Gastroretentive drug delivery systems

Streubel, A.; Siepmann, J.; Bodmeier, Roland

doi:10.1517/17425247.3.2.217

Cited by 256 publications

(158 citation statements)

References 116 publications

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“…This controlled release technology had made it possible to release drugs at a constant release rate for longer periods of time. However, this benefit had not satisfied a variety of important drugs that (i) are locally active in the stomach, (ii) have an absorption window in the stomach or in the upper small intestine, (iii) are unstable in the intestinal or colonic environment, or (iv) exhibit low solubilities at high pH values [1][2][3]. These limits promoted the development of gastroretentive drug delivery systems (GRDDS).…”

Section: Introductionmentioning

confidence: 99%

Development and Characterization of Gastroretentive Drug Delivery System for Ritonavir Tablets Using Natural Polymers

Chukka

Shaik

2017

Asian J Pharm Clin Res

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Objective: This study involves preparation and evaluation of floating tablets of ritonavir (RN) for improving the drug bioavailability by prolongation of gastric residence time. RN is an antiretroviral agent used in the treatment of HIV and viral diseases have been taken as a model drug in this investigation because of its low biological half-life (3-5 hrs). Moreover, it is primarily absorbed from stomach.Methods: RN floating tablets were prepared by the dry granulation technique, using guar gum and xanthan gum as polymers, sodium bicarbonate as effervescent agent, polyvinylpyrrolidone as binding agent, Dicalcium phosphate as diluents, crospovidone as swelling agent and magnesium stearate as lubricant. The prepared tablets were evaluated for various physicochemical parameters.Results: Drug-excipient interaction studies were conducted by Fourier transform infrared spectroscopy and differential scanning calorimetry. The results suggested that there was no incompatibility between the drug and polymers. The prepared tablets were evaluated for their physical characteristics. All the parameters were within the pharmacopoeial limits. Further, tablets were also studied for their floating properties and in vitro drug release characteristics. The tablets exhibited controlled and prolonged drug release profiles. The developed formulation was found to be stable. Conclusion:The developed floating tablets of RN exhibit prolonged release up to 12 hrs, and thus may improve bioavailability and minimize fluctuations in plasma drug concentrations.

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Section: Introductionmentioning

confidence: 99%

Development and Characterization of Gastroretentive Drug Delivery System for Ritonavir Tablets Using Natural Polymers

Chukka

Shaik

2017

Asian J Pharm Clin Res

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“…Oral controlled release drug delivery releases the drug at a predetermined rate with improved therapeutic result, ease of dosing administration, patient compliance and flexibility in formulation 2 . Gastro retentive drug delivery systems are capable of delaying the release rate either by diffusion and erosion of the polymer matrix which retain in the stomach by passing the gastric transit 3 . Microsphere are solid, approximately spherical particles which contain dispersed drug molecules either in solution or in crystalline form and the size ranges from 1 to 1000µm.…”

Section: Introductionmentioning

confidence: 99%

Formulation and in-Vitro Evaluation of Gastro-Retentive Microsphere Containing Calendula Officinalis for the Treatment of Peptic Ulcers Using Okra Mucilage and Ethyl Cellulose

Awasthi¹,

Thakur²,

Ghosh³

2016

Int. Res. J. Pharm.

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The objective of the research was to formulate and evaluate gastro retentive microspheres containing Calendula officinalis for the treatment of Peptic ulcer. An attempt has been made to improve bioavailability and patient compliance by utilizing the concept of microsphere. Microspheres were prepared by solvent evaporation method using ethyl cellulose and okra mucilage. Ethyl cellulose is responsible for sustained release of Calendula officnalis extract whereas okra mucilage aids in mucoadhesion of microsphere. Formulation was optimized using different concentration of polymers and excipients. The Optimized formulation F1 showed 94.31 % release of Calendula officinalis and drug content was found to be 88.3% of Calendula officinalis. The in-vitro studies showed that microspheres were capable of floating up to 12hours in simulated gastric fluid and sustained the release of Calendula officinalis for 12 hours. Scanning electron microscopy showed their spherical size, perforated smooth surface and a cavity inside microspheres.

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“…Prolonged gastric residence is expected to lead to an increased contact interval with the main absorption site of tacrolimus, the mucosa of the upper small intestine. Owing to its improved bioavailability combined with reduced frequency of administration and thus improved patient compliance, gastric retentive devices may also be used as extended-release drug delivery systems [21,22] . Several gastroretentive extended-release products are available on the market at present.…”

Section: Introductionmentioning

confidence: 99%

Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

2011

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Aim: To develop a novel gastroretentive drug delivery system based on a self-microemulsifying (SME) lipid mixture for improving the oral absorption of the immunosuppressant tacrolimus. Methods: Liquid SME mixture, composed of Cremophor RH40 and monocaprylin glycerate, was blended with polyethylene oxide, chitosan, polyvinylpyrrolidone and mannitol, and then transformed into tablets via granulation, with ethanol as the wetting agent. The tablets were characterized in respect of swelling, bioadhesive and SME properties. In vitro dissolution was conducted using an HCl buffer at pH 1.2. Oral bioavailability of the tablets was examined in fasted beagle dogs. Results: The tablet could expand to 13.5 mm in diameter and 15 mm in thickness during the initial 20 min of contact with the HCl buffer at pH 1.2. The bioadhesive strength was as high as 0.98±0.06 N/cm 2 . The SME gastroretentive sustained-release tablets preserved the SME capability of the liquid SME formations under transmission electron microscope. The drug-release curve was fit to the zero-order release model, which was helpful in reducing fluctuations in blood concentration. Compared with the commercially available capsules of tacrolimus, the relative bioavailability of the SME gastroretentive sustained-release tablets was 553.4%±353.8%. Conclusion: SME gastroretentive sustained-release tablets can enhance the oral bioavailability of tacrolimus with poor solubility and a narrow absorption window.

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Gastroretentive drug delivery systems

Cited by 256 publications

References 116 publications

Development and Characterization of Gastroretentive Drug Delivery System for Ritonavir Tablets Using Natural Polymers

Development and Characterization of Gastroretentive Drug Delivery System for Ritonavir Tablets Using Natural Polymers

Formulation and in-Vitro Evaluation of Gastro-Retentive Microsphere Containing Calendula Officinalis for the Treatment of Peptic Ulcers Using Okra Mucilage and Ethyl Cellulose

Novel gastroretentive sustained-release tablet of tacrolimus based on self-microemulsifying mixture: in vitro evaluation and in vivo bioavailability test

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