scholarly journals Performance Evaluation of a Novel Biosourced Co-Processed Excipient in Direct Compression and Drug Release

Polymers ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 988
Author(s):  
Rihab Benabbas ◽  
Noelia M. Sanchez-Ballester ◽  
Adrien Aubert ◽  
Tahmer Sharkawi ◽  
Bernard Bataille ◽  
...  
Keyword(s):  
Drug Release ◽  
Physical And Mechanical Properties ◽  
Release Time ◽  
Direct Compression ◽  
Disintegration Time ◽  
Ejection Force ◽  
Tablet Tensile Strength ◽  
Powder Flowability ◽  
Biopharmaceutical Properties ◽  
Dilution Potential

This study exposes the potential usefulness of a new co-processed excipient, composed of alginic acid and microcrystalline cellulose (Cop AA-MCC), for the preparation of immediate drug release tablets by direct compression. Evaluation of the physical and mechanical properties as well as the disintegration behavior of Cop AA-MCC in comparison to commercial co-processed excipients (Cellactose®, Ludipress®, Prosolv® SMCC HD90 and Prosolv® ODT) and to the physical mixture of the native excipients (MCC and AA), was carried out. The obtained results illustrate the good performance of Cop AA-MCC in terms of powder flowability, tablet tensile strength, compressibility, and disintegration time. Although, this new co-processed excipient showed a slightly high lubricant sensitivity, which was explained by its more plastic than fragmentary deformation behavior, it presented a low lubricant requirement due to the remarkably low ejection force observed during compression. Compression speed and dwell time seemed not to affect significantly the tabletability of Cop AA-MCC. The study exposed evenly the performance of Cop AA-MCC compared to Prosolv® ODT, in terms of tabletability and dissolution rate of Melatonin. Cop AA-MCC presented comparable hardness, lower dilution potential, higher lubricant sensitivity, lower ejection force, and faster Melatonin’s release time than Prosolv® ODT. In summary, Cop AA-MCC exhibited interesting physical, mechanical, and biopharmaceutical properties, which demonstrate its concurrence to commercially available co-processed excipients. Furthermore, the simplicity of its composition and the scalability of its elaboration makes this multifunctional excipient highly recommended for direct compression.

scholarly journals FORMULATION AND EVALUATION OF ORAL FAST DISINTEGRATING TABLET OF IBUPROFEN USING TWO SUPER DISINTEGRANTS

2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Orally Disintegrating Tablet ◽  
Rapid Release ◽  
Weight Variation ◽  
Fast Disintegrating Tablet

Objective: The aim of the present investigation was to design and evaluate orally disintegrating tablet (ODT) of Ibuprofen, a NSAID drug used for the treatment of arthritis with a view to improve its oral bioavailability. The focus of the current study was to develop ODT of Ibuprofen using super disintegrants for ease of administration and its physicochemical characterization.Methods: Tablets were made from blends by direct compression method. All the ingredients were passed through mesh no. 80. All the ingredients were co-ground in a pestle motor. The resulting blend was lubricated with magnesium stearate and compressed into tablets using the Cadmach single punch (round shaped, 8 mm thick) machine.Results: Physicals parameters of the prepared tablets like Hardness, Weight variation, Friability, thickness, drug content etc. found within the limits. The disintegration time of prepared ODTs was in the range of 45 to 55 seconds. In vitro dispersion time was found to be 22 to 52 seconds which may be attributed to faster uptake of water due to the porous structure formed by super disintegrants. Short disintegration and faster release of ibuprofen were observed with Cross carmellose sodium as compared to sodium starch glycollate.Conclusion: It is concluded that F3 offered the relatively rapid release of Ibuprofen when compared with other formulations. The increase in the concentrations of super disintegrants may lead to increase in the drug release. The formulation prepared with cross carmellose sodium was offered the relatively rapid release of Ibuprofen when compared with other concentrations of both the super disintegrant. 

scholarly journals Effect of a co-processed excipient on the disintegration and drug release profile of ibuprofen tablets

