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

Author(s):  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA ◽  
B. KUSUMA LATHA

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.

Author(s):  
A. HARI OM PRAKASH RAO ◽  
SANTOSH KUMAR RADA ◽  
SHAMBHAVI KANDUKURI

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.


2020 ◽  
Vol 13 (1) ◽  
pp. 52-65
Author(s):  
A. Bharathi ◽  
K.Vijaya Sree ◽  
D.Chandra Sekhar Naik

To evaluate fast dissolving tablets for Roflumilast employing with novel superdisintegrant using lepidium sativum mucilage by using 23 factorial design.The physical, chemical and micromeritic studies were evaluated for the prepared mucilage. To estabish fast dissolving tablets of Roflumilast with lepidium sativum mucilage ie a superdisinitegrant in different ratios by using direct compression method employing 23 factorial design. All the fast dissolving tablets were evaluated pre compression and post compression parameters like dissolution efficiency (DE%) percent of drug dissolved at 5 min (PD5). The Lepidium sativum mucilage was to be found fine,free flowing crystaline powder and excellent swelling nature in water. The FTIR and DSC studies were indicated to no interactions between roflumilast and Lepidium sativum mucilage. All the formulation batches shows good quality with regrad to drug content (98±0.092 to 100±0.026)hardness(3.4±0.43 to 3.6±0.64)friability (0.21±0.04 to 0.88±0.42). The optimized formulation batch shows less disintegrant time (52±0.24). The In– Vitro wetting time was less (i.e., 90s) in optimized formulation F2. The water absorption ratio of the formulated tablets was found to be in the range of (90.3±0.027 ). The cumulative drug dissolved in the optimized formulation F2 was found to be ( 99%) in 5 min. Lepidium sativum mucilage was found to be a super disintegrant which enhanced the dissolution efficiency when combined with Crospovidone, croscarmellose sodium, and hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.


Author(s):  
ANTHOSH KUMAR RADA ◽  
RAMYA M ◽  
SHAMBHAVI KANDUKURI

Objective: The main aim is to design, optimize, and evaluate ibuprofen fast-dissolving tablets by employing starch valerate-A novel super disintegrant. Methods: The fast-dissolving tablet of ibuprofen was prepared by employing starch valerate as super disintegrant in different proportions in each case by direct compression method using 23 factorial design, sodium starch glycolate, and crospovidone used as super disintegrants. In the 23 factorial design, these super disintegrants were applied to investigate the interaction effects of three variables, that is, (a) starch valerate, (b) sodium starch glycolate, and (c) crospovidone. The drug content, hardness, friability, disintegration time, and other dissolution characteristics were determined. Results: The starch valerate prepared was found to be fine, free-flowing, slightly crystalline powder. Starch xanthate exhibited good swelling in water with 125.2%. All the fast-dissolving tablets formulated employing starch valerate were of good quality with regard to drug content (100±5%), hardness (3.6–3.8 kg/sq. cm), and friability (0.11-0.12%). The disintegration time of all the formulated tablets was found to be in the range of 12±0.02 to 30±0.02s. The optimized formulation FL8 has the least disintegration time, that is, 12±0. 02s. The in vitro wetting time of the formulated tablets was found to be in the range of 21±0.09 to 44±0.10s. The in-vitro wetting time was less (i.e., 90s) in optimized formulation FL8. The water absorption ratio of the formulated tablets was found to be in the range of 30±0.12 to 100±0.09%. Conclusion: Starch valerate was found to be a super disintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, crospovidone, with the ibuprofen.


Author(s):  
A. HARI OM PRAKASH RAO ◽  
R. SANTOSH KUMAR ◽  
SHAMBHAVI KANDUKURI ◽  
M. RAMYA

Objective: To synthesize, characterize and evaluate starch glycolate as a superdisintegrant in the formulation of Glipizide fast dissolving tablets by employing 23 factorial designs. Methods: Starch glycolate was prepared and its physical and micromeritic properties were performed to evaluate it. The fast dissolving tablet of Glipizide was prepared by employing starch crotonate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design for the evaluation of tablet parameters like disintegration and dissolution efficiency in 5 min. Results: The starch glycolate prepared was found to be fine, free-flowing and amorphous. Starch glycolate exhibited good swelling in water with a swelling index (10%). The study of starch glycolate was shown by fourier transform infrared spectra (FTIR). The drug content (100±5%), hardness (3.5–4 kg/sq. cm), and friability (<0.15%) was been effective with regard to all the formulated fast dissolving tablets employing starch glycolate. The disintegration time of all the formulated tablets was found to be in the range of 13±0.015 to 180±0.014 sec. The optimized formulation F8 had the least disintegration time i.e., 13±0.015 sec. The wetting time of the tablets was found to be in the range of 8±0.015 to 95±0.013 sec. The In vitro wetting time was less (i.e., 8±0.015s) in optimized formulation F8. The water absorption ratio of the formulated tablets was found to be in the range of 75±0.012 to 150±0.014%. The percent drug dissolved in the optimized formulation F8 was found to be 99.95% in 5 min. Conclusion: Starch glycolate was an efficient superdisintegrant for fast-dissolving tablets. The disintegration and dissolution efficiency of the fast dissolving tablets of glipizide was good and depended on the concentration of superdisintegrant employed i.e., starch glycolate, sodium starch glycolate, crospovidone. The formulated fast dissolving tablets of glipizide exhibited good dissolution efficiency in 5 min which can be used for the fast therapeutic action of glipizide.


