Quantification of Metformin in Human Urine by Using Ion-pair HPLC Method| Chapter 2 | Medicine and Medical Research: New Perspectives Vol. 2

 

The aim of this study was to develop and validate a selective and sensitive ion-pairing HPLC–UV method for the determination of metformin in human urine using a conventional reversed-phase column. Urine provides a non-invasive sample collection method, and the determination of drug levels in urine is comparatively less complex than in plasma and other body fluids. The bioanalytical method was carried out using an RP-C18 column (250×4.0 mm; 5µm). A mobile phase consisting of acetonitrile and 10 mM sodium phosphate buffer (pH=6.0, 30:70 v/v) and sodium dodecyl sulfate (0.3%) was pumped at an isocratic flow rate of 1.00 mL/minute and quantification was achieved at 236 nm using a UV/VIS DAD. The applicability of the method was confirmed in a study of urinary excretion of metformin by healthy volunteers after oral administration of commercially available tablets. The calibration curves were linear (r2 >0.999) in the concentration ranges of 62.5–2000 µg/mL for metformin in urine. LOD and LOQ were found to be 12 µg/mL and 35 µg/mL, respectively. The method was found to be rapid, precise, and accurate for quantification of metformin in human urine. The study illustrates the characteristics of drug excretion at a single dose of metformin in healthy subjects. Drug excretion is in the trend of increase and accumulation, but the discharge rate is not constant, the accumulative urine drug method can indirectly reflect the metabolic process of the drug in the body. This method was successfully applied to a pharmacokinetic study of humans through oral administration.

 

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.

 

Please see the book here:- https://doi.org/10.9734/bpi/mmrnp/v2/1340

Bioequivalence Assessment of Two Metformin Tablet Formulations Based on Urinary Excretion Data | Chapter 6 | Pharmaceutical Science: New Insights and Developments Vol. 6

Metformin is an oral antihyperglycemic agent that has been widely used in the management of type 2 diabetes mellitus for decades. Metformin is slowly absorbed after oral administration, and about 60% of an oral dose is excreted in the urine as unchanged drug within 24 h. The aim of the present study was to assess the bioequivalence of two metformin tablet formulations available in the Albanian market (product R as reference formulation and product T as test formulation).

 

The bioequivalence study was performed in eighteen healthy volunteers in a two-treatment, open, crossover design. A single oral dose (tablet containing 850 mg of metformin) of each product was administered with one-week washout period. Urinary concentrations of metformin were measured by high-performance liquid chromatography (HPLC) method, and pharmacokinetic parameters were estimated by urinary excretion data. The bioequivalence was determined by the following parameters: the cumulative amount of metformin excreted in the urine, the total amount of metformin excreted in the urine and the maximum urinary excretion rate of metformin.  Various pharmacokinetic parameters like peak excretion rate [(dDU/dt)max], time for peak excretion rate (tmax), cumulative amount (Dcum0-24), total amount of drug recovered from urine (Dcum0-\(\infty\)), elimination half-life (t1/2), and terminal elimination rate constant (kel), were calculated for both the formulations. Student’s t-test (paired) at a 5% level of significance was used for testing the differences between the mean values obtained from two treatments using statistical software STATA 13. Pharmacokinetic parameters generated for the two treatments were also compared for significant differences using ANOVA.

 

The average cumulative amounts of metformin excreted in urine after administration of Formulation R and Formulation T were found to be 346.3 mg (40.74% of dose) and 358.7 mg (42.2% of dose), respectively. The urinary excretion profiles of metformin up to 24 h for both formulations were found to be similar. Statistical comparison (90% confidence intervals of ratio) of pharmacokinetic parameters were in compliance with the international standards, indicating that products R and T can be considered bioequivalents and therefore interchangeable. The study also recommends conducting bioequivalence evaluations for other key medications listed in the national reimbursement list.

Author(s) Details

Eva Troja
Profarma Company, Albania.

 

Please see the book here:- https://doi.org/10.9734/bpi/psnid/v6/5695

Effect of Metformin (MET) in Protection against Oxidative Stress and Pancreatic Damage Using an Animal Model | Chapter 6 | Pharmaceutical Science: New Insights and Developments Vol. 5

Aim: The present study investigated the effects of metformin (MET) in protection against oxidative stress and pancreatic damage using an animal model, to assess the effect of metformin on oxidative stress in vivo and in vitro.

 

Introduction: Diabetes mellitus is a worldwide health problem that has a deleterious impact on life expectancy and quality. People with diabetes have a higher oxidation state, which is detrimental to homeostasis. Numerous tissues have demonstrated the anti-oxidant qualities of metformin. An oral medication for diabetes called metformin aids in blood sugar regulation.