Bio-Research ◽  
2020 ◽  
Vol 18 (1) ◽  
Author(s):  
BB Mohammed ◽  
EJ John ◽  
NK Ajuji
Keyword(s):  
Drug Release ◽  
Release Profile ◽  
Angle Of Repose ◽  
Oral Dosage ◽  
Direct Compression ◽  
Drug Release Profile ◽  
Disintegration Time ◽  
Crushing Strength ◽  
Tablet Properties ◽  
Spray Dried

Tablets at present, remain the most preferred oral dosage form because of many advantages they offer to formulators as well as physicians and patients. The objective of this work was to determine the effect of co-processing on the disintegration and drug-release profile of ibuprofen tablets prepared from a co-processed excipient. The co-processed excipient (CE) containing lactose, gelatin and mucin in the ratio 90:9:1 was prepared using co-fusion. The excipient was evaluated for its physicochemical properties and then used to formulate tablets with the addition of a disintegrant by direct compression. The tablets were evaluated for their tablet properties and compared with tablets prepared with cellactose- 80® (CEL) and spray dried lactose® (SDL) and a physical mix (PM) of the co-processed ingredient. Results from evaluation of CE showed that flow rate, angle of repose, Carr’s index and Hausner’s ratio were 5.28 g/sec, 20.30o, 23.75 % and 1.31, respectively. Tablets prepared with CE had friability (0%), crushing strength (5.25) KgF, disintegration time (3 mins) and T50% (2 mins). For CEL, friability (0.4 %), crushing strength (7.25) KgF, disintegration time (1 min) and T50% (2 mins); SDL, friability (1.57 %), crushing strength (7.50) KgF, disintegration time (4 mins) and T50% (2 mins) and PM, friability (2.38 %), crushing strength (5.00) KgF, disintegration time (1 min) and T50% (2 mins). In conclusion, the disintegration time and drug release profile for CE was not superior but compared favorably with CEL, SDL and PM.  

scholarly journals FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISINTEGRATING TABLETS OF CINITAPRIDE HYDROGEN TARTARATE BY USING DIRECT COMPRESSION TECHNIQUE

2017 ◽  
Vol 9 (6) ◽  
pp. 98 ◽  
Author(s):  
Krishna Mohan Chinnala ◽  
Sirish Vodithala
Keyword(s):  
Drug Release ◽  
Water Absorption ◽  
Bulk Density ◽  
Direct Compression ◽  
Disintegration Time ◽  
Absorption Ratio ◽  
Wetting Time ◽  
Tapped Density ◽  
Fast Disintegrating Tablets

Objective: In the present study, efforts were taken to develop fast disintegrating tablets of Cinitapride hydrogen tartrate, is a gastro-prokinetic agent and antiulcer agent with an objective to achieve rapid disintegration, and further improving the bioavailability of the drug. Also, to resolve the swallowing problems (Dysphasia) in pediatric, geriatric patients by rapid disintegration in saliva and improve the patient compliance.Methods: Fast disintegrating tablets were prepared by direct compression method using superdisintegrants like crospovidone (CP), croscarmellose sodium (CCS), sodium starch glycolate (SSG) and combination of super-disintegrants in different concentrations. The prepared formulations were evaluated for the pre-compression parameters like bulk density, tapped density, Carr’s compressibility, Hausner’s ratio and angle of repose. The prepared batches of fast disintegrating tablets of Cinitapride hydrogen tartarate were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time, water absorption ratio, and in vitro dissolution profile.Results: Bulk density and tapped density were found in the range of 0.412–0.432 g/cc and 0.507–0.528 g/cc respectively. In all formulations, tablet weight and thickness were within mean±9.5% and mean±5% respectively. Wetting time values lie between 19.76 to 39.53 sec. Water absorption ratio ranged from 57.30 to 78.82 %. The in vitro disintegration time for all the 12 formulations varied from 17.43 to 38.61 seconds. Formulation F8 which contained crosspovidone have recorded drug release 96.94±0.47% at the end of 30 min.Conclusion: The formulation containing crospovidone (F8) showed better performance in terms of disintegration time and drug release when compared to other formulations.

