Improving the solubility of ampelopsin by solid dispersions and inclusion complexes

Ruan, Liping; Yu, Boyang; Fu, Guangmiao; Zhu, Daling

doi:10.1016/j.jpba.2005.01.030

Cited by 133 publications

(88 citation statements)

References 21 publications

(19 reference statements)

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“…The presence of hydrogen bonds and hydrophobic interactions between LPSF/FZ4 and the hydrophilic polymers in the solid dispersions is the primary cause of the rise in its solubility and dissolution. The basic mechanism is the effect of these interactions on the dimensions of particles and their distribution, as reported in other studies (22)(23)(24)(25)(26).…”

Section: Ftirmentioning

confidence: 70%

Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Guedes¹,

Oliveira²,

Hernandes³

et al. 2011

AAPS PharmSciTech

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Abstract. Solid dispersions have been used as a strategy to improve the solubility, dissolution rate, and bioavailability of poor water-soluble drugs. The increase of the dissolution rate presented by (5Z)-3-(4-chloro-benzyl)-5-(4-nitro-benzylidene)-imidazolidine-2,4-dione (LPSF/FZ4) from the solid dispersions is related to the existence of intermolecular interactions of hydrogen bond type (>N-H ... O<) between the amide group (>N-H) of the LPSF/FZ4 and the ether group (-O-) of the polyethyleneglycol polymer, or the carbonyl (C=O) of the polyvinylpyrrolidone polymer (PVP). The intensity of these interactions is directly reflected in the morphology acquired by LPSF/FZ4 in these systems, where a new solid phase, in the form of amorphous aggregates of irregular size, was identified through scanning electron microscopy and confirmed in the characterizations achieved using X-ray diffraction and thermal analysis of DSC. The solid dispersions with the polymer PVP, in higher concentrations, were revealed to be the best option to be used in the formulations of LPSF/FZ4 in both theoretical and experimental studies.

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Section: Ftirmentioning

confidence: 70%

Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Guedes¹,

Oliveira²,

Hernandes³

et al. 2011

AAPS PharmSciTech

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“…It seems that when the carbonyl group is joined by hydrogen bonds, the stretching band is shifted to lower frequency due to the weakening of the carbonyl radical double bond. This change also indicates that the vibration of the guest molecule (drug) is restricted due to the formation of an inclusion complex (19,20). …”

Section: Solid State Studiesmentioning

confidence: 98%

Characterization of ternary complexes of meloxicam-HPβCD and PVP or L-arginine prepared by the spray-drying technique

Elmaradny¹,

Mortada²,

Kamel³

et al. 2008

Acta Pharmaceutica

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Cyclodextrins and their derivatives play an important role in improving the therapeutic efficacy of drugs with poor solubility and/or stability problems. They are capable of alleviating the undesirable properties of drug molecules through the formation of inclusion complexes (1). Hydroxypropyl-b-cyclodextrin (HPbCD) is mainly selected for its higher solubility than other cyclodextrins and this generally results in more extensive solubilization ability toward lipophilic molecules, with a good safety profile (2). Ternary complexes of meloxicam (ME) (a poorly water soluble anti-inflammatory drug) with hydroxypropyl-b--cyclodextrin (HPbCD) and either a hydrophilic polymer, namely, polyvinyl pyrrolidone (PVP) or a basic amino acid such as L-arginine, were prepared by the spray-drying technique. The solubilizing efficiency, physical properties and dissolution behaviour of each ternary system of ME--HPbCD with either PVP or L-arginine were compared with those of the corresponding binary system of ME--HPbCD. Tablets compressed from the ternary system of ME-HPbCD-L-arginine were compared with plain and commercial tablets. Phase solubility experiments suggested the formation of an inclusion complex of A L type. Ternary system of ME-HPbCD-L-arginine exhibited a stability constant 30.3 times higher than the binary system of ME-HPbCD, while the ternary system of ME-HPbCD--PVP increased the stability constant 2.2 times only. The prepared complexes were characterized by scanning electron microscopy, differential scanning calorimetry and infra red spectroscopy. Ternary solid complexes indicated the presence of strong interactions between the components. The dissolution behaviour of ME from different ternary complexes was higher than its dissolution from the binary system. Tablets compressed from ternary complexes of ME-HPbCD-L-arginine highly improved drug release compared to plain and commercial tablets.

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“…DSC thermogram of EZE (Figure 4a) In thermograms of solid dispersions (Figures 4c, 4e, and 4g), the sharp melting peak of pure EZE was not visible, which might be because of complete dissolution of EZE in the melted polymer (1,20,21). DSC spectra of PEG 4000, PEG 6000, and Gelucire 44/14 show the dehydration peaks of lactose monohydrate at 148.17, 148.23, and 152.02 °C and decomposition peaks at 213.77, 215.09, and 221.54 °C, respectively.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 99%

Studies in Dissolution Enhancement of Ezetimibe by Solid Dispersions in Combination with a Surface Adsorbent

Parmar¹,

Shah²,

Sheth³

2011

Dissolution Technol.

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The aim of this investigation was to improve the dissolution properties of the water-insoluble drug ezetimibe (EZE) and potentially improve bioavailability. A combination of melt and adsorption techniques was employed for the preparation of solid dispersions. PEG 4000, PEG 6000, and Gelucire 44/14 were used as hydrophilic carriers, and lactose monohydrate was used as an adsorbent. Phase solubility curves are of A L type, indicating a linear relationship between drug solubility and carrier concentration. Dissolution studies reveal an improvement of in vitro drug release. Mathematical modeling indicates that drug release data are best described by the Korsmeyer-Peppas model, with Fickian diffusion as the possible drug-release mechanism. Physicochemical characterization of solid dispersions by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) suggests a reduction in drug crystallinity following dissolution enhancement. Hence, the present investigation reveals that the dissolution characteristics of EZE could be ameliorated in a solid dispersion.

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Improving the solubility of ampelopsin by solid dispersions and inclusion complexes

Cited by 133 publications

References 21 publications

Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Solid Dispersions of Imidazolidinedione by PEG and PVP Polymers with Potential Antischistosomal Activities

Characterization of ternary complexes of meloxicam-HPβCD and PVP or L-arginine prepared by the spray-drying technique

Studies in Dissolution Enhancement of Ezetimibe by Solid Dispersions in Combination with a Surface Adsorbent

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