 

Methods: This study investigated the effect of metformin on total antioxidant markers in the serum and pancreatic tissue of Alloxan-induced diabetic rats. Diabetic rats were randomised into five groups for treatment and received metformin (100,200,300 mg/kg) orally once daily for four weeks. The antioxidant potential of evaluated total antioxidant status (TAOS) in vivo and through DPPH (1,1-diphenyl-2-picryl-hydrazyl) scavenging assay at 517 nm in vitro.

 

Results: A Considerable drop in elevated blood glucose level was observed in the alloxan-induced diabetic. At a dose of 100,200,300mg/kg demonstrated increase significantly improvement rate percentage in (M100, M200, M300) were (40.701 %),(48.063%) and (48.101%) respectively after end of treatment compared to diabetic group that decrease (-243.340%), TAOS were significantly increased in treated group than diabetic group" p= 0.000* ".The percentage of improvement rate elevation in treatment M100, M200, and M300 was (133.202 %,148.433% and 194.358%) respectively, compared with diabetic, while that percentage was decreased (-65.677%). Also, it improved pancreas histopathology compared to the diabetic control group it improved pancreas histopathology compared to the diabetic control group Antioxidant activity using DPPH was found to increase in a concentration-time-dependent manner IC₅₀ of metformin (498.0 µg/ml), while ascorbic acid IC50 (µg/ml 29.62).

 

Conclusions: In "alloxan-induced diabetic rats", metformin provides "protective actions" against free radicals and oxidative stress, as well as improving pancreas tissue histology and lowering blood glucose levels.

 

Author (s) Details

Abeer Mansour Abdel Rasool
Department of Pharmacology, Collage of Pharmacy, University of Nineveh, Iraq.

 

Isam Hamo Mahmood
Department of Pharmacology, AL Noor University Collage, Bartella, Iraq.

 

Please see the book here:- https://doi.org/10.9734/bpi/psnid/v5/1665

Assessment of Bioequivalence Using Urinary Excretion Data: A Review | Chapter 11 | Pharmaceutical Research - Recent Advances and Trends Vol. 2

 

The present study highlights about assessment of bioequivalence using urinary excretion data. A rapid method for assessing the bioavailability of a drug is the use of urinary excretion data. This method is based on the principle that the urinary excretion rate of an unchanged drug is directly proportional to the plasma concentration of the drug. So, bioavailability can be calculated as the ratio of the total amount of unchanged drug in urine after administration of the test (T) and reference (R) formulations. Urine metabolite excretion data are not used to assess bioavailability since the drug undergoes metabolism in the body, anatomically and the rate of metabolism may vary for different reasons. This method applies to drugs that are excreted unchanged in the urine, e.g., some thiazide diuretics, sulfonamides, biguanides and drugs that act on the urinary tract, such as urinary antiseptics (nitrofurantoin and hexamine). It is concluded from this study that the formulations Glucophage and Metformin (tablets 850 mg) exhibit a similar elimination rate, which indicates a similarity in their bioavailability and bioequivalence. Based on this study, some drugs such as metformin can therefore be evaluated to simulate and predict absorption through urinary excretion data. Due to the high invasiveness of bioequivalence/bioavailability conventional studies, the prediction of absorption can be performed using the urinary excretion method. Furthermore, the urinary excretion methodology represents low costs, it is a less invasive method, and its throughput is viable when compared to the conventional method with blood samples.

 

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.

 

Please See the book here :- https://doi.org/10.9734/bpi/prrat/v2/679

Development and Validation of a HPLC Method for the Simultaneous Estimation of Simvastatin and Metformin | Chapter 10 | Advanced Concepts in Pharmaceutical Research Vol. 3

 Simvastatin is individual of the well-known statins that is a HMG-COA reductase inhibitor. Metformin hydrochloride is a well- known spoken antihyperglycemic drug. The present work has created and validated a precise and correct reverse phase liquid chromatographic means for the simultaneous estimation of simvastatin and metformin. This is cause the reversed step HPLC method is ultimate suitable for assessing two together ingredients happening at about the same time. The method was created utilizing a Jasco Auto polltaker HPLC with 50mM Sodium Dihydrogen Phosphate Monohydrate at pH 3.0 and Acetonitrile (30:70 v/v). UV-visible detectors were secondhand for the analysis, and 235 nm was used to monitor the eluents. Simvastatin and metformin were proved to have retention opportunities of 7.650 and 2.858 minutes, respectively. The approach was corroborated in terms of time, robustness, precision, and veracity. The planned method for the simultaneous quantitative perseverance was implemented efficiently.

