scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING TABLET OF APREPITANT BY USING NATURAL AND SYNTHETIC SUPERDISINTEGRANTS

2019 ◽  
pp. 64-71
Author(s):  
RAJNI BALA ◽  
SHAILESH SHARMA ◽  
IKGPTU
Keyword(s):  
Compression Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
First Pass Metabolism ◽  
First Pass ◽  
Croscarmellose Sodium ◽  
Improve Patient ◽  
Pass Metabolism ◽  
Natural And Synthetic

Objective: The present study was aimed to formulate fast dissolving tablets (FDTs) of Aprepitant (APT) using natural and synthetic superdisintegrants with the desired onset of action, increased bioavailability by reducing the frequency of dosage and also reduce the first-pass metabolism of the drug. Methods: In this research, the gum isolated from cordia dichotoma was investigated as super disintegrants in fast dissolving tablets (FDTs). The aprepitant tablets were prepared separately using cordia dichotoma (natural), sodium starch glycolate and croscarmellose sodium (synthetic) as superdisintegrants by direct compression method. The tablets were evaluated for various precompression and post-compression parameters. Results: The optimized formulation (APT F3) of cordia dichotoma (8%) showed satisfactory physicochemical properties, minimum disintegration time (34 seconds) and highest dissolution rate (86.52%) in 10 min than the other synthetic superdisintegrants. Also, the pharmacokinetic study of the optimized formulation showed effective results as compared with marketed product of aprepitant. Conclusion: The developed formulation can improve the onset of action as well as improve patient compliance.

scholarly journals Formulation And Evaluation of Fast Dissolving Oral Films Incorporated With Ramipril and β-Cyclodextrin Complex

2020 ◽  
pp. 390-395
Author(s):  
Puttaswamy Nirmala
Keyword(s):  
Cyclodextrin Complex ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Drug Content ◽  
Bcs Class Ii ◽  
First Pass Metabolism ◽  
First Pass ◽  
Oral Films ◽  
Low Solubility ◽  
Pass Metabolism

Ramipril being ACE inhibitor belongs to BCS class II drug with low solubility and undergoes first-pass metabolism that leads to reduced bioavailability of 28%. The current research is aimed at formulating and evaluating ramipril fast dissolving oral films (FDOF). Solubility enhancement of ramipril was done by formation of   inclusion complex with β-cyclodextrin in 3 ratios (1:0.5, 1:1, 1:2). Based on higher drug content and dissolution values the physical mixture of ramipril with β-cyclodextrin in 1:1 ratio (IC2) was chosen for further studies. Total 12 formulations of ramipril FDOF containing IC2 prepared with various polymers and evaluated for physicochemical properties. The optimized formulation F9 shown better tensile strength (11.6 g/cm2), significant % elongation (9.8) and maximum % drug content of 99.98 %. The formulation F9 exhibited minimum disintegration time of 9 sec that is desirable for immediate onset of action and maximum drug release. The FTIR data of F9 assured the compatibility of drug and formulation excipients, found to be stable for 180 days at accelerated conditions. The study confirmed that ramipril FDOF lead to quicker onset of action and enhanced therapeutic efficiency in comparison to marketed product.

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 Formulation and Evaluation of Mouth Dissolving Tablets Containing Losartan Potassium Using Natural Superdisinigrants

2017 ◽  
Vol 9 (05) ◽  
Author(s):  
Bhimi Kumari ◽  
Abhishek Soni ◽  
Shivali Singla ◽  
Sachin Goyal ◽  
Samriti Thakur ◽  
...  
Keyword(s):  
Losartan Potassium ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Fast Onset ◽  
Weight Variation ◽  
Time Dispersion ◽  
First Pass Metabolism ◽  
Wetting Time ◽  
Mouth Dissolving Tablet ◽  
Pass Metabolism

Losartan potassium is used as an antihypertensive drug but it goes under first pass metabolism due do which it has low bioavailability. Fast onset of action is major concern in the management of hypertension. Therefore the aim of this study is to formulate mouth dissolving tablet of losartan potassium to improve its bioavailability, to achieve fast onset of action and increase patient compliance. Mouth dissolving tablets were prepared by direct compression method using natural super disintegrating agents (banana powder and apple pectin) and evaluated for pre-compression parameters and post compression parameters such as appearance, dimensions, hardness, weight variation, friability, wetting time, dispersion time, water absorption ratio, disintegration and dissolution study. According to results of optimized batches it has been concluded that formulation batch F9 was an ideal batch which contain banana powder (2.5%) and cross povidone (2.5%) showed least disintegration time that is 26 seconds and maximum drug release of (99.68%) within 12 minutes and was best among all the formulations.

scholarly journals Formulation and Evaluation of Rapimelt Tablet of Anti-Vertigo Drug (Lorazepam)

