The evaluation of coated granules to mask the bitter taste of dihydroartemisinin

Shahzad, Yasser; Shah, Syed Nisar Hussain; Atique, Shabbar; Ansari, Muhammad Tayyab; Bashir, Furrukh; Hussain, Talib

doi:10.1590/s1984-82502011000200013

Cited by 11 publications

(6 citation statements)

References 18 publications

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“…The entrapment efficiency (EE) of the DHA in the GEL or HA nanoparticles was calculated as follows: 1 mL of solution containing the prepared DHA encapsulated within GEL or HA nanoparticles (defined as GEL/DHA or HA/DHA aggregates, respectively) were first centrifuged at 15,000 g for 90 min, 100 µL of the supernatant was removed, and the amount of nonencapsulated DHA was measured using high‐performance liquid chromatography (HPLC, Agilent 1100 series). The parameter of HPLC setting was referred to Shahzad et al with modification, briefly, using a C‐18 column, a mobile phase of 40% (v/v) acetonitrile, a flow rate of 1 mL/min and a detection wavelength of 210 nm. A standard curve for DHA was drawn, and the drug EE was calculated using the following formula:

EE false(% false) = [(Amount of total DHA - amount of non - encapsulatedDHA) / Amountof total DHA)] \times 100 %

…”

Section: Methodsmentioning

confidence: 99%

Enhanced apoptotic effects of dihydroartemisinin‐aggregated gelatin and hyaluronan nanoparticles on human lung cancer cells

et al. 2013

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Recent studies suggest that dihydroartemisinin (DHA), a derivative of artemisinin isolated from the traditional Chinese herb Artemisia annua L., has anticancer properties. Due to poor water solubility, poor oral activity, and a short plasma half-life, large doses of DHA have to be injected to achieve the necessary bioavailability. This study examined increasing DHA bioavailability by encapsulating DHA within gelatin (GEL) or hyaluronan (HA) nanoparticles via an electrostatic field system. Observations from transmission electron microscopy show that DHA in GEL and HA nanoparticles formed GEL/DHA and HA/DHA aggregates that were approximately 30-40 nm in diameter. The entrapment efficiencies for DHA were approximately 13 and 35% for the GEL/DHA and HA/DHA aggregates, respectively. The proliferation of A549 cells was inhibited by the GEL/DHA and HA/DHA aggregates. Fluorescent annexin V-fluorescein isothiocyanate (FITC) and propidium iodide (PI) staining displayed low background staining with annexin V-FITC or PI on DHA-untreated cells. In contrast, annexin V-FITC and PI stains dramatically increased when the cells were incubated with GEL/DHA and HA/DHA aggregates. These results suggest that DHA-aggregated GEL and HA nanoparticles exhibit higher anticancer proliferation activities than DHA alone in A549 cells most likely due to the greater aqueous dispersion after hydrophilic GEL or HA nanoparticles aggregation. These results demonstrate that DHA can aggregate with nanoparticles in an electrostatic field environment to form DHA nanosized aggregates.

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EE false(% false) = [(Amount of total DHA - amount of non - encapsulatedDHA) / Amountof total DHA)] \times 100 %

…”

Section: Methodsmentioning

confidence: 99%

Enhanced apoptotic effects of dihydroartemisinin‐aggregated gelatin and hyaluronan nanoparticles on human lung cancer cells

et al. 2013

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“…Published studies that have utilized the in vitro drug dissolution method to evaluate medicine palatability have employed a range of dissolution medium (water (7) to pH 6.8 phosphate buffer (8,9)), receptor fluid volume (10 ml (10) to 900 ml (8)), and dissolution time (2 min (8,9) to 5 min (7)).…”

Section: Introductionmentioning

confidence: 99%

Taste evaluation of a novel midazolam tablet for pediatric patients: In vitro drug dissolution, in vivo animal taste aversion and clinical taste perception profiles

