CN104688701A - Cefaclor tablet and preparation method thereof - Google Patents

Abstract

The invention discloses a cefaclor tablet and a preparation method thereof. By adding a novel excipient, the cefaclor tablet is prepared through an all-powder direct tabletting method, and adverse influences of moisture and heat on the stability of the cefaclor tablet are avoided. The cefaclor tablet prepared through the method is good in dissolution, high in stability and small in product size, the preparation method is simple in process, and quality is easy to control.

Description

A kind of cefaclor tablet and preparation method thereof

Technical field

The invention belongs to medical art, be specifically related to a kind of cefaclor tablet and preparation method thereof.

Background technology

Cefaclor belongs to second filial generation oral cephalosporin, is wide spectrum semi-synthetic cephalosporins antibiotic, all has very strong killing action to multiple gram positive bacteria and gram negative bacteria.Cefaclor is identical with cefadroxil with the activity of staphylococcus epidermidis to product penicillinase staphylococcus aureus, A group Hemolytic streptococcus, Streptococcus viridans, and to not producing enzyme staphylococcus aureus and pneumococcal antibacterial action, comparatively cefadroxil is strong 2 ~ 4 times.Gram negative bacilli is comprised to the activity of Escherichia coli and Klebsiella pneumoniae etc. to comparatively cefalexin is strong, similar with cefadroxil, to the activity of proteus mirabilis, Salmonella and Shigella, comparatively cefadroxil is strong.Cefaclor is applied to the infection caused by sensitive organism clinically, as respiratory tract infection, the infection of Er Bi section, urinary system infection, skin and soft tissue infection etc.

Cefaclor, to wet, thermally labile, adopts traditional wet granulation easily to cause label yellowish, related substance to raise.For improving its stability, have document (Chinese patent, CN103623412A) to adopt and first prepare blank granules, then add cefaclor crude drug and magnesium stearate, then cefaclor sheet prepared by tabletting, and the stability of product is improved.But because the particle size differences of blank auxiliary granule and crude drug is large, mixing homogeneity becomes the difficult point of quality control, also improve mixed process and tableting processes to the requirement of equipment.Also have document (Chinese Pharmaceutical, 2009,18 (4), 44 ~ 46.) to adopt a large amount of Lactis Anhydrous as filler, avoid wetting by direct compression technique, the impact of heat on cefaclor stability.But the consumption due to Lactis Anhydrous reaches every sheet about 105mg, and total tablet is 400mg heavily about, causes product size larger.

Summary of the invention

The object of this invention is to provide a kind of preparation method of new cefaclor sheet.The invention solves cefaclor in preparation process to wet and heat-labile problem, effectively prevent the problem that the cefaclor tablet sizes that adopts lactose full powder vertical compression to cause is large simultaneously.

Direct compression of full-powder is a kind of comparatively ideal preparation method of oral solid formulation, not only can reduce production cost, shorten the production cycle, can also avoid the wet and hot stability problem caused, be conducive to industrialization large-scale production.But realize full powder vertical compression, prescription and the several premise calls of technique demand fulfillment: (1) full mixture of powders should have good mobility; (2) full mixture of powders should have good formability; (3) under the rational formability of guarantee and mobility prerequisite, the size as far as possible controlling slice, thin piece is unsuitable excessive.

The drug content of cefaclor sheet 250mg specification greatly reduces compressibility and the mobility of direct compression.In order to improve mobility and the compressibility of full powder, if select conventional adjuvant (as lactose), then need larger use amount, this will make slice, thin piece oversize, affect direct technique, increase patient swallows difficulty.Therefore, the pharmaceutical excipient of a kind of high compressibility, high viscosity, agent of low hygroscopicity is selected to be the key of the technique solving large gauge cefaclor direct powder compression.

be BASF AG's development be applicable to large gauge, vertical compression type adjuvant to damp and hot sensitive product, there is high compressibility, high fluidity, agent of low hygroscopicity. be by lactose, PVP K30, crospovidone three according to a certain ratio, the complex to make through special process, compared with the simple mixtures of three kinds of compositions, there is the feature such as higher compressibility, more preferably particle size distribution, high adhesion, agent of low hygroscopicity.Its outstanding quality, make large gauge product can obtain higher hardness and extremely low friability under compression forces, and larger compression force does not affect the result of extraction of tablet yet yet.In addition, agent of low hygroscopicity, also can improve the problem of the poor stability that cefaclor sheet causes because of the moisture absorption.

Prescription and the technique preparing cefaclor sheet provided by the present invention, appropriate by adding excipient, realizes direct compression of full-powder. excellent characteristic, make the common filler of its amount ratio reduce 20 ~ 40%, under the prerequisite ensureing mobility and compressibility, ensure that the stripping of product, and solve the excessive difficult problem of cefaclor chip size.

A kind of cefaclor tablet provided by the present invention, it is characterized in that, prescription is composed as follows:

Its preparation method is as follows:

(1) by cefaclor crude drug with mixed with excipients crosses 100 mesh sieves, for subsequent use;

(2) 100 mesh sieves crossed by other adjuvants, for subsequent use;

(3) cefaclor taking recipe quantity with mixture, add the micropowder silica gel of recipe quantity, mix homogeneously;

(4) said mixture, adds the magnesium stearate of recipe quantity, mixes 1 ~ 2 minute;

(5) direct compression of full-powder, obtains cefaclor tablet.

