Sertraline-Cyclodextrin Complex Orodispersible Sublingual Tablet: Optimization, Stability, and Pharmacokinetics

Abouhussein, Dalia M N; Nabarawi, Mohamed A. El; Shalaby, Samia; El-Bary, A. Abd

doi:10.1007/s12247-019-09416-1

Cited by 15 publications

(13 citation statements)

References 39 publications

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“…Sertraline hydrochloride (SER) is an anti-depressant drug that belongs to selective serotonin reuptake inhibitors (SSRIs) class. It is widely prescribed for the treatment of major depressive disorders and other mental health disorders including obsessive-compulsive disorder (OCD), panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, and social phobia in a dose range of 25-200 mg/day orally [1,2]. SER is a hydrochloride salt of a weak base (pKa 9.48) that belongs to the biopharmaceutical classification system (BCS) class II drugs which are characterized by poor aqueous solubility that critically limits its dissolution rate.…”

Section: Introductionmentioning

confidence: 99%

“…As a result of low solubility, poor absorption, and extensive first-pass hepatic metabolism, SER shows low oral bioavailability (~ 44%). Thus, there is a great demand for strategies to improve SER bioavailability [2,4]. Moreover, it was reported that direct contact of SER with the upper gastrointestinal tract (GIT) results in many side effects including nausea, vomiting, and regurgitation especially with high doses.…”

Section: Introductionmentioning

confidence: 99%

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Development of a Novel Bilosomal System for Improved Oral Bioavailability of Sertraline Hydrochloride: Formulation Design, In Vitro Characterization, and Ex Vivo and In Vivo Studies

et al. 2022

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This study was proposed to develop an optimized sertraline hydrochloride (SER)–loaded bilosomal system and evaluate its potential for enhancement of drug oral bioavailability. A full 23 factorial design was used to prepare SER-loaded bilosomal dispersions by thin film hydration using span 60, cholesterol (CHL), and sodium deoxycholate (SDC). The investigated factors included the total concentration of span 60 and CHL (X1), span 60:CHL molar ratio (X2), and SER:SDC molar ratio (X3). The studied responses were entrapment efficiency (EE%) (Y1), zeta potential (Y2), particle size (Y3), and in vitro % drug released at 2 (Y4), 8 (Y5), and 24 h (Y6). The selected optimal bilosomal dispersion (N1) composition was 0.5% w/v (X1), 1:1 (X2), and 1:2 (X3). Then, N1 was freeze dried into FDN1 that compared with pure SER for in vitro drug release, ex vivo permeation through rabbit intestine, and in vivo absorption in rats. Moreover, storage effect on FDN1 over 3 months was assessed. The optimal dispersion (N1) showed 68 ± 0.7% entrapment efficiency, − 41 ± 0.78 mV zeta potential, and 377 ± 19 nm particle size. The freeze-dried form (FDN1) showed less % drug released in simulated gastric fluids with remarkable sustained SER release up to 24 h compared to pure SER. Moreover, FDN1 showed good stability, fivefold enhancement in SER permeation through rabbit intestine, and 222% bioavailability enhancement in rats’ in vivo absorption study compared to pure SER. The SER-loaded bilosomal system (FDN1) could improve SER oral bioavailability with minimization of gastrointestinal side effects. Graphical abstract

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Development of a Novel Bilosomal System for Improved Oral Bioavailability of Sertraline Hydrochloride: Formulation Design, In Vitro Characterization, and Ex Vivo and In Vivo Studies

et al. 2022

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“…Patents for tablets account for 188 files and are in the third place of importance after aqueous solutions and powders, also reflected in the communities formed through this word within the networks discussed before. Indeed, research around the multifunctional performance of CDs for oral, buccal, and sublingual tablets [ 99 , 100 ] would strengthen these technologies in the short term.…”