Author(s):  
CHANDRA SEKHAR NAIK D ◽  
BHARATHI A ◽  
BASAVESWARA RAO MV

Objective: The objective of the study was to evaluate Ocimum gratissimum mucilage as a novel superdisintegrant in the formulation of fast-dissolving tablets (FDT) of Biopharmaceutical Classification System-II drug (Ibuprofen) employing a 23 factorial design. Methods: O. gratissimum mucilage was extracted by seeds and it was subjected to physical, chemical, and micrometric studies were evaluated. To establish FDT of ibuprofen with O. gratissimum mucilage as a superdisintegrants in different ratios using direct compression method employing 23 factorial design. All the formulation tablets were evaluated pre-compression and post-compression parameters like dissolution efficiency (DE%) percent of drug dissolved at 5 min. Results: The mucilage was to be found fine, free-flowing crystalline powder, and excellent swelling nature in all suitable solvents and buffers. The Fourier transform infrared and differential scanning calorimetry studies were indicated to no interactions between ibuprofen and O. gratissimum mucilage. All the FDT formulated employing novel mucilage shows good quality with regard drug content (98.05±0.31–99.39±0.54), hardness (3.6– 4 kg/sq. cm), and friability (0.12–0.15%). The optimized formulation batch shows less disintegrant time (30±0.06). In vitro wetting time was less (i.e., 90 s) in optimized formulation F2. The water absorption ratio of the formulated tablets was found to be in the range of 99±0.56. The cumulative drug dissolved in the optimized formulation F2 was found to be 99% in 10 min. Conclusion: O. gratissimum mucilage was found to be a novel superdisintegrant which enhanced the DE when combined with crospovidone and croscarmellose sodium; hence, it could be used in the formulation of FDT to provide immediate release of the contained drug within 5 min.


Author(s):  
Santosh Kumar Rada ◽  
ANKITA GHOSH

Objective: To enhance the solubility of poorly soluble drugs by evaluating starch tartrate as a superdisintegrant in the formulation of fast dissolving tablets by employing 23 factorial design. Methods: Starch tartrate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch tartrate. The fast dissolving tablets of piroxicam were prepared by using starch tartrate as a superdisintegrant in different proportions by direct compression technique using 23 factorial design. The 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) were used in the evaluation of prepared fast dissolving tablets. Results: The superdisintegrant starch tartrate prepared was found to be fine, free-flowing slightly crystalline powder. Starch tartrate exhibited good swelling in water. The study between piroxicam and starch tartrate was shown the absence of interaction by fourier transform infrared spectra (FTIR) and differential scanning calorimetry (DSC). The drug content (99.83±0.56 %), hardness (3.7–3.9 kg/sq. Cm), and friability (0.12-0.15%) have been effective with regard to all the formulated fast dissolving tablets employing starch tartrate. The disintegration time of all the formulated fast dissolving tablets (FDTs) was found to be in the range of 12±0. 01 to 4500±0.02s. The optimized formulation F6 has the least disintegration time i.e., 12±0. 01s. The In vitro wetting time of the formulated tablets was found to be in the range of 35±0.09 to 1624±0.02s. The In–Vitro wetting time was less (i.e., 90s) in optimized formulation F6. The water absorption ratio of the formulated tablets was found to be in the range of 60±0.12 to 65±0.15%. The cumulative drug dissolved in the optimized formulation F6 was found to be 99.32±0.09% in 10 min. Conclusion: The dissolution efficiency of piroxicam was enhanced when starch tartrate was found to be a superdisintegrant when combined with crospovidone and, hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 10 min.