Cheung

Nguyen

Tang

et al. 2018

International Journal of Pharmaceutics

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Harmonized methodologies are urgently required for the taste evaluation of novel pediatric medicines. This study utilized in vitro, in vivo and clinical data to evaluate the palatability of a novel midazolam chocolate tablet. In vitro dissolution experiments showed the crushed tablet to release within 5 min 1.68 mg of midazolam into simulated saliva. This translated to a drug level of 0.84 mg/ml in the oral cavity, which would be higher than the midazolam bitterness detection threshold concentration of 0.03 mg/ml determined in a rat 'brief access taste aversion' (BATA) model. The visual analogue scale scores of patients aged 4-16 years prescribed with midazolam pre-surgery showed a clear preference for the midazolam chocolate tablets (3.35 ± 1.04, n = 20) compared to the control midazolam solution (1.47 ± 0.62, n = 17). The clinical data was in agreement with the in vivo rodent data in showing the novel chocolate tablet matrix to be effective at taste-masking the bitter midazolam.

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“…Slow discharge of the drug results into taste-masking due to drug is present in minimal and below the bitterness threshold in the oral cavity. In this analysis, the drug is analyzed from the dissolution media of phosphate buffer (pH 6.8) at concentrations below its bitterness threshold [43][44][45][46][47]. Threshold bitterness concentration is the lowest concentration that had a bitter taste.…”

Section: In Vitro Taste Evaluation Studymentioning

confidence: 99%

Development of Binary and Ternary Complex of Cefuroxime Axetil With Cyclodextrin for Improving Pharmaceutical Characteristics

Kaushik¹,

Verma²,

Purohit³

et al. 2020

Int J App Pharm

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Objective: The current research objective is systematic development and characterization of binary and ternary inclusion complexes of cefuroxime axetil with β-cyclodextrin to improve its pharmaceutical characteristics by using the kneading method. Methods: Phase solubility study was carried out using Higuchi and Connors method. Based on its result, binary complexes of cefuroxime axetil with different ratio of β-cyclodextrin were developed and characterized using differential scanning calorimeter (DSC), fourier transform infrared spectroscopy (FT-IR) and X-ray powder diffractometry (XRD). Then, binary complexes were analyzed for in vitro dissolution testing. The ternary complexes were developed using different ratio of PVP K-30 as a ternary component and evaluated for in vitro dissolution testing and in vitro taste masking. Results: Binary complex of cefuroxime axetil with β-cyclodextrin (1:1) showed better drug release than pure drug. During the development of the ternary complex, β-cyclodextrin (1:1) and 1% w/v PVP K-30 as a ternary agent resulted in an optimized ternary complex. The DSC, FT-IR and XRD studies clearly revealed the formation of binary and ternary complexes. The ternary complex showed better drug release of>85% within 30 min. in comparison to binary complex. The in vitro taste-masking study revealed the taste masking efficiency of the ternary complex of cefuroxime with β-cyclodextrin. Conclusion: The developed binary and ternary complex of cefuroxime axetil based on β-cyclodextrin with PVP K-30 showed improved in vitro dissolution rate and taste masking in comparison to pure drug. The drug release was better in ternary complexes. The present research work successfully shows the utility of binary and ternary complexes for improving pharmaceutical characteristics of cefuroxime axetil.

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The evaluation of coated granules to mask the bitter taste of dihydroartemisinin

Cited by 11 publications

References 18 publications

Enhanced apoptotic effects of dihydroartemisinin‐aggregated gelatin and hyaluronan nanoparticles on human lung cancer cells

Enhanced apoptotic effects of dihydroartemisinin‐aggregated gelatin and hyaluronan nanoparticles on human lung cancer cells

Taste evaluation of a novel midazolam tablet for pediatric patients: In vitro drug dissolution, in vivo animal taste aversion and clinical taste perception profiles

Development of Binary and Ternary Complex of Cefuroxime Axetil With Cyclodextrin for Improving Pharmaceutical Characteristics

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