Comparative Bioavailability of Metformin Hydrochloride Oral Solution Versus Metformin Hydrochloride Tablets in Fasting Mexican Healthy Volunteers

Garza-Ocañas, Lourdes; González-Canudas, Jorge; O, Eduardo Tamez-de la; Badillo-Castañeda, Christian Tadeo; Meza, Marco Vinicio Gómez; Romero-Antonio, Yulia; Molina-Pérez, Aarón; Amador-Hernández, Ana Gabriela

doi:10.1007/s12325-018-0853-3

Cited by 10 publications

(8 citation statements)

References 4 publications

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“…hydrochloride, chemically N,Ndimethylimidodicarbionimidic diamide hydrochloride (1,1diamethylbiguanide hydrochloride), belongs to the 'biguanide' class as shown in Figure 1 3,4 . After oral administration, metformin is mainly absorbed from the upper small intestine, and it undergoes limited systemic absorption (absolute bioavailability is about 50 to 60 %) with a half-life of about 3 h. Therefore, repeated administration of the conventional metformin hydrochloride tablets is needed for effective treatment [4][5][6] . 7 .…”

Section: Metforminmentioning

confidence: 99%

“…Following the expiry of the innovator drug patent (Glucophage®) in 2001, many generic pharmaceutical companies have manufactured oral metformin hydrochloride tablets and joined the market. 2,5 Such introduction of generic drug products from multiple sources into the markets improved availability and access to this life-saving drug especially in developing countries 8 . Moreover, these generic products are marketed with lower price and associated with public health cost reduction 9,10 .…”

Section: Metforminmentioning

confidence: 99%

“…Metformin hydrochloride reference standard solution was prepared in different concentrations (3,4,5,6, and 7 µg/ml) using phosphate buffer (pH = 6.8) medium. Their absorbances were measured at  max of 233 nm using a UV-Visible spectrophotometer (Double beam UV-Visible Spectrophotometer, T92+, PG instrument limited).…”

Section: Construction Of Calibration Curve For Metformin Hydrochloridementioning

confidence: 99%

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Comparative In Vitro Evaluation Of Different Brands Of Metformin Hydrochloride Film Coated Tablets Marketed In Addis Ababa, Ethiopia

Abatea

Temesgen

Nigatu

2020

Asian J Pharm Res Dev

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Metformin hydrochloride is a biguanide class of drug widely used to treat Type 2 diabetes mellitus. Its oral bioavailability is about 50 to 60 % with a half-life of about 3 h. This study focused on evaluation and comparison of the physicochemical properties of different brands of metformin hydrochloride (500mg) film coated tablets available in drug retail outlets in Addis Ababa, Ethiopia. Some different in vitro tests including hardness, weight variation, disintegration time, dissolution study, and assay were conducted as per United States Pharmacopeia. To compare dissolution profiles of the generic products against the innovator product (product A), a model independent method, similarity factor (f2), was also used. Weight variation result showed that all brand fall within the 5% limit from the average which is acceptable. Disintegration time of less than 15 minutes was observed for all brands. The in vitro drug release study results for the products ranged between 82 and 93% release within 30 minutes which is above 80% limit as per the United States Pharmacopeia requirement. The similarity f2 values for generic products ranged from 53 to 75%. Furthermore, assay value of the studied brands varied from 95.60 to 104.37% which was within standard limit (95-105%). It can be concluded that all brands of metformin hydrochloride tablets met pharmacopoeial specification for the tested parameters of physicochemical properties like weight variation, hardness of tablets, disintegration time, drug release study and assay.

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Section: Metforminmentioning

confidence: 99%

Section: Metforminmentioning

confidence: 99%

Section: Construction Of Calibration Curve For Metformin Hydrochloridementioning

confidence: 99%

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Comparative In Vitro Evaluation Of Different Brands Of Metformin Hydrochloride Film Coated Tablets Marketed In Addis Ababa, Ethiopia

Abatea

Temesgen

Nigatu

2020

Asian J Pharm Res Dev

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“… ( a ) Predicted plasma concentrations of metformin following different dosage of human. ( b ) Predicted (line) and observed (point) relationship between metformin dose and dose/AUC for different dose; shaded area, 0.5–2.0 folds of prediction; observations were cited from [ 13 , 15 , 16 , 19 , 20 , 27 , 68 , 69 , 84 , 88 , 89 , 90 , 91 , 92 , 93 , 94 , 95 , 96 , 97 , 98 , 99 , 100 , 101 , 102 , 103 , 104 , 105 , 106 , 107 , 108 , 109 , 110 , 111 , 112 , 113 ]. ( c ) Visual predictive checks (VPCs) of metformin plasma concentrations to time in 500 mg oral administration for human; solid line, the 50th percentiles; dashed lines, the 5 and 95th percentiles of the simulated populations; the shaded area, 90% confidence intervals of the simulated concentrations of the 5, 50 and 95th percentiles; and the point, observations, which were cited from [ 27 , 69 , 91 , 93 , 97 , 114 ].…”