2017 ◽  
Vol 9 (5) ◽  
pp. 51
Author(s):  
R. Santosh Kumar ◽  
T. Naga Satya Yagnesh ◽  
V. Goutham Kumar

Objective: To evaluate starch xanthate as a super disintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23 factorial design.Methods: Starch xanthate was synthesized by gelatinization process. The synthesized starch xanthate was subjected to physical and micromeritic evaluation. To establish as starch xanthate as a super disintegrant, fast dissolving tablet of ibuprofen was prepared employing starch xanthate 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).Results: The starch xanthate prepared was found to be fine, free flowing slightly crystalline powder. Starch xanthate 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 xanthate. All the fast dissolving tablets formulated employing starch xanthate 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 disintegration time of all the formulated tablets was found to be in the range of 13±0. 02 to 108±0.02s. The optimised formulation FL7 has the least disintegration time i.e., 13±0. 02s. The In vitro wetting time of the formulated tablets was found to be in the range of 90±0.15 to 369±0.17s. The In–Vitro wetting time was less (i.e., 90s) in optimized formulation FL7. The water absorption ratio of the formulated tablets was found to be in the range of 94±0.16 to 192±0.15%. The cumulative drug dissolved in the optimized formulation FL7 was found to be 99.63±0.24% in 5 min.Conclusion: Starch xanthate was found to be a super disintegrant which enhanced the dissolution efficiency when combined with sodium starch glycolate, croscarmellose sodium, with the ibuprofen and hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.


2018 ◽  
Vol 10 (6) ◽  
pp. 249
Author(s):  
Santosh Kumar Rada ◽  
T. Naga

Objective: To synthesize, characterize and evaluate starch xanthate as a superdisintegrant in the formulation of fast dissolving tablets by employing 23 factorial design.Methods: Starch xanthate was synthesized by gelatinization process. The physical and micromeritic properties were performed to evaluate the synthesized starch xanthate. The fast dissolving tablet of ibuprofen was prepared by employing starch xanthate as a superdisintegrant in different proportions in each case by direct compression method using 23 factorial design. The 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) were used in the evaluation of prepared fast dissolving tablets.Results: The starch xanthate prepared was found to be fine, free flowing slightly crystalline powder. Starch xanthate exhibited good swelling in water. The study between ibuprofen and starch xanthate was shown the absence of interaction by fourier transform infrared spectra (FTIR) and differential scanning calorimetry (DSC). The drug content (100±5%), hardness (3.6–4 kg/sq. cm), and friability (0.12-0.15%) has been effective with regard to all the formulated fast dissolving tablets employing starch xanthate. The disintegration time of all the formulated tablets was found to be in the range of 12±0.01 to 312±0.02s. The optimized formulation F5 has the least disintegration time i.e., 12±0.01s. The In vitro wetting time of the formulated 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., 90s) in optimized formulation F5. The water absorption ratio of the formulated tablets was found to be in the range of 16±0.16 to 174±0.21%. The cumulative drug dissolved in the optimized formulation F5 was found to be 99.83±0.56% in 5 min.Conclusion: The dissolution efficiency of ibuprofen was enhanced when starch xanthate was found to be a superdisintegrant when combined with sodium starch glycolate, croscarmellose sodium and, hence it could be used in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 5 min.


2019 ◽  
Vol 9 (1-s) ◽  
pp. 185-195
Author(s):  
SANTOSH KUMAR RADA ◽  
T. Naga Satya Yagnesh

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.


2019 ◽  
Vol 9 (2) ◽  
pp. 222-230
Author(s):  
Rada Santosh Kumar ◽  
T. Naga Satya Yagnesh

The present study involves in the evaluation of starch xanthate as a superdintegrant in the formulation of fast dissolving tablets of poorly soluble drugs employing 23factorial design. By using gelatinization process starch xanthate was synthesized. Then the synthesized starch xanthate was evaluated under physical and micromeritic methods. To develop starch xanthate as a superdisintegrant, fast dissolving tablet of aceclofenac was prepared by direct compression method employing starch xanthate in different proportions in each case employing 23 factorial design. All the prepared fast dissolving tablets were evaluated for drug content, hardness, friability, disintegration time and other dissolution characteristics like PD10, DE5 and K1. The prepared starch xanthate was found to be fine, free flowing slightly crystalline powder. Starch xanthate shown good swelling in water. The swelling index was 50% and all micrometric properties shown good flow and compressibility needed for solid dosage from manufacturing. All the formulated fast dissolving tablets employing starch xanthate were of good quality with regard to drug content, hardness and friability and fulfilled the official (IP/USP) requirements of compressed tablets with regard to the above mentioned physical properties. Starch xanthate was found to be a superdisintegrant which enhanced the dissolution efficiency when combined with croscarmellose sodium, with the aceclofenac and hence it could be utilized in the formulation of fast dissolving tablets to provide immediate release of the contained drug within 10 minutes. Keywords: Fast Dissolving, Superdisintegrant, Starch xanthate, Dissolution efficiency


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