Showing posts with label pharmacokinetics. Show all posts
Showing posts with label pharmacokinetics. Show all posts

Sunday, 4 January 2026

Fractional Pharmacokinetic Models in One-compartment Systems |Chapter 7 | Mathematics and Computer Science: Research Updates Vol. 8

 

Classical models typically use integer-order (ordinary) differential equations and predict exponential-like concentration decay after administration of drugs. These classical assumptions are adequate for many compounds but fail to capture anomalous behaviours seen in numerous drugs: long tails in concentration-time curves, non-exponential elimination, or irregular accumulation after repeated dosing. The study aimed to develop fractional pharmacokinetic models in one-compartment systems to enhance drug absorption. Fractional derivatives can be inserted into compartmental networks to create fractional multi-compartment models. Recent theoretical work provides a general framework for embedding fractional orders within compartmental mass-balance systems while preserving physically meaningful constraints (mass conservation and positivity), which is important for physiological interpretability. Practical implementations often use efficient strategies to reduce the cost of history terms (e.g., short-memory approximations, nonuniform time grids, or convolution quadrature approaches). Fractional models can inform controlled-release formulation design and the prediction of long-term toxicological accumulation. However, adoption in clinical pharmacology requires standardised parameter-estimation pipelines, software, and regulatory acceptance—areas currently under development. Widespread adoption will require advances in parameter estimation, computational tools, and translational validation, but the literature over the past two decades demonstrates clear progress and growing interest in fractional approaches.

 

 

Author(s) Details

Hemlata Saxena
Career Point University, Kota, India.

 

Please see the book here :- https://doi.org/10.9734/bpi/mcsru/v8/6795

Saturday, 13 September 2025

Dose Justification for Nanoparticle Formulation | Chapter 2 | Pharmaceutical Science: New Insights and Developments Vol. 8

 

Dose justification refers to the scientific rationale behind selecting a specific dose of a drug for human use. With the emergence of nanotechnology in pharmaceuticals, particularly nanoparticle formulations, this concept has evolved significantly. This study aims to shed light on the different approaches to justifying the dose of nanoparticles, using ibrutinib nanoparticles as an example. It also examines the relation between the dose and bioavailability, alongside considering relevant pharmacokinetic (PK) and pharmacodynamic (PD) parameters. The biopharmaceutical factors like Cmax, Tmax, and AUC are also considered for dose justification. The comparison of the radiation dose and nanoparticle dose taken internally or externally, and their relation, is highlighted. The NOAEL (No Observed Adverse Effect Level) and its limitations are discussed. The human equivalent dose and inhumane studies were listed along with the equivalent dose of nanoparticles. The Equivalent Dose Model, used in nanotoxicology, is presented as it calculates dose based on nanoparticle surface area rather than mass alone. Comprehensive data support the approval of the 50 mg nanoparticle dose, providing patients with a more effective and safer treatment option. Project Optimus by the FDA, which aims to refine and simplify oncology dose selection, is also considered. Key nanoparticle-specific factors like surface area and zeta potential are explained with the regulatory approvals. Nano drug formulations offer significant improvements in solubility and bioavailability. Incorporating PK/PD data, toxicity thresholds, nanoparticle-specific models, and regulatory guidelines ensures that the new dose maintains safety and efficacy. Finally, the integration of in silico modelling, Quantitative Structure-Activity Relationship model, and machine learning is proposed to enhance dose predictions, with standardised weighting factors suggested to improve risk assessment.

 

Author(s) Details

AVS Rajeswari
Department of Pharmaceutics, Arya College of Pharmacy, Kandi, Hyderabad, India.

 

B. Navya
Arya College of Pharmacy, Kandi, Hyderabad, India.

 

N. Sowmya
Arya College of Pharmacy, Kandi, Hyderabad, India.

 

P. Sailaja
Andhra University College of Pharmaceutical Sciences, Visakhapatnam, AP, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/psnid/v8/6145

Thursday, 10 July 2025

Evaluation of Pharmacokinetic Parameters of Cefquinome in Marathwadi Buffalo Calves, India | Chapter 9 | Innovations in Biological Science Vol. 10

 

