Procaine hydrochloride micro-capsules and preparation method thereof

A technology of procaine hydrochloride and capsule material, which is applied in the field of procaine hydrochloride microcapsules and its preparation, and can solve the problems of inability to restrain the hydrolysis of procaine hydrochloride, poor drug use compliance, and toxic substances, etc. , to achieve the effects of improving bioavailability, improving drug compliance, and stabilizing the dissolution rate

Active Publication Date: 2016-09-07
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 102366399 A provides a kind of procaine hydrochloride injection and its preparation method. By adding sodium chloride to the prescription, adjusting the pH value of the liquid and selecting sterilization conditions, the procaine hydrochloride injection can be improved to a certain extent. The stability of procaine injection, but because of its structure contains ester bond and primary aryl amino group, it can not restrain the hydrolysis of procaine hydrochloride to the greatest extent, 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 configuration and use, and the drug use compliance is poor

Method used

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  • Procaine hydrochloride micro-capsules and preparation method thereof

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Embodiment 1

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

[0020] The preparation method of the above-mentioned procaine hydrochloride microcapsules provided in this embodiment comprises the following steps: use absolute ethanol as a solvent to prepare a capsule material solution with an ethyl cellulose concentration of 1%, and then pulverize the procaine hydrochloride drug The particle size is less than or equal to 30 microns, suspended in the capsule material solution, and the mass ratio of procaine hydrochloride powder and capsule material is made into a uniformly dispersed suspension of 1: 1, and the spray drier is used at the import Under the condition that the te...

Embodiment 2

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

[0023] The preparation method of the above-mentioned procaine hydrochloride microcapsules provided in this embodiment comprises the following steps: using absolute ethanol as a solvent to prepare a capsule material solution with a sodium alginate concentration of 3%, and then pulverizing the procaine hydrochloride drug to Particle diameter is 10~30 microns, is suspended in capsule material solution, makes procaine hydrochloride powder and capsule material mass ratio and is the uniformly dispersed suspension of 1: 4, adopts described spray drier at inlet temperature 150 DEG C, outlet temperature are 90 DEG C, feeding rate is 15 milliliters / min...

Embodiment 3

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

[0026] The preparation method of the above-mentioned procaine hydrochloride microcapsules provided in this embodiment comprises the following steps: use absolute ethanol as a solvent to prepare a capsule material solution in which the concentration of acrylic resin RL100 is 5%, and then pulverize the procaine hydrochloride drug to Particle diameter is 1~25 microns, is suspended in capsule material solution, and the evenly dispersed suspension that makes procaine hydrochloride powder and capsule material mass ratio is 1: 6, adopts described spray drier at inlet temperature 80 ℃, outlet temperature is 60 ℃, feed rate is 10 millilit...

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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 in particular 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 class of local anesthetics that can reversibly block the generation and transmission of sensory nerve impulses, referred to as "local anesthetics". That is, in the case of staying awake, it can reversibly cause pain loss in local tissues. The earliest local anesthetic used was the alkaloid cocaine (cocaine) proposed from South American coca leaves. Due to the disadvantages of strong toxicity and addiction of cocaine, high-pressure sterilization is easy to hydrolyze and fail, the application is limited. In order to find a more ideal local anesthetic, people began to dissect, simplify and transform the structure of cocaine. Procaine hydrochloride, as one of the earliest synt...

Claims

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Application Information

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Patent Type & Authority Applications(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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