scholarly journals Effects of the Chinese Herbal Formulation (Liu Wei Di Huang Wan) on the Pharmacokinetics of Isoflavones in Postmenopausal Women

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Wirin Limopasmanee ◽  
Sunee Chansakaow ◽  
Noppamas Rojanasthien ◽  
Maleeya Manorot ◽  
Chaichan Sangdee ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Oral Dose ◽  
Single Oral Dose ◽  
Postmenopausal Women ◽  
Pharmacokinetic Parameters ◽  
Soy Milk ◽  
Open Label ◽  
Fixed Sequence ◽  
Time Curve ◽  
Oral Doses

A combination of soy isoflavones andLiu Wei Di Huang Wan(LWDHW) is potentially effective for postmenopausal women with intolerable vasomotor episodes who are not suitable candidates for hormonal therapy. The objective of this open-label, three-phase, crossover study was to determine the influence of both single and multiple oral doses of LWDHW on isoflavone pharmacokinetics in healthy postmenopausal women. Eleven subjects were assigned to receive the following regimens in a fixed sequence with washout periods of at least one week: Phase A, a single oral dose of soy milk; Phase B, a single oral dose of soy milk coadministered with LWDHW; and Phase C, multiple oral doses of LWDHW for 14 days followed by a single oral dose of soy milk. Blood samples were collected and mixed withβ-glucuronidase/sulfatase to hydrolyze isoflavone conjugates to their respective aglycones (i.e., daidzein and genistein) and were determined using high performance liquid chromatography. The pharmacokinetic parameters analyzed were maximal plasma concentrationCmax, time to reach peak concentrationTmax, area under the plasma concentration-time curve (AUC), and half-life (t1/2). The results found no statistically significant differences in pharmacokinetic parameters of daidzein and genistein among the three regimens.

scholarly journals Pharmacokinetics and Bioequivalence Study of Two Ciprofloxacin Hydrochloride Tablets in Chinese Healthy Volunteers Under Fasting and Fed Conditions: A Randomized, Open-Label, Two-Formulation, Two-Sequence, Two-Period, Single-Dose Crossover Study.

2020 ◽  
Author(s):  
Fei Qin ◽  
Gan-Mi Wang ◽  
Jin-Ying Huang ◽  
Jia-Rong Wu ◽  
Wen-Jie Song ◽  
...  
Keyword(s):  
Single Dose ◽  
Plasma Concentration ◽  
Oral Dose ◽  
Single Oral Dose ◽  
Pharmacokinetic Parameters ◽  
Open Label ◽  
Time Curve ◽  
Ciprofloxacin Hydrochloride ◽  
Concentration Time ◽  
Plasma Concentration Time Curve

Abstract BackgroundCiprofloxacin is a broad-spectrum fluoroquinolone antibiotic which is active against a wide range of Gram-positive and Gram-negative bacteria. The study mainly aimed to determine the bioequivalence of two branded ciprofloxacin hydrochloride tablets (250 mg) under the fasting and fed conditions.MethodsThe study was carried out in 48 healthy Chinese subjects under fasting and fed conditions with a randomized, open-label, two-formulation, two-sequence, two-period, single-dose crossover design. In each period of the study, the subjects were assigned to receive a single oral dose of 250 mg of ciprofloxacin hydrochloride. Blood samples were collected from an hour before dosing to 36 h after administration with 16 time points in total. The bioequivalence analysis was performed after ln-transformation of the ciprofloxacin pharmacokinetic parameters including maximum concentration (Cmax), area under the plasma concentration–time curve from time 0 to time t (AUC0-t), area under the plasma concentration-time curve from time 0 to infinity (AUC0-∞). Two formulations are considered bioequivalent if the 90% confidence intervals (CIs) for the test/reference geometric mean ratios (GMRs) for the ln-transformed pharmacokinetic parameters fall within the standard acceptance range of 80% – 125%. ResultsIn total of 48 subjects were enrolled in the fasting and fed studies, and one of the subjects was excluded before the administration. In the fasting study, the 90% CIs for the test/reference GMRs of the ln-transformed data for Cmax, AUC0–t, and AUC0–∞ were 85.41% to 100.97%, 95.40% to 100.27%, and 95.48% to 100.30%, respectively. For the fed study, the 90% CIs for the test/reference GMRs of the ln-transformed data for Cmax, AUC0–t, and AUC0–∞ were 90.15% to 113.75%, 99.10% to 103.77% and 99.11% to 103.80%, respectively. A total of 8 of 47 subjects experienced AEs in the fasting and fed studies.ConclusionsIn the study, the generic (test) product of ciprofloxacin hydrochloride 250 mg was bioequivalent to the innovator (reference) product after a single oral dose administration under the fasting and fed conditions. Both two brands of ciprofloxacin tablets were safe and well tolerated.Trial registrationThe clinical trial was registered at Center for the Drug Evaluation of the National Medical Products Administration (registration number: CTR20171152; date of registration：September 25, 2017; http://www.chinadrugtrials.org.cn/clinicaltrials.searchlistdetail.dhtml).

