Model-based description of disintegration time and dissolution rate of nanoparticle-loaded orodispersible films

2019 ◽  
Vol 132 ◽  
pp. 18-26 ◽  
Author(s):  
Denise Steiner ◽  
Jan Henrik Finke ◽  
Arno Kwade
Author(s):  
Ganesh kumar Gudas ◽  
Manasa B ◽  
Senthil Kumaran K ◽  
Rajesham V V ◽  
Kiran Kumar S ◽  
...  

Promethazine.HCl is a potent anti-emetic. The central antimuscarinic actions of antihistamines are probably responsible for their anti-emetic effects. Promethazine is also believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine -induced vomiting. Fast dissolving tablets of Promethazine.HCl were prepared using five superdisintegrants viz; sodium starch glycolate, crospovidone, croscarmellose, L-HPC and pregelatinised starch. The precompression blend was tested for angle of repose, bulk density, tapped density, compressibility index and Hausner’s ratio. The tablets were evaluated for weight variation, hardness, friability, disintegration time (1 min), dissolution rate, content uniformity, and were found to be within standard limit. It was concluded that the fast dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants. Among the different formulations of Promethazine.HCl was prepared and studied and the formulation S2 containing crospovidone, mannitol and microcrystalline cellulose combination was found to be the fast dissolving formulation. In the present study an attempt has been made to prepare fast dissolving tablets of Promethazine.HCl, by using different superdisintegrants with enhanced disintegration and dissolution rate. 


Processes ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 778
Author(s):  
Emőke-Margit Rédai ◽  
Paula Antonoaea ◽  
Nicoleta Todoran ◽  
Robert Alexandru Vlad ◽  
Magdalena Bîrsan ◽  
...  

The most used pharmaceutical formulations for children are syrups, suppositories, soft chewable capsules, and mini-tablets. Administrating them might create an administration discomfort. This study aimed to develop and evaluate orodispersible films (ODFs) for pediatric patients in which the fluoxetine (FX) is formulated in the polymeric matrix. Six FX fast dissolving films (10 mg FX/ODF), FX1, FX2, FX3, FX4, FX5, and FX6, were prepared by solvent casting technique. In the composition of the ODFs, the concentration of the hydroxypropyl methylcellulose and the concentration of the propylene glycol were varied. Each formulation of fluoxetine ODF was evaluated by determining the tensile strength, folding endurance, disintegration, behavior in the controlled humidity and temperature conditions, and adhesiveness. All the obtained results were compared with the results obtained for six ODFs prepared without FX. The disintegration time of the FX ODFs was of maximum 88 s for FX2. Via the in vitro releasing study of the FX from the ODFs it was noticed that FX1 and FX2 allow a better release of the drug 99.98 ± 3.81% and 97.67 ± 3.85% being released within 15 min. From the obtained results it was also confirmed that FX ODFs were found to follow first-order release kinetic.


2017 ◽  
Vol 9 (6) ◽  
pp. 39
Author(s):  
Zainab E. Jassim

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.


2014 ◽  
Vol 66 (8) ◽  
pp. 1102-1111 ◽  
Author(s):  
Maren Preis ◽  
Dorothee Gronkowsky ◽  
Dominik Grytzan ◽  
Jörg Breitkreutz

