scholarly journals Formulation and Evaluation of Effects of Superdisintegrants on Immediate Release Tablet of Linagliptin, a DDP-4 Inhibitor

2021 ◽  
Vol 24 (2) ◽  
pp. 168-179
Author(s):  
Tanoy Saha ◽  
Md Mahbubul Alam ◽  
Dilshad Noor Lira ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
Dosage Forms ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Disintegration Time ◽  
Weight Variation ◽  
Tablet Dosage ◽  
Release Tablet

The study aimed to develop and evaluate an immediate-release tablet dosage form of Linagliptin. Different concentrations (ranges 5-10%) of super-disintegrants, Croscarmellose sodium (CCS), and Sodium starch glycolate (SSG) were used to prepare nine tablet dosage forms (F1 to F9) through the direct compression method. The compatibility of the formulations was evaluated by FTIR to reveal any possible drug-excipient interactions and it was proved to be compatible with all formulations. Precompression (bulk density, tapped density, Carr’s index, Hausner’s ratio, and angle of repose) and post-compression parameters (weight variation, hardness, thickness, and friability) were analyzed for all tablets and the results were found satisfactory as well as within limits as per USP guidelines. All the formulated batches (F1 to F9) exhibited disintegration of tablets within 2 minutes, where formulation F9 represented the lowest disintegration time (51±3 sec) which was also found significantly better than the marketed product (310±5 sec). In terms of drug dissolution, 90% of drug release was observed for all nine formulations within 45 minutes and formulation F9 (5% CCS and 5% SSG) illustrated the rapid and highest dissolution rate compared to the marketed one’s, 100% drug release at 20 minutes and 91.77 % drug release at 30 minutes successively. The respective data sets of drug release were mathematically fitted to several kinetic models and for all formulations, drug release pattern obeyed first-order kinetics amongst those, formulation F2 (r2= 0.98), F4 (r2= 0.99), F5 (r2= 0.98), and F9 (r2= 0.97) were found to be best fitted in this kinetic norm. Based on disintegration time and dissolution data comparison to a brand leader market product, F9 was experienced as the best formulation. Furthermore, it was observed that if SSG and CCS were combined, then these two parameters were more improved compared to their separate uses. Thus, incorporation of the optimum amount of super-disintegrants in a formulation showed rapid swelling, faster disintegration as well as ease of dissolution of tablet dosage forms. Bangladesh Pharmaceutical Journal 24(2): 168-179, 2021

scholarly journals Fexofenadine HCl Immediate Release Tablets: In vitro Characterization and Evaluation of Excipients

2013 ◽  
Vol 16 (1) ◽  
pp. 1-9
Author(s):  
Shahriar Ahmed ◽  
Mehrina Nazmi ◽  
Ikramul Hasan ◽  
Sabiha Sultana ◽  
Shimul Haldar ◽  
...  
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
In Vitro Characterization ◽  
Weight Variation ◽  
Fexofenadine Hcl

Fexofenadine HCl immediate release tablets were designed to increase the dissolution rate by using superdisintegrants. Different formulations of Fexofenadine HCl were prepared by direct compression method. These formulations were evaluated for hardness, thickness, friability, weight variation, disintegration time, and in vitro dissolution study. The drug release from the formulations were studied according to USP specification (USP paddle method at 50 rpm for 60 minutes) maintaining the temperature to 37°C. Sodium starch glycolate, cross carmellose sodium, crospovidone (kollidon CL), ludiflash and xanthan gum were used in 3%, 6% and 8% concentrations as superdisintegrants. Thus, the ratio of superdisintegrants was changed whereas all the other excipients as well as the active drug (Fexofenadine HCl) remained same in every formulation. Here, 0.001N HCl was used as dissolution medium according to USP and absorbances were determined by using UV spectrophotometer at 217 nm. The F-3 and F-6 formulation prepared by 8% of Sodium starch glycolate and 8% of Cross carmellose sodium showed 99.99% drug release within 30 minutes and 45 minutes, respectively. The disintegration times of F-3 and F-6 formulation were within 9 seconds. The interactions between drug and excipients were characterized by FTIR spectroscopic study. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14483 Bangladesh Pharmaceutical Journal 16(1): 1-9, 2013

scholarly journals FORMULATION AND EVALUATION OF FLURBIPROFEN FAST DISINTEGRATING TABLETS USING NATURAL SUPERDISINTEGRANTS

