Stable solid dispersion of lurasidone hydrochloride with augmented physicochemical properties for the treatment of schizophrenia and bipolar disorder.

Abstract:

:Crystalline solid dispersion of lurasidone hydrochloride (LH) was made with various polar and non-polar small molecules to overcome the poor aqueous solubility issue. LH-Glutathione (GSH) solid dispersion in 1:1 ratio was prepared by co-grinding method and characterized by using differential scanning calorimetry (DSC), powder X-ray diffraction, Fourier transform infrared spectroscopy (FTIR) and Raman spectroscopy. GSH acts as antioxidant and reported for anti-schizophrenic activity may provide synergistic action with LH or reduce the side effects. LH in LH-GSH solid dispersion (SD) has shown improvement in solubility by 7.9 folds than plain drug which translated in terms of improved dissolution rate by two-folds. The in vitro dissolution results showed maximum dissolution rate with LH-GSH SD (97.85 ± 2.40%) compared to plain drug (50.5 ± 3.02%) at 15 min (t15 min, %) and thus, satisfying criteria of immediate release dosage form. DSC and FTIR data confirmed the stability of LH-GSH SD for 3 months at accelerated stability condition (40 ± 2°C and 75 ± 5% RH). The prepared LH-GSH SD can be used as a tool to target dual problems that is, enhanced physicochemical properties along with possible management of disorder which could be due to synergism with co-administered GSH. This approach is thought to be efficiently providing the relief to the psychological patients.

journal_name

Biopharm Drug Dispos

authors

Pardhi VP,Flora S

doi

10.1002/bdd.2252

subject

Has Abstract

pub_date

2020-11-01 00:00:00

pages

334-351

issue

8-9

eissn

0142-2782

issn

1099-081X

journal_volume

41

pub_type

杂志文章
  • Disposition kinetics of disopyramide in patients with renal insufficiency.

    abstract::The pharmacokinetics of an intravenous injection of disopyramide was studied in five normal subjects and six patients with varying degrees of renal impairment. The elimination rate constant (beta) was related to the endogenous creatinine clearance (Clcr). However, a decrease in beta was not observed until the Clcr was...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510010308

    authors: Shen DD,Cunningham JL,Shudo I,Azarnoff DL

    更新日期:1980-01-01 00:00:00

  • Metabolism and disposition of EXP631--a novel antidepressant analgesic.

    abstract::EXP631, 4-(3-thienyl)-alpha, alpha,1-trimethyl-4-piperidine-methanol hemi-fumarate salt (I), is a centrally acting non-opioid analgesic compound with monoamine uptake blocking properties. EXP631 has analgesic effects in several animal models. It is intended to be used for the treatment of moderate to moderately severe...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510140608

    authors: Wong YN,Burcham DL,Huang SM,Quon CY

    更新日期:1993-08-01 00:00:00

  • A pharmacokinetic evaluation of HIV protease inhibitors, cyclic ureas, in rats and dogs.

    abstract::The pharmacokinetics of a series of novel cyclic, non-peptide inhibitors of HIV protease were studied in rats or dogs after intravenous and oral administration. Six symmetrically substituted cyclic urea compounds (XK234, XM311, XM320, XM321, XM323, and XM412), which effectively inhibited HIV virus replication, with IC...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510150702

    authors: Wong YN,Burcham DL,Saxton PL,Erickson-Viitanen S,Grubb MF,Quon CY,Huang SM

    更新日期:1994-10-01 00:00:00

  • Pharmacogenomics of cancer chemopreventive isothiocyanate compound sulforaphane in the intestinal polyps of ApcMin/+ mice.

    abstract::Sulforaphane (SFN) is an isothiocyanate that is present in widely consumed vegetables. Previous studies have shown that SFN is effective in preventing carcinogenesis induced by carcinogens in rodents. Recently it was found that SFN could also suppress the growth of intestinal polyps in the ApcMin/+ mouse. In the prese...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.522

    authors: Khor TO,Hu R,Shen G,Jeong WS,Hebbar V,Chen C,Xu C,Nair S,Reddy B,Chada K,Kong AN

