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Long-acting brexpiprazole in-situ phase change gel injection and preparation method thereof

A gel injection, epipiprazole technology, applied in the field of pharmaceutical preparations, can solve the problems of limited release time, poor stability, poor injectability, etc., and achieves low equipment requirements, excellent fluidity and injectability, and operation. simple effect

Pending Publication Date: 2020-09-01
YAOPHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] The purpose of the present invention is to provide an improved sustained-release ebiprazole in situ phase change gel injection, which solves the problems of poor injectability and poor stability in the existing long-acting in situ gel technology. Good and limited release time, especially suitable for long-acting in situ gel injection of poorly soluble drug ebiprazole

Method used

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  • Long-acting brexpiprazole in-situ phase change gel injection and preparation method thereof
  • Long-acting brexpiprazole in-situ phase change gel injection and preparation method thereof
  • Long-acting brexpiprazole in-situ phase change gel injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of long-acting injectable ebiprazole phase-change gel based on soybean lecithin

[0042] Prescription screening: with MCT (medium chain triglyceride), GDO (glyceryl dioleate), Span-80, ethyl oleate, PVP (polyvinylpyrrolidone), propylene glycol, Tween-80 as additives, Using ethanol, aqueous ethanol and NMP (N-methyl-2-pyrrolidone) as solvents, the formulation of phase change gel based on soybean lecithin (model: S100) was screened. The screening prescription is shown in Table 1 below, and the unit of each component is "g".

[0043]

[0044] Preparation method: Weigh the ebiprazole raw material medicine of the prescription amount in Table 1, add solvents such as NMP and ethanol of various concentrations corresponding to the prescription amount, and dissolve the ebiprazole; then, add S100 soybean lecithin to the obtained solution in sequence And viscosity-increasing additives such as MCT, GDO, ethyl oleate, Pansi 80, PVP, propylene glycol and T...

Embodiment 2

[0049] Example 2 : Ebiprazole phase change gel injection based on egg yolk lecithin

[0050] Prescription screening: with MCT (medium chain triglyceride), GDO (glyceryl dioleate), Span-80, ethyl oleate, PVP (polyvinylpyrrolidone), propylene glycol, Tween-80 as additives, Ethanol, aqueous ethanol and NMP (N-methyl-2-pyrrolidone) were used as solvents to screen the formulation of phase change gel based on egg yolk lecithin (model: PL-100M). The screening prescription is shown in Table 4, and the unit of each component is "g".

[0051]

[0052] Preparation process: according to the preparation method of Example 1, first weigh the ebiprazole bulk drug in the prescription amount in Table 4, add the solvent NMP corresponding to the prescription amount or ethanol of different concentrations to dissolve it, and obtain the ebiprazole solution. Subsequently, add PL-100M egg yolk lecithin and viscosity-increasing additives such as MCT, GDO, soybean oil, Pansi 80, PVP, propylene gly...

Embodiment 3

[0056] Example 3 : Solubility of Ebiprazole in Phospholipid Gels

[0057] The appearance photos of two kinds of ebiprazole in-situ phase-change gel injections A and B prepared according to Example 1 and Example 2 are as follows: figure 1 shown. By comparison, it can be found that the appearance of the ebiprazole phase-change gel long-acting injection of the present invention and the gel injection disclosed in patents CN102526753B, CN107049932A, CN102008728B and CN104661648B (see figure 2 ) has a significant difference, which is mainly manifested in the different solubility of insoluble active ingredients, see Table 7.

[0058]

[0059] The results in Table 7 show that the phase-change gel injections of the present invention are all clear and transparent solutions, and the insoluble active ingredient ebiprazole can be completely dissolved, and there is no precipitation or crystal precipitation after standing, even after centrifugation at 4000rpm for 5min. No delaminatio...

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Abstract

The invention provides a long-acting brexpiprazole in-situ phase change gel injection and a preparation method thereof. Phospholipid is used as a matrix to dissolve a poorly water-soluble drug namelybrexpiprazole in NMP to prepare an injectable sustained release preparation, the in-situ phase change gel injection has excellent physical and chemical stability, and the drug release time can be maintained for 2 months. In addition, the preparation process is simple, low in equipment requirement and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a stable and sustainable release ebiprazole in-situ phase-change gel injection. Background technique [0002] Ebiprazole (brexpiprazole) is the first dopamine, partial 5-HT1A receptor agonist and 5-HT2A receptor antagonist compound jointly developed by Lundbeck of Denmark and Otsuka Pharmaceutical Company of Japan. The next blockbuster variety has better curative effect and tolerance. Its tablet was approved by the FDA in August 2015, and it is mainly used for schizophrenia and adjuvant treatment of severe depression. However, for psychiatric patients, oral tablet medication compliance is very poor, which further leads to a high relapse rate of this type of disease. [0003] Long-acting injections can significantly improve the problem of poor medication compliance in psychiatric patients. Administration by injection makes it easy for doctors and caregivers to find out...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/496A61K47/44A61K47/14A61K47/24A61K47/22A61P25/24A61P25/18
CPCA61K9/0024A61K9/06A61K31/496A61K47/14A61K47/22A61K47/24A61K47/44A61P25/18A61P25/24
Inventor 唐彬彭可垄刘丽孙宁宁岳涛田彦忻
Owner YAOPHARMA CO LTD
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