Development and Characterization of Zaleplon Solid Dispersion Systems: A Technical Note

Waghmare, Atish; Pore, Yogesh; Kuchekar, Bhanudas S.

doi:10.1208/s12249-008-9077-1

Cited by 26 publications

(13 citation statements)

References 27 publications

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“…All water used was deionized and then twice distilled in an all-glass apparatus, first from an alkaline solution of KMnO 4 . Zaleplon (99.7 % purity) was kindly donated by Belupo d. d. (Croatia).…”

Section: Methodsmentioning

confidence: 99%

“…3 The drug is a lipophilic compound which is virtually insoluble in water. 4 It has been recognised that a certain level of aqueous solubility is required of the drug substance to be readily delivered to the cellular membrane, but at the same time it has to be lipophilic enough to cross the membrane itself. In the case of lipophilic compounds such as ZAL, the dissolution in gastrointestinal media is often a ratelimiting step for the absorption, thus limiting the oral bioavailability of the drug.…”

Section: Zaleplon (Zal) N-mentioning

confidence: 99%

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Stability and Structure of Inclusion Complexes of Zaleplon with Natural and Modified Cyclodextrins

Jablan¹,

Weitner²,

Gabričević³

et al. 2011

Croat. Chem. Acta

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Abstract. The interaction between zaleplon (ZAL) and different cyclodextrins in aqueous solutions was investigated by spectrofluorimetric and phase solubility studies. Stability constants determined by both methods showed that among natural cyclodextrins, β-cyclodextrin (βCD) formed the most stabile complex but its solubilizing efficiency was limited. Among βCD derivatives, the complex stability and solubilisation efficiency decreased in order: randomly methylated-βCD (RAMEB) > sulphobutylether-βCD (SBEβCD ) > hydroxypropyl-βCD (HPβCD). The inclusion complexes of ZAL with βCD and RAMEB were further characterised by 1 H-NMR spectroscopy and the inclusion complex formation was confirmed in both cases. ROESY spectra showed two binding modes between ZAL and βCD which exist simultaneously in the solution. The first binding mode occurs by the inclusion of the phenyl ring of ZAL into the βCD central cavity via the wider rim of the cyclodextrin cone and is dominant. The second one is formed by the inclusion of pyrazolo[1,5-a]pyrimidine ring of ZAL.(doi: 10.5562/cca1800)

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Section: Methodsmentioning

confidence: 99%

Section: Zaleplon (Zal) N-mentioning

confidence: 99%

Stability and Structure of Inclusion Complexes of Zaleplon with Natural and Modified Cyclodextrins

Jablan¹,

Weitner²,

Gabričević³

et al. 2011

Croat. Chem. Acta

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“…The oral bioavailability is approximately 30% because it undergoes significant presystemic metabolism. [13] Zaleplon is rapidly absorbed after oral administration, its poor aqueous solubility (practically insoluble) can make its absorption dissolution rate limited and thus delay onset of action. The dissolution of drugs is a prime determinant in the absorption of poorly water-soluble drugs and also serves as a rate-limiting step.…”

Section: Introductionmentioning

confidence: 99%

“…The dissolution of drugs is a prime determinant in the absorption of poorly water-soluble drugs and also serves as a rate-limiting step. [13] The major disadvantage of Zaleplon is high dose and also causes for occurrence of (typically short-lived) hallucinations. It is now withdrawn from the market due to the high dose and inefficient therapeutic activity.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Sakhare¹

2017

AJP

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Objectives: The purpose of present research work was to develop mucoadhesive microparticles of Zaleplon for nasal delivery with the aim to avoid hepatic first-pass metabolism, improve therapeutic efficacy and enhance residence time in the treatment of insomnia. Materials and Methods: Chitosan-based microparticles were prepared by the coacervation method by varying the drug:polymer ratio. The microparticles were evaluated for particle size and shape and surface morphology by scanning electron microscopy, drug content, drug entrapment efficiency, swelling study, in vitro mucoadhesion, differential scanning calorimetric (DSC), X-ray diffraction (XRD), Fourier transform infrared (FTIR), in vitro drug release study, and ex vivo drug permeation. Results: Zaleplon microparticles showed irregular-shaped particles and particle size was found to be in the range of 4.97-10.6 μm, which is favorable for intranasal absorption. The prepared microparticles exhibited a good swelling index. The percentage drug content and entrapment efficiency was found to be in the range between 36.36% -80% and 37.65% -52.88%, respectively. In vitro mucoadhesion was performed by adhesion number using goat nasal mucosa and was observed in a range from 43.33 ± 4.409 to 75 ± 2.886%. It was observed that polymer concentration enhancement led to increased mucoadhesive strength. The results of DSC and XRD studies revealed the molecular amorphous dispersion of Zaleplon into the chitosan microparticles. IR spectra of Zaleplon along with excipient showed no interaction between Zaleplon and excipients. In vitro drug release from all the formulations was biphasic, being characterized by a slight "burst" followed by slow release. At the end of 12 h, F6 (1:6) showed drug release of 81.66 ± 1.545%, indicating sustained release. The permeation data of formulation from goat nasal mucosa was found near to that obtained with dialysis membrane in vitro. Conclusion: According to the obtained results, Zaleplon loaded chitosan microparticles prepared by coacervation method proved to be capable of sustained release and could be used through nasal route as an alternative to oral administration.

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“…To overcome the problems caused by poor aqueous solubility of zaleplon, some researchers have developed new drug delivery systems of zaleplon. Zaleplon loaded proliposomes prepared using hydrogenated soyphosphatidylcholine and cholesterol and solid dispersions of zaleplon using different hydrophilic carriers were prepared and have shown enhancement in the dissolution rate of zaleplon [5,6].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Zaleplon Microparticles Using Emulsion Solvent Diffusion Technique

Ibtehal¹,

Omaima²,

Arwa³

et al. 2012

J Pharm Drug Deliv Res

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Zaleplon is a BCS class II drug suffering from poor solubility. In a trial to improve its dissolution, emulsion solvent diffusion method (ESD) was used to prepare zaleplon microparticles using sodium lauryl sulfate (SLS) as surfactant. Optimization of drug system was achieved. Particle size values of the prepared microparticles were ranged from 6.57 μm to 20.30 μm with narrow particle size distribution range. Differential scanning calorimetry (DSC) and x-ray diffraction (XRD) were used for the characterization of the prepared systems. DSC and XRD patterns showed that the zaleplon microparticles possessed decreased crystallinity. Dissolution studies demonstrated that the systemized zaleplon microparticles exhibited significantly enhanced dissolution rate when compared to pure zaleplon. A correlation could be observed between the microparticle morphology and the dissolution rate, where zaleplon microparticles that exhibited the fastest dissolution profiles had a distinctive rod shape compared to the other systems. In contrast, pure zaleplon powder appeared as irregularly-shaped particles. In conclusion, the dissolution rate of zaleplon can be enhanced to a great extent by ESD technique.

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Development and Characterization of Zaleplon Solid Dispersion Systems: A Technical Note

Cited by 26 publications

References 27 publications

Stability and Structure of Inclusion Complexes of Zaleplon with Natural and Modified Cyclodextrins

Stability and Structure of Inclusion Complexes of Zaleplon with Natural and Modified Cyclodextrins

Untitled

Preparation of Zaleplon Microparticles Using Emulsion Solvent Diffusion Technique

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