Unlock instant, AI-driven research and patent intelligence for your innovation.

(S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof

A pyrrolidine acetamide and stability technology, applied in the field of 4-hydroxy-2-oxo-1-pyrrolidine acetamide particles and its preparation, can solve the problem of difficult control of particle size, strong hygroscopicity and easy adhesion of particles Problems such as agglomeration, simple and feasible preparation process, uniform particle size, and not easy to absorb moisture and agglomerate

Inactive Publication Date: 2017-12-26
CHONGQING RUNZE PHARM CO LTD
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The existing (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granules mainly have the problems of easy adhesion to the screen and difficulty in granulation during the granulation process. There are many particle powder layers during the preparation process, and the particle size is not easy to control. Poor stability, strong hygroscopicity of granules, easy to stick and agglomerate, short shelf life, poor taste of granules, difficult to be accepted by patients and other technical problems

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof
  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof
  • (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide granule is prepared according to the following steps:

[0026]

[0027] Preparation process:

[0028] 1. Preparation of adhesive: Take the prescribed amount of honey, put it in an iron pot, add purified water with 2 times the weight of honey, stir evenly, heat to 100-105°C, keep warm for 20-25 minutes, take it out, and use 80 Filter through a mesh sieve, take the filtrate, let it cool, add ethanol in the prescribed amount, stir to dissolve, and set aside;

[0029] 2. Pretreatment of raw and auxiliary materials: take the prescribed amount of (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide, mannitol, microcrystalline cellulose, sodium carboxymethyl cellulose, lactose, sucrose, ethyl alcohol Base maltol is placed in a universal pulverizer, pulverized through a 100-mesh sieve, and set aside;

[0030] 3. Granulation: Take the mixed powder obtained after pretreatment, put it in a wet granulator, add binder, start the granulat...

Embodiment 2

[0076] A stable (S)-4-hydroxyl-2-oxo-1-pyrrolidineacetamide granule is prepared according to the following steps:

[0077]

[0078] Preparation process: prepared according to the preparation process of Example 1. Observing the granulation process of the product did not find the phenomenon of sticking to the screen, and the product was easy to granulate. Carry out the test by the test method of embodiment 1, the Hughes angle test measurement result shows that this product granule fluidity is good, and the Hughes angle is lower than 34 °, and the loading difference test shows that the loading difference of this product is less than ± 5%. The quantity is stable and controllable. The results of the stability test show that the quality of the sample is stable in 6 months of acceleration and 24 months in the long-term. Therefore, the validity period of this product is at least 24 months. The taste survey shows that this product tastes good and is easily accepted by most patients....

Embodiment 3

[0080] A kind of (S)-4-hydroxyl-2 oxo-1-pyrrolidineacetamide granules, prepared according to the following steps:

[0081]

[0082] Preparation process: prepared according to the preparation process of Example 1. Observing the granulation process of the product did not find the phenomenon of sticking to the screen, and the product was easy to granulate. Carry out the test by the test method of embodiment 1, the Hughes angle test measurement result shows that this product granule fluidity is good, and the Hughes angle is lower than 34 °, and the loading difference test shows that the loading difference of this product is less than ± 5%. The quantity is stable and controllable. The results of the stability test show that the quality of the sample is stable in 6 months of acceleration and 24 months in the long-term. Therefore, the validity period of this product is at least 24 months. The taste survey shows that this product tastes good and is easily accepted by most patients....

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle with good stability. The particle is prepared from the following raw and auxiliary materials: 1 part of (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide, 0.8-1.4 parts of mannitol, 1.2-1.7 parts of microcrystalline cellulose, 1.1-1.6 parts of sodium carboxymethyl cellulose, 0.8-1.3 parts of lactose, 0.08-0.13 part of talcum powder, 0.9-1.5 parts of polyethylene glycol 4000, 0.8-1.3 parts of hydroxypropyl methylcellulose, 1-5 parts of sucrose, 0.2-0.7 part of ethyl maltol, 1.2-1.8 parts of honey, and 5-12 parts of ethanol with a volume fraction of 55%-70%. The (S)-4-hydroxy-2oxo-1-pyrrolidine acetamide particle prepared according to the invention has the advantages of no adhesion to a screen mesh, easy granulation, small powder layer content, uniform particle size, good fluidity, a repose angle of less than 34 degrees, a load difference of less than 5%, good storage stability, difficult moisture absorption and caking, a shelf life up to 24 months, and good taste, and can be accepted by most patients.

Description

technical field [0001] The invention mainly relates to the technical field of pharmacy, in particular to a stable (S)-4-hydroxy-2-oxo-1-pyrrolidineacetamide granule and a preparation method thereof. Background technique [0002] Oxiracetam (S-oxiracetam) is a synthetic hydroxyaminobutyric acid (BABOB) cyclic derivative. The drug was launched in Italy in 1987. The listed dosage forms are tablets, 800mg; capsules, 800mg; injection , 1g / 5ml. At present, only oxiracetam capsules and injections are on the market in China, and the main active ingredients used are racemates. Ye Lei et al mentioned in the patent publication No. CN 103735545 A that levoxiracetam has an obvious wake-promoting effect on coma caused by alcoholism, while dextro-oxiracetam has basically no effect. The wake-up effect is twice that of racemic oxiracetam; levo-oxiracetam has significant awakening effects on trauma and coma induced by anesthesia. Zhang Feng et al disclosed in the patent with the publicatio...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/38A61K47/46A61K31/4015A61P39/02A61P25/00A61P25/28
CPCA61K9/1652A61K9/1664A61K31/4015
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD