Melt sonocrystallization of ibuprofen: Effect on crystal properties

Maheshwari, Manish; Harshal, Jahagirdar; Paradkar, Anant

doi:10.1016/j.ejps.2005.01.013

Cited by 70 publications

(40 citation statements)

References 15 publications

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“…The melt sonocrystallization technique has recently been used for the nonsteroidal anti-inflammatory drug (NSAID) ibuprofen where insonation of the melt, dispersed in water, was carried out at ambient temperature with improvements in solubility, dissolution rate, and compression properties [Manish et al, 2005]. Similarly, Paradkar et al [2006] reported that melt sonocrystallization of the COX-2 inhibitor, celecoxib, demonstrated advantages over other approaches and can be exploited in terms of particle design for drug amorphorization.…”

Section: Introductionmentioning

confidence: 98%

Improvement of physicochemical and biopharmaceutical properties of flurbiprofen using melt sonocrystallization technique

El-Kamel

2008

Drug Development Research

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The aim of the present study was to investigate the suitability of the melt sonocrystallization technique to modify the undesirable properties of the nonsteroidal anti-inflammatory drug (NSAID), flurbiprofen (FBP), e.g., poor flowability, solubility, and dissolution rate and, consequently, poor bioavailability. FBP melt was poured in deionized water at 251C and sonicated for 4 min at an amplitude of 60% and cycle of 40 s on and 10 s off. The product obtained was evaluated using scanning electron microscopy (SEM), image analysis, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), and X-ray powder diffraction (XRPD). Flow properties, intrinsic dissolution rate, solubility, and bioavailability were also evaluated. The particle size of the treated FBP was significantly reduced. Thermal behavior and FT-IR spectra of untreated and treated FBP have shown no significant difference. Low-intensity peaks in the X-ray diffraction of treated FBP were noticed. In addition there was significant enhancement in the flow properties of treated FBP, as indicated by the value of angle of repose and the flow constants calculated from the Kawakita equation. The increased solubility of treated FBP was about 35%. The intrinsic dissolution rate of treated FBP increased by 2-fold. The dissolution rate studies revealed that 90% of the drug was released within 20 min for treated FBP compared with 60% released for the untreated drug. The relative bioavailability of treated FBP was increased by 2-fold compared with untreated drug.The use of melt sonocrystallization technique is a promising technique that may afford powder with improved flow and tablet functionality as well as improved dissolution and bioavailability. Drug Dev Res 69: [34][35][36][37][38][39][40][41] 2008 r2008 Wiley-Liss, Inc.

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Section: Introductionmentioning

confidence: 98%

Improvement of physicochemical and biopharmaceutical properties of flurbiprofen using melt sonocrystallization technique

El-Kamel

2008

Drug Development Research

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“…At this time dug goes into systemic circulation like small intestine where it can be solubilized. So, for this reason, this dosage form can be recommended [42].…”

Section: Floating Granulesmentioning

confidence: 99%

DISSOLUTION AND SOLUBILITY ENHANCEMENT STRATEGIES: CURRENT and NOVEL PROSPECTIVES

Sanjaymitra

Ganesh

2018

JCR

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The solubility is one of the important parameters to achieve the desired concentration of the drug in the systemic circulation in pharmacological response to be shown. The oral route is the most desirable and preferred method of administering therapeutic agents for their systemic effects, but the poor solubility of the drug is a major challenge for formulation scientist. Close to 40% of orally administered drugs suffer from formulation difficulties related to their water insolubility. Dissolution rate, absorption, distribution, and excretion of a moiety depend upon its solubility characteristics. Although several advantages associated with the oral route, the poorly soluble drugs suffer from slow dissolution and poor bioavailability. Based on solubility, drugs are classified into four classes of the BCS classification. Solubility challenges are faced in ClassII and Class IV of the BCS system this is important because most of the generic and NCE drugs come under class II drugs. The solubility behavior of drugs remains one of the most challenging aspects of formulation development. There are several methods available for solubility and dissolution enhancement of poorly water-soluble drugs. The aim of this clause is to distinguish the techniques of solubilization for the acquisition of effective absorption and improved bioavailability.

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“…Difference in the morphology and crystalline structure of unprocessed cefixime and nanoparticles can affect both pharmaceutical and biopharmaceutical properties such as solubility and dissolution profile of the drug. 26 Because, drugs in partial crystalline state tend to have higher dissolution rates since lower energy is needed to break the crystal lattice during the dissolution process. 27 As shown in Figure 6, dissolution rate and the amount of the dissolved drug from optimal nanosuspension were significantly higher than unprocessed cefixime and physical mixture of the drug with PVP.…”

Section: Discussionmentioning

confidence: 99%