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Ropivacaine nanometer lipid carrier temperature-sensitive in-situ gel and preparation method thereof

A nano-lipid carrier, ropivacaine technology, applied in the direction of capsule delivery, liquid delivery, microcapsules, etc., to achieve the effect of good reproducibility, not easy to lose, and easy to produce on a large scale

Inactive Publication Date: 2014-05-28
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, there is no literature report about making ropivacaine into nano-lipid carrier thermosensitive in situ gel preparation

Method used

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  • Ropivacaine nanometer lipid carrier temperature-sensitive in-situ gel and preparation method thereof
  • Ropivacaine nanometer lipid carrier temperature-sensitive in-situ gel and preparation method thereof
  • Ropivacaine nanometer lipid carrier temperature-sensitive in-situ gel and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1: Preparation of ropivacaine nano-lipid carrier thermosensitive in situ gel

[0065] Dissolve 25 mg of ropivacaine (Jinan Dexinjia Biotechnology Co., Ltd.), 100 mg of stearic acid, 40 mg of oleic acid, and 100 mg of soybean lecithin (lipiod from Germany) in 5 ml of acetone, and heat to 75°C to completely dissolve to form an organic phase;

[0066] Dissolve 250mg of HS-15 (BASF, Germany) in 10ml of water for injection, and heat to 75°C to completely dissolve to form the water phase;

[0067] Inject the organic phase into the water phase at a temperature of 75°C and a stirring speed of 500 r / min, and stir for 2.5 hours to completely volatilize the organic phase to obtain colostrum;

[0068] Pour the colostrum into 25ml of water at 0-2°C, and stir in an ice bath at a speed of 500r / min for 2h to obtain a colloidal solution of ropivacaine nano-lipid carrier;

[0069] In an ice bath, slowly add the blank temperature-sensitive gel matrix (poloxamer 407 accounting for...

Embodiment 2

[0070] Example 2: Preparation of ropivacaine nano-lipid carrier thermosensitive in situ gel

[0071] Take 30mg of ropivacaine, 200mg of glyceryl monostearate, 40mg of medium-chain triglycerides (Tieling Beiya Pharmaceutical Oil Co., Ltd.) and 150mg of soybean lecithin dissolved in 5ml of ethanol, and heat to 80°C to dissolve completely, forming The organic phase;

[0072] Dissolve 200mg of HS-15 in 15ml of water for injection, heat to 80°C to dissolve completely, and form the water phase; at a temperature of 80°C and a stirring speed of 1000r / min, inject the organic phase into the water phase, stir for 3 hours, and make The organic phase is completely volatilized to obtain colostrum;

[0073] Pour colostrum into 20ml of water at 0-2°C, and stir in an ice bath at a speed of 1000r / min for 2 hours to obtain a colloidal solution of ropivacaine nano-lipid carrier;

[0074] After diluting with water, observe its morphology with a H-7000 transmission electron microscope, as shown i...

Embodiment 3

[0076] Example 3: Preparation of ropivacaine nano-lipid carrier thermosensitive in situ gel

[0077] Dissolve 30mg of ropivacaine, 150mg of glyceryl monostearate, 50mg of oleic acid, and 150mg of lecithin (German lipiod) in 10ml of ethanol, and heat to 75°C to completely dissolve to form an organic phase;

[0078] Dissolve 300mg of sodium lauryl sulfate in 20ml of water for injection, heat to 75°C to dissolve completely, and form the water phase;

[0079] Inject the organic phase into the water phase at a temperature of 75°C and a stirring speed of 1000 r / min, and stir for 4 hours to completely volatilize the organic phase to obtain colostrum;

[0080] Pour the colostrum into 20ml of water at 0-2°C, and stir in an ice bath for 4 hours at a rotational speed of 1000r / min to obtain a colloidal solution of ropivacaine nano-lipid carrier;

[0081] In an ice bath, the blank thermosensitive gel matrix (poloxamer 407 accounting for 19% of the total system) was slowly added to the rop...

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Abstract

The invention belongs to the technical field of medicinal preparations and specifically to a ropivacaine nanometer lipid carrier temperature-sensitive in-situ gel and a preparation method thereof. The ropivacaine nanometer lipid carrier temperature-sensitive in-situ gel disclosed by the invention mainly comprises bulk drug ropivacaine, a solid lipid material, a liquid lipid material, a surfactant, a cosurfactant, a gel matrix and injection water. The preparation method is a high-temperature emulsification low-temperature setting and cold melt method. The ropivacaine nanometer lipid carrier temperature-sensitive in-situ gel prepared in the invention is applied through transdermal drug delivery and has the advantages of a slow release function, a high transdermal permeation rate, a high entrapment rate, high drug loading capacity, good biocompatibility and good stability.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a ropivacaine nano lipid carrier temperature-sensitive in-situ gel and a preparation method thereof. Background technique [0002] Ropivacaine (RPV), the chemical structural formula is as follows: [0003] [0004] Ropivacaine is another long-acting amide local anesthetic synthesized after mepivacaine and bupivacaine. The anesthesia intensity ratio between it and bupivacaine is about 1.2:1, but its action time is long, its toxicity to the heart is small, and its therapeutic ratio is high. It can produce the characteristics of sensory and motor nerve separation anesthesia to a certain extent. Epidural block and postoperative analgesia have been widely used in various nerve blocks and analgesia abroad. [0005] Due to the low water solubility of RPV, only 0.13mg / mL, ropivacaine hydrochloride is currently used clinically, and injections are gener...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/51A61K31/445A61P23/02
Inventor 汪滋民刘继勇王一翟光喜陆喆潘思华
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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