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Modified amylase-based nanometer helical oil phase-triggered quick-release material and preparation method thereof

A technology of amylose and oil phase, applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve problems such as stimulating dilated blood vessels, unfavorable blood pressure, hyperlipidemia, etc. To achieve the effect of promoting formation and maintenance, improving hydrophilic performance and improving lipophilicity

Inactive Publication Date: 2013-07-31
THE FIRST AFFILIATED HOSPITAL OF MEDICAL COLLEGE OF XIAN JIAOTONG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the emulsification stability of fat microemulsion is poor, and it is easy to leak propofol, causing injection pain; a large amount of fat emulsion can easily cause hyperlipidemia; at the same time, fat emulsion is also easy to breed bacteria, which is not conducive to drug preservation
[0004] Phosphorylmethoxypropofol is a prodrug prodrug of propofol that has entered into clinical trials, and has the advantages of good water solubility and no injection pain, but phosphorylmethoxypropofol needs to be enzymatically decomposed into propofol Propofol can only exert its drug effect, so the onset time and clearance time are prolonged, and the peak concentration is reduced. At the same time, it enzymatically hydrolyzes a molecule of propofol, accompanied by a molecule of formaldehyde, which stimulates the expansion of blood vessels and causes blood vessel irritation pain, which is also not conducive to maintenance of blood pressure

Method used

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  • Modified amylase-based nanometer helical oil phase-triggered quick-release material and preparation method thereof
  • Modified amylase-based nanometer helical oil phase-triggered quick-release material and preparation method thereof
  • Modified amylase-based nanometer helical oil phase-triggered quick-release material and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0037] see figure 2 , the preparation method of the nano-helical oil phase triggered immediate-release body based on modified amylose, comprising the following steps:

[0038] 1) Preparation of propionate amylose

[0039] Dissolve 1 g of amylose in 50 mL of DMSO solution at 80 °C, stir for 1 h, add 0.3 mL of propionic anhydride and 0.2 mL of 1-methylimidazole, react at 80 °C for 4 h, and collect amylose propionate by suction filtration with acetone precipitation.

[0040] Identification of the propionate amylose helical structure:

[0041] Such as image 3 X-ray diffraction patterns of amylose and propionate amylose are shown. The characteristic peaks of amylose are 14.9, 17.1, 19.6, 22.1, 23.7, etc., which are characteristic peaks of B-type starch crystallization, that is, loose crystallization; while the characteristic peaks of propionate amylose are 7.8, 12.7, 19.6, It is the characteristic peak of V-type starch crystallization, that is, helical crystallization.

[00...

Embodiment 2

[0045] The preparation method of the nano-helical oil phase triggered immediate-release body based on modified amylose comprises the following steps:

[0046] 1) Preparation of propionate amylose

[0047] Dissolve 1 g of amylose in 50 mL of DMSO solution at 60 °C, stir for 1 h, add 0.2 mL of propionic anhydride and 0.1 mL of 1-methylimidazole, react at 60 °C for 8 h, and collect amylose propionate by suction filtration with acetone precipitation.

[0048] 2) Preparation of Propofol-supported Amylose Propofol Nanohelix Immediate-release Body

[0049] Disperse 20 mg of amylose propionate in 20 mL of pH7.4 PBS solution, drop 100 mg of propofol into the solution, and stir magnetically for 15 min. The starch solution loaded with propofol was poured into a dialysis bag with a pore size of 5000D, placed in 1L of PBS solution for dialysis for 2 hours, and the dialysate was changed twice in the middle to remove free propofol. Aspirate the liquid in the dialysis bag, filter it with a 20...

Embodiment 3

[0051] The preparation method of the nano-helical oil phase triggered immediate-release body based on modified amylose comprises the following steps:

[0052] 1) Preparation of propionate amylose

[0053] Dissolve 1 g of amylose in 50 mL of DMSO solution at 90 °C, stir for 1 h, add 0.3 mL of propionic anhydride and 0.15 mL of 1-methylimidazole, react at 90 °C for 3 h, and collect amylose propionate by suction filtration with acetone precipitation.

[0054] 2) Preparation of Propofol-supported Amylose Propofol Nanohelix Immediate-release Body

[0055] Disperse 20 mg of amylose propionate in 20 mL of pH7.4 PBS solution, drop 80 mg of propofol into the solution, and stir magnetically for 15 min. The starch solution loaded with propofol was poured into a dialysis bag with a pore size of 5000D, placed in 1L of PBS solution for dialysis for 2 hours, and the dialysate was changed twice in the middle to remove free propofol. Aspirate the liquid in the dialysis bag, filter it with a ...

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Abstract

The invention discloses a modified amylase-based nanometer helical oil phase-triggered quick-release material and a preparation method thereof. The preparation method comprises that amylase which can form a helical structure is modified, then is coated with hydrophobic vein center action drugs such as propofol and forms a helical brain localization quick-release system. The helical brain localization quick-release system has good dispersibility in a water phase, has uniform particle sizes, has a stable particle size for a long time, does not leak propofol easily, can be stored easily, and reduces propofol injection pain. After being triggered by the oil phase, the modified amylase-based nanometer helical oil phase-triggered quick-release material can fast release propofol and is conducive to fast release of propofol at the blood-brain barrier. The preparation method has simple processes, adopts the nontoxic raw materials, does not produce toxic substances in production, carries out disinfection easily and can be industrialized easily.

Description

technical field [0001] The invention belongs to the technical field of brain-targeted immediate-release bodies, and relates to a nano-helical oil-phase triggered immediate-release body based on modified amylose and a preparation method thereof. Background technique [0002] Propofol, also known as 2,6-dipropofol, referred to as propofol, the chemical formula is C 12 h 18 O. Propofol contains a phenol structure, so it has strong lipophilicity, and has the advantages of rapid induction of anesthesia, rapid recovery, and no accumulation. However, propofol has poor hydrophilicity and cannot be directly injected into the human body. [0003] In order to improve the water solubility of propofol, various dosage forms of propofol drug carriers and precursors have been developed. At present, propofol fat emulsion is the most common in clinical practice, and there are many brands, such as Diprivan, Jingan, Dishening, Limengxin, Dishening, Leweijing, Jingan and so on. The method h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K47/36A61K45/00A61K31/05A61P23/00
Inventor 高巍景桂霞徐礼鲜张惠
Owner THE FIRST AFFILIATED HOSPITAL OF MEDICAL COLLEGE OF XIAN JIAOTONG UNIV
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