    更新日期:2006-12-01 00:00:00

  • Comparative pharmacokinetics and pharmacodynamics of two marketed bid formulations of diltiazem in healthy volunteers.

    abstract::Cardizem SR and Bi-Tildiem were both approved in their respective countries on the basis of clinical trials demonstrating efficacy and safety in the treatment of angina pectoris. In this cross-over randomized study, we assessed whether these two sustained-release formulations of diltiazem have equivalent pharmacokinet...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/bdd.2510140903

    authors: Guimont S,Landriault H,Klischer K,Grace M,Lambert C,Caillé G,Gossard D,Russell A,Raymond M,Hutchings E

    更新日期:1993-12-01 00:00:00

  • CYP2J2 is the major enzyme in human liver microsomes responsible for hydroxylation of SYL-927, a novel and selective sphingosine 1-phosphate receptor 1 (S1P1 ) agonist.

    abstract::SYL-927, a novel and selective S1P1 agonist, is transferred to its active phosphate for the regulation of lymphocyte recirculation. This in vitro metabolism study is to elucidate the P450-mediated oxidation pathway of SYL-927 in human liver microsomes (HLMs). The results demonstrated that the ω-1 hydroxylated metaboli...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2161

    authors: Yang S,Hu J,Li Y,Zhao Z

    更新日期:2018-11-01 00:00:00

  • Studies on the intravenous pharmacokinetics in rabbit and in vitro protein binding of two new salts of erythromycin: erythromycin maltobionate and erythromycin fumarate.

    abstract::Pharmacokinetics in rabbits following intravenous administration and in vitro protein binding were studied for two new salts of erythromycin (erythromycin maltobionate and erythromycin fumarate). Serum erythromycin levels following intravenous injection were described by two compartment model kinetics, and values for ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510130606

    authors: Basu SK,Manna PK,Goswami BB

    更新日期:1992-08-01 00:00:00

  • Alprazolam hydroxylation by mouse liver microsomes in vitro: the effect of age and phenobarbital induction.

    abstract::The effects of age on hepatic microsomal enzyme induction were studied in male CD-1 mice. Six week old and 1 year old animals were treated with either phenobarbital (80 mg kg-1) or saline once daily for 3d. Twenty-four hours after the last treatment, animals were sacrificed and livers were harvested. Hepatic microsoma...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(199703)18:2<139::aid-bdd7>

    authors: Charpentier KP,von Moltke LL,Poku JW,Harmatz JS,Shader RI,Greenblatt DJ

    更新日期:1997-03-01 00:00:00

  • Influence of acebutolol and metoprolol on cardiac output and regional blood flow in rats.

    abstract::Beta-adrenoceptor blocking drugs are widely used as effective antihypertensive and antianginal agents. We have determined the effect of beta-blockade in the rat to ascertain whether there are differences between metoprolol (MET) and acebutolol (AC) with respect to regional blood flow (RBF). Both AC and MET were admini...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/1099-081x(200005)21:4<121::aid-bdd216>3.0.

    authors: Mostafavi S,Lewanczuk R,Foster R

    更新日期:2000-05-01 00:00:00

  • The effect of oral dose volume on the absorption of a highly and a poorly water-soluble drug in the rat.

    abstract::The influence of dose volume on drug absorption following oral administration of a highly and a poorly water soluble drug was examined in male Sprague-Dawley rats. A constant mass of each 14C-labeled compound was given via gavage in dose volumes of 1, 5, 10, and 20 mL kg-1. Blood levels, as well as the quantitative ex...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510150508

    authors: Nickerson DF,Weaver ML,Tse FL

    更新日期:1994-07-01 00:00:00

  • Determination of the population pharmacokinetic parameters of sustained-release and enteric-coated oral formulations, and the suppository formulation of diclofenac sodium by simultaneous data fitting using NONMEM.

