Preparation and characterization of Domperidone- β-cyclodextrin complexes prepared by kneading method.

Swami, Gaurav; Koshy, M K; Pandey, Manisha; Saraf, Shubhini A.

doi:10.5138/ijaps.2010.0976.1055.01008

Cited by 12 publications

(8 citation statements)

References 28 publications

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“…It was performed by KBr pellet technique in which the samples were mixed with previously dried, saturated potassium bromide, and then pressed under a hydraulic pressure of 150 kg/cm 2 to form thin transparent disc pellet. The disc was placed in the IR sample holder and scanned over a range of 3600 to 400 cm -1 at ambient temperature [22,23].…”

Section: Fourier Transforms Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

Effect of Water Content in Kneading Method of Solid Dispersion Technique for Solubility Enhancement

2017

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Objective: The main objective of the research work was to optimize the water requirement/content used in kneading method for solid dispersion/inclusion complex formation between water insoluble drug and polymer.Methods: Nimesulide (model drug) and β-cyclodextrin were taken in a different ratio such as 1:1, 1:3 and 1:5 and, the mixture was triturated well for half hour. Water was incorporated to the mixture in different levels like 75%, 50%, 25% w/v in divided proportions and 0% (no water addition, but the mixture was triturated continuously). After each part of water addition, the mixture was triturated well for 10 min and dried using hot air over for 30 min at 50 °C and sieved using sieve no: 44. The complexes formed were subjected for various analytical characterization studies including solubility, particle size, the angle of repose, tapped density, Carr's index, fourier transform infrared spectrometry (FTIR), thermo gravimetric-differential thermal analysis (TG-TDA), x-ray diffraction (XRD) studies and in vitro dissolution studies. Results:The dissolution studies showed improvement in the release of nimesulide, which depended on the percentage level of water. The solubility of the sample was increased with increasing the concentration of the inclusion complex formed. Kneading method was proved to be a successful technique for formation of stable inclusion complex of nimesulide with β-cyclodextrin. All the formulations exhibited acceptable particle size and solubility in the range of 22.6±2 to 29±5 and 45±5 to 133±3.5 respectively. Conclusion:Nimesulide and β-cyclodextrin complex was successfully prepared and characterized for the drug-polymer stability and interactions. The result confirmed that the liquid content in the solid dispersion prepared by the kneading method played an important role in the dissolution of the poorly soluble drug.

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Section: Fourier Transforms Infrared Spectroscopy (Ftir)mentioning

confidence: 99%

Effect of Water Content in Kneading Method of Solid Dispersion Technique for Solubility Enhancement

2017

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“…Nasal route as an alternative to oral route has recently gained much importance due to its advantages like; ease of administration, improved patience compliance, higher effective surface area and rapid onset of action. 6 Despite of such advantages, nasal route possess several limitations like; limited nasal delivery volume (≤ 300µl) only single space between ≤ and 300, nasal irritation due to pH of developed formulation, solubility of drug component in limited nasal delivery volume and molecular weight of the drug molecule. 7 Hence, preformulation study is necessary to check the suitability of drug candidate for nasal formulation which is stable, safe and effective.…”

Section: Introductionmentioning

confidence: 99%

Preformulation Study of Domperidone: An Insight for Formulation and Development of Nasal Formulation

Rathod¹,

Suthar²,

Patel³

et al. 2018

IJPRS

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Preformulation is a group of studies that focus on the physicochemical properties of a new drug candidate that could affect the drug performance and the development of a dosage form. This could provide important information for formulation design or support the need for molecular modification. So, in the present study preformulation studies were performed on Domperidone (DM) to assess its suitability for nasal formulation. Domperidone is a peripherally acting dopamine D2 receptor antagonist which has high first pass metabolism after oral administration. The authenticity of DM was established by DSC and FITR spectra. An UV spectrophotometric method and LC-MS method were employed for determination of DM in bulk and blood plasma respectively. Saturation solubility, micromeritical properties, melting point, pH, hygroscopicity, and stability profile were studied. The UV method was linear in the range of 5-50 μg/ml. The low % CV values of intra-day and inter-day variations revealed that the proposed method is robust. The retention time of DM in LC-MS method was found to be 2.6 min. The method was proven robust by obtaining very high regression coefficient value (0.999). The results of the physicochemical study of drug revealed suitability of DM for nasal route. Moreover, the drug was found stable in different conditions.

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“…PEG 4000, PEG 6000 and Myrj 52 by melt granulation technique. In addition, multicomponent inclusion complexes of DMP were prepared using native cyclodextrin, cyclodextrin derivatives, hydroxypropyl cellulose, citric acid and other polymers by kneading method resulting in almost 92 to 100% of domperidone released after 5 to 60 min (Ghodke et al, 2009;Swami et al, 2010;Chavan et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of binary and ternary solid dispersions of domperidone by solvent evaporation method

Alaziz¹,

Sammour²,

El-Shamy³

et al. 2014

Afr. J. Pharm. Pharmacol.

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First-pass metabolism affects many oral medications and limits the attainment of their therapeutic level. It can be bypassed by administrating buccal dosage forms that allow systemic drug absorption via buccal mucosa. Drugs formulated as buccal medicaments should have an acceptable solubility in saliva. Numerous technologies had been experimented to increase the aqueous solubility of poorly water-soluble drugs e.g. solid dispersion technique. This technique is efficient for improving the solubility and dissolution rate of hydrophobic drugs and consequently improving their bioavailability. Domperidone is an antiemetic drug that undergoes extensive first-pass metabolism, having poor solubility in saliva and poor bioavailability. This study aimed to improve the aqueous solubility of domperidone at pH simulating saliva by preparing multicomponent solid dispersions using different carriers by solvent evaporation method. In vitro dissolution studies showed enhanced dissolution rates of all prepared systems with release kinetics approaching Higuchi model. Ternary solid dispersion (SD) of 1:9:0.25 drug/polyvinylpyrrolidone K30/pluronic F-127, respectively, achieved the highest dissolution rate. Physicochemical characterization of this SD using differential scanning calorimetry, Fouriertransform infrared spectroscopy, powder X-ray diffraction and scanning electron microscopy indicated the presence of an interaction between domperidone and polyvinylpyrrolidone K30 with evidence of drug amorphization that might be responsible for the enhanced dissolution rate.

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Preparation and characterization of Domperidone- β-cyclodextrin complexes prepared by kneading method.

Cited by 12 publications

References 28 publications

Effect of Water Content in Kneading Method of Solid Dispersion Technique for Solubility Enhancement

Effect of Water Content in Kneading Method of Solid Dispersion Technique for Solubility Enhancement

Preformulation Study of Domperidone: An Insight for Formulation and Development of Nasal Formulation

Formulation and evaluation of binary and ternary solid dispersions of domperidone by solvent evaporation method

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