Author(s) Details:

R. Varade,
Pacific University, Udaipur, Rajasthan, 313024, India.

H. Mishra,
K. J. Somaiya Institute of Engineering and Information Technology, Mumbai, MH, 400022, India.

Please see the link here: https://stm.bookpi.org/ACPR-V3/article/view/12703

Estimation of Metformin Hydrochloride, Gliclazide and Pioglitazone Hydrochloride: A UDDD-HPTLC Densitometry Method Validation Study | Chapter 12 | Novel Aspects on Pharmaceutical Research Vol. 3

 A plain and new UDDD-HPTLC method has happened developed and justified for their estimation of MET, GLZ and PIO all-inclusive and combined dose dosage form. Metformin (MET) is chemically, 1-carbamimidamido-N-N-dimethyl- methanimidamide. It is an oral antagonistic-diabetic drug from the biguanide class. It is the first-line drug for the treatment of type-2 diabetes, specifically in overweight and corpulent people and those accompanying normal sort function and evidences suggest possibly the best choice for people as political whole with heart attack.The  chromatographic  separation  of  these  drugs  was  completed activity  on  precoated  TLC  plates  silica  gel  60F254by  two  mobile steps consisting of Ammonium Sulphate: Methanol: Acetonitrile: Water (4:3:2:1) for MET and PIO and Toluene: Ethyl Acetate: Formic Acid (6:4:0.5) for GLZ individually for ideal separation and good judgment. The densitometric detection and calculation were carried out at 237 nm for MET and 200 nm for GLZ and PIO. The confirmation parameters were rigidly followed as per the ICH directions.Chromatographic separation of the standard answer of MET, GLZ and was performed. Briefly, the spot of the standard answer was applied on TLC plates. The TLC plates were developed by uninterrupted ascending growth by using miscellaneous solvents in the way that acetone, benzene, chloroform, ethyl acetate, intoxicating and toluene. The linearity range was got at 3000-8000ng/spot, 360-960 ng/spot, 90-240 ng/spot for MET, GLZ and PIO with r2value>0.999. The different parameters to a degree precision, reproducibility, strength were efficiently obtained believable. The proposed arrangement was successfully used for simultaneous perseverance of MET, GLZ and PIO in the commercial expression.In simultaneous belief, the different opposition of drugs makes it more burdensome to develop and confirm any chromatographic method. In comparison to HPLC, the submitted UDDD-HPTLC method is novel, less high-priced, simpler, smart, and more flexible. This method can be secondhand for routine quality control study because it authorizes simultaneous guess of all API on a single TLC plate accompanying a single application.

Author(s) Details:

Rajesh Varade,
Pacific University, Udaipur, Rajasthan-313024, India.

Harsha Mishra,
Pacific University, Udaipur, Rajasthan-313024, India and K. J. Somaiya Institute of Engineering and Information Technology, Mumbai, Mh-400022, India.

Please see the link here: https://stm.bookpi.org/NAPR-V3/article/view/10887

Reducing Heart Failure Risk in Diabetes Mellitus: Review of Therapeutics | Chapter 12 | Current Overview on Pharmaceutical Science Vol. 8

 Diabetes mellitus (DM) and heart attack (HF) are closely connected: patients accompanying diabetes are more likely to evolve HF, and those with HF are more likely to cultivate diabetes. Diabetic patients have an raised risk of developing HF by way of the abnormal cardiac management of glucose and free greasy acids, and because of the effect of the metabolic derangements of diabetes on the cardiovascular method. When the two diseases are thought-out separately, HF has a much bad prognosis than diabetes mellitus; so, treatment of HF is a arrangement in this patient group. Many drugs are immediately available to help public with diabetes achieve glycemic control. However, as the administration of diabetes becomes made-to-order, the next challenge will be to recognize therapeutic plans that will not only achieve and maintain glycemic control, but will also reverse existent problems. Given the high predominance of HF in DM, there is an important need to advance this field in order to recognize robust designs that will not only enhance general results in subjects accompanying DM and HF, but will also reduce the trend of developing HF initially. Newer therapies, in the way that sodium-glucose transport protein-2 inhibitors (SGLT-2 I) and sacubitril or valsartan, have proved promise in lowering the risk of heart attack in diabetics. This review will summarize novel cure for lowering the risk of HF in diabetic patients.

Author(s) Details:

Shreeharsh Godbole,
Department of Nephrology, Dr. D. Y. Patil Medical College, Hospital & Research Centre, Pune, Maharashtra, India.

Shreerang Godbole,
Department of Endocrinology, Institute for Treatment, Research in Diabetes and Endocrinology, Pune, Maharashtra, India.