Adopt the cefaclor sheet prepared by prescription provided by the invention and technique, within 30 minutes, dissolution is greater than 98%, and its sheet focuses on about 330mg.

Stripping is good, stability is high, product size is little to adopt the cefaclor tablet prepared by prescription provided by the invention and technique to have, and the preparation method technique provided is simple, and quality is easy to control.

Detailed description of the invention

Following exemplary embodiments is used for illustrating the present invention, and the simple replacement or improvement etc. done the present invention those skilled in the art all belong within the technical scheme that the present invention protects.

Embodiment 1:

The preparation of cefaclor sheet

Prescription forms:

Preparation method:

(1) by cefaclor crude drug with mixed with excipients crosses 100 mesh sieves, for subsequent use;

(2) 100 mesh sieves crossed by other adjuvants, for subsequent use;

(3) cefaclor taking recipe quantity with mixture, add the micropowder silica gel of recipe quantity, mix homogeneously;

(4) said mixture, adds the magnesium stearate of recipe quantity, mixes 1 ~ 2 minute;

(5) direct compression of full-powder, obtains cefaclor tablet.

Embodiment 2:

The preparation (contrast tablet 1) of cefaclor sheet

Prescription forms:

Preparation method:

(1) cefaclor crude drug is crossed 100 mesh sieves for subsequent use;

(2) all adjuvants are suitably dried rear mistake 100 mesh sieve for subsequent use;

(3) take the cefaclor of recipe quantity, lactose, pregelatinized Starch, 1/2 polyvinylpolypyrrolidone, mix homogeneously, slowly add with 5% starch slurry and keep stirring 10 minutes, soft material processed;

(4) cross 20 eye mesh screens to granulate;

(5) granule is in 45 ~ 55 DEG C of oven dry, 18 eye mesh screen granulate;

(6) after oven dry, granulate, the polyvinylpolypyrrolidone of additional 1/2 and magnesium stearate mix homogeneously, the cefaclor tablet of tabletting.

Embodiment 3:

The preparation (contrast tablet 2) of cefaclor sheet

Prescription forms:

Preparation method:

(1) supplementary material is crossed 100 mesh sieves, for subsequent use;

(2) cefaclor of recipe quantity, Lactis Anhydrous, cross-linking sodium carboxymethyl cellulose, micropowder silica gel mix homogeneously is taken;

(3) take the magnesium stearate of recipe quantity, join in above-mentioned mixed-powder;

(4) by said mixture direct powder compression, cefaclor tablet is obtained.

Embodiment 4:

Compressibility contrast test: according to the formulation and technology of embodiment 1, embodiment 2, embodiment 3, prepares the whole mixture of full powder and the whole mixture of granule respectively, adopts different compression force to suppress, and investigates hardness and the dissolution change of each embodiment sample.The results are shown in Table 1.

Table 1: the compressibility of each prescription and dissolution change under different pressures

Interpretation of result: in the pressure comparison test of table 1, the sample that embodiment 1 is prepared for formulation and technology of the present invention, embodiment 2 is samples of preparing of wet granulation technology routinely, and embodiment 3 is the samples prepared according to Lactis Anhydrous powder vertical compression technique.Find out from result of the test, along with compression force increases, three samples all show as hardness and become large, but by contrast, embodiment 1 provided by the invention increases with compression force, and hardness increases obviously, illustrate that the compressibility of embodiment 1 prescription is optimum.From dissolution aspect, along with the increase of compression force, the dissolution of three samples all has decline to a certain degree, but by contrast, the compression force size of embodiments of the invention 1 is minimum on dissolution impact.Comprehensive explanation, embodiments of the invention 1 prescription compressibility used is good, and the impact of dissolution pressed sheets power change is minimum.

Embodiment 5:

By the cefaclor tablet prepared by embodiment 1, embodiment 2, embodiment 3, influence factor's test is carried out in contrast, investigates the change of its character, dissolution and impurity.The results are shown in Table 2.

Table 2: influence factor's result of the test

Interpretation of result: find out from the result of the test of table 2, illumination condition 10 days, the related substance of embodiment 1, embodiment 2, tablet prepared by embodiment 3 all conforms with the regulations, and illustrates that cefaclor sheet is more stable to illumination; High temperature 60 DEG C of conditions 10 days, three sample related substances are all against regulation, illustrate that cefaclor sheet is unstable to high temperature, should avoid high temperature in technique as far as possible; High humidity 92.5% condition 10 days, embodiment 1,2,3 related substance is all against regulation, illustrate that cefaclor tablet stability affects by humidity environment larger, but from moisture absorption weightening finish index, embodiments of the invention 1 moisture absorption weightening finish is minimum, and slice, thin piece character ftractures, illustrate that formulation and technology hygroscopicity provided by the invention is low, improve the impact of humidity on cefaclor tablet stability to a certain extent.

Claims (2)

1. a cefaclor tablet, is characterized in that, prescription is composed as follows:

2. cefaclor tablet according to claim 1, its preparation method is as follows:

(1) by cefaclor crude drug with mixed with excipients crosses 100 mesh sieves, for subsequent use;

(2) 100 mesh sieves crossed by other adjuvants, for subsequent use;

(3) cefaclor taking recipe quantity with mixture, add the micropowder silica gel of recipe quantity, mix homogeneously;

(4) said mixture, adds the magnesium stearate of recipe quantity, mixes 1 ~ 2 minute;

(5) direct compression of full-powder, obtains cefaclor tablet.