Objective: To characterise a novel multifunctional pharmaceutical excipient and investigate its ef ect on paracetamol release from tablets prepared by direct compression.Methods: The excipient was prepared by co-proce...Objective: To characterise a novel multifunctional pharmaceutical excipient and investigate its ef ect on paracetamol release from tablets prepared by direct compression.Methods: The excipient was prepared by co-processing gelatinized maize starch with sodium carboxymethyl cellulose and microcrystalline cellulose in a ratio of 2:1:1, dried and pulverized into powder. The excipient formulated was characterized using Fourier transform infrared spectroscopy and dif erential scanning calorimetry. The excipient was used to prepare batches of tablets by direct compression with drug-excipient ratios of 1:1, 1:2, 1:3 and 1:4. Parameters evaluated on tablets include crushing strength, friability and in vitro dissolution studies. Results: Differential scanning calorimetry analysis revealed a crystalline excipient while Fourier transform infrared spectroscopy showed no interaction between the excipient and paracetamol. Tablets from all the batches gave average crushing strength values between 3.47 and 4.88 kp. The 1:1 and 1:2 tablet batches were comparable to each other while 1:3 and 1:4 were also comparable to one another in their dissolution proi les. The dissolution parameters of the 1:4 batch was faster with- m∞(90.5%), t50%(3.5 min), t70%(11.6 min) while that of ratio 1:1 was the least with- m∞(48.6%), m5min(23.8%). Their release kinetics followed a KorsmeyerPeppas model with a super case-II transport mechanism.Conclusions: The drug-excipient ratios of 1:3 and 1:4 gave pharmaceutically acceptable tablets that met the British Pharmacopoeia specii cations. The t50% value of the 1:4 batch of tablets may i nd its usefulness in formulating drugs for which a fast onset of action is desired.展开更多
Objective To compare the pharmacokinetics and relative biological availability of Paracetatool orally disintegrating tablets and general tablets in healthy volunteers. Methods In a random two periods crossover study, ...Objective To compare the pharmacokinetics and relative biological availability of Paracetatool orally disintegrating tablets and general tablets in healthy volunteers. Methods In a random two periods crossover study, 19 healthy male Chinses volunteers received a single dose of Paracetamol 500mg of two formularies respectively. The plasma concentration of paracetamol was determined by HPLC method. The pharmacokinetic parameters of the two preparation and the relative biological availability of Paracetamol orally disintegrating tablets and general tablets were caculated with statistical analysis. Results The main pharmacokinetic parameters of paracetamol orally disintegrating tablets and general tablets were （ 31436. 70 ± 7062. 80 μg · h^ -1· L^-1 and （29871.40 ± 7965.04） μg · h^ -1· L^-1 for AUC0-1 （33295. 7 ±7663. 10） μg · h^ -1· L^-1 and（31845. 20 ± 8830. 83 ） μg · h^ -1· L^-1 forAUC0-1（9. 71 ±2. 78） μg/ml and（10. 36 ±3. 86） μg/mlfor Cmax; （0. 82 ±0. 45）h and （0. 74± 0.67）hforTmax;（2.90±0. 42）h and （3. 13 ±0. 67）h for T1/2ke;（0.24 ±0.04） and （0.23 ±0.04） for Ke; （4. 1481±0. 4492 ） and （4. 0771 ±0. 8131 ） for mean residence time （ MRT） , respectively. Variance analysis showed that there was significant difference in AUC0-12 and Cmax between the two preparations. Conclusion The paracetamol orally disintegrating tablets and general tablets are bioequivalent and the relative biological availability of Paracetamol orally disintegrating tablets is （ 108 ± 19） %.展开更多
The application of artificial neural network(ANN) and near-infrared spectroscopy for pharmaceutical nondestructive quantitative analysis of Paracetamol was investigated. The artificial neural network patterns of Parac...The application of artificial neural network(ANN) and near-infrared spectroscopy for pharmaceutical nondestructive quantitative analysis of Paracetamol was investigated. The artificial neural network patterns of Paracetamol tablet medicines, powder medicines, first derivative spectra and second derivative spectra were established, and they were compared each other. The uncertain specimens were predicted. The parameters affecting ANN were discussed. A new network evaluation criterion, i.e., the degree of approximation, was employed, and the predicted results were reliable.展开更多
