Pharmaceutical composition containing brexpiprazole and amphiphilic polymer as well as preparation method and application of pharmaceutical composition

The technology of an amphiphilic polymer and bripiprazole is applied in the field of pharmaceutical compositions comprising bripiprazole and an amphiphilic polymer and the preparation thereof, and can solve the problem of poor medication compliance of patients, single medication compliance, use of Inconvenience and other problems, to achieve the effect of reducing clinical care costs, improving bioavailability, and convenient operation

Pending Publication Date: 2021-07-09
江苏谛奇医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although this invention increases the in vitro dissolution rate of brepiprazole, it still fails to avoid the shortcomings of solid preparations such as difficulty in swallowing, easy inhalation or choking, and patients avoiding medication, and the prepared tablets are not suitable. Suitable for special populations such as children and elderly patients, and the patient's medication compliance is poor
[0007] In view of this, in order to give full play to the clinical value of this new type of high-efficiency anti-schizophrenia drug, and to solve the defects of poor medication compliance and inconvenient use caused by the single clinically available dosage form, it is necessary to provide a drug with high bioavailability. Bripiprazole formulations that are convenient to use, have good compliance and stable quality, to solve the above problems

Method used

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  • Pharmaceutical composition containing brexpiprazole and amphiphilic polymer as well as preparation method and application of pharmaceutical composition
  • Pharmaceutical composition containing brexpiprazole and amphiphilic polymer as well as preparation method and application of pharmaceutical composition
  • Pharmaceutical composition containing brexpiprazole and amphiphilic polymer as well as preparation method and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0042] The present invention also provides a preparation method of a pharmaceutical composition comprising bripiprazole and an amphiphilic polymer, comprising the following steps:

[0043] S1. Grinding brepiprazole until the average particle size is less than 100 μm;

[0044] S2. Mix the prescribed amount of brepiprazole with the amphiphilic polymer and dissolve it in the solvent, then add purified water to redissolve after rotary evaporation, and obtain the brepiprazole-amphiphilic polymer inclusion compound after filtration ;

[0045] S3. Add a predetermined amount of film-forming agent, plasticizer, stabilizer, flavoring agent and opacifier to the bripiprazole-amphiphilic polymer clathrate obtained in step S2, and stir thoroughly to obtain a milky solution;

[0046] S4. Defoaming the milky solution obtained in step S3, coating it, drying it, cutting it and dividing it to obtain a pharmaceutical composition containing bripiprazole and an amphiphilic polymer.

[0047] In s...

Embodiment 1

[0051] This embodiment provides a pharmaceutical composition comprising breiprazole and amphiphilic polymer α-tocopheryl polyethylene glycol succinate (TPGS), the breiprazole is encapsulated in the lipophilic core of TPGS , the formation of bripiprazole-TPGS inclusion complex.

[0052] Wherein, the preparation method of brepiprazole-TPGS clathrate comprises the following steps:

[0053] S1. Grinding, sieving or jet milling is used to pulverize the bripiprazole, with the average particle size controlled below 100 μm, and set aside;

[0054] S2. Mix the prescribed amount of breiprazole and α-tocopheryl polyethylene glycol succinate (TPGS) and dissolve them in a predetermined amount of ethanol, then place them in a rotary evaporator, and evaporate to dryness at 50°C ethanol to obtain a thin film; then add a predetermined amount of purified water to the above-mentioned rotary evaporator, stir at 50° C. at a speed of 200 rpm for 1.5 h, and then filter to obtain the buripiprazole-T...

Embodiment 2～4 and comparative example 1

[0056] Embodiments 2 to 4 respectively provide a preparation method of brepiprazole-TPGS clathrate. Compared with Example 1, the difference is that the consumption and proportion of breiprazole and TPGS are changed. The corresponding raw material consumption of example and comparative example is as shown in table 1.

[0057] The consumption and proportioning of each raw material in Table 1 embodiment 1~4 and comparative example 1

[0058]

[0059] The encapsulation efficiency of the bripiprazole-TPGS inclusion compound prepared in Examples 1-4 and Comparative Example 1 was tested, and the results are shown in Table 2.

[0060] The encapsulation efficiency measurement result of table 2 embodiment 1~4 and comparative example 1

[0061] Example / Comparative example Encapsulation rate (%) Example 1 79.4±1.02 Example 2 82.4±1.02 Example 3 87.6±1.02 Example 4 86.2±0.98 Comparative example 1 76.3±1.02

[0062] It can be seen from Tabl...

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Abstract

The invention provides a pharmaceutical composition containing brexpiprazole and an amphiphilic polymer as well as a preparation method and application of the pharmaceutical composition. The pharmaceutical composition comprises brexpiprazole and an amphiphilic polymer, and the brexpiprazole is wrapped in a lipophilic core of an amphiphilic polymer micelle to form a brexpiprazole-amphiphilic polymer inclusion compound. Through the above mode, the solubility of the insoluble drug brexpiprazole in an aqueous medium can be greatly improved, so that the prepared pharmaceutical composition has shorter disintegration time limit and faster dissolution rate, and the bioavailability of the drug is effectively improved. Meanwhile, the pharmaceutical composition containing the brexpiprazole and the amphiphilic polymer is prepared into an oral cavity instant film agent, so that the oral cavity instant film agent can be quickly dissolved on a tongue and can be taken without water, so that the medication compliance and convenience of patients are effectively improved. The preparation method provided by the invention is convenient to operate, good in reproducibility, strong in controllability and relatively low in cost, and has good social benefits and economic benefits.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a pharmaceutical composition comprising bripiprazole and an amphiphilic polymer, a preparation method and application thereof. Background technique [0002] Brexiprazole (Brexpiprazole) is a blockbuster new psychiatric drug discovered by Japan's Otsuka Pharmaceutical and jointly developed by Denmark's Lundbeck Pharmaceutical and Japan's Otsuka Pharmaceutical. The drug was first approved for marketing by the FDA on July 10, 2015. The marketed dosage form is an ordinary solid oral tablet, which is taken orally once a day. It is used as a new type of schizophrenia and high-efficiency adjuvant drug for the treatment of severe depression. Its structural formula is as follows: [0003] [0004] The current clinical dosage form of this new type of highly effective antipsychotic drug is only ordinary solid oral tablets, and ordinary solid oral tablets are difficult to swallow, so t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/69A61K47/22A61K47/10A61K47/32A61K47/34A61K47/18A61K31/496A61P25/18A61P25/24
CPCA61K9/006A61K47/6949A61K47/22A61K47/10A61K47/32A61K47/34A61K47/183A61K31/496A61P25/18A61P25/24A61K9/7007
Inventor 金牮胡华胜陈寅郝超张桂森
Owner 江苏谛奇医药科技有限公司
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