Freeze drying: exploring potential in development of orodispersible tablets of sumatriptan succinate

Gugulothu, Dalapathi; Desai, Preshita; Pandharipande, Pranav P.; Patravale, Vandana

doi:10.3109/03639045.2013.871551

Cited by 13 publications

(20 citation statements)

References 30 publications

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“…It is also useful for the patients, where the underlying disease disrupts swallowing ability (e.g. migraine, Parkinson's disease) [7][8][9] . Studies have shown distinct patient preference for ODTs over regular tablets in certain disease conditions [10][11][12] .…”

Section: Introductionmentioning

confidence: 99%

Formulation and development of orodispersible sustained release tablet of domperidone

Patil

Tiwari

Repka

et al. 2015

Drug Development and Industrial Pharmacy

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Abstract:Commercially available domperidone orodispersible tablets (ODT) are intended for immediate release of the drug but none of them have been formulated for sustained action. The aim of the present research work was to develop and evaluate orodispersible sustained release tablet (ODT-SR) of domperidone, which has the convenience of ODT and benefits of controlled release product combined in one. The technology comprised of developing sustained release microspheres (MS) of domperidone, followed by direct compression of MS along with suitable excipients to yield ODT-SR which rapidly disperses within 30 seconds and yet the dispersed MS maintain their integrity to have a sustained drug release. The particle size of the MS was optimized to be less than 200 μm to avoid the grittiness in the mouth. The DSC thermograms of MS showed the absence of drug-polymer interaction within the microparticles, while SEM confirmed their spherical shape and porous nature. Angle of repose, compressibility and Hausner's ratio of the blend for compression showed good flowability and high percent compressibility. The optimised ODT-SR showed disintegration time of 21 seconds and matrix controlled drug release for 9 h. Invivo pharmacokinetic studies in Wistar rats showed that the ODT-SR had a prolonged MRT of 11.16 h as compared 3.86 h of conventional tablet. The developed technology is easily scalable and holds potential for commercial exploitation.

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Section: Introductionmentioning

confidence: 99%

Formulation and development of orodispersible sustained release tablet of domperidone

Patil

Tiwari

Repka

et al. 2015

Drug Development and Industrial Pharmacy

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show abstract

“…The open pore structure and amorphous nature of the low density tablet, 11.8 ± 0.3 × 10 -3 g/mL, were designed for rapid release of drug in low volumes of fluid. Additionally, the size and shape of the tablet were fashioned based on the recommendations of healthcare professionals experienced in treating overdose patients [27]. These dimensions contrast with smaller orally disintegrating tablets currently marketed, for example Imodium Instants® have a diameter of 7.5 mm [27].…”

Section: In Vitro Disintegration Assay For Buccal Tabletsmentioning

confidence: 99%

“…A wide range of mannitol to gelatin concentration ratios were investigated to allow selection of a predominantly amorphous formulation for further investigation. Gelatin acts as a binder and provides structural strength, resistance to breakage and a highly porous spongy structure [27].…”

Section: In Vitro Disintegration Assay For Buccal Tabletsmentioning

confidence: 99%

“…Both mannitol and salts are incorporated within freeze-dried materials to bridge and intercalate these tight polymer aggregates and thus expand the porous structure [42]. Thus, high concentrations of gelatin in the formulation increase the likelihood of strong inter-polymer chain attractions, resulting in water trapping and the subsequent formation of gels [27]. Unlike other studies, for example Gugulothu et al [27], where this problem was overcome by lowering the gelatin content and compensating with crystalline mannitol as a supporting agent, we have shown that it is possible to increase the ratio of gelatin to mannitol and form amorphous tablets (Figures 2 & 3).…”

