scholarly journals Modification of natural hydrocolloid as disintegrant in aceclofenac tablet formulation

2021 ◽  
Vol 11 (2) ◽  
pp. 42-50
Author(s):  
Vandana Gupta ◽  
Ashish Manigauha

The purpose of present exploration was to modify kappa (k)-Carrageenan, by crosslinking, and assessed it as a tablet disintegrant to strengthen the solubility of the drug (aceclofenac) in tablet formulation. Modified k-Carrageenan was synthesized by reacting it with epichlorhydrin at heterogenous  conditions. The swelling action of the product was investigated in order to optimize reaction circumstances for chemical cross-linking. Best modified k-Carrageenan procured by optimizing the reaction conditions and it was characterized for swelling index, particle size distribution, solubility, viscosity, gel strength and Fourier transform infrared spectroscopy (FTIR). Influence of modified k-Carrageenan on dissolution profile of therapeutic was also investigated along with other evaluation parameters. Modified k-Carrageenan exhibiting significant swelling index which is comparable to that of superdisintegrants. On comparative investigation as a tablet disintegrant by preparing anhydrous dicalcium phosphate tablet, modified k-Carrageenan showed disintegration time less than 20 seconds. Dissolution of aceclofenac (Class II) tablet formulaion utilizing modified k-Carrageenan was comparable with commercially available superdisintegrants. Faster dissolution of the accommodated drug was achieved with modified k-Carrageenan which was comparable with dissolution of the tablet formulation containing other superdisintegrants. The competent concentration of k-Carrageenan was found to be 5-15% as tablet disintegrant. Modified k-Carrageenan might be encouraging tablet disintegrant in fast dissolving formulations and can be worn in direct compression method. Keywords: k-Carageenan. Epichlorhydrin. Aceclofenac. Crosslinking. Superdisintegrant

Author(s):  
Vo Thanh Hoa ◽  
Bui Thi Thu Huong ◽  
Do Quang Duong ◽  
Nguyen Duc Hanh

Objective: The E. ulmoides and G. jasminoides (EG) tablets containing 67 mg E. ulmoides spray-dried extract (ESE) and 173 mg G. jasminoides spray-dried extract (GSE) were prepared by employing the direct compression method. Due to the poor flowability and compressibility of the two spray-dried extracts, various excipients were added at different ratios so that the blends can be compressed into tablets with the required standards. This study aimed at the cause-effect relations and optimization of the EG tablet formulation.Methods: Different diluents including dibasic calcium phosphate anhydrous (DCPA), silicified microcrystalline cellulose (SMCC), spray-dried lactose (SDL) and the active ingredients (blend of ESE and GSE at the ratio of 67:173, w/w) were separately investigated their own physical properties. The binary mixtures of the active ingredients with different ratios of DCPA, SMCC, and SDL were evaluated their flowability. D-optimal design based on three independent variables (% DCPA, % croscarmellose sodium (CCS) and % SMCC) was applied to evaluate the cause-effect relations and optimize the EG tablet formulation. The weight variation, disintegration time, hardness and friability were investigated as four dependent variables.Results: The flowability of the powders was found to be affected by the particle size distribution, particle shape and density. The three diluents could significantly improve the flowability of the active ingredients. All independent variables had significant effects on the dependent variables. An increase in % SMCC reduced the weight variation, hardness and increased the friability of tablets. Disintegration time was found to be in the negative relations with % CCS. The tablet hardness was in positive relations with % DCPA. The optimized EG tablet formulation composed of 9 % DCPA (w/w), 35 % SMCC (w/w), and 14 % CCS (w/w) of the excipient blend. The weight variation, disintegration time, hardness and friability of the optimized EG tablets were found to be 1.8 %, 11.7 min, 61.4 N, and 0.5 %, respectively.Conclusion: The ESE and GSE could be formulated into tablet by using direct compression method. The cause-effect relations and optimization of EG tablet formulation were studied and reported for the first time.


2017 ◽  
Vol 9 (4) ◽  
pp. 92
Author(s):  
Hrishav Das Purkayastha ◽  
Bipul Nath

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. 


2020 ◽  
Vol 859 ◽  
pp. 3-8
Author(s):  
Vipaluk Patomchaiviwat ◽  
Sontaya Limmatvapirat ◽  
Chaisai Sirisapaya ◽  
Rohanee Kolae ◽  
Kulmanee Anantakul ◽  
...  

