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Aprepitant medicine composition and method for improving bioavailability of Aprepitant medicine composition

A technology for aprepitant and composition, which is applied in the field of aprepitant pharmaceutical composition and its preparation, can solve the problems of reduced solubility and dissolution rate, easy recrystallization, large amount of auxiliary materials, etc., and achieves improved solubility and reduced Extrusion temperature, effect of maintaining stability

Active Publication Date: 2018-07-27
NANJING HERON PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The inventors of the present invention also used the HME technology to prepare the above-mentioned aprepitant pharmaceutical composition. The amount of aprepitant adjuvant is relatively large, and the storage is difficult. The metastable solid dispersion has physical instability and is easy to Re-crystallization, leading to problems such as a decrease in solubility and dissolution rate, conducted a lot of research and explored a variety of ways

Method used

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  • Aprepitant medicine composition and method for improving bioavailability of Aprepitant medicine composition
  • Aprepitant medicine composition and method for improving bioavailability of Aprepitant medicine composition
  • Aprepitant medicine composition and method for improving bioavailability of Aprepitant medicine composition

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Effect test

Embodiment 1

[0036] The selection of embodiment 1 carrier

[0037] The present invention screens the commonly used carrier types, and finally selects the enteric carrier material as the main carrier of aprepitant drug, selected from cellulose acetate phthalate, cellulose acetate trimellitate, cellulose acetate succinate, ortho Methylcellulose phthalate, Ethylhydroxymethylcellulose phthalate, Hydroxypropylmethylcellulose phthalate, Hydroxypropylmethylcellulose acetate succinate, Hydroxypropyl acetate maleate methyl cellulose, hydroxypropyl methyl cellulose trimellitate, carboxymethyl ethyl cellulose, polyvinyl butyrate phthalate, polyvinyl acetate phthalate, methyl One or more of acrylic acid / ethyl acrylate copolymer and methacrylic acid / methyl methacrylate copolymer. And for further screening, the enteric carrier material is preferably selected from hydroxypropylmethylcellulose acetate succinate (HPMCAS).

[0038] HPMCAS is a mixed ester of acetic acid and succinic acid of HPMC. It is a ...

Embodiment 2

[0043] The selection of embodiment 2 nonionic surfactants

[0044] Span is a kind of non-ionic surfactant, which is formed by esterification of sorbitol and various long-chain fatty acids (lauric acid, palmitic acid, stearic acid, oleic acid, etc.), and is divided into mono-, di-, and tri-esters. The trade name is Span. The types include Span20, Span40, Span60, Span65, Span80, Span85, and the molecular structure of Span contains hydrophilic sorbitol and hydrophobic fatty acids, and the HLB value is usually in the range of 2-9. It is insoluble in water and not easy to disperse in water, but soluble in ethanol, ether and other organic solvents. It belongs to oil-soluble non-ionic non-ionic surfactant and is a water-in-oil (W / O) emulsifier.

[0045] The Span variety can be used as a solubilizer in the pharmaceutical industry. The present invention screens nonionic surfactants one by one, and finally selects Span as the solubilizer for the auxiliary enteric carrier. The data in t...

Embodiment 3

[0046] Embodiment 3 preparation of aprepitant pharmaceutical composition

[0047] 1. Prescription: The specific composition and dosage of the aprepitant pharmaceutical composition are shown in Table 2:

[0048] The prescription and dosage of table 2 aprepitant pharmaceutical composition, the unit dose of aprepitant is calculated by 80mg

[0049]

[0050] 2. Preparation method:

[0051] (1) Aprepitant, enteric carrier material, and nonionic surfactant are pulverized respectively according to the consumption in Table 1, cross a 40-60 mesh sieve, add in a mixer and mix uniformly; or directly mix the above materials according to Table 1 The amount is put into the twin-screw extruder;

[0052] (2) According to the melting point or glass transition temperature of the drug and excipients, set the extrusion temperature of different sections of the hot-melt extruder to 120-150°C, specifically Zone2 120°C, Zone3 120°C, Zone4 120°C, and Zone5 150°C , Zone6 150°C, Zone7 150°C...

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Abstract

The invention discloses an Aprepitant medicine composition, which comprises Aprepitant, at least one kind of intestine soluble carrier material and at least one kind of nonionic surfactant. The carrier is preferably hydroxypropyl methylcellulose succinate acetate, is favorably for dispersing the Aprepitant medicine to the inside in the molten state; in addition, after the addition of the nonionicsurfactant span, the consumption of the carrier is further reduced; the extrusion temperature is lowered. The invention provides a method for preparing the medicine composition using the Aprepitant asactive ingredients; the problems that in the preparation process of a conventional Aprepitant medicine composition by using an HME technology, the auxiliary material consumption of the Aprepitant isgreat; the storage is difficult, the metastable solid dispersion body has instable physical performance; recrystallization can easily occur; the solubility and dissolving-out speed reduction can be caused, and the like are solved.

Description

technical field [0001] The invention relates to an aprepitant pharmaceutical composition and a preparation method thereof, in particular to a pharmaceutical composition with aprepitant as an active component, and a method for increasing its solubility and dissolution rate to improve its bioavailability. Background technique [0002] Nausea and vomiting are one of the most common chemotherapy-related adverse reactions that cause great distress to cancer patients. Aprepitant was approved for marketing in the US and the EU in 2003. It is the first NK-1 receptor antagonist for antiemesis, and it is used in combination with other antiemetic drugs to prevent high-grade or toxic vomiting tumors Acute or delayed nausea and vomiting during the initial or repeated course of chemotherapy. Aprepitant is almost insoluble in water, and the Log P (P is the oil-water partition coefficient) at pH 7.0 is 4.8, so it belongs to the fourth category according to the BCS classification-low solubi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K47/38A61K47/26A61P1/08
CPCA61K31/5377A61K47/26A61K47/38
Inventor 包玉胜陶莉马冲郑慧娟闵涛陆晨光王芳
Owner NANJING HERON PHARMA SCI & TECH CO LTD
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