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Sustained release preparation of isothiocyanate compound

A technology of ester compounds and isothiocyanic acid, applied in the direction of non-active ingredients of polymer compounds, active ingredients of esters, medical preparations of non-active ingredients, etc., can solve the problem of making stable and commercially available sustained-release preparations , Poor formability and solubility, easy to volatilize, etc.

Active Publication Date: 2014-12-03
JC (WUXI) CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, because ITCs are incompatible with most pharmaceutical excipients, and are easy to volatilize, their formability and solubility are poor, making it difficult to make stable and commercially available sustained-release preparations.
[0004] In summary, there is still a lack of a pharmaceutical composition of sustained-release isothiocyanate compounds or derivatives thereof with better performance in the art.

Method used

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  • Sustained release preparation of isothiocyanate compound
  • Sustained release preparation of isothiocyanate compound
  • Sustained release preparation of isothiocyanate compound

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0131] The present invention also provides a preparation method of a sustained-release preparation of an isothiocyanate compound or a derivative thereof, the method comprising the following steps:

[0132] Provide isothiocyanate compounds or their derivatives;

[0133] Melting the sustained-release material and mixing it with the isothiocyanate compound or its derivatives to form a first dispersion;

[0134] The first dispersion is mixed with other excipients and prepared into a formulation.

[0135] The isothiocyanate compounds or their derivatives can be prepared by conventional methods, or obtained through commercial channels.

[0136] In another preferred example, the preparation is prepared by the following method:

[0137] The active ingredients are mixed and melted with biodegradable polymer materials, and then extruded into strips through a porous device. The strips are generally about 1mm in diameter. After being cut into lengths containing a single dose of medicine...

Embodiment 1

[0143] Embodiment 1: Excipient compatibility test

[0144] Method: Isothiocyanate compounds and auxiliary materials are mixed in a certain proportion (methods include simple mixing, melting, etc.). A blank group of auxiliary materials is set in parallel for each auxiliary material. After preparation, put it into a glass container, seal it, and then place it at 60°C for inspection, and detect it on day 0, day 5, and day 10.

[0145] Determination conditions: HPLC-UV method is used to determine the content of isothiocyanate compounds in the mixture, and the impurities in the process are monitored.

[0146] result:

[0147] Some of the data are as follows (investigated with phenylethyl isothiocyanate as the target):

[0148] The content change of phenylethyl isothiocyanate in the different auxiliary materials of table 1

[0149]

[0150] From the data in the above table, it can be seen that the compatibility of the commonly used sustained and controlled release materials h...

Embodiment 2

[0152] Embodiment 2: auxiliary material stability experiment

[0153] On the basis of the excipient compatibility test in Example 1, the stabilizing effect of different excipients on isothiocyanate compounds was further investigated.

[0154] Method: Melt or grind the excipients and isothiocyanate compounds in a certain proportion and mix them evenly, put them in a vial, expose them at 60°C, and measure the isothiocyanate in the mixture by HPLC-UV method at different time points content of esters.

[0155] The results are shown in Table 2-Table 3.

[0156] Table 2

[0157]

[0158] table 3

[0159]

[0160] The results of Tables 2 and 3 suggest:

[0161] Different auxiliary materials have a protective effect on the stability of isothiocyanate compounds under the test conditions, and medium chain oil> beeswax, microcrystalline wax, carnauba wax> other auxiliary materials; In terms of additives, wax or oil excipients have significant advantages in inhibiting the decli...

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Abstract

Disclosed is a sustained-release preparation or capsule of isothiocyanate compounds or derivatives thereof, the sustained-release preparation containing (a) a therapeutically effective amount of isothiocyanate compounds or derivatives thereof; (b) a pharmaceutically acceptable carrier, and the capsule containing a capsule shell and a pharmaceutical composition consisting of components (a) and (b) inside the capsule shell. The sustained-release preparation is stable and has a good compatibility and sustained-release effect; the capsule significantly improves the stability of the drug, and masks the smell of the isothiocyanate compounds and reduces irritation.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular, the invention relates to a slow-release preparation of isothiocyanate compounds or derivatives thereof. Background technique [0002] PCT application WO2007 / 056941 (Use of isothiocyanate compounds in prostate diseases and skin cancer) reported the role of isothiocyanate compounds in the treatment and prevention of prostate diseases. The above-mentioned isothiocyanate compounds have the characteristics of reliable quality and mature technology, but there are many deficiencies in clinical application. Studies have shown that the half-life of isothiocyanate compounds in the human body is very short, about 2 hours, and they belong to drugs that are rapidly metabolized and excreted. Therefore, with common preparations, patients need to take medication multiple times to maintain the required blood drug concentration, the desired therapeutic effect can be achieved, which brings...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/26A61K47/44A61K47/42A61K47/38A61K47/36A61K47/34A61K47/32A61P35/00A61P13/08A61P17/00A61P29/00
CPCA61K9/4841A61K31/26A61P13/08A61P17/00A61P29/00A61P35/00
Inventor 程景才顾国林王永霞
Owner JC (WUXI) CO INC
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