Studies on Diclofenac -&amp;#946;- Cyclodextrin Inclusion Complexes

Attama, AA; Ndibe, O. N.; Nnamani, Petra O.

doi:10.18579/jpcrkc/2004/3/3/79682

Cited by 6 publications

(4 citation statements)

References 5 publications

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“…Five ml of each molar solution was filled in screw capped vials and the excess quantity of the drug was added to each vial separately. [ 7 14 ] The vials were shaken at an ambient temperature, for 48 hours, using a laboratory shaker (Remi). The supernatant solutions were collected carefully and filtered using Whatman filter paper (No.…”

Section: Methodsmentioning

confidence: 99%

Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes

Ghosh¹,

Biswas²,

Ghosh³

2011

Journal of Young Pharmacists

102

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Silymarin is a hepatoprotective agent, having poor water solubility and oral absorption of about 23 – 47%, leading to low bioavailability of the drug. The aim of the present study is to improve the solubility and dissolution rate and in turn the hepatoprotective activity of the drug, by formulating its inclusion complex with beta (β)-cyclodextrin, using different methods. The phase solubility analysis indicates the formation of 1:1 molar inclusion complex of the drug with beta cyclodextrin. Apparent stability constant for Silymarin (Kc) was 722 K-1 with β-cyclodextrin complex. The inclusion complexes were prepared by four different methods, namely, physical mixing, kneading, co-precipitation, and solvent evaporation. The prepared complexes were characterized using differential scanning colorimetry, scanning electron microscopy, and x-ray diffractometry. The inclusion complex prepared by the co-precipitation methods exhibits an overall best result, with respect to the formulation of sustained release formulations.

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Section: Methodsmentioning

confidence: 99%

Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes

Ghosh¹,

Biswas²,

Ghosh³

2011

Journal of Young Pharmacists

102

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“…Cyclodextrins form inclusion complexes in aqueous media and can improve in vivo formulation dissolution, even if complexation occurs after ingestion. 22 Much research [36][37][38] has focused on describing the improved transport capacity and permeation of drugs from complexes formed with cyclodextrins. The increase of the apparent solubility induces a rise in the thermodynamic activity of the formulation in the transport mechanisms of the cell and, therefore, leads to a rapid release at this level.…”

Section: Discussionmentioning

confidence: 99%

Comparative assessment of effectiveness of ketoprofen and ketoprofen/beta-cyclodextrin complex in two experimental models of inflammation in rats

Grecu¹,

Nastasa²,

Ilie

et al. 2013

Lab Anim

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Oral administration of non-steroidal anti-inflammatory drugs (NSAIDs) can lead to adverse effects such as gastrointestinal distress. The complexation of different groups of active substances with b-cyclodextrin (b-CD) has drawn considerable interest over recent years. The purpose of this study was to analyze the ketoprofen/b-cyclodextrin (K/b-CD) conjugate complex as well as to assess its anti-inflammatory effect after oral administration (doses of 30 mg/m 2 and 15 mg/m 2 of body surface), compared with ketoprofen. The studies were done on two models of experimentally-induced acute inflammation in rats (n ¼ 48, 6/group), by means of intraplantar administration of a 10% aqueous kaolin suspension and intraperitoneal administration of a 1% sodium thioglycolate solution. The dynamics of the acute inflammatory process and the anti-inflammatory effects were monitored using plethysmometric determinations after 3, 6, 9, 12, 24 and 48 h (plantar inflammation), and the absorbance of the exudates (spectrophotometrically read) and nucleated cell counts after 24 h (peritoneal inflammation). The coupling of ketoprofen with b-CD resulted in increased solubility (100% in 60 min) of the newly-formed product, which further resulted in a higher bioavailability compared with ketoprofen (<40% in 120 min). In both models of experimentally-induced inflammation, the K/b-CD complex had a higher anti-inflammatory activity than ketoprofen.

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“…A phase solubility study was performed for 5-fluorouracil drugs in which excess amount of 5-fluorouracil (100 mg) in a conical flask of 50 ml, which already contain β-cyclodextrin different concentration range from 0.25 to 2 mol in distilled water as a media [25,26]. Containers were shaken non-stop for 3 d (24 h) at 30 rpm at 37 °C to attain an equilibrium state [27,28].…”

Section: Phase Solubility Studymentioning

confidence: 99%

An ADDUCT: 5-Fluorouracil INCORPORATED Β-Cd INCLUSION COMPLEX FOR SOLUBILITY AND STABILITY ENHANCEMENT IN DOSAGE FORMS

Singh

DEORA²

2022

Int J App Pharm

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Objective: Current work aimed to enhance solubility and stability of 5-fluorouracil drugs by preparing inclusion complex with β-cyclodextrin. Methods: In this study, inclusion complex preparation ratio selected on the basis of slope and Kc (binding constant) value in between 5-fluorouracil-β-cyclodextrin and best method out of the physical mixture, kneading method, and co-evaporation method for solubility and stability enhancement is selected on the basis of % yield, drug content, dissolution rate study and stability study. Results: Based on the phase solubility graph, a 1:1 ratio was selected for complex formation by Kc value which decided a quite stable form of a complex. The characterization of all three types of inclusion complex was performed by DSC and SEM. It proved that different moiety of the complex was formed, but all are quite stable with negligible interaction. The kneading method as the best inclusion complex at ratio 1:1 was selected after evaluating by performing percent yield and drug content and dissolution rate study for solubility profile and physical appearance, drug content, and drug release study for stability profile. Conclusion: We finally conclude that the Kc value proved that the inclusion complex is quite stable and ready to convert in any dosage form of choice. Inclusion complex formed by kneading method is one of the best options among all three techniques for solubility and stability enhancement of drug, which definitely help for a 5-fluorouracil drug to convert into a better dosage form to treat carcinoma.

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Studies on Diclofenac -β- Cyclodextrin Inclusion Complexes

Cited by 6 publications

References 5 publications

Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes

Preparation and Evaluation of Silymarin β-cyclodextrin Molecular Inclusion Complexes

Comparative assessment of effectiveness of ketoprofen and ketoprofen/beta-cyclodextrin complex in two experimental models of inflammation in rats

An ADDUCT: 5-Fluorouracil INCORPORATED Β-Cd INCLUSION COMPLEX FOR SOLUBILITY AND STABILITY ENHANCEMENT IN DOSAGE FORMS

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