scholarly journals Influence of Fructooligosaccharide on Pharmacokinetics of Isoflavones in Postmenopausal Women

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Supanimit Teekachunhatean ◽  
Sujitra Techatoei ◽  
Noppamas Rojanasthein ◽  
Maleeya Manorot ◽  
Chaichan Sangdee
Keyword(s):  
Oral Dose ◽  
Single Oral Dose ◽  
Postmenopausal Women ◽  
Pharmacokinetic Parameters ◽  
Two Phase ◽  
Fixed Sequence ◽  
Blood Samples ◽  
Single Oral Administration ◽  
Oral Doses ◽  
To Receive

The objective of the present paper was to determine the influence of fructooligosaccharide (FOS) on the pharmacokinetics of isoflavones in healthy postmenopausal women. The study was a fixed-sequence, two-phase, crossover study. Twelve subjects received a single oral dose of 300 mL of a soy beverage. Blood samples were collected before the dose and at 0.5, 1, 2, 4, 6, 8, 10, 12, 24, and 32 h after the administration of the soy beverage. After a washout period of at least 1 week, subjects were assigned to receive oral doses of FOS, 5 g each time, twice a day (after breakfast and dinner) for 14 days, followed by a single oral dose of the same soy beverage on the next day. Blood samples were then collected at the same time points mentioned previously. Plasma isoflavone concentrations were determined by HPLC. Continuous oral administrations of FOS followed by a single oral administration of soy beverage caused significant increases inCmax, AUC0–32, and AUC0–∞of genistein and AUC0–32of daidzein, comparing to those obtained following a single oral dose of soy beverage alone. Other pharmacokinetic parameters (Tmaxandt1/2of both aglycones and AUC0–∞of daidzein) between both regimens were not significantly different.

scholarly journals Herb-Drug Interaction betweenEchinacea purpureaand Darunavir-Ritonavir in HIV-Infected Patients

2010 ◽  
Vol 55 (1) ◽  
pp. 326-330 ◽  
Author(s):  
José Moltó ◽  
Marta Valle ◽  
Cristina Miranda ◽  
Samandhy Cedeño ◽  
Eugenia Negredo ◽  
...  
Keyword(s):  
High Performance ◽  
Geometric Mean ◽  
Echinacea Purpurea ◽  
The Body ◽  
Pharmacokinetic Parameters ◽  
Root Extract ◽  
Open Label ◽  
Fixed Sequence ◽  
Time Curve ◽  
Sequence Study

ABSTRACTThe aim of this open-label, fixed-sequence study was to investigate the potential ofEchinacea purpurea, a commonly used botanical supplement, to interact with the boosted protease inhibitor darunavir-ritonavir. Fifteen HIV-infected patients receiving antiretroviral therapy including darunavir-ritonavir (600/100 mg twice daily) for at least 4 weeks were included.E. purpurearoot extract capsules were added to the antiretroviral treatment (500 mg every 6 h) from days 1 to 14. Darunavir concentrations in plasma were determined by high-performance liquid chromatography immediately before and 1, 2, 4, 6, 8, 10, and 12 h after a morning dose of darunavir-ritonavir on days 0 (darunavir-ritonavir) and 14 (darunavir-ritonavir plus echinacea). Individual darunavir pharmacokinetic parameters were calculated by noncompartmental analysis and compared between days 0 and 14 with the geometric mean ratio (GMR) and its 90% confidence interval (CI). The median age was 49 (range, 43 to 67) years, and the body mass index was 24.2 (range, 18.7 to 27.5) kg/m2. Echinacea was well tolerated, and all participants completed the study. The GMR for darunavir coadministered with echinacea relative to that for darunavir alone was 0.84 (90% CI, 0.63-1.12) for the concentration at the end of the dosing interval, 0.90 (90% CI, 0.74-1.10) for the area under the concentration-time curve from 0 to 12 h, and 0.98 (90% CI, 0.82-1.16) for the maximum concentration. In summary, coadministration ofE. purpureawith darunavir-ritonavir was safe and well tolerated. Individual patients did show a decrease in darunavir concentrations, although this did not affect the overall darunavir or ritonavir pharmacokinetics. Although no dose adjustment is required, monitoring darunavir concentrations on an individual basis may give reassurance in this setting.

