Ziconotide injection hypodermic implant and preparation method thereof

A ziconotide, injection-type technology, applied in anti-inflammatory agents, pharmaceutical formulations, peptide/protein components, etc., can solve the problems of unstable product emulsification effect, affecting the sustained release effect of preparations, and sudden drug release. The effect of easy control of drug dose, complete encapsulation, and small loss of activity

Inactive Publication Date: 2014-04-09
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Chinese patent application CN102125517A discloses a low-concentration vesicular phospholipid gel of small molecule peptide drugs and its preparation method. Although the vesicular phospholipid gel has achieved a sustained release effect, it uses The high-pressure emulsification process is used, and the prepared product has the defect of unstable emulsification effect. Long-term storage will cause demulsification, resulting in sudden release of the drug, which affects the sustained-release effect of the preparation.

Method used

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  • Ziconotide injection hypodermic implant and preparation method thereof
  • Ziconotide injection hypodermic implant and preparation method thereof
  • Ziconotide injection hypodermic implant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Preparation of Ziconotide Injectable Subcutaneous Implant

[0036] 1. Prescription (1000 sticks)

[0037]

[0038] 2. Preparation of Ziconotide Microcapsules with PLGA as Skeleton

[0039] Dissolve PLGA (Mn=20000, LA:GA=50:50) completely in dichloromethane to prepare 2% PLGA dichloromethane solution, and disperse ziconotide in 2% PLGA dichloromethane solution , formulated into a solution containing ziconotide, and spray-dried at 25°C under a pressure of 0.2 MPa to obtain microcapsules.

[0040] 3. Preparation of temperature-sensitive hydrogel

[0041] Mix Poloxamer 407 with 1ml of water for injection at a low temperature of 20°C, let it stand still to fully swell to a solution state, and make a hydrogel solution.

[0042] 4. Preparation of Ziconotide Injectable Subcutaneous Implant

[0043] Add the ziconotide microcapsule powder into the hydrogel solution, mix evenly, add mannitol and freeze-dry to prepare 1000 ziconotide injection-type subcutaneous im...

Embodiment 2

[0045] Example 2: Preparation of Ziconotide Injectable Subcutaneous Implant

[0046] 1. Prescription (1000 sticks)

[0047]

[0048] 2. Preparation of Ziconotide Microcapsules with PLGA as Skeleton

[0049] Completely dissolve PLGA (Mn=20000, LA:GA=50:50) in chloroform to prepare a 10% PLGA chloroform solution, disperse ziconotide in 10% PLGA chloroform solution, and make a preparation containing ziconotide Notide solution, freeze-dried to obtain microcapsules.

[0050] 3. Preparation of temperature-sensitive hydrogel

[0051] Mix PLGA-PEG-PLGA (molecular weight: 5000) with 1ml of water for injection at a low temperature of 15°C, let it stand still to fully swell to a solution state, and make a hydrogel solution.

[0052] 4. Preparation of Ziconotide Injectable Subcutaneous Implant

[0053] Add the ziconotide microcapsule powder into the hydrogel solution, mix evenly, add mannitol and freeze-dry to prepare 1000 ziconotide injection-type subcutaneous implants.

[0054] Be...

Embodiment 3

[0055] Example 3: Preparation of Ziconotide Injectable Subcutaneous Implant

[0056] 1. Prescription (1000 sticks)

[0057]

[0058] 2. Preparation of Ziconotide Microcapsules with PLGA as Skeleton

[0059] Dissolve PLGA (Mn=10000, LA:GA=75:25) completely in acetone to prepare a 20% PLGA acetone solution, disperse Ziconotide in 20% PLGA acetone solution, and prepare Ziconotide Notide solution was spray-dried at 25°C and 3MPa pressure to prepare microcapsules.

[0060] 3. Preparation of temperature-sensitive hydrogel

[0061] Mix PLGA-PEG-PLGA (molecular weight: 4000) with 1ml of water for injection at a low temperature of 15°C, let it stand still to fully swell to a solution state, and make a hydrogel solution.

[0062] 4. Preparation of Ziconotide Injectable Subcutaneous Implant

[0063] Add the ziconotide microcapsule powder into the hydrogel solution, mix evenly, add mannitol and freeze-dry to prepare 1000 ziconotide injection-type subcutaneous implants.

[0064] Be...

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Abstract

The invention belongs to the technical field of medicine preparation, and discloses a preparation method of a ziconotide injection hypodermic implant as well as the ziconotide injection hypodermic implant prepared by the method. The implant prepared by the method is dissolved by sterile water for injection before use and is then injected to human subcutaneous tissues. The implant prepared by the method is a novel sustained-release preparation which can be subcutaneously injected in form of a liquid. Under the effect of body temperature, the liquor becomes a gel which is slowly released in vivo, so that a long-acting effect of treating and relieving pains is realized.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to a ziconotide injection-type subcutaneous implant and a preparation method thereof. Background technique [0002] Pain is an unpleasant subjective sensory and emotional experience related to tissue damage or potential damage. It is a common symptom of many diseases. Solving pain is the common wish of many medical workers. In the past, opioids and non-steroidal analgesics were the mainstay of clinical treatment, but the therapeutic effect on chronic neurogenic pain was not ideal. With the in-depth research on pain, it is found that the release of pain mediators is reduced after blocking N-type calcium ion channels, which can produce obvious analgesic effects. N-type voltage-sensitive calcium channel (NVSCC) can be specifically blocked by ω-conotoxin (ω-conotoxin, ω-Ctx). At present, more than a dozen kinds of ω-conotoxins have been discovered. With the progress of re...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/17A61K9/19A61P29/00A61P25/04
Inventor 郑春莲康旭徐春莲马亚平袁建成
Owner HYBIO PHARMA
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