The pharmacokinetics of cefquinome are studied in different animals such as camel, sheep, piglets, chicken, mice, dogs, pigs, and calves. However, these studies are conducted in different parts of the world and there is no data available from India. Therefore, this study aims to evaluate the Pharmacokinetic parameters of Cefquinome in Marathwadi Buffalo Calves. An experiment was performed on six healthy Marathwadi buffalo calves of either sex of age above 6 months and weighing between 80 to 120 kg to study the different pharmacokinetic parameters after a single intravenous administration @ 2 mg/kg body weight by microbiological assay technique. After intravenous administration of the drug, blood samples (4 ml each) of buffalo calves were collected from the external jugular vein using disposable needles in clot activator tubes at different time intervals. The schedule of blood collection for pharmacokinetic studies after intravenous administration was at 0, 5, 10, 15, 30 min and 1, 2, 4, 6, 8, 10, 12 and 24 hrs. The serum levels of cefquinome were estimated by microbiological assay technique using a large glass plate. Different Pharmacokinetic parameters were calculated as described by different scientists and analyzed by randomized block design, and the significance was tested at 5% and 1% levels as per. The peak serum concentration, elimination half-life, volume of distribution, total body clearance, absorption half-life and area under curve values found were 1.74 ± 0.151 mcg/ml at 2.5 min of sampling time, 1.97±0.14 h, 3.97 ± 0.83 L/kg (Vd(B)) and 2.86 ± 0.34L/kg (Vdss), 1.11 ± 0.13 L/kg.h-1, 0.10 ± 0.02 h, and 1.93 ± 0.23 µg/ml/hr respectively. The bioavailability of cefquinome in buffalo calves was found to be 165.38 %. It may be concluded that the elimination half-life of cefquinome was 2.54 h in Marathwadi buffalo calves indicating the repeating of doses at 12 to 15 h intervals in Marathwadi buffalo calves and the loading dose would be double than the maintenance dose of cefquinome after intravenous administration. The microbiological assay technique was found to be suitable for the estimation of serum cefquinome concentration in laboratories where the LC/MS facilities are not available.

 

Author(s) Details

M. K. Patil
College of Veterinary and Animal Sciences, Udgir Dist. Latur, Maharashtra-413517, India.

 

A. P. Somkuwar
Nagpur Veterinary College, Seminary Hills, Nagpur-440006, Maharashtra, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/ibs/v10/1206

Monday, 17 March 2025

Advancements in Therapeutic Drug Monitoring: Integrating Pharmacokinetics, Pharmacodynamics, and Bayesian Approaches for Personalised Medicine | Chapter 6 | Pharmaceutical Research: Recent Advances and Trends Vol. 9

 Therapeutic drug monitoring (TDM) is a critical process in clinical pharmacology that involves measuring drug concentrations in biological fluids to optimize drug dosage and ensure efficacy while avoiding toxicity. By incorporating pharmacokinetics (PK) and pharmacodynamics (PD) principles, TDM allows for individualized therapy, particularly for drugs with narrow therapeutic indices. Recent advancements, including population pharmacokinetic approaches and Bayesian estimation, have enhanced the precision of TDM. This review highlights the evolution of TDM, its role in optimizing patient outcomes, and emerging techniques such as pharmacodynamic monitoring to further individualize and refine therapeutic regimens.

 

Author (s) Details

 

V. Himabindu
Department of Pharmaceutics, Anurag Pharmacy College (Affiliated to JNTUH, Hyderabad), Kodad, Telangana, India.

 

G. Sangeetha Roy
Department of Pharmacy Practice, Anurag Pharmacy College (Affiliated to JNTUH, Hyderabad), Kodad, Telangana, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/prrat/v9/3134

Thursday, 27 February 2025

Developments in Nanosuspension Technology for Enhancing the Solubility and Bioavailability of Poorly Soluble Drugs | Chapter 7 | Pharmaceutical Science: New Insights and Developments Vol. 3

Drug formulation is greatly impacted by solubility around 40% of recently generated medications have poor water solubility. Improved solubility is a crucial step in the formulation of drugs and nanosuspensions have shown promise in tackling this problem. Nanosuspensions are made using a variety of methods including solvent evaporation, high-pressure homogenization and media milling. In addition to increasing a drug's solubility and bioavailability, nanosuspensions may affect its pharmacokinetics which may improve its safety and therapeutic effectiveness. The main objectives of recent studies and developments in nanosuspension technology have been to enhance formulation techniques, boost in-vitro and in-vivo performance and broaden their use in a variety of therapeutic domains. Additionally, the manufacturing and characterization of nanosuspensions have been improved by the use of patented techniques. In the formulation of nanosuspensions, key parameters like particle size, surface area, entrapment efficiency, and drug loading play a significant role in determining the overall performance of the drug. These factors directly influence the bioavailability, stability, and therapeutic effectiveness of the formulation. Balancing these parameters is critical to achieving the desired outcomes in drug delivery. This review emphasizes the promise of nanosuspensions as a flexible remedy for medications that are poorly soluble, highlighting their importance in contemporary drug research and their noteworthy influence on pharmaceutical innovation.