2020 ◽  
Vol 13 (4) ◽  
pp. 341-349
Author(s):  
B. M. Kadu ◽  
S. Bhasme ◽  
R. D. Bawankar ◽  
D. R. Mundhada
Keyword(s):  
Rapid Onset ◽  
Dissolution Time ◽  
Direct Compression ◽  
Compression Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Ft Ir ◽  
Wetting Time ◽  
Mouth Feel

A. Rapimelt tablet of Lorazepam was prepared by direct compression method using Indion 414, Cross Carmellose Sodium and sodium starch glycolate as superdisintegrants with aim to get rapid onset of action, improve bioavailability and to give pleasant taste and better mouth feel. The tablets prepared were evaluated for various parameters like various density parameters, thickness, hardness, friability, disintegration time, wetting time and invitro dissolution time and were found to be within limits as per Indian Pharmacopoeia. FT-IR spectra of physical mixture of Lorazepam with Indion 414showedretention of basic peaks of Lorazepam. The developed formulation of Lorazepam batch F5 (10% Indion 414) showed good palatability and dispersed within 30 seconds as compared to Crosscarmellose Sodium batches F1-F3 and Sodium starch glycolate batches F6-F9.

scholarly journals Formulation development and evaluation of Orally Disintegrating Tablets Rizatriptan Benzoate

2021 ◽  
pp. 79-87
Author(s):  
Saibabu Ch ◽  
Triveni P
Keyword(s):  
Formulation Development ◽  
Compression Method ◽  
Drug Molecule ◽  
Onset Of Action ◽  
Rizatriptan Benzoate ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Orally Disintegrating Tablets ◽  
Wetting Time ◽  
Croscarmellose Sodium

Formulation research is oriented towards safety, efficacy and quick onset of action of existing drug molecule through novel concepts of drug delivery. Orally disintegrating tablets of Rizatriptan benzoate were prepared by direct compression method to provide faster relief from pain to migraine sufferers. About eleven formulations for the present study were carried out. Croscarmellose sodium, Crospovidone and Sodium starch glycolate (SSG) were used as superdisintegrants, while microcrystalline cellulose was used as diluent. The prepared batches of tablets were evaluated for weight variation, hardness, friability, wetting time, invitro dispersion time, drug content and invitro dissolution studies. The formulation containing combination of Croscarmellose sodium and Sodium starch glycolate showed rapid invitro dispersion time as compared to other formulations. The optimized formulation dispersed in 8 seconds. It also showed a higher water absorption ratio and 99.58% of drug is released within 2 minutes.

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.

scholarly journals FORMULATION AND EVALUATION OF SUBLINGUAL FILMS OF APIXABAN

2019 ◽  
Vol 7 (2) ◽  
Author(s):  
Arjun L. Joshi ◽  
Anil G Raval
Keyword(s):  
Dosage Form ◽  
Nonvalvular Atrial Fibrillation ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Film Forming ◽  
Dependent Variables ◽  
Maximum Stability ◽  
32 Factorial Design ◽  
Improve Patient ◽  
Pass Metabolism

The concept of sublingual film dosage form has become popular as new delivery system. This system will provide maximum therapeutic efficacy, increased bioavailability and maximum stability by reducing the frequency of dosage. It will also avoid first pass metabolism of the drugs. This system provides more rapid drug absorption from the pre gastric area which may provide quick onset of action. The present research aimed to prepare sublingual films of apixaban reduces the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. The film was prepared using solvent casting method and optimized employing 32 factorial design considering two independent variables film forming polymer (HPMC E5) and PEG 400. Disintegration time, drug release and folding endurance were taken as dependent variables. The prepared optimized formulation showed minimum disintegration time (35 s), highest dissolution rate (99 %) and satisfactory physicochemical properties. It is evident from the above results that the developed formulation can be an innovative dosage form to improve the drug delivery, onset of action as well as improve patient compliance. Key Words: Apixaban, Sublingual films, HPMC

Development and Evaluation of Novel Fast Disintegrating Acetaminophen Tablets

2015 ◽  
Vol 8 (1) ◽  
pp. 2748-2755
Author(s):  
Anil M Pethe ◽  
A.T. Patil ◽  
D R Telange ◽  
A A Tatode
Keyword(s):  
Delivery System ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Easy Access ◽  
Direct Compression ◽  
Compression Method ◽  
First Pass Metabolism ◽  
First Pass ◽  
Poor Absorption ◽  
Pass Metabolism

