Formulation of zein based compression coated floating tablets for enhanced gastric retention and tunable drug release

Raza, Ali; Shen, Naian; Li, Juehong; Chen, Yunsu; Wang, Jin‐Ye

doi:10.1016/j.ejps.2019.01.025

Cited by 38 publications

(18 citation statements)

References 37 publications

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“…During the period of study, volunteers were allowed free access to only water. 18 The study was fully explained to the volunteers before starting the study, and the informed consent forms were signed by each volunteer as per declarations of Helsinki (Brazil 2013).…”

Section: In Vivo Studies In Vivo Radiographic Studymentioning

confidence: 99%

<p>Promising Swellable Floating Bupropion Tablets: Formulation, in vitro/in vivo Evaluation and Comparative Pharmacokinetic Study in Human Volunteers</p>

Teaima¹,

Hamid²,

Shoman³

et al. 2020

DDDT

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Purpose Bupropion is an antidepressant drug that facilitates weight loss. It is a highly water-soluble drug that needs multiple dosing, so it is considered a potential candidate for oral controlled-release dosage form. The aim of this research was to formulate and evaluate satiety-inducing swellable floating bupropion tablets by direct compression targeting depression associated with eating disorders. Various combinations of natural and semi-synthetic hydrogels were selected to achieve maximum swelling and remaining buoyant in the stomach. This synergistically enhances weight loss by increasing satiety. Methods An I-optimal mixture design was conducted to establish the optimal quantitative composition of tablets. Friability, floating lag time, swelling index after 4 and 8 hours, along with the percent of bupropion released at 1 and 8 hours were selected as dependent variables. The optimized formulation was characterized by physicochemical properties, thermal stability, and chemical interaction. In vivo radiographic evaluation of gastric residence besides, the oral bioavailability relative to marketed Wellbutrin ® sustained-release tablets were investigated using human volunteers. Results The optimized formulation (73.3 mg xanthan, 120 mg glucomannan, 8.4 mg tamarind kernel powder, 78.3 mg HPMC K15M) was achieved with the overall desirability equals 0.782. In vivo radiographic study showed that formulation was retained for >8 hours in the stomach. Compared with the marketed BUP tablets, the C max was almost the same with a significant increase (p =0.004) for T max . Conclusion Using combinations of these hydrogels would be promising gastroretentive delivery systems in the control of bupropion rate release with enhanced floating and swelling features.

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Section: In Vivo Studies In Vivo Radiographic Studymentioning

confidence: 99%

<p>Promising Swellable Floating Bupropion Tablets: Formulation, in vitro/in vivo Evaluation and Comparative Pharmacokinetic Study in Human Volunteers</p>

Teaima¹,

Hamid²,

Shoman³

et al. 2020

DDDT

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“…CO 2 causes the floatation of the tablet and helps maintain tablet buoyancy by getting trapped in the hydrocolloid matrix of the system. It also influences drug release properties [1,53,103,104]. One disadvantage of effervescent systems is the fact that, unless low-density materials are used, they show long floating lag times if the generation of gas bubbles that will promote buoyancy is not fast enough and are, therefore, under the risk of premature gastric emptying [105].…”

Section: Effervescent Floating Systemsmentioning

confidence: 99%

Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

2021

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There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologies have the potential to achieve retention of the dosage form in the upper gastrointestinal tract (GIT) that can be sufficient to ensure complete solubilisation of the drugs in the stomach fluids, followed by subsequent absorption in the stomach or proximal small intestine. This can be beneficial for drugs that have an “absorption window” or are absorbed to a different extent in various segments of the GIT. Therefore, gastroretentive technologies in tandem with controlled-release strategies could enhance both the therapeutic efficacy of many drugs and improve patient compliance through a reduction in dosing frequency. The paper reviews different gastroretentive drug delivery technologies and controlled-release strategies that can be combined and summarises examples of formulations currently in clinical development and commercially available gastroretentive controlled-release products. The different parameters that need to be considered and monitored during formulation development for these pharmaceutical applications are highlighted.

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“…Tablets with 80 mg weight were prepared using multiple station tablet punching machine equipped with 6 mm concave round die-punch tooling (A.K. Industries, Nakodar, India) [30,31].…”

Section: Preparation Of Core Tablet Of Domperidonementioning

confidence: 99%

Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression Coated Mu-Coadhesive Tablets of Domperidone

Puri¹,

Sharma²,

Kumar³

et al. 2021

Preprint

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Background: Mucoadhesive polymers represent a major part of site-specific and localized retention strategies in oral drug delivery. Present research was designed to synthesize and characterize a novel mucoadhesive carbohydrate polymer (thiolated gum ghatti; TGG) which was further employed to fabricate mucoadhesive tablets of domperidone using an industrially viable compression coating technique. Methods: Thiolation of gum ghatti was achieved by the ester formation (esterification) between hydroxyl group and carboxyl group of gum ghatti and thioglycolic acid. Results: TGG was characterized by various physico-chemical techniques such as FTIR, XRD, SEM and DSC techniques. In rheological studies, the observed viscosities of pure gum-mucin were 45.45 and 71.75 mPas and that of thiolated gum were 78.7 and 112.58 mPas respectively in water and simulated gastric fluid. Signifi-cant increase in viscosity for thiolated gum may be attributed to increased macromolecular interactions responsible for enhanced mucoadhesive potential of thiolated gum. In-silico studies corroborate the role of mucin gum interaction and energetic stabilization for en-hanced mucoadhesion properties of thiolated gum. Ex-vivo mucoadhesion strength of gum ghatti and thiolated gum ghatti coated tablets was found to be ranging between 4.67± 0.79 to 8.99± 0.75 g and 11.76± 1.34 to 18.83± 2.07 g respectively. Conclusion: Thiolated gum ghatti may be regarded as a promising polymer for developing different mucoadhesive drug delivery systems.

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Formulation of zein based compression coated floating tablets for enhanced gastric retention and tunable drug release

Cited by 38 publications

References 37 publications

<p>Promising Swellable Floating Bupropion Tablets: Formulation, in vitro/in vivo Evaluation and Comparative Pharmacokinetic Study in Human Volunteers</p>

<p>Promising Swellable Floating Bupropion Tablets: Formulation, in vitro/in vivo Evaluation and Comparative Pharmacokinetic Study in Human Volunteers</p>

Gastroretentive Technologies in Tandem with Controlled-Release Strategies: A Potent Answer to Oral Drug Bioavailability and Patient Compliance Implications

Synthesis and Characterization of Thiolated Gum Ghatti as a Novel Excipient: Development of Compression Coated Mu-Coadhesive Tablets of Domperidone

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