Ginger Extract-Loaded Solid Dispersion System with Enhanced Oral Absorption and Antihypothermic Action

2017 ◽  
Vol 65 (7) ◽  
pp. 1365-1370 ◽  
Author(s):  
Hideyuki Sato ◽  
Mizuki Ogino ◽  
Keisuke Yakushiji ◽  
Hiroki Suzuki ◽  
Ken-ichi Shiokawa ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Ginger Extract ◽  
Dispersion System

Megestrol acetate-loaded self-micellizing solid dispersion system for improved oral absorption and reduced food effect

2019 ◽  
Vol 49 ◽  
pp. 586-593
Author(s):  
Shimul Halder ◽  
Hiroki Suzuki ◽  
Yoshiki Seto ◽  
Hideyuki Sato ◽  
Satomi Onoue
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Food Effect ◽  
Megestrol Acetate ◽  
Dispersion System

scholarly journals Preparation, characterization and evaluation of the in vivo trypanocidal activity of ursolic acid-loaded solid dispersion with poloxamer 407 and sodium caprate

2015 ◽  
Vol 51 (1) ◽  
pp. 101-109 ◽  
Author(s):  
Josimar Oliveira Eloy ◽  
Juliana Saraiva ◽  
Sérgio de Albuquerque ◽  
Juliana Maldonado Marchetti
Keyword(s):  
Ursolic Acid ◽  
Solid Dispersion ◽  
Oral Absorption ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Drug Dissolution ◽  
Limiting Factors ◽  
Sodium Caprate ◽  
Trypanocidal Activity

Ursolic acid is a promising candidate for treatment of Chagas disease; however it has low aqueous solubility and intestinal absorption, which are both limiting factors for bioavailability. Among the strategies to enhance the solubility and dissolution of lipophilic drugs, solid dispersions are growing in popularity. In this study, we employed a mixture of the surfactants poloxamer 407 with sodium caprate to produce a solid dispersion containing ursolic acid aimed at enhancing both drug dissolution and in vivo trypanocidal activity. Compared to the physical mixture, the solid dispersion presented higher bulk density and smaller particle size. Fourier Transform Infrared Spectroscopy results showed hydrogen bonding intermolecular interactions between drug and poloxamer 407. X-ray diffractometry experiments revealed the conversion of the drug from its crystalline form to a more soluble amorphous structure. Consequently, the solubility of ursolic acid in the solid dispersion was increased and the drug dissolved in a fast and complete manner. Taken together with the oral absorption-enhancing property of sodium caprate, these results explained the increase of the in vivo trypanocidal activity of ursolic acid in solid dispersion, which also proved to be safe by cytotoxicity evaluation using the LLC-MK2 cell line.

scholarly journals ENHANCEMENT OF THE SOLUBILITY AND THE DISSOLUTION RATE OF TAMOXIFEN CITRATE SOLID DISPERSION USING SOLUPLUS BY SOLVENT EVAPORATION TECHNIQUE

2019 ◽  
Vol 12 (1) ◽  
pp. 216 ◽  
Author(s):  
Hayder Hussein Abduljabbar ◽  
Shaimaa Nazar Abd Alhammid
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Oral Absorption ◽  
Fourier Transforms ◽  
Amorphous State ◽  
Solvent Evaporation ◽  
Solubility Behavior ◽  
Tamoxifen Citrate ◽  
Complete Disintegration ◽  
Evaporation Technique

