An investigation on host-guest complexation of Metformin hydrochloride with hydroxypropyl-α-cyclodextrin for enhanced oral bioavailability

Roselet, S. Lizy; Kumari, J. Prema

doi:10.1016/j.matpr.2019.06.650

Cited by 5 publications

(4 citation statements)

References 15 publications

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“…Its glycemic control is attributed primarily to its ability to suppress hepatic glucose production. − As a hydrophilic molecule, it has high solubility and low intestinal and cell membrane permeability, limiting its absorption and thus affecting oral bioavailability, which ranges from 40 to 60% . Additionally, metformin has a saturable absorption level and an inverse relationship between the dose being ingested by the patient and its absorption rate. , Consequently, due to its low bioavailability, metformin is administered multiple times a day at an average dosage of 500 mg/day (up to 850 mg/day), which may cause many undesirable side effects, such as vomiting, nausea, abdominal discomfort, diarrhea, and headaches. , To address issues with low absorption, different strategies have been developed to enhance metformin’s bioavailability, including a floating cellulose-based hollow-core tablet, a water-in-oil microemulsion system, a hydrogel-forming microneedle platform for transdermal delivery, and complexation with hydroxypropyl-α-cyclodextrin, among others.…”

Section: Introductionmentioning

confidence: 99%

“…7,8 Consequently, due to its low bioavailability, metformin is administered multiple times a day at an average dosage of 500 mg/day (up to 850 mg/day), which may cause many undesirable side effects, such as vomiting, nausea, abdominal discomfort, diarrhea, and headaches. 9,10 To address issues with low absorption, different strategies have been developed to enhance metformin's bioavailability, including a floating cellulose-based hollowcore tablet, 11 a water-in-oil microemulsion system, 12 a hydrogel-forming microneedle platform for transdermal delivery, 13 and complexation with hydroxypropyl-α-cyclodextrin, 14 In this work, we report on a microstirring pill loaded with metformin to enhance the glucose-lowering effect of the drug for the treatment of T2DM. During the past decade, synthetic micromotors have served as highly efficient platforms for active drug delivery, and major developments have led to important progress that could benefit medicine.…”

Section: Introductionmentioning

confidence: 99%

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A Microstirring Oral Pill for Improving the Glucose-Lowering Effect of Metformin

et al. 2023

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Type 2 diabetes mellitus (T2DM) is characterized by hyperglycemia due to persistent insulin resistance, resulting in elevated blood glucose levels. Metformin is the most prescribed oral drug for lowering high blood glucose levels in T2DM patients. However, it is poorly absorbed and has low bioavailability. Here, we introduce magnesium-based microstirrers to a metformin-containing pill matrix to enhance the glucose-lowering effect of metformin. The resulting microstirring pill possesses a built-in mixing capability by creating local fluid transport upon interacting with biological fluid to enable fast pill disintegration and drug release along with accelerated metformin delivery. In vivo glucose tolerance testing using a murine model demonstrates that the metformin microstirring pill significantly improves therapeutic efficacy, lowering blood glucose levels after a meal more rapidly compared to a regular metformin pill without active stirring. As a result, the microstirrers allow for dose sparing, providing effective therapeutic efficacy at a lower drug dosage than passive metformin pills. These encouraging results highlight the versatility of this simple yet elegant microstirring pill technology, which enhances drug absorption after gastrointestinal delivery to improve therapeutic efficacy.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

A Microstirring Oral Pill for Improving the Glucose-Lowering Effect of Metformin

et al. 2023

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“…Los sistemas de indometacina con βCD y 2HP−βCD han sido también estudiados por ITC y espectrofotometría UV-Visible para determinar las constantes de formación de estas interacciones (Hipólito-Nájera et al, 2019). También se ha estudiado la complejación del clorhidrato de metformina con hidroxipropilα-ciclodextrina en estado sólido y líquido con el objetivo de mejorar la biodisponibilidad oral del fármaco (Roselet, 2020). En la mayoría de los estudios se reporta una estequiometría fármaco:CD de 1:1.…”

Section: Introductionunclassified

Estudio de la inclusión de diflunisal en 2-hidroxipropil-β-ciclodextrina

Gómez‐Balderas

Ponce-Pérez

González-Barbosa

et al. 2023

ICBI

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El diflunisal (HDif) es un analgésico y antiinflamatorio no esteroidal, sus efectos terapéuticos resultan de la inhibición en la producción de prostaglandinas. Los complejos de inclusión de antiinflamatorios con 2-hidroxipropil-β-ciclodextrina (2HP−βCD), incrementa la solubilidad del fármaco en agua y reducen efectos secundarios de medicamentos; por ejemplo, en el cyclodexÒ (piroxicam-βCD). En este trabajo se estudió la formación del complejo de diflunisal aniónico (Dif) con 2HP−βCD mediante titulación calorimétrica isotérmica, en agua a 30 ºC y pH neutro. La inclusión es exotérmica (ΔHº = −3.13 kcal/mol), genera entropía (TΔSº = 2.20 kcal/mol) y es espontánea (ΔGº = −5.24 kcal/mol). Además, se realizó el modelado molecular del complejo de inclusión, encontrando que las interacciones tipo van der Waals y los puentes de hidrógeno son responsables de la estabilidad del complejo.

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“…Metformin HCL (metformin), “chemically designated as 1,1-dimethylbiguanide hydrochloride”, is an oral hypoglycemic agent widely used in the treatment of type-2 diabetes mellitus (T2DM), specifically in overweight and obese individuals [ 1 , 2 ]. The hypoglycemic effect of metformin is owing to its ability in the suppression of hepatic glucose production and increases the peripheral sensitivity to insulin with higher safety [ 3 ].…”

Section: Introductionmentioning

confidence: 99%

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

et al. 2020

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Compression of cohesive, poorly compactable, and high-dose metformin hydrochloride into the orally disintegrating tablet (ODT) is challenging. The objective of this study was to develop metformin ODT using the moisture activated dry granulation (MADG) process. There are no reports in the literature regarding the development of ODT based on MADG technology. The feasibility of developing metformin ODT was assessed utilizing a 32 full factorial design to elucidate the influence of water amount (X1) and the amount of pregelatinized starch (PGS; X2) as independent variables on key granules and tablets’ characteristics. The prepared granules and tablets were characterized for granule size, bulk density, flow properties, tablets’ weight variation, breaking force, friability, capping tendency, in vitro and in vivo disintegration, and drug release. Regression analysis showed that X1 and X2 had a significant (p ≤ 0.05) impact on key granules and tablets’ properties with a predominant effect of the water amount. Otherwise, the amount of PGS had a pronounced effect on tablet disintegration. Optimized ODT was found to show better mechanical strength, low friability, and short disintegration time in the oral cavity. Finally, this technique is expected to provide better ODT for many kinds of high-dose drugs that can improve the quality of life of patients.

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An investigation on host-guest complexation of Metformin hydrochloride with hydroxypropyl-α-cyclodextrin for enhanced oral bioavailability

Cited by 5 publications

References 15 publications

A Microstirring Oral Pill for Improving the Glucose-Lowering Effect of Metformin

A Microstirring Oral Pill for Improving the Glucose-Lowering Effect of Metformin

Estudio de la inclusión de diflunisal en 2-hidroxipropil-β-ciclodextrina

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

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