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Deshpande, Arati; Shah, Navnit; Rhodes, C. T.; Malick, Waseem

doi:10.1023/a:1012171010492

Cited by 174 publications

(27 citation statements)

References 7 publications

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“…19) The paddle rotation speed was kept at 75 rpm and temperature of 37Ϯ0.5°C was maintained. At predetermined time interval of 1,2,3,4,5,6,7,8,10,12,14,16 and 24 h, 10 ml sample was withdrawn, filtered, suitably diluted and assayed at 288 nm by UV spectrophotometer (Shimadzu 1700).…”

Section: Methodsmentioning

confidence: 99%

“…The controlled gastric retention of solid dosage forms may be achieved by Mucoadhesion, 4) Floatation, 5) Sedimentation, 6) Expansion, 7) Modified shape system 8) and Simultaneous administration of pharmacological agents. 9,10) Gastroretentive floating drug delivery system (GRFDDS) has bulk density lower than gastric fluids and thus remains buoyant in the stomach without affecting the gastric emptying rate for a prolonged period of time.…”

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confidence: 99%

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Preparation and Evaluation of Gastroretentive Floating Tablets of Silymarin

Garg¹,

Gupta²

2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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The present study performed by preparation and evaluation of floating tablets of Silymarin as model drug for prolongation of gastric residence time. Floating effervescent tablets were formulated by various materials like hydroxypropyl methylcellulose (HPMC) K 4M, K 15M, psyllium husk, swelling agent as crospovidone and microcrystalline cellulose and gas generating agent like sodium bicarbonate and citric acid and evaluated for floating properties, swelling characteristics and in vitro drug release studies. Floating noneffervescent tablets were prepared by polypropylene foam powder and different matrix forming polymers like HPMC K 4M, Carbopol 934P, xanthan gum and sodium alginate. In vitro drug release studies were performed and drug release kinetics evaluated using the linear regression method was found to follow both the Higuchi and the Korsemeyer and Peppas equation. The drug release mechanism was found fickian type in most of the formulations. The developed floating tablets of Silymarin may be used in clinic for prolonged drug release for at least 24 h, thereby improving the bioavailability and patient compliance.

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Section: Methodsmentioning

confidence: 99%

mentioning

confidence: 99%

Preparation and Evaluation of Gastroretentive Floating Tablets of Silymarin

Garg¹,

Gupta²

2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…These include polymeric bioadhesive systems, 1) swelling and expanding systems, 2,3) and floating drug delivery systems. 4,5) The principle of buoyant preparation offers a simple, practical approach to achieve increased gastric residence time for the dosage form and sustained drug release.…”

Section: Regular Articlementioning

confidence: 99%

“…(2) where Q t is the fractional amount of drug dissolved in time t, Q 0 is the initial amount of drug in the solution, K 1 is the firstorder release constant, and t is release time. (3) where Q t is the fractional amount of drug dissolved in time t, K H is the Higuchi dissolution constant, and t is release time. (4) where Q 0 is the initial amount of drug in the pharmaceutical dosage form, Q t is the remaining amount of drug in the pharmaceutical dosage form at time t, K s is a constant incorporating the surface-volume relation, and t is release time.…”

mentioning

confidence: 99%

Floating and Sustained-Release Characteristics of Effervescent Tablets Prepared with a Mixed Matrix of Eudragit L-100-55 and Eudragit E PO

