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Cefetamet pivoxil hydrochloride liposome solid preparation

A technology of ceftamet pivoxil hydrochloride and solid preparations, which is applied in the field of ceftamet pivoxil hydrochloride liposome solid preparations and its preparation method, can solve the problems of low bioavailability, unsatisfactory long-term stability, and Encapsulation efficiency is not high, to achieve the effect of improving dissolution and bioavailability, significant curative effect, and improving product quality

Inactive Publication Date: 2012-04-04
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] CN1319533C discloses a dispersible tablet of ceftamet pivoxil hydrochloride and its preparation method. The preparation method adopts a boiling granulation process, and at the same time, auxiliary materials are mixed and pressed into tablets; CN101732260A discloses a granule of ceftamet pivoxil hydrochloride and its preparation method , made of ceftazidime pivoxil hydrochloride fine particles and pharmaceutically acceptable auxiliary materials; CN101612138B discloses a ceftazidime pivoxil hydrochloride capsule and a preparation method thereof, the content of which is composed of 59% effective active ingredients, 10-15% Disintegrating agent, 1-3% solubilizer, 20-28% filler, 2-3% lubricant composition; Yet the bioavailability of the ceftamet pivoxil hydrochloride preparation prepared by above-mentioned traditional method is low, and long-term stability is unsatisfactory
CN101721371A discloses a solid preparation of ceftamet pivoxil hydrochloride submicroemulsion, comprising 1 part of ceftamet pivoxil hydrochloride submicroemulsion particles, 0.4-3 parts of diluent, 0-0.5 parts of disintegrant, 0-0.2 parts of binder part, 0-6 part of flavoring agent, 0-0.4 part of flavoring agent and 0-0.2 part of lubricant, and the submicron emulsion particles of ceftamet pivoxil hydrochloride include 1 part of ceftamet pivoxil hydrochloride, 2.25-15 parts of cholesterol, 1.2-13 parts of poloxamer 188, 0.5-6 parts of sodium deoxycholate, but the ceftametoxo pivoxil hydrochloride submicroemulsion preparation has problems such as low encapsulation efficiency and poor stability

Method used

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  • Cefetamet pivoxil hydrochloride liposome solid preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1 Ceftamet pivoxil hydrochloride liposome tablet

[0044] Prescription (1000 tablets)

[0045]

[0046] Preparation Process:

[0047] (1) Accurately weigh 150g of dicetyl phosphate, 150g of cholesterol, and 100g of Tween 80, place in a pear-shaped bottle, add 1000ml of isopropanol, mix well, place in a rotary evaporator and evaporate to dryness for 20 minutes to form a film;

[0048] (2) Adding 125g ceftazidime hydrochloride and 1000ml pH in the pear-shaped bottle is a phosphate buffered saline solution of 6.2, spins and dissolves for 30 minutes, ultrasonically makes the solution transparent for 15 minutes, and filters through a 0.45 μm microporous membrane;

[0049] (3) The above-mentioned filtrate is placed in -20 ℃ and frozen for 5 hours, taken out, placed at room temperature to melt, then ultrasonicated for 5 minutes, and spray-dried to obtain ceftazidime hydrochloride liposome powder;

[0050] (4) Mix ceftazidime hydrochloride liposome powder with 1...

Embodiment 2

[0053] Embodiment 2 Cefetamet pivoxil hydrochloride liposome sheet

[0054] Prescription (1000 tablets)

[0055]

[0056] Preparation Process:

[0057] (1) Weigh 100g dicetyl phosphate, 200g cholesterol, 150g Tween 80, place in a pear-shaped bottle, add 1000ml isopropanol, mix well, place in a rotary evaporator and evaporate to dryness for 60 minutes to form a film;

[0058] (2) Adding 250g ceftazidime hydrochloride and 1000ml pH in the pear-shaped bottle is a phosphate buffered saline solution of 6.2, spins and dissolves for 30 minutes, ultrasonically makes the solution transparent for 30 minutes, and filters with a 0.45 μm microporous membrane;

[0059] (3) The above-mentioned filtrate is placed in -20 ℃ and frozen for 12 hours, taken out, melted, and then ultrasonicated for 10 minutes, and spray-dried to obtain ceftazidime hydrochloride liposome powder;

[0060] (4) Ceftamet pivoxil hydrochloride liposome powder is mixed with 200g dextrin, 15g crospovidone, crosses 80 ...

Embodiment 3

[0063] Embodiment 3 Cefetamet pivoxil hydrochloride liposome particle

[0064] Prescription (1000 bags)

[0065]

[0066]

[0067] Preparation Process:

[0068] (1) Weigh 180g dicetyl phosphate, 160g cholesterol, 50g Tween 80, place in a pear-shaped bottle, add 1000ml chloroform, place in a rotary evaporator and evaporate to dryness for 120 minutes to form a film;

[0069] (2) Add 250g ceftazidime hydrochloride and 1000ml pH to the citrate buffer of 6.2 in the pear-shaped bottle, rotate and dissolve for 30 minutes, ultrasonically make the solution transparent for 30 minutes, and filter through a 0.45 μm microporous membrane;

[0070] (3) The above-mentioned filtrate is placed in -20 DEG C and frozen for 5 hours, taken out, melted, and then ultrasonicated for 10 minutes, and spray-dried to obtain ceftazidime hydrochloride liposome powder;

[0071] (4) Mix ceftazidime pivoxil hydrochloride liposome powder with 240g lactose, 20g crospovidone and 1g steviol glycoside, cros...

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Abstract

The invention provides a cefetamet pivoxil hydrochloride liposome solid preparation and a preparation method thereof. The cefetamet pivoxil hydrochloride liposome solid preparation comprises 125 parts of cefetamet pivoxil hydrochloride, 20 to 250 parts of aluminum dicetyl phosphate, 50 to 200 parts of cholesterol, 10 to 150 parts of tween 80 and 100 to 250 parts of other medicinal auxiliary materials. The cefetamet pivoxil hydrochloride liposome solid preparation can be processed into tablets and particles. The cefetamet pivoxil hydrochloride liposome solid preparation has a high entrapment rate, even particle sizes and long retention time of drugs in blood circulation. The preparation method of the cefetamet pivoxil hydrochloride liposome solid preparation improves preparation quality, reduces toxic and side effects, needs simple equipment, is easy for operation and is suitable for industrialized large-scale production.

Description

technical field [0001] The invention relates to a ceftamet pivoxil hydrochloride liposome solid preparation and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Cefetamet Pivoxil Hydrochloride (Cefetamet Pivoxil Hydrochloride), chemical name (6R, 7R)-3-methyl-7-[(Z)-2-(2-amino-4-thiazolyl)-2-(methoxy Amino)-acetylamino]-8-oxo-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid pivaloyloxymethyl ester hydrochloride, molecular formula C 20 h 25 N 5 o 7 S 2 ·HCl, molecular weight 548.04, structural formula: [0003] [0004] Ceftamet pivoxil is an orally absorbed ester prodrug of bioactive ceftazime, which is the C 2 - Esters of carboxylic acids combined with trimethylacetoxymethyl. The ester is a broad-spectrum antibiotic, which has antibacterial and bactericidal effects on Gram-negative and positive bacteria, especially against Streptococcus pneumoniae, Haemophilus influenzae, and Klebsiella. And pallid spi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/546A61K47/34A61P31/04
Inventor 廖爱国
Owner HAINAN MEIDA PHARMA
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