Estimation of Dissolution Rate of Salicylamide in Complexing Media Using a Theoretical Diffusion Model

Donbrow, M.; Touítou, Elka

doi:10.1002/jps.2600670124

Cited by 9 publications

(3 citation statements)

References 21 publications

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“…The observed increase in the rate may be due to the increase in solubility, ae expected from Fig. 1, although other factors such as diffusion coefficient, wettability, and the dissociation of the complex in the diesolution medium (17) should be considered in the rate enhancement.…”

Section: Methodsmentioning

confidence: 92%

Inclusion Complexation of Prostaglandin F2α with γ-Cyclodextrin in Solution and Solid Phases

Uekama

Hirayama

Fujise

et al. 1984

Journal of Pharmaceutical Sciences

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Section: Methodsmentioning

confidence: 92%

Inclusion Complexation of Prostaglandin F2α with γ-Cyclodextrin in Solution and Solid Phases

Uekama

Hirayama

Fujise

et al. 1984

Journal of Pharmaceutical Sciences

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“…Various authors suggested that dissolution rates from drug-CD binary systems are also dependent on other factors, such as diffusion and dissociation of the complex in the dissolution medium [13,14] or decrease in crystallinity and enhanced wettability of the drugs by the inclusion complexation [15]. The higher dissolution rate and efficiency values observed with the ME-␥-CD 1:1 and 1:2 M kneaded and coevaporated binary systems when compared with other ME-CD 1:1 and 1:2 M kneaded and coevaporated binary systems may be due to the formation of amorphous solid inclusion complexes as indicated from the DSC and XRD diffractograms.…”

Section: Dissolution Studiesmentioning

confidence: 99%

Physicochemical characterization and dissolution properties of meloxicam–cyclodextrin binary systems

Naidu

Chowdary

Murthy

et al. 2004

Journal of Pharmaceutical and Biomedical Analysis

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The objective of the work is physicochemical characterization of meloxicam (ME)-cyclodextrin (CD) binary systems both in solution and solid states and to improve the dissolution properties of meloxicam via complexation with alpha-, beta- and gamma-cyclodextrins. Detection of inclusion complexation was done in solution state by means of phase solubility analysis, mass spectrometry and 1H nuclear magnetic resonance (NMR) studies, and in solid state using differential scanning calorimetry (DSC), powder X-ray diffractometry, and in vitro dissolution studies. Phase solubility, mass spectrometry and 1H NMR studies in solution state revealed 1:1M complexation of meloxicam with all CDs. A true inclusion of ME with gamma-CD at 1:1 and 1:2M in solid state was confirmed by DSC, powder XRD and scanning electron microscopy (SEM) studies. Dissolution properties of ME-CDs binary systems were superior when compared to pure ME.

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“…The differences observed among the solubilizing effi- ciency and stability constant values did not reflect the similar differences in improving the dissolution rate and efficiency values of the binary systems. Various authors suggested that dissolution rates from drug-CD binary systems are also dependent on other factors, such as diffusion and dissociation of the complex in the dissolution medium 13,14 and decrease in crystallinity and enhanced wettability of the drugs by the inclusion complexation. 15 In the present investigation, mainly crystallinity of the drug along with other factors played an important role in increasing dissolution rate and efficiency values of N-CDs kneaded and coevaporated binary systems as evidenced by RDC values obtained from powder X-RD studies ( Table 4).…”

Section: Dissolution Studiesmentioning

confidence: 99%

Physicochemical characterization and dissolution properties of nimesulide-cyclodextrin binary systems

et al. 2003

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side effects, and a high therapeutic index.1 N is a relatively weak inhibitor of prostaglandin synthesis in vitro and appears to exert its effect through a variety of mechanisms including free radical scavenging, effects on histamine release, the neutrophil myeloperoxidase pathway, bradykinin activity, tumor necrosis factor-a release, cartilage degradation, metalloprotease synthesis, phosphodiesterase type IV inhibition, platelet aggregation, and synthesis of platelet activating factor. It also exhibits a significant selectivity toward cyclooxygenase-2 (COX-2) versus COX-1 inhibition, which may explain the lower incidence of gastric side effects. However, recent findings reported that N has a higher risk of hepatic toxicity when compared to other marketed NSAIDs.2,3 Like many nonsteroidal anti-inflammatory drugs, N is very sparingly soluble in water (≈ 0.01 mg/mL). 4 The poor aqueous solubility and wettability of N gives rise to difficulties in pharmaceutical formulations for oral or parenteral delivery, which may lead to variable bioavailability. To overcome these drawbacks, increasing the aqueous solubility of N is an important goal. Hence, in this investigation, inclusion complexation of N was tried with α-, β-, and γ-cyclodextrins (CDs) with the aim to improve its pharmaceutical properties (ie, aqueous solubility and dissolution properties). ABSTRACTThe objective of this work is physicochemical characterization of nimesulide-cyclodextrin binary systems both in solution and solid state and to improve the dissolution properties of nimesulide (N) via complexation with α-, β, and γ-cyclodextrins (CDs). Detection of inclusion complexation was done in solution by means of phase solubility analysis, mass spectrometry, and 1 H nuclear magnetic resonance ( 1 H-NMR) spectroscopic studies, and in solid state using differential scanning calorimetry (DSC), powder xray diffractometry (X-RD), scanning electron microscopy (SEM), and in vitro dissolution studies. Phase solubility, mass spectrometry and 1 H-NMR studies in solution revealed 1:1 M complexation of N with all CDs. A true inclusion of N with β-CD at 1:2 M in solid state was confirmed by DSC, powder X-RD and SEM studies. Dissolution properties of N-CD binary systems were superior when compared to pure N.

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Estimation of Dissolution Rate of Salicylamide in Complexing Media Using a Theoretical Diffusion Model

Cited by 9 publications

References 21 publications

Inclusion Complexation of Prostaglandin F2α with γ-Cyclodextrin in Solution and Solid Phases

Inclusion Complexation of Prostaglandin F2α with γ-Cyclodextrin in Solution and Solid Phases

Physicochemical characterization and dissolution properties of meloxicam–cyclodextrin binary systems

Physicochemical characterization and dissolution properties of nimesulide-cyclodextrin binary systems

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