 

Author (s) Details

 

Saravanakumar Kasimedu
Department of Pharmaceutics, Seven Hills College of Pharmacy (Autonomous), Tirupati, Andhra Pradesh 517561, India.

 

Srividya Kanchibhotla
Department of Pharmaceutics, Seven Hills College of Pharmacy (Autonomous), Tirupati, Andhra Pradesh 517561, India.

 

Anusha Neelampalle
Department of Pharmaceutics, Seven Hills College of Pharmacy (Autonomous), Tirupati, Andhra Pradesh 517561, India.

 

Sai Mahesh Chengalasetty
Department of Pharmaceutics, Seven Hills College of Pharmacy (Autonomous), Tirupati, Andhra Pradesh 517561, India.

 

Lithin Sadum
Department of Pharmaceutics, Seven Hills College of Pharmacy (Autonomous), Tirupati, Andhra Pradesh 517561, India.

 


Chanhukya Dharmavaram
Department of Pharmaceutics, Seven Hills College of Pharmacy (Autonomous), Tirupati, Andhra Pradesh 517561, India.

 

Nagaveni Pommala
Department of Pharmaceutics, S.V.U. College of Pharmaceutical Sciences, S.V. University, Tirupati,
Andhra Pradesh 517502, India.

 

Lithin Sadum
Department of Pharmaceutics, Seven Hills College of Pharmacy (Autonomous), Tirupati, Andhra Pradesh 517561, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/psnid/v3/4459

Saturday, 1 February 2025

Advancements in Antibiotic Therapy: The Role and Future Scope of Ceftobiprole as a Fifth-generation Cephalosporin | Chapter 1 | Pharmaceutical Science: New Insights and Developments Vol. 2

The emergence of antibiotic resistance is a critical issue in modern medicine, significantly challenging the effectiveness of current antimicrobial agents. Among these, cephalosporins have played a central role in treating various bacterial infections. However, the rapid evolution of resistant pathogens, including those with extended-spectrum beta-lactamase (ESBL) and carbapenem-resistant mechanisms, necessitates the development of new-generation antibiotics. This chapter focuses on Ceftobiprole, a fifth-generation cephalosporin with potent activity against multidrug-resistant bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and penicillin-resistant Streptococcus pneumoniae.

Ceftobiprole’s pharmacokinetics and pharmacodynamics underscore its efficacy and safety, demonstrating high tissue penetration and a stable profile in renal excretion, which supports its use in severe infections like complicated skin and soft tissue infections (cSSTIs) and community-acquired pneumonia (CAP). Its mechanism of action involves binding to penicillin-binding proteins (PBPs), especially PBP2a in MRSA, disrupting cell wall synthesis and effectively neutralizing resistant pathogens. Regulatory approvals across Europe, Canada, and additional regions highlight Ceftobiprole's success as a critical therapeutic agent, and ongoing research aims to expand its indications to hospital-acquired infections.

As antibiotic resistance continues to rise, the development of advanced agents like Ceftobiprole is essential. This chapter reviews its clinical applications, history, and evolution, alongside its potential for integration into antimicrobial stewardship programs to mitigate resistance. Ceftobiprole’s broad spectrum and promising efficacy position it as a vital tool for addressing resistant infections, underscoring the importance of continued innovation in antibiotic development.

 

Author (s) Details

 

Hariharan M
Department of Pharmacy Practice, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Chennai 603 203, Tamil Nadu, India.

 

Sankari A
Department of Pharmacy Practice, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Chennai 603 203, Tamil Nadu, India.

 

MG Rajanandh
Department of Pharmacy Practice, SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur, Chennai 603 203, Tamil Nadu, India.

Please see the book here:-https://doi.org/10.9734/bpi/psnid/v2/3531 

Tuesday, 14 January 2025

Advancements in Therapeutic Drug Monitoring: Integrating Pharmacokinetics, Pharmacodynamics, and Bayesian Approaches for Personalised Medicine | Chapter 6 | Pharmaceutical Research: Recent Advances and Trends Vol. 9

 

Therapeutic drug monitoring (TDM) is a critical process in clinical pharmacology that involves measuring drug concentrations in biological fluids to optimize drug dosage and ensure efficacy while avoiding toxicity. By incorporating pharmacokinetics (PK) and pharmacodynamics (PD) principles, TDM allows for individualized therapy, particularly for drugs with narrow therapeutic indices. Recent advancements, including population pharmacokinetic approaches and Bayesian estimation, have enhanced the precision of TDM. This review highlights the evolution of TDM, its role in optimizing patient outcomes, and emerging techniques such as pharmacodynamic monitoring to further individualize and refine therapeutic regimens.

 

Author(s)details:-

 

V. Himabindu
Department of Pharmaceutics, Anurag Pharmacy College (Affiliated to JNTUH, Hyderabad), Kodad, Telangana, India.

