scholarly journals Impact of Tablet Shape on Drug Dissolution Rate Through Immediate Released Tablets

2020 ◽  
Vol 10 (4) ◽  
pp. 656-661
Author(s):  
Fatima Molavi ◽  
Hamed Hamishehkar ◽  
Ali Nokhodchi
Keyword(s):  
Dissolution Rate ◽  
Release Kinetics ◽  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Time ◽  
Sufficient Information ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Dissolution Efficiency

Purpose : The aim of this study was to evaluate the influence of the geometric shape on the dissolution rate of the domperidone, a drug model for immediate release dosage form. In this regard, a lack of sufficient information about the effective dissolution rate of the drugs regarding their shapes has made this issue an interesting subject for researchers. Methods: For this purpose, three tablet shapes, namely flat and biconvex both in a round and oblong shapes, with different four sizes were modelled for the preparation of domperidone tablet. In vitro dissolution test was accomplished using a USP dissolution apparatus II. The drug dissolution rate was assessed by calculating various dissolution parameters; e.g., dissolution efficiency (DE), mean dissolution rate (MDR), mean dissolution time (MDT), and difference and similarity factors (f1 and f2 ). Results: Regarding the disintegration time, the larger tablets showed a faster disintegration time. When the size of the tablets was smaller, the amount of released drug was significantly decreased. In addition, #9 tablets with a flat or biconvex geometry had obvious effects on the DE values. Generally, biconvex tablets had higher DE percentage than the flat tablets. Conclusion: Noticeable differences in dissolution parameters by considering the different geometric shapes play an important role in the drug release kinetics which makes a significant effect on quick onset of action in oral administration.

DESIGN AND OPTIMIZATION OF IMMEDIATE RELEASE TABLETS OF HYDROCHLOROTHIAZIDE USING THE DESIGN OF EXPERIMENTS APPROACH

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 27-33
Author(s):  
H Kathpalia ◽  
◽  
K. Jogi
Keyword(s):  
Design Of Experiments ◽  
Design Space ◽  
Corn Starch ◽  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Time ◽  
Drug Candidate ◽  
Disintegration Time ◽  
Time Required

The aim of the present study was to develop and optimize immediate release tablets using hydrochlorothiazide (HCTZ) as a model drug candidate applying Design of Experiments (DoE) approach. Immediate release tablets were prepared using corn starch as a disintegrant and Polysorbate 80 as a solubilizer. Risk assessment was carried out with subsequent application of 22 factorial design in duplicate for evaluating the interactions and effects of the design factors on critical quality attributes. The design space was obtained by applying DOE and multivariate analysis, so as to ensure desired disintegration time (DT) and in vitro drug dissolution. Immediate release tablets were evaluated for hardness, thickness, friability and in vitro drug dissolution. Optimized formulation obtained from the design space exhibits DT of around 38s, while dissolution time, T96% (time required to release 96% of the drug) was about 45 min. The independent variables have a significant effect over the dependent responses, which can be deduced from Contour plots and surface response graphs. The predicted values matched well with the experimental values and the result demonstrated the feasibility of the design model in the development and optimization of HCTZ immediate release tablets.

scholarly journals DESIGN, OPTIMIZATION AND EVALUATION OF ACECLOFENAC FAST DISSOLVING TABLETS EMPLOYING STARCH VALERATE–A NOVEL SUPERDISINTEGRANT

2021 ◽  
pp. 168-176
Author(s):  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA ◽  
B. KUSUMA LATHA
Keyword(s):  
Factorial Design ◽  
Immediate Release ◽  
Compression Method ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Sodium Starch Glycolate ◽  
Wetting Time ◽  
Croscarmellose Sodium ◽  
Dissolution Efficiency