2016 ◽  
Vol 9 (6) ◽  
pp. 247 ◽  
Author(s):  
Mohammed Sarfaraz ◽  
Surendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Lepidium Sativum ◽  
Disintegration Time ◽  
Natural Sources ◽  
Weight Variation ◽  
Wetting Time ◽  
Tapped Density ◽  
Fast Disintegrating Tablets

ABSTRACTObjective: The main objective of this research was to formulate Fast disintegrating tablets of Flurbiprofen incorporating superdisintegrants, isolated from natural sources like Plantago ovata (PO) seeds, Lepidium sativum (LS) seeds and agar-agar.Methods: Superdisintegrants were isolated from their natural sources using reported methods. Swelling index and hydration capacity was determined for the natural superdisintegrants to know their disintegration capacity. The tablet formulations were designed using isolated natural superdisintegrants. The powder blends were evaluated for pre-compressional parameters like angle of repose, bulk density, tapped density, carr’s index, and hausner’s ratio. Fast disintegrating tablets were prepared by direct compression method. The compressed tablets were characterized for post compression parameters.Results: All formulations had hardness, friability, weight variation and drug content within the pharmacopoeial limits. The wetting time was 84 to 254 sec, in vitro disintegration time was between 59.2 to 221 sec, and in-vitro drug release was as low as 11.80% (LS1) to a maximum of 98.99% (PO4) after 4 min of study. Among all, optimized formulation was PO4, as it showed good wetting time (84 sec), fastest disintegration time (59.2 sec), dispersion time (135 sec) and drug release of 98.99.% within 4 min.Conclusion: Flurbiprofen FDT’s were successfully developed using isolated natural disintegrants. The natural disintegrants isolated showed promising results and can prove as effective alternative for synthetic disintegrants.

scholarly journals DEVELOPMENT, FORMULATION AND EVALUATION OF MECLOFENAMATE FAST DISSOLVING TABLETS

2021 ◽  
Vol 10 (1) ◽  
pp. 59-67
Author(s):  
Mahipal Shakkarwal ◽  
Dr. Mukesh Sharma ◽  
Dr. Ram Garg ◽  
Shankar Lal Soni ◽  
Gopal Kumar Paswan ◽  
...  
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation ◽  
Suitable Treatment ◽  
The Stability

The demands for fast dissolving tablets have received ever increasing day by day during the last 10-15 years for the onset of action. In the present study, the effect of superdisintegrant was compared with synthetic super disintegrants and other conventional super disintegrants in the of fast dissolving tablet formulation of Meclofenamate. Meclofenamate is an antihypertensive drug and in case of hypertension immediate treatment is required so the proposed investigation is totally based to provide the suitable treatment for hypertension. In the present work 9 formulations of Fast dissolving tablets of Cilnidipine were prepared by using Synthesized Co-proceed was evaluated and compiles with the official standards, parameters and specifications. Various formulations were prepared using four different superdisintegrant namely- kyron T-304, sodium starch glycolate, cross carmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose , bulk density , tapped density , and then tablet  evaluated post-compression parameters like thickness , drug content , hardness , weight variation  , wetting time , friability , disintegration time , dissolution time, drug release study. Formulation A8 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation A8 showed 98.64% drug release at the end of 3 minutes. The best formulations were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline and standards.

scholarly journals Formulation, Evaluation and Optimization of Orodispersible Tablets of Naproxen sodium by using Superdisintegrant

2019 ◽  
Vol 9 (4-s) ◽  
pp. 462-468
Author(s):  
Mohd. Razi Ansari ◽  
Sumer Singh ◽  
M.A. Quazi ◽  
Yaasir Ahmed Ansari ◽  
Jameel Abbas
Keyword(s):  
Patient Compliance ◽  
Naproxen Sodium ◽  
Rapid Onset ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation

