The impact of polymers on 3D microstructure and controlled release of sildenafil citrate from hydrophilic matrices

Krupa, Anna; Tabor, Zbisław; Tarasiuk, Jacek; Strach, Beata; Pociecha, Krzysztof; Wyska, Elżbieta; Wroński, Sebastian; Łyszczarz, Ewelina; Jachowicz, Renata

doi:10.1016/j.ejps.2018.04.023

Cited by 6 publications

(2 citation statements)

References 31 publications

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“…Various poloxamers types are available on the market, including poloxamer 188 (P-188), poloxamer 184 (P-184), poloxamer 401 (P-401), poloxamer 108 (P-108), poloxamer 402 (P-402), poloxamer 408 (P-408), and poloxamer 407 (P-407) [ 40 ]. The application of P-188 to develop controlled release systems has been reported previously, for example, for tetramethylpyrazine [ 41 ], sildenafil citrate [ 42 ], and indomethacin [ 43 ]. However, to the best of our knowledge, DLZ-modified release preparation using different dosage forms and materials have been reported [ 44 , 45 ], but no study has used P-188 in a controlled release matrix system for DLZ.…”

Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System

et al. 2021

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Diltiazem hydrochloride is a calcium channel blocker, which belongs to the family of benzothiazepines. It is commonly used to treat hypertension and atrial fibrillation. Even though the drug has high solubility, its high permeability and rapid metabolism in the liver can limit the bioavailability and increase the dose frequencies for up to four times per day. This study focused on a polymer matrix system not only to control the drug release but also to prolong the duration of bioavailability. The polymer matrices were prepared using different ratios of poloxamer-188, hydroxypropyl methylcellulose, and stearyl alcohol. In vitro and in vivo assessments took place using 24 rabbits and the results were compared to commercially available product Tildiem® (60 mg tablet) as reference. Overall, the rate of drug release was sustained with the gradual increase of poloxamer-188 incorporated with hydroxypropyl methylcellulose and stearyl alcohol in the matrix system, achieving a maximum release period of 10 h. The oral bioavailability and pharmacokinetic parameters of diltiazem hydrochloride incorporated in polymer matrix system were similar to commercial reference Tildiem®. In conclusion, the combination of polymers can have a substantial effect on controlling and prolonging the drug release pattern. The outcomes showed that poloxamer-188 combined with hydroxypropyl methylcellulose and stearyl alcohol is a powerful matrix system for controlling release of diltiazem hydrochloride.

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Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System

et al. 2021

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“…Dissolution testing has been a subject of scientific research since the pioneering work of Noyes and Whitney [26]. Although the pharmaceutical industry has applied it for a long time to confirm batch-to-batch consistency, it has received increased attention after the correlation between in vitro dissolution profiles and bioavailability was discovered [27,28,29,30]. In vitro dissolution profiles are often part of the target product quality profile of the modern quality by design approach [31], and are vital in the approval of new products or existing products after changes in technology [32].…”

Section: Introductionmentioning

confidence: 99%

Fast, Spectroscopy-Based Prediction of In Vitro Dissolution Profile of Extended Release Tablets Using Artificial Neural Networks

et al. 2019

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The pharmaceutical industry has never seen such a vast development in process analytical methods as in the last decade. The application of near-infrared (NIR) and Raman spectroscopy in monitoring production lines has also become widespread. This work aims to utilize the large amount of information collected by these methods by building an artificial neural network (ANN) model that can predict the dissolution profile of the scanned tablets. An extended release formulation containing drotaverine (DR) as a model drug was developed and tablets were produced with 37 different settings, with the variables being the DR content, the hydroxypropyl methylcellulose (HPMC) content and compression force. NIR and Raman spectra of the tablets were recorded in both the transmission and reflection method. The spectra were used to build a partial least squares prediction model for the DR and HPMC content. The ANN model used these predicted values, along with the measured compression force, as input data. It was found that models based on both NIR and Raman spectra were capable of predicting the dissolution profile of the test tablets within the acceptance limit of the f2 difference factor. The performance of these ANN models was compared to PLS models using the same data as input, and the prediction of the ANN models was found to be more accurate. The proposed method accomplishes the prediction of the dissolution profile of extended release tablets using either NIR or Raman spectra.

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The use of the Brouers–Sotolongo fractal kinetic equation for the study of drug release

Brouers

Al-Musawi

2019

Adsorption

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The impact of polymers on 3D microstructure and controlled release of sildenafil citrate from hydrophilic matrices

Cited by 6 publications

References 31 publications

In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System

In Vitro and In Vivo Evaluation of Oral Controlled Release Formulation of BCS Class I Drug Using Polymer Matrix System

Fast, Spectroscopy-Based Prediction of In Vitro Dissolution Profile of Extended Release Tablets Using Artificial Neural Networks

The use of the Brouers–Sotolongo fractal kinetic equation for the study of drug release

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