Objective: To synthesize, characterize and evaluate starch valerate as a superdisintegrant in the formulation of aceclofenac fast dissolving tablets by employing 23 factorial design. Methods: Starch valerate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of aceclofenac was prepared by employing starch valerate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min. Results: The starch valerate prepared was found to be fine, amorphous and free flowing. Starch valerate exhibited good swelling in water with swelling index (125.2%). The study of starch valerate was shown by fourier transform infrared spectra (FTIR). The drug content (200±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch valerate. The disintegration time of all the formulated tablets was found to be in the range of 14±0.04 to 25.7±0.02 sec. The optimized formulation F4 had the least disintegration time i.e., 12.8±0.02 sec. The wetting time of the tablets was found to be in the range of 76±0.21 to 217±0.17s. The In vitro wetting time was less (i.e., 28±0.02s) in optimized formulation F4. The water absorption ratio of the formulated tablets was found to be in the range of 46±0.12 to 100±0.27%. The percent drug dissolved in the optimized formulation F8 was found to be 99.93% in 5 min. Conclusion: Starch valerate, when combined with sodium starch glycolate, croscarmellose sodium, with aceclofenac, was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 5 min.

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 Design, optimization and evaluation of aceclofenac fast dissolving tablets employing starch glutarate: A new superdisintegrant

2019 ◽  
Vol 9 (2) ◽  
pp. 259-269
Author(s):  
Rada Santosh Kumar ◽  
T. Naga Satya Yagnesh
Keyword(s):  
Amorphous Powder ◽  
Immediate Release ◽  
Order Rate Constant ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Drug Content ◽  
Poorly Soluble ◽  
Dissolution Efficiency

In solid dosage forms, fast dissolving tablets has proven the best way for ease of administration for the pediatrics and geriatric patients. The current study involves in the evaluation of starch glutarate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. Starch glutarate was synthesized by esterification process. The synthesized starch glutarate was subjected to physical and micromeritic evaluation. To establish as starch glutarate as a superdisintegrant, fast dissolving tablet of aceclofenac was prepared employing starch glutarate in different proportions in each case by direct compression method employing 23 factorial design. All fast dissolving tablets prepared were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), Dissolution efficiency in 5 min (DE5%) and first order rate constant (K1). The starch glutarate prepared was found to be fine, free flowing amorphous powder. Starch glutarate exhibited good swelling in water. Fourier transform infrared spectra (FTIR) and Differential scanning calorimetry (DSC) study indicated the absence of interaction between aceclofenac and starch glutarate. All the fast dissolving tablets formulated employing starch glutarate were of good quality with regard to drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (0.12-0.15%). The optimized formulation F8 has the least disintegration time i.e., 30±0.02s. The in vitro wetting time was less (i.e., 90s) in optimized formulation F8. The cumulative drug dissolved in the optimized formulation F8 was found to be 99.15±0.56% in 15 min. Starch glutarate was found to be a superdisintegrant which enhanced the dissolution efficiency when combined with crospovidone, croscarmellose sodium, with the aceclofenac and hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 15 minutes. Keywords: Fast dissolving, Superdisintegrant, Starch glutarate, Dissolution efficiency.

scholarly journals Design, optimization and evaluation of ibuprofen fast dissolving tablets employing starch succinate: A new superdisintegrant

2019 ◽  
Vol 9 (2) ◽  
pp. 270-279
Author(s):  
Rada Santosh Kumar ◽  
T. Naga Satya Yagnesh
Keyword(s):  
Oral Administration ◽  
Oral Drug Delivery ◽  
Immediate Release ◽  
Order Rate Constant ◽  
Oral Drug ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Drug Content ◽  
Dissolution Efficiency

The current scenario emphasize on oral administration. The main disadvantage in oral administration was difficulty in swallowing for pediatric and geriatric patients. To solve this problem in oral drug delivery system, the formulation of fast dissolving systems found to be the best alternatives.  The present investigation involves in the evaluation of starch succinate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. Starch succinate was synthesized by esterification process. The synthesized starch succinate was subjected to physical and micromeritic evaluation. All fast dissolving tablets were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first order rate constant(K1). The starch succinate prepared was found to be fine, free flowing crystalline powder. Starch succinate exhibited good swelling in water. Fourier transform infrared spectra (FTIR) and Differential scanning calorimetry (DSC) study indicated the absence of interaction between ibuprofen and starch succinate. All the fast dissolving tablets formulated employing starch succinate were of good quality with regard to drug content (200±2%), hardness (3.6–4.0 kg/sq. cm), and friability (0.12-0.15%). The optimised formulation F8 has the least disintegration time i.e., 15±0. 02s. The in–vitro wetting time was less (i.e., 15s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 31.4±0.01 to 68.0±0.04%. The cumulative drug dissolved in the optimized formulation F8 was found to be 99.81± 0.22% in 5 min. Starch succinate was found to be a superdisintegrant which enhanced the dissolution efficiency with the ibuprofen and hence it could be used in the formulation of fast dissolving tablets to bring immediate release of the contained drug within 5 minutes. Keywords: Fast dissolving, Superdisintegrant, Starch succinate, Dissolution efficiency.