scholarly journals Effect of Short-Course Oral Ciprofloxacin on Isoflavone Pharmacokinetics following Soy Milk Ingestion in Healthy Postmenopausal Women

2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Nathathai Temyingyong ◽  
Nut Koonrungsesomboon ◽  
Nutthiya Hanprasertpong ◽  
Mingkwan Na Takuathung ◽  
Supanimit Teekachunhatean
Keyword(s):  
Oral Dose ◽  
Gut Microbiota ◽  
Single Oral Dose ◽  
Postmenopausal Women ◽  
Plasma Concentrations ◽  
Soy Milk ◽  
Blood Samples ◽  
Short Course ◽  
Oral Ciprofloxacin ◽  
Milk Ingestion

Soy isoflavones have several potential benefits related to postmenopausal health. Isoflavone glycosides, found predominantly in nonfermented soy products, e.g., soy milk, require conversion by gut microbiota to their respective bioavailable aglycones prior to absorption into portal circulation. Use of short-course oral ciprofloxacin for the treatment of acute uncomplicated cystitis, the incidence of which is increasing among postmenopausal women, might adversely affect gut microbiota. The objective of this one-group pre-post treatment study was to determine the effect of short-course oral ciprofloxacin on isoflavone pharmacokinetics in healthy postmenopausal women. Eleven postmenopausal subjects were assigned to consume a single oral dose of 375 mL UHT soy milk (SOY phase). Blood samples were collected immediately before soy milk ingestion and at specific times for 32 hours after soy milk ingestion. Following a washout period of at least seven days, subjects were assigned to take 250 mg oral ciprofloxacin after breakfast and dinner for three days, followed by a single oral dose of 375 mL UHT soy milk the next day (CIPRO/SOY phase). Blood samples were collected at the same time points as in the SOY phase. Plasma samples were treated withβ-glucuronidase/sulfatase and plasma concentrations of aglycones (genistein and daidzein) were determined using high-performance liquid chromatography.Cmax,AUC0-t, andAUC0-∞of both aglycones andTmaxof genistein obtained from the CIPRO/SOY phase were significantly lower than those obtained from the SOY phase, whileTmaxof daidzein and t1/2of both aglycones in the two phases were not significantly different.

scholarly journals Evaluation of Doravirine Pharmacokinetics When Switching from Efavirenz to Doravirine in Healthy Subjects

2016 ◽  
Vol 61 (2) ◽  
Author(s):  
Ka Lai Yee ◽  
Rosa I. Sanchez ◽  
Patrice Auger ◽  
Rachael Liu ◽  
Li Fan ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Healthy Subjects ◽  
Geometric Mean ◽  
Transcriptase Inhibitor ◽  
Open Label ◽  
Genetic Barrier ◽  
Fixed Sequence ◽  
Time Curve ◽  
Cyp3a4 Substrate

ABSTRACT Doravirine is a novel, potent nonnucleoside reverse transcriptase inhibitor (NNRTI) for the treatment of patients with human immunodeficiency virus type 1 (HIV-1) infection that demonstrates a high genetic barrier to resistance and that has been well tolerated in studies to date. Doravirine is a candidate for patients switching from less-well-tolerated NNRTIs, such as efavirenz. While doravirine is a cytochrome P450 3A4 (CYP3A4) substrate, efavirenz induces CYP3A4; therefore, the pharmacokinetics of both drugs following a switch from efavirenz to doravirine were assessed. This was a 3-period, fixed-sequence, open-label study. Healthy adults were dosed with doravirine at 100 mg for 5 days once daily (QD) (period 1). Following a 7-day washout, efavirenz was administered at 600 mg QD for 14 days (period 2). Subsequently, doravirine was administered at 100 mg QD for 14 days (period 3). Blood samples were collected for pharmacokinetic analyses. Twenty healthy subjects were enrolled, and 17 completed the study. One day after efavirenz cessation, the doravirine area under the concentration-time curve from predosing to 24 h postdosing (AUC0–24), maximum observed plasma concentration (C max), and observed plasma concentration at 24 h postdosing (C 24) were reduced by 62%, 35%, and 85%, respectively, compared with the values with no efavirenz pretreatment. These decreases recovered to 32%, 14%, and 50% for AUC0–24, C max, and C 24, respectively, by day 14 after efavirenz cessation. The doravirine C 24 reached projected therapeutic trough concentrations, based on in vitro efficacy, on day 2 following efavirenz cessation. Geometric mean efavirenz concentrations were 3,180 ng/ml on day 1 and 95.7 ng/ml on day 15, and efavirenz was present at therapeutic concentrations (>1,000 ng/ml) until day 4. Though doravirine exposure was transiently decreased following efavirenz treatment cessation, dose adjustment may not be necessary to maintain therapeutic concentrations of at least one drug during switching in a virologically suppressed population.