The objective of this study was to investigate the effect of modified hydroxypropyl tapioca starch (HPTS) and % drug loading on physical property of tablet. Paracetamol was used as model drug because of its poor compressibility. The filler ability of modified HPTS such as hydroxyl propyl oxidized tapioca starch (HPOTS), hydroxyl propyl crosslinked tapioca starch (HPCTS) and pregelatinized tapioca starch (PTS) were evaluated and compared with the commercial starch (Starch 1500®). Tablets were prepared by direct compression method and the percent drug loading were 15, 30, 45, 60, 75%. For modified HPTS, the hardness of the tablets tended to decrease when the concentration of paracetamol increased. At drug concentrations of 15-30%, HPOTS exhibited good performance of tablet as indicated by the high hardness, low friability and acceptable disintegration time. The obtained results were better than HPTS and comparable to Starch 1500®. Moreover, the results revealed that tablet containing PTS provided the highest hardness and prolonged disintegration time (>30 min) while tablet containing HPCTS showed rapid disintegration time (<2 min). Therefore, modified HPTS disclosed promising properties for application as tablet filler


Author(s):  
Bui Thi Thu Huong ◽  
Boonyaphat Monsatta ◽  
Nguyen Duc Hanh ◽  
Phan Hoang Doan Phuong ◽  
Do Quang Duong

Objective: The aim of this study was to develop and optimize the formulation of tablets containing Aquilaria crassna extract using the direct compression method.Methods: D-optimal design based on three independent variables was applied to evaluate the cause-effect relations and optimize the A. crassna tablet formulation. The weight variation (Y1), disintegration time (Y2), hardness (Y3) and friability (Y4) were investigated with respect to three independent variables including % dicalcium phosphate anhydrous (DCPA) in filler (X1), % filler (X2) and % croscarmellose sodium (CCNa) (X3). The dissolution study of the optimized A. crassna tablets were investigated in simulated gastric fluid (SGF) (pH 1.2) using a validated high-performance liquid chromatography (HPLC) method for mangiferin analysis.Results: All investigation factors were found to have significant effects on the physical properties of A. crassna tablet. The tablet hardness and the disintegration time increased in positive relations with the ratios of DCPA. The results exhibited the negative relations between disintegration time and the percentages of CCNa. The optimized A. crassna tablet formulation which included 35 % (w/w) DCPA in filler, 60 % (w/w) filler and 7% (w/w) CCNa possessed the weight variation of 1.38 % (w/w), the disintegration time of 6.29 min, the hardness of 85.63 N and the friability of 0.41 % (w/w). The optimized A. crassna tablet formulation was experimentally examined which demonstrated a good agreement between the experimental and predicted values. Mangiferin was found to release completely from the optimized A. crassna tablets within 30 min.Conclusion: The cause-effect relations and optimization of A. crassna tablet formulation were investigated and reported for the first time. The A. crassna spray-dried extract could be formulated into tablet by direct compression method with good mechanical properties and acceptable release profile.


2016 ◽  
Vol 27 (1) ◽  
pp. 58-61
Author(s):  
Valeriu Iancu ◽  
Florentina Roncea ◽  
Radu George Cazacincu ◽  
Dumitru Lupuleasa

Abstract Orally disintegrating tablets (ODTs) are dosage forms which disintegrate in mouth within seconds without need of water. This type of quality in dosage form can be attained by addition of different varieties of excipients. Pharmaburst™ 500 is a co-processed excipient system which allows rapid disintegration and low adhesion to punches. The aim of the present study was to develop and evaluate 25 mg diclofenac sodium ODTs (orodispersible tablets) batches by direct compression method at different compression forces 10 kN (F1) and 20 kN (F2) and directly compressible excipients used in different ratio (Avicel PH 102, magnesium stearate and coprocessed excipient Pharmaburst™ 500, 70% and 80% w/w). The obtained batches were analyzed for appearance, tablet thickness, uniformity of weight, hardness, friability, disintegration time, and non-compendial methods (wetting time). Co-processed Pharmaburst™ 500 excipient 70% used for sodium diclofenac ODT obtaining determined good results for quality control tests evaluation.


2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Y. Eshovo Apeji ◽  
IY. Muhammad ◽  
A. Kehinde Olowosulu ◽  
G. Owoicho Okpanachi ◽  
A. Rukayat Oyi

Abstract Diluents are essential components of a tablet formulation. The type of diluent used in a formulation influences the quality of tablets produced from that formulation. The aim of this study was to evaluate the tableting properties of co-processed excipients (C-PEs) incorporated as diluents in tablet formulation by wet granulation. Metronidazole tablets were prepared by wet granulation incorporating different diluents that were either single component excipients (SCEs) (lactose and microcrystalline cellulose) or C-PEs (Ludipress®, StarLac®, Prosolv® and AVICEL®HFE). The granules obtained for each formulation were evaluated for particle size analysis, flow properties and compression properties. Tablets weighing 500 mg were compressed from the metronidazole granules on a Single Station Tablet Press using a 12 mm punch and die tooling system. The tablets were kept for 24 h post-production, and the properties of weight uniformity, thickness, tensile strength, friability, disintegration time and dissolution profile evaluated subsequently. Results of granule properties showed that variations in parameters evaluated was as a result of differences in the type and composition of diluent used in formulation. Compactibility and tabletability profile of metronidazole granules revealed a better performance with granules processed with C-PE based diluents compared to SCE-based diluents. Tablets formulated with C-PEs as diluents were uniform in tablet weight, disintegrated faster and yielded a faster drug release compared to tablet formulations containing SCEs as diluent. This study reveals the performance advantage of C-PEs as diluents in tablets manufactured by wet granulation and highlights the importance of rational selection of excipients during tablet formulation.