Among the different type of route of administration oral route for drug administration is most common route in which Orodispersible tablet is preferred for the patient which are unconscious, week or for immediate control. The tablet gets dispersed in mouth cavity without water, present study deals with formulation of Naproxen sodium mouth dissolving tablets using super disintegrants. Naproxen sodium is analgesic and NSAID, used for the treatment of pain and inflammation caused by different condition such as osteoarthritis, rheumatoid arthritis and menstrual cramps. However gastric discomfort caused by naproxen sodium result in poor patient compliance associated with it conventional doses form but now days Naproxen sodium MDTs produces rapid onset of action and minimise gastric discomfort associated with it. Thus improves patient compliance, enhance bioavailability and reduces the dose of drug. MDTs are formulated by direct compression method using super disintegrants in different proportion. The powder blend is subjected to pre-compression evaluation parameters like bulk density, true density, and tapped density and angle of repose. Formulations are evaluated for weight variation, hardness, wetting time, water absorption time, disintegration time. And in vitro dissolution studies and all formulations complies Pharmacopoeias standards. The tablets are evaluated and result compared for all five formulation the most efficacious super disintegrants for MTDs of Naproxen sodium as suggested by the dispersion time, disintegration time and drug dissolution profiles. Keywords: - MDT, Naproxen Sodium, crosscarmellose Sodium, Sodium starch glycolate, Cross-povidone.

scholarly journals Use of hydrophilic and hydrophobic polymers for the development of controlled release tizanidine matrix tablets

2014 ◽  
Vol 50 (4) ◽  
pp. 799-818 ◽  
Author(s):  
Tariq Ali ◽  
Muhammad Harris Shoaib ◽  
Rabia Ismail Yousuf ◽  
Sabahat Jabeen ◽  
Iyad Naeem Muhammad ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Weight Variation ◽  
Vitro Release

The aim of the present study was to develop tizanidine controlled release matrix. Formulations were designed using central composite method with the help of design expert version 7.0 software. Avicel pH 101 in the range of 14-50% was used as a filler, while HPMC K4M and K100M in the range of 25-55%, Ethylcellulose 10 ST and 10FP in the range of 15 - 45% and Kollidon SR in the range of 25-60% were used as controlled release agents in designing different formulations. Various physical parameters including powder flow for blends and weight variation, thickness, hardness, friability, disintegration time and in-vitro release were tested for tablets. Assay of tablets were also performed as specified in USP 35 NF 32. Physical parameters of both powder blend and compressed tablets such as compressibility index, angle of repose, weight variation, thickness, hardness, friability, disintegration time and assay were evaluated and found to be satisfactory for formulations K4M2, K4M3, K4M9, K100M2, K100M3, K100M9, E10FP2, E10FP9, KSR2, KSR3 & KSR9. In vitro dissolution study was conducted in 900 ml of 0.1N HCl, phosphate buffer pH 4.5 and 6.8 medium using USP Apparatus II. In vitro release profiles indicated that formulations prepared with Ethocel 10 standard were unable to control the release of drug while formulations K4M2, K100M9, E10FP2 & KSR2 having polymer content ranging from 40-55% showed a controlled drug release pattern in the above mentioned medium. Zero-order drug release kinetics was observed for formulations K4M2, K100M9, E10FP2 & KSR2. Similarity test (f2) results for K4M2, E10FP2 & KSR2 were found to be comparable with reference formulation K100M9. Response Surface plots were also prepared for evaluating the effect of independent variable on the responses. Stability study was performed as per ICH guidelines and the calculated shelf life was 24-30 months for formulation K4M2, K100M9 and E10FP2.

scholarly journals Formulation and Optimization of Orodispersible Tablet of Loratadine Using Box Behnken Design

2019 ◽  
Vol 9 (4-A) ◽  
pp. 86-94
Author(s):  
Aliasgar Kundawala ◽  
Pratik Patel ◽  
Khushbu Chauhan ◽  
Anjali Desai ◽  
Dhwani Kapadia
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Taste Masking ◽  
Disintegration Time ◽  
Box Behnken Design ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Wetting Time