Please see the link here: https://stm.bookpi.org/COPS-V8/article/view/9873

Pharmacogenetics of Allelic Variants of CYP2C9 and Clinical Implications among Mexican Patients with Diabetes Mellitus Type 2 Undergoing Treatment with Glibenclamide and Metformin | Chapter 7 | Current Overview on Pharmaceutical Science Vol. 7

 Diabetes  Mellitus Type 2 (DMT2) is a important public health concern in Mexico as well as everywhere.  The majority of Mexican cases with diabetes mellitus type 2 (DMT2) (67.9-85.0%) are prescribed sulphonylureas (SUs), that are metabolized by cytochrome P450 2C9. The polymorphisms of CYP2C9 are thought to be being the reason for the extensive variability about SU responses. The current member aims todescribe CYP2C9 polymorphisms (*2, *3 and IVS8-109T) within a sample of Mexican patients accompanying DMT2, while suggesting the potential clinical implications in conditions of glibenclamide response instability. The study included 248 patients accompanying DMT2 who initially agreed to be studied, those contained in the study were treated accompanying glibenclamide (n=11), glibenclamide combined with metformin (n=112) or metformin (n=76), and were afterward genotyped using a reverse transcription all-inclusive polymerase chain reaction (PCR), endpoint allelic bias and PCR amplifying enzymatic restriction fragment long variety. Glibenclamide significantly reduced the pre?prandial sweet liquid (P<0.01) and the percentage of glycated red body fluid (%HbA1c; P<0.01) for IVS8-109A>T compared with linked glibenclamide and metformin treatment. Concerning the various situations with respect to the different genotypes, the percentages acquired were as follows: Glibenclamide A/A, HbA1c<6.5=33.3%; glibenclamide + metformin A/A, HbA1c<6.5=24.6%; gliben-clamide A/T, HbA1c<6.5=33.3%; glibenclamide + metformin A/T, HbA1c<6.5=25%; glibenclamide T/T, HbA1c<6.5=100%; and glibenclamide + metformin T/T, HbA1c<6.5=12.5%. Overall, these judgments show that, while genetically customised prescriptions remain a good goal for increasing healing success, neither allelic modifications nor dosages evidenced a strong equating with biomarker levels within the intentional population; thus, more exact experimental and practical investigations are needed.

Author(s) Details:

Patricia Cuautle Rodríguez,
Department of Pharmacology, School of Medicine, National University of Mexico, Mexico City, Mexico.

Nidia Samara Rodríguez-Rivera,
Departamento de Farmacología, Facultad de Medicina, UNAM, Mexico City, Mexico.

Fernando de Andrés Segura,
Department of Analytical Chemistry and Food Technology, Faculty of Pharmacy, University of Castilla-La Mancha, Albacete, Spain.

Adrián LLerena,
Institute of Biosanitary Research of Extremadura and of the Clinical Research Center of the University Hospital of Badajoz, Spain.

Fernando Castillo-Nájera,
Centro de Salud T-III Portales, Servicios de Salud, Gobierno de la Ciudad de México, México.

Juan Molina-Guarneros,
Departamento de Farmacología, Facultad de Medicina, UNAM, Mexico City, Mexico.

Please see the link here: https://stm.bookpi.org/COPS-V7/article/view/9699

AMP-kinase is the Main Target of Metformin in Regulating Type 2 Diabetes | Chapter 8 | Research Highlights in Disease and Health Research Vol. 2

 AMP-mobilized protein kinase (AMPK) is a major cellular manager that is activated when natural energy levels are low and provokes glucose rude answer in skeletal muscle, oily acid oxidation in adipose and added tissues, and decreases hepatic glucose production. The incitement of AMPK's metabolic effects, particularly the metabolic shift from fat combination to fat oxidation and its capability to promote power glucose uptake, proper to be beneficial in things with insulin resistance and/or type 2 diabetes. Since, AMPK is a principal regulator of energy equilibrium, it has been considered expected an important therapeutic aim for controlling human ailments including the metabolic syndrome. AMPK equips to be the key target substance causing chemicals to split into simpler substances of metformin to reduce plasma sweet liquid levels. Also, thiazolidinediones (TZDs) and 2-deoxyglucose have been shown expected indirect activators of AMPK. In this review, we discuss only the likely underlying devices of metformin's miraculous strategies (in threatening plasma glucose level) at the microscopic level, which will also specify an updated reference for the clinicians and analysts.F

Author(s) Details:

Rashidul Haque,
Department of Nephrology, Government Medical College & Superspeciality Hospital, Aurangabad, Maharashtra, India.

