Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion

Abdulqader, Alaa A.; Al-Khedairy, Eman B. H.

doi:10.31351/vol26iss1pp50-60

Cited by 6 publications

(6 citation statements)

References 9 publications

(13 reference statements)

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“…The X-ray diffraction was done for pure ONDS and the selected formula using an X-ray diffractometer (Philips, USA), the operating voltage and current were (40 kV and 30 mA), respectively. Samples were scanned at 2θ from (0 -80°) for qualitative studies, and the scanning rate was (4°/min) [5].…”

Section: 8c Xrd Analysismentioning

confidence: 99%

“…Ondansetron (ONDS), a serotonin receptor (5 -HT3) antagonist, treats nausea and vomiting induced by illness, surgery, chemotherapy, radiotherapy, and pregnancy [5]. Ondansetron is a weak base with a pKa of 7.4 (an amphiphilic molecule); its salt is soluble in acidic media and considered a class-II drug (low soluble, high permeable) according to the biopharmaceutics classification system (BCS) [6].…”

Section: Introductionmentioning

confidence: 99%

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Preparation, Evaluation, and Histopathological Studies of Ondansetron-Loaded Invasomes Transdermal Gel

SALIH,

MUHAMMED

2024

jrp

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Ondansetron is a serotonin receptor antagonist for treating nausea and vomiting. Its multiple daily doses and extensive first-pass metabolism faced parenteral and oral administration challenges. The transdermal route enhances its bioavailability as it bypasses the first-pass effect. Invasome vesicles improve the skin permeation of ondansetron via its unique components, lecithin, limonene, and ethanol, which are considered efficient permeation enhancers. The current study intends to develop a gel containing ondansetron as invasomes vesicles with appropriate texture and efficient skin penetration. Two gelling agents, hydroxypropyl methylcellulose K4M and carbopol 934P, were used at two concentrations (0.5 and 1%, w/w). Formulas were evaluated regarding pH, content uniformity, viscosity, spreadability, and ex vivo permeation. The selected formula (F3), which contained ondansetron (5%, w/w) and used carbopol 934P at (0.5%, w/w), was homogeneous, with proper viscosity (21,500 ± 390 mPa.s) at rest and enough spreadability (3.4 ± 0.45 cm). The ex vivo permeation showed permeation flux (Jss) was (280.4 ± 3.5 g/cm2.h) with a shorter lag time (0.5 ± 0.1 h). Characterization studies revealed nanosized vesicles (Dav. = 202.9 ± 0.5 nm) as spherical shapes dispersed within a gel matrix. In vivo, skin irritation and histopathology studies using male Wistar albino rats demonstrated that (F3) was biocompatible, with no irritation reported for six consecutive days. In conclusion, the invasomes gel of ondansetron utilizing carbopol (0.5%, w/w) was prepared for transdermal delivery, offering effective permeation and safe application. An invasomes-loaded gel is considered a novel formulation, giving an efficient and realistic therapeutic option for treating vomiting.

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Section: 8c Xrd Analysismentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Preparation, Evaluation, and Histopathological Studies of Ondansetron-Loaded Invasomes Transdermal Gel

SALIH,

MUHAMMED

2024

jrp

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“…to completely remove the residual amount of the solvent as shown in Figure (2). The resulted product was crushed using mortar and pestle and sieved through no.60 sieve size and kept in a desiccator to be subjected to further investigations (7) .…”

Section: Preparation Of Acf-solid Dispersion Preparation Of Acf-sd By...mentioning

confidence: 99%

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Alezzy

2024

Tikrit J. Pharm. Sci.

