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A kind of puerarin freeze-dried Pickering emulsion and preparation method thereof

A technology of Pickering emulsion and puerarin, which is applied in the direction of freeze-drying transportation, pharmaceutical formula, emulsion transportation, etc. It can solve the problems of poor stability and achieve the effect of good stability and easy transportation and storage

Active Publication Date: 2020-06-30
SOUTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The invention prepares a puerarin freeze-dried Pickering emulsion, which solves the problem of poor long-term stability of the puerarin nanocrystal self-stabilizing Pickering emulsion

Method used

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  • A kind of puerarin freeze-dried Pickering emulsion and preparation method thereof
  • A kind of puerarin freeze-dried Pickering emulsion and preparation method thereof
  • A kind of puerarin freeze-dried Pickering emulsion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Weigh 350mg of puerarin, add 63mL of water phase (with 1mol L -1 The pH of the aqueous phase adjusted by sodium hydroxide is 11.5), 19000rpm high-speed shearing 2min, 800bar high-pressure homogenization 3min, then measure 7mL oil phase (chuanxiong oil: oleic acid macrogolglyceride=9:1, v / v ), added in a high-pressure homogenizer, 80MPa continued homogenization for 3min, and obtained puerarin nanocrystal self-stabilizing Pickering emulsion.

[0040] Take 2 mL of newly prepared puerarin nanocrystalline self-stabilizing Pickering emulsion and add it to a vial, add 0.16 g (8%) of lyoprotectant (trehalose, maltose), mix well, and process according to the following process conditions respectively , to obtain the puerarin freeze-dried emulsion.

[0041] Process A: Pre-freeze at -40°C for 6 hours, then sublimate and dry according to the following procedures: -40°C for 18h, -15°C for 6h, 0°C for 4h, 15°C for 4h, and the vacuum degree is lower than 5Pa.

[0042] Process B: Pre-...

Embodiment 2

[0049] Weigh 350mg of puerarin, add 63mL of the water phase (use 1mol L-1 sodium hydroxide to adjust the pH of the water phase to 11.5), high-speed shear at 19000rpm for 2min, and high-pressure homogenization at 800bar for 3min, then measure 7mL of the oil phase (Chuanxiong Oil: oleic acid polyethylene glycol glyceride=9:1, v / v), add in the high-pressure homogenizer, 80MPa continues homogeneous 3min, obtains puerarin nanocrystal self-stabilizing Pickering emulsion (puerarin nanocrystal self-stabilizing Stabilized Pickering Emulsion).

[0050] Take 2 mL of newly prepared puerarin nanocrystalline self-stabilizing Pickering emulsion and add it to a vial, add different kinds of compatible freeze-drying protectants, trehalose, maltose and HPMC K4M, HP-β-CYD and PVP K30 respectively by 1 : 1 ratio, the dosage is 8%, mixed evenly, pre-frozen at -80°C for 24 hours, sublimated and dried according to the following procedure: 10°C for 15 hours, and the vacuum degree is lower than 5Pa to ...

Embodiment 3

[0057] Weigh 350mg of puerarin, add 63mL of the water phase (use 1mol L-1 sodium hydroxide to adjust the pH of the water phase to 11.5), high-speed shear at 19000rpm for 2min, and high-pressure homogenization at 800bar for 3min, then measure 7mL of the oil phase (Chuanxiong Oil: oleic acid polyethylene glycol glyceride=9:1, v / v), add in the high-pressure homogenizer, 80MPa continues homogeneous 3min, obtains puerarin nanocrystal self-stabilizing Pickering emulsion (puerarin nanocrystal self-stabilizing Stabilized Pickering Emulsion).

[0058] Take 2 mL of newly prepared puerarin nanocrystalline self-stabilizing Pickering emulsion and add it to a vial, and mix maltose, trehalose and PVP K30 at 1:1, 2:1, 4:1, 8:1 and 16:1 respectively , added at 4%, 8% and 12%, mixed evenly, pre-frozen at -80°C for 24 hours, sublimated and dried according to the following procedure: 10°C for 15 hours, and the vacuum degree was lower than 5Pa to obtain a puerarin freeze-dried emulsion.

[0059] ...

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Abstract

The invention discloses a puerarin freeze-dried Pickering emulsion and a preparation method thereof. Raw materials for preparing the puerarin freeze-dried Pickering emulsion consist of the following ingredients in percentage: 0.1% to 5.0% of puerarin, 5% to 10% of oil phase, 1% to 10% of freeze-drying protective additive and the balance of water. A puerarin raw material medicine is added into a water phase, primary puerarin suspension is prepared by using a high-speed shearing machine, and then puerarin nanocrystalline suspension is obtained by using a high pressure homogenizer. The oil phaseis added into the puerarin nanocrystalline suspension, and then a puerarin nanocrystalline stable Pickering emulsion is prepared by using the high pressure homogenizer. Next, the freeze-drying protective additive is added, the puerarin nanocrystalline stable Pickering emulsion and the freeze-drying protective additive are uniformly mixed, and a mixture is freeze-dried to obtain the puerarin freeze-dried Pickering emulsion.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a puerarin freeze-dried Pickering emulsion and a preparation method. Background technique [0002] Puerarin is an isoflavone derivative with a crown-expanding effect extracted from the traditional Chinese medicine Pueraria lobata, which exists in the roots of the leguminous plants Pueraria lobata and Pueraria mirifica. Puerarin has the effects of reducing fever, calming and increasing coronary blood flow, and has a protective effect on acute myocardial hemorrhage caused by vasopressin. It is mainly used clinically for coronary heart disease, angina pectoris, and hypertension. Puerarin is an insoluble drug with low bioavailability. When the pH is above 10, the stability of puerarin is not good, and the structure of the mother nucleus may be irreversibly damaged. [0003] Pickering emulsion is a new type of emulsion in which solid particles replace surfactan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/19A61K31/352A61K47/14A61K47/44A61K47/26A61K47/36A61K47/32A61P9/10A61P9/12
CPCA61K9/107A61K9/19A61K31/352A61K47/14A61K47/32A61K47/36A61K47/44A61P9/10A61P9/12
Inventor 张继芬
Owner SOUTHWEST UNIV