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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 polyorthoester, polar aprotic solvent and viscosity reducing agent triglyceride, the viscosity of the obtained composition is relatively high, the needle penetration is poor, and the convenience of clinical administration is poor
[0014] In addition, according to the literature Anesth Analg.2006Sep; 103(3):608-14, when nerve fibers are exposed to low concentrations of local anesthetics for a long time, it will lead to a significant delay in the growth of neurites, and the axonal transport of actin Destroyed, causing damage to nerve fibers, producing symptoms such as neuroinflammation or neurofibrosis
[0015] At present, the above-mentioned patent documents all use commonly used excipients in this field. Although the resulting composition has a certain sustained-release effect, it has low drug availability, high irritation at the injection site, large safety hazards, poor needle penetration, and complicated processes. , poor stability and other shortcomings
The composition of the present invention is improved on the basis of existing research techniques, and an appropriate amount of drug effect enhancer is added, which can not only maintain the slow-release effect and good stability of the composition, but also prolong the duration of conventional sustained-release preparations under the same dosage. The duration of the drug effect, and can reduce the effective therapeutic dose under the same analgesic drug effect, improve the motor nerve block situation, and improve the safety of medication, which has not been reported in this field

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

Embodiment 1

[0134] Preparation of depot pharmaceutical compositions

[0135] The preparation process of the composition in Table 8: add the prescribed amount of ropivacaine into the drug solvent, stir until dissolved to obtain a drug solution; add the medicinal phospholipids to the corresponding medicinal oils, and shear at high speed to obtain the medicinal phospholipids Completely dissolve; add the drug solution therein, stir evenly, then add the drug effect enhancer, stir to obtain the drug-containing solution, filter and subpackage, fill with nitrogen, seal, and then sterilize with moist heat to obtain a clear and transparent liquid.

[0136] Table 8. Pharmaceutical Composition Prescription

[0137]

[0138] The results show that the compositions prepared after adding an appropriate amount of medicinal phospholipids are all clear and transparent, and the purpose of improving the solubility of the drug in the composition system is achieved.

[0139] The preparation process of the...

experiment example 1

[0153] Experimental Example 1 Stability Investigation

[0154] Place the pharmaceutical composition of Preparation Example 1 to observe its appearance to judge its stability. When there is no visible precipitate, it can be considered that the standing stability of the composition is good.

[0155] Table 13. Stability investigation results of pharmaceutical compositions

[0156]

[0157]

[0158] The results showed that the prepared compositions were all clear and transparent, indicating that they had good storage stability. However, the preparation provided by CN109316602A (i.e. Comparative Example 6) had obvious precipitation after being left for 5 hours, showing poor stability.

[0159] Select part of the composition and put it under the corresponding conditions, and detect the content and the total amount of related substances according to the following method.

[0160] Testing equipment:

[0161] High performance liquid chromatograph 1260, Agilent Technologies Co...

experiment example 2

[0174] Experimental example 2 Acupuncture Determination of Pharmaceutical Compositions

[0175] A 21G needle was used to test the penetrability of the composition, and the test results are shown in Table 15.

[0176] Table 15. Results of Viscosity Measurements for Pharmaceutical Compositions

[0177] combination injectable Composition 3 to Composition 25 Moderate viscosity, can pass through 21G needle smoothly Comparative example 4 Difficult injection, high viscosity, poor needle penetration Comparative example 5 Low viscosity, can pass through 21G needle smoothly

[0178] The results show that the composition involved in the present invention has suitable needle passability; while the injection of Comparative Example 4 is difficult and the needle passability is extremely poor.

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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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