Section: In Vitro Disintegration Assay For Buccal Tabletsmentioning

confidence: 99%

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Amorphous Formulation and in Vitro Performance Testing of Instantly Disintegrating Buccal Tablets for the Emergency Delivery of Naloxone

et al. 2016

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The aim of this study was to develop a freeze-dried buccal tablet for the rapid delivery of naloxone in opioid overdose. The tablet composition was optimized to produce an amorphous matrix, which was confirmed by the absence of peaks associated with crystallinity observed by differential scanning calorimetry and powder X-ray diffraction. Tablets with high gelatin content lacked adequate porosity. Mannitol was added to the formulation to bridge and intercalate gelatin's tight polymer aggregates, however sodium bicarbonate was also required to prevent crystallization within the tablets. A linear reduction in mannitol's recrystallization enthalpy was observed with increasing sodium bicarbonate concentration (ΔrecryH = -20.3[NaHCO3] + 220.9; r(2) = 0.9, n = 18). The minimum sodium bicarbonate concentration for full inhibition of mannitol crystallization was 10.9% w/w. Freeze-dried tablets with lower amounts of sodium bicarbonate possessed a crystalline fraction that PXRD identified as mannitol hemihydrate from the unique peak at 9.7° 2θ. Mannitol's greater affinity for both ions and residual water rather than its affinity for self-association was the mechanism for the inhibition of crystallization observed here. The optimized tablet (composition mannitol 24% w/w (4.26 mg), gelatin 65% w/w (11.7 mg), sodium bicarbonate 11% w/w (1.98 mg), and naloxone 800 μg) formed predominantly amorphous tablets that disintegrated in less than 10 s. Optimized tablets were chemically and physically stable over 9 months storage at 25 °C. As speed of drug liberation is the critical performance attribute for a solid dosage form designed to deliver drug in an emergency, a novel imaging based in vitro disintegration assay for buccal tablets was developed. The assay was optimized with regard to conditions in the buccal cavity: i.e., temperature 33-37 °C, volume of medium (0.1-0.7 mL), and use of mucin-containing biorelevant medium. The disintegration assay was sensitive to temperature, medium volume, and medium composition; naloxone tablet disintegration was extremely rapid, with full disintegration ranging from 5 to 20 s. In conclusion, rapidly disintegrating tablets have been developed which are suitable for proof-of-concept clinical trial in humans to determine the pharmacokinetics of naloxone delivered via the buccal route.

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“…Development of a fast disintegrating formulation of sumatriptan would be beneficial in increasing the efficacy and patient compliance. 23 By these formulations disintegration time in the stomach would be saved and the chance of mucosal absorption in oral cavity would also be increased. 7 Sumatriptan succinate is a highly water soluble and bitter drug.…”

mentioning

confidence: 99%

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2017

IJPSR

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Sumatriptan succinate, a selective 5-hydroxytryptamine-1 receptor agonist, is an antimigraine drug with bitter-taste. The present study was performed to prepare and evaluate eudragit-E microparticles containing sumatriptan and formulate fast disintegrating tablets of drug microparticles to increase patient-compliance and improve the efficacy of drug. Microparticles were prepared by solvent-evaporation method using waterdichloromethane/PVA and water-dichloromethane/liquid paraffin systems. The effect of different variables (polymer:drug ratio, PVA concentration and solvents combination ratios) on particle size and encapsulation efficiency of the microparticles was investigated. The final microparticles were evaluated for particle size, loading percent, taste-masking, thermal analysis and in-vitro release profile. The drug loading were higher in w/o/o emulsion than w/o/w. Mean particle size was not statistically different for different formulations. Sumatriptan release rate from eudragit-E microparticles was very fast in HCl 0.1 N medium and release profile was acceptable for fast disintegrating tablets. The prepared tablets were evaluated for in-vitro disintegration time, weight variation, hardness, friability and in-vitro drug release. The optimized formulation (F6) (provided a pleasant taste and mouth-feel) disintegrated within 20 seconds and released more than 70% of drug within 15 minutes. Tablets formulated by drug loaded eudragit-E microparticles could be a promising formulation for tastemasking and decreasing failure in triptans therapy.

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Freeze drying: exploring potential in development of orodispersible tablets of sumatriptan succinate

Cited by 13 publications

References 30 publications

Formulation and development of orodispersible sustained release tablet of domperidone

Formulation and development of orodispersible sustained release tablet of domperidone

Amorphous Formulation and in Vitro Performance Testing of Instantly Disintegrating Buccal Tablets for the Emergency Delivery of Naloxone

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