文摘Objective: To characterise a novel multifunctional pharmaceutical excipient and investigate its ef ect on paracetamol release from tablets prepared by direct compression.Methods: The excipient was prepared by co-processing gelatinized maize starch with sodium carboxymethyl cellulose and microcrystalline cellulose in a ratio of 2:1:1, dried and pulverized into powder. The excipient formulated was characterized using Fourier transform infrared spectroscopy and dif erential scanning calorimetry. The excipient was used to prepare batches of tablets by direct compression with drug-excipient ratios of 1:1, 1:2, 1:3 and 1:4. Parameters evaluated on tablets include crushing strength, friability and in vitro dissolution studies. Results: Differential scanning calorimetry analysis revealed a crystalline excipient while Fourier transform infrared spectroscopy showed no interaction between the excipient and paracetamol. Tablets from all the batches gave average crushing strength values between 3.47 and 4.88 kp. The 1:1 and 1:2 tablet batches were comparable to each other while 1:3 and 1:4 were also comparable to one another in their dissolution proi les. The dissolution parameters of the 1:4 batch was faster with- m∞(90.5%), t50%(3.5 min), t70%(11.6 min) while that of ratio 1:1 was the least with- m∞(48.6%), m5min(23.8%). Their release kinetics followed a KorsmeyerPeppas model with a super case-II transport mechanism.Conclusions: The drug-excipient ratios of 1:3 and 1:4 gave pharmaceutically acceptable tablets that met the British Pharmacopoeia specii cations. The t50% value of the 1:4 batch of tablets may i nd its usefulness in formulating drugs for which a fast onset of action is desired.
文摘Objective To compare the pharmacokinetics and relative biological availability of Paracetatool orally disintegrating tablets and general tablets in healthy volunteers. Methods In a random two periods crossover study, 19 healthy male Chinses volunteers received a single dose of Paracetamol 500mg of two formularies respectively. The plasma concentration of paracetamol was determined by HPLC method. The pharmacokinetic parameters of the two preparation and the relative biological availability of Paracetamol orally disintegrating tablets and general tablets were caculated with statistical analysis. Results The main pharmacokinetic parameters of paracetamol orally disintegrating tablets and general tablets were （ 31436. 70 ± 7062. 80 μg · h^ -1· L^-1 and （29871.40 ± 7965.04） μg · h^ -1· L^-1 for AUC0-1 （33295. 7 ±7663. 10） μg · h^ -1· L^-1 and（31845. 20 ± 8830. 83 ） μg · h^ -1· L^-1 forAUC0-1（9. 71 ±2. 78） μg/ml and（10. 36 ±3. 86） μg/mlfor Cmax; （0. 82 ±0. 45）h and （0. 74± 0.67）hforTmax;（2.90±0. 42）h and （3. 13 ±0. 67）h for T1/2ke;（0.24 ±0.04） and （0.23 ±0.04） for Ke; （4. 1481±0. 4492 ） and （4. 0771 ±0. 8131 ） for mean residence time （ MRT） , respectively. Variance analysis showed that there was significant difference in AUC0-12 and Cmax between the two preparations. Conclusion The paracetamol orally disintegrating tablets and general tablets are bioequivalent and the relative biological availability of Paracetamol orally disintegrating tablets is （ 108 ± 19） %.
文摘The application of artificial neural network(ANN) and near-infrared spectroscopy for pharmaceutical nondestructive quantitative analysis of Paracetamol was investigated. The artificial neural network patterns of Paracetamol tablet medicines, powder medicines, first derivative spectra and second derivative spectra were established, and they were compared each other. The uncertain specimens were predicted. The parameters affecting ANN were discussed. A new network evaluation criterion, i.e., the degree of approximation, was employed, and the predicted results were reliable.
