Medicinal composition containing cefpodoxime proxetil cyclodextrin inclusion compound and preparation thereof
A technology of cyclodextrin inclusion complex and cefpodoxime axetil, which can be applied to medical preparations containing active ingredients, pharmaceutical formulations, non-active ingredients of polymer compounds, etc. Acid and alkali resistance, low water solubility and other problems, to achieve the effect of easy dissolution, less side effects of hemolysis, and high water solubility
Inactive Publication Date: 2008-09-17
NANJING NORMAL UNIVERSITY +1
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AI Technical Summary
Problems solved by technology
[0003] At present, the research on cefpodoxime axetil mainly focuses on the technology and products of oral preparations. After taking cefpodoxime axetil orally, children absorb it very quickly. Cefpodoxime axetil with a potency of 6mg / kg orally once on an empty stomach can reach C after 2 hours. max , about 3.7~5.5mg / L, but the water solubility of cefpodoxime axetil is low, oral bioavailability 50% (the clinical application of the third generation oral cephalosporins, Chinese Journal of New Drugs and Clinics, 2004, 23 (11) :744-746)
Cefpodoxime axetil has the characteristics of low stability of ester cephalosporins, and the product has poor light, heat and humidity stability, especially not acid and alkali resistance
Method used
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Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0072] Mix 10g of β-cyclodextrin with 20ml of pure water, heat, add 5g of cefpodoxime axetil (molar ratio about 1:1) at 50°C, mix and stir for 3 hours, add dilute NaHCO drop by drop 3 The solution was then cooled at 5°C for 24 hours; filtered, washed twice with water, and dried under reduced pressure at room temperature to obtain a solid clathrate.
Embodiment 2
[0074] Essentially the same as Example 1, but substituting 15 g of hydroxypropyl-β-cyclodextrin for the β-cyclodextrin.
Embodiment 3
[0076] It is basically the same as Example 1, but with 20g of sulfobutyl-β-cyclodextrin for clathrate; 100 ml of pure water and 20g of sulfobutyl-β-cyclodextrin are mixed and heated.
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The invention provides a medicine composition comprising the cefpodoxime proxetil cyclodextrin inclusion compound. The basic composition comprises the cefpodoxime proxetil and the pharmacy-acceptable cyclodextrin; the cyclodextrin is chosen from one or a plurality of Beta -cyclodextrin, sulfobutyl- Beta -cyclodextrin, hydroxypropyl- Beta -cyclodextrin or hydroxypropyl-sulfobutyl- Beta -cyclodextrin. The invention has the advantages of increasing the solubility and stability of the medicine, meanwhile lower hemolysis irritability and higher activity. The invention also provides the preparation method of the medicine composition.
Description
technical field [0001] The invention relates to a pharmaceutical composition containing ester prodrug cephalosporin antibiotic cyclodextrin and a preparation method thereof. Background technique [0002] Cefpodoxime proxetil (cefpodoxime proxetil, trade name: Shibo), chemical name: (6R, 7R)-7-[2-(2-amino-4-thiazolyl)-(Z)-2-(methoxysubstance Amino)-acetylamino]-3-methoxymethyl-8-oxo-5-thia-1-azabicyclo-[4.2.0]oct-2-ene-2-carboxylic acid isopropoxycarbonyloxyethyl Esters, molecular formula: C 21 h 27 N 5 o 9 S 2 , Molecular weight: 557.60, this product is white or almost white powder, odorless or slightly specific odor, slightly bitter taste. Cefpodoxime axetil is a new type of oral cephalosporin antibacterial drug of the third generation. Its structural feature is that the 7th position of the cephalosporin nucleus structure is connected with a methoxylated imidazole side chain. Antibacterial activity, clinically can achieve better curative effect on staphylococcal infe...
Claims
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Patent Timeline
Login to View More IPC IPC(8): A61K31/546A61K47/40A61P31/04
Inventor 任勇高剑峰韩彬彬马学琴
Owner NANJING NORMAL UNIVERSITY
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