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Procaine hydrochloride microcapsules and preparation method thereof

A technology of procaine hydrochloride and capsule material is applied in the field of procaine hydrochloride microcapsules and preparation thereof, and can solve the problems of not being able to restrain the hydrolysis of procaine hydrochloride to the greatest extent, poor drug use compliance, toxic substances and the like , to achieve the effect of improving bioavailability, improving medication compliance, and stable dissolution rate

Active Publication Date: 2019-01-08
ZHENGZHOU BARY ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the patent CN 102366399A provides a kind of procaine hydrochloride injection and its preparation method, by adding sodium chloride in the prescription, adjusting the pH value of the liquid and selecting sterilization conditions to improve the procaine hydrochloride injection to a certain extent. The stability of caine injection, but because its structure contains ester bonds and primary aryl amino groups, it cannot restrain the hydrolysis of procaine hydrochloride to the greatest extent, and it is easy to be hydrolyzed to generate toxic substances. Its poor stability greatly affects its use. ; At the same time, it still needs to be protected from light during the configuration and use, and the drug use compliance is poor

Method used

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  • Procaine hydrochloride microcapsules and preparation method thereof

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Embodiment 1

[0019] This embodiment provides a procaine hydrochloride microcapsule, which is composed of procaine hydrochloride powder with a particle size of 30 microns or less and an ethyl cellulose capsule material including the procaine hydrochloride powder, and The mass ratio of the base cellulose to the ethyl cellulose capsule material is 1:1.

[0020] The preparation method of the procaine hydrochloride microcapsules provided in this embodiment includes the following steps: using absolute ethanol as a solvent to prepare a capsule solution with a concentration of 1% ethyl cellulose, and then pulverize the procaine hydrochloride drug To the particle size is less than or equal to 30 microns, suspend in the capsule material solution to prepare a uniformly dispersed suspension with a mass ratio of procaine hydrochloride powder to capsule material of 1:1, and use the spray dryer at the entrance Under the conditions of a temperature of 60°C, an outlet temperature of 40°C, a feed rate of 5 ml / ...

Embodiment 2

[0022] This embodiment provides a procaine hydrochloride microcapsule, which is composed of procaine hydrochloride powder with a particle size of 10-30 microns and a sodium alginate capsule material including the procaine hydrochloride powder, and the seaweed The mass ratio of sodium sulfate to the ethyl cellulose capsule material is 1:4.

[0023] The preparation method of the procaine hydrochloride microcapsules provided in this embodiment includes the following steps: using absolute ethanol as a solvent to prepare a capsule material solution with a sodium alginate concentration of 3%, and then crush the procaine hydrochloride drug to The particle size is 10-30 microns, suspended in the capsule material solution to prepare a uniformly dispersed suspension with a mass ratio of procaine hydrochloride powder to capsule material of 1:4, using the spray dryer at an inlet temperature of Under the conditions of 150°C, outlet temperature of 90°C, feed rate of 15 ml / min, and nozzle press...

Embodiment 3

[0025] This embodiment provides a procaine hydrochloride microcapsule, which is composed of procaine hydrochloride powder with a particle size of 1-25 microns and an acrylic resin RL100 capsule material including the procaine hydrochloride powder, and the acrylic The mass ratio of the resin RL100 to the ethyl cellulose capsule material is 1:6.

[0026] The preparation method of the aforementioned procaine hydrochloride microcapsules provided in this embodiment includes the following steps: using absolute ethanol as a solvent to prepare a capsule material solution with an acrylic resin RL100 concentration of 5%, and then pulverize the procaine hydrochloride drug to The particle size is 1-25 microns, suspended in the capsule material solution to prepare a uniformly dispersed suspension with a mass ratio of procaine hydrochloride powder to capsule material of 1:6, using the spray dryer at an inlet temperature of Under the conditions of 80°C, outlet temperature of 60°C, feed rate of ...

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Abstract

The invention provides procaine hydrochloride micro-capsules. The procaine hydrochloride micro-capsules are prepared from procaine hydrochloride powder and a capsule material coating the procaine hydrochloride powder, wherein the mass ratio of the procaine hydrochloride powder to the capsule material is 1 to 1-6, and the capsule material is a cellulose derivative, acrylic resin RL100, gelatin, arabic gum or alginate. The invention further provides a preparation method of the procaine hydrochloride micro-capsules. The procaine hydrochloride micro-capsules can improve the stability of procaine hydrochloride, reduce side effects, reduce various adverse drug reactions and improve the medication compliance of patients.

Description

Technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a procaine hydrochloride microcapsule and a preparation method thereof. Background technique [0002] Anesthetics play a very important role in clinical practice. Local anesthetics are a kind of local anesthetics that can block the occurrence and transmission of sensory nerve impulses reversibly in the local administration, referred to as "local anesthetics". That is, when staying awake, it can reversibly cause local tissue pain to disappear. The earliest application of local anesthetics is the alkaloid cocaine (cocaine) proposed from the leaves of coca in South America. Cocaine is highly toxic, addictive, and easy to hydrolyze in high pressure disinfection, which limits its application. In order to find a more ideal local anesthetic, people began to analyze, simplify and modify the structure of cocaine. As the earliest synthetic local anesthetic, procaine hydro...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K31/245A61K47/38A61K47/36A61K47/42A61K47/32A61P23/02
CPCA61K9/5026A61K9/5036A61K9/5042A61K9/5057A61K31/245
Inventor 陈长青王福芳周衡邓俊陈慧娟王颖丁佳丽李攀
Owner ZHENGZHOU BARY ANIMAL PHARMA
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