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Freeze-dried ropivacaine hydrochloride composition for injection

A technology of ropivacaine hydrochloride and its composition, which is applied in the field of medicine, and can solve the problems of poor stability, unstable ropivacaine hydrochloride preparation, light and heat resistance, etc.

Active Publication Date: 2019-07-05
CHENGDU TIANTAISHAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The ropivacaine hydrochloride preparation has the characteristics of poor stability, and its reason is that ropivacaine hydrochloride has enantiomers, and the phenomenon of enantiomeric transition easily occurs in aqueous solution, resulting in the unstable ropivacaine hydrochloride preparation (such as See Chinese Patent Application No. 2007100130274 and Chinese Patent Application No. 2014104487577)
The prescriptions and preparation methods published in the above several patents on ropivacaine hydrochloride preparations only mention sodium chloride, sodium hydroxide or hydrochloric acid, and there is no substance that inhibits the transformation of enantiomers, so it does not solve the problem. Poor stability, not resistant to light and heat, easy to freeze, etc.
[0014] However, in terms of maintaining the excellent properties of the medicament such as its stability, there is still a need for improvement in the prior art

Method used

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  • Freeze-dried ropivacaine hydrochloride composition for injection
  • Freeze-dried ropivacaine hydrochloride composition for injection
  • Freeze-dried ropivacaine hydrochloride composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0094] Embodiment 1: Preparation of ropivacaine hydrochloride freeze-dried powder injection

[0095] formula:

[0096] Ropivacaine hydrochloride 75mg,

[0097] Lactose 40mg,

[0098] Acid-base regulator: appropriate amount, adjust the pH to the specified value in the following preparation method,

[0099] Water for injection: add to 3ml.

[0100] Preparation method:

[0101] (a) take by weighing ropivacaine hydrochloride, lactose of prescription quantity, add prescription quantity 60% water for injection, stir and make to dissolve;

[0102] (b) Add activated carbon (0.1% by volume of the medicinal liquid) to the medicinal liquid obtained in the previous step, adjust the pH value of the solution to 3.2 with an acid-base regulator, stir for 2.0 hours at a temperature of 25° C., filter for decarbonization, and use an acid-base regulator to The regulator adjusts the pH of the solution to 5.0;

[0103] (c) Add water for injection to the full amount of the prescription, ...

Embodiment 2

[0106] Embodiment 2: Preparation of ropivacaine hydrochloride freeze-dried powder injection

[0107] formula:

[0108] Ropivacaine hydrochloride 75mg,

[0109] Lactose 45mg,

[0110] Acid-base regulator: appropriate amount, adjust the pH to the specified value in the following preparation method,

[0111] Water for injection: add to 3.75ml.

[0112] Preparation method:

[0113] (a) take by weighing ropivacaine hydrochloride, lactose of prescription quantity, add prescription quantity 65% ​​water for injection, stir and make to dissolve;

[0114] (b) Add activated carbon (0.05% by volume of the medicinal solution) to the medicinal solution obtained in the previous step, adjust the pH value of the solution to 3.0 with an acid-base regulator, stir for 2.0 hours at a temperature of 20°C, filter for decarbonization, and use an acid-base regulator to The regulator adjusts the pH of the solution to 5.5;

[0115] (c) Add water for injection to the full amount of the prescr...

Embodiment 3

[0118] Embodiment 3: Preparation of ropivacaine hydrochloride freeze-dried powder injection

[0119] formula:

[0120] Ropivacaine hydrochloride 75mg,

[0121] Lactose 35mg,

[0122] Acid-base regulator: appropriate amount, adjust the pH to the specified value in the following preparation method,

[0123] Water for injection: add to 2.5ml.

[0124] Preparation method:

[0125] (a) take by weighing ropivacaine hydrochloride, lactose of prescription quantity, add prescription quantity 55% water for injection, stir and make dissolving;

[0126] (b) Add activated carbon (0.15% by volume of the medicinal solution) to the medicinal solution obtained in the previous step, adjust the pH value of the solution to 3.5 with an acid-base regulator, stir for 2.3 hours at a temperature of 30° C., filter for decarbonization, and use an acid-base regulator to The regulator adjusts the pH4.5 of the solution;

[0127] (c) Add water for injection to the full amount of the prescription...

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Abstract

The invention relates to a freeze-dried ropivacaine hydrochloride composition for injection. The freeze-dried ropivacaine hydrochloride composition comprises ropivacaine hydrochloride and lactose, for example, 75 parts by weight of ropivacaine hydrochloride and 20-60 parts by weight of lactose. The composition is basically prepared by a method comprising the following steps: weighing a formulated amount of ropivacaine hydrochloride and lactose, adding an appropriate amount of injection water, and stirring for dissolution; adding active carbon into a medicinal solution obtained in the previous step, stirring, and filtering to remove carbon; refilling the injection water to a full formulated amount, stirring uniformly, measuring the pH value of the solution and optionally measuring the content of active ingredients, and adjusting the pH value to 4.0-6.0 by using a pH value regulator if necessary; carrying out sterilization and filtration on the medicinal solution, and filling the solution into a penicillin bottle; and carrying out freeze-drying to remove water, and carrying out tamponment. The freeze-dried ropivacaine hydrochloride composition for injection, provided by the invention, has excellent pharmaceutical properties as described in the specification.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a local anesthetic pharmaceutical composition, in particular to a ropivacaine hydrochloride freeze-dried powder injection pharmaceutical composition with excellent properties. The invention also relates to a preparation method of the ropivacaine hydrochloride freeze-dried powder injection pharmaceutical composition. The pharmaceutical composition of ropivacaine hydrochloride freeze-dried powder for injection can be used for surgical anesthesia; epidural anesthesia, including caesarean section; acute pain control; continuous epidural infusion or intermittent single administration, such as postoperative or Pain in labor; regional block. The ropivacaine hydrochloride powder for injection prepared by the invention has excellent physical and chemical properties. Background technique [0002] Ropivacaine is a long-acting amide local anesthetic. Its pharmacological properties are low...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K47/26A61K31/445A61P23/02A61P29/00
CPCA61K9/19A61K31/445A61K47/26
Inventor 赵东明方专陈娟张莲莲吴国庆伍隆霞
Owner CHENGDU TIANTAISHAN PHARMA
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