Bani-Jaber

Alkawareek

Al-Gousous

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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Regular ArticleSeveral approaches are used to prolong gastric retention time. These include polymeric bioadhesive systems, 1) swelling and expanding systems, 2,3) and floating drug delivery systems. 4,5) The principle of buoyant preparation offers a simple, practical approach to achieve increased gastric residence time for the dosage form and sustained drug release. 6) In addition, it offers a greater safety for clinical uses than some other approaches. 7) To achieve an intragastric floating system, low-density additives (e.g., fatty acids and fatty alcohols) and gas-generating agents (effervescent type) are used.8) The effervescent type consists of a polymeric matrix containing effervescent components, such as Na-bicarbonate. The matrices are fabricated so that upon arrival in the stomach, carbon dioxide is liberated by the acidity of the gastric contents and is entrapped in a gelling hydrocolloid. This produces an upward motion of the dosage form and maintains its buoyancy.9) Among the hydrocolloids used for this purpose are hydroxypropyl methylcellulose, chitosan, and carboxymethylcellulose.The use of two polymers having opposite charges to form an interpolyelectrolyte complex has recently achieved attention because of the capability of the interpolyelectrolyte complex to achieve more extended drug release than single polymers. The interpolyelectrolyte complex can be synthesized and then used as a matrix former, which was studied for chitosan and polyacrylic acid for the purpose of stomachcontrolled antibiotic delivery. 10) Alternatively, the two polymers are physically mixed to form the matrix, and the interpolyelectrolyte complex is formed in situ during exposure to a simulated gastric fluid. The later approach was studied for chitosan and carboxymethylcellulose as a gastric-specific delivery system for clarithromycin. 11)Polymethacrylates are synthetic cationic or anionic polymers of dimethyl-aminoethylmethacrylates, methacrylic acid, and methacrylic acid esters in varying ratios. They are used in pharmaceutical formulations as film coating agents, bindings, direct-compression excipients, and gel bases.12) Eudragit E (EE) is a cationic polymer prepared by copolymerization of butyl methacrylate, 2-dimethylaminoethylmethacrylate, and methyl methacrylate with mole ratio of 1 : 2 : 1.13) It is soluble in gastric fluid below pH 5.0. 13) Eudragit ® L-100-55 (EL) is an anionic copolymer based on methacrylic acid and methyl methacrylate.14) It exhibits pH dependent solubility and is soluble at pH values higher than 5.5. 14) Although polymethacrylates are widely used in pharmaceutical delivery systems for sustained drug release, their use as matrix former in floating tablets for local drug delivery in the stomach was not routinely addressed in the literature. The influence of Na-bicarbonate on the physicochemical properties of controlled-release hot-melt extruded (HME) tablets containing Eudragit RS PO and/or EE, in comparison with corresponding tablets made using direct compression, was previously investigated. 15...

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“…To overcome these problems oral controlled dosage form with gastro retentive properties were developed [4]. These include bioadhesive or mucoadhesive systems [5], swelling and expanding systems [6,7], floating systems [8,9] and other delayed gastric emptying devices. The principle of floating preparation offers a simple and practical approach to achieve increased gastric residence time for the dosage form and sustained drug release [10].…”

Section: Introductionmentioning

confidence: 99%

Sustain Release Formulation and Evaluation of Ofloxacin Floating Delivery System

Patel

Naik

Raval

2014

ILCPA

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Floating tablets has been accepted as a process to achieve controlled drug delivery by prolonging the residence time of the dosage form at the site of absorption, thereby improving and enhancing the bioavailability of drug. The objective of present study outlines the development and characterization the floating drug delivery system of Ofloxacin to enhance its bioavailability and therapeutic efficacy, using different grades of polymer along with effervescent agent sodium bicarbonate and citric acid. Ofloxacin is a synthetic chemotherapeutic second-generation antibiotic of the fluoroquinolone class. Different tablet formulations were formulated by wet granulation technique and were evaluated for physical parameters like Tablet Thickness, Hardness, % Friability, Weight variation, Content uniformity, In vitro buoyancy, Swelling index, In vitro dissolution study and drug release mechanisms. As the concentration of the polymer in the formulations increased the release of drug decreased. Hence it was considered as suitable candidate for formulation as floating drug delivery system. Different kinetic models were applied to drug release data in order to evaluate release mechanisms and kinetics. The optimized formula F4 showed better sustained drug release with good floating properties and fitted best to be Korsmeyer-Peppas model with R 2 value of 0.9575. As the n value for the Korsmeyer-Peppas model was found be more than 0.5 it follows Non-Fickian diffusion mechanism. FTIR result showed that there is no drug excipients interaction.

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Abstract: When this tablet is ingested, the chances of its elimination through the pylorus should be greatly reduced due to tablet's expansion, and due to its disintegration or loss in integrity it should then be expelled out of the stomach at the end of the drug release.

Cited by 174 publications

References 7 publications

Preparation and Evaluation of Gastroretentive Floating Tablets of Silymarin

Preparation and Evaluation of Gastroretentive Floating Tablets of Silymarin

Floating and Sustained-Release Characteristics of Effervescent Tablets Prepared with a Mixed Matrix of Eudragit L-100-55 and Eudragit E PO

Sustain Release Formulation and Evaluation of Ofloxacin Floating Delivery System

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