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Development, characterization, comparative pharmacokinetic and pharmacodynamic studies of iloperidone solid SMEDDS and liquisolid compact.

Published on Mar 12, 2020in Drug Development and Industrial Pharmacy2.367
· DOI :10.1080/03639045.2020.1742142
Dinesh Suram1
Estimated H-index: 1
(Kakatiya University),
Arjun Narala2
Estimated H-index: 2
(Kakatiya University),
Kishan Veerabrahma9
Estimated H-index: 9
(Kakatiya University)
Abstract
Abstract:Iloperidone (ILO) is an anti-psychotic, used in schizophrenia. It has low bioavailability (36%) due to low solubility and first pass effect. Oral solid self microemulsifying drug delivery ...
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References49
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#1Mitali H. Patel (MSU: Maharaja Sayajirao University of Baroda)H-Index: 3
#2Krutika K. Sawant (MSU: Maharaja Sayajirao University of Baroda)H-Index: 24
Abstract The global aim of this research was to develop and evaluate self-microemulsifying drug delivery system (SMEDDS) to improve oral bioavailability of Lurasidone Hydrochloride (LH). A chylomicron flow blocking approach was used to evaluate lymphatic drug transport. The developed LH-SMEDDS was composed of Capmul MCM C8 (oil), Cremophor EL (surfactant) and Transcutol HP (co-surfactant). Highest microemulsifying area was obtained at 3:1 ratio (surfactant:cosurfactant) and mean globule size was...
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#1Dong Shik KimH-Index: 10
#2Jung Hyun ChoH-Index: 1
Last. Dong Wuk KimH-Index: 17
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#1Ho Yong Son (CAU: Chung-Ang University)H-Index: 3
#2Bo Ram Chae (CAU: Chung-Ang University)H-Index: 4
Last. Young Wook Choi (CAU: Chung-Ang University)H-Index: 24
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To improve the dissolution behavior of telmisartan (TMS), a poorly water-soluble angiotensin II receptor blocker, TMS-phospholipid complex (TPC) was prepared by solvent evaporation method and characterized by differential scanning calorimetry and powder X-ray diffractometry. The crystalline structure of TMS was transited into an amorphous state by TPC formation. The equilibrium solubility of TPC (1.3–6.1 mg/mL) in various vehicles was about 100 times higher than that of TMS (0.009–0.058 mg/mL). ...
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#1Katla Venu Madhav (Kakatiya University)H-Index: 1
#2Veerabrahma Kishan (Kakatiya University)H-Index: 8
The objective was to study the phase behavior of different formulations, to identify the micro emulsion area and to prepare solid SMEDDS particles (SSMED) of loratadine (LOR) for improving oral bioavailability (BA). Formulations were prepared with either Lauroglycol 90 or Peceol as oils, Solutol HS15 as surfactant and Transcutol P as co-surfactant. Then water titrations were done to know the phase behavior to identify microemulsion zone. The SSMEDs were prepared by physical adsorption on novel s...
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#1Hamzah M. Beakawi Al-Hashemi (UPM: King Fahd University of Petroleum and Minerals)H-Index: 1
#2Omar Saeed Baghabra Al-Amoudi (UPM: King Fahd University of Petroleum and Minerals)H-Index: 25
Abstract The abundance of granular materials and powders that are being used in several fields, along with their broad applications, requires a comprehensive understanding of both their macro- and micro-mechanical behavior. The fabric and structural properties, or the inter-particle properties, such as the angle of repose, do affect the behavior of granular materials. This comprehensive review indicates that the angle of repose of granular material is an essential parameter to understand the mic...
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#1Fang Li (Anhui University of Chinese Medicine)H-Index: 1
#2Rongfeng HuH-Index: 2
Last. Jihui Tang (Anhui Medical University)H-Index: 2
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Abstract Huperzine A (Hup-A) is a poorly water-soluble drug with low oral bioavailability. A self-microemulsifying drug delivery system (SMEDDS) was used to enhance the oral bioavailability and lymphatic uptake and transport of Hup-A. A single-pass intestinal perfusion (SPIP) technique and a chylomicron flow-blocking approach were used to study its intestinal absorption, mesenteric lymph node distribution and intestinal lymphatic uptake. The value of the area under the plasma concentration–time ...
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#1Mei Lu (SPU: Shenyang Pharmaceutical University)H-Index: 4
#2Haonan Xing (SPU: Shenyang Pharmaceutical University)H-Index: 7
Last. Pingtian Ding (SPU: Shenyang Pharmaceutical University)H-Index: 5
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Abstract Most of the newly developed drug candidates are lipophilic and poorly water-soluble. Enhancing the dissolution and bioavailability of these drugs is a major challenge for the pharmaceutical industry. Liquisolid technique, which is based on the conversion of the drug in liquid state into an apparently dry, non-adherent, free flowing and compressible powder, is a novel and advanced approach to tackle the issue. The objective of this article is to present an overview of liquisolid techniqu...
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#1Ahmed Khames (Beni-Suef University)H-Index: 1
AbstractBCS class II drugs usually suffer inadequate bioavailability as dissolution step is the absorption rate limiting step. In this work, the effect of solubility increase at the main absorption site for these drugs was investigated using risperidone as a drug model. Liquisolid technique was applied to prepare risperidone per-oral tablets of high dissolution rate at intestinal pH (6.8) using versatile nonionic surfactants of high solubilizing ability [Transcutol HP, Labrasol and Labrasol/Labr...
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#1Venu Madhav Katla (Kakatiya University)H-Index: 1
#2Kishan Veerabrahma (Kakatiya University)H-Index: 9
Abstract The objective of the study was to develop solid self micro emulsifying drug delivery system (SSMED) for enhancement of oral bioavailability of losartan (LOS). Solubility of LOS in various vehicles was determined. Micro emulsion region was identified by constructing phase diagram containing surfactant: co-surfactant mixture (1:1 and 2:1), oil and water. Formulations were initially checked for droplet size upon addition to water. The formulations, which resulted in in vitro dissolution. T...
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#1Marzia Cirri (UniFI: University of Florence)H-Index: 30
#2Alessandra RoghiH-Index: 1
Last. Paola Mura (UniFI: University of Florence)H-Index: 47
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Abstract The aim of this work was to develop effective fast-dissolving tablet formulations of glyburide, endowed with improved dissolution and technological properties, investigating the actual effectiveness of the Solid-Self MicroEmulsifying Drug Delivery System (S-SMEDDS) approach. An initial screening aimed to determine the solubility of the drug in different oils, Surfactants and CoSurfactants allowed the selection of the most suitable components for liquid SMEDDS, whose relative amounts wer...
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