scholarly journals SYNTHESIS AND CHARACTERIZATION OF STARCH MALONATE: DEVELOPMENT OF FAST DISSOLVING TABLETS OF ACECLOFENAC BY 23 FACTORIAL DESIGNS

2021 ◽  
pp. 87-102
Author(s):  
ANNU KUMARI ◽  
R. SANTOSH KUMAR
Keyword(s):  
Design Method ◽  
Research Work ◽  
Stability Study ◽  
Drug Dissolution ◽  
Esterification Reaction ◽  
Poorly Soluble Drugs ◽  
Disintegration Time ◽  
Dsc Studies ◽  
23 Factorial Design ◽  
Poorly Soluble

Objective: The aim of the research work is to develop a new superdisintegrant (starch malonate) which can help in enhancing the solubility and drug dissolution of poorly soluble drugs. Hence, starch malonate (new superdisintegrant) was prepared and has been evaluated for its superdisintegrant property by incorporating it into fast dissolving tablets of Aceclofenac. Methods: Superdisintegrant was developed by using esterification reaction. Prepared starch malonate was then subjected for different characterization tests (solubility, pH, melting point, swelling index, FTIR, DSC studies. 23 factorial design method was used to formulate fast dissolving tablets of aceclofenac employing starch malonate. Two known superdisintegrants croscarmellose sodium and crospovidone have been used along with starch malonate in combinations to develop fast dissolving tablets. Prepared tablets were then subjected to different tests for tablets like hardness, friability, disintegration time, dissolution studies. A stability study was performed to determine the stability of the formulation. Design expert study was conducted to know the interaction between different superdisintegrants and to select best optimized formulation in among all formulations. Results: Starch malonate prepared was found to be fine, free flowing slightly crystalline powder, insoluble in aqueous and organic solvents. Tablets of all formulations were of excellent quality concerning drug content (100±5%), hardness (3.8-4.2 kg/cm2), and friability (less than 0.15%). In all formulations, formulation F2 found to be optimized formulation with least disintegration time 38 S, less wetting time 17±0.08 s and enhanced percent dissolved rate in 5 min i.e., 99.84% as compared to other formulations. Conclusion: From this it was concluded that starch malonate can be used as a novel superdisintegrant to enhance the drug dissolution of poorly soluble drugs. Optimized formulation F2 showed enhanced drug dissolution at 5% concentration as compared to other formulation and showed least disintegration time and enhanced drug dissolution as compared to other formulations and pure drug.

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 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.

Fabrication and Evaluation of Mouth Dissolving Strips of Metoclopramide Hydrochloride by Using Novel Film Former

2021 ◽  
pp. 5515-5520
Author(s):  
Hemant A. Deokule ◽  
Smita S. Pimple ◽  
Praveen D. Chaudhari ◽  
Ajit S. Kulkarni
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Systemic Circulation ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Visual Appearance ◽  
Dsc Studies ◽  
Weight Variation ◽  
Metoclopramide Hydrochloride

Fast dissolving strips are used as novel approaches, as it dissolves rapidly in mouth and directly reaches the systemic circulation. In present research work, an attempt has been made to prepare mouth dissolving strips of Metoclopramide hydrochloride by using a novel film former Pullulan by solvent casting method. A33 full factorial design was utilized for the optimization of the effect of independent variables such as the amount of Pullulan, amount of PEF 400, amount of SSG on mechanical properties, and % drug release of strips. The drug compatibility studies using FTIR and DSC studies formulated strips were characterized for their physicochemical parameter like weight variation, visual appearance, folding endurance, thickness, disintegration time, drug content, and in vitro dissolution studies. FTIR and DSC studies revealed that the polymer is compatible with the drug. It was found that the optimum levels of the responses for a fast release strip could be obtained at low levels of Pullulan, PEG400, and SSG. The prepared strip was clear transparent and had a smooth surface. The surface pH was found 4.8 to 5.2 be in the range of to which is close to salivary pH, which indicates that strips may have less potential to irritate the oral mucosa, thereby they are comfortable. The drug release was found to be between 90.94 to 100.5% in 2 min. The in-vitro disintegration time of strips prepared with Pullulan was in the range of 19 to 57 sec. As the concentration of SSG increases the decrease in the disintegration time of strips a decrease. The dissolution rate increased with an increase in the concentration of SSG. Hence, it can be inferred that the fast dissolving oral strips of Metoclopramide hydrochloride may produce rapid action thereby improving bioavailability and enhance the absorption by avoiding the first-pass effect.

scholarly journals Novel application of mixed solvency concept in the development of oral liquisolid system of a poorly soluble drug, cefixime and its evaluation