 

G. Sangeetha Roy
Department of Pharmacy Practice, Anurag Pharmacy College (Affiliated to JNTUH, Hyderabad), Kodad, Telangana, India.

 

Please See the book here :-  https://doi.org/10.9734/bpi/prrat/v9/3134

Wednesday, 31 May 2023

The Influence of Amiodarone Complexation with 2-Hydroxypropyl- β -Cyclodextrin in Oral Matrix Tablets Delivery: In vitro and In vivo Evaluation | Chapter 2 | Progress in Chemical Science Research Vol. 9

 The present work is engaging attention the new synthesized and distinguished three component ion-exchanger. Inorganic cation-exchanger have drawn the attention to their discrimination, temperature, warm and chemical stabilities. The most warm and chemical properties concerning this material is prepared by intermixing answers of sodium molybdate (0.1 M), sodium arsenate (0.1 M) and antimony(III) chloride (0.1 M) solution indifferent volume percentages at pH-1. All of the samples' Ion-exchange capacities were assessed utilizing a column method. For in-depth reasonings, the chosen sample was synthesised in large quantities. Its ion-exchange competency of synthesized material for Na+ has happened found expected 2.30 meq/g. The loss of weight and change in colour of the ion-exchanger was noticed in each case and ion-exchange capacity was contingent upon column arrangement. Antimony(III) molybdoarsenate is good ion-exchange capacity and is resistant up to a fairly extreme heat, and fairly resistant in different sour, basic and organic news. The prepared material was characterised utilizing a variety of limits, including FTIR, TGA curve, X-ray dissemination, pH titration, Kd values, thermal & synthetic stabilities, and other studies. The attained binary and water softening separations for differing analytical practical uses have dressed as a demonstration of the synthesised ion- exchanger.

Author(s) Details:

Andreea Creteanu,
Department of Pharmaceutical Technology, Faculty of Pharmacy, Grigore T. Popa University of Medicine and Pharmacy of Iasi, 16th Universitatii St., 700115, Iasi, Romania.

Daniela Pamfil,
Physical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, Romania.

Cornelia Vasile,
Physical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, Romania.

Alina Ghilan,
Physical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, Romania.

Gladiola Tantaru,
Department of Analytical Chemistry, Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy, 16th University St., 700115, Iasi, Romania.

Please see the link here: https://stm.bookpi.org/PCSR-V9/article/view/10696

The Influence of Amiodarone Complexation with 2-Hydroxypropyl- β -Cyclodextrin in Oral Matrix Tablets Delivery: In vitro and In vivo Evaluation | Chapter 2 | Progress in Chemical Science Research Vol. 9

 The aims of this study were to improve both the solubility of the amiodarone hydrochloride (AMD) and its controlled release from the inclusion complexes with 2-hydroxypropyl- β-cyclodextrin (HP- β-CD).The complexation with cyclodextrins (CDs) is a method to optimize the therapeutic performance of the insoluble drugs, including AMD. The inclusion complexes were prepared by co-precipitation and freeze-drying. The solubility enhancement of AMD/HP- β-CD inclusion complexes increase by 4–22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS), zeta-potential (ZP) analysis, scanning electron microscopy (SEM) and differential scanning calorimetry (DSC).

The obtained inclusion complexes (AMD/HP- β-CD) showed an increase in solubility by more than 200%.

Two kinds of formulations have been tested namely of AMD/HP- β-CD inclusion complexes both as powdered form and as matrix tablets containing Kollidon®SR (KOL), Chitosan (CHT) and one containing only pure AMD as a control sample. The kinetics of AMD release form the two kinds of formulations was evaluated by in vitro and in vivo studies. The active substance release was followed by in vitro release testing and the results were analyzed by fitting into four representative mathematical models for the modified release oral formulations. The release of the active substance from the matrix modified tablets is dependent on its solubility degree in the dissolution medium as well as on the composition of the matrix forming polymers. It was found that both formulations showed superior pharmacokinetic performance by improving both loading and release properties in respect with those of the pure low soluble AMD drug.

In vitro kinetic study reveals a complex mechanism of release which occurred in three steps, the first one is attributed to a burst effect and the other two to different bondings existing in inclusion complexes. Two factors have been calculated to assess the release profile of amiodarone: f1 - the similarity factor and f2 - the difference factor. Akaike index and the correlation coefficient were the criteria used for selecting the model that most faithfully depicted the release profile of each studied formulation.

In vivo tests on complexed aminodarone loaded in matrix tablets containing KOL and CHT revealed a multiple (at least two) peaks release diagram because of both structure of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).