    abstract::Data from sustained-release and enteric-coated oral formulations, and the suppository formulation of diclofenac sodium are fitted simultaneously using NONMEM and the general linear model, ADVAN 5. Absorption and disposition parameters, serum levels, and absorption profiles were determined. The in vivo absorption profi...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(199804)19:3<169::aid-bdd83

    authors: Idkaidek NM,Amidon GL,Smith DE,Najib NM,Hassan MM

    更新日期:1998-04-01 00:00:00

  • Regional gastrointestinal delivery of remogliflozin etabonate in humans.

    abstract::Remogliflozin etabonate (RE) is the prodrug of remogliflozin (R), an inhibitor of renal glucose transport designed to reduce blood glucose concentrations for the treatment of type 2 diabetes. This open-label, randomized, single-dose, four-way crossover study, (with one add-on arm) in eight healthy men evaluated the re...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章,随机对照试验

    doi:10.1002/bdd.1824

    authors: O'Connor-Semmes RL,Sandefer EP,Hussey EK,Tao W,Doll WJ,Page RC,Dobbins R

    更新日期:2013-03-01 00:00:00

  • Uptake of verteporfin by articular tissues following systemic and intra-articular administration.

    abstract::Photodynamic therapy (PDT) using the photosensitizer BPD-Verteporfin (liposomal benzoporphyrin derivative-monoacid ring A) has been shown in previous studies to be effective in the amelioration of inflammatory arthritis in both the MRL-lpr mouse and the New Zealand White (NZW) rabbit models, and could potentially offe...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/(sici)1099-081x(199809)19:6<395::aid-bdd11

    authors: Chowdhary RK,Ratkay LG,Canaan AJ,Waterfield JD,Richter AM,Levy JG

    更新日期:1998-09-01 00:00:00

  • Inhibition of rat hepatic mitochondrial aldehyde dehydrogenase isozymes by repeated cyanamide administration: pharmacokinetic-pharmacodynamic relationships.

    abstract::The inhibition of rat hepatic mitochondrial aldehyde dehydrogenase (ALDH) isozymes was studied in apparent steady-state conditions after repeated intra-peritoneal cyanamide administration. The low-Km mitochondrial ALDH isozyme was more susceptible to cyanamide-induced inhibition (DI50 = 0.104 mg kg-1) than the high-Km...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510140508

    authors: Pruñonosa Piera J,Obach R,Sagristá ML,Bozal J

    更新日期:1993-07-01 00:00:00

  • Pharmacokinetics and pharmacodynamics of furosemide after direct administration into the stomach or duodenum.

    abstract::The pharmacokinetics and pharmacodynamics of furosemide were compared after an oral administration or a direct administration of Lasix into the duodenum in humans (40 mg). Furosemide was absorbed quickly after a direct administration of Lasix into the duodenum; the peak plasma concentration of furosemide was reached w...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/(sici)1099-081x(199712)18:9<753::aid-bdd63

    authors: Lee WI,Yoon WH,Shin WG,Song IS,Lee MG

    更新日期:1997-12-01 00:00:00

  • Disposition of a silicon-containing amide, an inhibitor of acyl-CoA: cholesterol acyltransferase, in dog and rat.

    abstract::The pharmacokinetics of 3-(decyldimethylsilyl)-N-[2-(4-methylphenyl)-1-phenylethyl]propanamide (DMPP), an inhibitor of acyl-CoA:cholesterol acyltransferase, have been studied in the dog and the rat using 14C and 3H dual-labelled drug. In both species, gastrointestinal absorption of DMPP was slow and incomplete, amount...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510080504

    authors: Tse FL,Jaffe JM

    更新日期:1987-09-01 00:00:00

  • The development of a population physiologically based pharmacokinetic model for mycophenolic mofetil and mycophenolic acid in humans using data from plasma, saliva, and kidney tissue.

    abstract:BACKGROUND:Mycophenolic acid (MPA) is used widely to prevent graft rejection in kidney-transplant patients. Therapeutic drug monitoring (TDM) in plasma requires an invasive procedure that is inconvenient, especially in pediatric patients. TDM in saliva is a more convenient non-invasive alternative compared with plasma....