scholarly journals Herb-Drug Interaction between Echinacea purpurea and Etravirine in HIV-Infected Patients

2012 ◽  
Vol 56 (10) ◽  
pp. 5328-5331 ◽  
Author(s):  
José Moltó ◽  
Marta Valle ◽  
Cristina Miranda ◽  
Samandhy Cedeño ◽  
Eugenia Negredo ◽  
...  
Keyword(s):  
High Performance ◽  
Geometric Mean ◽  
Echinacea Purpurea ◽  
Interquartile Range ◽  
Pharmacokinetic Parameters ◽  
Root Extract ◽  
Open Label ◽  
Fixed Sequence ◽  
Time Curve ◽  
Content Type

ABSTRACTThe aim of this open-label, fixed-sequence study was to investigate the potential of the botanical supplementEchinacea purpureato interact with etravirine, a nonnucleoside reverse transcriptase inhibitor of HIV. Fifteen HIV-infected patients receiving antiretroviral therapy with etravirine (400 mg once daily) for at least 4 weeks were included.E. purpurearoot/extract-containing capsules were added to the antiretroviral treatment (500 mg every 8 h) for 14 days. Etravirine concentrations in plasma were determined by high-performance liquid chromatography immediately before and 1, 2, 4, 6, 8, 10, 12, and 24 h after a morning dose of etravirine on day 0 and etravirine plusE. purpureaon day 14. Individual etravirine pharmacokinetic parameters were calculated by noncompartmental analysis and compared between days 0 and 14 by means of the geometric mean ratio (GMR) and its 90% confidence interval (CI). The median age was 46 years (interquartile range, 41 to 50), and the median body weight was 76 kg (interquartile range, 68 to 92). Echinacea was well tolerated, and all participants completed the study. The GMR for etravirine coadministered withE. purpurearelative to etravirine alone was 1.07 (90% CI, 0.81 to 1.42) for the maximum concentration, 1.04 (90% CI, 0.79 to 1.38) for the area under the concentration-time curve from 0 to 24 h, and 1.04 (90% CI, 0.74 to 1.44) for the concentration at the end of the dosing interval. In conclusion, the coadministration ofE. purpureawith etravirine was safe and well tolerated in HIV-infected patients; our data suggest that no dose adjustment for etravirine is necessary.

An evaluation of the drug interaction potential of netupitant with digoxin.

2012 ◽  
Vol 30 (15_suppl) ◽  
pp. e19530-e19530
Author(s):  
Sybille Baumann ◽  
Silvia Olivari Tilola ◽  
Tulla Spinelli ◽  
Wolfgang Timmer
Keyword(s):  
Steady State ◽  
Oral Dose ◽  
Clinical Chemistry ◽  
Vital Signs ◽  
Therapeutic Index ◽  
Pharmacokinetic Parameters ◽  
Open Label ◽  
Fixed Sequence ◽  
Safety Parameters