Optimization and In Vitro Evaluation of Famotidine Loaded Effervescent Orally Disintegrating Tablets using a Central Composite Design

2021 ◽  
Vol 16 ◽  
Author(s):  
Ramesh Kumar ◽  
Ravinder Verma ◽  
Ritu Kaushik ◽  
Prerna Kaushik ◽  
Parijat Pandey ◽  
...  
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Central Composite Design ◽  
Pediatric Population ◽  
Direct Compression ◽  
Disintegration Time ◽  
Orally Disintegrating Tablets ◽  
Swallowing Problems ◽  
Central Composite

Background: Over the years, effervescent orally disintegrating tablets (ODTs) have proved their worth over conventional tablets in overcoming the swallowing problems associated with the geriatric and pediatric population. The addition of effervescent agents in ODT provides a rapid disintegration along with masking of the slightly bitter taste of drugs and is worth exploring. Objective: The present research investigation deals with the preparation of effervescent ODTs by direct compression with rapid disintegration and adequate hardness using the central composite design response surface methodology. Method: Central composite design was used to study the effect of concentration of crospovidone (X1) and concentration of citric acid and sodium bicarbonate (X2) as independent factors on the two responses: disintegration time (Y1) and drug release (Y2). The tablets were prepared by direct compression approach using directly compressible mannitol. Results: Central composite design was used to study the effect of concentration of crospovidone (X1) and concentration of citric acid and sodium bicarbonate (X2) as independent factors on the two responses: disintegration time (Y1) and drug release (Y2). The tablets were prepared by direct compression approach using directly compressible mannitol. Conclusion: The results obtained in the present investigation revealed a successful development of famotidine effervescent ODTs with a better release profile compared to marketed formulation.

Formulation and Evaluation of Fast Dissolving Tablet of Ondansetron by Utilizing Liquisolid Compact Technique

2021 ◽  
pp. 163-168
Author(s):  
Sanket Jain ◽  
Sujit Pillai ◽  
Rampal Singh Mandloi ◽  
Nikhlesh Birla
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Compression Method ◽  
Disintegration Time ◽  
Dissolution Studies ◽  
Drug Content ◽  
Ftir Studies ◽  
Site Of Action

Ondansetron is an anti-emetic drug which is insoluble in water. The present study was aimed to formulate and evaluate oral fast dissolving tablet of Ondansetron by Utilizing Liquisolid Compact Technique. The tablets were prepared by direct compression method and characterized by UV, FTIR studies. Six formulations (F1-F6) of ondansetron were prepared and tablets were evaluated for weight variations, hardness, thickness, friability, disintegration time, drug content and In-vitro dissolution studies gave satisfactory result. TF6 was found to be the best and acceptable formulation whose drug content was about 99.17±0.05 and percentage (%) drug release 97.49±2.03 in 10 min, high as compare to other formulation and has low disintegration time 17±0.01 as compare to other formulation which indicates that drug is rapidly dissolved and available at the site of action.

FORMULATION AND EVALUATION OF MICROSPHERE BASED ORO DISPERSIBLE TABLETS OF SUMATRIPTAN SUCCINATE

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (03) ◽  
pp. 28-38
Author(s):  
S. B. Baliga ◽  
B. P Manjula ◽  
M. Geetha ◽  
Keyword(s):  
Drug Release ◽  
Liquid Paraffin ◽  
Entrapment Efficiency ◽  
Taste Masking ◽  
Direct Compression ◽  
Disintegration Time ◽  
Sumatriptan Succinate ◽  
Dispersible Tablets ◽  
Effervescent Agents