2021 ◽  
Vol 10 (6) ◽  
pp. 3781-3788
Author(s):  
Peeush Singhal

Background Around 33% of the populace (fundamentally pediatric and geriatric) has gulping hardships, bringing about helpless consistence with oral tablet drug treatment which prompts decreased in general treatment viability. For this explanation, tablets that can quickly break down or deteriorate in the oral cavity have drawn in a lot of consideration. Objective research was designed to develop and evaluate boosted orally fast disintegrating tablets (OFDT) for oro-buccal drug delivery of oseltamivir phosphate. Methods In the present study six formulations of mouth dissolving tablet of oseltamivir were prepared by direct compression method using SSG as a super disintegrating agent with lactose, talcum, mannitol, SLS and starch. The prepared tablets were then subjected to various evaluation parameters. Results every one of the outcomes was observed to be inside satisfactory reaches. The formulation F6 manufacturing utilizing SSG 50mg and SLS 10mg showed the higher medication content (98%), while the formulation F2 showed the least medication content (92%). It was seen that with the increment in SSG concentration, the medication content was additionally increased. SEM concentrate on showed request of expanding unpleasantness of tablet surface is F1<F2<F3<F4<F5<F6. The expanding unpleasantness may be answerable for higher % of medication release. Formulation F1 showed the most elevated medication discharge (97.735%), while the formulation F5 showed the least medication discharge (56.24%). Finally, it was inferred that SSG, SLS, D-mannitol, starch, lactose, and talcum powder can be effectively utilized in the formulation of Oseltamivir phosphate mouth dissolving tablets. Conclusion: From the above work it was presumed that the formulation of the Oseltamivir Phosphate was observed to be more achievable than the regular one.


Author(s):  
Sanket Jain ◽  
Sujit Pillai ◽  
Rampal Singh Mandloi ◽  
Nikhlesh Birla

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.


2018 ◽  
Vol 4 (1) ◽  
pp. 86-102 ◽  
Author(s):  
A. Acharya ◽  
G.B.K. Kumar ◽  
P. Goudanavar ◽  
K. Dhakal

Background: Recent developments in fast dissolving tablets have brought convenience in dosing to pediatric and elderly patients who have trouble in swallowing tablets.The main objective of the present study is to formulate fast dissolving tablet of Lornoxicam by direct compression method.Methods: Guar gum and crospovidone were used as natural and synthetic superdisintegrants respectively. Fast dissolving tablet of Lornoxicam were prepared by direct compression technique using three different approaches; superdisintegrant addition, sublimation, and solid dispersion.Results: IR and DSC studies showed no interaction between the drug and the excipients. All formulation showed disintegration time ranging from 16.09-42.54 second. Wetting time and disintegration time decreased by increasing the super disintegrant concentration from 2.5% to 5% w/w. Formulae L16 gave the best in- vitro disintegration and dissolution results, which would be due to swelling effect of Gaur gum and amorphization of the drug during the solid dispersion preparation.The best formulation L16 was subjected to stability testing for 3 month and results showed no significant change in appearance, hardness, drug content and dissolution profile of the tablets, hence tablet is stable throughout its stability studies.Conclusion: It was concluded that fast dissolving tablets of Lornoxicam were formulated successfully with desired characteristics which disintegrated rapidly; provided rapid onset of action; and enhanced the patient convenience and compliance.JMMIHS,2018;4(1):86-102


2019 ◽  
Vol 11 (1) ◽  
pp. 117
Author(s):  
Rasha Khalid Al-dhahir ◽  
Myasar Al-kotaji

Objective: The aim of this work was to formulate and evaluate orally disintegrating tablets of cinnarizine that were prepared by direct compression method using different types of diluents and super disintegrants. The rationale behind this work was to accelerate the disintegration of the tablet to provide rapid dissolution, quick action and enhanced bioavailability of the drug.Methods: The tablets were prepared by direct compression method using different types of diluents as mannitol, microcrystalline cellulose (MCC), and lactose. Different super disintegrants were used such as crospovidone (CP), sodium starch glycolate (SSG) and Kyron T-314; Kyron T-314 was used in different concentrations of 5%, 6%, 7%, and 8%. The prepared formulae (F1-F9c) were subjected to flowability studies and post-compression evaluation studies. The optimized formula was selected depending on the time of disintegration and dissolution; then it was subjected to drug-excipient compatibility study and stability study.Results: Flowability results were ranging from excellent, excellent to good, and good to fair according to the type of the diluent used. All of the prepared tablets showed acceptable hardness, friability, drug content, and disintegration. A rapid disintegration of 11.66±2.25 s with the highest percentage 2 min-drug release of 74.55±3.01% was obtained by using the diluent lactose and the super disintegrant Kyron T-314 (8%) in the formula F9c. The infrared spectroscopic studies of the formula F9c showed no drug-excipient interaction. In addition, the stability study indicated that the optimized formula is a stable formula.Conclusion: Formula F9c of a rapidly disintegrating tablet was easy to be manufactured, and the results showed that this formula had a rapid disintegration, high dissolution profile, no noticeable chemical incompatibility and it was stable upon storage.


Sign in / Sign up

Export Citation Format

Share Document