2018 ◽  
Vol 8 (6-s) ◽  
pp. 5-8 ◽  
Author(s):  
Rinshi Agrawal ◽  
RK Maheshwari
Keyword(s):  
Drug Loading ◽  
Research Work ◽  
Water Soluble ◽  
Dsc Studies ◽  
Water Soluble Drug ◽  
Poorly Soluble ◽  
Poorly Water Soluble ◽  
Poorly Soluble Drug ◽  
Model Drug ◽  
Poorly Water Soluble Drug

Application of mixed solvency has been employed in the present research work to develop a liquisolid system (Powder formulation) of poorly water soluble drug, cefixime (as model drug). Material and Methods: For poorly water soluble drug cefixime, combination of solubilizers such as sodium acetate, sodium caprylate and propylene glycol as mixed solvent systems were used to decrease the overall concentration of solubilizers required to produce substantial increase in solubility and thereby resulting in enhanced drug loading capacity of cefixime. The procured sample of cefixime was characterized by melting point, IR, UV and DSC studies. Stability studies of liquisolid system of cefixime were performed for two months at room temperature, 30˚C and 40˚C. All the formulations were physically, chemically, and microbiologically stable. Conclusion: Mixed solvency concept has been successfully employed for enhancing the drug loading of poorly water soluble drug, cefixime. Keywords: Solubility, cefixime, liquisolid system, mixed solvency concept.

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 FORMULATION AND OPTIMIZATION OF CURCUMIN SOLID DISPERSION PELLETS FOR IMPROVED SOLUBILITY

2019 ◽  
pp. 36-46
Author(s):  
SANJEEVANI DESHKAR ◽  
ARUN SATPUTE
Keyword(s):  
Solid Dispersion ◽  
Weight Ratio ◽  
Poloxamer 407 ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Dsc Studies ◽  
Poorly Soluble ◽  
Extrusion Spheronization

Objective: The present study was aimed at designing of solid dispersion based pellets of curcumin (Cu) for improving its solubility. Methods: Solid dispersion (SD) of Cu was prepared by the melt method using Poloxamer 407 (Pol 407) at a different weight ratio of Cu-Pol 407 (1:2, 1:3, 1:5, 1:7, 1:10). The solid dispersion was characterised by FTIR, SEM, DSC, XRD and evaluated for saturation solubility in water, drug content and in vitro dissolution. The pellets of Cu solid dispersion were prepared by extrusion spheronization technique and optimization was performed by 32full factorial design. The pellets were evaluated for size distribution, flow properties, hardness, disintegration and in vitro drug dissolution. Results: From the phase solubility analysis, Pol 407 was selected as a Solid dispersion carrier. The formation of Cu-SD by melt method using Pol 407, was confirmed from FTIR and DSC studies. XRD studies indicated a change of Cu from crystalline to amorphous form. There was a significant increase of Cu when formulated as SD compared to plain Cu. The optimization of extrusion spheronization process revealed the significant effect of Cu-Pol 407 ratio (p<0.0001) on in vitro dissolution of pellets. Higher Cu dissolution was obtained with Cu-SD pellets compared to plain Cu pellets. Conclusion: The present study demonstrated the potential of Cu-SD pellets in improving the solubility of poorly soluble Cu.

Stability Study of fast Disintegrating tablets of Nisoldipine as per ICH Guidelines

2021 ◽  
pp. 5843-5844
Author(s):  
Seema Saini ◽  
Rajeev Garg
Keyword(s):  
Research Work ◽  
Storage Period ◽  
Pharmaceutical Product ◽  
Stability Study ◽  
Disintegration Time ◽  
Drug Content ◽  
Ich Guidelines ◽  
Significant Difference ◽  
Fast Disintegrating Tablet ◽  
The Stability

The stability study is a critical parameter to be evaluated in a pharmaceutical product development cycle. A pharmaceutical scientist pays a great deal of heed in testing a product stability. The present research work focused on conducting stability study of fast disintegrating tablet batch of Nisoldipine (NFDT). The various parameters evaluated were weight, hardness, friability, disintegration time, drug content and % drug released. The stability study of optimized fast disintegrating tablet batch NFDT was performed according to ICH guidelines. For the study plan, fast disintegrating tablet batch was placed in a wide mouth air tight containers, which were charged into the stability chamber. The temperature was adjusted at 40°C ± 2°C and relative humidity of 75% ± 5%. The study period was of 6 months. The fast disintegrating tablet batch NFDT did not showed any significant difference in weight, hardness, % friability and disintegration time. The drug content was also reported to be in limits of acceptance. The % drug released at various time intervals was insignificantly changed during its storage period. Hence, the prepared tablets were stable during their storage period.

scholarly journals Formulation and Evaluation of Mouth Dissolving Film of Prochlorperazine Maleate

