Enhancing the Hypolipidemic Effect of Simvastatin in Poloxamer-Induced Hyperlipidemic Rats via Liquisolid Approach: Pharmacokinetic and Pharmacodynamic Evaluation

El-Say, Khalid M.; Ahmed, Tarek A.; Ahmed, Osama A. A.; Elimam, Hanan

doi:10.1208/s12249-020-01754-5

Cited by 14 publications

(7 citation statements)

References 56 publications

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“…The in vitro drug release of the prepared 3D-printed tablet formulations was studied using the paddle type USP dissolution test apparatus (type II), DT 700 LH device, Erweka GmbH DT 700 (Heusenstamm, Germany). The test was carried out in 900 mL of distilled water containing 0.1% sodium lauryl sulfate at 37 °C [ 31 , 32 ]. The paddle speed was adjusted at 75 rpm.…”

Section: Methodsmentioning

confidence: 99%

Development of Multi-Compartment 3D-Printed Tablets Loaded with Self-Nanoemulsified Formulations of Various Drugs: A New Strategy for Personalized Medicine

et al. 2021

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This work aimed to develop a three-dimensional printed (3DP) tablet containing glimepiride (GLMP) and/or rosuvastatin (RSV) for treatment of dyslipidemia in patients with diabetes. Curcumin oil was extracted from the dried rhizomes of Curcuma longa and utilized to develop a self-nanoemulsifying drug delivery system (SNEDDS). Screening mixture experimental design was conducted to develop SNEDDS formulation with a minimum droplet size. Five different semi-solid pastes were prepared and rheologically characterized. The prepared pastes were used to develop 3DP tablets using extrusion printing. The quality attributes of the 3DP tablets were evaluated. A non-compartmental extravascular pharmacokinetic model was implemented to investigate the in vivo behavior of the prepared tablets and the studied marketed products. The optimized SNEDDS, of a 94.43 ± 3.55 nm droplet size, was found to contain 15%, 75%, and 10% of oil, polyethylene glycol 400, and tween 80, respectively. The prepared pastes revealed a shear-thinning of pseudoplastic flow behavior. Flat-faced round tablets of 15 mm diameter and 5.6–11.2 mm thickness were successfully printed and illustrated good criteria for friability, weight variation, and content uniformity. Drug release was superior from SNEDDS-based tablets when compared to non-SNEDDS tablets. Scanning electron microscopy study of the 3DP tablets revealed a semi-porous surface that exhibited some curvature with the appearance of tortuosity and a gel porous-like structure of the inner section. GLMP and RSV demonstrated relative bioavailability of 159.50% and 245.16%, respectively. Accordingly, the developed 3DP tablets could be considered as a promising combined oral drug therapy used in treatment of metabolic disorders. However, clinical studies are needed to investigate their efficacy and safety.

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Section: Methodsmentioning

confidence: 99%

Development of Multi-Compartment 3D-Printed Tablets Loaded with Self-Nanoemulsified Formulations of Various Drugs: A New Strategy for Personalized Medicine

et al. 2021

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“…41 By producing a liquisolid, the solubility of poorly soluble medications is increased because the highly porous surface area promotes wetting and molecular dispersion of the drug, which improves its solubility and dissolution. Liquisolids of drugs like ketoprofen, 42 simvastatin, 43 and carvedilol 44 and progesterone 45 etc. are reported in the literature.…”

Section: Techniques For Solubility Improvementmentioning

confidence: 99%

Co-crystallization: a green approach for the solubility enhancement of poorly soluble drugs

Bhatia,

Devi

2024

CrystEngComm

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“…A glimepiride dose of 10 mg/kg was used [42]. Each tablet formulation was crushed and suspended in 1% carboxymethyl cellulose to facilitate its administration to the animals through a gastric tube as previously mentioned with simvastatin liquisolid tablets [43] and rosuvastatin orodispersible tablets [37]. Blood samples (250 µL) were collected from the animals through retro-orbital puncturing under light ether anesthesia at 0.5, 1, 2, 4, 6, 8, 12 and 24 h. The collected plasma samples were immediately separated by centrifugation at 6000 rpm for 10 min and stored at −20 • C. The protocol for this study received prior approval from the Research Ethics Committee, Faculty of Pharmacy, King Abdulaziz University, KSA (Reference No.…”

Section: In Vivo Studymentioning

confidence: 99%

Development of 3D-Printed, Liquisolid and Directly Compressed Glimepiride Tablets, Loaded with Black Seed Oil Self-Nanoemulsifying Drug Delivery System: In Vitro and In Vivo Characterization

et al. 2022

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Glimepiride is characterized by an inconsistent dissolution and absorption profile due to its limited aqueous solubility. The aim of this study was to develop glimepiride tablets using three different manufacturing techniques, as well as to study their quality attributes and pharmacokinetics behavior. Black seed oil based self-nanoemulsifying drug delivery system (SNEDDS) formulation was developed and characterized. Glimepiride liquisolid and directly compressed tablets were prepared and their pre-compression and post-compression characteristics were evaluated. Semi-solid pastes loaded with SNEDDS were prepared and used to develop three-dimensional printing tablets utilizing the extrusion technique. In vivo comparative pharmacokinetics study was conducted on Male Wistar rats using a single dose one-period parallel design. The developed SNEDDS formulation showed a particle size of 45.607 ± 4.404 nm, and a glimepiride solubility of 25.002 ± 0.273 mg/mL. All the studied tablet formulations showed acceptable pre-compression and post-compression characteristics and a difference in their in vitro drug release behavior. The surface of the liquisolid and directly compressed tablets was smooth and non-porous, while the three-dimensional printing tablets showed a few porous surfaces. The inner structure of the liquisolid tablets showed some cracks and voids between the incorporated tablet ingredients while that of the three-dimensional printing tablets displayed some tortuosity and a gel porous-like structure. Most of the computed pharmacokinetic parameters improved with the liquisolid and three-dimensional printed tablets. The relative bioavailabilities of the three-dimensional printed and liquisolid tablets compared to commercial product were 121.68% and 113.86%, respectively. Therefore, the liquisolid and three-dimensional printed tablets are promising techniques for modifying glimepiride release and improving in vivo performance but more clinical investigations are required.

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Enhancing the Hypolipidemic Effect of Simvastatin in Poloxamer-Induced Hyperlipidemic Rats via Liquisolid Approach: Pharmacokinetic and Pharmacodynamic Evaluation

Cited by 14 publications

References 56 publications

Development of Multi-Compartment 3D-Printed Tablets Loaded with Self-Nanoemulsified Formulations of Various Drugs: A New Strategy for Personalized Medicine

Development of Multi-Compartment 3D-Printed Tablets Loaded with Self-Nanoemulsified Formulations of Various Drugs: A New Strategy for Personalized Medicine

Co-crystallization: a green approach for the solubility enhancement of poorly soluble drugs

Development of 3D-Printed, Liquisolid and Directly Compressed Glimepiride Tablets, Loaded with Black Seed Oil Self-Nanoemulsifying Drug Delivery System: In Vitro and In Vivo Characterization

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