1.Introduction of Product
Cefaclor was a semi-synthetic cephalosporin antibiotic with a broad spectrum of bactericidal activity, the activity against Staphylococcus aureus which could produce penicillin enzyme,Hemolytic streptococcus A,Streptococcus viridans and Staphylococcus epidermidis was same with the Cefadroxil. the activity againsted Staphylococcus aureus which could��t produce penicillin enzyme and pneumococcus was 2-4 times stronger than Cefadroxil.the activity againsted gram-positive including Escherichia coli and Klebsiella sp was stronger than Cefalexin, was similar with Cefadroxil, the activity againsted Proteus mirabilis, Salmonella and Shigella was stronger than Cefadroxil.2.9-8mg/L of the product could restrain all the Haemophilus influenzae,including the fungoid resistance to Ampicillin.Moraxella catarrhalis and neisseria gonorrhoeae were sensitive to Cefaclor. indole-positive Proteus,Salmonella,Acinetobacter spp and Pseudomonas species were resistancer to Cefaclor.The function mechanism was restrainning the synthesis of the cell wall.
Our company had developed this Cefaclor Dispersible Tablets earlier in domestic and foreign, we had the mature technology in developing dispersible tablets, the dispersible tablets could be rapidly disintegrated in 15 seconds.it was the best dosage-forms for child and elder.
The composition of Cefaclor dispersible tablets: Cefaclor, Sodium Lauryl Sulfate, low-Substituted Hydroxyproxyl Cellulose, Microcrystalline Cellulose and so on,wet-compression technology was adopted to prepare the tablets.
Disintegration time and dispersive stability
As related stipulation to the dispersible tablets in pharmacopoeia,Took two pieces, put into 100ml water(warm is 20��1��) and shaking,3 minutes it should disintegrated completely and passed through mesh second.
Jerques six batches of samples as follow,the result as Table 1.
Table 1 the result of Cefaclor dispersible tablets��disintegration time and the disperser stabilitity
| batch No average times of Disintegration(s) dispersive stability
20000504 12.2 up to the mustard
20000506 11.7 up to the mustard
20000508 13.1 up to the mustard
20010312 12.6 up to the mustard
20010314 12.4 up to the mustard
20010316 13.2 up to the mustard
The result indicated that six batches of samples disintegrated in 3 mins and the dispersive stability was up to the related requests of the CP2005 second.
Cefaclor was well absorbed gastro-intestinal tract with after oral administration,and appeared to be widely distributed in the body, the oral doses of 500 mg producing peak plasma concentrations of about 13.44 mg/L at 0.56 hour(tmax),the plasma half-life was 0.57 hour(t1/2),This may achieved the enough density in pus in the eardrum, The density was highest in the saliva and the tear. About 25% was bound to plasma proteins, approximately 15% a dose in vivo metabolism.It was rapidly excreted by the kidneys,approximately 77% of a dose appeared unchanged in the urine within 8 hours,the concentrations in urine was high,it was excreted by the kidneys approximates 0.05%,the concentrations in kidneys was low,The hemodialysis could excrete it partially.
Among 67 total 126 patients, we enrolled 67 patients(group A) in test group in which patients were treated by Cefaclor,0.5g,tid;and other 59 patients(group B) were in the control group in which patients were treated by Cefradine, 0.5g,tid; the period of treatment were 10-14d, results:In the randomized controlled trial, the clinic recovery the efficacy rate of group A was 92.54% group B was 77.97%,the rate of bacterial elimination was 84.75% and 70.00% respectiveily,which indicated a signinficant difference in statistics(p<0.05).Conclusion:Cefaclor had the stronger treatment of under respiratory tract infection.the rate of adverse reactions was low,high safty, which had reliable clinic effect was worthy of application on the treatment of under respiratory tract infection.
460 child patients with respiratory tract bacterial infections were treated with cefaclor,the period of treatment was 7d,results: the totle effective rates were 91.30%, the rate of the treatment of acute tonsillitis was 84.75%, the acute bronchitis is 95.00% and bronchopneumonia is 81.88%.
52 with urinosexual tract infections were treated with cefaclor in comparison with 46 patients of the same diseases treated with cefradine. results:The total effective and bacterial eradication rates were 92.3% and 87%,the simple urinosexual tract infective rates were 100.0% and 94.1%, the complex urinosexual tract infective rates were 90.5% and 84.2%,the rates of treatment of prostatitis were 83.3% and 80.0%,which indicated no signinficant difference in statistics(P>0.05) between the two arms in total effective rate. The total effective and bacterial eradication rates were 88.9% and 82.9%, with no significant difference((P>0.05)),Incidence rates of ADRs were 5.8% for active arm and 8.7% for control arm.conclusion:Cefaclor was effective in treatment of urinosexual tract infection especially mild and moderate urinary infections with mild ADRs.