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Midazolam liquid preparation, preparation method therefor and use of midazolam liquid preparation

A technology of liquid preparations and midazolam, which is applied in the field of pharmaceutical preparations, can solve the problems of sodium saccharin carcinogenicity and poor stability of syrups, so as to improve product safety, meet children's clinical drug needs, and reduce degradation products. The effect produced

Active Publication Date: 2021-08-06
XINJIANG TEFENG PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Another literature report [3] , Sodium saccharin has a risk of carcinogenicity, and the US FDA canceled the qualification of saccharin as "generally recognized as safe"
At the same time, the syrup has poor stability and needs to be stored under specific conditions (20-25°C), and the validity period is only 18 months

Method used

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  • Midazolam liquid preparation, preparation method therefor and use of midazolam liquid preparation
  • Midazolam liquid preparation, preparation method therefor and use of midazolam liquid preparation
  • Midazolam liquid preparation, preparation method therefor and use of midazolam liquid preparation

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0091] Experimental Example 1 Stability Test of Influencing Factors

[0092] With the midazolam oral solution that U.S. commercially available midazolam syrup and the general preparation method of the present invention make, according to Chinese Pharmacopoeia 2020 edition four general rule 9001 regulations, respectively put high temperature (60 ℃ ± 2 ℃), light (4500lx ±500lx, 25°C) to carry out the influence factor test, take samples at 0 and 30 days respectively, investigate related substances and contents, and evaluate palatability.

[0093] Table 4 Influencing factor experiment

[0094]

[0095] Note: / No relevant information. * The palatability is comprehensively evaluated from three aspects: smell, taste and aftertaste. The total score of 5 people is 45 points. The higher the score, the better the taste.

[0096] Compared with the midazolam syrup commercially available in the United States, the number of degradation products, the maximum single impurity, and the tot...

experiment example 2

[0097] Experimental Example 2 Accelerated Stability Test

[0098] With midazolam oral solution that U.S. commercially available midazolam syrup and the embodiment of the present invention make, according to Chinese Pharmacopoeia 2015 edition four general rule 9001 regulations, carry out accelerated stability test, respectively at 0,1,2,3 , June (reference preparation 0, March, and June) samples were taken, the pH value, related substances and contents were investigated, and the palatability was evaluated.

[0099] Table 5 accelerated stability test

[0100]

[0101] Note: * The palatability is comprehensively evaluated from three aspects: smell, taste and aftertaste. The total score of 5 people is 45 points. The higher the score, the better the taste.

[0102] Accelerated for 6 months, the content of midazolam syrup commercially available in the U.S. was significantly reduced to 88.9%, and the total impurities reached 9.3%. 0.30%, the stability is significantly better th...

experiment example 3

[0103] Experimental example 3 long-term stability test

[0104]Put the midazolam syrup commercially available in the United States and the midazolam oral solution prepared in the embodiment of the present invention at 25 ± 2°C, RH 60% The long-term stability test was carried out under the condition of ±5%, and samples were taken at 0, 3, 6, 9, 12, 18, 24, and 36 months, respectively, and the pH, degradation products and content were detected to evaluate the palatability.

[0105] Table 6 Long-term stability experiment

[0106]

[0107] Note: * The palatability is comprehensively evaluated from three aspects: smell, taste and aftertaste. The total score of 5 people is 45 points. The higher the score, the better the taste.

[0108] Compared with the 18-month storage validity period of the commercially available midazolam syrup in the U.S., the midazolam oral solution provided by the present invention has a storage validity period of up to 36 months at room temperature, and ...

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Abstract

The invention provides a midazolam liquid preparation, a preparation method therefor and use of the midazolam liquid preparation. Particularly, the invention provides a liquid preparation containing midazolam or pharmaceutically acceptable salts thereof, sodium cyclamate, a halogenated saccharose sweetener and a raspberry flavoring essence, a preparation method for the liquid preparation and use of the liquid preparation in preparation or drugs for treating insomnia, epilepsy and anxiety or tranquilizers or anesthetics. Through a specific adjuvant combination, the liquid preparation prepared by the method has the advantages that the palatability of the midazolam can be effectively improved, and the requirements of children on clinical medication are met; and meanwhile, the liquid preparation is simple in formula, and the safety of the product is improved. Furthermore, due to selection of a pH regulator and / or a flavoring agent, the stability of the midazolam can be improved remarkably (for example, the generation of degraded substances is reduced, properties are not changed after storage, crystal precipitation is absent, and the like).

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a sedative-hypnotic pharmaceutical preparation. More specifically, the invention provides a midazolam liquid preparation suitable for oral use by children. Background technique [0002] Midazolam is mainly used for preoperative sedation and anxiolysis in pediatric patients. Domestically approved midazolam products include tablets and injections, which cannot meet the needs of children. According to reports [1] , about a third of children and teens refuse pills, which require professionals to administer and cause fear and distress to children. In contrast, the oral solution has good compliance and can better meet the clinical medication needs of children. [0003] Midazolam has obvious bitter taste and extremely poor taste. The difficulty in preparing oral solution is to take into account both good taste and quality stability. [0004] The Unite...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/5517A61K47/12A61K47/26A61P25/20A61P25/08A61P25/22A61P23/00
CPCA61K31/5517A61K9/0095A61K47/12A61K47/26A61P25/20A61P25/08A61P25/22A61P23/00
Inventor 云琦张蓉黄雅洁金凡李雅娟陶亮
Owner XINJIANG TEFENG PHARMA
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