Formulation Development of Immediate Release Pellets of Tadalafil: Solidification Approach for Nanosuspension

Ubgade, Shobha; Kilor, Vaishali; Bahekar, Vidya; Ittadwar, Abhay

doi:10.22159/ijap.2019v11i4.32331

Cited by 5 publications

(6 citation statements)

References 13 publications

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“…After optimisation of the formula, the immediate release pellets of canagliflozin were prepared by applying 2 3 factorial design using nanosuspension as a binder. [13] From the formulation and production result, it was observed that microcrystalline cellulose was used as pelletizing aids and sodium starch glycolate as super disintegrant, gave acceptable spherical pellets with good yield, low friability and satisfactory flow properties. Based on the observations, 30% of MCC, 10% of SSG and spheronization speed of 800 rpm with time 10 mm were selected as formulation and process parameters.…”

Section: Preparation Of Immediate Release Pelletsmentioning

confidence: 99%

“…In vitro dissolution studies [13,19] In vitro drug release studies of pellets were performed using the USP Apparatus I (basket) at a speed of 75 rpm in 900 ml of 0.75% w/v of SLS and the medium at 37.0±2°C. Canagliflozin is soluble in many organic solvents (methanol, dimethyl sulfoxide) and insoluble in aqueous media and freely soluble in 0.75% w/v of SLS.…”

Section: Tan (θ) = H/rmentioning

confidence: 99%

“…[9] One of the major challenges of the pharmaceutical researchers is to develop an enabling formulation which can make poorly water-soluble drugs highly soluble to overcome the low bioavailability problem of the drugs. Many strategies have been used to improve the aqueous solubility of poorly soluble drugs such as complexation [10] , micronisation [11] , lipid based formulations, use of cosolvents, solid dispersions [12] , pellets [13] , etc. However, these techniques often lead to poor solubility, toxicity, high production costs [14] and therefore fails at commercial level.…”

Section: Introductionmentioning

confidence: 99%

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A recent solidification approach for nanosuspension: formulation, optimisation and evaluation of canagliflozin immediate release pellets

Patel¹,

Patel²

2022

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Introduction: Canagliflozin is a BCS class IV drug. Nanosuspension is known to enhance the saturation solubility and dissolution rate of poorly soluble drugs owing to the increased surface area of nanosized particles. Aim: In the present study, we aimed to improve the dissolution characteristics of a poorly water-soluble drug canagliflozin by nanosuspension formulation and stability of this solubility enhancing system - nanosuspension can be improved by converting them into solidified forms as immediate release pellets. Materials and methods: Canagliflozin nanosuspension was formulated using the media milling method. Poloxamer 407 was used to stabilise nanosuspension. Prepared nanosuspensions were subjected to the characterisation of particle size, polydispersity index (PDI), and drug content. Optimised nanosuspension (NS1) was solidified by converting into immediate release pellets: as improved stability, where canagliflozin nanosuspension was used as a binder. Pellets were prepared by +extrusion-spheronization technique using microcrystalline cellulose (MCC) as pelletizing aid and sodium starch glycolate as super disintegrant. Different important process parameters e.g. concentration of sodium starch glycolate (A), spheronization speed (B) and spheronization time (C) were investigated by 23 factorial design to accomplish desired disintegration time (R1) and drug release at 10 min (R2). Results: The optimised nanosuspension had 120.5 nm particle size, 99.14% drug content and the optimised immediate release pellets (PF5) disintegrated within 23.29 second, and had 99.11% drug content. In vitro dissolution studies showed 89.59% drug release within 10 min in 0.75% w/v SLS. Scanning electron microscopy (SEM) confirmed uniform and spherically shaped pellets. Fourier transform infrared spectrometry (FTIR) and differential scanning calorimetry (DSC) analysis reveal no significant interaction between drug and excipients. Conclusions: It can be concluded from the findings of this study that the formulation of nanosuspension and its use as a binder in the formulation of immediate release pellets should be investigated further in order to improve the dissolution rate and formulation stability.

