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A modified amylose-based nanohelical oil-phase triggered immediate-release body and its preparation method

A technology of amylose and oil phase, which is applied in the direction of medical preparations containing non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problem of onset time, prolonged clearance time, and poor emulsification stability of fat microemulsion , Fat emulsion is easy to breed bacteria and other problems, to achieve the effect of improving hydrophilic performance, not easy to leak, and excellent reaction efficiency

Inactive Publication Date: 2014-10-29
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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  • A modified amylose-based nanohelical oil-phase triggered immediate-release body and its preparation method
  • A modified amylose-based nanohelical oil-phase triggered immediate-release body and its preparation method
  • A modified amylose-based nanohelical oil-phase triggered immediate-release body and its preparation method

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Experimental program
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Effect test

Embodiment 1

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

[0038] 1) Preparation of propionate amylose

[0039] Dissolve 1 g of amylose in 50 mL 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 propionate amylose by acetone precipitation and suction filtration.

[0040] Identification of the helical structure of propionate amylose:

[0041] like 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 the characteristic peaks of type B-starch crystallization, that is, loose crystals; while the characteristic peaks of propionate amylose are 7.8, 12.7, 19.6, respectively. It is the characteristic peak of V-starch crystallization, namely spiral crystallization.

[0042] ...

Embodiment 2

[0045] The preparation method of the nano-spiral 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 propionate amylose by acetone precipitation and suction filtration.

[0048] 2) Preparation of propofol propofol nano-helix immediate release on amylose propionate

[0049] Disperse 20 mg of propionate amylose in 20 mL of pH 7.4 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 a 1L PBS solution for 2h dialysis, and the dialysate was changed twice in between to remove free propofol. Aspirate the liquid in the dialysis bag, filter it with a 200nm syringe fi...

Embodiment 3

[0051] The preparation method of the nano-spiral 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 propionate amylose by acetone precipitation and suction filtration.

[0054] 2) Preparation of propofol propofol nano-helix immediate release on amylose propionate

[0055] 20 mg of propionate amylose was dispersed in 20 mL of pH 7.4 PBS solution, 80 mg of propofol was dropped into the solution, and the solution was magnetically stirred for 15 min. The starch solution loaded with propofol was poured into a dialysis bag with a pore size of 5000D, placed in a 1L PBS solution for 2h dialysis, and the dialysate was changed twice in between to remove free propofol. Aspirate the liquid in the dialysis bag,...

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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-located quick-release bodies, and relates to a nano-spiral oil phase-triggered quick-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, chemical formula C 12 H 18 O. Propofol contains phenol structure, so it has strong lipophilicity, and has the advantages of rapid induction of anesthesia, rapid recovery, and no accumulation. It is the main intravenous anesthetic for clinical anesthesia induction, maintenance and sedation of critically ill patients in ICU. However, propofol has poor hydrophilicity and cannot be directly injected into the human body. [0003] In order to improve the water solubility of propofol, propofol drug carriers and precursors in various dosage forms have been developed. At present, the most common clinically is propofol fat emulsion preparation, there are ma...

Claims

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Application Information

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Patent Type & Authority Patents(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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