Author(s) Details:

Andreea Creteanu,
Department of Pharmaceutical Technology, Faculty of Pharmacy, Grigore T. Popa University of Medicine and Pharmacy of Iasi, 16th Universitatii St., 700115, Iasi, Romania.

Daniela Pamfil,
Physical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, Romania.

Cornelia Vasile,
Physical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, Romania.

Alina Ghilan,
Physical Chemistry of Polymers Department, Petru Poni Institute of Macromolecular Chemistry, 41A Gr. Ghica Voda Alley, RO700487, Iasi, Romania.

Gladiola Tantaru,
Department of Analytical Chemistry, Faculty of Pharmacy, “Grigore T. Popa” University of Medicine and Pharmacy, 16th University St., 700115, Iasi, Romania.

Please see the link here: https://stm.bookpi.org/PCSR-V9/article/view/10696

Saturday, 25 February 2023

Therapeutic Drug Monitoring of Gentamicin in a Patient with Delayed Wound Healing | Chapter 6 | Perspective of Recent Advances in Medical Research Vol. 12

 Gentamicin, secondhand for the treatment of weighty gram-negative contaminations, has a narrow therapeutic index. This property can lead to various side effects, accordingly, therapeutic drug listening (TDM) is important in gentamicin therapy.This division aims to report the pharmacokinetics of gentamicin when using a previously-daily drug regimen.The patient, a 78-period-old male, weighed 78 kg and was 1.75 m tall. He was introduced into the hospital accompanying a wound infection provoked by chronic appendage ischaemia. A once-daily drug of gentamicin (360 mg by infusion over 30 record) in combination accompanying flucloxacillin was prescribed to this patient. A gentamicin ancestry sample was taken every day for four days: Day 1 = 1.4 mg/L, Day 2 = 2.1 mg/L, Day 3 = 2.1 mg/L, Day 4 = 1.6 mg/L. The patient’s antitoxin creatinine was 88 µmol/L during the four days. To decide the dosage and break for gentamicin administration, the Hartford nomogram was working. A once-day-to-day dosing regimen of gentamicin can bring about the clinical and bacteriological cure of contamination. In addition, the Hartford nomogram is a reliable finish for keeping path of gentamicin's once-daily application schedule.

Author(s) Details:

Saeed Fahad Algahtani,
Department of Clinical Pharmacy, Infectious Disease Pharmacist, Prince Sultan Armed Forces Hospital In Madinah, Saudi Arabia.

Fahad M. Alqahtani,
Drug Information and Poisoning Center, Al Kharj Military Industries Corporation Hospital, Saudi Arabia.

Mohammed Qahl,
Department of Pharmacy, Northern Area Armed Forces Hospital, Saudi Arabia.

Please see the link here: https://stm.bookpi.org/PRAMR-V12/article/view/9660

Tuesday, 20 December 2022

A Rare Association of Skin Adverse Reaction to Phenytoin| Chapter 8 | Current Innovations in Medicine and Medical Science Vol. 10

 Phenytoin is a usually used anticonvulsant drug in children and persons for tonic clonic and biased seizures with common aftereffects like nausea, stomach pain, loss of appetite, wax hypertrophy etc. We encountered a patient 34-year-traditional male who bestowed with history of individual episode of convulsion, for that he was prescribed Tab Phenytoin 100mg double daily by oral route. After 15 days he grown rash over trunk which contaminate the whole carcass in two days associated with itching and climbing. There was no familial or personal history of drug aversion or skin conditions. Physical examination revealed diversified, purpuric macules and papules mainly on the body with scaling. Patient was acknowledged and subjected to investigations, that showed common report. Tab Phenytoin was withdrawn and Tab Prednisolone 40mg orally day-to-day was given and tapered by 10mg already in 15 days during that the lesions slowly showed bettering. Symptoms resolved completely in 2 weeks following in position or time phenytoin withdrawal and no adverse follow-up reported. Thus the same case presentation exhibits a rare antagonistic effect of phenytoin on skin.


Author(s) Details:

S. Suma,
Saveetha Medical College and Hospital, Chennai, Tamil Nadu, India.

K. Tejashwini,
Cognizant Technology Solutions, Mysore, Karnataka, India.

V. Hari Prasad,
Department of Forensic Medicine, Panimalar Medical College and Hospital, Chennai, India.

Please see the link here: https://stm.bookpi.org/CIMMS-V10/article/view/8868

Thursday, 24 November 2022

Comparison of Bioavailability and Pharmacokinetic of Two Formulations of Metformin 850 mg Tablets in Healthy Albanian Volunteers| Chapter 8 | Challenges and Advances in Pharmaceutical Research Vol. 9

