PEG-PLGA sustained release microsphere with encapsulated buprenorphine and preparation method thereof

A technology of PEG-PLGA and slow-release microspheres, applied in the field of pharmaceutical preparations, to achieve the effects of alleviating pain, good biocompatibility, and increasing patient compliance

Active Publication Date: 2016-05-25
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Overcome the inconvenience in the way of administration

Method used

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  • PEG-PLGA sustained release microsphere with encapsulated buprenorphine and preparation method thereof
  • PEG-PLGA sustained release microsphere with encapsulated buprenorphine and preparation method thereof
  • PEG-PLGA sustained release microsphere with encapsulated buprenorphine and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1: Preparation of buprenorphine sustained-release microspheres

[0044] (1) Weigh 10 mg of buprenorphine hydrochloride, dissolve it in 0.5 ml of methanol, and add N,N,N',N'-tetramethyl ethylenediamine and stirred overnight. Obtain 20mg / ml (according to buprenorphine hydrochloride) buprenorphine base, standby.

[0045] (2) Weigh 20 mg of polyethylene glycol-polylactic acid-glycolic acid copolymer carrier material and dissolve it in 900 μl of dichloromethane, and dissolve completely. Measure 100 μl of the above buprenorphine base solution and add it into the carrier material solution, so that the final volume of the organic phase is 1 ml. Ultrasonic dissolved and mixed, and then stirred at 800r / min for 4h to mix thoroughly.

[0046] (3) Under stirring conditions, use a needle to draw the organic phase deep into the bottom of the liquid surface and slowly add it to an aqueous solution of polyvinyl alcohol with a mass fraction of 1%, emulsify for 30 minutes at...

Embodiment 2

[0049] Embodiment 2: Preparation of buprenorphine sustained-release microspheres

[0050] (1) Take by weighing 15mg of buprenorphine hydrochloride, be dissolved in 0.5ml tetrahydrofuran, after fully dissolving, add N,N-diisopropylethylamine equivalent to 2 times the molar amount of buprenorphine hydrochloride wherein, stir overnight. Obtain 30mg / ml (according to buprenorphine hydrochloride) buprenorphine base, standby.

[0051] (2) Weigh 20 mg of polyethylene glycol-polylactic acid-glycolic acid copolymer carrier material and dissolve it in 900 microliters of dichloromethane, and dissolve completely. Measure 100 microliters of the above-mentioned buprenorphine base solution and add it into the carrier material solution, so that the final volume of the organic phase is 1 ml. Ultrasonic dissolved and mixed, and then stirred at 800r / min for 4h to mix thoroughly.

[0052] (3) Under stirring conditions, use a needle to draw the organic phase deep into the bottom of the page and ...

Embodiment 3

[0055] Embodiment 3: Preparation of buprenorphine sustained-release microspheres

[0056] (1) Weigh 20 mg of buprenorphine hydrochloride, dissolve it in 0.5ml N,N dimethylformamide or dimethyl sulfoxide, and add 2 times the molar amount of buprenorphine hydrochloride to it after fully dissolving triethylamine, stirred overnight. Obtain 40mg / ml (according to buprenorphine hydrochloride) buprenorphine base, standby.

[0057] (2) Weigh 20 mg of polyethylene glycol-polylactic acid-glycolic acid copolymer carrier material and dissolve it in 900 microliters of dichloromethane, and dissolve completely. Measure 100 microliters of the above-mentioned buprenorphine base solution and add it into the carrier material solution, so that the final volume of the organic phase is 1 ml. Ultrasonic dissolved and mixed, and then stirred at 800r / min for 4h to mix thoroughly.

[0058] (3) Under stirring conditions, use a needle to draw the organic phase deep into the bottom of the page and slowl...

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Abstract

The invention discloses a PEG-PLGA sustained release microsphere with encapsulated buprenorphine and a preparation method thereof. The preparation method is as below: conducting debydrochlorination on buprenorphine to prepare alkali, and conducting a single emulsion method to obtain the PEG-PLGA sustained release microsphere with encapsulated buprenorphine. The weight ratio of buprenorphine (calculated by buprenorphine hydrochloride) to polyethylene glycol-polylactic acid-glycolic acid copolymer is 2-6:10, and the buprenorphine sustained release microsphere has particle size of 10-50 micron. The invention employs for the first time the hydrochloric acid-single emulsion method to prepare the buprenorphine sustained release microspheres with high drug loading, obvious sustained-release effect and good biocompatibility, and can develop a variety of administration approaches, such as intravenous injection, and subcutaneous and intramuscular non-intravenous administration approaches. The invention has good application prospect, and can improve patient compliance.

Description

technical field [0001] The invention relates to a sustained-release microsphere and a preparation method thereof, in particular to a buprenorphine-loaded PEG-PLGA sustained-release microsphere and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] At present, cancer, as a high-incidence and refractory disease, has gradually become one of the main causes of human death due to disease. In addition to the discomfort caused by cancer treatment, cancer patients also suffer from cancer pain. Therefore, in cancer treatment, it is very important to choose appropriate drugs and methods to reduce cancer pain of patients. At present, among the drugs for alleviating cancer pain, non-anesthetic buprenorphine hydrochloride or buprenorphine is widely used in this field, and the preparations on the market include injections, sublingual tablets and the like. However, because these preparations are metabolized quickly...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/485A61K47/34A61P35/00A61J3/00
CPCA61J3/00A61K9/0002A61K9/1641A61K31/485
Inventor 翟光喜刘梦锐杜洪亮
Owner SHANDONG UNIV
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