Evaluation and Characterization of Sildenafil 50 mg Orodispersible Tablets Using Sublimation Technique

Ahmed Abbas,Wedad Sakran,Wael Ibrahim,Aliaa Badawi

doi:10.21608/aprh.2018.5126.1065

Ahmed Abbas, Wedad Sakran + Show 2 more

Open Access

https://doi.org/10.21608/aprh.2018.5126.1065

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Abstract

Objective: The aim of this work focused on formulation and evaluation of sildenafil 50 mg orodispersible tablets by sublimation technique. Methods: Active ingredient and excipients mixtures were evaluated for physicochemical changes of the drug utilizing FTIR spectroscopy and DSC thermal analysis. Nineteen proposed formulae N1-N19 were prepared by sublimation technique using menthol as a sublimating agent. Three different types of superdisintegrants (sodium starch glycolate, croscarmellose sodium and plasidone XL) were used in three different ratios (3, 6 and 9 % w/w), percentage of inter-granular and intragranular disintegrant. Hydrophilic filler such as mannitol and hydrophobic filler such as microcrystalline cellulose were used in the ratio (1:1, 2:1 and 4:1 w/w).Elimination of bitterness using sucralose as a potent sweetener. Granulation was achieved by alcoholic solution of PVP K25 as binder at Diosna® high shear mixer. Lubricant (hydrophobic magnesium stearate and hydrophilic sodium stearyl fumarate). Un-lubricated granules were characterized for bulk density, tapped density, true density, particle size distribution, Carr'sindex, Hausner ratio, flow rate and angle of repose. Tablets were firstly compressed on rotary machine then subjected to vacuum oven at 60ᵒC for 6 hours. Post compression characterization for tablets after sublimation including content uniformity, average weight, hardness, thickness, In-vitro disintegration, friability, wetting time, assay and dissolution profile of the proposed formulae against the immediate release marketed tablet Viagra ® 50 mg tablet. Results: The formula (N 16) which granulated using 1% PVP k25 with 9% plasidone XL (60% of it is inter-granular while 30% intra-granular), menthol 1%, Microcrystalline cellulose: Mannitol 1:1 and magnesium stearate was the most effective formulation as it showed wetting time of 30.7 seconds, disintegration time of 25 seconds and cumulative % drug release of 92.8 and 95.8 % after 1 and 3 minute respectively. Conclusion: Sildenafil 50 mg ODT successfully was prepared by sublimation technique with better wetting time, disintegration time, assay dissolution profile, hardness and friability.

Highlights

The oral route of administration is the most preferred route due to its many advantages like ease of administration, accurate dosage, self‐medication, pain avoidance, versatility and patient compliance[1].US FDA defined fast dissolving or disintegrating tablets (FDT) as “A solid dosage form containing medicinal substances which disintegrates rapidly within a matter of seconds, when placed upon the tongue”
The Differential Scanning Calorimetry (DSC) thermograms of physical mixtures of drug and different excipients illustrated in Figure 2 reveal no significant change in the melting point of sildenafil citrate in the presence of excipients, indicating no interaction between the drug and excipient[14, 41]
The sharp endothermic peak signifies that SC was in a pure crystalline state. It notice that there was no shift in SC peak upon mixing with plasidone XL reveal endothermic melting peak at 203°C, Sodium starch glycolate at 202.48 °C, croscarmellose sodium at 202.76 °C, Sucralose at broad endothermic peak at 216 °C, pineapple at 204 °C, PVP K25 have two endothermic peak at 200 °C and other peak 193.84 specific for PVP k25, menthol at 193.84 and other specific peak for menthol 48.76 °C and, microcrystalline cellulose at 199 °C, sodium stearyl fumarate have two peak 197 °C for SC and 125 for sodium stearyl fumarate, magnesium stearate at 202 °C, Aerosil 200 at 203 °C, as shown in http://aprh.journals.ekb.eg/ 299

Summary

Introduction

The oral route of administration is the most preferred route due to its many advantages like ease of administration, accurate dosage, self‐medication, pain avoidance, versatility and patient compliance[1].US FDA defined fast dissolving or disintegrating tablets (FDT) as “A solid dosage form containing medicinal substances which disintegrates rapidly within a matter of seconds, when placed upon the tongue”. Forms like tablets and capsules is difficulty in swallowing, leading to patient's incompliance in case of geriatric patients. Dysphagia is commonly found among all age groups. Due to this problem, approximately 50% of population suffers. The difficulty in swallowing may be due to the taste, size and surface of dosage form. Sometimes water is not accessible so a patient feels difficulty in swallowing solid dosage form[3]

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Conclusion