In this study, attempts were made to design and developed disintegrating drug delivery system, Acetaminophen fast disintegrating tablet (AFDT) by combining super disintegrants and direct compression method. Acetaminophen is widely used as “over the counter” and “common household drug” as analgesic and antipyretic along with poor absorption due to first pass metabolism. So we aimed to use our novel delivery system to achieve rapid absorption in patients like mentally ill, bed ridden and those who do not have easy access to water. The (AFDT) were produced by combining three super disintegrants viz. Croscarmellose, Crospovidone and Sodium starch glycolate in 4% w/w as ratio of (1:1, 1:2, 2:1) using direct compression method. The optimized batch (A3) of tablet were evaluated for post – compression parameters like hardness (4.5 ± 0.75 kg.cm2), friability ((0.76 %), wetting time (42 ± 0.92 sec), water absorption ratio (98.6 %), disintegration time (24.00 ± 0.83 sec.) were found to be acceptable according to standard limits. The in vitro release rate of acetaminophen from (AFDT) was found to be more than that simple formulation in pH (5.8) using USP dissolution test apparatus type-II. These results indicated that, the new (AFDT) formulation system combined advantage of faster release of acetaminophen, which had better effects of rapid oral absorption. Therefore, the AFDT may be used as fast disintegrating delivery system for OTC drug with poor absorption due to first pass metabolism.

scholarly journals Formulation and evaulation of triazolam odts by direct compression forselection & optimization of super disintegrates

2021 ◽  
pp. 36-45
Author(s):  
Sudhakar Kancharla ◽  
Prachetha Kolli ◽  
Dr.K.Venkata Gopaiah
Keyword(s):  
Geriatric Patients ◽  
Methyl Cellulose ◽  
The Other ◽  
Direct Compression ◽  
Solvent Casting ◽  
Compression Method ◽  
Casting Method ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Croscarmellose Sodium

Oral Disintegrating Tablets of Triazolam were formulated with an aim to improve the versatility, patient compliance, and accurate dosing. The formulations ere developed with an objective to use by the pediatric and geriatric patients. Triazolam Oral Disintegrating Tablets were prepared by direct compression method using cross povidone, croscarmellose sodium, sodium starch  glycolate and combinations of CP+CCS, and CP + SSG as super disintegrates exhibited good pre-formulation and tableting properties of three super disintegrates, the formulation contained combination of CP + CCS showed better performance in terms of disintegration time when compared to other formulations. Order of the super disintegrates activity is as follows. (CP + CCS) > (CP + SSG) > CP > CCS >SSG The formulation F15 was found to be the best among all twenty Triazolam ODT formulations because it has exhibited faster disintegration time (17.66 sec) when compared to the other formulations and it showed 99.87±0.18% drug release at the end of 25 min. Triazolam Oral Disintegrating Films were prepared by solvent casting method using different grades of Hydroxypropyl Methyl Cellulose like HPMC – E15, HPMC – 5cps, HPMC – 50cps. Based on disintegration and dissolution results it was concluded that the formulation F15 contained CP 5% + CCS 5% was the best formulation among all otherformulations.

scholarly journals Critical Review of Lipid-Based Nanoparticles as Carriers of Neuroprotective Drugs and Extracts

Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 563
Author(s):  
Filipe Fernandes ◽  
Mónica Dias-Teixeira ◽  
Cristina Delerue-Matos ◽  
Clara Grosso
Keyword(s):  
Brain Parenchyma ◽  
Drug Bioavailability ◽  
Onset Of Action ◽  
Routes Of Administration ◽  
Neuroprotective Drugs ◽  
First Pass Metabolism ◽  
First Pass ◽  
The Central Nervous System ◽  
The Brain ◽  
Pass Metabolism

The biggest obstacle to the treatment of diseases that affect the central nervous system (CNS) is the passage of drugs across the blood-brain barrier (BBB), a physical barrier that regulates the entry of substances into the brain and ensures the homeostasis of the CNS. This review summarizes current research on lipid-based nanoparticles for the nanoencapsulation of neuroprotective compounds. A survey of studies on nanoemulsions (NEs), nanoliposomes/nanophytosomes and solid lipid nanoparticles (SLNs)/nanostructured lipid carriers (NLCs) was carried out and is discussed herein, with particular emphasis upon their unique characteristics, the most important parameters influencing the formulation of each one, and examples of neuroprotective compounds/extracts nanoencapsulated using these nanoparticles. Gastrointestinal absorption is also discussed, as it may pose some obstacles for the absorption of free and nanoencapsulated neuroprotective compounds into the bloodstream, consequently hampering drug concentration in the brain. The transport mechanisms through which compounds or nanoparticles may cross BBB into the brain parenchyma, and the potential to increase drug bioavailability, are also discussed. Additionally, factors contributing to BBB disruption and neurodegeneration are described. Finally, the advantages of, and obstacles to, conventional and unconventional routes of administration to deliver nanoencapsulated neuroprotective drugs to the brain are also discussed, taking into account the avoidance of first-pass metabolism, onset of action, ability to bypass the BBB and concentration of the drug in the brain.

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