Self-assembled oligopeptide capable of inducing biological mineralization of local anesthetic and long-acting local anesthetic and analgesic pharmaceutical preparation prepared from self-assembled oligopeptide

A technology of local anesthetics and short peptides, applied in the direction of anesthetics, drug combinations, active ingredients of heterocyclic compounds, etc., can solve the problems of complex synthesis process, local tissue irritation, high cost, etc., and achieve simple preparation process and biocompatibility Good, the effect of improving the drug loading capacity

Active Publication Date: 2022-04-29
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the synthesis process of HTX-011 is complex and costly, and its degradation products may cause local tissue irritation, which limits its application

Method used

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  • Self-assembled oligopeptide capable of inducing biological mineralization of local anesthetic and long-acting local anesthetic and analgesic pharmaceutical preparation prepared from self-assembled oligopeptide
  • Self-assembled oligopeptide capable of inducing biological mineralization of local anesthetic and long-acting local anesthetic and analgesic pharmaceutical preparation prepared from self-assembled oligopeptide
  • Self-assembled oligopeptide capable of inducing biological mineralization of local anesthetic and long-acting local anesthetic and analgesic pharmaceutical preparation prepared from self-assembled oligopeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Embodiment 1: Synthetic short peptide of the present invention

[0077] The conventional peptide solid-phase synthesis method was used to synthesize the following short peptides: DA7D, DL5E, V5D, EA4F2E, EDY2A4 and EGA3V2E. The purity of the obtained short peptides is greater than 95%.

[0078] (1) Asp-Ala-Ala-Ala-Ala-Ala-Ala-Ala-Asp (SEQ ID NO. 1), abbreviated as DA7D.

[0079] (2) Asp-Leu-Leu-Leu-Leu-Leu-Glu (SEQ ID NO. 2), abbreviated as DL5E.

[0080] (3) Val-Val-Val-Val-Val-Asp (SEQ ID NO.3), abbreviated as V5D.

[0081] (4) Glu-Ala-Ala-Ala-Ala-Phe-Phe-Glu (SEQ ID NO. 4), abbreviated as EA4F2E.

[0082] (5) Glu-Asp-Tyr-Tyr-Ala-Ala-Ala-Ala (SEQ ID NO.5), abbreviated as EDY2A4.

[0083] (6) Glu-Gly-Ala-Ala-Ala-Val-Val-Glu (SEQ ID NO. 6), abbreviated as EGA3V2E.

Embodiment 2

[0084] Embodiment 2: Preparation of Lido-DA7D pharmaceutical preparation of the present invention

[0085] (1) Preparation of DA7D mother solution: DA7D was dissolved in water to prepare 5 mM DA7D mother solution, and ultrasonicated for 5 minutes (ultrasonic power 100W).

[0086] (2) Lidocaine mother liquor preparation: Lidocaine hydrochloride powder was dissolved in water to prepare 80 mM lidocaine mother liquor.

[0087] (3) Magnetically stir 5mL of DA7D mother liquor at room temperature (2000rpm / min), add 5mL of lidocaine mother liquor to DA7D mother liquor drop by drop with a pipette, continue magnetic stirring for 30min after addition, and then sonicate for 10min (ultrasonic power 100W) to obtain the Lido-DA7D mixture.

[0088] (4) Take the Lido-DA7D mixture, adjust the pH to 7.0 with 1M NaOH, let it stand for 1 hour, and a visible crystal precipitate appears, then centrifuge at 12000rpm for 5 minutes, separate the supernatant and the precipitate, and the obtained precip...

Embodiment 3

[0089] Embodiment 3: prepare Ropi-DL5E pharmaceutical preparation of the present invention

[0090] (1) Preparation of DL5E mother solution: 3 mM DL5E mother solution was prepared by dissolving DL5E in water, and ultrasonicated for 5 minutes (ultrasonic power 100 W).

[0091] (2) Preparation of ropivacaine mother liquor: dissolving ropivacaine hydrochloride powder in water to prepare 20 mM ropivacaine mother liquor.

[0092] (3) Magnetically stir 5mL of DL5E mother liquor at room temperature (2000rpm / min), add 5mL of ropivacaine mother liquor to the DL5E mother liquor drop by drop with a pipette, continue magnetic stirring for 30min after addition, and then sonicate for 10min (ultrasonic Power 100W) to obtain the Ropi-DL5E mixture.

[0093] (4) Take the Ropi-DL5E mixture, adjust the pH to 7.0 with 1M NaOH, let it stand for 1 hour, and a visible crystal precipitate appears, then centrifuge at 12000rpm for 5 minutes, separate the supernatant and the precipitate, and the obtaine...

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PUM

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Abstract

The invention provides a self-assembled oligopeptide capable of inducing biological mineralization of a local anesthetic and a long-acting local anesthesia and analgesia medicinal preparation prepared from the self-assembled oligopeptide, and belongs to the field of pharmacy. According to the oligopeptide disclosed by the invention, the self-assembled nanostructure with negative charges on the surface is combined with local anesthetic molecules through the charge effect, and the local anesthetic is induced to be biomineralized under the condition that the alkaline pH regulator is used as an auxiliary agent, so that uniform micron-level injectable drug crystals are formed. The medicine crystal is used as a medicine preparation, has good biocompatibility, can effectively delay the release rate of the medicine and prolong the local anesthesia and analgesic effects, and has good application prospects in preparation of medicines with long-acting local anesthesia and long-acting analgesic effects.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a self-assembled short peptide capable of inducing the biomineralization of local anesthetics and a prepared long-acting local anesthesia and analgesic drug preparation. Background technique [0002] Local anesthetics (referred to as local anesthetics) are a class of ion channel blockers, which can inhibit the transmission of nerve impulses by blocking ion channels on the neuronal cell membrane, thereby achieving anesthesia and analgesic effects. The local anesthetics currently used clinically are almost all water-soluble small molecule drugs with a molecular weight of about 300 Daltons, which have fast diffusion, absorption and clearance, and a short half-life in the body. The effect is generally only a few hours, which cannot meet the current clinical requirements for long-term surgery and postoperative analgesia. [0003] To prolong the duration of local anesthetic drugs, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K47/64A61K45/00A61P23/02A61K31/167A61K31/445A61K31/245
CPCC07K7/06A61K47/64A61K45/00A61P23/02A61K31/167A61K31/445A61K31/245
Inventor 邱峰彭飞张文胜
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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