 Aim: The aim concerning this study was to equate the bioavailability and pharmacokinetics of two formulations of metformin 850 mg tablets: GLUCOPHAGE® from Merck Santè laboratories (remark product) and METFORMINE from Profarma (test device) in healthy Albanian volunteers.Methods: An open label, randomized, two-ending, two-way crossover study was acted in twenty healthy signs up for a single 850 mg shot of metformin tablets. Pharmacokinetic parameters in the way that maximum plasma aggregation (Cmax), the area under the curve limited to a particular time (AUC0-14h), the field under the curve to infinite occasion (AUC0-∞), and the time to reach the maximum red body fluid concentration (Tmax) were persistent. The formulations were considered bioequivalent if the mathematical mean ratios of ln-transformed Cmax and AUC0-∞ principles were within the similarity range of 80%-125%.Results: Two Way ANOVA analysis of the ln-converted Cmax and AUC0-∞ indicated that nobody of the effects checked (formulation, ending, within and between-subject variances and continue) was statistically significant. The bioequivalence study results accompanied 90% confidence of breaks (90 % CI) for pharmacokinetic parameters like Cmax (91.8-115.6 %); AUC0-14 (90.4-109.2 %) AUC0-∞ (90.1-109.1%) and that were within the range of 0.80-1.25. A p advantage of less than 0.05 was deliberate statistically significant.Conclusion: The fruit METFORMINE (produced by Profarma Sh.a) is bioequivalent and, therefore, adequately interchangeable concerning AUC0-∞ and Cmax when compared accompanying the reference crop (GLUCOPHAGE®).

Author(s) Details:

Eva Troja,
University of Medicine, Albania.

Please see the link here: https://stm.bookpi.org/CAPR-V9/article/view/8678

Tuesday, 11 October 2022

Ion-pair HPLC Method for the Quantification of Metformin in Human Plasma and Its Application | Chapter 1 | Challenges and Advances in Pharmaceutical Research Vol. 7

The purpose of this work is to develop and validate a traditional reverse phase column-based, ion-pairing HPLC-UV technique for the detection of metformin in human plasma.

Between November 2014 and February 2015, the Department of Biomedical Sciences at the University of Medicine's "Mother Tereza" hospital centre undertook this experimental investigation.

The method used in this investigation to identify metformin was ion-pair separation followed by UV detection on plasma samples that had been deproteinized and dichloromethane washed. An analytical LiChrocart® 100 RP 18 (125 x 4.0mm i.d., 5 m particle size) C18 column was used to perform the separation. At an isocratic flow rate of 1.25 mL/minute, sodium dodecyl sulphate (0.3%) and 10 mM sodium phosphate buffer (pH=6.0; 32.5:67.5, v/v) were pumped as the mobile phase. Quantification was carried out at 236 nm using a UV/Vis DAD. For metformin in plasma concentration ranges of 50–1600 ng/mL, the calibration curves were linear (r > 0.9998). With a minimal detection limit of 18 ng/ml, the test enables the measurement of metformin for therapeutic drug monitoring. The inter-day and intra-day assay coefficients of variation fell within clinically significant limits. For all three of the plasma quality control concentrations that were looked at, absolute recovery was reported to be better than 90%. The suggested method for measuring metformin in human plasma was discovered to be quick, exact, and accurate. This method was successfully applied to an oral dosage pharmacokinetic study in humans.

Author(s) Details:

Eva Troja,
Profarma SH.A. Pharmaceutical Industry, Tirana, Albania.

Leonard Deda,
Department of Biomedical Sciences, Faculty of Medicine, University of Medicine, Tirana, Albania.

Gëzim Boçari,
Department of Biomedical Sciences, Faculty of Medicine, University of Medicine, Tirana, Albania.

Please see the link here: https://stm.bookpi.org/CAPR-V7/article/view/8364

Friday, 27 May 2022

Determination of Clinical Pharmacokinetics of Quinine and its Relationship with Treatment Outcomes in Children, Pregnant Women, and Elderly Patients| Chapter 11 | Challenges and Advances in Pharmaceutical Research Vol.3

The study looked at existing data on quinine pharmacokinetics in children, pregnant women, and the elderly, identified factors that influence quinine pharmacokinetics, and looked at the relationship between quinine pharmacokinetics and treatment outcomes (therapeutic and safety) for various dosage regimens.

Web of Sciences, Cochrane Library, Scopus, and PubMed were the databases utilised in this systematic search for relevant research papers published up to October 2020 using the given search parameters. Quinine pharmacokinetics were found to be impacted by the severity of illness, administration methods, and nutritional status in these susceptible individuals. The recommended doses for both simple and severe malaria are often sufficient for the elderly and children with uncomplicated malaria. Dose changes may be essential in pregnant women with both simple and severe malaria, as well as children with complex malaria. In these vulnerable patient groups, pharmacokinetic studies with large sample numbers and a revision of the MIC (minimum inhibitory concentration) should be considered.