Author(s):  
Uday Kumar Thummala ◽  
Eswar Guptha Maddi ◽  
Prameela Rani Avula

The fixed dose combination of ledipasvir (LDV) and sofosbuvir (SBV) is approved by USFDA in 2014 for the treatment of Hepatitis C virus infection and is available in the form of tablets. In the present work, the principal aim is to explore orodispersible films type dosage form to impart its characteristic advantages to these poorly soluble drugs so as to improve their bioavailability and ease of administration. Solid dispersions with low viscosity grade methyl cellulose A 15-LV (MC A 15-LV) at different ratios with LDV and SBV were prepared and evaluated to check their ability in improving the solubility of the drugs. The best drug to polymer ratio was selected to develop the films, using other excipients including plasticizer and superdisintegrant. Solvent casting method was used to develop the films. Three formulation parameters were selected as independent factors viz. thickness of the film (50-150 µm), concentration of superdisintegrant (sodium starch glycolate 6-10%) and concentration of plasticizer (polyethylene glycol 400, 10-20%). Disintegration time (DT), time for 90% dissolution (T90%) of LDV and time for 90% dissolution of SBV were taken as the response variables. The experiment was designed using Box-Behnken design. Among the polymers, MC A 15-LV produced maximum solubility at 1:2 ratio. The films obtained were found to have good tensile strength and % elongation with disintegration times in the range of 43-162 sec. The T90% values for LDV and SDV were found to be in the range of 8.4-21.2 min and 7.2-18.4 respectively. All the three formulation factors were found to have significant effect on the three responses. The optimum formulation was identified at 100 µm thickness, 10% superdisintegrant and 20% plasticizer which showed DT of 89 sec with T90% values of 8.4 min and 7.2 min for LDV and SBV respectively. The rapid disintegration and dissolution of the films signified that the set objective was achieved.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 470 ◽  
Author(s):  
Konstantina Chachlioutaki ◽  
Emmanouil K. Tzimtzimis ◽  
Dimitrios Tzetzis ◽  
Ming-Wei Chang ◽  
Zeeshan Ahmad ◽  
...  

Child-appropriate dosage forms are critical in promoting adherence and effective pharmacotherapy in pediatric patients, especially those undergoing long-term treatment in low-resource settings. The present study aimed to develop orodispersible films (ODFs) for isoniazid administration to children exposed to tuberculosis. The ODFs were produced from the aqueous solutions of natural and semi-synthetic polymer blends using electrospinning. The spinning solutions and the resulting fibers were physicochemically characterized, and the disintegration time and isoniazid release from the ODFs were assessed in simulated salivary fluid. The ODFs comprised of nanofibers with adequate thermal stability and possible drug amorphization. Film disintegration occurred instantly upon contact with simulated salivary fluid within less than 15 s, and isoniazid release from the ODFs in the same medium followed after the disintegration profiles, achieving rapid and total drug release within less than 60 s. The ease of administration and favorable drug loading and release properties of the ODFs may provide a dosage form able to facilitate proper adherence to treatment within the pediatric patient population.


Author(s):  
K Kareemuddin Ansari ◽  
Neeraj Sharma

Valdecoxib is a selective COX- II inhibitor with anti – inflammatory, analgesic and antipyretic properties. The poor aqueous solubility of the drug leads to variable dissolution rates. In the present study an attempt has been made to prepare fast dissolving tablets of Valdecoxib in the oral cavity with enhanced dissolution rate. The fast dissolving tablets of Valdecoxib was prepared with some carriers (polymers) and super disintegrants such as Polyvinyl Pyrrolidone (PVP), Sodium Carboxy Methyl Cellulose (SCMC), Crospovidone NF and β – Cyclodextrin. The above mentioned all carriers and superdisintegrants were taken in different proportions of 5, 10, and 15%. All the formulations of the fast dissolving tablets of Valdecoxib were prepared by direct compression technique. The blend was examined for Angle of repose, Bulk density, Compressibility index and Hausner’s ratio. The prepared tablets were evaluated for hardness, drug content uniformity, friability, disintegration time and dissolution rate. An effective pleasant testing formulation released 99.88% drug within 10 minutes. The prepared formulations drug release was found to be comparable with the marketed dispersible tablets. Keywords: Fast dissolving tablets, Super-disintegrants, Valdecoxib, Crosspovidone, Sodium Carboxy Methyl Cellulose.


