<i>In vitro</i> and <i>in vivo</i> techniques to assess the performance of gastro-retentive drug delivery systems: a review

Parikh, Dhaivat; Amin, Avani

doi:10.1517/17425247.5.9.951

Cited by 23 publications

(17 citation statements)

References 86 publications

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“…Considering all these aspects, researchers initiated development of formulation that possess capability of gastric retention, that is, gastroretentive dosage form (GRDF). These dosage forms will be advantageous for drugs that have an absorption window within gastrointestinal (GI) tract, pH-dependent absorption from stomach, drugs for local action or having stability problem at high pH or in intestine and colon [3,4].…”

Section: Introductionmentioning

confidence: 99%

Formulation optimization of gastroretentive drug delivery system for allopurinol using experimental design

Sharma

Shah

Parikh

et al. 2014

Expert Opinion on Drug Delivery

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Introduction: The objective of the present investigation was to develop a multiparticulate modified release system of methylphenidate hydrochloride (HCl) generating biphasic release profile from single core. Materials and Methods: Wurster (bottom spray fluid bed coating) process was employed to develop extended release (ER) pellets of methylphenidate HCl. Impact of various formulation variables was assessed using statistical interpretation such as analysis of variance. A 3 2 (two factor, three level) factorial design was employed to study the effect of independent variables (ER polymer [Eudragit RSPO/ Eudragit RLPO/Ethocel] concentration and plasticizer concentration), on dependent variables (drug release at 3 rd and 8 th h). Optimization was done by fitting experimental data to the software program (Design Expert). The design space for formulation variables (ER polymer concentration and plasticizer concentration) and its influence on drug release was developed. Results and Discussion: Fabricated pellets were characterized for various physicochemical parameters. In vitro release data observed from the optimized formulation was fitted into various kinetic equations. The optimized formulation showed desired drug release at both 3 rd and 8 th h as 60.33% ± 0.58% and 93.33% ± 0.58%, respectively. Capsules showed an initial burst release preceding a more gradual ER phase following first order kinetics and Fickian diffusion process. Conclusion: Methylphenidate HCl ER pellets were successfully developed by employing bottom spray fluid bed coating (Wurster) technique. The factorial experimental design facilitated the formulation and optimization of modified drug delivery system of methylphenidate HCl.

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Section: Introductionmentioning

confidence: 99%

Formulation optimization of gastroretentive drug delivery system for allopurinol using experimental design

Sharma

Shah

Parikh

et al. 2014

Expert Opinion on Drug Delivery

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“…[9][10][11] Most oral sustained-control release drug delivery systems effectively regulate drug release into the system; however, drug bioavailability is low because of low drug concentration in local tissue. Therefore, gastric retention agents are significant in treating stomach diseases with the advantages of improving drug efficacy and reducing drug toxicity.…”

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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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“…Thus there is an urgent need to develop a more authentic in vivo mucoadhesion testing method. Parikh and Amin 66 described the in vitro and in vivo techniques to efficiently evaluate the floating, raft-forming and expandable systems. According to current good manufacturing practices, it is necessary to identify potential and critical in-process controls that can affect the quality of the drug product.…”

Section: Analytical Specification For 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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In vitro and in vivo techniques to assess the performance of gastro-retentive drug delivery systems: a review

Cited by 23 publications

References 86 publications

Formulation optimization of gastroretentive drug delivery system for allopurinol using experimental design

Formulation optimization of gastroretentive drug delivery system for allopurinol using experimental design

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

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