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Azasetron hydrochloride lipidosome injection

A technology of injection and agar, which is applied in the field of medicine, can solve the problems of low bioavailability, low stability, and easy decomposition without overcoming, and achieve the effects of simple preparation method, increased retention time, and improved bioavailability

Inactive Publication Date: 2012-09-26
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The azasetron hydrochloride injection or tablet prepared by the traditional method in the prior art simply mixes azasetron hydrochloride and excipients, and the stability is not high in the long-term storage process, and the easy decomposition is not overcome. defects, and low bioavailability

Method used

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  • Azasetron hydrochloride lipidosome injection
  • Azasetron hydrochloride lipidosome injection
  • Azasetron hydrochloride lipidosome injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Azasetron Hydrochloride Liposomal Injection

[0033] Prescription (1000 bottles):

[0034]

[0035] Preparation Process:

[0036] (1) Take 10g azasetron hydrochloride, 100g cephalin, 50g cholesterol, 20g Span 80 and 5g sodium thiosulfate by weight components and place them in a pear-shaped bottle, add in 500ml acetone, heat and stir to disperse evenly, Acetone was removed under reduced pressure on a rotary evaporator to obtain a phospholipid film;

[0037] (2) Take by weighing 80g mannitol and 80g dextran and add 500ml water to dissolve, then pour into a pear-shaped bottle and shake gently, so that the phospholipid film is eluted and dispersed in a hydration medium for dissolution to obtain a liposome suspension;

[0038] (3) Pour the above-mentioned suspension into the homogenizer, and continue to homogenize;

[0039] (4) Remove the bacteria and heat source through the ultrafiltration membrane of the above-mentioned homogenized suspension, then circulat...

Embodiment 2

[0040] Example 2 Azasetron Hydrochloride Liposomal Injection

[0041] Prescription (1000 bottles):

[0042]

[0043]

[0044] Preparation Process:

[0045] (1) Take 10g azasetron hydrochloride, 150g cephalin, 100g cholesterol, 10g Span 80 and 2g sodium thiosulfate by weight components and place them in a pear-shaped bottle, add in 800ml acetone, heat and stir to disperse evenly, Acetone was removed under reduced pressure on a rotary evaporator to obtain a phospholipid film;

[0046] (2) Take 100g mannitol and 100g dextran by weight and add 500ml water to dissolve, then pour into a pear-shaped bottle and shake gently, so that the phospholipid film is eluted and dispersed in a hydration medium for dissolution to obtain a liposome suspension;

[0047] (3) Pour the above-mentioned suspension into the homogenizer, and continue to homogenize;

[0048] (4) Remove the bacteria and heat source through the ultrafiltration membrane of the above-mentioned homogenized suspension, ...

Embodiment 3

[0049] Example 3 Azasetron Hydrochloride Liposomal Injection

[0050] Prescription (1000 bottles):

[0051]

[0052] Preparation Process:

[0053] (1) Weigh 10g of azasetron hydrochloride, 50g of cephalin, 80g of cholesterol, 50g of Span 80 and 8g of sodium thiosulfate in a pear-shaped bottle by weight, add 500ml of acetone, heat and stir to disperse evenly , Remove acetone under reduced pressure on a rotary evaporator to prepare a phospholipid film;

[0054] (2) Take by weight 90g of mannitol and 90g of dextran and add 500ml of water to dissolve it and pour it into a pear-shaped bottle and shake gently, so that the phospholipid film is eluted and dispersed in a hydration medium for dissolution to obtain a liposome suspension;

[0055] (3) Pour the above-mentioned suspension into the homogenizer, and continue to homogenize;

[0056] (4) Remove the bacteria and heat source through the ultrafiltration membrane of the above-mentioned homogenized suspension, then circulate s...

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Abstract

The invention provides an azasetron hydrochloride lipidosome injection, which is mainly prepared from azasetron hydrochloride, cephalin, cholesterol, span 80, antioxidant and cryoprotectant. The lipidosome injection has favorable stability of the preparation; in the freeze-drying process, the lipidosome cannot be broken due to dehydration, fuse, ice crystal and the like; after hydrated dissolution, the lipidosome can also keep favorable entrapment rate; and meanwhile, according to a product prepared by adopting the method, the side effect is small, the quality of the preparation product is improved, the toxic or side effect is reduced and the bioavailability of a medicament is improved.

Description

technical field [0001] The invention relates to a new preparation of azasetron hydrochloride, in particular to an azasetron hydrochloride liposome injection and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Azasetron hydrochloride (azasetron), chemical name (±) N-(1-azabicyclo[2,2,2]oct-3-yl)-6-4-methyl-3-oxo-3, 4-Dihydro-2H-1,4-benzoxazine-8-carboxamide hydrochloride, formula C 17 h 20 ClN 3 o 3 ·HCl, molecular weight 386.28, structural formula: [0003] [0004] Azasetron hydrochloride is a 5-hydroxytryptamine receptor antagonist antiemetic drug researched and developed by Japan Jifu Pharmaceutical Co., Ltd., which was launched in Japan in December 1995. Azasetron has a strong selective antagonistic effect on 5HT3 receptors, and can competitively antagonize the depolarization of the nerve membrane caused by 5HT3 in isolated tissue specimens of rat vagus nerve and superior cervical ganglion, Azasetron Joan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/538A61K47/34A61P1/08
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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