e19530 Background: The new, highly selective neurokinin-1 receptor antagonist netupitant (NETU) has been developed to provide protection from nausea and vomiting in patients receiving emetogenic chemotherapy. There is evidence from in vitro studies that NETU is a substrate for and a weak inhibitor of the P-glycoprotein (Pgp). Pgp plays a major role in the pharmacokinetics of digoxin (DIG), a cardiac glycoside with a narrow therapeutic index. The possible interaction between NETU and Pgp has been assessed by analysing the effect of NETU on DIG pharmacokinetics. Safety parameters have also been assessed. Methods: This study was an open-label, fixed-sequence design to evaluate the effect of NETU on DIG at steady state in 16 healthy volunteers (8 male and 8 female). A loading dose of 3 x 0.5 mg DIG (0.5 mg every 6 hours) was given on day 1, followed by a daily oral dose of 0.25 mg DIG for 11 consecutive days (days 2-12); NETU was administered as single oral dose of 450mg on day 8. Serial blood and urine samples were collected for the determination of the pharmacokinetic parameters. Physical examination, vital signs, electrocardiogram (ECG), adverse events, clinical chemistry, hematology, urinalysis, and overall tolerability were reported. Results: Based on the AUC(0-24h) parameter at steady-state, the extent of DIG exposure was not influenced by NETU coadministration. The confidence interval of Cmin was within the 80-125% equivalence limits, while the observed Cmax was slightly over 125%, which was not considered clinically relevant. The excretion of DIG in urine was 57% after NETU coadministration compared to 55% of DIG alone. There were no gender-specific differences in the extent of absorption (AUC) for DIG, and no safety-related influence of DIG or NETU was observed on safety and laboratory assessments, vital signs, or ECG parameters. Based on historical data NETU pharmacokinetics was not affected by DIG coadministration. Conclusions: No clinically relevant interactions occurred between NETU and DIG. The results of this study suggest that the coadministration of NETU with Pgp substrates may not require dose adjustments. Study treatments were well tolerated.

scholarly journals PHARMACOKINETIC COMPARISON OF MONTELUKAST SODIUM FORMULATIONS AFTER A SINGLE ORAL DOSE IN HEALTHY GUINEA PIGS

2019 ◽  
pp. 165-169
Author(s):  
NEELAM SINGH ◽  
Giriraj T Kulkarni ◽  
Yatendra Kumar ◽  
GIRIRAJ T KULKARNI
Keyword(s):  
Plasma Concentration ◽  
Oral Dose ◽  
Single Oral Dose ◽  
Guinea Pigs ◽  
Elimination Rate ◽  
Pharmacokinetic Parameters ◽  
Time Data ◽  
Concentration Time ◽  
Montelukast Sodium ◽  
Significant Difference

Objective: Pharmacokinetic evaluation of montelukast sodium chronomodulated capsules (sustained-release solid dispersion of drug enclosed in pH-sensitive film-coated hard gelatin shell) and marketed tablets has been carried out in this study. Methods: A single oral dose of prepared capsules and marketed conventional tablets was administered in healthy male Dunkin-Hartley albino guinea pigs. Blood samples were collected at different time intervals and plasma concentration of drug was determined by reversed-phase high-performance liquid chromatography. Different pharmacokinetic parameters were assessed from plasma drug concentration-time profile by one-compartment model, first-order kinetics. Results: Pharmacokinetic parameters such as time to reach maximum concentration, elimination rate constant, elimination half-life, and mean residence time data indicates that drug release from chronomodulated capsules is significantly prolonged with initial release lag time of 3.5–4 h in comparison with marketed conventional tablets. However, maximum drug plasma concentration, area under the concentration-time curve, and apparent volume of distribution values show non-significant difference between capsules and marketed tablets. Conclusion: The findings specified that capsules were providing time controlled delivery of drug at a desired rate for prolonged time, which may be helpful for the prevention of episodic attack of asthma in early morning hours.

An Evaluation of the Potential for Pharmacokinetic Interaction between Tramadol and Cytochrome P450 2D6 Inhibitor Promethazine

2014 ◽  
Vol 989-994 ◽  
pp. 1041-1043
Author(s):  
Ping Liu ◽  
Liang Sun ◽  
Jian Zhang ◽  
Rui Chen Guo
Keyword(s):  
Single Dose ◽  
Plasma Concentration ◽  
Pharmacokinetic Interaction ◽  
Apparent Volume ◽  
Volume Of Distribution ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Open Label ◽  
Tramadol Hydrochloride ◽  
Time Curve

In this single-center, randomized, open-label, 3-way crossover study, subjects received each of the following: a single dose of Tramadol Hydrochloride Injection (THI) 35 mg, a single dose of Promethazine Hydrochloride Injection (PHI) 45 mg, and single dose of Compound Tramadol Hydrochloride Injection (CTHI) 80mg. Blood was collected and plasma was analyzed for the pharmacokinetic parameters (maximum plasma concentration [Cmax], time to Cmax [Tmax], area under the plasma concentration-time curve, plasma elimination half-life, clearance, and apparent volume of distribution) of Tramadol and Promethazine. In general, several pharmacokinetic interactions were observed between Tramadol and Promethazine in the present study.

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