Cefprozil suspension pharmaceutical composition

Abstract

The invention relates to a cefprozil suspension pharmaceutical composition, in particular to a suspension pharmaceutical composition containing cefprozil and xanthan gum. The cefprozil and the xanthan gum are uniformly mixed according to a certain proportion, pharmaceutic adjuvants, such as appropriate amount of disintegrating agent, diluent, flavoring agent, deodorant or lubricant and the like, are added in the mixture, then, the mixture is prepared into standard suspension in a manner of dry granulation or directly filling dry powder. The xanthan gum used as a suspending aid is less in dosage and excellent in adding suspension, the stability of the basic remedy is excellent, and simultaneously, the composition is free from solubilizer and preservative, so that the problem that the existing cefprozil suspension is long in dispersion time in water and low in safety, and has various accessories; and the compliance for taking the composition by a patient is further improved while the effectiveness and the safety of clinical application are ensured.

Description

technical field [0001] The invention relates to a suspension pharmaceutical composition of cefprozil, in particular to a suspension pharmaceutical composition of cefprozil and xanthan gum. Background technique [0002] Cefprozil (cefprozil, BMY28100, CFPZ) is a non-ester oral cephalosporin originally developed by Bristol-Myers in 1983. Its molecular structure is related to cephalexin, cefadroxil and cefaclor. There is a p-hydroxyphenylglycine substituent at the 7-position of the cephalosporin nucleus, and a propenyl side chain at the 3-position. The structural formula of its monohydrate is as follows: [0003] [0004] Formula 1: Cefprozil monohydrate structural formula, C 18 h 19 N 3 o 5 S·H 2 o [0005] The antibacterial spectrum of cefprozil includes the main Gram-positive and negative bacteria of common respiratory tract infections and urinary tract infections. The streptococcal activity is superior to cefaclor, and the activity against Haemophilus influenzae a...

AI Technical Summary

Problems solved by technology

However, research has found that although the use of sodium carboxymethylcellulose as a suspending agent can better suspend the main drug, the dosage is relatively large (the dosage ratio of the main drug to the suspending agent is at least 1: 1). Rapid gelation makes the granules easy to stick into agglomerates, which requires long-term shaking or stirring, and poor dispersion, which brings inconvenience to patients.

Although adding a disintegrant can improve the dispersion effect, the disintegrant is insoluble in water and easily settles. In order to ensure that the sedimentation volume ratio of the oral suspension meets the requirements, it is necessary to increase the amount of the suspending agent, and the viscosity of the solution increases. When the smell of medicine stays in the mouth, it is not easy to remove

Therefore, the amount of the two restricts each other, and it is difficult to obtain a product with good suspending effect and good dispersibility

[0011] The inventor found that the single-dose dry suspension was in the form of granules with a small amount of powder when conducting comparative research on the products on the market. It took a long time to disperse when it met water, and it was easy to stick into agglomerates. It took a long time to stir to dissolve it. Dispersed into a suspension state, which brings inconvenience to patients; the multi-dose dry suspension is in the form of powder, and the dispersibility is slightly better, but deposits appear within 3 hours, although the deposits have good redispersibility, but Long-term storage will increase the sediment, and the redispersibility will become poor. It needs to be shaken several times during the storage period to maintain the suspension state of the solution

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