Use of 5-aminolevulinic acid and derivatives in a solid form for photodynamic treatment and diagnosis

A technology of aminolevulinic acid and photodynamic therapy, which is applied in the field of photodynamic therapy and diagnosis of diseases such as cancer, and can solve problems such as the reduction of the efficacy of preparations

Inactive Publication Date: 2010-11-24
PHOTOCURE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such preparations also generally address the reduced efficacy of known formulations when treating these areas of the body

Method used

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  • Use of 5-aminolevulinic acid and derivatives in a solid form for photodynamic treatment and diagnosis
  • Use of 5-aminolevulinic acid and derivatives in a solid form for photodynamic treatment and diagnosis
  • Use of 5-aminolevulinic acid and derivatives in a solid form for photodynamic treatment and diagnosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] Embodiment 1 - the suppository containing 5-ALA hexyl ester

[0115] Each suppository (2g) contains:

[0116] 5-aminolevulinic acid hexyl ester hydrochloride (HAL HCl) 100mg, 10mg or 0.8mg, ethylenediaminetetraacetic acid disodium salt (EDTA) 40mg

[0117] Appropriate amount of Witepsol S 55 or S 58

[0118] Suppositories are prepared by suspending HAL HCl and ethylenediaminetetraacetic acid disodium salt in liquid Witepsol. The mixture is filled into molded and cooled suppositories.

Embodiment 2

[0119] Example 2 - Stability of 5-ALA hexyl ester in suppositories, based on Witepsol S55

[0120] Suppositories containing hexyl 5-aminolevulinate hydrochloride (HAL HCl) were prepared as described in Example 1. The stability of HAL HCl in suppositories (based on Witepsol S55) was investigated by HPLC analysis. Stability was tested at room temperature (25°C) and freezer temperature (2-8°C). The results are shown in Table 1 below.

[0121] Table 1 Stability of 100 mg HAL HCl, based on Witepsol S 55

[0122]

[0123] * The test value is calculated as % of the theoretical concentration of HAL HCl in the preparation

[0124] The results in Table 1 show that suppositories containing HAL HCl (based on Witepsol S55) are stable for at least 3 months at room and refrigerator temperatures.

Embodiment 3

[0125] Example 3 - Stability of 5-ALA hexyl ester in suppositories, based on Witepsol S58

[0126] Suppositories containing hexyl 5-aminolevulinate hydrochloride (HAL HCl) were prepared as described in Example 1. The stability of HAL HCl in suppositories (based on Witepsol S58) was studied by HPLC analysis. Stability was tested at room temperature (25°C) and freezer temperature (2-8°C). The results are shown in Table 2 below.

[0127] Table 2. Stability of 100 mg HAL HCl, based on Witepsol S 58

[0128]

[0129] * The test value is calculated as % of the theoretical concentration of HAL HCl in the preparation

[0130] The results in Table 2 show that suppositories containing HAL HCl (based on Witepsol S58) are stable for at least 3 months at room and refrigerator temperatures.

[0131] Reference ratio

[0132] Four batches of aqueous cream containing 160 mg / g methyl 5-aminolevulinate (MAL) were left at room temperature (25° C.) for 3 months and their MAL content w...

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Abstract

The present invention relates to the use of a photosensitiser which is 5-ALA or a precursor or derivative thereof (e.g. an ALA ester), in the manufacture of a pharmaceutical product for use in the photodynamic treatment or diagnosis of cancer, an infection associated with cancer, or in the treatment or diagnosis of a non-cancerous condition, wherein said pharmaceutical product is in the form of a solid. The invention also relates to solid pharmaceutical products for use in such methods, e.g. suppositories, pessaries, tablets, pellets and capsules which comprise 5-ALA or a precursor or derivative thereof (e.g. an ALA ester) and at least one pharmaceutically acceptable carrier or excipient. Such products are particularly suitable for use in the photodynamic treatment or diagnosis of cancerous or non not cancerous conditions in the lower part of the gastrointestinal system or in the female reproductive system, e.g. in the treatment or diagnosis of colorectal cancer or cervical cancer.

Description

technical field [0001] The present invention relates to methods of photodynamic therapy and diagnosis of conditions such as cancer, and in particular to solid pharmaceutical preparations comprising the photosensitizer 5-aminolevulinic acid (5-ALA) or its precursors or derivatives (e.g. 5-ALA esters) application in such methods. The pharmaceutical preparations described herein are particularly suitable for use in the treatment or diagnosis of cancerous or non-cancerous conditions in the lower part of the gastrointestinal system (especially the lower small intestine, colon and rectum) or the female reproductive system (ie uterus, cervix, vagina). Background technique [0002] Photodynamic therapy (PDT) is a relatively new technology used to treat various cancers and other diseases. PDT involves administration of a photosensitizer followed by exposure to photoactivating light to activate the photosensitizer and convert it into a cytotoxic form that causes cell destruction and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61P35/00A61K49/00A61K9/02A61K9/28A61K9/48A61K31/197
CPCA61K9/1652A61K9/5042A61K9/2866A61K9/205A61K9/4858A61K9/284A61K9/0031A61K9/5073A61K31/197A61K9/2846A61K9/1635A61K9/2013A61K9/4891A61K9/2054A61K9/02A61K49/0021A61K9/2077A61K9/0075A61K41/0061A61K9/2886A61K9/0034A61K31/221A61P1/00A61P15/00A61P31/20A61P35/00A61K9/14A61K9/20A61K9/28A61K9/48A61K41/0057A61K49/00
Inventor 乔·克拉韦内斯格雷·斯滕斯鲁德阿斯拉克·戈达尔乔恩·埃瑞克·布伦德恩比约恩·克莱姆
Owner PHOTOCURE
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