Novel self-floating tablet for enhanced oral bioavailability of metformin based on cellulose

Huh, Hyun Wook; Na, Young-Guk; Kang, HeeChol; Kim, Minki; Han, Min-Gu; Pham, Thi Mai Anh; Lee, Hyeonmin; Baek, Jong-Suep; Lee, Hong-Ki; Cho, Cheong-Weon

doi:10.1016/j.ijpharm.2020.120113

Cited by 19 publications

(11 citation statements)

References 46 publications

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“… 2019 ; Wook Huh et al. 2021 ). The in vivo profile showed slower elimination is for metformin administrated in the formulation.…”

Section: Discussionmentioning

confidence: 99%

“…Wook Huh et al. ( 2021 ) evaluated a hollow-core floating tablet (HCFT) based in mixture of hydroxypropyl and microcrystalline cellulose showing a higher bioavailability with the same MRT, approximately 35 h, compared to a commercial metformin tablet. Among the different materials that have been associated to MET for obtaining MET nanoparticles, only PLGA was able to sustain MET plasma concentration over 72 h, with higher AUC and Vz/F.…”

Section: Discussionmentioning

confidence: 99%

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In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model

Pereira

Lima

Silva-Júnior

et al. 2021

Pharmaceutical Biology

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“… 2019 ; Wook Huh et al. 2021 ). The in vivo profile showed slower elimination is for metformin administrated in the formulation.…”

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model

Pereira

Lima

Silva-Júnior

et al. 2021

Pharmaceutical Biology

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“…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%

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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“…This can also increase patient compliance by lowering the frequency of dose; drugs with shorter half-lives can produce a significantly better therapeutic effects. One of the most prevalent types of GRDDS is the floating/pulsatile drug delivery system (FDDS/PDDS), which increases the drug absorption by extending the GRT within the upper GIT (effervescent or non-effervescent) [ 3 , 4 , 5 , 6 ].…”

Section: Introductionmentioning

confidence: 99%

Design and Evaluation of Losartan Potassium Effervescent Floating Matrix Tablets: In Vivo X-ray Imaging and Pharmacokinetic Studies in Albino Rabbits

Rahamathulla

Saisivam²,

Alshetaili

et al. 2021

Polymers

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Losartan potassium (LP) is an angiotensin receptor blocker used to treat hypertension. At higher pH, it shows poor aqueous solubility, which leads to poor bioavailability and lowers its therapeutic effectiveness. The main aim of this research was to develop a direct compressed effervescent floating matrix tablet (EFMT) of LP using hydroxyl propyl methylcellulose 90SH 15,000 (HPMC-90SH 15,000), karaya gum (KG), and an effervescent agent, such as sodium bicarbonate (SB). Therefore, an EFMT has been developed to prolong the stomach residence time (GRT) of a drug to several hours and improve its bioavailability in the stomach region. The blended powder was evaluated for pre-compression characteristics, followed by post-compression characteristics, in vitro floating, water uptake studies, and in vitro studies. The optimized formulation of EFMT was investigated for in vivo buoyancy by X-ray imaging and pharmacokinetic studies in Albino rabbits. The results revealed that the parameters of pre- and post-compression were within the USP limits. All tablets showed good floating capabilities (short floating lag time <1 min and floated for >24 h), good swelling characteristics, and controlled release for over 24 h. The Fourier-transform infrared (FTIR) and differential scanning calorimetry (DSC) spectra showed drug–polymer compatibility. The optimized formulation F3 (HPMC-90SH 15,000-KG) exhibited non-Fickian diffusion and showed 100% drug release at the end of 24 h. In addition, with the optimized formulation F3, we observed that the EFMT floated continuously in the rabbit’s stomach area; thus, the GRT could be extended to more than 12 h. The pharmacokinetic profiling in Albino rabbits revealed that the relative bioavailability of the optimized LP-EFMT was enhanced compared to an oral solution of LP. We conclude that this a potential method for improving the oral bioavailability of LP to treat hypertension effectively.

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Novel self-floating tablet for enhanced oral bioavailability of metformin based on cellulose

Cited by 19 publications

References 46 publications

In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model

In vitro-in vivo availability of metformin hydrochloride-PLGA nanoparticles in diabetic rats in a periodontal disease experimental model

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

Design and Evaluation of Losartan Potassium Effervescent Floating Matrix Tablets: In Vivo X-ray Imaging and Pharmacokinetic Studies in Albino Rabbits

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