Author(s) Details:

Teerachat Saeheng,
Center of Excellence in Pharmacology and Molecular Biology of Malaria and Cholangiocarcinoma, Chulabhorn International College, Thammasat University, Rangsit Campus, 99 Moo 18 Phaholyothin Road, Klong Luang District, Pathumthani 12121, Thailand.

Kesara Na-Bangchang,
Center of Excellence in Pharmacology and Molecular Biology of Malaria and Cholangiocarcinoma, Chulabhorn International College, Thammasat University, Rangsit Campus, 99 Moo 18 Phaholyothin Road, Klong Luang District, Pathumthani 12121, Thailand and Drug Discovery and Development Center, Office of Advanced Science and Technology, Thammasat University, Thailand.

Please see the link here: https://stm.bookpi.org/CAPRV-3/article/view/6951

Development of a Validated Chromatographic Method for Determination of Repaglinide from in vivo Study Samples for Pharmacokinetic Application| Chapter 2 | Challenges and Advances in Pharmaceutical Research Vol.3

The goal of the research was to create a simple and sensitive bioanalytical technique for detecting Repaglinide in rabbit plasma for pharmacokinetic studies. The technique was developed utilising a C18 (2) analytical column (5, 2504.6 mm) and a mobile phase of Acetonitrile:0.05 percent Trifluroacetic acid in water (55:45, v/v) at a flow rate of 1 mL/min in RP-HPLC. With suitable system suitability conditions, the retention times of Repaglinide and Rabeprazole were determined to be 4.3 and 5.1 minutes, respectively. The method is linear (r2=0.9987) for a concentration range of 10 to 1000 ng/mL. The accuracy (98.17 percent), intra-, and inter-day precision (2.9 percent), recovery (101.212.19%), and process efficiency (99.773.74%) were all good, with no matrix influence. In bench-top, short-term, and long-term stability analyses, the analyte in samples was shown to be stable for up to 6 hours, 3 freeze-thaw cycles, and not more than 2 months. The pharmacokinetic parameters (Cmax-139.33 ng/mL; Tmax-0.763 h; KE-0.540 h-1; Ka-2.548 h-1; T1/2-1.22 h; AUC0--378.1 ng*h/mL; AUMC0--874.67 ng*h2/mL; MRT-2.32 h; Vd-18.69 L; CLT-10.6 L/h) were determined from time-dependent plasma concentration For the pharmacokinetic evaluation of Repaglinide in rabbit, the established bioanalytical approach proved selective and sensitive.

Author(s) Details:

Raja Navamanisubramanian,
Crescent School of Pharmacy, BSACIST, Vandalur, Chennai, India.

Sabitha Panchagiri,
Department of Pharmacy Practice, Sri Ramachandra Faculty of Pharmacy, SRIHER, Chennai, India.

Raghunandan Nerella,
Department of Pharmaceutical Chemistry, Talla Padmavathi College of Pharmacy, Warangal, India.

Shanmuganathan Seetharaman,
Department of Pharmaceutics, Sri Ramachandra Faculty of Pharmacy, SRIHER, Chennai, India.

Please see the link here: https://stm.bookpi.org/CAPRV-3/article/view/6942

Thursday, 3 March 2022

The Individualized Management Approach for Acute Poisoning: A Review | Chapter 2 | Current Aspects in Pharmaceutical Research and Development Vol.9

 Acute poisoning is a common occurrence that demands quick treatment decisions in order to achieve the best potential outcome. The only way to get those results is to take an individualised strategy. Promoting awareness among healthcare professionals dealing with acute poisoning about the importance of pharmacokinetics and adhering to certain criteria when considering interventions like activated charcoal, antidotes, or specific investigations could help them improve their risk assessment and management strategies. The purpose of this review is to discuss the most important aspects to consider when creating a personalised care plan for poisoning victims. This review was based on relevant publications discovered through a PubMed search. The review takes into account our perspectives as specialists from the Drug and Poison Information Center at King Saud University (KSU) (DPIC).

Author(s) Details:

Muneera Al-Jelaify,
Pharmacy Services, King Khalid University Hospital, King Saud University Medical City, Riyadh, Saudi Arabia and Pediatric Intensive Care Unit, Pediatrics Department, King Khalid University Hospital, King Saud University Medical City, Riyadh, Saudi Arabia.


Suliman Al Homidah,
Pharmacy Services, King Khalid University Hospital, King Saud University Medical City, Riyadh, Saudi Arabia.

