Optimization of HPMC and carbopol concentrations in non-effervescent floating tablet through factorial design

Acharya, S.; Patra, Sradhanjali; Pani, Nihar Ranjan

doi:10.1016/j.carbpol.2013.11.060

Cited by 67 publications

(42 citation statements)

References 29 publications

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“…Auxiliary materials should have good liquidity, compressibility, suitable bulk density, and large pharmaceutical accommodation. 17) Therefore, this study selected hydrophilic gel skeleton materials, hydroxypropyl methyl cellulose, foaming agent sodium bicarbonate, flow aid powder silica gel, filler lactose, and microcrystalline cellulose as tablet accessories. All materials and accessories passed through sieve no.…”

Section: Methodsmentioning

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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Section: Methodsmentioning

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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“…The typical concentration of L-HPC 93 for tablet disintegration is 2.5-5.0% [9]. 94 Several articles have aimed at designing floating tablets which can 95 prolong the drug delivery time to 8 or more hours [10][11][12]. Numerous 96 articles have suggested that a gastric residence of 5 or more hours 97 may only be achieved with sufficient food or beverage consumption 98 [13][14][15][16]; however, it results in varying pH and unpredictable gastric [17], which is considered the media of fasting.…”

Section: Introductionmentioning

confidence: 99%

Preformulation studies and optimization of sodium alginate based floating drug delivery system for eradication of Helicobacter pylori

Diós

Nagy

Pál

et al. 2015

European Journal of Pharmaceutics and Biopharmaceutics

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“…It also suggested that the gel layer formed by HPMC by taking up water from the medium, enabled efficient entrapment of the carbon dioxide gas bubbles generated by NaCO 3 and citric acid dispersed in a HPMC matrix which increased the tablet porosity thereby causing the tablet to float for a longer period of time. Thus, both hydration and porosity played an important role in making the tablet buoyant (Acharya et al 2014). Another parameter influencing the characteristic of effervescent floating tablets is the FLT.…”

Section: In Vitro Buoyancy Studiesmentioning

confidence: 99%

“…Briefly, a tablet was weighed (W 0 ) and placed in a glass beaker, containing 200 mL of pH 1.2 hydrochloric acid buffer, maintained in a water bath at 37 ± 0.5°C (Dorozynski et al 2004). At regular time intervals, the tablets were removed and the excess surface liquid was carefully removed using a filter paper (Patel et al 2009;Tadros 2010;Acharya et al 2014). The swollen tablet was then reweighed (W t ).…”

Section: Swelling Studymentioning

confidence: 99%

Preparation and evaluation of gastroretentive effervescent floating drug delivery system of Samchulkunbi-tang

Pradhan

Lee

Kim

et al. 2015

Journal of Pharmaceutical Investigation

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The aim of this study was to develop a hydrophilic matrix based controlled release gastroretentive drug delivery system (GRDDS) for Samchulkunbi-tang (ST), a traditional Korean herbal medicine widely used for treatment of chronic gastritis and gastric ulcers. Effervescent floating GRDDS of ST was prepared by non-aqueous wet granulation method. Hydroxypropyl methylcellulose 2208 (100,000 cps) was used as the hydrophilic polymer, while the combination of sodium bicarbonate (NaHCO 3 ) and citric acid was used as the gas-generating agents. Formulation optimization was done by altering the amount of polymer and floating aid, keeping the tablet weight constant. Tablet properties including floating lag time (FLT), total floating time (TFT) and swelling index were measured to determine the optimized formulation. Scanning electron microscopy analysis revealed the surface morphology of the swollen tablet with concomitant gas bubbles. Optimized formulation showed satisfactory controlled in vitro drug release for more than 8 h with excellent buoyancy properties (FLT of 30 s, TFT [12 h). Therefore, the developed formulation of ST in the form of a floating tablet would provide effective gastroprotection and can be a promising approach to delivery of the drug in the upper gastrointestinal tract.

show abstract

Optimization of HPMC and carbopol concentrations in non-effervescent floating tablet through factorial design

Cited by 67 publications

References 29 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

Preformulation studies and optimization of sodium alginate based floating drug delivery system for eradication of Helicobacter pylori

Preparation and evaluation of gastroretentive effervescent floating drug delivery system of Samchulkunbi-tang

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