2019 ◽  
Vol 9 (6) ◽  
pp. 110-115
Author(s):  
Rajat Pawar ◽  
Ravi Sharma ◽  
Gajanan Darwhekar
Keyword(s):  
Oral Bioavailability ◽  
Research Work ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation ◽  
Two Factors ◽  
Experimental Trials

This research work was aimed to enhance the oral bioavailability and provide faster onset of action of Prochlorperazine maleate (used for the treatment nausea and vomiting) by formulating its mouth dissolving film (MDF). Prochlorperazine belongs to BCS II and oral bioavailability of it’s about 11-15%. The MDF of Prochlorperazine  maleate was prepared by solvent casting  method using HPMC (film forming agent),Glycerol (plasticizer), Betacyclodextrin (solubilizing agent), Citric acid (saliva stimulating agent), Mannitol (sweetening agent). The formulation was optimized by two factors, three levels (32) was used for the formulation optimization of fast dissolving film of Prochlorperazine maleate and experimental trials are performed on all 9 formulation. In which the amount of HPMC, Glycerol were selected as independent variables (factor) varied at three different level: low (-1), medium (0), and high (+1) levels. The drug release and disintegration time used as dependent variables (response). and formulation was evaluated for weight variation, thickness, folding endurance, drug content, in- vitro disintegration, in vitro dissolution study and stability study. Based on results it was concluded that MDF (F3) showed enhanced bioavailability and faster onset of action. Keywords: Prochlorperazine maleate, Mouth dissolving film, bioavailability

scholarly journals Designing fabrication and evaluation of Oral fast Disintegrating tablet of Ranitidine HCL

2019 ◽  
Vol 9 (1) ◽  
pp. 95-102
Author(s):  
Afroza Akbar Patel ◽  
Siraj N Shaikh ◽  
Huzaifa Patel ◽  
Afzal Band ◽  
Ahmed Shaoor
Keyword(s):  
Drug Release ◽  
Optimization Technique ◽  
Research Work ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Compression Technique ◽  
Disintegration Time ◽  
Fenugreek Gum ◽  
Fast Disintegrating Tablets

The aim of this research work was to design develop & evaluate oral fast disintegrating tablets of Ranitidine HCL. The Orodispersible tablets of Ranitidine HCl were prepared by using direct Compression technique with a Synthetic Superdisintegrant such as Crosspovidone and a natural Superdisintegrant Fenugreek gum in different concentration. 32 factorial designs was applied to study the effect of independent variables,  concentration of Crosspovidone & Fenugreek gum on dependent variables like Cumulative % Drug release and Disintegration time by using design expert software. Prepared oral fast disintegrating tablets evaluated for Pre and Post-compression parameters. The prepared tablets exhibited satisfactory physico-chemical characterise especially fast disintegration & dissolution property. Full factorial design and optimization technique successfully used in the development oral fast disintegrating tablets. Comparing the all the formulations, formulation F9 was considered as optimized formulation which shows excellent fast disintegration, in vitro dissolution, and faster drug release within 6 min in comparison to other batches also stable in stability study. Keywords:  Fast disintegrating, Ranitidine, Crosspovidone, Gum, Optimizations, Water absorption ratio

An Evaluation of Dictyophora indusiata Mucilage as a Binder in Tablet Formulations

2021 ◽  
Vol 901 ◽  
pp. 22-27
Author(s):  
Kanokporn Burapapadh ◽  
Narumon Changsan ◽  
Chutima Sinsuebpol ◽  
Phennapha Saokham
Keyword(s):  
Research Work ◽  
Edible Mushroom ◽  
High Viscosity ◽  
Commercial Product ◽  
Drug Dissolution ◽  
Disintegration Time ◽  
Pharmaceutical Excipients ◽  
Tablet Formulations ◽  
Paracetamol Tablet

Dictyophora indusiata known as bamboo mushroom is an edible mushroom in Genus Dictyophora, Family Phallaceae that could produce highly viscous mucilage encased in the peridium. The viscous mucilage is clear-colorless hydrocolloid with high viscosity and high adhesive nature which made it possible to be developed into pharmaceutical excipients. This research work aimed at the application of the mucilage as a tablet binder. The mucilage was prepared as redispersible powder by lyphilization before used. The dried mucilage could be effectively used as a binder in paracetamol tablet formulations both as dry and wet binder. Increasing of the dried mucilage amount caused the stronger tablet with higher disintegration time. The optimum concentrations of the dried mucilage in tablet formulations were 2.0% w/w as dry binder and 1.0% w/w as wet binder. The obtained tablets revealed low friability and fast disintegration time. The drug dissolution was conformable to USP37 standard and comparable to that of commercial product. Accordingly, the Dictyophora indusiata mucilage could be functionally used as a tablet binder

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