Please see the link here: https://stm.bookpi.org/CAPRD-V9/article/view/5962

Saturday, 4 July 2020

Development of Validated LC-MS/MS Method for Pharmacokinetic and Bioequivalence Studies of Azelastine in Korean Healthy Volunteers | Chapter 5 | Current Topics in Medicine and Medical Research Vol. 1

The pharmacokinetic (PK) and bioequivalence (BE) studies of two formulations of azelastine (AZ) was carried out in 18 healthy male Korean volunteers according to a randomized crossover-design and were performed by a new validated liquid chromatography coupled to tandem mass spectrometry (LCMS/MS) method for quantitative analysis of plasma AZ. Subjects were given single dose of 2 tablets of 1 mg AZ of each formulation with 240 ml of water to subjects on 2 treatment days separated by one week washout period. After dosing, serial blood samples were collected for a period of 96 hours. AZ and the clomipramine (IS) were separated using a mobile phase of acetonitrile-5 mM NH4AC (8:2, v/v, pH=6.4) with flow rate of 0.25 ml/min over Luna C18 column. Analysis required 0.2 ml of plasma and involved a solid extraction with an Oasis HLB cartridge by on-line clean-up extraction automation system and then directly injected into HPLC with an API 3000 MS system by multiple reactions monitoring (MRM) mode. Several PK parameters (including AUC0-t, AUC0-infinity, Cmax, Tmax, T1/2 and Ke) were determined from the plasma concentration of AZ of both formulations. The AUC and Cmax was tested for BE after log-transformation of the data. The ionization was optimized using ESI (+) and selectivity was achieved by MS-MS analysis, m/z 112.0 and m/z 86.1 for AZ and IS, respectively. The calibration curves with r2>0.999 were linear over a working range of 20∼2000 pg/ml. No endogenous compounds were found to interfere with the analysis. The inter- and intra-day accuracy was in the ranges of 89.9∼109.3% and precision of inter- and intra-day expressed as relative standard deviation were 2.73∼8.79 %. No significant difference was found based on ANOVA; 90% confidance intervals (91.77∼101.94% for AUC0-t; 90.44∼ 106.27% for AUC0-infinity; 92.22∼108.57% for Cmax) for the test and reference drugs were found within FDA guideline of 80∼125%. Based on these statistical considerations, it was concluded that test drug was bioequivalent to the reference drug and therefore, may be interchangeably in the management of allergic or bronchial asthma and prophylaxis of mucositis due to cancer chemoradiotherapy. This validated method was found to be good performance on PK and BE studies for AZ. (Cancer Prev Res 12, 84-91, 2007). 

Author (s)  Details

Professor Ju-Seop Kang,
Department of Pharmacology and Clinical Pharmacology Laboratory, College of Medicine, Hanyang University, Seoul 133-791, Korea.

View Book :- http://bp.bookpi.org/index.php/bpi/catalog/book/195

Modern Methods for Analysis of Antiepileptic Drugs in the Biological Fluids for Pharmacokinetics, Bioequivalence and Therapeutic Drug Monitoring Studies: Advanced Research | Chapter 4 | Current Topics in Medicine and Medical Research Vol. 1

Epilepsy is a chronic disease occurring in approximately 1.0% of the world’s population. About 30% of the epileptic patients treated with available antiepileptic drugs (AEDs) continue to have seizures and are considered therapy-resistant or refractory patients. The ultimate goal for the use of AEDs is complete cessation of seizures without side effects. Because of a narrow therapeutic index of AEDs, a complete understanding of its clinical pharmacokinetics is essential for understanding of the pharmacodynamics of these drugs. These drug concentrations in biological fluids serve as surrogate markers and can be used to guide or target drug dosing. Because early studies demonstrated clinical and/or electroencephalographic correlations with serum concentrations of several AEDs, it has been almost 50 years since clinicians started using plasma concentrations of AEDs to optimize pharmacotherapy in patients with epilepsy. Therefore, validated analytical method for concentrations of AEDs in biological fluids is a necessity in order to explore pharmacokinetics, bioequivalence and Therapeutic Drug Monitoring (TDM) in various clinical situations. There are hundreds of published articles on the analysis of specific AEDs by a wide variety of analytical methods in biological samples have appears over the past decade. This review intends to provide an updated, concise overview on the modern method development for monitoring AEDs for pharmacokinetic studies, bioequivalence and therapeutic drug monitoring. 

Author(s) Details

Professor Ju-Seop Kang,
Department of Pharmacology and Clinical Pharmacology Laboratory, College of Medicine, Hanyang University, Seoul 133-791,

View Book :- http://bp.bookpi.org/index.php/bpi/catalog/book/195