Sultana Rajia,
Department of Nephrology, Government Medical College & Superspeciality Hospital, Aurangabad, Maharashtra, India

Please see the link here: https://stm.bookpi.org/RHDHR-V2/article/view/9616

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

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

Determining the Factors Associated with Prognosis of Non-Alcoholic Fatty Liver Disease | Chapter 19 | Recent Developments in Medicine and Medical Research Vol. 10

 Non-alcoholic fatty liver disease (NAFLD) is a condition that occurs at the intersection of obesity, metabolic syndrome, and liver failure. Metformin's role in individuals with non-alcoholic fatty liver disease has been explored in recent studies. This finding hasn't been looked into on a global basis, nor has it been looked into in diverse ethnic groups.

The goal of this study is to determine the risk variables related with the prognosis of nonalcoholic fatty liver disease in a cohort of patients in Palestine's southern West Bank.

Methods: A retrospective cohort research included 300 NAFLD patients who visited the Hebron Governmental Hospital's internal medicine department between October 2017 and September 2018. This study included 233 patients who had been diagnosed with non-alcoholic fatty liver disease. Patients' profiles were combed through for recent lab test results, comorbidity, and medication history. SPSS V20 was used to analyse the data. The non-alcoholic fatty liver disease fibrosis score calculator was used to calculate the liver fibrosis score.

The study included 230 non-alcoholic fatty liver disease patients (58.6% of whom were females) with an average age of 54.78 (12.27) years. Nearly 65.5 percent of these individuals have a BMI of more over 30 kg/m2. When compared to non-alcoholic fatty liver disease individuals who are not diabetic, 62.25 percent of the 58 diabetes patients in this study had a liver fibrosis score > 0.676. Diabetes and fibrosis score had a statistically significant link (=0.000). There was also a significant link between hyperlipidemia and non-alcoholic fatty liver disease patients' fibrosis score (=0.023), as well as a significant relationship between fibrosis score and hypertension (=0.000). In the same study, there was a significant association between NAFLD patients on statin therapy and those who were not on statin therapy, with a value of 0.015. Metformin did not appear to have a significant association between non-alcoholic fatty liver disease patients who used it and those who did not.

Conclusion: Diabetes, hypertension, hyperlipidemia, and statin use were all linked to a poor prognosis for NAFLD. All NAFLD patients must maintain strict hypertension and dyslipidemia management.

Author(S) Details

Muamar M. A. Shaheen
Department of Clinical Pharmacy, Hebron University, Hebron, P.O. Box 40, Palestine.

Mohanad Saleh
Department of Clinical Pharmacy, Hebron University, Hebron, P.O. Box 40, Palestine and Respiratory Department and Attending Internist at Intensive Care Unit Respiratory Department, Al-Ahli Hospital, Hebron, Palestine.

Deema Sider
Department of Clinical Pharmacy, Hebron University, Hebron, P.O. Box 40, Palestine.

Reem A. l. Natsheh
Department of Clinical Pharmacy, Hebron University, Hebron, P.O. Box 40, Palestine.

Raghad Dweik
Department of Clinical Pharmacy, Hebron University, Hebron, P.O. Box 40, Palestine.

View Book:- https://stm.bookpi.org/RDMMR-V10/article/view/4641

Determining the Efficacy and Safety of Teneligliptin and Metformin Versus Glimepiride and Metformin in Patients of Type-2 Diabetes Mellitus Uncontrolled with Monotherapy | Chapter 6 | Technological Innovation in Pharmaceutical Research Vol. 10

 Type 2 diabetes mellitus is one of the most common non-communicable diseases, with both short- and long-term effects.

Material and Methods: The study included 60 patients, divided into two groups of 30 patients each. Teneligliptin 10 mg once a day and metformin 500 mg twice a day after meals were administered to Group 1 participants for 12 weeks. Glimepiride 1 mg once a day and metformin 500 mg twice a day after meals were administered to Group 2 patients for 12 weeks. Following the signed consent, the patient's medical history, clinical examination, and biochemical tests such as FBG, PPBG, HbA1c, and lipid profile were performed. FBG and PPBG were repeated every week for a total of 12 weeks. HbA1c and lipid profiles were measured at the start and end of the trial.

The change in FBG was greater in group 1 than in group 2. When comparing the drop in PPBG in patients in groups 1 and 2 there was a highly significant difference in group 1. HbA1c, total cholesterol, triglyceride levels, HDL, and LDL levels all changed more in group 1 than in group 2.

Conclusion: When compared to Glimepiride and metformin, teneligliptin and metformin resulted in a larger improvement in glycaemic and lipid profiles. Teneligliptin is therefore more effective than glimepiride.

Author (S) Details

Nitika Hans
Department of Pharmacology, Government Medical College, Amritsar, Punjab, India.

