scholarly journals Formulation and Evaluation of Ritonavir Immediate Release Tablets by Hot Melt Extrusion Method

2019 ◽  
Vol 9 (4-A) ◽  
pp. 63-71
Author(s):  
Shaik. Md. Zakir Hussain ◽  
J. Shiva ◽  
Goli Venkateswarlu ◽  
D Suthakaran ◽  
Syed Ghouse

In the present work, an attempt has been made to develop immediate release coated tablets of Ritonavir by hot met extrusion method using 16 station rotary tablet punching machine. The blend of all the formulations showed good flow properties such as bulk density, tapped density. The prepared IR coated tablets of ritonavir shown good post compression parameters. They passed all the quality control evaluation parameters as per USP limits. Among all the formulations, F5 formulation showed maximum % drug release i.e., 99 % in 120 mins hence it is considered as optimized formulation. The optimized formulation was compared to innovator tablets. Keywords: Ritonavir, HPMC, Ethyl cellulose, Copovidone immediate release tablets.

Author(s):  
K Sunand ◽  
V Sandhya ◽  
A Swapna ◽  
K Prasanth ◽  
A Vijaya ◽  
...  

In the present work, an attempt has been made to develop fast disintegrating tablets of Selegiline, were as sodium starch glycolate, cross povidone and cross carmellose sodium were employed as super disintegrating agents to enhance the solubility and dissolution rate of drug molecule. Formulations were prepared by direct compression method using 6mm punch on 8 station rotary tablet punching machine. The blend of all the formulations showed good flow properties such as angle of repose, bulk density and tapped density. The prepared tablets have shown good post compression parameters and they passed all the quality control evaluation parameters as per IP limits. Among all the formulations F2 formulation showed maximum percentage drug release i.e., 97.26 % in 45 min, hence it is considered as optimized formulation. The F2 formulation contains SSG as super disintegrate in the concentration of 24mg.


2017 ◽  
Vol 8 (4) ◽  
Author(s):  
Bhukya Nagaraju ◽  
B Ramu ◽  
S V Saibaba ◽  
B Rajkamal

<p>In the present work, an attempt has been made to develop gastro retentive floating tablets of Doxofylline<strong> .</strong>HPMC K4M and carbopol were used as controlled release polymers<strong>.</strong> All the formulations were prepared by direct compression method on 12 station rotary tablet punching machine. The blend of all the formulations showed god flow properties such as angle of repose, bulk density, tapped density. The prepared tablets were shown good post compression parameters and they passed all the quality control evaluation parameters as per I.P limits. FH 5 was the best optimized floating formulation because it released drug completely in 12hrs.It was also observed that the increasing concentration of polymers had a retarding effect on the drug release from the polymer matrices.</p>


2015 ◽  
Vol 14 (9) ◽  
pp. 1541-1547
Author(s):  
T Dang ◽  
Y Cui ◽  
Y Chen ◽  
X Meng ◽  
B Tang ◽  
...  

Purpose: To prepare and evaluate colon specific drug delivery system of diclofenac sodium for highly localized delivery to the colon.Methods: The colon specific drug delivery system was prepared as matrix-type microspheres using Ethyl Cellulose (EC), Cellulose Acetate Phthalate (CAP), and Eudragit L 100-55 by the Solvent Evaporation Method. Microspheres were evaluated for physical properties like drug content, particle size, bulk density and angle of repose.Results: The size range of the microcapsules was 228 to 608 μm while drug content was between 74.49 and 91.50 % depending on the polymer used and the  polymer ratio. Mean bulk density was < 1.2 g/ml which indicates the good flow properties, while angle of repose was < 40 o, indicating free-flowing properties. The microspheres were spherical in shape with smooth and nonporous surface, except that the microspheres containing EC and CAP exhibited a rough and porous  surface. The microspheres containing Eudragit L 100-55 in combination with other polymers gave better sustained release (78.9 and 76.6 % at the end of 8 h for  formulation F4 and F5, respectively) than the others.Conclusion: Microspheres prepared with drug: EC: CAP ratio of 1:2:1 show the highest drug content, possess good flow properties and surface morphology, as well as promising drug release for colon specific drug delivery of diclofenac sodium for possible treatment of colorectal cancer.Keywords: Diclofenac, Colorectal cancer, Microspheres, Ethyl cellulose, Cellulose acetate phthalate, Eudragit L 100-55


2018 ◽  
Vol 6 (4) ◽  
pp. 81-85 ◽  
Author(s):  
S S Dudhamal ◽  
P S Kawtikwar ◽  
S N Nagoba

Lagenaria siceraria (Bottle gourd) is a common name in every household. Its medicinal values were identified many years ago, and still people use this plant for many disorders. Extrusion spheronization technique was employed for preparation of the pellets, to study the effect of crosscarmellose sodium, on it. The pellets were prepared by use of combination of Avicel PH 101 and lactose that indicated good flow properties. The superdisintegrant used was crosscarmellose sodium between concentration 2 to 8%, to study the effect of it on the pellets. The superdisintegrant showed low disintegration time at low concentration, while as the concentration of it increased, it extended the disintegration time. Thus, optimum concentration needs to be designed for successful formulation. Batch D3 of 6% crosscarmellose sodium concentration showed the requisite characteristic in terms of all the evaluation parameters, with DT up to 50 to 55 seconds. Thus, use of this superdisintegrant alone, but in low concentration, can be helpful, or else combination of this with other superdisintegrants can be approached, or else new superdisintegrants can be tried. Thus, the study indicated the effect of superdisintegrant for formulation of dispersible pellets. Keywords: Extrusion-Spheronization,  Crosscarmellose sodium, Lagenaria siceraria, Pellets


