A dissolution test for fesoterodine low dose extended-release tablets using liquid chromatographic(LC) method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically at ...A dissolution test for fesoterodine low dose extended-release tablets using liquid chromatographic(LC) method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically at controlled temperature(40 1C) using a mobile phase of acetonitrile:methanol:0.03 M ammonium acetate(p H 3.8)(30:15:55, v/v/v), run at a flow rate of 1.5 m L/min and detected at 208 nm. The best dissolution conditions for this formulation were achieved using a USP apparatus 2(paddle) at 100 rpm and 900 m L of phosphate buffer at p H 6.8 as the dissolution medium.Validation parameters such as the specificity, linearity, accuracy, precision, and robustness were evaluated according to international guidelines, giving results within the acceptable range. The kinetic parameters of drug release were also investigated using model-dependent methods and the dissolution profiles were best described by the Higuchi model. The validated dissolution test can be applied for quality control of this formulation.展开更多
We developed a novel portable and automated dissolution test analyzer for rapid and high precision in vitro dissolution testing of drugs.The analyzer consists of a flow-through-cell drug dissolution system,an automate...We developed a novel portable and automated dissolution test analyzer for rapid and high precision in vitro dissolution testing of drugs.The analyzer consists of a flow-through-cell drug dissolution system,an automated sequential sampling system,a high-speed capillary electrophoresis(HSCE)system,and a data acquisition system.Combining the high-temporal resolution flow-gating sampling approach with HSCE,which has outstanding advantages of efficient separation and resolution,the analyzer can achieve rapid analysis and exhibits the ability in miniaturization for on-site assessment of different active pharmaceutical ingredients.To integrate the flow-through-cell dissolution system with HSCE,a specially designed flow-gating-injection(FGI)interface was employed.The performance of the analyzer was investigated by analyzing the dissolution of immediate-release drugs including single dose(amoxicillin dispersible tablets)and fixed dose combination(amoxicillin and clavulanate potassium)drug tablets with the high-temporal resolutions of 12 s and 20 s,respectively.The dissolution profiles of different active pharmaceutical ingredients could be simultaneously and automatically monitored with high repeatability and accuracy.The analyzer was successfully utilized for the pharmaceutical quality control and bio-relevant dissolution testing,as well as in vivo-in vitro correlation analysis.Our portable analyzer is miniaturized,convenient and of low-cost,and will provide a valuable tool for dissolution testing in pharmaceutical research and development.展开更多
Nimodipine(NMD)is a dihydropyridine calcium channel blocker with selectivity for cerebral blood vessels and the major therapeutic indication of NMD is for the prevention and treatment of delayed ischemic neurological...Nimodipine(NMD)is a dihydropyridine calcium channel blocker with selectivity for cerebral blood vessels and the major therapeutic indication of NMD is for the prevention and treatment of delayed ischemic neurological disorders and other cerebrovascular disorders,such as stroke which is associated with biological rhythm.This study was mainly designed to solve the drawback of conventional NMD solid dosage form,low bioavailability and limited clinical efficacy,by preparing enteric solid dispersion(SD)and the SD was prepared via melting method.The physical state of the dispersed NMD in the polymer matrix was characterized by differential scanning calorimetry(DSC),powder X-ray diffraction(PXRD)and dissolution studies.Compared with pure drug and physical mixture,the dissolution of NMD-SD was enhanced dramatically(about 80%).Furthermore,in consideration of the biological rhythm of stroke,we first obtained a delayed-release tablet containing NMD-SD by a direct powder compression method.As shown in the dissolution studies,the tablet released less than 10%in the artificial gastric acid in the initial 2 h and released 32.1%,75%,more than 90%at 4,10 and 14 h respectively in the artificial intestinal fluid.This investigation has solved the problems of oral solid dosage forms of NMD,and it has the good industry prospect.展开更多
<span style="font-family:Verdana;">In</span><span style="font-family:""> </span><span style="font-family:""><span style="font-family:Verdan...<span style="font-family:Verdana;">In</span><span style="font-family:""> </span><span style="font-family:""><span style="font-family:Verdana;">recent years, consumers are becoming more health-conscious. Supplements are becoming popular as they can be purchased easily. In Japan, the “Food with Function Claims” system began in 2015;the market for supplements is expected to continue to expand. However, the use of some supplements has not been supported with sufficient scientific evidence;some products have even caused health problems. </span><span style="font-family:Verdana;">In addition</span><span style="font-family:Verdana;">, consumers may not be able to make correct decisions based on the information from the Internet. Unlike medicine, the instruction on the usage of supplements is not precise. Therefore, improving the quality of the information on the supplements will become more necessary in the future. This study aims to improve the quality of the information on supplements by surveying the disintegration and dissolution behavior of the carnitine-containing supplements and evaluated the</span><span style="font-family:Verdana;">ir quality. The products tested here were supplements containing commercial carnitine. Disintegration test and dissolution test were conducted according to the Japanese Pharmacopoeia. Carnitine was quantified by high-performa</span><span style="font-family:Verdana;">nce liquid chr</span><span style="font-family:Verdana;">omatography. The disintegration tests revealed that the products </span><span style="font-family:Verdana;">had different disintegration times, varying from 35 to 100 minutes;some products took more than 5 hours to disintegrate. Thus, some products had a slow rise in their dissolution rate. These results suggest that the carnitine-containing supplements used in this study may affect the absorption process. Therefore, in the case of oral administration, the expected effect might not </span><span style="font-family:Verdana;">be achieved depending on the product.</span></span>展开更多
基金CAPES(Coordenacao de Aperfeicoamento de Pessoal de Nível Superior)FAPERJ(Fundacao de Amparo a Pesquisa do Estado do Rio de Janeiro)for the financial support
文摘A dissolution test for fesoterodine low dose extended-release tablets using liquid chromatographic(LC) method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically at controlled temperature(40 1C) using a mobile phase of acetonitrile:methanol:0.03 M ammonium acetate(p H 3.8)(30:15:55, v/v/v), run at a flow rate of 1.5 m L/min and detected at 208 nm. The best dissolution conditions for this formulation were achieved using a USP apparatus 2(paddle) at 100 rpm and 900 m L of phosphate buffer at p H 6.8 as the dissolution medium.Validation parameters such as the specificity, linearity, accuracy, precision, and robustness were evaluated according to international guidelines, giving results within the acceptable range. The kinetic parameters of drug release were also investigated using model-dependent methods and the dissolution profiles were best described by the Higuchi model. The validated dissolution test can be applied for quality control of this formulation.
