Bilayer Matrix Tablets for Prolonged Actions of Metformin Hydrochloride and Repaglinide

He, Wei; Huang, Shi-Jing; Zhou, Changyong; Cao, Lin; Yao, Jing; Zhou, Jianping; Wang, Guangji; Yin, Lifang

doi:10.1208/s12249-014-0229-1

Cited by 11 publications

(6 citation statements)

References 33 publications

(37 reference statements)

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“…Formulations F3 and F4 also include NaCMC to granulate the metformin HCl and it contributes to stabilize the gel layer. The presence of NaCMC increased the robustness and resistance of the hydrated gel layer of the matrices [33].…”

Section: Discussionmentioning

confidence: 99%

Controlled Release of Highly Hydrophilic Drugs from Novel Poly(Magnesium Acrylate) Matrix Tablets

et al. 2020

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The potential of a new poly(magnesium acrylate) hydrogel (PAMgA) as a pharmaceutical excipient for the elaboration of matrix tablets for the extended release of highly hydrophilic drugs was evaluated. The polymer was synthetized with two different crosslinking degrees that were characterized by FTIR and DSC. Their acute oral toxicity was determined in a mouse model, showing no toxicity at doses up to 10 g/kg. Matrix tablets were prepared using metformin hydrochloride as a model drug and the mechanisms involved in drug release (swelling and/or erosion) were investigated using biorrelevant media. This new hydrogel effectively controlled the release of small and highly hydrophilic molecules as metformin, when formulated in matrix tablets for oral administration. The rate of metformin release from PAMgA matrices was mainly controlled by its diffusion through the gel layer (Fickian diffusion). The swelling capacity and the erosion of the matrix tablets influenced the metformin release rate, that was slower at pH 6.8, where polymer swelling is more intensive, than in gastric medium, where matrix erosion is slightly more rapid. The crosslinking degree of the polymer significantly influenced its swelling capacity in acid pH, where swelling is moderate, but not in intestinal fluid, where swelling is more intense.

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Section: Discussionmentioning

confidence: 99%

Controlled Release of Highly Hydrophilic Drugs from Novel Poly(Magnesium Acrylate) Matrix Tablets

et al. 2020

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“…On the other hand, the release profiles obtained for tablets 4 and 5 need to be investigated for commercial utilization from the point of view of oral absorbability. He et al [14] revealed that sustained-release tablets containing metformin and repaglinide showed bioavailabilities equal to those of rapid-release tablets in in vivo studies with beagle dogs. Metformin and repaglinide are used for models of water-soluble and poorly water-soluble drug compounds, respectively; the sustained-release tablets exhibited release profiles similar to our data obtained in vitro.…”

Section: Formulation and Characterization Of Controlled-release Table...mentioning

confidence: 99%

“…The hydration rate increases with the amount of hydroxypropyl, which can slowly dissolve in cold water, as it is a viscous solution. By utilizing these characteristics, HPMC was incorporated into the inside of a tablet for sustained-release systems, the efficacy of which was supported by several studies in vitro and in vivo [9,13,14]. However, it has not yet been reported whether the HPMC-containing tablets reached the lower-intestinal sites between the ileum and colon.…”

Section: Introductionmentioning

confidence: 99%

Clinical Demonstrations of Controlled-Release Tablets Constructed by the Combined Usage of Shellac and Hydroxypropyl Methylcellulose

Wakamatsu¹,

Sato²,

Uryu³

et al. 2021

Future Pharmacology

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A new tablet system was examined for an intestinal delivery system using hydroxypropyl methylcellulose (HPMC) and shellac. HPMC was incorporated into the inside of the tablet, and shellac was coated on the surface, which was evaluated for its controlled-release property through several dissolution tests, firstly in vitro and then via two kinds of clinical studies with healthy volunteers. The clinical studies were originally designed by employing X-ray photography for the movements of the tablets in the gastrointestinal tract and an electronical device to easily analyze the absorption profile of glucose, a model compound. It was found that the dissolution of the tablet was strongly suppressed in a simulated gastric fluid (pH 1.2) and subsequently started to disintegrate in a simulated intestinal fluid (pH 6.8). The first human study with X-ray photography revealed that the model tablets could pass through the stomach without disintegrating. The controlled release of the tablets was further confirmed via analyses of the AUC, Cmax, and Tmax for the blood glucose concentration with other volunteers. The AUC and Cmax were significantly reduced by using our system, thus concluding that the delivery system combined with the addition of HPMC and a shellac coating unequivocally leads to controlled release in the human gastrointestinal tract.

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“…7 These formulations were reported to improve the relative bioavailability of REP around 111% to 113% compared to oral bolus. Further, bilayer matrix tablets for prolonged release of metformin hydrochloride and REP, 8 gastro retentive drug delivery of REP through mucoadhesive tablets, 9 floating microspheres, 10,11 mucoadhesive microsphere 12 and mucoadhesive nanoparticles 13 were reported. Yet, those formulations could not overcome the first-pass effect of REP due to GIT is being their common site of administration.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetic Investigation to Study the In Vivo Bioavailability of Thiolated Chitosan Based Repaglinide Buccal Tablets

Navamanisubramanian¹,

Nerella²,

Shanmuganathan

2020

Pharm Sci

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Background: Repaglinide (REP) is an antihyperglycemic drug having low bioavailability due to its extensive first-pass metabolism. The present study aimed to develop and pharmacokinetic investigte the thiolated chitosan (TC) based buccal tablets of REP for improved bioavailability. Methods: TC was prepared by conjugation of L-cysteine with chitosan. The amount of free thiol groups present in TC was determined by UV-spectrophotometry using Ellman’s reagent. TC based REP buccal tablets were prepared by two layers co-compression method and characterized for in vitro and ex vivo parameters. The in vivo performance of prepared REP buccal tablets was assessed by the pharmacokinetic study in New Zealand white rabbits. Results: The prepared TC resulted in 87%w/w yield with 52.3±3.2 μM free thiol functional groups per 10 mg of TC. The prepared formulations have good flow nature and compressibility, acceptable thickness (2.02 to 2.1 mm), weight (60.11 to 61.06 mg), surface pH (6.59 to 6.81) and drug content (98.92 to 101.08 %w/w). The presence of TC significantly improved the mucoadhesion strength, sustained the in vitro release and enhanced the ex vivo permeation of REP buccal tablets. The shelf life of REP buccal tablets was found to be 15.07 months in accelerated storage conditions. The prepared REP buccal tablets (V5) have area under the curve (712.22±15.91 ng/mL/h) and mean residence time (4.66±0.25 h) was 1.89 and 1.83 folds higher than oral bolus respectively. Conclusion: TC based REP buccal tablets are capable of controlled transbuccal release of REP for a prolonged time and have better bioavailability than oral bolus.

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Bilayer Matrix Tablets for Prolonged Actions of Metformin Hydrochloride and Repaglinide

Cited by 11 publications

References 33 publications

Controlled Release of Highly Hydrophilic Drugs from Novel Poly(Magnesium Acrylate) Matrix Tablets

Controlled Release of Highly Hydrophilic Drugs from Novel Poly(Magnesium Acrylate) Matrix Tablets

Clinical Demonstrations of Controlled-Release Tablets Constructed by the Combined Usage of Shellac and Hydroxypropyl Methylcellulose

Pharmacokinetic Investigation to Study the In Vivo Bioavailability of Thiolated Chitosan Based Repaglinide Buccal Tablets

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