Development and In Vitro/In Vivo Evaluation of Etodolac Controlled Porosity Osmotic Pump Tablets

Abdelbary, Ahmed; Tadros, Mina Ibrahim; Alaa-Eldin, Ahmed Adel

doi:10.1208/s12249-011-9608-z

Cited by 25 publications

(13 citation statements)

References 22 publications

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“…The values of difference factor and similarity factor indicate that there was no significant difference between drug release profiles at different pH conditions as well as at different agitation intensities. In CPOP systems, pH and agitation intensity do not have any role in release mechanism of drugs (37). The physical observation of CPOP after completion of drug release study showed that increase in size of the tablet due to osmotic pressure leads to inflow of dissolution medium though the semipermeable membrane.…”

Section: Discussionmentioning

confidence: 98%

Development and Evaluation of a Once-Daily Controlled Porosity Osmotic Pump of Tapentadol Hydrochloride

2015

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Abstract. The present study aimed to prepare, optimize, and evaluate Tapentadol hydrochloride controlled porosity osmotic pump (CPOP) and to achieve the drug release at nearly zero-order. The CPOP was prepared by the coating of polymers (Eudragit RSPO and RLPO) on a directly compressed core tablet. A Box-behnken experimental design was applied to optimize the parameters for CPOP. The optimized batch was characterized for in vitro drug release study, effect of pH, osmolarity and agitation intensity, and surface morphology and stability study. In vivo pharmacokinetic studies were performed on New Zealand white rabbits for CPOP and marketed tablet. All the batches showed a drug release ranging from 29.87 to 56.92% after 12 h; and from 59.64 to 99.96% after 24 h. There was no change in the drug release pattern at different pH and agitation intensities. The drug release was found to decrease with increasing osmolarity of dissolution media.An in vivo study showed a higher mean residence time, area under the curve, and biological half-life (T 1/2 ) than the marketed tablet with low rate of elimination (Ke) and a 2.35-fold increase in relative bioavailability. The result showed that the amounts of sodium chloride and PEG 400 were contributing positively while the number of coats was negatively affecting the drug release. The drug release was found to be independent of physiological conditions. The stability testing showed that the prepared CPOP was stable for 3 months at accelerated conditions. The prepared CPOP was found to deliver Tapentadol hydrochloride at zero-order for up to 24 h.

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Section: Discussionmentioning

confidence: 98%

Development and Evaluation of a Once-Daily Controlled Porosity Osmotic Pump of Tapentadol Hydrochloride

2015

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“…The estimated pharmacokinetics parameters included; C max (the maximum drug concentration; ng/mL), t max (the time to reach C max ; h), MRT 0-∞ (the mean residence time, h), AUC (0-48h) (the area under the plasma concentration -time curve from zero to 48 h; ng h/mL) and AUC (0-∞) (the area under the curve from zero to infinity; ng h/mL) 30 . The relative bioavailability was calculated by dividing AUC (0-48h) of F6 over AUC (0-48h) of Benicar ® tablets.…”

Section: Pharmacokinetic and Statistical Analysesmentioning

confidence: 99%

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2018

IJPSR

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ABSTRACT:Olmesartan medoxomil (OLM) is a lipophilic (log P = 4.31) antihypertensive drug suffering from limited oral bioavailability in humans (26%) due to its low aqueous solubility, uncontrolled enzymatic conversion to the active metabolite (Olmesartan; OL) and efflux by drug resistance pumps. Surmounting such limitations via incorporation of OLM into selfnanoemulsifying drug delivery systems (SNEDDS). Based on OLM-equilibrium solubility studies in various oils, surfactants and co-surfactants, Capmul ® MCM, Tween ® 20, Cremophor ® EL and polyethylene glycol -400 (PEG) were combined in different ratios to plot ternary phase diagrams. OLM-loaded SENDDS were developed and evaluated forparticle size, polydispersity index (PDI), zeta potential, self-emulsification time, morphology, drug released percentages after 5-min (Q 5min %), 1 hour (Q 1h %) and dissolution efficiency percentages (DE 1h %). The OL pharmacokinetics from SNEDDS (F6) and Benicar ® tablets were evaluated (LC-MS/MS) in rabbits. Spherical OLM-loaded SNEDDS were developed. The best-achieved SNEDDS (F6) showed short emulsification time (13 s), fine droplet size (60.00nm), low PDI (0.25), negative zeta potential (-14.4mV), promising dissolution parameters; Q 5min % (29.78%), Q 1h % (66.69%) and DE 1h % (47.96%) and enhanced in vivo absorption characteristics; shorter T max , higher C max and larger AUC (0−48h ; suggesting its potential for the enhancement of the oral absorption of practically insoluble drugs; like OLM.

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“…For drugs that are administered orally, dissolution and intestinal permeation are considered as the rate-limiting steps for the absorption. Therefore, if an excellent correlation exists between in vitro dissolution test and a bioavailability parameter, then controlling the dissolution profile will permit the evaluation of bioavailability [57][58][59].…”

Section: In Vitro In Vivo Correlation (Ivivc) For Lipid Nanoformulationsmentioning

confidence: 99%

Lipid‐Based Nano‐Delivery for Oral Administration of Poorly Water Soluble Drugs (PWSDs): Design, Optimization and in vitro Assessment

Kazi¹

2017

Advanced Technology for Delivering Therapeutics

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Currently, more than 90% of compounds identified are water insoluble and or poorly water soluble, which is a bottle neck in the development of many new drug candidates. These poorly soluble drug molecules are difficult to formulate using conventional approaches and are associated with numerous formulation-related performance issues. Formulating these compounds using lipid-based systems is one of the rapidly growing interests and suitable drug delivery strategies. Lipid formulations such as selfemulsifying/microemulsifying/nanoemulsifying drug delivery systems (SEDDS/ SMEDDS/SNEDDS) have been attempted in many researches to improve the bioavailability and dissolution rate for their better dispersion properties. One of the greatest advantages of incorporating the poorly soluble drug into such formulation products is their spontaneous emulsion and or microemulsion/nanoemulsion formation in aqueous media. The performance and ongoing advances in manufacturing technologies have rapidly introduced lipid-based drug formulations as commercial products into the marketplace with several others in clinical development. The current chapter aims to present the characteristics feature, development and utilization of oral lipid-based nanoformulations within the drug delivery regime. The content of the chapter also provides an insight into the in vitro evaluation of lipid-based nanosystems and their limitations.

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Development and In Vitro/In Vivo Evaluation of Etodolac Controlled Porosity Osmotic Pump Tablets

Cited by 25 publications

References 22 publications

Development and Evaluation of a Once-Daily Controlled Porosity Osmotic Pump of Tapentadol Hydrochloride

Development and Evaluation of a Once-Daily Controlled Porosity Osmotic Pump of Tapentadol Hydrochloride

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Lipid‐Based Nano‐Delivery for Oral Administration of Poorly Water Soluble Drugs (PWSDs): Design, Optimization and in vitro Assessment

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