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Rhynchophylline solid lipid nanoparticles and its preparation method and freeze-dried powder preparation

A technology of solid lipid nanometer and rhynchophylline, which is applied in freeze-dried transportation, powder transportation, pharmaceutical formulations, etc., can solve the problems of poor solubility of rhynchophylline and achieve good stability and uniform distribution

Active Publication Date: 2021-12-03
王盟
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The object of the present invention is to provide a kind of rhynchophylline solid lipid nanoparticle and preparation method thereof, the obtained rhynchophylline solid lipid nanoparticle can improve the defect of rhynchophylline poor solubility and improve the bioavailability of rhynchophylline , while the present invention also provides a freeze-dried powder preparation of rhynchophylline solid lipid nanoparticles

Method used

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  • Rhynchophylline solid lipid nanoparticles and its preparation method and freeze-dried powder preparation
  • Rhynchophylline solid lipid nanoparticles and its preparation method and freeze-dried powder preparation
  • Rhynchophylline solid lipid nanoparticles and its preparation method and freeze-dried powder preparation

Examples

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Effect test

Embodiment 1

[0039] Weigh 50mg glyceryl monostearate, 50mg Tween 80 and 100mg Solutol HS 15 (polyethylene glycol-15 hydroxystearate), heat and melt at 80°C to form an oil phase, and accurately weigh 2.00mg rhynchophylline Dissolve in the oil phase; take another 10ml of purified water and heat it to 80°C as the water phase; after the oil phase is completely melted, quickly add the water phase into the oil phase, stir at 2000r / min for 5min, and the nanoemulsion can be formed. Then place it in an ice-water bath to cool to obtain rhynchophylline solid lipid nanoparticle suspension.

[0040] The encapsulation efficiency and drug loading capacity of rhynchophylline solid lipid nanoparticles were determined by ultrafiltration: take 0.5ml of the prepared rhynchophylline solid lipid nanoparticle suspension, add ultrapure water to dilute to 3ml, and mix well Place in ultrafiltration tube, 3000r / min, centrifuge 5min, take supernatant, under chromatographic conditions (chromatographic column uses octa...

Embodiment 2

[0051] Adding a lyoprotectant before making rhynchophylline SLN into freeze-dried powder is to prevent rhynchophylline SLN from being destroyed during the freeze-drying process, and on the other hand, to obtain a dense and full appearance, no color difference, and layer, lyophilized powder with smaller particle size.

[0052] In this example, the best lyoprotectants were screened from mannitol, sucrose, glucose and trehalose, and their dosages and ratios are shown in Table 1.

[0053] The experimental operation for preparing rhynchophylline SLN freeze-dried powder in this embodiment is: use an analytical balance to weigh 15 prescription amounts of lyoprotectants (in % (w / v) of rhynchophylline SLN suspension) according to Table 1 ), add in 15 cillin bottles successively, then draw 2ml prepared rhynchophylline SLN suspensions with pipette gun respectively and add in the above-mentioned cillin bottles successively. Use a pipette gun to draw 2ml of the prepared rhynchophylline SL...

Embodiment 3

[0066] Weigh 500mg glyceryl monostearate, 50mg Tween 80 and 50mg Solutol HS 15 (polyethylene glycol-15 hydroxystearate), heat and melt at 65°C to form an oil phase, and accurately weigh 6.0mg rhynchophylline Dissolve in the oil phase; take another 3.0ml of purified water and heat it to 65°C as the water phase; after the oil phase is completely melted, quickly add the water phase into the oil phase and stir at 50r / min for 15min to form a nanoemulsion , and then cooled in an ice-water bath to obtain rhynchophylline solid lipid nanoparticle suspension.

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Abstract

The invention belongs to the technical field of nanomedicine, and specifically relates to a rhynchophylline solid lipid nanoparticle and a preparation method thereof and a freeze-dried powder preparation. The rhynchophylline solid lipid nanoparticle of the present invention is prepared by a nanoemulsification method: First, rhynchophylline is dissolved in the melted oil phase, then added to the water phase and stirred to form a nanoemulsion, and then the nanoemulsion is placed in an ice-water bath to obtain; wherein: the oil phase is glyceryl monostearate, Tween 80, A mixture of polyethylene glycol‑15 hydroxystearates; the aqueous phase is purified water. The rhynchophylline solid lipid nanoparticles prepared by the present invention are spherical and spherical, have no adhesion to each other, are evenly distributed, have good stability, have high encapsulation efficiency, and have a high drug loading capacity; they can improve the rhynchophylline Dissolution, dialysis method rhynchophylline solid lipid nanoparticles 6h in vitro cumulative release percentage is 50.45%; the rhynchophylline solid lipid nanoparticles freeze-dried powder prepared by the present invention has a smaller particle size after reconstitution, appearance, color and luster , and good redispersibility.

Description

technical field [0001] The invention belongs to the technical field of nanomedicine, and in particular relates to a rhynchophylline solid lipid nanoparticle, a preparation method thereof and a freeze-dried powder preparation. Background technique [0002] Uncaria is the dry hooked stem branch of Rubiaceae Uncaria, Uncaria sessileus, Uncaria tomentosa, Uncaria large-leaf or Uncaria sinensis. Modern pharmacological research shows that Uncaria mainly acts on the cardiovascular system and central nervous system, and has the functions of lowering blood pressure, sedation, anticonvulsion, antiepileptic, anti-inflammation, analgesia, anti-oxidation, anti-mutation, anti-tumor, immunity, brain protection, relief Alzheimer's disease effects. The total alkaloids of Uncaria uncaria are the main medicinal substances of Uncaria uncaria to exert its clinical therapeutic effect. The chemical structural formula of rhynchophylline is as follows: [0003] [0004] The total alkaloids of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/19A61K47/14A61K47/26A61K31/438A61P9/12A61P25/08
CPCA61K9/1075A61K9/19A61K31/438A61K47/14A61K47/26A61P9/12A61P25/08
Inventor 田宝成王盟季旭明毕倩宇崔红霞吕传峰
Owner 王盟