Section: Resultsmentioning

confidence: 99%

When Cyclodextrins Met Data Science: Unveiling Their Pharmaceutical Applications through Network Science and Text-Mining

et al. 2021

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We present a data-driven approach to unveil the pharmaceutical technologies of cyclodextrins (CDs) by analyzing a dataset of CD pharmaceutical patents. First, we implemented network science techniques to represent CD patents as a single structure and provide a framework for unsupervised detection of keywords in the patent dataset. Guided by those keywords, we further mined the dataset to examine the patenting trends according to CD-based dosage forms. CD patents formed complex networks, evidencing the supremacy of CDs for solubility enhancement and how this has triggered cutting-edge applications based on or beyond the solubility improvement. The networks exposed the significance of CDs to formulate aqueous solutions, tablets, and powders. Additionally, they highlighted the role of CDs in formulations of anti-inflammatory drugs, cancer therapies, and antiviral strategies. Text-mining showed that the trends in CDs for aqueous solutions, tablets, and powders are going upward. Gels seem to be promising, while patches and fibers are emerging. Cyclodextrins’ potential in suspensions and emulsions is yet to be recognized and can become an opportunity area. This is the first unsupervised/supervised data-mining approach aimed at depicting a landscape of CDs to identify trending and emerging technologies and uncover opportunity areas in CD pharmaceutical research.

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“…For SLT, super disintegrants affect the rate of dissolution. The dissolution (USP type I) apparatus contain 900 ml buffer pH 6.8 (Abouhussein et al, 2019;Pandey et al, 2010) at 37 ± 0.5 • C temperature and the shaft rotate at 100 rpm. Randomly selected tablets from each batch have been considered for the dissolution test.…”

Section: In Vitro Dissolution Studymentioning

confidence: 99%

Development of Nifedipine sublingual tablets using disintegrants as release modifiers

Swapna

Maheswaramma

Hemalatha³

et al. 2020

ijrps

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The current study mainly focused on treating cardiovascular diseases such as angina pectoris and chronic hypertension by modifying the existing commercial tablet available for Nifedipine. The limitation of Nifedipine is poor solubility, which comes under BCS class II drug category, which needs improvement in formulation to achieve better bioavailability. The objective of this research work is to enhance the oral bioavailability (first-pass metabolism in the liver (42–56%)) of Nifedipine by improving dissolution property. Sublingual fast dissolving tablets of Nifedipine formulated by sublimation method, designed to increase its disintegration time in the presence of saliva. This formulation is helpful for paediatric and geriatric patients who are unable to swallow the conventional tablet. Sublimation of camphor makes the tablet more porous and improve disintegration time as well. The direct compression method is used with different ratio of Croscarmellose Sodium (CS) and Sodium Starch Glycolate (SSG) as super disintegrants to formulate Nifedipine loaded Sublingual tablets. All formulations contain various ratio between super disintegrants and camphor, followed by the sublimation method. FTIR and DSC studies were conducted to investigate compatibility between drugs and disintegrants. Formulated tablets were subjected for precompression parameters, e.g., bulk density, tapped density, Carr’s index, Hausner’s ratio, angle of repose and for post-compression parameters, e.g. weight variation, thickness, hardness, friability, drug content, wetting time, disintegration time followed by dissolution study and found satisfactory as per IP.

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Sertraline-Cyclodextrin Complex Orodispersible Sublingual Tablet: Optimization, Stability, and Pharmacokinetics

Cited by 15 publications

References 39 publications

Development of a Novel Bilosomal System for Improved Oral Bioavailability of Sertraline Hydrochloride: Formulation Design, In Vitro Characterization, and Ex Vivo and In Vivo Studies

Development of a Novel Bilosomal System for Improved Oral Bioavailability of Sertraline Hydrochloride: Formulation Design, In Vitro Characterization, and Ex Vivo and In Vivo Studies

When Cyclodextrins Met Data Science: Unveiling Their Pharmaceutical Applications through Network Science and Text-Mining

Development of Nifedipine sublingual tablets using disintegrants as release modifiers

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