Gastro-floating tablets of cephalexin: Preparation and in vitro/in vivo evaluation

Yin, Lifang; Chao, Qin; Chen, Kaisheng; Zhu, Chunli; Cao, Hui; Zhou, Jianping; He, Wei; Zhang, Qiang

doi:10.1016/j.ijpharm.2013.05.011

Cited by 51 publications

(33 citation statements)

References 30 publications

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“…Floating tablets of cephalexin are reported using HPMC as matrix and sodium bicarbonate as a gas forming agent (Yin et al, 2013). Tablets of valacyclovir hydrochloride containing PEO and sodium bicarbonate exhibited prolonged buoyancy due to entrapment of carbon dioxide (CO 2 ) in the polymer gel matrix (Upadhyay et al, 2014).…”

Section: Resultsmentioning

confidence: 99%

Controlled release floating multiparticulates of metoprolol succinate by hot melt extrusion

Malode

Paradkar

Devarajan

2015

International Journal of Pharmaceutics

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Section: Resultsmentioning

confidence: 99%

Controlled release floating multiparticulates of metoprolol succinate by hot melt extrusion

Malode

Paradkar

Devarajan

2015

International Journal of Pharmaceutics

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“…Therefore, gastric retention agents are significant in treating stomach diseases with the advantages of improving drug efficacy and reducing drug toxicity. 12) Preliminary experiments showed that paeonol has certain inhibitory effects for Helicobacter pylori and gastric ulcer. We aimed to develop a sustained-release oral dosage of paeonol to increase the partial blood-drug concentration in the stomach.…”

mentioning

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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“…HPMC is a hydrophilic polymer and is strong enough to retard the release depending upon its viscosity and concentration [27] . Formulations with three different grades of HPMC (K4, K15, and K100) in three different concentrations (12.5, 25, and 37.5% w/w) including all other ingredients were accurately weighed and these powder blends were used for the preparation of sustained release tablets by direct compression method.…”

Section: Resultsmentioning

confidence: 99%

Formulation and Evaluation of Gastro-bilayer Floating Tablets of Simvastatin as Immediate Release Layer and Atenolol as Sustained Release Layer

Swain¹,

Pendela²,

Panda³

2016

ijps

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Swain, et al.: Gastro-bilayer Floating Tablets of Simvastatin and AtenololCombination therapy is highly desired to deliver atenolol and simvastatin for dyslipidemia and hypertension as a concomitant drug treatment. On other hand, atenolol has poor absorption in lower gastrointestinal tract, short half-life and simvastatin has poor solubility. Therefore, the present study was to develop gastro-bilayer floating matrix tablet in which simvastatin was incorporated as immediate layer and atenolol as sustained release layer. Gastro-bilayer floating tablets were prepared by direct compression method and optimized using hydroxypropyl methylcellulose K100 (37.5% w/w) as release retardant and sodium bicarbonate as a gas-forming agent. The immediate release layer comprised sodium starch glycolate as superdisintegrant. The tablets of optimized formulations floated on the test medium for more than 12 h with 9 min of floating lag time. Atenolol release was sustained for 12 h via diffusion mechanism and more than 96% release of simvastatin within 15 min was achieved. It can be concluded that, the biphasic drug release pattern was successfully achieved through the formulation of gastro-floating bilayer tablets in this study, allowing strengthened combination therapy for hypertension and dyslipidemia.

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Gastro-floating tablets of cephalexin: Preparation and in vitro/in vivo evaluation

Cited by 51 publications

References 30 publications

Controlled release floating multiparticulates of metoprolol succinate by hot melt extrusion

Controlled release floating multiparticulates of metoprolol succinate by hot melt extrusion

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

Formulation and Evaluation of Gastro-bilayer Floating Tablets of Simvastatin as Immediate Release Layer and Atenolol as Sustained Release Layer

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