Sustained-release diclofenac potassium orally disintegrating tablet incorporating eudragit ERL/ERS: possibility of specific diclofenac-polymer interaction

Qandil, Amjad M.; Assaf, Shereen M.; Ani, Enas A. Al; Yassin, Alaa Eldeen B.; Obaidat, Aiman A.

doi:10.1007/s40005-013-0065-4

Cited by 10 publications

(5 citation statements)

References 23 publications

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“…Friability was under the limit of 0.5%. Disintegration time the orodispersible portion of all produced formulations obtained in the range of 18-60sec [23]. The obtained results confirm that the formulation FD-05 was within the specified limits according to USP, 2017 and showed in Tables 5 and 6.…”

Section: Physical Characterization Of Obtained Tabletssupporting

confidence: 77%

Development, Feasibility Assessment and in-vitro Evaluation of Diclofenac Potassium Multilayered Tablets

Abbas

Yousuf

Laghari

et al. 2021

JPRI

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Introduction: Diclofenac potassium has widely been utilized as an analgesic and anti-inflammatory agent. To achieve rapid onset of action with prolonged therapeutic action is an immense need of time. In present project a study was conducted on preparation with physicochemical determination of diclofenac potassium tablets, this unique tablet have duel characteristics like rapid onset of action due to orodispersible coat and extended release of API due to sustained release core. Methodology: As diclofenac potassium is not sensitive to water so wet granulation method was efficiently employed to prepare the granules of sustained release core, while direct compression was done to prepare orodispersible outer coat layer in order to give rapid release. Results and Discussion: In evaluations granules characteristics and tablet properties were studied. Result of both pre compression and post compression studies were coming in pharmacopeia acceptable ranges. The orodispersible layer disintegrated with in 18sec, which gives sufficient amount of API as loading dose, in order to maintain the plasma drug concentration in therapeutic range the core will release drug in sustained manner within 10 hours in gastrointestinal tract (GIT) fluid (pH 6.8). The results of kinetic models were complying with Higuchi model. Conclusion: In present work, a rapid release outer dispersible layer of drug was constructed on a sustained release core. Results of study gives expected outcomes to maintained initial concentration of drug which persist for long time. The combination of sodium starch glycolate, dry starch, and cross povidone exhibited promising super disintegrant efficiency while Hydroxypropylmethyl cellulose K15 showed excellent sustained release properties.

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Section: Physical Characterization Of Obtained Tabletssupporting

confidence: 77%

Development, Feasibility Assessment and in-vitro Evaluation of Diclofenac Potassium Multilayered Tablets

Abbas

Yousuf

Laghari

et al. 2021

JPRI

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“…There are many advantages of the emulsion cross-linking method, for example, it can be done under ambient temperature with constant stirring 26 and no special equipment is needed. 27 In additional, the chemical cross-linking method uses glutaraldehyde as the cross-linking agent to induce the rigidity of microspheres. The influence of process parameters, such as stirring speed, mixing time, and temperature, was analyzed.…”

Section: Resultsmentioning

confidence: 99%

A novel tetrandrine-loaded chitosan microsphere: characterization and in vivo evaluation

Guo

Cang

2016

DDDT

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In this study, novel tetrandrine-loaded chitosan microspheres were prepared by the emulsion cross-linking method. The systems were then characterized for physicochemical properties and in vitro drug release. In addition, the pharmacokinetics and tissue distribution of microspheres were further verified in animal models. Particle-size distribution indicated that the size of microspheres was within the range of 7–15 μm, with a median diameter of 12.4 μm. The drug loading and entrapment efficiency of the formulation were 34.6%±12.5% and 87.3%±9.7% (mean ± SD), respectively. In vitro release showed a typical sustained and long-term drug release behavior. The Higuchi equation was the model that fit best with release data. Maintaining a relatively constant plasma concentration in the long-term drug treatment is an outstanding pharmacokinetic advantage of tetrandrine microspheres in vivo. Moreover, compared with tetrandrine solution, tetrandrine microspheres produced a lower drug concentration in the heart, liver, and kidneys. This indicated that the microspheres used in this study were preferable for targeting lung tissue versus other tissues. No damage to the tissues of the lung was found in histopathological examination.

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“…According to a previous reference reported [ 19 ], the O/O solvent evaporation (SE) method was selected to prepare the microspheres here. There are many advantages for the method of SE, for example, it can be done under ambient temperature with constant stirring [ 32 ] and no special equipment was needed [ 33 ]. Thus, it is usually chosen and applied in the preparation of microspheres.…”

Section: Resultsmentioning

confidence: 99%

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

Xie

Lin

Xing³

et al. 2015

PLoS ONE

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Poor patient compliance, untoward reactions and unstable blood drug levels after the bolus administration are impeding the pharmacotherapy for insobriety. A long-acting preparation may address these limitations. The aim of this paper was to further investigate the in vitro characteristics and in vivo performances of nalmefene microspheres. Nalmefene was blended with poly (lactide-co-glycolide) (PLGA) to prepare the target microspheres by an O/O emulsification solvent evaporation method. The prepared microspheres exhibited a controlled release profile of nalmefene in vitro over 4 weeks, which was well fitted with a first-order model. In vitro degradation study showed that the drug release in vitro was dominated by both drug diffusion and polymer degradation mechanisms. Pharmacokinetics study indicated that the prepared microspheres could provide a relatively constant of nalmefene plasma concentration for at least one month in rats. The in vivo pharmacokinetics profile was well correlated with the in vitro drug release. Pharmacodynamics studies revealed that the drug loaded microspheres could produce a long-acting antagonism efficacy on rats. These results demonstrated the promising application of injectable PLGA microspheres containing nalmefene for the long-term treatment of alcohol dependence.

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Sustained-release diclofenac potassium orally disintegrating tablet incorporating eudragit ERL/ERS: possibility of specific diclofenac-polymer interaction

Cited by 10 publications

References 23 publications

Development, Feasibility Assessment and in-vitro Evaluation of Diclofenac Potassium Multilayered Tablets

Development, Feasibility Assessment and in-vitro Evaluation of Diclofenac Potassium Multilayered Tablets

A novel tetrandrine-loaded chitosan microsphere: characterization and in vivo evaluation

In Vitro and In Vivo Evaluations of PLGA Microspheres Containing Nalmefene

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