Coamorphization combined with complexation enhances dissolution of lurasidone hydrochloride and puerarin with synchronized release

Frerking, Matthew, Salvador Borges, and Martin Wilson. Are some minis multiquantal? J. Neurophysiol. 78: 1293–1304, 1997. The amplitude distribution of miniature postsynaptic currents (minis) in many central neurons has a large variance and positive skew, but the sources of this variance and skew are unresolved. Recently it has been proposed that spontaneous Ca2+ influx into a presynaptic bouton with multiple release sites could cause spontaneous multiquantal minis by synchronizing release at all sites in the bouton, accounting for both the large variance and skew of the mini distribution. We tested this hypothesis by evoking minis with internally perfused, buffered Ca2+ and the secretagogue α-latrotoxin, both in the absence of external Ca2+. With these manipulations, the synchronized release model predicts that the mini distribution should collapse to a Gaussian distribution with a reduced coefficient of variation. Contrary to this expectation, we find that mini amplitude distributions under these conditions retain a large variance and positive skew and are indistinguishable from amplitude distributions of depolarization-evoked minis, strongly suggesting that minis are uniquantal.

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Optimization of Nanostructured Lipid Carriers of Lurasidone Hydrochloride Using Box-Behnken Design for Brain Targeting: In Vitro and In Vivo Studies

Journal of Pharmaceutical Sciences ◽

10.1016/j.xphs.2019.05.001 ◽

2019 ◽

Vol 108 (9) ◽

pp. 3082-3090 ◽

Cited By ~ 11

Author(s):

Imrana Jazuli ◽

Annu ◽

Bushra Nabi ◽

Thasleem moolakkadath ◽

Tausif Alam ◽

...

Keyword(s):

Nanostructured Lipid Carriers ◽

In Vivo Studies ◽

Brain Targeting ◽

Box Behnken Design ◽

Lurasidone Hydrochloride

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Synchronized release of dopamine and serotonin in the medial and lateral hypothalamus of rats

Neuroscience ◽

10.1016/s0306-4522(00)00374-2 ◽

2000 ◽

Vol 101 (3) ◽

pp. 657-663 ◽

Cited By ~ 46

Author(s):

S.O Fetissov ◽

M.M Meguid ◽

C Chen ◽

G Miyata

Keyword(s):

Lateral Hypothalamus ◽

Synchronized Release

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Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals

AAPS PharmSciTech ◽

10.1208/s12249-015-0449-z ◽

2015 ◽

Vol 17 (5) ◽

pp. 1150-1158 ◽

Cited By ~ 15

Author(s):

Sunny Shah ◽

Bhavin Parmar ◽

Moinuddin Soniwala ◽

Jayant Chavda

Keyword(s):

Design Optimization ◽

Lurasidone Hydrochloride

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Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets

Asian Journal of Organic & Medicinal Chemistry ◽

10.14233/ajomc.2019.ajomc-p209 ◽

2019 ◽

Vol 4 (2) ◽

pp. 121-129

Author(s):

Satya Sankar Sahoo ◽

Chandu Babu Rao

Keyword(s):

Patient Compliance ◽

Oral Drug Delivery ◽

Particle Diameter ◽

Water Soluble ◽

In Vivo Studies ◽

Oral Drug ◽

Water Soluble Drugs ◽

Fast Disintegrating Tablets ◽

Lurasidone Hydrochloride

Formulation of poorly water-soluble drugs for oral drug delivery has always been a difficult task for formulation scientists. Lurasidone hydrochloride is one such agent which is used to control bipolar depre-ssion. The objective of this study was to formulate and optimize lurasi-done nanosuspension, further formulating optimized nanosuspensions as fast disintegrating tablets for improved patient compliance. In the present study, lurasidone nanosuspension was prepared by nanomilling technique. Optimized nanosuspension has mean particle diameter of 248.9 nm, polydispersity index of 0.127 and zeta potential of 18.1 mV. The lyophilized optimized nanocrystals, optimize nanosuspension as granulating fluid and as top spraying dispersion for granulation in fluid bed granulator being used to formulate fast disintegrating tablets with suitable super disintegrant. Croscarmellose sodium was found to be best superdisintegrant compared to sodium starch glycolate and crospovidone, as its acts by both mechanism swelling and wicking. Its swells 4-8 folds in less than 10 s. Many folds increase in the rate of drug release observed compare to micronized lurasidone and marketed product. There was no change in crystalline nature after nanomilling as characterized by XRD and FTIR, and it was found to be chemically stable with high drug content. The developed fast disintegrating tablets would be an alternative better formulation than its conventional formulation to address its bioavailability issue and for improved patient compliance. However, this should be further confirmed by appropriate in vivo studies.

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