Section: Figurementioning

confidence: 99%

A Whole-Body Physiologically Based Pharmacokinetic Model Characterizing Interplay of OCTs and MATEs in Intestine, Liver and Kidney to Predict Drug-Drug Interactions of Metformin with Perpetrators

Yang

Zhang

et al. 2021

Pharmaceutics

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Transmembrane transport of metformin is highly controlled by transporters including organic cation transporters (OCTs), plasma membrane monoamine transporter (PMAT), and multidrug/toxin extrusions (MATEs). Hepatic OCT1, intestinal OCT3, renal OCT2 on tubule basolateral membrane, and MATE1/2-K on tubule apical membrane coordinately work to control metformin disposition. Drug–drug interactions (DDIs) of metformin occur when co-administrated with perpetrators via inhibiting OCTs or MATEs. We aimed to develop a whole-body physiologically based pharmacokinetic (PBPK) model characterizing interplay of OCTs and MATEs in the intestine, liver, and kidney to predict metformin DDIs with cimetidine, pyrimethamine, trimethoprim, ondansetron, rabeprazole, and verapamil. Simulations showed that co-administration of perpetrators increased plasma exposures to metformin, which were consistent with clinic observations. Sensitivity analysis demonstrated that contributions of the tested factors to metformin DDI with cimetidine are gastrointestinal transit rate > inhibition of renal OCT2 ≈ inhibition of renal MATEs > inhibition of intestinal OCT3 > intestinal pH > inhibition of hepatic OCT1. Individual contributions of transporters to metformin disposition are renal OCT2 ≈ renal MATEs > intestinal OCT3 > hepatic OCT1 > intestinal PMAT. In conclusion, DDIs of metformin with perpetrators are attributed to integrated effects of inhibitions of these transporters.

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“…Therefore, repeated administration of the conventional metformin hydrochloride tablets is mandatory for effective treatment. [10][11][12] According to Biopharmaceutical Classi cation System (BCS), metformin is classi ed under class III drugs. 13 For such drugs, permeability is the rate-limiting step for drug absorption.…”

Section: Introductionmentioning

confidence: 99%

Physicochemical Quality of Metformin Hydrochloride tablet Brands available in Jimma Town, South west, Ethiopia

Mekonnen¹,

Bekele²,

Suleiman³

et al. 2021

Preprint

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Introduction: Metformin hydrochloride, classified under the class of biguanide, is an oral anti-diabetic agent used in type 2 diabetes mellitus patients. According to the biopharmaceutical classification system, metformin is classified as a Class III drug. This study aims to compare the quality of metformin hydrochloride 500 mg tablets available in Jimma town.Methods: The physical characteristic, packaging and labeling information of samples were evaluated according to the WHO guideline. In-vitro tests such as weight variation, friability, dissolution rate, and assay were performed on six brands of metformin hydrochloride tablets available in Jimma town following method outlined in USP. Experimental data were analyzed using SPSS- 20 and one-way ANOVA. To compare the dissolution profiles of the generic products with innovator product, a model-independent approach, similarity factor (f2), difference factor (f1) and dissolution efficiency (DE) were used.Results: All the tested brands were in line with the WHO specifications for physical characteristics, packaging and labeling of pharmaceuticals. Insumet had percent weight deviation more than 5% and failed to comply with the USP specification for uniformity of weight. Statistically, all brands had significant difference in their mean weight variation (P<0.001). The assay results range from 95.21% to 99.61% showing that all the brands met the USP requirement. Moreover, a single point dissolution test results of the brands ranged from 85.4% to 96.7% showing compliance to USP specification. Conclusion: No brand showed any sign of counterfeit and only Insumet failed to comply with the USP specification for weight variation test. All brands complied with the United States Pharmacopeia specification for the friability, assay and single point dissolution test. Furthermore, the model-independent approach and dissolution efficiency revealed that all the brands were interchangeable with the comparator product.

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Comparative Bioavailability of Metformin Hydrochloride Oral Solution Versus Metformin Hydrochloride Tablets in Fasting Mexican Healthy Volunteers

Cited by 10 publications

References 4 publications

Comparative In Vitro Evaluation Of Different Brands Of Metformin Hydrochloride Film Coated Tablets Marketed In Addis Ababa, Ethiopia

Comparative In Vitro Evaluation Of Different Brands Of Metformin Hydrochloride Film Coated Tablets Marketed In Addis Ababa, Ethiopia

A Whole-Body Physiologically Based Pharmacokinetic Model Characterizing Interplay of OCTs and MATEs in Intestine, Liver and Kidney to Predict Drug-Drug Interactions of Metformin with Perpetrators

Physicochemical Quality of Metformin Hydrochloride tablet Brands available in Jimma Town, South west, Ethiopia

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