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A technology of cefprozil and composition, which is applied in the field of pharmaceutical compositions containing cefprozil and cellulose derivatives, and can solve the problems of drug inactivation and antibacterial activity
Active Publication Date: 2010-07-21
SINOPHARM SHANTOU JINSHI PHARMA CO LTD
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The β-lactam ring is the most unstable part in the structure of the compound. Under acid and alkaline conditions or in the presence of β-lactamase, it is prone to hydrolysis and ring opening and loses antibacterial activity. Metal ions, temperature and oxidants can catalyze The above degradation reactions, resulting in the inactivity of the drug
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Embodiment 1
[0040] Mix 2000g of cefprozil, 240g of microcrystalline cellulose pH302 and 40g of hydroxypropyl cellulose LH11 in a three-dimensional mixer for 50-70 minutes until the cefprozil is fully dispersed and adhered to the cellulose derivatives; In the press, the pressure is adjusted to 0.5-5 MPa, the rotating speed is 200-300 rpm, and pressed into a hard sheet; the sheet can be directly pressed into a tablet.
[0041] According to requirements, the obtained flakes are crushed with a granulator or pulverizer, and passed through a 18-100 mesh sieve to obtain the powder of the cefprozil pharmaceutical composition of the present invention.
Embodiment 2～13
[0043] According to the method of Example 1, the cefprozil pharmaceutical compositions of Examples 2-13 were prepared using the composition shown in Table 1 below.
[0058] Preparation method: Mix cefprozil, microcrystalline cellulose pH302 and hydroxypropyl cellulose LH11 in a three-dimensional mixer for 50 to 70 minutes until cefprozil is fully dispersed and adhered to cellulose derivatives; put the above mixture into dry In the press, the pressure is adjusted to 0.5-8 MPa, the speed is 200-300 rpm, and pressed into a hard sheet.
[0059] The resulting flakes are crushed with a granulator or pulverizer, mixed with pregelatinized starch, croscarmellose sodium, magnesium stearate, talc powder and micropowder silica gel in a three-dimensional mixer for 10 to 20 minutes, After mixing uniformly, eac...
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Abstract
The invention relates to a cefprozil medicinal composition, in particular to a medicinal composition containing cefprozil and cellulose derivatives, which is prepared by a dry granulation method. The cefprozil and the cellulose derivatives are uniformly mixed, and the mixture is pressed into plates under the pressure of 0.1 to 25MPa so as to form tight combination; and then, according to requirements, the plates are prepared into tablets, powder, granules or capsules. The medicinal composition can further contain other conventional auxiliary materials; the obtained plates are ground, mixed with a diluent, a disintegrating agent, a lubricating agent, an adhesive and / or other auxiliary materials; and the mixture is prepared into tablets, powder, granules, suspension or capsules according to requirements. The dry granulation process is adopted; and after the cefprozil and the cellulose derivatives are tightly combined through proper pressure, the beta-lactam ring of the cefprozil is effectively prevented from ring-opening degradation, the stability of the medicinal composition is improved, and the effectiveness and safety of clinical medication are further guaranteed.
Description
technical field [0001] The invention relates to a cefprozil pharmaceutical composition, in particular to a pharmaceutical composition containing cefprozil and cellulose derivatives. Background technique [0002] Cephalosporins are antibiotics with a β-lactam ring in their structure. The β-lactam ring in the mother nucleus is an essential part of antibacterial activity and cannot be cleaved. If the β-lactam ring is broken, its antibacterial effect will disappear. The β-lactam ring is the most unstable part in the structure of the compound. Under acid and alkaline conditions or in the presence of β-lactamase, it is prone to hydrolysis and ring opening and loses antibacterial activity. Metal ions, temperature and oxidants can catalyze The above-mentioned degradation reaction causes the drug to lose its activity. The efficacy and safety of drugs in clinical application are related to degradation products. Therefore, providing active drugs with high stability and high purity ca...
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