Raft-forming gastro-retentive formulations based on Centella asiatica extract-solid dispersions for gastric ulcer treatment

Mahattanadul, Sirima; Issarachot, Ousanee; Puttarak, Panupong; Wiwattanapatapee, Ruedeekorn

doi:10.1016/j.ejps.2019.105204

Cited by 31 publications

(31 citation statements)

References 33 publications

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“…Recently, raft-forming systems based on liquid formulations for controlled delivery of herbal medicines to the stomach for treatment of gastric ulcers have attracted increasing attention. The poorly water soluble compounds curcumin and the glycoside-rich centella extract, when incorporated in liquid, raft-forming formulations showed superior curative effect on gastric ulcers compared to unformulated compounds and the anti-ulcer drug, lansoprazole ( Kerdsakundee et al, 2015 , Wannasarit et al, 2020 ). However, the raft-forming liquid dosage forms display several limitations compared with the solid dosage forms including lower stability due to chemical reaction and microbial contamination, more stringent packaging requirements and less convenient portability ( Prajapati et al, 2013 ).…”

Section: Introductionmentioning

confidence: 99%

Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers

Bunlung

Nualnoi

Issarachot

et al. 2021

Saudi Pharmaceutical Journal

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Gastroretentive raft-forming formulations were developed in liquid and chewable tablet dosage forms to achieve prolonged delivery of quercetin in the stomach. The formulations contained a solid dispersion of quercetin and polyvinylpyrrolidone (PVP K 30) at a 1:10 w/w ratio to improve the solubility of the flavonoid. The formulations also contained sodium alginate as a gel forming agent, calcium carbonate as a calcium source and carbon dioxide producer and hydroxypropyl methylcellulose K100M as a drug release retarding polymer. The chewable tablets incorporated mannitol as a diluent. Both liquid and chewable tablet formulations exhibited rapid floating behaviour (lag time < 1 min) and long floating duration (>24 h) in 0.1 N HCl. The optimized liquid formulation showed superior characteristics based on high raft strength (10.4 g) and sustained release of quercetin (93 % over 8 h) whereas the optimized chewable tablet formulation exhibited lower raft strength (7.2 g) and lower drug release (79 % in 8 h). The optimized liquid and chewable tablet formulations were found to induce anti-inflammatory activity in cell culture using RAW 264.7 cells macrophages and enhance the migration of human gastric adenocarcinoma (AGS) epithelial cells in vitro , indicating wound healing potential for treatment of gastric ulcers.

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Section: Introductionmentioning

confidence: 99%

Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers

Bunlung

Nualnoi

Issarachot

et al. 2021

Saudi Pharmaceutical Journal

Self Cite

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“…Wannasarit et al reported the development of a gastroretentive raft-forming system based on Eudragit ® EPO-Centella asiatica extract-solid dispersions containing the poorly soluble asiaticoside and madecassoside which have proven to be effective against gastric ulcers [121,122]. The solid dispersion approach proved to be able to enhance the aqueous solubility of the glycosides, while the presence of HPMC K100M in the raft ensured a sustained release of the compounds over 8 h with the release kinetics and mechanism being controlled by Fickian diffusion for both glycosides.…”

Section: Raft-forming Systemsmentioning

confidence: 99%

“…The solid dispersion approach proved to be able to enhance the aqueous solubility of the glycosides, while the presence of HPMC K100M in the raft ensured a sustained release of the compounds over 8 h with the release kinetics and mechanism being controlled by Fickian diffusion for both glycosides. Furthermore, the raft strength was higher than 7 g and hence could be considered strong and coherent and be able to withstand the peristaltic movements of the gastrointestinal tract [122,123].…”

Section: Raft-forming 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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“…Five tablets of each formulation were picked randomly and thickness was measured individually. 28 Friability: The friability of the prepared tablets was determined using Roche friability apparatus. It is expressed in percentage (%).…”

Section: Interparticle Porosity Post Compression Evaluationmentioning

confidence: 99%

Formulation and evaluation of raft forming pirenzepinedihydrochloride floating tablets for peptic ulcer

Rajmane¹,

Trivedi²,

Nandgude³

2022

ijhs

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Objective: Over past few decades, Peptic ulcer disease remains a common condition despite the lots of novelty in treatment. The objective of this research work was to formulate gastro retentive floating tablet by raft approach using Pirenzepine dihydrochloride (PNZ) as drug candidate. Formulation also contained a raft forming agent (sodium alginate) along with alkalizing agents (Calcium carbonate and Sodium Bicarbonate). Raft strength was only affected by the amount of Raft forming agent, Calcium carbonate and Sodium Bicarbonate. Method: Tablets were prepared by direct compression method and evaluated for raft strength, acid neutralization capacity, weight variation, % drug content, thickness, hardness, friability and In vitro drug release. Experimental work: A Box Behnken design was used in present study for optimization. Amount of gel forming agent, amount of cross-linkingagentsand floating agent were selected as independent variables. Raft strength, Acid neutralization capacity, and drug release were selected as dependent variables. Result: Raft strength, Acid neutralization capacity and In vitro drug release of all the experimental batches were found to be satisfactory. F10 batch was optimized based on maximum raft strength, good acid neutralization capacity and control drug release. Drug-excipients compatibility study showed no interaction between drug and excipients.

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Raft-forming gastro-retentive formulations based on Centella asiatica extract-solid dispersions for gastric ulcer treatment

Cited by 31 publications

References 33 publications

Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers

Development of raft-forming liquid and chewable tablet formulations incorporating quercetin solid dispersions for treatment of gastric ulcers

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

Formulation and evaluation of raft forming pirenzepinedihydrochloride floating tablets for peptic ulcer

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