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Background: Aceclofenac (ACF) is a non-steroidal anti-inflammatory drug with potent anti-inflammatory and analgesic properties. ACF is belongs to BCS class II which has poor solubility in water (practically insoluble) and high permeability that leads to a low dissolution rate and reduced bioavailability. Objective: to enhance the solubility and dissolution rate of ACF using the solid dispersion method (SD) by two common techniques which were solvent evaporation (SE) and kneading (Kn) by using different carriers Mannitol, PVP k30, Soluplus®, and Urea in both techniques at 1:1 and 1:5 wight ratio. Methods: The effects of type of carrier and preparation method on solubility and dissolution rate of SD were studied. Solid dispersions were characterized for their, percentage yield, drug content, drug solubility and in-vitro dissolution rate in comparison with pure drug. Results: The best formula is obtained by the Kn formula (F16) which was formulated by the use of ACF: Soluplus®: with a weight ratio of 1:5 which gave a high percentage yield (99.5%), high drug content (99.8± 0.003%) and the best solubility enhancement which was 361 folds compared to pure ACF and faster dissolution rate which was 80% in 10 minutes compared to 20% for pure drug. Conclusion: the solubility and in-vitro dissolution rate of ACF was efficiently improved when prepared by SD techniques, utilizing both solvent evaporation and kneading methods. Furthermore, the kneading method was superior to solvent evaporation method due to the greater enhancement of solubility and dissolution rate obtained by all carriers and ratios with higher improvement by 1:5 ratio, and can be considered a successful and efficient strategy for solubility and in-vitro dissolution rate improvement of hydrophobic drugs.

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“…The practical yield per cent (PY %) of the prepared EXB-solid dispersion was conducted to know the efficiency of each preparation method. The (PY %) was determined by calculating the ratio of the actual weight of the obtained solid dispersion on the theoretical mass of drug and carrier (equation 1) (13) .…”

Section: Determination Of Practical Yield Per Cent (Py %) Of the Prep...mentioning

confidence: 99%

Enhancement of Aqueous Solubility and Dissolution Rate of Etoricoxib by Solid Dispersion Technique

AlKhalidi

Jawad²

2020

IJPS

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Etoricoxib (EXB) is a highly selective cox-2 inhibitor which belongs to the non-steroidal anti-inflammatory drug (NSAID). EXB is a class II drug according to the biopharmaceutical classification system (BCS), which possess a very low aqueous solubility in water. In the present study, many trials were made to improve the aqueous solubility and dissolution rate of EXB by solid dispersion technique. Eighteenth EXB formulas were formulated as a solid dispersion using a variety of hydrophilic polymers (as carriers) including poloxamer 407 (PXM 407), poloxamer 188 (PXM 188) and polyethylene glycol 4000 (PEG 4000) at different drug: polymer ratios (1:1, 1:3 and 1:5). These formulas were prepared by two methods; solvent evaporation and fusion method. The prepared formulas were evaluated for practical yield percent (PY %), drug content, saturated solubility and release rate, Fourier transforms infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD). It was found that the solubility was affected by the polymer type and the method of preparation. The polymers (as carriers) used to prepare EXB- solid dispersion showed improvement in the solubility in the following descending order; PXM 407>PXM 188> PEG 4000. The optimum formula (SD15) composed of the drug: PXM 407 at a ratio of 1:5 was prepared by solvent evaporation showed 7.76 folds (676.40%) solubility improvement as compared to pure EXB. The optimum formula showed a release rate of 99.8% through the first 15 min. The advance characterization of the selected formula indicated the possible transformation of the drug to the amorphous state. Keywords: EXB, Solid dispersion, PXM 407, PXM 188, PEG 4000.

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Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion

Cited by 6 publications

References 9 publications

Preparation, Evaluation, and Histopathological Studies of Ondansetron-Loaded Invasomes Transdermal Gel

Preparation, Evaluation, and Histopathological Studies of Ondansetron-Loaded Invasomes Transdermal Gel

Solubility and Dissolution Rate Enhancement of Aceclofenac by Solid Dispersion Employing Kneading and Solvent Evaporation Techniques

Enhancement of Aqueous Solubility and Dissolution Rate of Etoricoxib by Solid Dispersion Technique

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