2020 ◽  
Vol 35 (5) ◽  
pp. 458-470
Author(s):  
S. Gopi ◽  
B. A. Ramsay ◽  
J. A. Ramsay ◽  
M. Kontopoulou

Abstract Blends of polycaprolactone (PCL) and poly(3-hydroxyoctanoate) P(3HO) were prepared by melt compounding. These immiscible blends exhibited droplet-matrix morphology at compositions up to 30 wt% P(3HO). Even though the addition of amorphous P(3HO) decreased the crystallinity of PCL, the crystallization temperature of the blends increased by 6 to 7 8C. Blends containing up to 30 wt% P(3HO) had higher crystallization rates, and lower crystallization half-times compared to neat PCL. The viscosity of PCL decreased upon addition of P(3HO), making the blends suitable for processing using a 3D bioplotter. Compositions with 10 to 30 wt% P(3HO) were ideal for processing, because of their improved crystallization kinetics, reduced stickiness and good flow properties. Estimation of the interfacial tension by fitting the Palierne model to the linear viscoelastic properties of the blends revealed good compatibility, which gave rise to synergistic effects in the thermal and mechanical properties. The fibres prepared by 3D bioplotting maintained droplet matrix morphology, with finer particle size than the original compounded material. In addition to favourable viscosity and thermal properties, the extruded fibres containing 30 wt% P(3HO) had comparable modulus to the neat PCL, while exhibiting good ductility. These blends may be suitable alternatives to PCL for biomedical applications, because they provide a range of crystallinities, crystallization rates and viscosities.


2013 ◽  
Vol 89 (Suppl 1) ◽  
pp. A379.1-A379
Author(s):  
A Bolzan ◽  
M Bazzo ◽  
E Santos ◽  
E Ayer ◽  
L Wildner ◽  
...  

2021 ◽  
Vol 11 ◽  
Author(s):  
Hardik Rana ◽  
Rushikesh Chaudhari ◽  
Vaishali Thakkar ◽  
Tejal Gandhi

Background: The better control of the drug release with immediate effect is the major concern to achieve better therapeutic action and patient compliance. The failure of the solid dispersion complex during storage as well as in-vivo is another concern for the oral solid dosage form. Objective: The prime objective of the present study was to optimize the biphasic minitablet incorporating quality by design approach using the combination of waxy erodible and water-impermeable excipients. Exploration of Soluplus as a precipitation inhibitor and Dexolve as a solubility enhancer in oral solid dosage form was the secondary objective. Methods: The drug-Excipient compatibility study was assessed by FTIR. Clozapine was chosen as a model drug that has poor aqueous solubility. The complex was formulated using B-cyclodextrin or HP B-CD or Dexolve by kneading method. The screening of solubility enhancers and their amount were performed based on phase solubility study. The precipitation inhibitor was screened as per the parachute effect study. Immediate release minitablets were formulated using a direct compression method using different disintegrating agents. The IR minitablets were evaluated for different evaluation parameters. The sustained release minitablets was formulated by hot-melt granulation technique incorporating the Precirol ATO 5 as a waxy excipient and ethyl cellulose as water impermeable excipient. The SR minitablet was optimized using a central composite design. The amount of Precirol ATO 5 and ethyl cellulose were chosen as independent variables and % drug release at 1, 6, and 10 h was selected as responses. The designed batches were evaluated for different pre and post compressional parameters. The IR and SR minitablets were filled in a capsule as per dose requirement and evaluated for in-vitro drug release. The in-vivo plasma concentration was predicted using the Back calculation of the Wagner – Nelson approach. Results: Drug – Excipient study revealed that no significant interaction was observed. Dexolve was screened as a solubility enhancer for the improvement of the solubility of clozapine. The Soluplus was chosen as a precipitation inhibitor from the parachute effect study. The immediate-release tablet was formulated using Prosolv EASYtab SP yield less disintegration time with better flowability. The sustained release mini-tablet was formulated using Precirol ATO 5 and ethyl cellulose. Two-dimensional and three-dimensional plots were revealed the significant effect of the amount of Precirol ATO 5 and ethyl cellulose. The overlay plot locates the optimized region. The in-vitro drug release study revealed the desired drug release of the final combined formulation. The in-vivo plasma concentration-time confirms the drug release up to 12h. Conclusion: The biphasic mini-tablets were formulated successfully for better control of drug release leads to high patient compliance. The use of soluplus as a precipitation inhibitor is explored in the oral solid dosage form for a poorly aqueous drug. Prosolv EASYtab SP was incorporated in the formulation as super disintegrant. The amount of Precirol ATO 5 and ethyl cellulose had a significant effect on drug release in sustained-release minitablet. The approach can be useful in the industry.


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