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A kind of nano micelles of aprepitant

A prepitant nano, aprepitant technology, applied in the field of aprepitant nano-micelle preparations, can solve the problems affecting the long-term stability of micelles, low bioavailability, poor water solubility, etc., to achieve drug safety The effect of easy quality control, good safety and simplified preparation process

Active Publication Date: 2021-10-01
FUBICHENG SHANGHAI PHARMA TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

CN105997869A discloses a vitamin K1 micellar injection, including the following components: vitamin K1, cholate, phospholipid, pH regulator and water for injection, CN109549924A discloses SKLB023 mixed micelles and its preparation method and use, including the following Prepared from the raw and auxiliary materials with the above weight ratio: 1-30 parts of SKLB023, 30-80 parts of phospholipids, 20-70 parts of bile salt, which overcomes the shortcomings of SKLB023, such as poor water solubility, short half-life and low bioavailability
At the same time, the surfactant itself has many defects, especially in the preparation of injections, there are potential side effects such as toxicity, hemolysis, and acid-base problems that affect the long-term stability of micelles

Method used

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  • A kind of nano micelles of aprepitant
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  • A kind of nano micelles of aprepitant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Aprepitant nanomicelle, made of the following ingredients:

[0053] Aprepitant 1 g

[0054] Phosphatidylcholine 20 g

[0055] Phosphatidylglycerol 0.5g

[0056] Ethanol 11.5g (considering the volatilization of ethanol during the preparation process)

[0057] Sucrose 7.69g

[0058] Sodium Oleate 0.775g

[0059] Water for injection 105mL

[0060] Preparation:

[0061] heating and mixing aprepitant, phosphatidylcholine, phosphatidylglycerol and ethanol with stirring for 10 minutes to dissolve them in excess ethanol to prepare an ethanol solution;

[0062] Stirring and mixing sucrose, sodium oleate and water for injection at room temperature for 30 minutes to prepare an aqueous phase;

[0063] The aqueous phase and the ethanol solution are sheared at a high speed above 10,000rpm, and then homogenized by a high-pressure homogenizer at 2,000bar to form nanomicelles. After filtering through a 0.22um syringe filter, the finished nanomicelles are obtained.

[0064] The f...

Embodiment 2

[0066] Aprepitant nano-micelle, its composition:

[0067] Aprepitant 1 g

[0068] Phosphatidylcholine 20 g

[0069] Phosphatidylglycerol 0.5g

[0070] Ethanol 8g (considering the volatilization of ethanol during the preparation process)

[0071] Sucrose 7.69g

[0072] Water for injection 105mL.

[0073] Preparation:

[0074] heating and mixing aprepitant, phosphatidylcholine, phosphatidylglycerol and ethanol for 15 minutes, dissolving them in excess ethanol to prepare an ethanol solution;

[0075] Stirring and mixing sucrose and water for injection at room temperature for 25 minutes to prepare an aqueous phase;

[0076] The aqueous phase and ethanol solution are sheared at a high speed above 10,000rpm, and then homogenized by a high-pressure homogenizer at 1,500bar to form nanomicelles. After filtering through a 0.22um syringe filter, the finished nanomicelles are obtained.

[0077] The formulation is a clear, transparent, yellow to brown solution. The measured pH was ...

Embodiment 3

[0079] Aprepitant nano-micelle, its composition:

[0080] Aprepitant 1 g

[0081] Phosphatidylcholine 20g

[0082] Phosphatidylglycerol 1g

[0083] Ethanol 12g (considering the volatilization of ethanol during the preparation process)

[0084] Sucrose 7.69g

[0085] Water for injection 105mL.

[0086] Preparation:

[0087] heating and mixing aprepitant, phosphatidylcholine, phosphatidylglycerol and ethanol for 15 minutes, dissolving them in excess ethanol to prepare an ethanol solution;

[0088] Stirring and mixing sucrose and water for injection at room temperature for 25 minutes to prepare an aqueous phase;

[0089] The aqueous phase and ethanol solution are sheared at a high speed above 10,000rpm, and then homogenized by a high-pressure homogenizer at 1,500bar to form nanomicelles. After filtering through a 0.22um syringe filter, the finished nanomicelles are obtained.

[0090] The formulation is a clear, transparent, yellow to brown solution. The measured pH was 8....

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Abstract

The invention provides an aprepitant nano-micelle preparation, which comprises aprepitant, phospholipid, sucrose, ethanol and water for injection, wherein the phospholipid contains phosphatidylcholine and phosphatidylglycerol. The injection of the invention has better physical and chemical stability, makes the drug quality easier to control, the process is more simplified, the clinical drug is safer, the cost is lower, and the accessibility of the drug is improved.

Description

technical field [0001] The invention relates to an aprepitant preparation, in particular to a novel nano-micelle preparation of aprepitant. Background technique [0002] Chemotherapy-induced nausea and vomiting (CINV) is the most common adverse reaction in cancer patients during chemotherapy. Aprepitant is mature in clinical application as an antiemetic agent. Unlike other emetogenic pathways, aprepitant can maintain central nervous system for a long time Active, inhibits acute and delayed emesis associated with emetogenic chemotherapy, increases activity of standard antiemetic therapy against chemotherapy-induced emesis. [0003] However, aprepitant has low solubility and poor absorption, the solubility in water is only 0.55 μg / m1, little absorption in the gastrointestinal tract, and low oral bioavailability are the main factors restricting the efficacy of aprepitant. At present, aprepitant is mainly oral capsule preparation, but due to the low bioavailability of oral caps...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/5377A61K47/10A61K47/24A61K47/26A61P1/08
CPCA61K9/1075A61K31/5377A61K47/10A61K47/24A61K47/26A61P1/08
Inventor 潘弘印志刘子煊常海民游欢欢甘莉
Owner FUBICHENG SHANGHAI PHARMA TECH CO LTD