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Preparation method of tanshinone IIA microsphere preparation

A technology of tanshinone and microspheres, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can solve the problem of unsatisfactory drug loading and encapsulation efficiency, poor patient compliance, and biological half-life. Short and other problems, to achieve superior sustained release, improve curative effect, reduce the effect of dose

Active Publication Date: 2015-04-29
GUIZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent medicine preparations clinically used to treat cardiovascular diseases, such as tablets, capsules, granules, and injections, but they have unsatisfactory drug loading and encapsulation efficiency, are insoluble or slightly soluble in water, have low bioavailability, and poor absorption. Poor problem, which affects its curative effect to a certain extent
And its biological half-life is short, it is necessary to increase the number of administrations to achieve the corresponding blood concentration, and the patient's compliance is poor

Method used

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  • Preparation method of tanshinone IIA microsphere preparation
  • Preparation method of tanshinone IIA microsphere preparation
  • Preparation method of tanshinone IIA microsphere preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: Tanshinone II A - Preparation of PLLA microspheres:

[0055] (1) Preparation of O phase: 10 mg of tanshinone Ⅱ A Dissolve PLLA in 2 mL of dichloromethane (DCM) to obtain a PLLA concentration of 75 g / ml, vortex and mix to form O phase, and set aside;

[0056] (2) Preparation of the W phase: dissolve the surfactant PVA in 150 mL of deionized water to obtain a PVA concentration of 3 mg / mL to form the W phase and set aside;

[0057] (3) Preparation of emulsion: Stir at a constant speed of 1000 rpm at a temperature of 4°C, slowly add the above phase O into phase W to prepare an O / W emulsion;

[0058] (4) Formation of microspheres: under ice bath conditions, stir at a constant speed at a speed of 1000 rpm until the organic solvent is completely volatilized;

[0059] (5) Collection of microspheres: leave to settle, remove supernatant, collect by suction filtration on a filter, wash with distilled water 3 times, put in a desiccator and dry at room temperature f...

Embodiment 2

[0060] Embodiment 2: Tanshinone II A - Preparation of PLLA microspheres:

[0061] (1) Preparation of O phase: 35 mg of tanshinone Ⅱ A Dissolve 75mg / mL PLLA in 1mL DCM, vortex and mix well, make phase O, set aside;

[0062] (2) Preparation of phase W: Dissolve PVA in 150 mL of deionized water to obtain a PVA concentration of 3 mg / mL to form phase W for later use;

[0063] (3) Preparation of emulsion: Stir at a constant speed of 800 rpm at a temperature of 4°C, and slowly add the above phase O into phase W to prepare an O / W emulsion;

[0064] (4) Formation of microspheres: under ice bath conditions, stir at a constant speed at a speed of 1000 rpm until the organic solvent is completely volatilized;

[0065] (5) Collection of microspheres: leave to settle, remove supernatant, collect by suction filtration on a filter, wash with distilled water 3 times, put in a desiccator and dry at room temperature for 48 hours to obtain.

Embodiment 3

[0066] Embodiment 3: Tanshinone II A Preparation of Microsphere Formulation:

[0067] (1) Preparation of O phase: 35 mg of tanshinone Ⅱ A Dissolve 75mg / mL PLLA in 2mL DCM, vortex and mix well, make phase O, set aside;

[0068] (2) Preparation of phase W: Dissolve PVA in 150 mL of deionized water to obtain a PVA concentration of 3 mg / mL to form phase W for later use;

[0069] (3) Preparation of emulsion: Stir at a constant speed of 1500 rpm at a temperature of 4°C, slowly add the above phase O to phase W to prepare an O / W emulsion;

[0070] (4) Formation of microspheres: under ice bath conditions, stir at a constant speed at a speed of 1500 rpm until the organic solvent is completely volatilized;

[0071] (5) Collection of microspheres: leave to settle, remove supernatant, collect by suction filtration on a filter, wash with distilled water 3 times, put in a desiccator and dry at room temperature for 48 hours to obtain.

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Abstract

The invention discloses a preparation method of a tanshinone IIA microsphere preparation. The method comprises the following steps: dissolving tanshinone IIA and a high-molecular polymer in an organic solvent, then adding the solvent into a dispersion medium, conducting emulsification, volatilizing the organic solvent, and finally conducting suction filtration, washing and drying to obtain tanshinone IIA microspheres. The method provided by the invention not only increases the drug loading capacity and the encapsulation efficiency, but also has the characteristics of good solubility, high stability, safety, no toxicity, good slow-release property, good persistence and high efficiency.

Description

technical field [0001] The present invention relates to Tanshinone II A The invention discloses a preparation method of a microsphere preparation, which belongs to the field of microsphere preparations. Background technique [0002] Microspheres refer to tiny spherical entities formed by dissolving or dispersing drugs in polymer materials, spherical or spherical in shape. The particle size of microspheres generally ranges from 1 to 500 μm, which can be used for injection, oral administration, nasal drop or subcutaneous implantation. The release speed of the drug achieves the purpose of long-term effect, and can protect the drug from being degraded by enzymes in the body, mask the bad taste of the drug, reduce the number of administration and drug stimulation, and improve the curative effect and drug stability. For example, the sustained release time of leuprolide microspheres is as long as 6 months, changing the original way of daily administration and greatly reducing the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/58A61K47/34A61K47/32A61P9/00A61P9/10A61P7/02
Inventor 沈祥春陶玲徐旖旎朱娅芳周雪
Owner GUIZHOU MEDICAL UNIV
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