Sumatriptan succinate (SS) is a drug used in the treatment of migraine headaches, but suffers from low patient compliance due to its unpalatable bitter taste. The purpose of the present work was to prepare taste-masked oro dispersible tablets (ODTs) of SS by incorporating drug loaded microspheres into tablets for use in patients experiencing difficulty in swallowing. Microspheres loaded with SS were prepared by solvent evaporation technique. Eudragit EPO, a pH-sensitive aminoalkylmethacrylate copolymer, was used for coating the drug particles, acetone as solvent for the polymer and light liquid paraffin as an encapsulating medium. Drug : polymer ratio of 1:1 was considered to be optimized formulation with a yield of 99.96%, entrapment efficiency of 61.55%, particle size ranging from 30.32 – 90.96μm and in vitro drug release of 85.06% within an hour. FTIR studies suggested absence of drug-excipient interaction. Tablets prepared by direct compression containing microspheres and effervescent agents were evaluated for pre-compression and post-compression parameters. The wetting time, in vitro dispersion time and in vitro disintegration time of the tablets were found to be 39 sec, 35 sec and 32 sec, respectively. The drug release from the tablet was about 85.44% within an hour. The SEM of final ODTs revealed that the microspheres remained intact even after compression. Stability studies indicated that the selected formulation was stable. The results obtained suggested that effective taste-masking was achieved for SS using the technique of microencapsulation and ODTs of acceptable characteristics were obtained by adding effervescent agents followed by direct compression.

scholarly journals Disintegrant Properties of Microcrystalline Cellulose isolated from Rami (Boehmeria nivea L. Gaud) in Dimenhydrinate tablets by Wet Granulation and Direct compression

2021 ◽  
Vol 2 (3) ◽  
Author(s):  
Nagina Gulab Belali ◽  
Anis Y. Chaerunisaa ◽  
Taofik Rusdiana
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Physical Properties ◽  
Process Parameters ◽  
Microcrystalline Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Disintegration Time ◽  
Boehmeria Nivea ◽  
Significant Difference

Microcrystalline cellulose was isolated from rami (Boehmeria Nivea L. Gaud), and applied as disintegrant in tablets of dimenhydrinate, made by direct compression and wet granulation. The aim of this study is to produce dimenhydrinate tablets with Microcrystalline Cellulose Rami (MCC Rami) isolated from Rami (Boehmeria Nivea L. Gaud), as a disintegrant and assess the effect of MCC Rami and Granulation technique on physical properties of drug such as, disintegration time, drug release and dissolution. Formulations of dimenhydrinate 100mg tablets were prepared with a combination of mannitol and lactose as a filler and MCC Rami as disintegrant in a concentration of 10-20%. The formulas were directly compressed or were compressed into tablets after wet granulation. The mechanical properties, drug release, physical properties and effects of process parameters, methods of applying disintegrant in tablet formulas were examined. A significant difference in disintegration time of tablets that were produced by direct compression and wet granulation was seen, that can be attributed to the porous structure of granules that enhanced fast disintegration, which had eventually improved dissolution and drug release. F1 and F2 with MCC Rami and physical mixture of MCC Rami with crosspovidone as a disintegrant that were directly compressed disintegrated in 79 and 72 seconds respectively thats not a significant difference, however when MCC was applied in an intragranular way its disintegration time is 67 seconds. The results showed that the method of disintegrant application and press of tableting has a significant effect on drug release and dissolution.Keywords : Microcrystalline Cellulose, wet granulation, disintegrant, Boehmeria Nivea L. Gaud.

scholarly journals FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF LAMOTRIGINEUSING DISCRETE SUPER DISINTEGRANTS AND COPROCESSED EXCIPIENTS

2020 ◽  
pp. 28-35
Author(s):  
RAJASEKHAR POONURU ◽  
ROHINI CHERUKU ◽  
PAVAN JULURI ◽  
KHADEERA JABEEN ◽  
SWETHA SREERAMULA ◽  
...  
Keyword(s):  
Drug Release ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Eudragit E ◽  
Orodispersible Tablet ◽  
Wetting Time ◽  
Prompt Action ◽  
Extrusion Method

Objective: The present study was designed to formulate and evaluate the orodispersible tablets of lamotrigine after enhancing its solubility. Methods: Lamotrigine was made into an inclusion complex with eudragit E 100 my kneading and mass extrusion method and later this mixture is compressed into orodispersible tablet using various super disintegrants and co-processed excipients to reduce the disintegration time for providing prompt action through rapid drug release. Results: Lamotrigine ODTs containing F-melt (F1-3%, F2-5%) dispersed in lesser time of (9±0.11) and (21±0.58) compared to formulations with polyplasdone XL-10 and primellose as super disintegrants respectively with F1 showing short wetting time. The water absorption was also was found to be more for formulation with 3% F-Melt. Conclusion: Lamotrigine orodispersible tablets were prepared by direct compression technique by using 3% and 5% of three super disintegrants (f-melt, primellose and polyplasdone XL-10). Disintegration time of F1 (3% f-melt) formulation was found to be least (7 sec).