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Section: Preparation Of Immediate Release Pelletsmentioning

confidence: 99%

Section: Tan (θ) = H/rmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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A recent solidification approach for nanosuspension: formulation, optimisation and evaluation of canagliflozin immediate release pellets

Patel¹,

Patel²

2022

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“…Hence, there is a pressing need to develop colonspecific oral solid dosage form. In this framework, pellets offer advantages such as predictable gastric transit time, minimum local irritation, enhanced bioavailability, reduced dose dumping and readily coatable which render them suitable for controlled drug delivery [10][11][12][13][14]. Prolonged residence time, specific pH level and microbial environment of colon represent the key elements for colon targeting [15].…”

Section: Introductionmentioning

confidence: 99%

Formulation Development of Colon Targeted Mesalamine Pellets: In Vitro-in Vivo Release Study

Bahekar

Wadher

2019

Int J App Pharm

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Objective: This study was intended to investigate the potential of the colon specificity approach comprising of use of pH-sensitive and time-dependent polymers in combination for precise colonic release of Mesalamine or 5-Aminosalicylic acid (5-ASA). Methods: The extrusion and spheronization method, preferably employed in industry for allowing high dose capacity to formulate, was used to prepare drug pellets. The Wurster coating technique used for aqueous coatings of Eudragit NE 40D as an inner coat and Eudragit FS30D as outer coat. The changing pH media used for in vitro release study of optimization batches for both the coating levels. A scanning electron microscope (SEM) was used to evaluate coating thickness and surface morphology. Results: The pharmacokinetic parameters of formulation evaluated by in vivo study in rabbits revealed that the uncoated formulation released the drug too early in the gastrointestinal tract (GIT) with a mean Cmax of 1205.28±0.37 µg/ml at 2 h after administration, whereas desired lag time was achieved in case of coated pellets exhibiting mean Cmax 465.94±0.21 µg/ml and tmax of 8 h. Conclusion: The in vitro and in vivo release study divulge the reliability of approach involving the use of pH sensitivity and time dependency of polymer for drug release in a single formulation for the treatment of colonic diseases. Hence, the present study provides constructive results for colon targeting of 5-ASA pellets with industrially feasible processes.

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“…Hence, the development of prominent colonspecific oral solid dosage form is an extreme dictate today. In this scaffold, multiparticulate system must be utilized due to its advantages such as predictable gastric transit time, minimum local irritation, enhanced surface area, reduced dose dumping and readily coatable which render them suitable for controlled drug delivery [10][11][12][13][14] . Prolonged residence time, specific pH level and microbial environment of colon represent the input essentials for colon targeting 15 .…”

mentioning

confidence: 99%

Untitled

2019

IJPSR

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This study was an attempt to explore the latent of colon specificity approach utilizing pH-sensitive and time-dependent characteristics of polymers for defined colonic release of 5-Fluorouracil (5-FU). Method: The pellets were prepared by extrusion-spheronization method which is an industry-accepted method due to its ease of formulation. The prepared pellets were the matrix of 5-Fluorouracil with pH-sensitive and time-dependent polymers, i.e. Eudragit FS30D and Eudragit NM30D respectively. The changing pH media used for in-vitro release study of optimization batches for both the polymer concentrations. The Optical microscopy and Scanning electron microscope (SEM) was used to evaluate texture and surface morphology. Results: The t 10%, t 30%, t 50%, and t 90% values for optimized formulation were found as 2.7 h, 6.2 h, 8.7 h and 18.2 h respectively. These values were extrapolated from invitro release vs. time plot which also indicated that the required lag time of 6-8 h was achieved. The in-vivo roentgenography or X-ray imaging study was used to confirm the lag time and transition path of colon targeted matrix pellets. Conclusion: The present study provides assurance for colon targeting of 5-FU pellets with industrially feasible processes. The combination of pH-sensitive and time-dependent polymers in development of pellets contributed to promising and precise drug release at colonic site. The in-vivo roentgenography study also further strengthen proposal of 6-8 h of lag time which was determined based on the in-vitro drug release study. INTRODUCTION: According to the ASCO (American Society of Clinical Oncology), the proportion of patients diagnosed with colorectal cancer under the age of 50 was increased from 10% in 2004 to 12.2% in 2015 in the United States alone.

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Formulation Development of Immediate Release Pellets of Tadalafil: Solidification Approach for Nanosuspension

Cited by 5 publications

References 13 publications

A recent solidification approach for nanosuspension: formulation, optimisation and evaluation of canagliflozin immediate release pellets

A recent solidification approach for nanosuspension: formulation, optimisation and evaluation of canagliflozin immediate release pellets

Formulation Development of Colon Targeted Mesalamine Pellets: In Vitro-in Vivo Release Study

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