition containing idebenone and its preparation method
  • A kind of pharmaceutical composition containing idebenone and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: Types and dosage screening of idebenone pharmaceutical composition suspension excipients

[0049] First, prepare polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (Soluplus), hydroxypropylmethylcellulose (HPMC), poloxamer containing 0.2-8.0% (w / v) (F127, F68), sodium deoxycholate (NaDC), sodium dodecyl sulfate (SDS), polyvinylpyrrolidone (PVP), etc., disperse 5% (w / v) idebenone in 20 mL of the above aqueous phase was mixed on a magnetic stirrer for 30 min, then transferred to a 100 mL ball mill jar, and 50 g of 0.4 mm zirconia ball mill balls were added at the same time, and ground for 104 min by a ball mill. Measure the particle size (Z-average) and polydispersity index (PDI) of each prescription as shown in Table 1, when the concentration of auxiliary materials is 1%, the particle size distribution diagrams of various auxiliary materials are as follows: figure 1 shown. The results of the data in Table 1 show that the stabilizi...

Embodiment 2

[0057] Example 2: Preparation process screening of idebenone pharmaceutical composition suspension

[0058] According to the two optimal prescriptions screened out, the grinding process was optimized. Because the grinding power and grinding time have a great influence on the efficiency of sample grinding, too long grinding time will affect the content of related substances and the dispersion state of particles, and the idebenone selected in the present invention has a low melting point, and the preparation method produces More heat, in order to ensure good stability of the prepared pharmaceutical composition, the grinding process is optimized to improve the grinding efficiency.

[0059] Firstly, the total grinding time is screened, the grinding power is fixed at 35Hz, and the particle size distribution is investigated at different grinding times. The results are as follows Figure 4 As shown, the particle size change rate slowed down after grinding to 40min, and the particle ...

Embodiment 3

[0073] Example 3: Preparation and crystal form characterization of a freeze-dried powder of idebenone pharmaceutical composition

[0074] In order to investigate the existing state of the drug in the pharmaceutical composition, the prepared liquid preparation was solidified by using a freeze-drying method. In order to maintain the superior characteristics of the preparation, it is necessary to add a lyoprotectant before lyophilization to maintain the integrity of the nanostructure of the preparation, and the particle size distribution can still be maintained after redispersion, so the type of lyoprotectant was screened.

[0075] First, carry out preliminary screening of the type and concentration of the lyoprotectant, add 2%-10% (w / v) lyoprotectant to the pharmaceutical composition suspension after grinding, the lyoprotectant is selected from maltose ( maltose), lactose, D-mannitol, sucrose, sorbitol, cyclodextrin, dextran and polyethylene glycol (PEG 4000, PEG6000 ). The pa...

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Abstract

The invention relates to a pharmaceutical composition containing idebenone and a preparation method thereof, in particular to a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and idebenone that can improve cognitive behavior A pharmaceutical composition of benzoquinone and a preparation method thereof belong to the technical field of pharmaceutical preparations. The pharmaceutical composition comprises idebenone, a stabilizer and a freeze-drying protective agent, wherein the percentage composition of each component in the composition is as follows: idebenone accounts for 20-50%, and stabilizer accounts for 2-50%. 10%, freeze-drying protective agent accounts for 40-60%, and the weight ratio of idebenone to stabilizer is 15:1-3:1. The present invention uses freeze-drying technology to freeze-dry the prepared pharmaceutical composition suspension to obtain a powdered pharmaceutical composition, and the freeze-dried powder of the pharmaceutical composition can be rapidly dispersed into Nanosuspension state.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing idebenone and a preparation method thereof, in particular to a pharmaceutical composition containing polyethylene caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer and idebenone which can improve cognitive behavior A pharmaceutical composition of benzoquinone and a preparation method thereof belong to the technical field of pharmaceutical preparations. Background technique [0002] Idebenone is coenzyme Q 10 Short-chain derivatives of , originally developed by Takeda Corporation of Japan for the treatment of cognitive impairment diseases. Idebenone has a dual mechanism of action: (1) by inhibiting lipid peroxidation, it protects mitochondria from the damage of reactive oxygen species, and finally protects the cell membrane; (2) by participating in the electron transfer of the mitochondrial respiratory chain, it promotes the formation of ATP and brain metabolism. Based o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/122A61K47/34A61P25/28
CPCA61K9/19A61K31/122A61K47/34A61P25/28
Inventor 付强马敏超
Owner SHENYANG PHARMA UNIVERSITY
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