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Photosensitive medicinal preparation containing amino poly-carboxylic acid modification tetraphenylporphyrin compound and purpose thereof

A technology of tetraphenylporphyrin and amino polycarboxylic acid, which is applied in the field of medicine, can solve problems such as poor solubility, influence on the stability of curative effect, and molecular polarity reduction, and achieve broad application prospects, high fluorescence quantum yield and Effects of optical stability, good biocompatibility

Active Publication Date: 2013-06-12
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the strong fat solubility of porphyrin itself, and the introduction of four benzene rings, its molecular polarity becomes smaller, and its solubility in water is poor, which reduces the bioavailability of the photosensitizer and affects the stability of the curative effect.

Method used

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  • Photosensitive medicinal preparation containing amino poly-carboxylic acid modification tetraphenylporphyrin compound and purpose thereof
  • Photosensitive medicinal preparation containing amino poly-carboxylic acid modification tetraphenylporphyrin compound and purpose thereof
  • Photosensitive medicinal preparation containing amino poly-carboxylic acid modification tetraphenylporphyrin compound and purpose thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 tablet

[0027] Get 0.3kg amino polycarboxylic acid modified tetraphenylporphyrin compound, add 0.5kg starch, 0.1kg magnesium stearate, 0.2kg carboxymethyl cellulose, 2.7kg ethanol (volume percentage composition is 70%), 2.5kg Microcrystalline cellulose and 3.2kg cornstarch are mixed thoroughly to form wet granules, dried at 60-70°C for 2-4 hours, and pressed into tablets. Tablets are made into tablets. The excipients used as excipients include magnesium sulfate, corn starch, and talcum powder. The specifications are: 5mg, 10mg, 20mg, 50mg, and 100mg.

[0028] In practice, the tetraphenylporphyrin compound modified with aminopolycarboxylic acid is the compound represented by the following formula (I) and its pharmaceutically acceptable salts such as potassium salt, sodium salt, ammonium salt and the like.

[0029]

[0030] Among them, R 1 = H, OH, OCH 3 ;

[0031]

Embodiment 2

[0032] Embodiment 2 capsules

[0033] Get 0.3kg amino polycarboxylic acid modified tetraphenylporphyrin compound, add 0.02kg magnesium stearate, 0.2kg carboxymethyl cellulose, 0.48kg microcrystalline cellulose, fully stir and mix to make wet granules, and make the The wet granules are directly dried at 60-70° C. for 2-4 hours, and then filled into empty capsule shells, and each capsule contains 20 mg of amino polycarboxylic acid modified tetraphenylporphyrin compound.

Embodiment 3

[0034] Embodiment 3 sustained and controlled release tablet

[0035] Get 0.3kg aminopolycarboxylic acid modified tetraphenylporphyrin compound, add 0.07kg hydroxypropyl methylcellulose, 0.25kg carboxymethylcellulose, 0.37kg ethanol (volume percentage is 70%), 0.1kg hard Magnesium fatty acid, etc. are fully stirred and mixed to form wet granules, dried at 60-70°C for 2-4 hours, and pressed into tablets.

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Abstract

The invention discloses a photosensitive medicinal preparation containing amino poly-carboxylic acid modification tetraphenylporphyrin compound. Each unit dose contains 1mg-100mg of the amino poly-carboxylic acid modification tetraphenylporphyrin compound. The each unit dosage is the total amount of the medicinal preparation used everyday. The amino poly-carboxylic acid modification tetraphenylporphyrin compound can be used in combination with other medicine or is singly used. Through addition of a drug carrier which is acceptable in pharmacy, the amino poly-carboxylic acid modification tetraphenylporphyrin compound accounts for 0.5%-40% the total weight of the medicinal preparation and can be prepared to any dosage form accepted clinically. The invention further provides application of the medicinal preparation on preparation of photosensitive antitumor drug and in the near infrared fluorescence imaging filed. The photosensitive medicinal preparation containing the amino poly-carboxylic acid modification tetraphenylporphyrin compound is low in toxicity, convenient to apply, wide in tumor suppression spectrum, good in tumor control rate, good in effect of malignant tumor treatment through photodynamic therapy, high in fluorescence quantum yield and optical stability in a near-infrared area, good in biocompatibility, capable of having a certain ability of penetrating the biological barrier, and wide in application prospect in the near infrared fluorescence imaging field.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical preparation containing amino polycarboxylic acid modified tetraphenylporphyrin compound and its application in photodynamic therapy of tumors and near-infrared fluorescence imaging. Background technique [0002] Photodynamic therapy (PDT) is a new technology for tumor treatment that came out in the late 1970s. It is the product of the organic combination of laser technology, light guide technology, optical information processing technology, biophotochemical technology and modern medical technology. At present, it has been approved and recognized by the health departments of many countries, and has become a routine method of tumor treatment, which is widely promoted and applied clinically. [0003] Because malignant tumors have the characteristics of rapid growth, easy recurrence, and easy metastasis, it is difficult to eradicate tumors and take into ...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K49/00A61P35/00
Inventor 刘天军洪阁曹波陈靖京毛丽娜吕丰
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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