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Cefalexin liposome and medicinal composition thereof

A technology of cephalexin and cephalexin, which is applied in the field of pharmaceutical compositions containing the cephalexin liposome, can solve the problems of poor stability, bioavailability, and low encapsulation efficiency, and achieve convenient clinical medication and low toxicity and side effects Small, full pharmacodynamic effect

Inactive Publication Date: 2009-11-18
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The defect of the liposomes produced by the above technology is that the encapsulation efficiency is low, and the dosage form made by combining it with pharmaceutical excipients is also poor in stability and bioavailability, which fails to solve the problems existing in the prior art. technical challenge

Method used

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  • Cefalexin liposome and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] The preparation of embodiment 1 cephalexin liposome

[0042] Recipe: Cefalexin 50g

[0043] Egg Yolk Lecithin 300g

[0044] Cholesterol 100g

[0045] Poloxamer 188 80g

[0046] Preparation Process

[0047] (1) Dissolve 50g cephalexin, 300g egg yolk lecithin, 100g cholesterol and 80g poloxamer 188 in 1500ml isopropanol, mix well, remove isopropanol under reduced pressure on a rotary thin film evaporator, and obtain a phospholipid film ;

[0048] (2) Add 1000ml of pH=6.0 carbonate buffer solution, shake and stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and obtain a liposome suspension;

[0049] (3) freeze-drying the suspension to prepare cephalexin liposomes.

Embodiment 2

[0050] The preparation of embodiment 2 cephalexin liposome

[0051] Prescription: Cefalexin 50g

[0052] Hydrogenated egg yolk lecithin 50g

[0053] Cholesterol 200g

[0054] Poloxamer 188 150g

[0055] Preparation Process

[0056] (1) Dissolve 50g cephalexin, 50g soybean lecithin, 200g cholesterol and 150g poloxamer 188 in 1500ml tert-butanol, mix well, remove tert-butanol under reduced pressure on a rotary thin film evaporator, and obtain a phospholipid film ;

[0057] (2) Add 1000ml of pH=6.0 sodium citrate buffer solution, shake, stir to make the phospholipid film fully hydrated, high-speed homogeneous emulsification, and obtain a liposome suspension;

[0058] (3) The suspension is spray-dried to obtain cephalexin liposomes.

Embodiment 3

[0059] The preparation of embodiment 3 cephalexin granules

[0060] Cefalexin liposome (calculated as cephalexin) 50g

[0061] Lactose 80g

[0062] Mannitol 160g

[0063] Dextrin 50g

[0064] Hypromellose 3g

[0065] Sucrose 120g

[0066] Chocolate essence 6g

[0067] Remarks: the meaning of "cephalexin liposome (calculated as cephalexin) 50g" is that the cephalexin liposome actually used contains 50g of cephalexin active ingredient, and the following examples are all explanations for this meaning.

[0068] Preparation Process

[0069] (1) Take 3g hypromellose and dissolve it in 150ml of 50% ethanol solution to make 2% hypromellose 50% ethanol solution, as a binding agent, for subsequent use;

[0070] (2) pulverize the liposome containing 50g cephalexin, cross 80 mesh sieves, and set aside;

[0071] (3) Weigh 80g lactose, 160g mannitol, 50g dextrin and 120g sucrose, pass through an 80 mesh sieve, mix, and set aside;

[0072] (4) Mix the above raw and auxiliary materia...

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Abstract

The invention discloses a cefalexin liposome and a medicinal composition thereof. The cefalexin liposome is mainly prepared from cefalexin, phospholipid, cholesterol and poloxamer 188 in certain proportion.

Description

technical field [0001] The invention relates to a cephalexin liposome and a preparation method thereof, in particular to a pharmaceutical composition containing the cephalexin liposome, and the pharmaceutical composition can be in various pharmaceutically acceptable dosage forms. Background technique [0002] Cefalexin, its chemical name is: (6R,7R)-3-methyl-7-[(R)-2-amino-2-phenylacetamido-8-oxo-5-thia-1-aza Bicyclo[4.2.0oct-2-ene-2-carboxylic acid-hydrate, is a derivative synthesized by chemically modifying the 7-position amino group and the 3-position acetoxymethyl group of 7-ACA, belonging to the first generation of cephalosporins In addition to Enterococcus and methicillin-resistant Staphylococcus, Streptococcus pneumoniae, Hemolytic Streptococcus, and Penicillinase-producing Staphylococcus Most strains are susceptible to it. Cefalexin has a good antibacterial effect on Neisseria, but Haemophilus influenzae is less sensitive to it; Cephalexin has a certain antibacteri...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/16A61K9/20A61K9/48A61K9/22A61K9/52A61K9/00A61K31/545A61K47/34A61P31/04A61P11/02A61P11/04A61P27/16A61P11/00A61P13/00A61P17/00A61K47/10A61K47/24A61K47/28
Inventor 王明
Owner HAINAN MEIDA PHARMA
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