scholarly journals FORMULATION AND EVALUATION OF SUMATRIPTAN IMMEDIATE RELEASE TABLETS

2018 ◽  
Vol 8 (5) ◽  
pp. 241-247
Author(s):  
P Munija ◽  
G Srikanth
Keyword(s):  
Performance Testing ◽  
Immediate Release ◽  
Oral Dosage ◽  
Drug Dissolution ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Sumatriptan Succinate ◽  
Orodispersible Tablet ◽  
Drastic Effect ◽  
Mouth Feel

The rationale of this investigation is to design an immediate release oral dosage of Sumatriptan succinate by using microcrystalline cellulose as filler, camphor and menthol as subliming agents by direct compression method .The basic objective of this dissertation is to develop an orodispersible tablet of sumatriptan succinate used in anti-migraine with an aim of reduces the lag time and providing faster onset of action to relief the acute migraine effect immediately. Disintegrates and disperses in oral cavity within 30 seconds without the need of drinking water. Has pleasant mouth feel and there is no after taste or grittiness. Successfully discriminates the ability of three superdisintegrants to promote drug dissolution and proposes a model formulation for disintegrants performance testing and quality control purposes. The formulation F6 containing 8% of CCS and 10% of menthol showed disintegration time of 18seconds after drying. Menthol as subliming agent was found to be most effective of all other subliming agents as it had showed drastic effect on the drug release. Keywords: Sumatriptan succinate, sublimation, menthol, anti-migraine

scholarly journals Design, optimization and evaluation of ibuprofen fast dissolving tablets employing starch tartrate: A new superdisintegrant

2019 ◽  
Vol 9 (2) ◽  
pp. 160-169
Author(s):  
Rada Santosh Kumar ◽  
T. Naga Satya Yagnesh
Keyword(s):  
Immediate Release ◽  
Order Rate Constant ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Drug Content ◽  
Current Scenario ◽  
Poorly Soluble ◽  
Wetting Time ◽  
Dissolution Efficiency

The current scenario deals with the study of fast dissolving tablets for the patients suffering from swallowing, sickness ,etc.  The present investigation involves in the evaluation of starch tartrate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. Starch tartrate was synthesized by esterification process. The synthesized starch tartrate was subjected to physical and micromeritic evaluation. All fast dissolving tablets were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like percent dissolved in 5 min (PD5), dissolution efficiency in 5 min (DE5%) and first order rate constant(K1). The starch tartrate prepared was found to be fine, free flowing slightly crystalline powder. Starch tartrate exhibited good swelling in water.Fourier transform infrared spectra (FTIR) and Differential scanning calorimetry (DSC) study indicated the absence of interaction between ibuprofen and starch tartrate. All the fast dissolving tablets formulated employing starch tartrate were of good quality with regard to drug content (200±5%), hardness (3.6–3.9 kg/sq. cm), and friability (0.12-0.15%). The optimised formulation F2 has the least disintegration time i.e., 9±0. 03s. The in–vitro wetting time was less (i.e., 60s) in optimized formulation F2. The water absorption ratio of the formulated tablets was found to be in the range of 27.53±0.12 to 69.75±0.18%. The cumulative drug dissolved in the optimized formulation F2 was found to be 100.17±0.56% in 5 min. Starch tartrate was found to be a superdisintegrant which enhanced the dissolution efficiency with the ibuprofen and hence it could be used in the formulation of fast dissolving tablets to bring immediate release of the contained drug within 5 minutes. Keywords: Fast dissolving, Superdisintegrant, Starch tartrate, Dissolution efficiency.

