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Stabilizer for hydrophobic compounds

A technology of hydrophobic compounds and stabilizers, applied in the directions of active ingredients of hydroxyl compounds, non-active ingredients of polymer compounds, drug combinations, etc., can solve problems such as insufficient stability.

Inactive Publication Date: 2009-03-25
NANOCARRIER
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, neither of the above methods can achieve sufficient stability

Method used

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  • Stabilizer for hydrophobic compounds
  • Stabilizer for hydrophobic compounds
  • Stabilizer for hydrophobic compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Example 1: Stabilization of hinokitiol under the action of block copolymer

[0058] Weigh 1 mg of hinokitiol (Wako, Osaka) and 10 mg of PEG-PBLA-5-20-100, PEG-PBLA-12-40-50, or PEG-PBLA-12-50-50 in a screw cap test tube bottle , after dissolving in dichloromethane, dichloromethane was volatilized under a nitrogen stream to obtain a film formed of hinokitiol and block copolymer. 3 ml of ultrapure water was added to the film, and stirred at 4° C. for 12 hours under light-shielding. The obtained microcapsule solution was irradiated with ultrasonic waves for 5 minutes, the particle diameter was measured, and the hinokinaki alcohol not encapsulated in the microcapsules was separated by gel filtration (PD-10 columns). Hinokitiol has a maximum absorption peak at 330nm in water, and hinokitiol wrapped in block copolymer microcapsules has maximum absorption peaks at 324nm and 372nm. The following table 1 shows the embedding rate (the ratio of the amount of drug embedded in the...

Embodiment 2

[0064] Example 2 The stability of Hinokitiol under the action of block copolymer to light

[0065] The aqueous solution of microencapsulated hinokitiol (the sample of experiment 1-6 shown in table 1), under the light of laboratory, preserves at room temperature, to their absorption intensity change through time measurement, as figure 2 As shown, the absorption intensity at 324 nm was maintained at 85% after one day, 53% after 7 days, and 40% after 14 days, indicating that the photolysis of hinokinol was inhibited by microencapsulation. again, figure 2 The results shown represent the average of the absorbance at 324 nm for the microcapsules of experiments 1-6. That is, it can be considered figure 1 The isomerization reaction shown is sterically hindered by microencapsulation. In addition, the hindrance of this isomerization reaction was also observed when hinokitiol / block polymer was 1mg / 1.2mg as the starting substance (that is, hinokitiol was in a state of excess relative...

Embodiment 3

[0066] Example 3: Thermal Stability of Microencapsulated Hinokitiol under the Effect of Block Copolymer

[0067] The aqueous solution of microencapsulated hinokitiol (the sample of experiment 1-6 shown in table 1) is stored under shading at 37°C, and their absorption intensity changes are measured over time, and the absorption maximum at 324nm is after 14 days Still remain at 97%, show that microencapsulation effect makes the thermal decomposition of hinokitiol be suppressed completely ( image 3 ). Since the spectrum in the case of thermal decomposition is exactly the same as the spectrum in the case of photolysis, it can be considered that the decomposition products in the case of photolysis and thermal decomposition are cyclopentene derivatives, and that the inhibition of thermal decomposition and the inhibition of photolysis are caused by the same caused by the mechanism.

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Abstract

The present invention provides a stabilizer for hydrophobic compounds, particularly hinokitiol, which consists of a block copolymer comprising at least a hydrophilic segment and a hydrophobic segment as the essential components.

Description

technical field [0001] The present invention relates to a stabilizer for stabilizing light- and heat-unstable hydrophobic compounds, especially hinokitiol, and a stabilizer composed of a block copolymer containing at least a hydrophilic segment and a hydrophobic segment and a stable method to exploit it. Background technique [0002] Regardless of whether it is a natural product or a synthetic compound, and regardless of whether it is a compound with excellent activity, there are many cases where it cannot be practically used in the fields of medicine, food, and agricultural chemicals due to lack of stability. For example, hinokitiol (β-thujaplicin), 4-isopropenyltropolone (β-dolabrin), γ-thujaplicin, etc. (γ-thujaplicin), α-thujaplicin (α-thujaplicin), and 4-acetyltroplone (4-acetyltroplone) and other compounds having a 7-membered ring. Among them, hinokitiol was purified from Taiwan hinoki by Ye Fu et al. in 1963, and its chemical structural formula was determined, and i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K31/07A61K31/122A61K31/365A61K31/375A61K45/00A61P31/04A61P43/00A61K47/34
CPCA61K31/375A61K31/07A61K9/1075A61K31/365A61K31/122A61P31/04A61P43/00A61K47/42
Inventor 西谷孝子加藤泰己
Owner NANOCARRIER
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