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2-amino-2-(2-[4-octyl phenyl]ethyl)-1,3-propanediol hydrochloride preparation and preparation method thereof

A technology of propylene glycol hydrochloride and octylphenyl, which is applied in pharmaceutical formulations, aerosol delivery, and medical preparations containing active ingredients. problems, to avoid the first-pass effect of the liver, enhance the curative effect, and have good compatibility

Inactive Publication Date: 2011-02-09
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, most of the current research on FTY720 focuses on the analysis of its pharmacological effects, and there are very few studies on its preparations. There are no reports about FTY720 creams and ointments at home and abroad.
The reason is that FTY720 is unstable in aqueous solution (pH>5.0), and has poor compatibility with most pharmaceutical excipients, making it difficult to establish quality standards for preparations

Method used

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  • 2-amino-2-(2-[4-octyl phenyl]ethyl)-1,3-propanediol hydrochloride preparation and preparation method thereof
  • 2-amino-2-(2-[4-octyl phenyl]ethyl)-1,3-propanediol hydrochloride preparation and preparation method thereof
  • 2-amino-2-(2-[4-octyl phenyl]ethyl)-1,3-propanediol hydrochloride preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Prescription Main drug and excipient name Dosage, mass percentage (g / g)

[0062] FTY720 0.1%

[0063] Glyceryl Monostearate 9%

[0064] White Petrolatum 7.5%

[0065] Liquid Paraffin 35%

[0066] Paraffin wax 3.3%

[0067] Span 60 3%

[0068] Methylparaben 0.1%

[0069] Tween 80 4%

[0070] Distilled water 38%.

[0071] Weigh the main ingredients and auxiliary materials according to the above proportions, heat white petrolatum, Span 60, liquid paraffin, solid paraffin and glyceryl monostearate to 80°C and melt through a No. 9 sieve (ie, 200 mesh sieve) to obtain the oil phase , standby; mix Tween-80, methyl p-hydroxybenzoate and distilled water, heat to 80°C to dissolve, cool to 25°C, adjust the pH to 3 with hydrochloric acid with a concentration of 3% by volume, and then add the main drug FTY720 to prepare The water phase was obtained and set aside; in a water bath at 80°C and stirring at 20...

Embodiment 2

[0080] Prescription Main drug and excipient name Dosage, mass percentage (g / g)

[0081] FTY720 0.3%

[0082] Glyceryl Monostearate 9%

[0083] White Petrolatum 7.5%

[0084] Liquid paraffin 34.8%

[0085] Paraffin wax 3.3%

[0086] Span 60 3%

[0087] Methylparaben 0.1%

[0088] Tween 80 4%

[0089] Distilled water 38%.

[0090] The preparation method was the same as that in Example 1 except that the main ingredient and auxiliary materials were weighed according to the above proportions, and an FTY720 cream with a FTY720 mass percentage of 0.3% was prepared.

[0091] The storage stability test and the transdermal penetration rate test of the main ingredient were carried out on the above-mentioned cream. The experimental results showed that the above-mentioned cream had a moderate viscosity, a delicate paste with uniform color, stable properties, and the content reached 99% to 102% of the labeled amount. %, and as time goes on, the drug can effectiv...

Embodiment 3

[0093] Prescription Main drug and excipient name Dosage, mass percentage (g / g)

[0094] FTY720 1%

[0095] Glyceryl Monostearate 8.8%

[0096] White Petrolatum 7.5%

[0097] Liquid paraffin 34.3%

[0098] Paraffin wax 3.3%

[0099] Span 60 3%

[0100] Methylparaben 0.1%

[0101] Tween 80 4%

[0102] Distilled water 38%.

[0103] The preparation method was the same as that in Example 1 except that the main ingredients and auxiliary materials were weighed according to the above proportions, and FTY720 cream with 1% by mass of FTY720 was obtained.

[0104] The storage stability test and the transdermal penetration rate test of the main ingredient were carried out on the above-mentioned cream. The experimental results showed that the above-mentioned cream had a moderate viscosity, a delicate paste with uniform color, stable properties, and the content reached 99% to 102% of the labeled amount. %, and a...

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PUM

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Abstract

The invention discloses a 2-amino-2-(2-[4-octyl phenyl]ethyl)-1,3-propanediol hydrochloride preparation, which is prepared from the following raw materials in percent by mass: 0.01 percent-5 percent of 2-amino-2-(2-[4-octyl phenyl]ethyl)-1,3-propanediol hydrochloride, 0.1 percent-0.2 percent of methyl parahydroxybenzoats, 1 percent-55 percent of water-soluble excipients, 10 percent-98 percent of fat-soluble excipients and 0.5 percent-30 percent of emulsifying agent. The preparation is uniform and stable, wherein the compatibility of the pharmaceutic adjuvants with FTY720 is favorable without interference on the FTY720 and particularly on the quality detection of a finished product, which benefits the control of the quality of the finished product. The invention also discloses a preparation method of the 2-amino-2-(2-[4-octyl phenyl]ethyl)-1,3-propanediol hydrochloride preparation, which has the characteristics of simple operation and easy control, and is suitable for industrial production.

Description

technical field [0001] The invention relates to the field of chemical drug preparations, in particular to a 2-amino-2-(2-[4-octylphenyl]ethyl)-1,3-propanediol hydrochloride preparation and a preparation method thereof. Background technique [0002] 2-Amino-2-(2-[4-octylphenyl]ethyl)-1,3-propanediol hydrochloride is a new type of immunomodulator, referred to as FTY720, and its molecular formula is C 19 h 33 NO 2 HCl, molecular weight 343.94, its structural formula is as follows: [0003] [0004] FTY720 is an analogue of sphingosine, its main function is to reduce the number of lymphocytes in peripheral blood and tissues by inducing lymphocyte homing and apoptosis, and reduce the intensity of immune response, but it does not cause lymphocyte death, Lymphocytes can quickly return to normal after drug withdrawal, so normal immune function is not affected. Foreign studies have proved that FTY720 can be used to treat rejection after organ transplantation and autoimmune dis...

Claims

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Application Information

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IPC IPC(8): A61P37/06A61K9/06A61K31/137A61P37/08
Inventor 邱利焱徐健朱心强
Owner ZHEJIANG UNIV
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