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Pharmaceutical composition containing alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate, tartrate or combination thereof, and preparation method therefor

A technology of octaconediamide and composition, which is applied in the field of preparation of the pharmaceutical composition, can solve problems such as high hygroscopicity, difficulty in maintaining a solid state, difficulty in mass production of solid preparations, and influence on physical and chemical stability, and achieve simplified production and Commercialization process, prevention of production of related substances, effects of safe manufacturing

Pending Publication Date: 2021-06-08
CRYSTAL GENOMICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, since the alkylcarbamoylnaphthyloxyoctenoyl hydroxyamide has a property of absorbing moisture in the atmosphere, there is a problem of being susceptible to physicochemical stability
Extensive purification operations to remove related substances produced by moisture absorption increase production costs, and high hygroscopicity makes it difficult to maintain a solid state, making it difficult to mass-produce solid dosage forms
Disadvantage is the need for a separate refrigerated storage device or method (e.g. packaging)

Method used

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  • Pharmaceutical composition containing alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate, tartrate or combination thereof, and preparation method therefor
  • Pharmaceutical composition containing alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate, tartrate or combination thereof, and preparation method therefor
  • Pharmaceutical composition containing alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate, tartrate or combination thereof, and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1 to 4

[0102] In order to prepare convenient administration and easy-to-manufacture tablet compositions, based on the results of compatibility studies, use alkylcarbamoylnaphthyloxyoctenoyl hydroxyamide phosphate and as shown in Table 1 in the composition Additives with defined stability are used to prepare tablet compositions.

[0103] (E)-N1-(3-(dimethylamino)propyl)-N8-hydroxyl-2-((naphthalene-1-yloxy)methyl)-2-octenediamide phosphate compound (CG200745PPA ) as alkylcarbamoylnaphthyloxyoctenoyl hydroxyamide phosphate. The unit of weight in the table below is mg.

[0104] Due to the poor-flowing nature of CG200745PPA, the tablet composition was prepared by a granulation method using ethanol as a binder instead of a direct compression method. In addition, due to the characteristics of the CG200745PPA raw material, it may be difficult to separate the tablet from the punch when subjected to compression pressure during tablet compression. Therefore, the ratio of the added excipients...

Embodiment 5 to 8

[0112] In order to improve the sticking phenomenon, tablets were manufactured by increasing the amount of excipients and decreasing the amount of main ingredients (as shown in Table 3). In addition, Table 4 shows the results of tablet compression evaluation.

[0113] [table 3]

[0114]

[0115]

[0116] [Table 4]

[0117]

Embodiment 9 and 10

[0119] CG200745PPA can be used as an anticancer agent. Most of the subjects to be administered are patients undergoing chemotherapy. Therefore, if the tablet size is increased, not only is the tablet very difficult to take, but there is also a fear of rejection when taking the tablet. Therefore, in the present invention, it is intended to improve this. Capsule formulation compositions with less physical impact on manufacture and simple processes such as tablet compression process are prepared. As shown in the compositions of Table 5, for ease of dosing, the minimum amount of manufacturable excipients was used, and to simplify the process, direct mixing was employed. In addition, Table 7 shows the results of evaluating fluidity according to the angle of repose measurement standard shown in Table 6 (General Chapters; 1174, USP) using an angle of repose tester and a degree of sticking.

[0120] EMBO CAPS (hard capsule, manufactured by Suheung) was used for capsule #0 and capsu...

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Abstract

The present invention relates to a pharmaceutical composition containing an alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate compound (hereinafter referred to as CG200745PPA) or a derivative thereof, and can provide a pharmaceutical composition in a tablet, granule, powder, capsule, dry syrup or injection form. By providing the composition in various forms, a suitable form can be selected and easily applied when oral administration is difficult.

Description

technical field [0001] The present invention relates to a pharmaceutical composition comprising an alkylcarbamoylnaphthyloxyoctenoyl hydroxyamide phosphate compound, an alkylcarbamoylnaphthyloxyoctenoyl hydroxyamide tartrate compound, or a combination thereof. [0002] In addition, the invention relates to a process for the preparation of the pharmaceutical composition. Background technique [0003] Histones are basic proteins that bind to DNA in the eukaryotic nucleus, and reversible histone acetylation occurs on the amino groups of specific lysine residues in each histone molecule. This histone acetylation reaction is related to the formation of chromatin higher-level structure or cell division cycle, so it participates in the regulation of gene information expression, and is stably regulated by histone acetyltransferase (HAT) and histone deacetylase (HDAC) . These enzymes are known to induce transcriptional activity by neutralizing the positive charge of lysine residues...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/165A61K9/00A61P35/00
CPCA61P35/00A61K31/165A61K9/1623A61K9/2018A61K9/19A61K9/0019A61K9/0053A61K9/0095A61K9/2009A61K9/2013A61K9/2054A61K9/485A61K9/4858A61K9/4866
Inventor 曹在平曹重明
Owner CRYSTAL GENOMICS INC