Development of Floating Gastroretentive Drug Delivery System Based on a Novel Excipient for Metformin Hydrochloride Using Mixture Design

Pawar, Rajesh; Jagdale, Swati; Randive, Dheeraj S.

doi:10.22159/ijpps.2020v12i10.38678

Cited by 2 publications

(1 citation statement)

References 32 publications

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“…However, drug bioavailability resulting from this administration mode is about 56%, because part of the active ingredient is lost, being not properly available where it is mostly absorbed, i.e. in the upper gastrointestinal tract [42][43][44][45][46][47][48][49][50][51][52][53][54][55][56][57]. Therefore, controlled release of metformin at its absorption window could be highly beneficial.…”

Section: Introductionmentioning

confidence: 99%

Development of a multi-component gastroretentive expandable drug delivery system (GREDDS) for personalized administration of metformin

Uboldi,

Chiappa,

Rossi

et al. 2023

Expert Opinion on Drug Delivery

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Objectives Efficacy and compliance of type II diabetes treatment would greatly benefit from dosage forms providing controlled release of metformin in the upper gastrointestinal tract. In this respect, the feasibility of a new system ensuring stomach-retention and personalized release of this drug at its absorption window for multiple days was investigated. MethodsThe system proposed comprised of a drug-containing core and a viscoelastic umbrella-like skeleton, which were manufactured by melt-casting and 3D printing. Prototypes, alone or upon assembly and insertion into commercially-available capsules, were characterized for key parameters: thermo-mechanical properties, accelerated stability, degradation, drug release, deployment performance and resistance to simulated gastric contractions.Results Each part of the system was successfully manufactured using purposely-selected materials and the performance of final prototypes matched the desired one. This included: i) easy folding of the skeleton against the core in the collapsed administered shape, ii) rapid recovery of the cumbersome configuration at the target site, even upon storage and iii) prolonged release of metformin.Conclusions Composition, geometry and performance of the system developed in this work were deemed acceptable for stomach retention and prolonged as well as customizable release of metformin at its absorption window, laying promising bases for further development steps.

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Section: Introductionmentioning

confidence: 99%

Development of a multi-component gastroretentive expandable drug delivery system (GREDDS) for personalized administration of metformin

Uboldi,

Chiappa,

Rossi

et al. 2023

Expert Opinion on Drug Delivery

View full text Add to dashboard Cite

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Statistical Design of Experiment-Based Formulation Development and Optimization of Floating Matrix Tablet of Anti-Emetic Drug

DIAS,

BOBDE,

DESAI

2024

Int J App Pharm

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Objective: To employ Design of Experiment (DOE) for designing a floating matrix tablet of Domperidone Maleate (DM) using novel direct compression grade polymer METHOCEL K4M DC2 that offers advantages of extended or sustained release, providing for cost-effective manufacturing. Methods: To prepare floating matrix tablets containing DM, the direct compression method was employed. The tablets were optimised using a 22 Central Composite Design (CCD). Concentration of the sustained release polymer METHOCEL DC2 K4M grade (X1= A) and Concentration of the floating agent potassium bicarbonate (KHCO3) (X2= B) were the independent variables selected whereas floating lag time (Y1), drug release at 1 h (Y2), 4 h (Y3), 6 h (Y4) and 8 h (Y5) were the 5 dependent variables employed in the study design. Fourier Transform Infrared (FTIR) analysis was utilised to analyse drug-excipient compatibility, revealing no discernible interaction, and various mathematical models were employed to study the drug release mechanism. Results: The prepared tablets were evaluated for weight, thickness, hardness, friability, and assay and the results were found to be satisfactory. The optimised formulation predicted by the software was found to have a desirability value of 0.982, containing 60 mg of METHOCEL DC2 K4M and 20 mg of KHCO3, was prepared and evaluated. Predicted and experimental results were found to be comparable for all the responses. All formulations were shown to fit well into Zero-order release kinetics, but the optimised formulation (F4), with R2= 0.9893 and n= 2.2797, exhibited the best fitting in both the Zero-order and Korsmeyers-Peppas model. Conclusion: The study conducted revealed that floating tablets of DM could be developed using KHCO3 as a gas-generating agent with sustained drug release till 14 h using polymer METHOCEL DC2 K4M.

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Development of Floating Gastroretentive Drug Delivery System Based on a Novel Excipient for Metformin Hydrochloride Using Mixture Design

Cited by 2 publications

References 32 publications

Development of a multi-component gastroretentive expandable drug delivery system (GREDDS) for personalized administration of metformin

Development of a multi-component gastroretentive expandable drug delivery system (GREDDS) for personalized administration of metformin

Statistical Design of Experiment-Based Formulation Development and Optimization of Floating Matrix Tablet of Anti-Emetic Drug

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