Development and Evaluation of Sustained Release Gastroretentive Minimatrices for Effective Treatment of H. pylori Infection

Badhan, Atul C.; Mashru, Rajashree; Shah, Priyanka; Thakkar, Arti; Dobaria, Nitin

doi:10.1208/s12249-009-9231-4

Cited by 42 publications

(19 citation statements)

References 27 publications

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“…The sustained-release system can achieve effective therapeutic drug concentrations in the systemic circulation over an extended period. 13) In this study, we selected the floating system to increase gastric residence time and to sustain drug release for developing gastric retention tablets of paeonol (GRT-P). We designed the formulation of gastric retention and sustained release for 8 h by considering gastric emptying time, gastric retention factors, and dietary habits.…”

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confidence: 99%

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Zhang

Han

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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This study aims to develop a gastroretentive sustained-release drug delivery system of paeonol using floating properties and to investigate its therapeutic effects in rat models. The gastric retention tablets of paeonol (GRT-Ps) were prepared by a direct compression method, and the Box-Behnken design was used to optimize its formulation. The optimized formulation containing 15% NaHCO 3 and a 2 : 1 ratio of paeonol and HPMC-K4M floated within 1 min and remained afloat for more than 8 h in the simulated gastric fluid (200 mL, pH 1.2) and simultaneously showed the desired sustained drug release. Moreover, small tablets (3 mm) were prepared according to the same formulation and the process technology of big tablets (8 mm). A similar drug release behavior was observed between two kinds of tablets ( f 2 52), and then the evaluations of efficacy and retention capacity in vivo were conducted with small tablets. In vivo retention studies showed that the T max (2 h) of GRT-P in rat stomachs was significantly extended compared with the T max (0.5 h) of normal reference preparation. Compared with the model group, low and high doses of GRT-P could significantly inhibit the increase of malondialdehyde (MDA) in serum. Studies showed that the higher MDA content in inflammation tissue increases the inflammatory response. The ulcer inhibition rates of GRT-P in the highdose group were 59.0 and 64.1% in the ranitidine group. Results indicated that GRT-Ps had the potential for a sustained drug release and an enhanced gastric residence time with relatively high drug concentrations in the tissue distribution.Key words paeonol; gastric retention tablet; sustained release; gastric ulcer; efficacy Paeonol, also called peony phenol, is the active component of a traditional Chinese medicine, namely, moutan cortex (Paeonia suffruticosa ANDREWS, Ranunculaceae).1) Paeonol has been extensively studied for its anti-inflammatory, antioxidant, anti-atherosclerosis, anti-diabetic, and anti-mutagenic effects.2,3) However, paeonol has significant growth-inhibitory and apoptosis-inducing effects in gastric cancer cells in vitro and in vivo.4) Moreover, studies have shown that paeonol prevents inflammatory diseases of the alimentary canal, such as irritable gastric ulcer, with minimal side effects.5) However, studies on the ethanol-induced gastric ulcer effect of paeonol are lacking. Currently, the listed paeonol dosages are administered via ordinary oral tablets and injection. However, paeonol has poor water solubility, easy oxidation, and a short biological half-life. [6][7][8] The paeonol products are unable to prolong effective drug concentration in blood to influence the oral bioavailability of a drug. Therefore, the present study, which is based on the properties of paeonol, has been designed to develop gastric retention tablets using modern technology to achieve prolonged presence in the stomach, thereby improving treatment of gastric ulcer. This approach has a profound clinical significance in developing a novel sustained-release delivery syst...

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confidence: 99%

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Zhang

Han

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…For most cases, it is an ideal platform for the preparation of protocols for bioequivalence studies and biwaiver applications. The US FDA also provides guidelines for bioavailability and bioequivalence studies for orally administered drug products 74 . In vitro-in vivo correlation (IVIVC) is a useful tool that can exploit potential future problems associated with the biowaiver principles.…”

Section: Bioequivalence/bioavailability Studies In Grddsmentioning

confidence: 99%

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Chordiya¹,

Gangurde²,

Borkar³

2017

Current Science

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Gastroretentive drug delivery systems (GRDDS) can overcome drawbacks associated with oral drug delivery, by defeating natural physiological principles. Various gastroretentive technologies have been developed in the past, but few of them achieved commercial success. Numerous mechanisms like floating, sinking, effervescence, swelling, bioadhesion, magnetic, etc. have been proposed over the years. At present, the polymeric swellings monolithic systems are popular. Dual working technology would be a possible way to overcome drawbacks associated with different GRDDS. Before development of a drug product, the principles of scale-up and process validation must be considered to improve the quality and market availability of GRDDS. Knowledge of all regulatory aspects will help deliver a product to the market within a reasonable time-frame and in a cost-effective manner.

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“…Badhan et al designed and optimized the sustained release gastroretentive mini matrices of amoxicillin using xanthan gum, rate-controlling polymers (HPMC K100M CR/PEO coagulant (1:1)), carbopol 974P and a gas-generating couple (sodium bicarbonate/citric acid (3:1)). The optimized formulation was said to be optimum because it had minimum buoyancy lag time of 7 min, required maximum time of 9.39 h for 95% drug release and had higher bioadhesive capabilities, indicating its sustained drug release and gastric retention capability [71]. Elsewhere, a new coated multiple-unit floating system was designed for sustained release of levodopa from floating minitablets.…”

Section: In Vitro Buoyancy and Drug Release Propertiesmentioning

confidence: 99%

Drug release kinetics and physicochemical characteristics of floating drug delivery systems

Adibkia

Hamedeyazdan

Javadzadeh

2011

Expert Opinion on Drug Delivery

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Developing an efficient floating dosage form is reliant on a better understanding of the relation between formulation variables and performance of the floating systems. Generally, the combination of two buoyancy mechanisms and gas-generating systems with swellable polymers would be beneficial for obtaining an appropriate floating lag time and duration of buoyancy, which in turn guarantees optimum efficiency of the pharmaceutical dosage form.

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Development and Evaluation of Sustained Release Gastroretentive Minimatrices for Effective Treatment of H. pylori Infection

Cited by 42 publications

References 27 publications

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Formulation Optimization of Gastro-Retention Tablets of Paeonol and Efficacy in Treatment of Experimental Gastric Ulcer

Technologies, Optimization and Analytical Parameters in Gastroretentive Drug Delivery Systems

Drug release kinetics and physicochemical characteristics of floating drug delivery systems

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