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2206

    authors: Alsmadi MM,Alfarah MQ,Albderat J,Alsalaita G,AlMardini R,Hamadi S,Al-Ghazawi A,Abu-Duhair O,Idkaidek N

    更新日期:2019-11-01 00:00:00

  • Pharmacokinetics of dihydroartemisinin in Artekin tablets for single and repeated dosing in Chinese healthy volunteers.

    abstract::Aim. To study the pharmacokinetics of dihydroartemisinin (DHA) in Artekin (compound dihydroartemisinin) tablets in Chinese healthy volunteers. Methods. Eighteen healthy volunteers (9 males, 9 females) received Artekin tablets for oral administration. The plasma samples of DHA were analysed by liquid-liquid extraction ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/bdd.607

    authors: Hong X,Liu CH,Huang XT,Huang TL,Ye SM,Ou WP,Wang NS,Mi SQ

    更新日期:2008-05-01 00:00:00

  • Pharmacokinetics and pharmacodynamics of furosemide after intravenous and oral administration to spontaneously hypertensive rats and DOCA-salt-induced hypertensive rats.

    abstract::The pharmacokinetics and pharmacodynamics of furosemide were investigated after intravenous (i.v.), 1 mg/100 g body weight, and oral administration, 2 mg per 100 g body weight, to spontaneously hypertensive rats (SHRs) and deoxycorticosterone acetate-salt-induced hypertensive rats (DOCA-salt rats). After i.v. administ...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2510150302

    authors: Jang SH,Lee MG,Kim ND

    更新日期:1994-04-01 00:00:00

  • Bioavailability of propranolol and bendrofluazide formulations.

    abstract::In this comparative bioavailability study in 12 healthy volunteers the blood level profiles of both propranolol and bendrofluazide were studied following the multiple oral administration of the drugs as a fixed combination (Inderetic) and as a free combination at doses of 80 mg propranolol twice daily and 2.5 mg bendr...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/bdd.2510020209

    authors: McAinsh J,Holmes BF,Baber NS,Young J

    更新日期:1981-04-01 00:00:00

  • Exploring the compatibility mechanism of ShengDiHuang Decoction based on the in situ single-pass intestinal perfusion model.

    abstract::Affecting the absorption of active ingredients in the intestine serves as one of the important compatibility mechanisms of traditional Chinese medicine. The aim of this study was to investigate the compatibility mechanism of ShengDiHuang Decoction (SDHD) by using the single-pass intestinal perfusion in situ model. The...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2211

    authors: Yang H,Hao Q,Cheng J,Wang M,Zou J,Zhang X,Guo D

    更新日期:2020-02-01 00:00:00

  • Intravenous administration of paclitaxel in Sprague-Dawley rats: what is a safe dose?

    abstract::Few studies describe the administration of Taxol to rats; however, rats are typically used to study the toxicity of new drugs or novel formulations. A dose finding study was conducted to determine a safe dose of Taxol following intravenous administration in rats. Male Sprague-Dawley rats received a bolus of paclitaxel...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.503

    authors: Shord SS,Camp JR

    更新日期:2006-05-01 00:00:00

  • The relationship between pharmacokinetic behaviour of glycyrrhizin and hepatic function in patients with acute hepatitis and liver cirrhosis.

    abstract::The pharmacokinetic behavior of glycyrrhizin in four patients with acute hepatitis (hepatitis group) and six patients with liver cirrhosis (cirrhosis group) receiving chronically an IV administration of a 120 mg dose once a day or once every other day of glycyrrhizin was investigated. The plasma concentration of glycy...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/bdd.2510160103

    authors: Yamamura Y,Tanaka N,Santa T,Kotaki H,Aikawa T,Uchino K,Osuga T,Sawada Y,Iga T

    更新日期:1995-01-01 00:00:00

  • Prediction of clinical effects of infliximab administered for inflammatory bowel disease based on pharmacokinetic and pharmacodynamic modeling.

