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Solid compositions comprising 5-aminolevulinic acid

A composition and solid-state technology, which can be used in medical preparations containing active ingredients, drug combinations, and medical preparations with non-active ingredients, etc., and can solve problems such as delayed culture period

Inactive Publication Date: 2012-11-28
PHOTOCURE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is therefore a delay in the form of an incubation period between the administration of the precursor and the process of photoactivation and thus diagnosis

Method used

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  • Solid compositions comprising 5-aminolevulinic acid
  • Solid compositions comprising 5-aminolevulinic acid
  • Solid compositions comprising 5-aminolevulinic acid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0180] Embodiment 1: solid composition among the present invention

[0181] Coated capsules containing n-hexylaminolevulinate (HAL) hydrochloride (HAL HCl) (Phototherapy ASA, Norway) by mixing the compounds listed under "Capsule Composition" at a temperature above their melting point to prepare. The mixture was poured into HPMC capsules and banded with a mixture of HPMC (3.1 mg), gellan gum (0.015 mg) and trisodium citrate (0.05 mg) in water. The capsules are moisture-proof coating (6.3mg / cm 2 ) and Opadry (AMB) coating, followed by enteric coating (8mg / cm 2 , for 80% of the L 30D-55 and 20% FS 30D, both dispersed in water) to form a pH-sensitive film that decomposes at pH 6.5 and above.

[0182]

[0183] Of all the capsules containing Miglyol 812 as triglyceride, capsule A is a solid pharmaceutical product outside the scope of the present invention as it contains no emulsifier. Capsules B and C contain anionic emulsifiers, and capsules D to H contain nonionic emu...

Embodiment 2

[0184] Example 2: Dissolution of HAL

[0185] Capsules A-H prepared in Example 1 were used for in vitro dissolution studies. In order to simulate the human intraperitoneal environment, the capsule was first immersed in 500 ml of 0.1M HCl dissolution medium (1) at a temperature of 37° C. for one hour. The capsules were then taken out of the medium and immersed in 500 ml of pH 6.5 phosphate buffered aqueous solution (2) at a temperature of 37° C. to simulate the internal environment of the human terminal ileum, ie the water environment and pH. A "USP 711" complying dissolution apparatus equipped with paddles and sinkers was used in two immersions. Capsules are placed on the sinker and immersed in the dissolution medium. The rotation speed was set at 75 rpm. 2 ml samples of dissolution medium were manually withdrawn at 5, 15, 30, 60, 120 and 180 minutes, respectively. The sample was filtered (40 μm HDPE filter membrane) and its HAL content was detected by HPLC. The HAL con...

Embodiment 3

[0196] Example 3: In vivo release of HAL HCl

[0197] In order to evaluate the transfer of enteric-coated capsules, that is, the solid pharmaceutical product of the present invention, in the gastrointestinal tract to determine the release location of the composition in the enteric-coated capsules and the release of HAL HCl in the emptied, i.e., cleared colon. distribution, we performed gamma-scan imaging studies on healthy male volunteers.

[0198] Gamma scan imaging can assess the physical integrity of the solid pharmaceutical product of the present invention as it moves through the gastrointestinal tract. Detailed information on the timing and anatomical location of the breakdown of the drug can thus be obtained. will Enterion TM Site-specific delivery capsules are used in gamma-scan imaging studies, thus allowing drug delivery to specific sites within the GI tract. The capsule is 35mm long and 10-12mm in diameter, and can deliver solutions, suspensions or powders to sp...

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Abstract

This invention relates to solid compositions and solid pharmaceutical products for use in methods of photodynamic diagnosis of cancer, pre-cancerous and non-cancerous conditions in the lower part of the gastrointestinal system. The solid pharmaceutical compositions and pharmaceutical products comprise an active ingredient which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative of 5-ALA or pharmaceutically acceptable salts thereof. The invention relates further to methods of photodynamic diagnosis of cancer, pre-cancerous and non-cancerous conditions of the lower gastrointestinal tract, wherein the solid pharmaceutical compositions and pharmaceutical products are used.

Description

technical field [0001] The invention relates to a solid composition and a solid pharmaceutical product used in a photodynamic diagnosis method for cancer, precancerous lesions and non-cancerous lesions in the lower half of the gastrointestinal system. The solid pharmaceutical composition and pharmaceutical product contain an active ingredient, which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative of 5-ALA or a pharmaceutically acceptable salt thereof. The present invention also relates to a photodynamic diagnosis method for cancer, precancerous lesions and non-cancerous lesions of the lower gastrointestinal tract, wherein the solid pharmaceutical composition and pharmaceutical products are used. Background technique [0002] Photodynamic diagnosis (PDD) is a relatively new technique used to diagnose precancerous, cancerous, and noncancerous lesions. PDD involves the application of a photosensitizer or a precursor thereof to the site of treatment. The photosen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K9/02A61K47/14A61K31/197
CPCA61K9/2013A61K47/14A61K9/02A61K9/4858A61K51/00A61K41/0061A61K49/0036A61K49/00A61K9/0031A61K31/197A61K9/0009A61P11/02A61P35/00A61K9/20A61K9/48
Inventor 欧迪维格·塞莱格·赫兰格雷·斯滕斯鲁德比约恩·克莱姆乔恩·埃瑞克·布伦德恩阿斯拉克·戈达尔乔·克拉韦内斯
Owner PHOTOCURE
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