基金supported by the National Natural Science Foundation of China(Grant No.21775017)the Natural Science Foundation of Jilin Province,China(Grant No.20180101174JC)。
文摘We developed a novel portable and automated dissolution test analyzer for rapid and high precision in vitro dissolution testing of drugs.The analyzer consists of a flow-through-cell drug dissolution system,an automated sequential sampling system,a high-speed capillary electrophoresis(HSCE)system,and a data acquisition system.Combining the high-temporal resolution flow-gating sampling approach with HSCE,which has outstanding advantages of efficient separation and resolution,the analyzer can achieve rapid analysis and exhibits the ability in miniaturization for on-site assessment of different active pharmaceutical ingredients.To integrate the flow-through-cell dissolution system with HSCE,a specially designed flow-gating-injection(FGI)interface was employed.The performance of the analyzer was investigated by analyzing the dissolution of immediate-release drugs including single dose(amoxicillin dispersible tablets)and fixed dose combination(amoxicillin and clavulanate potassium)drug tablets with the high-temporal resolutions of 12 s and 20 s,respectively.The dissolution profiles of different active pharmaceutical ingredients could be simultaneously and automatically monitored with high repeatability and accuracy.The analyzer was successfully utilized for the pharmaceutical quality control and bio-relevant dissolution testing,as well as in vivo-in vitro correlation analysis.Our portable analyzer is miniaturized,convenient and of low-cost,and will provide a valuable tool for dissolution testing in pharmaceutical research and development.
基金special construction projects fund which belongs to“Taishan ScholardPharmacy Specially Recruited Experts”.
文摘Nimodipine(NMD)is a dihydropyridine calcium channel blocker with selectivity for cerebral blood vessels and the major therapeutic indication of NMD is for the prevention and treatment of delayed ischemic neurological disorders and other cerebrovascular disorders,such as stroke which is associated with biological rhythm.This study was mainly designed to solve the drawback of conventional NMD solid dosage form,low bioavailability and limited clinical efficacy,by preparing enteric solid dispersion(SD)and the SD was prepared via melting method.The physical state of the dispersed NMD in the polymer matrix was characterized by differential scanning calorimetry(DSC),powder X-ray diffraction(PXRD)and dissolution studies.Compared with pure drug and physical mixture,the dissolution of NMD-SD was enhanced dramatically(about 80%).Furthermore,in consideration of the biological rhythm of stroke,we first obtained a delayed-release tablet containing NMD-SD by a direct powder compression method.As shown in the dissolution studies,the tablet released less than 10%in the artificial gastric acid in the initial 2 h and released 32.1%,75%,more than 90%at 4,10 and 14 h respectively in the artificial intestinal fluid.This investigation has solved the problems of oral solid dosage forms of NMD,and it has the good industry prospect.
文摘<span style="font-family:Verdana;">In</span><span style="font-family:""> </span><span style="font-family:""><span style="font-family:Verdana;">recent years, consumers are becoming more health-conscious. Supplements are becoming popular as they can be purchased easily. In Japan, the “Food with Function Claims” system began in 2015;the market for supplements is expected to continue to expand. However, the use of some supplements has not been supported with sufficient scientific evidence;some products have even caused health problems. </span><span style="font-family:Verdana;">In addition</span><span style="font-family:Verdana;">, consumers may not be able to make correct decisions based on the information from the Internet. Unlike medicine, the instruction on the usage of supplements is not precise. Therefore, improving the quality of the information on the supplements will become more necessary in the future. This study aims to improve the quality of the information on supplements by surveying the disintegration and dissolution behavior of the carnitine-containing supplements and evaluated the</span><span style="font-family:Verdana;">ir quality. The products tested here were supplements containing commercial carnitine. Disintegration test and dissolution test were conducted according to the Japanese Pharmacopoeia. Carnitine was quantified by high-performa</span><span style="font-family:Verdana;">nce liquid chr</span><span style="font-family:Verdana;">omatography. The disintegration tests revealed that the products </span><span style="font-family:Verdana;">had different disintegration times, varying from 35 to 100 minutes;some products took more than 5 hours to disintegrate. Thus, some products had a slow rise in their dissolution rate. These results suggest that the carnitine-containing supplements used in this study may affect the absorption process. Therefore, in the case of oral administration, the expected effect might not </span><span style="font-family:Verdana;">be achieved depending on the product.</span></span>
