Unlock instant, AI-driven research and patent intelligence for your innovation.

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

A technology of photodynamic therapy, aminolevulinate, used in the field of treatment or diagnosis of cancerous or non-cancerous conditions in the lower part of the gastrointestinal system or in the female reproductive system, capable of solving problems such as reduced efficacy of preparations

Inactive Publication Date: 2015-01-28
PHOTOCURE
View PDF10 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

[0118] Embodiment 1 - the suppository containing 5-ALA hexyl ester

[0119] Each suppository (2g) contains:

[0120] 5-aminolevulinic acid hexyl ester hydrochloride (HAL HCl) 100mg, 10mg or 0.8mg, ethylenediaminetetraacetic acid disodium salt (EDTA) 40mg

[0121] Appropriate amount of Witepsol S 55 or S 58

[0122] 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

[0123] Example 2 - Stability of 5-ALA hexyl ester in suppositories, based on Witepsol S55

[0124] 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.

[0125] Table 1100 mg HAL HCl stability based on Witepsol S 55

[0126]

[0127] *The test value is calculated as % of the theoretical concentration of HAL HCl in the preparation

[0128] 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

[0129] Example 3 - Stability of 5-ALA hexyl ester in suppositories, based on Witepsol S58

[0130] 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.

[0131] Table 2. Stability of 100 mg HAL HCl, based on Witepsol S 58

[0132]

[0133] *The test value is calculated as % of the theoretical concentration of HAL HCl in the preparation

[0134] 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.

[0135] Reference ratio

[0136] 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 was...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
melting pointaaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The present invention relates to a solid pharmaceutical product provided in the form of a suppository which comprises a photosensitiser which is a 5-ALA ester of general formula I, or a pharmaceutically acceptable salt thereof: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ R 2 2 N-CH 2 COCH 2 -CH 2 CO-OR 1 €ƒ€ƒ€ƒ€ƒ€ƒ(I) (wherein R 1 represents a substituted or unsubstituted, straight-chained, branched or cyclic alkyl group; and each R 2 independently represents a hydrogen atom); and at least one pharmaceutically acceptable carrier or excipient which is a hard fat or a mixture of hard fat and additives. The pharmaceutical product may be used in the photodynamic treatment of cancer, and infections associated with cancer, and in the treatment of non-cancerous conditions, in particular in treating cancerous or non-cancerous conditions in the female reproductive system, for example cervical cancer and infections caused by the human papillomavirus.

Description

[0001] The application date is December 12, 2008, the application number is 200880120455.X, and the invention title is "Application of 5-aminolevulinic acid and its derivatives in solid form in photodynamic therapy and diagnosis" divisional application. technical field [0002] 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 [0003] Photodynamic therapy (PDT) is a relatively new te...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/14A61P35/00
CPCA61K9/28A61K41/0057A61K9/2866A61K9/4858A61K9/284A61K49/00A61K9/5073A61K9/1635A61K9/2054A61K9/02A61K49/0021A61K9/2077A61K9/0075A61K9/0031A61K9/1652A61K9/5042A61K9/205A61K9/14A61K31/197A61K9/2846A61K31/221A61K9/2013A61K9/4891A61K9/48A61K9/20A61K41/0061A61K9/2886A61K9/0034A61P1/00A61P15/00A61P31/20A61P35/00
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