scholarly journals FORMULATION AND EVALUATION OF ORODISPERSIBLE TABLETS OF A MODEL ANTI-HYPERTENSIVE DRUG

2017 ◽  
Vol 9 (10) ◽  
pp. 34
Author(s):  
S. P. Hiremath ◽  
Chidambar Makanapur
Keyword(s):  
Drug Release ◽  
Dissolution Time ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Drug Content ◽  
Orodispersible Tablets ◽  
Time Dispersion ◽  
Wetting Time ◽  
Croscarmellose Sodium

Objective: The rationale of the current work was to formulate and evaluate orodispersible tablets by direct compression technique with a vision to augment patient compliance and rapid onset of action.Methods: Nine orodispersible formulations of propranolol were formulated by direct compression method using sodium starch glycolate, crospovidone and croscarmellose sodium as the super disintegrants. The prepared formulations were evaluated for wetting time, drug content, in vitro disintegration time, dispersion time, dissolution time and also projected to kinetic treatment to know the pattern of drug release. Further, the discovered promising formulation was subjected to stability studies.Results: Based on the results obtained, formulation F9 containing6 mg of croscarmellose sodium exhibited good wetting time, dispersion time, and disintegration time and drug release compared to orodispersible tablets prepared with other super disintegrants. The stability studies piloted as per International Conference on Harmonisation guidelines on the promising formulationF9disclosedno significant changes in the colour (white), drug content (94.87±0.141 mg), hardness (2.93±0.18 kg/cm2), disintegration time (17.11±0.089 s), and drug release after 4 w. After 60 s, the percentage drug release of F9 was found to be 98.52 % and 96.30 % after 1 and 4 w, respectively.Conclusion: Orodispersible tablets of propranolol hydrochloride were formulated successfully by employing direct compression technique. From the investigation, it can be reasonably concluded that F9 batch orodispersible tablets of propranolol with 6 mg of crospovidone exhibited maximum cumulative drug release in 60 s.

scholarly journals Formulation and Evaluation of Piroxicam Fast Dissolving Tablets Using Direct Compression and Sublimation Method

2020 ◽  
Vol 10 (3-s) ◽  
pp. 17-25
Author(s):  
Inder Kumar ◽  
Dipima Chaudhary ◽  
Bhumika Thakur ◽  
Vinay Pandit
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Stability Study ◽  
Drug Dissolution ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Sublimation Method ◽  
The Stability

Objective: In the present research work, fast dissolving tablets of Piroxicam were formulated by two different techniques i.e. direct compression method and sublimation method using different superdisintegrants. Methods: Twelve formulations were prepared (PXM1 to PXM12) in which first six formulation were prepared by direct compression technique and other six formulation were prepared by sublimation method by using camphor as a sublimating agent. Result and Discussion: All the formulations were subjected for precompression, post compression parameters, and shows all the data within the specific limits. Formulation PXM4 containing 5 % crospovidone showed 99.480 ± 0.291 % drug release in 20 min which was more than the drug release of rest of the formulations. The optimized formulation PXM4 was compared with the marketed formulation and it revealed that drug release of PXM4 was found to be 99.397 ± 0.751 % in 20 min, which was greater than the marketed formulation. Finally, results were statistically analysed by the application of one way ANOVA and t-test. The stability study of the optimized formulation PXM4 showed no significant changes in, drug content, disintegration time and in-vitro drug release. Conclusion: Piroxicam can be successfully prepared using direct compression technique and it will enhance the drug dissolution, which will further increase absorption and bioavailability of the drug. Keywords: Direct compression, fast dissolving tablets, sublimation, Piroxicam.

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