The efficient development of a sildenafil orally disintegrating tablet using a material sparing and expedited approach

Wang, Chenguang; Sun, Changquan Calvin

doi:10.1016/j.ijpharm.2020.119816

Cited by 10 publications

(3 citation statements)

References 41 publications

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“…Breaking force (KP) = 4.54 + 0.5583 × X 1 + 0.2133 × X 2 (8) Friability is the second property related to the strength of the tablet. The main objective of the friability test was to estimate the ability of prepared tablets to resist abrasion during packaging and handling [30].…”

Section: Breaking Force and Friabilitymentioning

confidence: 99%

“…Nasal, transdermal, and sublingual delivery systems have been investigated as alternative administration routes of sildenafil to improve bioavailability, attain rapid onset of action, and reduce the side effects associated with food intake [7,8]. However, sublingual delivery system is preferred to avoid the drawbacks associated with nasal and transdermal delivery systems [7].…”

Section: Introductionmentioning

confidence: 99%

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Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

et al. 2021

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Sildenafil citrate undergoes first-pass metabolism, resulting in poor oral bioavailability at 25–41% of the administered dose. This study aimed to design and optimize fast-disintegrating tablets for the sublingual delivery of sildenafil citrate to improve bioavailability and facilitate rapid onset of action. The design-of-experiment (DoE) approach using 32 full factorial design was conducted to develop a new formulation of sildenafil fast-disintegrating sublingual tablets (FDSTs) using the fluid-bed granulation technique. The levels of partially pre-gelatinized starch (5–15%) and microcrystalline cellulose (10–60%) were selected as independent formulation variables. The prepared FDSTs were investigated for physical properties. Further, the optimum formulation was chosen for in vivo study in rabbits. Regression analysis showed that independent variables have a significant (p < 0.05) influence on critical attributes of FDSTs. The optimized formulation showed acceptable mechanical strength (friability <1.0%) with very fast disintegration (14.561 ± 0.84 s) and dissolution (94.734 ± 2.76% after 15 min). Further, the optimized formulation demonstrated a significant increase (p < 0.01) in Cmax and AUC0–∞ with short tmax compared to the market product (Viagra®). Based on these results, using the DoE approach, a high level of assurance was achieved for FDSTs’ product quality and performance.

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Section: Breaking Force and Friabilitymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Exploitation of Design-of-Experiment Approach for Design and Optimization of Fast-Disintegrating Tablets for Sublingual Delivery of Sildenafil Citrate with Enhanced Bioavailability Using Fluid-Bed Granulation Technique

et al. 2021

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“…Acesulfame (Acs, Figure b), a relatively strong acid (p K a = 2.0), is a calorie-free sugar substitute that is 200 times sweeter than sucrose, with an excellent safety profile . Hence, Acs is a good candidate for masking the bitterness of SMT through forming a sweet crystalline complex, as demonstrated in other drugs. − We hypothesized that the multiple functional groups (amide and sulfonyl amide) of Acs make it possible to form a sweet crystal of SMT through intermolecular interactions with hydrogen donating groups, i.e., amine (−NH 2 ) and sulfonamide (−NH−), and accepting groups, i.e., sulfoxy −O–, amine −N–, and pyrimidine −N–, of SMT. , This work was performed to test the hypothesis that SMT can form a salt with Acs and, if so, evaluate mechanical properties of such a new salt for suitability in developing an oral tablet formulation. The formation of new multicomponent crystals is expected to modify both physicochemical and mechanical properties of SMT.…”

Section: Introductionmentioning

confidence: 99%

Sweet Sulfamethazine Acesulfamate Crystals with Improved Compaction Property

Liu

Wang

Chen

et al. 2021

Crystal Growth & Design

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Sulfamethazine (SMT) is a sulfonamide antibacterial drug used to treat or prevent infections in both humans and animals. However, SMT has an unfavorable taste and poor compaction behavior. To overcome these problems, a 1:1 complex with an artificial sweetener, acesulfame (Acs), was prepared and characterized. The single crystal structure suggests that the new complex, SMT-Acs, is a salt. This was confirmed by analysis of C-N bond length and comparison to multicomponent SMT crystals with known ionization states of SMT and Fourier transformation infrared spectroscopy. The applicability of the ΔpK a rule in multicomponent crystals of SMT is discussed. SMT-Acs exhibits better tabletability than SMT, which is attributed to its greater plasticity as shown by Heckel and Kuentz -Leuenberger analysis. The greater plasticity of SMT-Acs is consistent with the presence of slip planes identified by combined energy framework and topological analysis of the crystal structure.

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