Preparation Technology and Optimization of Formulation of Hydroxycamptothecin Sustained-released Tablets / 中国药房

OBJECTIVE:To prepare hydroxycamptothecin sustained-release tablets and to optimize its preparation technology and formulation.METHODS:The preparation technology and formulation were optimized by orthogonal experiment taking the type of excipient polylactic acid (A),tabletting pressure (B),ratio of HCPT to PLA (C) as factors with the deviation degree of the accumulative release percentage as evaluation index.Then the optimized results were verified.RESULTS:The optimal technology and formulation were as follows:A was PLA (20 000),B was 250 N,C was 1∶5.The deviation degree of the formulation was verified to be 2.963.CONCLUSION:The hydroxycamptothecin sustained-release tablets prepared in optimized preparation technology and formulation are up to the standard on preparation.

Study on the bioequivalence of gliclazide sustained released tablet in healthy volunteers / 中国药理学通报

Aim To evaluate the bioequivalence of two preparations of gliclazide in healthy volunteers.Methods The concentration of gliclazide was measured by high performance liquid chromatography(HPLC) after a single or multiple dosage of gliclazide sustained released tablet in healthy volunteers.The pharmacokinetic parameters of the two preparations were calculated by 3P97 program.LnAUC0~∞,lnAUC0~72 and lnAUC0~? were used to evaluate the bioequivalence of the two preparations with analysis of variance and two one-side t-test.Results Both the gliclazide extended action tablet were best fitted to one-compartment model.The main parameters of the tested and reference gliclazide after a single dose were as follows:Cmax(2.07?0.61) and(2.26?0.61)mg?L-1;Tmax(5.10?0.55)h and(5.05?0.51)h;T12Ka(1.50?0.26)h and(1.52?0.27)h;T12Ke(8.89?1.56)h and(8.68?1.72)h;MRT(22.63?1.01)h and(22.38?0.93)h;AUC0~72(39.19?8.03)mg?h-1?L-1 and(39.26?8.37)mg?h-1?L-1;AUC0~∞:(45.80?9.51)mg?h-1?L-1 and(45.57?9.76)mg?h-1?L-1;F0~72 and F0~∞(100.19?6.22)% and(100.85?5.88)%,respectively.The main parameters of the tested and reference gliclazide after multiple dose were as follows:Cmax(4.83?0.86)mg?L-1 and(4.69?0.64)mg?L-1;Cmin(0.68?0.14) mg?L-1 and(0.66?0.12)mg?L-1;Tmax:(4.10?0.45) h and(4.10?0.55)h;T12Ka:(2.03?0.53)h and(2.04?0.40)h;T12Ke:(7.24?0.87)h and(7.09?1.14)h;MRT(9.17?0.30)h and(9.19?0.37)h;AUCSS:(41.62?6.48) mg?h-1?L-1 and(42.18?6.03)mg?h-1?L-1;Cav:(1.73?0.27)mg?L-1 and(1.76?0.25)mg?L-1;DF(240.85%?34.07)and(230.23%?24.80%) respectively.The relative bioavailability was(98.60?4.60)%.The AUC0~T,AUC0~∞ or AUCSS,Cmax and Tmax were bioequivalent between the two preparations.Conclusion The tested and reference gliclazide sustained released tablet are bioequivalent.

Pharmacokinetics and bioequivalence of sustained-released tablet of nefopam / 中国临床药理学与治疗学

AIM: To verify the bioequivalence between sustained released tablet of nepopam and normal one. METHODS: 18 volunteers were randomly devided into two groups. Double periodical crossed design was used, and poly dose of nefopam was administered to 18 volunteers following single dose after one week interval. The concentration of nefopam hydrochloride in serum was determinated by HPLC, and the related parameters came out through 3p97 programme. RESULTS: In the single dose test the drug concentration of sustained released tablet maitained 2040 mg?L -1 for 10 h ,c max was ( 45.8 ?15.7) mg?L -1 ,t peak was ( 3.4 ? 0.8) h , and the corresponding parameters of normal tablet were over 20 mg?L -1 for 7.5 h ,( 72.7 ?26.0) mg?L -1 ,and ( 1.6 ? 0.6) h . The AUC was ( 363.4 ? 107.1 ) and ( 374.8 ?125.7) mg?h?L -1 respectively, and F was ( 1.02 ? 0.25 ). In the poly dose test the c max of sustained released and normal one was ( 31.50 ? 12.65 ) and ( 33.68 ?10.51) mg?L -1 ,c min was ( 13.4 ? 4.4 ) and ( 10.9 ?5.4) mg?L -1 , t peak was ( 2.6 ? 0.6 ) and ( 1.22 ? 0.46) h , and FI was ( 0.77 ? 0.26 ) and ( 1.04 ? 0.18 ) respectively. CONCLUSION: The sustained released tablet is credible and the two types of tablet are equieffective in AUC.