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1.
Drug Metab Pers Ther ; 37(4): 383-391, 2022 12 01.
Artigo em Inglês | MEDLINE | ID: mdl-36027921

RESUMO

OBJECTIVES: A comparative dissolution kinetics test (CDKT) and bioequivalence studies of generic proton pump inhibitors (PPIs) do not model pharmacological acid suppression (PAS) and pathological duodenogastric reflux (PDGR). This study aimed to model them in CDKT to assess drugs stability and potential pantoprazole-clarithromycin interactions. METHODS: In CDKT, PDGR (dissolution medium pH 7.00 ± 0.05, preexposure at pH 1.20 ± 0.05) and PAS (pH 4.00 ± 0.05) were modelled for original pantoprazole (OP) and its generics (GP1-4). In CDKT with high-performance liquid chromatography, dissolution gastric medium in adequate (pH 4.00 ± 0.05) and inadequate (pH 1.20 ± 0.05) PAS were modelled for original clarithromycin (OC) and its generics (GC1-4). RESULTS: After exposure in pH 7.00 ± 0.05, pantoprazole was released from GP1 within 10 min in the amount of 68.8%. In рН 4.00 ± 0.05, 83.0% and 81.5% of pantoprazole were released from GP1 and GP4. When OP, GP2 and GP3 were placed in pH 7.00 ± 0.05, pantoprazole was released in amount: 99.4%, 88.0% and 98.2%. Clarithromycin releasing from OC, GC1, GC2, GC3, GC4 in pH 4.00 ± 0.05 was 93.5%, 91.6%, 92.9%, 79.4% and 83.0%. In pH 1.20 ± 0.05: 9.7%, 6.7%, 8.5%, 33.3%, 28.8%. CONCLUSIONS: Destruction of enteric coats of some local pantoprazole generics in CDKT-models might be a potential factor for inadequate therapy.


Assuntos
Claritromicina , Helicobacter pylori , Humanos , Claritromicina/farmacologia
2.
Pharmacogenomics ; 21(10): 677-694, 2020 07.
Artigo em Inglês | MEDLINE | ID: mdl-32539557

RESUMO

Background: The aim of this study was to determine the prevalence of CYP2C9, VKORC1, CYP2C19, ABCB1, CYP2D6 and SLCO1B1 genes polymorphisms among residents of the Volga region (Chuvash and Mari) and northern Caucasus (Kabardins and Ossetians). Materials & methods: The study involved 845 apparently healthy volunteers of both sexes of the four different ethnic groups living in the Russian Federation: 238 from the Chuvash ethnic group, 206 Mari, 157 Kabardins and 244 Ossetians. Results: Significant differences were identified in allele frequency of CYP2C9, VKORC1, CYP2C19, ABCB1, CYP2D6 and SLCO1B1 genes polymorphisms between the Chuvash and Kabardins, Chuvash and Ossetians, Mari and Kabardians, Mari and Ossetians.


Assuntos
Biomarcadores/metabolismo , Doenças Cardiovasculares/genética , Sistema Cardiovascular/metabolismo , Etnicidade/genética , Alelos , Doenças Cardiovasculares/metabolismo , Feminino , Frequência do Gene/genética , Humanos , Masculino , Farmacogenética/métodos , Testes Farmacogenômicos/métodos , Polimorfismo Genético/genética , Prevalência , Federação Russa
3.
Drug Metab Pers Ther ; 34(3)2019 10 14.
Artigo em Inglês | MEDLINE | ID: mdl-31606725

RESUMO

Background High values of endogenous levels of magnesium (Mg) in the body and mechanisms of homeostasis regulation make it difficult to assess the bioavailability of these drugs. The aim of this study was to assess the Mg concentration in blood in volunteers and in erythrocytes in patients with hypomagnesemia. Methods The study included 20 healthy volunteers and 62 patients with chronic heart failure (CHF) I-III functional class (FC) NYHA classification. We studied the composition of Mgorotate and Mgorotate plus potassium (К)orotate. Blood sampling was carried out at 8 a.m. and within 10 h after administering the drugs. Measurement of Mg pharmacokinetic parameters: AUC (concentration of the active substance-time), and Cmax (maximum concentration) in volunteers and measurement of the concentration of Mg in erythrocytes of patients. Results The results indicated that both the AUC in volunteers and concentration of Mg in erythrocytes of patients are comparable, and the differences are not statistically significant. Conclusions The study showed that the standard method of calculating the AUC (total serum Mg) is insufficient for comparative evaluation of Mg absorption due to the high levels of its endogenous content and a small increase in concentration after taking the drugs. It is advisable to assess the concentration of Mg in the red blood cells of patients.


Assuntos
Insuficiência Cardíaca/sangue , Magnésio/sangue , Magnésio/farmacocinética , Administração Oral , Adolescente , Adulto , Disponibilidade Biológica , Doença Crônica , Eritrócitos/química , Eritrócitos/metabolismo , Feminino , Voluntários Saudáveis , Humanos , Magnésio/administração & dosagem , Masculino , Pessoa de Meia-Idade , Sais/administração & dosagem , Sais/sangue , Sais/farmacocinética , Adulto Jovem
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