scholarly journals OPTIMISATION OF STARCH OXALATE AS A NOVEL SUPERDISINTEGRANT IN FAST DISSOLVING SYSTEMS OF POORLY SOLUBLE DRUGS

2019 ◽  
Vol 9 (1-s) ◽  
pp. 185-195
Author(s):  
SANTOSH KUMAR RADA ◽  
T. Naga Satya Yagnesh
Keyword(s):  
Factorial Design ◽  
Amorphous Powder ◽  
Immediate Release ◽  
Poorly Soluble Drugs ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Drug Content ◽  
Poorly Soluble ◽  
Dissolution Efficiency

Objective: To enhance the solubility of poorly soluble drugs by using 23 factorial design in the formulation of fast dissolving tablets by employing starch oxalate as a superdisintegrant. Methods: Starch oxalate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch oxalate. By using 23 factorial design, atenolol fast dissolving tablet was prepared by employing starch oxalate as a superdisintegrant in different proportions in each case by direct compression method. In the evaluation of fast dissolving tablets the drug content, hardness, friability, disintegration time and other dissolution characteristics were utilized. Results: The starch oxalate prepared was found to be fine, free-flowing completely amorphous powder. The compatibility between atenolol and starch oxalate were studied and showed no interaction. The drug content, hardness, and friability have been effective with regard to all the formulated fast dissolving tablets employing starch oxalate. The optimised formulation F8 has the least disintegration time i.e., 24±0.06s. The In–vitro wetting time was less (i.e., 28s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be more in F8 formulation 94.42±0.18%. The cumulative drug dissolved in the optimized formulation F8 was found to be 98.70±0.24% in 5 min. Conclusion: The dissolution efficiency of atenolol was enhanced when starch oxalate was found to be a superdisintegrant when combined with sodium starch glycolate, crospovidone and, hence to provide immediate release of the formulated fast dissolving tablets contained drug it could be used.

scholarly journals OPTIMIZATION OF STARCH CROTONATE AS A NOVEL SUPERDISINTEGRANT IN THE FORMULATION OF FAST DISSOLVING TABLETS THROUGH 23 FACTORIAL DESIGN

2021 ◽  
pp. 247-256
Author(s):  
A. HARI OM PRAKASH RAO ◽  
SANTOSH KUMAR RADA ◽  
SHAMBHAVI KANDUKURI
Keyword(s):  
Factorial Design ◽  
Immediate Release ◽  
Compression Method ◽  
Disintegration Time ◽  
23 Factorial Design ◽  
Sodium Starch Glycolate ◽  
Wetting Time ◽  
Croscarmellose Sodium ◽  
Dissolution Efficiency

Objective: To synthesize, characterize and evaluate starch crotonate as a superdisintegrant in the formulation of Piroxicam fast dissolving tablets by employing 23 factorial design. Methods: Starch crotonate was synthesized and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of Piroxicam were prepared by employing starch crotonate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design. Results: The starch chrotonate prepared was found to be fine, free flowing and amorphous. Starch crotonate exhibited good swelling in water with swelling index (50%). The study of starch crotonate was shown by fourier transform infrared spectra (FTIR). The drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (<0.15%) have been effective with regard to all the formulated fast dissolving tablets employing starch crotonate. The disintegration time of all the formulated tablets was found to be in the range of 18±03 to 66±03 sec. The optimized formulation F8 had the least disintegration time i.e., 18±03 sec. The wetting time of the tablets was found to be in the range of 49.92±0.11 to 140±0.18s. The In vitro wetting time was less (i.e., 74±0.37s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 27.58±0.01 to 123.07±0.33%. The percent drug dissolved in the optimized formulation F8 was found to be 99.83% in 10 min. Conclusion: Starch crotonate, when combined with sodium starch glycolate, croscarmellose sodium, with Piroxicam was found to be an effective super disintegrant which improved the dissolution efficiency and could therefore be used in the formulation of quick dissolving tablets to provide immediate release of the contained drug within 10 min.

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