View Book :- https://stm.bookpi.org/TIPR-V10/article/view/2843

An Overview on Polycystic Ovary Syndrome (PCOS) | Chapter 2 | Technological Innovation in Pharmaceutical Research Vol. 6

 PCOS, or polycystic ovarian syndrome, is one of the most common female endocrine disorders, affecting 6-15 percent of women. PCOS causes hormonal imbalances and metabolism issues in women, which can have an impact on their overall health and attractiveness. Although insulin resistance is not invariably present, androgen excess and insulin resistance are now acknowledged to be responsible for much of the phenotypic appearance. It's marked by an irregular menstrual cycle and acne, and it's linked to type 2 diabetes and cardiovascular disease. A prospective window of opportunity to avoid the risk of related consequences exists when PCOS is managed effectively. The treatment aims to address (IR), hyperandrogenism's consequences, irregular menstruation, and infertility in general. The genesis, pathophysiology, diagnosis, and therapy of polycystic ovarian syndrome are the focus of this review paper.

Author (s) Details

Dr. C. Muhas
Department of Pharmacy Practice, KTN College of Pharmacy, Chalavara, Palakkad, Kerala, India.

Dr. K. M. Nishad
Department of Pharmaceutics, Jamia Salafiya Pharmacy College, Pulikkal, Kerala, India.

Prof (Dr), P. P. Naseef
Department of Pharmaceutics, Moulana College of Pharmacy, Perintalmanna, Kerala, India.

K. Abdul Vajid
Department of Pharmaceutics, Moulana College of Pharmacy, Perintalmanna, Kerala, India.

View Book :- https://stm.bookpi.org/TIPR-V6/article/view/1702

A Brief Discussion on High Glucose with Insulin Induces Cell Cycle Progression and Activation of Oncogenic Signaling of Bladder Epithelial Cells Cotreated with Metformin and Pioglitazone | Chapter 9 | Challenges in Disease and Health Research Vol. 6

 Metformin and pioglitazone are two common oral hypoglycemic agents used to treat diabetes. According to new research, these drugs may contribute to bladder cancer. There is substantial evidence linking diabetes to breast, colon, liver, and pancreatic cancer. The purpose of this study was to look into the molecular mechanisms that underpin the effects of metformin and pioglitazone on bladder epithelial carcinogenesis in type 2 diabetes. Human bladder epithelial cells (HBlEpC) were treated with metformin or pioglitazone in the presence of high glucose and insulin levels. The 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay and a cell viability and proliferation assay were used to assess cell viability and proliferation. The bromodeoxyuridine incorporation assay was used to examine cell cycle regulatory factors and oncogene expression, while western blotting was used to examine cell cycle regulatory factors and oncogene expression. Metformin and pioglitazone inhibited cell viability in a concentration- and time-dependent manner, which was reversed by high glucose with or without insulin. In HBlEpC co-treated with pioglitazone and metformin, prolonged exposure to high glucose and insulin levels increased cyclin D, cyclin-dependent kinase 4 (Cdk4), and Cdk2 expression while suppressing cyclin-dependent kinase inhibitors p21 and p15/16. Under high stress, the tumor suppressor proteins p53 and cav-1 were downregulated, while the oncogenic protein c-myc was upregulated. Supplementation of glucose and insulin in HBlEpC patients receiving pioglitazone and metformin. In drug-treated cells, prolonged exposure to high glucose with or without insulin decreased the expression of B cell lymphoma 2-associated X (Bax) and failed to increase the expression of extracellular signal-regulated kinase (ERK) and p38 mitogen-activated protein kinase (p38MAPK). These findings imply that hyperglycemic and insulinemic conditions promote cell cycle progression and oncogenic signaling in drug-treated bladder epithelial cells, and that uncontrolled hyperglycemia and hyperinsulinemia are likely to be more cancer risk factors than diabetes drugs. Furthermore, our findings shed light on how these conditions enhance the carcinogenic effect in drug-treated bladder epithelial cells and suggest that uncontrolled hyperglycemia and hyperinsulinemia in diabetics are likely more dangerous than TZD administration or PPAR stimulation in a clinical setting.

Author (S) Details

Daejin Kim
Department of Anatomy, Inje University College of Medicine, Busan 614-735, Republic of Korea.

Byul-Nim Ahn
T2B Infrastructure Center for Ocular Disease, Inje University Busan Paik Hospital, Busan, Republic of Korea.

Yeong Seok Kim
Department of Anatomy, Inje University College of Medicine, Busan 614-735, Republic of Korea.

Dae Young Hur
Department of Anatomy, Inje University College of Medicine, Busan 614-735, Republic of Korea.

Jae Wook Yang
T2B Infrastructure Center for Ocular Disease, Inje University Busan Paik Hospital, Busan, Republic of Korea and Department of Ophthalmology, Inje University College of Medicine, Inje University Busan Paik Hospital, Busan, Republic of Korea.

Ga Bin Park
Department of Biochemistry, Kosin University College of Medicine, Busan 49267, Republic of Korea.

