Floating Elementary Osmotic Pump Tablet (FEOPT) for Controlled Delivery of Diethylcarbamazine Citrate: a Water-Soluble Drug

Khan, Zulfequar Ahamad; Tripathi, Rahul; Mishra, Brahmeshwar

doi:10.1208/s12249-011-9699-6

Cited by 25 publications

(19 citation statements)

References 26 publications

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“…Buoyancy was achieved because of the constant imbibition of HCl within the microspheres, which reacted with NaHCO 3 and liberated CO 2 gas. Furthermore, this CO 2 gas was easily entrapped within the complex network of microspheres and allowed the PAM‐ g ‐Psy–NaAlg CMs to float on the aqueous surface …”

Section: Resultsmentioning

confidence: 99%

Preparation and evaluation of composite microspheres of polyacrylamide‐grafted polysaccharides

Tripathi

Mishra

2013

J of Applied Polymer Sci

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The poor mechanical strength and instability of polysaccharide's gel takes away opportunities for versatile application. The grafting of polyacrylamide (PAM) onto polysaccharide was found to be an efficient tool for transforming its properties and obtaining stable and robust composite microspheres (CMs). In this study, free-radical polymerization reaction was used for the grafting of PAM onto the polysaccharide backbone, and their hydrogel CMs were obtained through an ionotropic gelation method. Porous and buoyant CMs were obtained through the incorporation of sodium bicarbonate into the reaction mixture. Characterizations were done through Fourier transform infrared spectroscopy, thermal and scanning electron microscopy analysis. The mechanical strength and squeezing capacity were evaluated extensively through a modified syringe method developed in-house. The squeezing capacity of grafted CMs diminished with the formation of a complex interpenetrating network. The Young's modulus, swelling kinetics, mechanical strength, and squeezing capacity of the grafted microspheres were compared extensively.

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Section: Resultsmentioning

confidence: 99%

Preparation and evaluation of composite microspheres of polyacrylamide‐grafted polysaccharides

Tripathi

Mishra

2013

J of Applied Polymer Sci

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“…angle of repose, bulk density, tapped density, compressibility index (Carr's index) and Hausner's ratio using standard procedures [10][11][12].…”

Section: Pre-compression Evaluationmentioning

confidence: 99%

Development and Evaluation of Gastroretentive Floating Tablets of a Quinapril HCL by Direct Compression Technique

Mali

Bathe

2017

Int J Pharm Pharm Sci

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Objective: The present study was undertaken with an objective to design, develop and evaluate gastro retentive floating tablets of an antihypertensive drug, quinapril HCl, which release the drug in a sustained manner over a period of 12 h. Methods:In this research work, we used hydrophilic polymer hydroxypropyl methylcellulose (HPMC K4M), the gas generating agent sodium bicarbonate and citric acid at different ratios for the preparation of tablets. ) and floating lag time. The high concentration of HPMC K4M and citric acid gives a sustained release for quinapril HCl floating tablets. The tablets were prepared by direct compression technique and evaluated for tablet thickness, hardness, weight variation, friability, floating lag time and In vitro drug release. Results:The In vitro drug release indicated the floating dosage forms showed slower release when the concentration of HPMC K4M increases. Formulation F4 having ratio 25:8 (HPMC K4M: citric acid) was considered as an optimised formulation which shows satisfactory sustained drug release and remained buoyant on the surface of the medium for more than 12 h. It can also conclude that floating drug delivery system of quinapril HCl can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability. Conclusion:The developed effervescent based floating tablets are a promising floating drug delivery system for oral sustained administration of quinapril HCl.

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“…The selected plasticizers were widely used to enhance properties of coating film in coating process. [36][37][38] The hydrophilicity of plasticizers could affect the dissolution rate of drug, so plasticizers were screened in accordance with the solubility in water. The hydrophilicity of plasticizers in water is increased in the sequence of castor oil, TEC, and PEG 6000.…”

Section: Effect Of Coating Agents (Eudragit ® Rl/rs) and Coating Levementioning

confidence: 99%

Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

Kim

et al. 2013

CHEMICAL & PHARMACEUTICAL BULLETIN

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Doxazosin mesylate (DXM) sustained release pellets were prepared by an extrusion-spheronization and fluid-bed coating technique. The core pellets containing DXM were prepared by extrusion-spheronization technique, and coated by a fluid-bed coater to control the release of DXM. The factors affecting to properties of pellets, such as diluent content, type and coating level of coating agents and plasticizers were studied in the present study. Polymethacrylate derivatives (Eudragit ® RS PO and RL PO) were used for coating agents, and polyethylene glycol 6000 (PEG 6000), triethyl citrate (TEC) and castor oil were as plasticizers. To evaluate the properties of prepared pellets, the size of prepared pellets was investigated by sieve analysis technique and the morphology of pellets was evaluated by scanning electron microscopy. Through the dissolution test, factors that have an effect on the dissolution of the drug were evaluated. As the content ratio of microcrystalline cellulose (MCC) had increased, the dissolution was proportionally sustained. Eudragit ® RS PO had more marked sustaining effect on the dissolution rate than Eudragit ® RL PO, and the effect was more pronounced with the increased coating level. PEG 6000 was an appropriate plasticizer for DXM pellets, and increasing the content of PEG 6000, was also slightly decreasing the dissolution rate.Key words sustained release; pellet; extrusion-spheronization; fluid-bed coating; doxazosin mesylate Doxazosin mesylate (DXM) is a selective inhibitor of α 1 -adrenergic receptors and has been demonstrated to be effective for the treatment of hypertension and benign prostatic hyperplasia.1-3) DXM lowers the blood pressure of hypertensive patients by blocking postjunctional α 1 -adrenergic receptors, and then systemic vascular resistance decreases. 4)Taking a DXM can cause first-dose side effects like hypotension because of the rapid increase of drug concentration in the blood.5) Therefore the usual therapy of DXM is initially starting with a low dose (1 mg/d) and gradually increased up to the daily maximum recommended dose (16 mg/d).2) In order to overcome the adverse effects of DXM and to improve inconvenience of the regimen, various studies for controlled-release dosage forms of DXM have been conducted. [6][7][8] Application of the controlled release system to DXM could have benefits such as reducing the adverse effects by minimizing the fluctuation of drug concentration in the plasma. DXM could cause a significant reduction in blood pressure after administration of the first dose, so a formulation of sustained release of DXM could avoid this first dose effect. Among several systems for controlled release of the model drug, multi-unit dosage forms such as pellets or beads coated with polymers used as a release retardant has several advantages. The single unit dosage form like tablets has been widely used because of its simple and cost-effective manufacturing operations and ease of administration. 9,10) In comparison with a single unit dosage form, the multi-unit dosag...

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Floating Elementary Osmotic Pump Tablet (FEOPT) for Controlled Delivery of Diethylcarbamazine Citrate: a Water-Soluble Drug

Cited by 25 publications

References 26 publications

Preparation and evaluation of composite microspheres of polyacrylamide‐grafted polysaccharides

Preparation and evaluation of composite microspheres of polyacrylamide‐grafted polysaccharides

Development and Evaluation of Gastroretentive Floating Tablets of a Quinapril HCL by Direct Compression Technique

Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

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