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Cefetamet pivoxil hydrochloride submicron emulsion solid preparation and new application thereof

A technology of ceftazidime hydrochloride and metil submicroemulsion, which is applied in the field of medicine, can solve the problems of low dissolution rate, sticky granulation of raw materials, poor stability, etc., and achieve increased solubility, improved stability, and low cost Effect

Inactive Publication Date: 2010-06-09
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The object of the present invention is to provide a kind of ceftamet pivoxil hydrochloride submicroemulsion solid preparation and its new application, specifically, through the solid preparation of ceftamet pivoxil hydrochloride treated by microemulsification and its new application, well solved The currently marketed ceftamet pivoxil hydrochloride solid preparation has poor stability, low dissolution rate, and sticky granulation of raw materials, and it can also be used to prepare drugs for the treatment of suppurative cholangitis, and has obtained satisfactory technical results

Method used

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  • Cefetamet pivoxil hydrochloride submicron emulsion solid preparation and new application thereof
  • Cefetamet pivoxil hydrochloride submicron emulsion solid preparation and new application thereof
  • Cefetamet pivoxil hydrochloride submicron emulsion solid preparation and new application thereof

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Embodiment 1

[0046] The preparation of embodiment 1 ceftamet pivoxil hydrochloride submicron emulsion particles

[0047]Add 1650g of cholesterol, 1025g of poloxamer 188 and 575g of sodium deoxycholate into 20L of water for injection, then add 250g of ceftazidime hydrochloride and mix evenly, heat and stir in a water bath at 80°C until it melts, and cut it with a tissue masher Stir for 15 minutes at a rotating speed of 13000r / min to obtain the first emulsion, then circulate and emulsify it through a high-pressure homogenizer for 5 times to obtain an emulsion, and then spray dry to obtain 3248g of submicron emulsion particles of ceftazidime hydrochloride, with a yield of 92.8%.

Embodiment 2

[0050] The preparation of embodiment 2 ceftamet pivoxil hydrochloride submicron emulsion particles

[0051] Add 500g of cholesterol, 325g of poloxamer 188 and 125g of sodium deoxycholate into 6000ml of water for injection, then add 125g of ceftazidime hydrochloride and mix well, heat and stir in a water bath at 90°C until it melts, and cut it with a tissue masher Stir for 20min, rotating speed 12000r / min, get first emulsion, then circulate emulsification through high-pressure homogenizer 5 times, get emulsified liquid, then freeze-dry in large plate, pulverize, obtain the submicroemulsion particle 988g of ceftamet pivoxil hydrochloride, yield 91.9 %.

Embodiment 3

[0054] The preparation of embodiment 3 ceftamet pivoxil hydrochloride submicron emulsion particles

[0055] Add 1250g of cholesterol, 750g of poloxamer 188 and 437.5g of sodium deoxycholate into 15,000ml of water for injection, then add 125g of ceftazidime hydrochloride and mix evenly, heat and stir in a water bath at 70°C until it melts, and cut it with a tissue masher. Cut and stir for 20min, rotating speed 15000r / min, to obtain the primary emulsion, and then circulate emulsification through a high-pressure homogenizer for 5 times to obtain an emulsion, then spray dry to obtain 2390g of submicron emulsion particles of ceftamet pivoxil hydrochloride, with a yield of 93.3%.

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Abstract

The invention provides a cefetamet pivoxil hydrochloride submicron emulsion solid preparation, which comprises the following components in part by weight: 1 part of cefetamet pivoxil hydrochloride submicron emulsion grains, 0.4 to 3 parts of diluent, 0 to 0.5 part of disintegrating agent, 0 to 0.2 part of adhesive, 0 to 6 parts of flavoring agent, 0 to 0.4 part of aromatizer and 0 to 0.2 part of lubricant. The invention also discloses application of the preparation in preparation of a medicament for treating cholangitis, particularly acute pyogenic cholangitis.

Description

technical field [0001] The invention relates to a submicroemulsion solid preparation of ceftamet pivoxil hydrochloride and its new application, in particular to a solid preparation of ceftamet pivoxil hydrochloride after microemulsification treatment and its new application, belonging to the technical field of medicine. Background technique [0002] Acute suppurative cholangitis is caused by bile stasis due to biliary stricture or occlusion, coupled with bacterial infection and acute suppurative symptoms. Patients may present with chills and high fever, jaundice and right upper quadrant pain, accompanied by nausea and vomiting. As the disease progresses, the toxins produced by bacteria continue to enter the blood circulation through the hepatic sinusoids and sepsis and toxic shock occur. Oxygen produces a large number of oxygen free radicals, promotes the production of various inflammatory mediators, induces pancreatitis, and leads to multiple organ failure such as liver, ki...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K9/48A61K31/546A61K47/34A61P1/16A61P31/04A61K47/10A61K47/28
Inventor 王明
Owner HAINAN MEIDA PHARMA
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