In present study Orodispersible tablets (ORDT) of Loratadine were prepared and optimized. Solid dispersion of Loratadine- β cyclodextrin complex were prepared and used in preparation of Orodispersible tablets. Various super-disintegrating agent like Cross carmellose sodium, Cross povidone and Kyron T-314 were employed for faster disintegrating effect. The 24 factorial and Box-Behnken design were utilized to optimize the tablet formulation. The Orodispersible tablet of Loratadine was optimized by Box Behnken Design, where concentrations Kyron T-314, CRP and Pearlitol SD200 were employed and its effect on Disintegration time (DT), Wetting time (WT) and % drug release at 20 min (Q20) was evaluated. Precompression parameters like angle of repose, bulk density, % compressibility, Hausner’s ratio was studies. The different batches of Orodispersable tablets were prepared and evaluated for disintegration time, friability, wetting time and drug release studies. Different batches prepared showed disintegration time in the range of 23 ± 2.52 to 59 ± 2.64, wetting time in between 27± 0.57 to 66.3 ± 3.4, drug release (Q 20) in between 86.1 ± 0.6 to 96.7 ± 0.4 in 20 min., friability less than 1 % and hardness 3.4 to 4.2 Kg/cm2. The optimized formula when compared with marketed product it showed faster disintegration time and rapid drug dissolution in phosphate buffer 6.8. The solid dispersion of Loratadine not only helped improve in solubility but may also help in taste masking. Keywords: Orodispersible tablets, Loratadine, β cyclodextrin Solid dispersion

scholarly journals Production of Itraconazole Nanocrystal-Based Polymeric Film Formulations for Immediate Drug Release

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 960
Author(s):  
Anna Karagianni ◽  
Leena Peltonen
Keyword(s):  
Drug Release ◽  
Physicochemical Characterization ◽  
Methyl Cellulose ◽  
Immediate Release ◽  
Polymeric Film ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Weight Variation ◽  
Film Forming

In order to improve the solubility properties of BCS class II drug itraconazole, fast dissolving oral polymeric film formulations based on itraconazole nanocrystals were produced. Drug nanocrystals were manufactured by the wet pearl milling technique. In polymeric film formulations, hydroxypropyl methyl cellulose (HPMC) was used as a film forming polymer, and glycerin was used as a plasticizer. For nanocrystal suspensions and film formulations, thorough physicochemical characterization was performed, including particle sizing and size deviation, film appearance, weight variation, thickness, folding endurance, drug content uniformity, disintegration time, and dissolution profile. After milling, the nanoparticles were 369 nm in size with a PI value of 0.20. Nanoparticles were stable and after redispersion from film formulations, the particle size remained almost the same (330 nm and PI 0.16). The produced films were flexible, homogeneous, fast disintegrating, and drug release rate from both the nanosuspension and film formulations showed immediate release behavior. Based on the study, the film casting method for production of itraconazole nanocrystal based immediate release formulations is a good option for improved solubility.

scholarly journals PREPARATION AND CHARACTERIZATION OF CHITOSAN SUCCINATE AS COATING POLYMER FOR ENTERIC-COATED TABLET

2018 ◽  
Vol 10 (1) ◽  
pp. 343
Author(s):  
Silvia Surini ◽  
Koko Prakoso
Keyword(s):  
Drug Release ◽  
Dosage Forms ◽  
Disintegration Time ◽  
Coating Agent ◽  
Water Solvent ◽  
Enteric Coated Tablet ◽  
Coated Tablet ◽  
Enteric Coated ◽  
Tablet Dosage

Objective: This present study was aimed to evaluate the potential of chitosan succinate as a coating polymer.Methods: In this study, chemical modification of chitosan was performed by substituting a succinate group into chitosan’s amine group. This reactionused a water-solvent method to obtain chitosan succinate. Chitosan succinate was characterized and used as a coating agent in enteric-coated tabletdosage forms containing sodium diclofenac as the drug model at concentrations of 3% and 4% and combined it with hydroxypropyl methylcellulosephthalate (HPMCP) in ratios of 3:1 and 2:1 (3%). The obtained tablets were evaluated based on their physical appearance, uniformity of weight andsize, thickness film, disintegration time for an hour in acid, and dissolution profile.Results: Although the enteric-coated tablets with 3% and 4% chitosan succinate dissolved after 1 h in acid, they could not hold drug release in theacid medium under 10%. The enteric-coated tablet combined with chitosan succinate and HPMCP (3:1 and 2:1) at 3% did not dissolve after 1 h in theacid medium and could hold drug release up to 8.53% in acid.Conclusion: A combination of chitosan succinate and HPMCP (3:1 and 2:1) at 3% has a better ability to hold drug release in acid medium and met therequirement as a coating in enteric-coated tablet dosage forms.

