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Phthalocyanine-temperature sensitive gel preparation and preparation method thereof

A temperature-sensitive gel and gel preparation technology, which is applied in antifungal agents, pharmaceutical formulations, aerosol delivery, etc., can solve the problems of high skin phototoxicity, clinical application limitations, and complex synthesis routes, and achieve easy-to-obtain synthetic raw materials, The liquid is not easy to lose, and the effect of high biocompatibility

Active Publication Date: 2019-08-23
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Hematoporphyrin derivatives have shown certain curative effects, but also exposed serious shortcomings: the maximum absorption wavelength (380nm-420nm) is not in the red light region (650nm-800nm) with better transmittance to human tissue, and the skin phototoxicity is large , is a mixture, the composition is unstable, etc., so the clinical application is limited, so the development of a new generation of photosensitizers is an international research hotspot
However, the synthesis route of Pc4 is complicated, the preparation cost is high, and the stability is poor.

Method used

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  • Phthalocyanine-temperature sensitive gel preparation and preparation method thereof

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preparation example Construction

[0026] The preparation method of phthalocyanine-thermosensitive gel preparation of the present invention comprises the following steps:

[0027] (1) Weigh different amounts of Poloxamer 407 and Poloxamer 188, add deionized water, stir magnetically for 12-48 hours to disperse evenly, and refrigerate at 1-4°C for 12-72 hours to freeze The gel is fully swollen and dispersed evenly to obtain a temperature-sensitive gel matrix;

[0028] (2) dissolving phthalocyanine in water, dimethyl sulfoxide or ethanol to make a mother liquor of 0.5-2mmol / L;

[0029] (3) Take a certain amount of phthalocyanine mother liquor, add it into the temperature-sensitive gel matrix, and adjust the feeding ratio of the phthalocyanine mother liquor and the temperature-sensitive gel matrix, so that the weight content of phthalocyanine in the preparation is 0.001-1%. Stir evenly to obtain a photosensitizer-thermosensitive gel preparation; store in a refrigerator at 1-4°C for later use.

[0030] The phthalo...

Embodiment 1

[0033] (1) Synthesis and physical and chemical properties of silicon phthalocyanine

[0034] Synthesize a series of axially substituted phthalocyanine complexes with reference to Chinese patents ZL200610200598.4 and ZL201210155097.4, including bis[4-(1-methyl-4-acetylpiperazine)phenoxy]silicone phthalocyanine diiodide compound, bis[2-(4-piperidine)ethoxy]silicone phthalocyanine, bis[4-(2-aminoethyl)phenoxy]silicone phthalocyanine, bis[4-(2-N,N- Dimethylaminoethyl) phenoxy] silicon phthalocyanine diiodide, bis(N,N-dimethyl-4--piperidinyloxy) silicon phthalocyanine diiodide. The inventor of the above-mentioned patent is the same inventor as the present applicant.

[0035] (2) Synthesis and physicochemical properties of zinc phthalocyanine

[0036] A range of zinc phthalocyanines including 1-(N-methyl-4-morpholineethoxy)zinc phthalocyanine iodide, 2-(N-methyl-4-morpholineethoxy)zinc phthalocyanine iodide , 1-(4-piperazineethoxy)zinc phthalocyanine, 1-[4-(2-aminoethyl)phenoxy]zin...

Embodiment 2

[0039] Preparation and properties of phthalocyanine-thermosensitive gel preparation

[0040] Weigh 2.5g of poloxamer 407 and 0.2g of poloxamer 188, add 10g of deionized water, stir magnetically for 24 hours to disperse evenly, put them in a refrigerator at 4°C for 48 hours to fully swell the gel and disperse evenly. A thermosensitive gel matrix is ​​obtained. Dissolve bis[4-(2-aminoethyl)phenoxy]silicone phthalocyanine in dimethyl sulfoxide or ethanol to prepare a 1 mmol / L mother solution.

[0041] Take 0.9 mL of the above-mentioned thermosensitive gel base (TG), add 0.1 mL of bis[4-(2-aminoethyl)phenoxy] silicon phthalocyanine solution with a concentration of 1 mmol / L 1, and stir evenly to obtain TG with a concentration of 100 μM Bis[4-(2-aminoethyl)phenoxy]silicone phthalocyanine-thermosensitive gel preparation (the weight percentage of phthalocyanine is 0.0081wt%). Store in a 4°C refrigerator for later use.

[0042] The test method of phase transition temperature: phase ...

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Abstract

The invention belongs to the field of pharmaceutical preparations or photodynamic medicines, and particularly relates to a phthalocyanine-temperature sensitive gel preparation and a preparation methodthereof. The phthalocyanine-temperature sensitive gel preparation is prepared from 19-23 wt% of poloxamer 407, 1.1-1.7 wt% of poloxamer 188, 0.001-1 wt% of phthalocyanine and the balance water and organic solvents. The temperature sensitive gel preparation has the advantages that gel is changed into a solid quickly when the temperature reaches 29-31 DEG C, the medicine can be attached to the surface of the skin and serve as a local medicine dosage form for the skin, application is convenient, and medicine liquid is not easily lost. The phthalocyanine-temperature sensitive gel preparation canserve as a photosensitive medicament for treating tinea unguium and tinea pedis and has significant clinical application value.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations or photodynamic drugs, and in particular relates to a photosensitizer-thermosensitive gel preparation and a preparation method thereof. Background technique [0002] Photodynamic therapy (or photodynamic therapy), in essence, is the application of the photosensitization reaction of photosensitizers (or photosensitizers) in the medical field. The process of action is to first inject the photosensitizer into the body, and after a period of time (this waiting time is to allow the drug to be relatively enriched in the target body), the target body is irradiated with light of a specific wavelength (for the target in the body cavity, the target body can be irradiated with the help of optical fiber). The photosensitizer enriched in the target stimulates a series of photophysical and photochemical reactions under light excitation to generate active oxygen and destroy the target. Photodynamic th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K9/06A61K47/10A61P31/10A61P17/00
CPCA61K9/0014A61K9/06A61K41/0071A61K47/10A61P17/00A61P31/10
Inventor 黄剑东郑碧远林滔郭军
Owner FUZHOU UNIV
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