Objective: The aim of the present study was the enhancement in the solubility of tamoxifen citrate using solid dispersion which is considered as a great solution to overcome the poor water solubility behavior of tamoxifen citrate (TMX) by solvent evaporation technique using Soluplus® as a novel carrier then formulate it as an orodispersible tablet.Method: A total of 24 formulas were prepared as a solid dispersion by solvent evaporation method using Soluplus® as a polymeric solubilizer in the ratio of 1:1, 1:3, 1:5, 1:7, and 1:10 then formulated as orodispersible tablets by incorporating three types of superdisintegrants; croscarmellose, crospovidone, and sodium starch glycolate (SSG) with the solid dispersion. Characterization of the formulation was done using differential scanning colorimetry, Fourier transforms infrared spectroscopy, X-ray diffraction, and scanning electron microscope and the best formula was selected according to the disintegration and dissolution tests.Results and Discussion: Formula 22 were selected as the best formula which contains mixed types of superdisintegrants; croscarmellose and SSG with the fastest complete disintegration of 6.5 s and complete dissolution with <2 min.Conclusion: Accordingly, TMX was successfully enhanced its water solubility by converting its crystalline structure into the amorphous state through solid dispersion with Soluplus® and formulated as an orodispersible tablet to improve its oral absorption.

Preparation of fenofibrate solid dispersion using electrospray deposition and improvement in oral absorption by instantaneous post-heating of the formulation

2013 ◽  
Vol 450 (1-2) ◽  
pp. 123-128 ◽  
Author(s):  
Kohsaku Kawakami ◽  
Shaoling Zhang ◽  
Rohit Singh Chauhan ◽  
Narimoto Ishizuka ◽  
Marina Yamamoto ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Oral Absorption ◽  
Electrospray Deposition

scholarly journals Design and Characterization of Phosphatidylcholine-Based Solid Dispersions of Aprepitant for Enhanced Solubility and Dissolution

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 407
Author(s):  
Sooho Yeo ◽  
Jieun An ◽  
Changhee Park ◽  
Dohyun Kim ◽  
Jaehwi Lee
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
Promising Alternative ◽  
Dispersion System ◽  
Enhanced Solubility ◽  
Water Soluble Drugs

This study aimed to improve the solubility and dissolution of aprepitant, a drug with poor aqueous solubility, using a phosphatidylcholine (PC)-based solid dispersion system. When fabricating the PC-based solid dispersion, we employed mesoporous microparticles, as an adsorbent, and disintegrants to improve the sticky nature of PC and dissolution of aprepitant, respectively. The solid dispersions were prepared by a solvent evaporation technique and characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry, and X-ray powder diffraction. The FTIR results showed that aprepitant interacted with the PC carrier by both hydrogen bonds and van der Waals forces that can also be observed in the interaction between aprepitant and polymer carriers. The solid dispersions fabricated with only PC were not sufficient to convert the crystallinity of aprepitant to an amorphous state, whereas the formulations that included adsorbent and disintegrant successfully changed that of aprepitant to an amorphous state. Both the solubility and dissolution of aprepitant were considerably enhanced in the PC-based solid dispersions containing adsorbent and disintegrant compared with those of pure aprepitant and polymer-based solid dispersions. Therefore, these results suggest that our PC-based solid dispersion system is a promising alternative to conventional formulations for poorly water-soluble drugs, such as aprepitant.

Development of a rebamipide solid dispersion system with improved dissolution and oral bioavailability

2014 ◽  
Vol 38 (4) ◽  
pp. 522-533 ◽  
Author(s):  
Roshan Pradhan ◽  
Tuan Hiep Tran ◽  
Ju Yeon Choi ◽  
Im Soon Choi ◽  
Han-Gon Choi ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Dispersion System

scholarly journals Enhancement of Oral Bioavailability of Curcumin by a Novel Solid Dispersion System

2015 ◽  
Vol 16 (6) ◽  
pp. 1327-1334 ◽  
Author(s):  
Liandong Hu ◽  
Yanjing Shi ◽  
Jian Heng Li ◽  
Na Gao ◽  
Jing Ji ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Dispersion System

scholarly journals Amorphous Solid Dispersion of Meloxicam Enhanced Oral Absorption in Rats With Impaired Gastric Motility

2018 ◽  
Vol 107 (1) ◽  
pp. 446-452 ◽  
Author(s):  
Hiroki Suzuki ◽  
Keisuke Yakushiji ◽  
Saori Matsunaga ◽  
Yukinori Yamauchi ◽  
Yoshiki Seto ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Gastric Motility ◽  
Oral Absorption ◽  
Amorphous Solid ◽  
Amorphous Solid Dispersion
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