Enhancement of Solubility and Dissolution Rate of Domperidone by Utilizing Different Techniques

Ibrahim, El-Nobi A.; El-Faham, T. H.; Mohammed, F. A.; Eleraky, Nermin E.

doi:10.21608/bfsa.2011.63250

Cited by 7 publications

(3 citation statements)

References 23 publications

(28 reference statements)

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“…In case of RLS the drug converts in its molecular form get homogenized with the carrier and remain adsorb on the surface without need of any coating material. The drug release from RLS was brisk and demonstrated sheer upsurge in rate of dissolution in contrast to pure drug GLD [44].…”

Section: Dissolution Rate Studiesmentioning

confidence: 97%

Studies on Refined Liquisolid System for Simultaneous Improvement of Content Uniformity and Dissolution Profile of Glimepiride

2019

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Objective: To improve and compare dissolution contour of poorly soluble BCS Class II drug Glimepiride (GLD) by altering it to conventional solid dispersion (CSD), surface solid dispersion (SSD) and refined liquisolid system (RLS). Methods: The three formulations of GLD namely CSD, SSD and RLS were fabricated using the conventional methods by employing the suitable polymer and solvent system. These formulations were optimized on the basis of powder flow properties, FTIR, DSC and XRD analysis. All the optimized formulations were compared to the marketed formulation for content uniformity and dissolution rate. Results: The characteristic analysis of all the optimized formulations was obtained in the standard range. The average content uniformity (% age) of Marketed formulation, CSD, SSD and RLS found to be 88.28±0.721, 92.91±0.789, 95.98±0.478, 99.32±0.744 respectively. The in vitro dissolution rate (%age at 30 min time interval) fall in the range 59.78±0.036, 75.78±0.013, 93.11±0.019, 93.99±0.062 and 98.55±0.043 for pure drug, Marketed formulation, CSD, SSD and RLS respectively. All the analytical studies exhibited improved homogeneity/distribution of the drug in RLS. Conclusion: The RLS formulation presented sheer expansion in the content uniformity and dissolution contour of GLD at a minimal cost.

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Section: Dissolution Rate Studiesmentioning

confidence: 97%

Studies on Refined Liquisolid System for Simultaneous Improvement of Content Uniformity and Dissolution Profile of Glimepiride

2019

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“…It is categorized as a class II drug − based on the Biopharmaceutical Classification System (BCS). Because of its very low solubility in water, the bioavailability of domperidone drops to 13–17% after taken orally. , In addition, its poor aqueous solubility may limit its ability to be transported via the buccal or rectal regions. , With the intention of overcoming the disadvantage of poor aqueous solubility, a lot of methods have been put forward in the previous works. ,− The most effective technique for enhancing the drug solubility in water is to mix a miscible and safe cosolvent with neat water. ,, The method requires an understanding of the accurate solubility of the drug in a number of neat and mixed solvents. Accordingly, it is very important to know the solubility of domperidone for many pharmaceutical systems.…”

Section: Introductionmentioning

confidence: 99%

Domperidone Solubility in Aqueous Cosolvent Mixtures of N,N-Dimethylformamide, Isopropanol, Dimethyl Sulfoxide, and Ethanol: Thermodynamic Modeling and Preferential Solvation Analysis

Zheng

Zhao

2019

J. Chem. Eng. Data

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The determination of solubility of domperidone in aqueous cosolvent mixtures of isopropanol, N,N-dimethylformamide (DMF), dimethyl sulfoxide (DMSO), and ethanol was carried out by a shake-flask method over the temperatures from 293.15 to 333.15 K under local atmospheric pressure p = 101.1 kPa. It may be observed that the domperidone solubility increased and then decreased as the mass fractions of DMF (DMSO, isopropanol, or ethanol) increased. The maximum solubility data was found with the cosolvent composition of 0.8 in mass fraction. The determined solubility values were correlated using the Jouyban–Acree, van’t Hoff–Jouyban–Acree, and Apelblat–Jouyban–Acree models. The attained average relative deviations were smaller than 7.56%. Preferential solvation analysis of domperidone was performed by the inverse Kirkwood–Buff integral method. The preferential solvation parameters (δx 1,3) by the cosolvent showed positive values in the composition regions of 0.20 < x 1 < 0.50 for DMF, 0.24 < x 1 < 0.55 for isopropanol, 0.20 < x 1 < 0.45 for DMSO, and 0.24 < x 1 < 0.61 for ethanol. Domperidone was solvated preferentially by the cosolvents in these regions. We may conjecture that the drug acts as a Lewis acid in the presence of isopropanol (DMF, DMSO, and ethanol) molecules.

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“…Few research articles have reported on ternary solid dispersion systems using conventional carriers. [ 11 12 13 14 ] Only few new carriers have been developed in the last decade due to increasing regulatory demands. It is, therefore, recommended to build up new carrier systems made up of a combination of two or more well-known excipients.…”

Section: Introductionmentioning

confidence: 99%

Formulation and evaluation of fast dissolving tablet containing domperidone ternary solid dispersion

Patel¹,

Patel²,

Patel³

2014

Int J Pharma Investig

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Introduction:Fast dissolving tablet containing domperidone ternary solid dispersion was developed to improve the dissolution of drug and stability of solid dispersion.Materials and Methods:Binary and ternary solid dispersions were prepared by fusion method. They were characterized by solubility study, in vitro dissolution, dissolution efficiency, and stability study. The solid state properties of solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Ternary solid dispersion was successfully incorporated into fast dissolving tablet by direct compression method. Tablets were characterized for pre-compression parameters, post-compression parameters, and stability study.Results:Optimized ternary solid dispersion containing ratio 1:2:1.5 of drug: Gelucire 50/13: Poloxamer 188 gave maximum dissolution. The FTIR, DSC, and XRD studies of solid dispersions were confirmed the formation of solid dispersion. Ternary solid dispersion was more stable compared to binary solid dispersion at accelerated environment conditions for one month as confirmed by DSC study. Crospovidone as a superdisintegrant (4%) showed good result with disintegration time of 19 s and dissolution near to 100% in 0.1N HCL at 30 min.Conclusion:The studies indicated that the dissolution of drug and stability of solid dispersion was improved in the presence of ternary agent (surfactant) as compared to binary solid dispersion. It was concluded that fast dissolving tablet containing ternary solid dispersion was stable at accelerated environmental conditions for 1 month.

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Enhancement of Solubility and Dissolution Rate of Domperidone by Utilizing Different Techniques

Cited by 7 publications

References 23 publications

Studies on Refined Liquisolid System for Simultaneous Improvement of Content Uniformity and Dissolution Profile of Glimepiride

Studies on Refined Liquisolid System for Simultaneous Improvement of Content Uniformity and Dissolution Profile of Glimepiride

Domperidone Solubility in Aqueous Cosolvent Mixtures of N,N-Dimethylformamide, Isopropanol, Dimethyl Sulfoxide, and Ethanol: Thermodynamic Modeling and Preferential Solvation Analysis

Formulation and evaluation of fast dissolving tablet containing domperidone ternary solid dispersion

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