Cefprozil suspension pharmaceutical composition

A technology of cefprozil and composition, which is applied in the field of suspension pharmaceutical composition of cefprozil and xanthan gum, can solve the problems of poor redispersibility, long dispersion time, inconvenience for patients to take medicine, etc., and achieve good redispersibility, High product safety and good suspension effect

Inactive Publication Date: 2011-08-10
SHANDONG INST OF PHARMA IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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,

Method used

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  • Cefprozil suspension pharmaceutical composition
  • Cefprozil suspension pharmaceutical composition
  • Cefprozil suspension pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1 adopts the xanthan gum of different viscosity to prepare the cefprozil dry suspension of different specifications

[0060] According to the method under the viscosity item of xanthan gum, the second part of the Chinese Pharmacopoeia 2010 edition, the viscosities of xanthan gum a, b, and c are about 1385mPa·s, 1840mPa·s and 2230mPa·s.

[0061] 1. The single-dose prescription contains 125mg, 250mg, and 500mg of cefprozil (based on anhydrous substance, crushed)

[0062] prescription:

[0063]

[0064] Process:

[0065] Weigh an appropriate amount of cefprozil and pulverize it to below 75 μm (equivalent to passing through a 200-mesh sieve), weigh 20 times the amount of raw and auxiliary materials according to each prescription and mix them evenly, and then divide them into two parts, one in powder state for later use, and the other The granules are made into granules by a dry granulator, and the granules below 80 mesh are collected for future use.

[0066...

Embodiment 2

[0093] Embodiment 2 adopts magnesium aluminum silicate of different viscosities and xanthan gum compatibility to prepare different specifications of cefprozil dry suspension

[0094] Xanthan gum with a viscosity of 1840mPa·s is used, and it is compatible with magnesium aluminum silicate a, b, and c with viscosities of 245mPa·s, 1202mPa·s, and 2317mPa·s respectively.

[0095] 1. The single-dose prescription contains 125mg, 250mg, 500mg of cefprozil (according to anhydrous substance, not pulverized)

[0096] prescription:

[0097]

[0098] Process:

[0099] Weigh 20 times the prescription amount of xanthan gum and magnesium aluminum silicate, first mix the two, and then mix with the remaining raw and auxiliary materials, and then make granules through a dry granulator, and collect the granules below 80 mesh for future use.

[0100] Detection indicators and methods:

[0101] With embodiment 1-1.

[0102] result:

[0103]

[0104] Note: 1- a few visible particles; 2- no...

Embodiment 3

[0117] Embodiment 3 On the basis of Example 1, different types of disintegrants are added to prepare single and multiple doses of cefprozil dry suspension

[0118] Xanthan gum with a viscosity of 1415mPa·s was used to carry out disintegrant screening test in combination with different disintegrants in a certain proportion.

[0119] Single dose of cefprozil dry suspension prescription containing main drug 125mg:

[0120]

[0121]

[0122] Prescription of multiple doses of cefprozil dry suspension containing 5g of the main drug:

[0123]

[0124] result:

[0125] The sedimentation volume ratios measured by the aforementioned method were all qualified, and no obvious sedimentation was seen after standing for 3 hours.

[0126]

[0127] The results showed that the preferred disintegrants were crospovidone, sodium starch glycolate and croscarmellose sodium.

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K31/545A61K47/36A61K47/38A61P31/04
Inventor 张雯张曼红孙玲赵爱丽
Owner SHANDONG INST OF PHARMA IND
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