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Sustained-release microsphere drug delivery system and preparation method thereof

A technology of slow-release microspheres and microspheres, which can be used in drug delivery, drug combination, pharmaceutical formulations, etc., and can solve problems such as blocked needles, patient pain, and drug storage time leakage.

Active Publication Date: 2021-07-23
安徽荣灿生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This type of multivesicular liposome preparation is made into a suspension, and the drug contained in it may leak over time during storage, which is not conducive to the long-term preservation of the product
[0005] Moreover, most of the currently marketed microsphere preparations based on polymers and liposomes have a particle size in the range of 20-60 μm, and the microspheres under this particle size distribution are prone to sedimentation, which will cause serious harm to patients when they are used for injection. Causes significant pain and in some cases requires surgery to complete the administration
Moreover, the particle size of large-sized microspheres is often distributed in the range of several microns to tens of microns, and the uniformity is poor. Moreover, the existing large-sized microspheres have poor resuspension in aqueous solution and are easy to agglomerate. , there is a risk of clogging the needle

Method used

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  • Sustained-release microsphere drug delivery system and preparation method thereof
  • Sustained-release microsphere drug delivery system and preparation method thereof
  • Sustained-release microsphere drug delivery system and preparation method thereof

Examples

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preparation example Construction

[0066] According to the above requirements, one aspect of the present invention provides a method for preparing injectable and storable drug sustained-release microspheres, which comprises the steps of:

[0067] 1) preparing the water phase W of the organic stabilizer aqueous solution;

[0068] 2) dissolving the water-soluble drug in the water phase to obtain a drug solution S;

[0069] 3) dissolving the biodegradable polymer material in an organic solvent to obtain the oil phase O;

[0070] 4) mixing the drug solution S and the oil phase O, and emulsifying to obtain an S / O type primary emulsion;

[0071] 5) inject the primary emulsion S / O obtained in step 4) into the water phase W prepared in step 1, and emulsify to obtain the S / O / W type secondary pre-emulsion;

[0072] 6) homogenizing the S / O / W pre-emulsion obtained in step 5), wherein the S / O / W pre-emulsion can optionally be injected into the aqueous phase W obtained in step 1);

[0073] 7) Optionally volatilize the orga...

Embodiment 1

[0207] Synthesis and characterization of embodiment 1 polylactic acid-polyethylene glycol (PLA-PEG)

[0208] Material: Polyethylene glycol methyl ether (mPEG-OH, purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.)

[0209] D, L-lactide (purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.)

[0210] 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU, purchased from Shanghai Aladdin Biochemical Technology Co., Ltd., English full name is 1,8-Diazabicyclo[5.4.0]undec -7-ene)

[0211] Benzoic acid (purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.)

[0212] All other reagents were of analytical grade and purchased from Shanghai Titan Technology Co., Ltd.

[0213] Method: Dissolve mPEG-OH (0.08mmol, 0.4g) in a round bottom flask filled with 10mL of anhydrous dichloromethane, add D,L-lactide (19.41mmol, 2.8g) and DBU (0.19mmol, 185.5 μL), the round bottom flask was sealed, and the reaction was stirred at room temperature. After 1 h, the polymerizati...

Embodiment 2

[0215] Example 2 Preparation of injectable storable ropivacaine hydrochloride sustained-release microspheres

[0216] Material: PLA-PEG prepared in Example 1 or commercially available (such as: Jinan Daigang Biological Engineering Co., Ltd.)

[0217] Ropivacaine hydrochloride (purchased from Shanghai Macklin Biochemical Technology Co., Ltd.)

[0218] Polyvinyl alcohol (Mw ~ 27,000, purchased from Shanghai Macklin Biochemical Technology Co., Ltd.)

[0219] All other reagents were of analytical grade and purchased from Shanghai Titan Technology Co., Ltd.

[0220]Method: Dissolve 4mg of ropivacaine hydrochloride in 1ml of 0.2% polyvinyl alcohol aqueous solution to obtain inner water phase W1, dissolve 40mg of PLA-PEG in 2ml of dichloromethane to form oil phase O; prepare 0.5% polyethylene Alcohol aqueous solution is used as the external water phase W2; the obtained ropivacaine hydrochloride solution W1 is injected into the oil phase O, and ultrasonically mixed (Q700, Qsonica, U...

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Abstract

The invention provides a preparation method of injectable and storable drug sustained-release microspheres, the drug sustained-release microspheres prepared by the method, and its use for preparing medicines for preventing, treating or alleviating pain or inflammation.

Description

[0001] The invention relates to the field of sustained-release drug delivery systems, in particular to polymer-based sustained-release preparations and preparation methods thereof. [0002] technical background [0003] Microsphere (Microparticle or Microsphere) technology is a new type of pharmaceutical preparation developed in recent years. It has high clinical transformation and application value. It usually uses biodegradable polymer materials as a reservoir, which can enhance the water solubility of drugs and effectively maintain them. Drug stability, improved pharmacokinetics and bioavailability, and long-term drug release in the body at a controlled rate. The FDA-approved medical polymer material polylactic acid PLA and its copolymer with glycolic acid (poly(lactic-co-glycolic acid), PLGA) has excellent safety and biocompatibility, providing adjustable degradation kinetics to Controlled drug release is an ideal microsphere carrier material and has been widely used in var...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/445A61K47/32A61K9/19A61P29/00A61P19/02A61P37/02A61P25/02A61P35/00A61P19/06A61P31/22A61P17/02A61P3/10A61P19/00A61P21/00A61P19/04A61P23/02
CPCA61K9/0019A61K9/1635A61K9/19A61K31/445A61P3/10A61P17/02A61P19/00A61P19/02A61P19/04A61P19/06A61P21/00A61P23/02A61P25/02A61P29/00A61P31/22A61P35/00A61P37/02
Inventor 章雪晴
Owner 安徽荣灿生物科技有限公司
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