Jung Eun Jang
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

Eun Ju Lee
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

Min Jeong Kwon
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

Tae Nyun Kim
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

Mi Kyung Kim
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

Jeong Hyun Park
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

Byoung Doo Rhee
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

Soon Hee Lee
Department of Internal Medicine, College of Medicine, Inje University, Busan, Republic of Korea.

View Book :- https://stm.bookpi.org/CDHR-V6/article/view/1669

Computational Studies and Geometry Optimization of Antidiabetic Drug, N,N-dimethylimido Dicarbo Nimidic Diamide | Chapter 9 | Current Perspectives on Chemical Sciences Vol. 10

 Metformin (N,N-dimethylimidodicarbonimidicdiamide) is an oral antidiabetic drug of the biguanide class. It is the first-line treatment for persons with type 2 diabetes who are overweight or obese and have normal renal function. ACD/I-lab was used to perform in silico nuclear resonance magnetic spectroscopy of metformin. Chemical shifts of methyl protons 6 and 7 occurred as a singlet at 3.03 ppm, while chemical shifts of amino protons 3, 5, 10 and 11 appeared as a singlet at positions 10.16, 6.66, 8.57, and 8.38 ppm, respectively. Chemical shifts of 158.20 and 159.10 ppm were seen in the imine carbons, whereas chemical alterations of 38.77 ppm were seen in the methyl carbons at positions 6 and 7. Argus lab software was used to undertake all conformational analysis (geometry optimization) studies on a window-based computer. The metformin structure was created by Argus Lab, and the semi-empirical Parametric Method 3 was used to minimise it (PM3). The least potential energy was calculated using the geometry convergence algorithm in the Argus lab programme. Surfaces were used to map the density of the highest occupied molecular orbital (HOMO), the lowest unoccupied molecular orbital (LUMO), and electrostatic potentials (ESP). The minimal potential energy estimated with Argus lab software's geometry convergence function was 41.537840 kcal/mol. The molecule's most stable configuration is this energy minimum.

Author (s) Details

I. E. Otuokere
Department of Chemistry, Michael Okpara University of Agriculture, Nigeria.

C. O. Alisa
Department of Chemistry, Federal University of Technology, Nigeria.

View Book :- https://stm.bookpi.org/CPCS-V10/article/view/1230

Development of RP-HPLC Method for Simultaneous Estimation of Metformin and Pioglitazone in Pharmaceutical Formulation | Chapter 11 | Technological Innovation in Pharmaceutical Research Vol. 3

A fast, selective, speedy, accurate, and cost-effective reverse phase HPLC technique has been devised for the simultaneous quantification of metformin and pioglitazone from pharmaceutical dosage forms. The experiment was carried out on a phenomenex C18 column (25 cm x 4.6 mm i.d., 5 mm i.d., 5 mm i.d., 5 mm i.d., 5 mm i.d., 5 mm i.d., 5 mm i.d., phosphate buffer phase containing acetonitrile (adjusted to pH 5.0 using orthophosphoric acid) at a flow rate of 1. ml/min (50:50 v/v). The wavelength of detection was 258 nm. As a measure of internal control, The drug etoricoxib was utilized. The retention times for paracetamol, aceclofenac, and etoricoxib were 4.75, 6.44, and 6.44, respectively. 8.83 minutes and 8.83 minutes, respectively. In terms of precision, linearity, detection limit, and detection limit, The established method was validated in terms of quantitation and solution stability. These medications' dosage forms in combination dosage forms can be calculated using the provided procedure. Raw materials, formulations, and dissolution tests can all be checked using the current RPHPLC equipment.

Author (s) Details

S. Alexandar
Department of Pharmaceutical Chemistry, Vinayaka Mission’s College of Pharmacy, Vinayaka Missions Research Foundation (Deemed to be University), Yercaud Main Road, Salem – 636008, India.

View Book :- https://stm.bookpi.org/TIPR-V3/article/view/1154

Metformin as an Adjuvant Therapy Attenuates Dextran Sulphate Sodium-induced Acute Colitis in Rats: A Recent Study | Chapter 3 | Technological Innovation in Pharmaceutical Research Vol. 3

 The goal of this study is to see if patients with inflammatory bowel diseases (IBDs) are resistant to routine treatment. Immunosuppressive medications like sirolimus (SIR) and tacrolimus (TAC) have been proven to work. However, they have adverse effects that limit their use. Metformin (MET) is an anti-diabetic drug. medication, having anti-inflammatory properties that are promising. As a result, the goal of this research was to confirm the effect of the In the treatment of experimentally produced pain, concurrent administration of MET with SIR or TAC colitis is a disease that affects the digestive system. The Dextran sulphate (DSS) induced colitis model was used in this study.