2021 ◽  
Vol 12 (3) ◽  
pp. 1967-1976
Author(s):  
Kumar Babu P ◽  
Venkatachalam A ◽  
Bhaskar Reddy K

The purpose of this study is to make Nebivolol more efficient by converting it into a liquid solid composite compressed tablet. Blending cum sonication process was used to create the liquid solid composite. By altering the independent variables such as vehicle, carrier, and superdisintegrants, nearly 12 compositions were created in a 23 factorial design with four centre points. The influence on response, such as disintegration time in seconds and wetting time in seconds, was then determined. In addition, the liquid solid composite was compacted into a tablet and its percent invitro drug release was assessed. Based on disintegration time and wetting time, the optimal solid liquid compacts sustained release tablet formulation was identified to be LSC6 , which may be ideal candidates for boosting the solubility and dissolution rate of less soluble medications like Nebivolol.


1970 ◽  
Vol 2 ◽  
pp. 42-48
Author(s):  
Md Mosharaf Miazi ◽  
M Mohiuddinn A Choudhury ◽  
M Habibur Rahman ◽  
Abedur Rahman

The objective of this study was to evaluate the effects of magnesium hydroxide (MH) on disintegration time (DT) and dissolution profile of diclofenac sodium (DS) plain tablet. The tablets of DS were formulated with conventionally used excipients and investigational agent Mg [OH]2. Different parameters of tablets like hardness, thickness, friability, and disintegration time and dissolution rate were determined to assess the effects of MH on these parameters. The physical resistance against abrasion or shock of DS-MH tablets had been noticed by the results of hardness and friability test which were within the limits of standard specification. The disintegration times of tablets of the experimental batches except one, found 2.0 to 25 minutes were also within the limits of standard specification. The release rates of DS in simulated gastric fluid (SGF) at 30 minutes were inspiring about batches FO3: 84.78% and FO4: 90.38%. A positive correlation of coefficient determined between quantity of Mg(OH)2 in different batches of tablets and their effects on dissolution rate was found statistically significant (r = 0.66). The tmax of DS was not affected by the presence or increment of MH as evident in rtmax= 0.50. The overall study indicated that Magnesium hydroxide didn't affect the different physical parameters of plain tablet rather it in certain quantity while present in some batches assisted rapid disintegration and release profile of active content Diclofenac sodium. The DS-MH plain tablet to provide rapid disintegration, dissolution and absorption hence fastest anti-inflammatory action with acid neutralizing benefits by MH, might be considered sincerely Key words: Diclofenac Sodium; Magnesium Hydroxide; Disintegration; Dissolution DOI:10.3329/jbsp.v2i0.984 J Bangladesh Soc Physiol. 2007 Dec;(2): 42-48.    


Author(s):  
Zeina D Salman

The present study was aimed to integrate the developed and optimized ketotifen fumarate dispersion into Orodispersible tablets formulations, to enhance the dissolution rate and bioavailability aspects of the drug. Ketotifen fumarate solid dispersion was prepared using different concentrations of poloxamer 407via solvent evaporation and fusion method. Solubility study, x-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) and other investigations were done. Ten formulations of the optimum dispersed ketotifen fumarate Orodispersible tablets were prepared with various superdisintegrants, the results of in vitro - in vivo tests revealed that, the dispersion of the drug in the polymer considerably enhanced the solubility, the batch (Fsd 3) prepared by fusion method showed increased the solubility as ~2-fold compared with a pure drug. FTIR spectra, SEM and XRD data, showed amorphrization of ketotifen fumarate, which explains the better dissolution rate of the drug from its solid dispersions. Formulation F1 containing 15%w/w of crospovidone was showed in vitro- in vivo disintegration time (17 sec., 15 sec. respectively) and percent of drug dissolved in 2 min. was 90.04%, proved to be the optimum formulation, which is required for obtaining rapidly disintegrating tablets. The solubility of the drug had increased, and the resultant orodispersible tablets can be considered as a promising dosage form to achieve better patient compliance.


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