Reservoir type ropivacaine pharmaceutical composition as well as preparation method and application thereof

A technology of ropivacaine and its composition, which is applied in the storage type ropivacaine pharmaceutical composition and the field of preparation of drugs for treating postoperative pain, and can solve gastrointestinal adverse reactions, irritation and systemic adverse reactions, drugs Low effective utilization and other problems, to achieve the effect of improving bioavailability and effective bioavailability, solving clinical treatment and safety needs, and prolonging effective treatment time

Active Publication Date: 2021-07-16
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preparation has high viscosity and poor needle passability, which brings inconvenience to clinical use.
At the same time, the effective bioavailability of its drugs is low, which will lead to the waste of drugs
[0010] CN109316602A provides a compound slow-release drug delivery system composed of local anesthetics, non-steroidal anti-inflammatory drugs, solvents and slow-release materials. Although it has a certain slow-release analgesic effect and the function of promoting wound healing, the non-steroidal anti-inflammatory drug Body anti-inflammatory drugs have a capping effect, and have the disadvantages of easily causing gastrointestinal adverse reactions, nervous system and cardiovascular system toxicity
At the same time, the proportion of organic solvents is relatively large, reaching 30-40%, which is easy to cause irritation at the injection site and poses a safety hazard
[0011] CN108743952A provides a kind of phospholipid-miscible solvent-oil as carrier local anesthetic slow release preparation and preparation method, it adopts benzyl benzoate, ethanol and benzyl alcohol as solvent, the total amount of solvent is as high as 40~50%, it is easy to cause injection Partial irritation and systemic adverse reactions, there are potential safety hazards
Similarly, non-steroidal anti-inflammatory drugs have a capping effect and have the disadvantages of easily causing gastrointestinal adverse reactions, nervous system and cardiovascular system toxicity
In addition, the delivery carrier is composed of polyorthoest

Method used

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  • Reservoir type ropivacaine pharmaceutical composition as well as preparation method and application thereof
  • Reservoir type ropivacaine pharmaceutical composition as well as preparation method and application thereof
  • Reservoir type ropivacaine pharmaceutical composition as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Example

[0104] Contractions 1 and 2:

[0105] According to the prescription listed in Table 1, the medicinal grease and the drug solvent are mixed, and the ropivacaine is added to the drug, vortex, ultrasound, to obtain a muddy opaque liquid;

[0106] Attempting to dissolve the ropivacaine first in the drug solvent, the dissolution process is relatively rapid, then adding the amount of medicinal grease, vortex, and immediately exhibits white turbidity.

[0107] Table 1. Pharmaceutical composition

[0108]

Example

[0129] Contractions 8 and 9:

[0130] The equivalent amount of hydrochloride, propylene glycol, soy lecithin S100, castor oil, glycine added to a predominantly round bottom flask, weighing, adding excess absolute ethanol, placing the flask is placed in ultrasonic waves. Ultrasound makes each component completely dissolved. At this time, the round bottom flask was then applied to a suitable rotary evaporator, and the reduced pressure evaporated to the round bottom flask weight change indicated that no water ethanol had been removed. Cool the flask to room temperature, add the amount of fish oil, mix, transfer the content to the glass vial, and save room temperature.

[0131] Table 7. Prescription Information of the proportion 8 and 9

[0132] prescription Contrast 8 ratio (w / w) Contrast 9 ratio (w / w) Robi-hydrochloride 4.5％ 4.5％ Soy lecithin S100 42％ 42％ castor oil 38.2％ 23.2％ Propanediol 15％ 15％ Fish oil 3322 / 15％ Glutinum 0.3％ 0...

Example Embodiment

[0133] Example 1

[0134] Preparation of reserve type pharmaceutical compositions

[0135] The preparation process of the composition of Table 8: Pivopivaca of the prescription amount is stirred to dissolve, resulting in a pharmaceutical solution by adding a drug solvent, resulting in a pharmaceutical solution to the corresponding pharmaceutical oil, high speed shear to a pharmacy phospholipid Completely dissolved; in which the drug solution is added, stir even, then the drug-efficient reinforcing agent is added, stirred, and the mixture containing a drug containing solution, filtration, nitrogen nitrogen seal, and then sterilized, to obtain a clear and transparent liquid.

[0136] Table 8. Pharmaceutical composition

[0137]

[0138] The results showed that the obtained composition was prepared after adding an appropriate amount of pharmaceutically acceptable phospholipid, and the resulting composition was clear and transparent, and the purpose of improving the solubility of t...

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PUM

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Abstract

The invention provides a reservoir type ropivacaine pharmaceutical composition as well as a preparation method and application thereof. The pharmaceutical composition comprises: ropivacaine, a pharmaceutical solvent, a medicinal phospholipid, medicinal oil, and pharmaco enhancers, a non-essential antioxidant and a non-essential acid-base regulator. The pharmaceutical composition has a controllable release behavior and a sustained release effect, can significantly reduce the peak serum concentration of the drug, maintain a stable plasma concentration in the body, prolong the effective treatment time, reduce the effective therapeutic dose, improve the utilization of the drug, and reduce the risk of neurotoxicity. The pharmaceutical composition has a long-lasting analgesic effect and can be used for pain treatment.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a storage type ropivacaine pharmaceutical composition, a preparation method thereof, and an application thereof for preparing a medicine for treating postoperative pain. The pharmaceutical composition has controllable release behavior and sustained release effect, can significantly reduce the peak plasma concentration of the drug, maintain a stable blood drug concentration in the body, prolong the effective treatment time, reduce the effective treatment dose, improve the utilization rate of the drug, and reduce neurological stress. Risk of toxicity, long-acting analgesic effect, can be used to treat postoperative pain. Background technique [0002] Postoperative pain is a comprehensive response to soft tissue trauma during hypersensitive surgery that stimulates the central nervous system. Cause various complications, have a strong impact on the postoperative rehabil...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/12A61K47/24A61K47/44A61K31/445A61P29/00
CPCA61K9/08A61K9/0019A61K47/12A61K47/24A61K47/44A61K31/445A61P29/00A61P23/02
Inventor 甘勇郭仕艳孙银银朱全垒
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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