scholarly journals Preparation and Evaluation of Natural Gum-Based Immediate Release Metformin Hydrochloride Tablet

2018 ◽  
Vol 21 (2) ◽  
pp. 101-108
Author(s):  
Sreebash Chandra Bhowmik ◽  
Marzia Alam ◽  
Md Saiful Islam Pathan
Keyword(s):  
Immediate Release ◽  
Angle Of Repose ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Class Iii ◽  
Aegle Marmelos ◽  
Disintegration Time ◽  
Weight Variation ◽  
Natural Gum

Metformin hydrochloride is a first line BCS class III oral anti-diabetic drug used for the treatment of type 2 diabetes. The main goal of this study was to formulate, prepare and evaluate natural gum-based immediate release metformin hydrochloride tablet. Seven different formulations of compressed tablets were prepared following wet granulation process using different concentrations (10, 20, 30, 50, 60, 70, 80 and 90 mg) of Aegle marmelos gum as a binder. Aegle marmelos gum is a biodegradable natural gum which is economic, easily available and found useful as tablet binder for both conventional and novel dosage forms. Other excipients used in the formulation were microcrystalline cellulose (MCC), croscarmellose sodium (CCS), maize starch, colloidal silicon dioxide (CSD), sodium starch glycolate (SSG), magnesium stearate etc. In the present study, the compressed tablets were evaluated for weight variation, thickness, hardness, friability, disintegration time and dissolution. In vitro drug release study was carried out in phosphate buffer (pH 6.8) at 37 ± 0.5oC with 50 rpm using USP Dissolution Apparatus 2-Paddle method. The flowability of granules for all the batches was optimum which reflected in the bulk density and angle of repose. It can be concluded from this study that combination of Aegle marmelos as a binder with other excipients can be prospectively used in the preparation of metformin hydrochloride immediate release (IR) tablet.Bangladesh Pharmaceutical Journal 21(2): 101-108, 2018

scholarly journals Preparation and Evaluation of Palonosetron Hydrochloride Oral Thin Film

2019 ◽  
Vol 22 (2) ◽  
pp. 228-234 ◽  
Author(s):  
Sreebash Chandra Bhowmik ◽  
Marzia Alam ◽  
Md Saiful Islam Pathan
Keyword(s):  
Thin Film ◽  
Research Work ◽  
Pharmaceutical Journal ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Disintegration Time ◽  
Weight Variation ◽  
Folding Endurance

The purpose of the current study was to develop a fast dissolving polymeric oral thin film containing palonosetron hydrochloride having good mechanical properties, fast disintegration, dissolution and good drug content uniformity. Solvent casting method was used to prepare the films. Compatibility between drugs and excipients were studied using FTIR and HPLC. Nine different formulations of film from F1 to F9 were prepared using different concentration of polymer A at drug-polymer A ratio (1:26), (1:28), (1:30), (1:32), (1:34), (1:36), (1:38), (1:40), (1:42) and at polymer A-plasticizer B of (65:10), (70:10), (75:10), (40:10), (42.5:10), (45:10), (47.5:10), (50:10), (52.5:10), respectively. The in vitro dissolution study was carried out in phosphate buffer (pH 6.8) at 37±0.5oC and 50 rpm using USP XXIV paddle method. Physicochemical evaluations of all the batches were performed including weight variation, thickness, folding endurance, pH, in vitro disintegration and drug release, FTIR and content uniformity test. Maximum and minimum drug dissolution were found in F6 (108.7%) and in F1 (98.5%), respectively. The maximum and minimum disintegration time were in F9 (43.8 sec) and F1 (25 sec), respectively which demonstrated that disintegration of the film was directly proportional to the polymer A and plasticizer B concentration. It is quite evident from the present research work that the film prepared using polymer A-plasticizer B were smooth, mechanically strong and easy to peel out. Among all the batches, formulation F5 showed best results with respect to disintegration (33 sec), drug dissolution (105%), content uniformity (98.51%) and folding endurance (731). Therefore, it can be said that combination of polymer A and plasticizer B can be prospectively used for the preparation of palonosetron hydrochloride oral thin film. Bangladesh Pharmaceutical Journal 22(2): 228-234, 2019

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