    abstract::Infliximab (IFX) is used as a therapeutic agent for ulcerative colitis (UC) and Crohn's disease (CD). Although the dosage regimen has been established through clinical trial experience, it has yet to be assessed with a pharmacokinetic and pharmacodynamic model. The present study analysed sequential changes of clinical...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2198

    authors: Kimura K,Yoshida A,Katagiri F,Takayanagi R,Yamada Y

    更新日期:2019-07-01 00:00:00

  • Stability of cucurbitacin E in human plasma: chemical hydrolysis and role of plasma esterases.

    abstract::It was shown previously that the anticancerous cytotoxic oxygenated triterpenes, cucurbitacin E (Cuc E) and its deacetylated form, cucurbitacin I (Cuc I), interacted differently with human serum albumin. In this study, the biochemical stability of Cuc E was investigated in vitro by reverse-phase high performance liqui...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.673

    authors: Saade M,Magdalou J,Ouaini N,Greige-Gerges H

    更新日期:2009-10-01 00:00:00

  • Influence of dose on the distribution kinetics of ciprofloxacin and ofloxacin in the isolated hindlimb of the rat.

    abstract::The aim of this study was to determine whether the dose influences the distribution kinetics of ciprofloxacin and ofloxacin in muscle- bone- and skin-tissues included in the isolated hindlimb of the rat. Experiments were carried out in the isolated perfused hindlimb of the rat, administering a single dose of 45, 450 o...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.245

    authors: Casquero-Dorado AC,Colino CI,Martínez MS,Sánchez-Navarro A

    更新日期:2000-11-01 00:00:00

  • Effect of concomitant colestipol hydrochloride administration on the bioavailability of diltiazem from immediate- and sustained-release formulations.

    abstract::Effects of concomitant colestipol administration on plasma concentrations of diltiazem and desacetyldiltiazem from immediate-release (IR) and sustained-release (SR) formulations were assessed in two studies. In the first study, 12 subjects received 120-mg diltiazem hydrochloride (diltiazem) SR capsules or 120-mg dilti...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章

    doi:10.1002/bdd.330

    authors: Turner SW,Jungbluth GL,Knuth DW

    更新日期:2002-12-01 00:00:00

  • Intravenous pharmacokinetics, oral bioavailability and dose proportionality of ragaglitazar, a novel PPAR-dual activator in rats.

    abstract::Pharmacokinetics of ragaglitazar (a novel phenoxazine derivative of aryl propanoic acid), a potent insulin sensitizing and lipid-lowering compound was studied in Wistar rats. A single dose of 1, 3 or 10 mg/kg of ragaglitazar was given orally to male rats (n=4 per dose level) to evaluate dose proportionality. In anothe...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.413

    authors: Jagannath K,Chaluvadi MR,Mullangi R,Mamidi NV,Srinivas NR

    更新日期:2004-10-01 00:00:00

  • Pharmacokinetic interaction between flurbiprofen and antacids in healthy volunteers.

    abstract::Gastrointestinal distress resulting from drug intake is often remedied by administering the drug with antacids. However, antacids have been shown to modify the absorption and excretion of many drugs. This study was designed to delineate the effects of aluminium and magnesium hydroxide antacid suspension (Maalox) on th...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1002/bdd.2510100610

    authors: Caillé G,du Souich P,Vézina M,Pollock SR,Stalker DJ

    更新日期:1989-11-01 00:00:00

  • A quantitative threshold for high/low extent of urinary excretion of compounds in humans.

    abstract::In this study, a quantitative threshold was determined for the high/low extent of urinary excretion (UE) of compounds in humans, using a straightforward but robust statistical method known as receiver operating characteristic curve (ROC) analysis, and also 18 potential physicochemical determinants of UE were evaluated...

    journal_title:Biopharmaceutics & drug disposition

    pub_type: 杂志文章

    doi:10.1002/bdd.2013

    authors: Dave RA,Morris ME

    更新日期:2016-07-01 00:00:00