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Preparation and application of biodegradable bupivacaine microspheres with high drug loading

A bupivacaine and biodegradation technology, which is applied in the directions of drug combinations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. The problem of large drug volume, etc., to achieve the effect of reducing the number of doses and toxic and side effects, the process is mature, and the action time is prolonged

Active Publication Date: 2019-10-25
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, although these three types of new drug delivery systems significantly prolong the action time of bupivacaine, they all have defects such as low drug loading, large administration volume, and limited application fields.

Method used

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  • Preparation and application of biodegradable bupivacaine microspheres with high drug loading
  • Preparation and application of biodegradable bupivacaine microspheres with high drug loading
  • Preparation and application of biodegradable bupivacaine microspheres with high drug loading

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Embodiment 1: Bupivacaine polylactic acid microspheres (BUP-PLLA-MS)

[0039] PLLA (IV=2.0dl / g) was used as the carrier, the weight ratio of bupivacaine to carrier material (BUP:PLLA) was 70:30, and the volume ratio of the oil-water phase was 1:136. The formulation composition is shown in Table 1.

[0040]Preparation method: Dissolve PLLA and BUP in DCM as organic phase or dispersed phase, 50ml of 1% PVA and 0.6% Tween 80 aqueous solution as aqueous phase or continuous phase, quickly add organic phase to aqueous phase, high speed shear at 8000rpm Cut and emulsify for 5 minutes to form O / W type colostrum, then disperse into 700ml 1% PVA aqueous solution to form a uniform and stable emulsion, and evaporate at 40°C for 20 minutes to remove DCM to obtain solidified microspheres, which are washed, filtered, and dried to obtain cloth Pivacaine poly(L-lactic acid) microspheres. The particle size is 34.54±9.73 μm, and the drug loading is 68.86%. Scanning electron microscopy (...

Embodiment 2

[0041] Embodiment 2: Bupivacaine polylactic acid microspheres (BUP-PLLA-MS)

[0042] PLLA (IV=2.0dl / g) was used as the carrier, the weight ratio of bupivacaine to carrier material (BUP:PLLA) was 75:25, and the oil-water phase volume ratio was 1:150. The composition of the prescription is shown in Table 1.

[0043] The microsphere preparation method in Example 1 was adopted to obtain bupivacaine poly(L-lactic acid) microspheres. The particle size is 33.29±9.58 μm, and the drug loading is 70.97%. SEM observation shows that the shape of the microspheres is round, the surface is smooth, and there are tiny holes (see image 3 ). In the pH 7.4 phosphate buffer solution in vitro, the microspheres can continuously and slowly release the drug, and the cumulative release of bupivacaine in 7 days is 75% (see Figure 4 ).

Embodiment 3

[0044] Embodiment 3: Bupivacaine polylactic acid microspheres (BUP-PLLA-MS)

[0045] PLLA (IV=2.0dl / g) was used as the carrier, the weight ratio of bupivacaine to carrier material (BUP:PLLA) was 80:20, the volume ratio of the oil-water phase was 1:187.5, and the composition of the prescription was shown in Table 1.

[0046] The microsphere preparation method in Example 1 was adopted to obtain bupivacaine poly(L-lactic acid) microspheres. The particle size is 31.83±5.36 μm, and the drug loading capacity is 74.94%. SEM observation shows that the microspheres are round in shape, smooth in surface and free of drug adsorption (see image 3 ). In the pH7.4 phosphate buffer solution in vitro, the microspheres can release the drug continuously and slowly, and the cumulative release of bupivacaine in 5 days is greater than 90%. The prescription microspheres have a high drug loading capacity and are suitable for sustained release (see Figure 4 ).

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Abstract

The invention relates to the technical field of pharmaceutical preparations, and provides a preparation method of biodegradable bupivacaine microspheres with high drug loading capacity. Bupivacaine microspheres entrapping free alkali are prepared by utilizing biodegradable high-molecular-weight polylactic acid as a carrier material according to an emulsified solvent evaporation method. The frozen-dried bupivacaine microspheres are dispersed in a medium for injection so as to be subjected to local injection administration, and is used for postoperative analgesia or is used for relieving local pains; the weight ratio of bupivacaine to the carrier material is (75:25) to (85:15), the drug loading capacity of the bupivacaine in the microspheres is not less than 60%, and medicaments can be completely released within 5-7 days.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations and relates to the preparation of biodegradable bupivacaine microspheres with high drug loading. Background technique [0002] In recent years, microsphere preparations based on biodegradable polymer materials have developed into a mature new drug delivery system. After this type of preparation is injected into the body, it stays at the site of administration in the form of a drug depot (Depot), releasing the drug slowly and continuously for a long period of time, significantly reducing the number of administrations and improving patient compliance. [0003] Bupivacaine (Bupivacaine, BUP) is a long-acting amide local anesthetic with fast onset, long duration of action, and strong analgesic and analgesic effects. It is widely used in spinal anesthesia, epidural anesthesia, brachial plexus block, It is commonly used in the form of hydrochloride in the treatment of postoperative ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/445A61K47/34A61P23/02
CPCA61K9/1647A61K31/445
Inventor 徐晖于洪丹王绍宁徐静华于美玲
Owner SHENYANG PHARMA UNIVERSITY
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