Methodology: For 9 days, colitis was induced by giving 5 percent DSS in water twice a day via oral gavage. MET 200 mg/kg can be used alone or in conjunction with SIR. On day 7, 1 mg/kg or TAC 1 mg/kg was begun and continued for a total of 12 days. After that, histological and immunohistochemical staining of distal colon tissues was performed. The levels of pro-inflammatory cytokines such as tumour necrosis factor-alpha (TNF-), interleukin (IL)-1, IL-6, and IL-17A were then evaluated in tissue homogenates. The effects of DSS and the levels of all proinflammatory cytokines were dramatically reduced by MET, SIR, or TAC. Furthermore, MET enhances the effects of SIR and TAC.

Conclusion: When it came to DSS-induced colitis, MET exhibited a significant anti-inflammatory effect. As a result, it could be a viable adjuvant therapy for IBD management. Inhibition of NF-B activation was one of the mechanisms behind the impact. This study can be utilized as a foundation for pilot clinical trials to examine the effect of MET on IBD, given the size of its efficacy and its safety profile. The findings of this study, however, need to be further confirmed and translated into clinical consequences.

Author (s) Details

Rania M. Magadmi
Pharmacology Department, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia.

Fahad H. Aljahdali
Pharmacology Department, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia and Compliance Management at Directorate of Health Affairs in Jeddah City, Jeddah, Saudi Arabia.

Mustafa Alsawy
Department of Histology and Cytology, Faculty of Medicine, Al-Azhar University, Egypt.

Ahmed S. Ali
Pharmacology Department, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia and Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Egypt.

Fatemah O. Kamel
Pharmacology Department, Faculty of Medicine, King Abdulaziz University, Jeddah, Saudi Arabia.

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The Improvement in Cardiovascular Risk Markers with Glimepiride in Pre-diabetic non-obese Subjects: Similar to Obese Cohort Treated with Metformin | Chapter 13 | Highlights on Medicine and Medical Research Vol. 5

 Background: Over a 5- to 9-year period (mean, 7.20.2), we found that glimepiride was more effective than metformin in delaying the progression from pre-diabetes to type 2 diabetes in non-obese subjects. Metformin was the first-line treatment for newly diagnosed diabetics who were overweight. Furthermore, neither group experienced any deaths or adverse cardiovascular conditions, which could be due to beneficial improvements in lipids and cardiovascular surrogate markers. The impact of interventions on lipids and cardiovascular surrogate markers, on the other hand, was not documented.

Prior to intervention, cardiovascular risk factors such as lipid fractions, such as serum Total cholesterol (TC), Triglyceride (TG), Low Density Lipoprotein Cholesterol (LDLC), High Density Lipoprotein Cholesterol (HDLC), and other markers, such as homocysteine (HomC), highly sensitive C-Reactive Protein (CRP), Fibrinogen (FIBR), and Plasminogen Activator Inhibitor1 (PAI1).

Subjects and Methods: The sample included 18 non-obese subjects, 10 men and 8 women between the ages of 27 and 78, and 20 obese subjects, 10 men and 10 women between the ages of 32 and 81, who had pre-diabetes (fasting plasma glucose of 100 to 125 mg/dl and/or HbA1c of 5.7 to 6.4 percent). The research lasted 5 to 9 years (mean: 7.20.2). Glimepiride was given to non-obese subjects, while metformin was given to obese subjects. At each visit during the study, subjects were counselled on lifestyle intervention (appropriate diet and exercise).Individual lipids and CV markers were compared at the start of the study, six months later, and at the end of the study for each group, as well as between groups for baseline and end-of-study levels.

Results: In the glimepiride group, significant improvements in all parameters occurred after treatment (Post Rx) at 6 months and were sustained until the end of the study. HbA1C ( percent ): 6.2 0.2, 5.5 0.1*, 5.7 0.1*; TC (mg/dl): 212 15, 174 13*, 178 14*; TG (mg/dl): 202 32, 162 28*, 178 14*; LD HDLC was not affected in any way. Obese people who were given metformin experienced similar improvements. There were no major differences between the two groups at the start, 6 months, or end of the research.

Conclusion: Glimepiride is equally efficient in enhancing lipid profiles and cardiovascular surrogate markers in nonobese subjects with Pre diabetes as metformin is in obese subjects, explaining similar cardiovascular results in both classes.

Author (s) Details

Reshma Esmail
Mount Saint Mary College, Los Angeles, California, USA.

Udaya Manohar Kabadi
University of Iowa, Iowa City, Iowa, USA and Des Moines University, Des Moines, Iowa, USA.

View Book :- https://stm.bookpi.org/HMMR-V5/article/view/700