Formulation and Evaluation of Dispersible tablets of a Model Anti-Parasitic Drug

Author(s):  
S. Preethi ◽  
S. Padmapriya ◽  
A. N. Rajalakshmi

The study was aimed to formulate and evaluate dispersible tablets of a model anti-parasitic drug (XXX) with an objective to produce fast dispersion of tablets by reducing the disintegration time using three superdisintegrants like Sodium Starch Glycolate (SSG), Crospovidone (PVP K30) and Croscarmellose sodium (CCS) and also diluents namely MCC and Lactose by changing their concentrations in each formulations. Totally six formulations (F1-F6) were prepared by direct compression method and evaluated for hardness, thickness, weight variation, friability, wetting volume, wetting time, water absorption ratio, uniformity of dispersion, in-vitro disintegration time, Drug content, in-vitro dissolution test and release kinetics study. FTIR studies was carried out to see possible drug excipients interaction. The stability studies were performed as per ICH guidelines. Among the formulations F6 formulation was found to be promising as it showed better results than other five formulations with In-vitro disintegration time, percentage drug release and dispersion time of 16 ± 0.93 seconds, 98.32±0.54% and 66±1.30 seconds respectively. Further the FTIR results revealed that there was no interactionF between drug and excipients. Stability study of formulation showed no significant changes in tablet properties and the drug follows Higuchi release kinetics with Fickian diffusion mechanism.

Author(s):  
MEGHANA RAYKAR ◽  
MALARKODI VELRAJ

Objective: This study aims to Formulate Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate with the increase in bioavailability and patient compliance. Methods: Mouth Dissolving Tablets (MDTs) of Tofacitinib Citrate were developed by full factorial design at 32levelsand prepared by direct compression method using super integrants like sodium starch glycolate, Ludiflash. The tablets were compressed into compacts on a 10 station tablet machine. The bulk drug was characterised by determining, MP, Solubility, pH and FTIR spectra. Results: The weight variation, hardness and diameter, thickness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies, and stability study, tablet thickness, weight variation and drug content post compression parameters remained consistent and reproducible. All the formulations showed, almost 100 percent of drug release within 75 min. Formulations F1, F2 and F3 were prepared with 5 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F1<F2<F3. Formulations F4, F5 and F6 were prepared with 10 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F4<F5<F6. Formulations F7, F8 and F9 were prepared with 15 mg of SSG and 20 mg, 30 mg, and 40 mg Ludiflash which shows % release of drug in the order of F7<F8<F9. Conclusion: It is concluded that the amount of superdisintegrants decreases disintegration time of tablets, decreases wetting time, increases the cumulative % drug release causes better absorption.


Author(s):  
Avani R. Gosai ◽  
Sanjay B. Patil ◽  
Krutika K. Sawant

The objective of the present investigation was to prepare oro dispersible tablets of ondansetron hydrochloride, because of its application in emesis condition, fast onset of action and avoidance of water is highly desirable. Tablets were prepared by direct compression using sodium starch glycolate and croscarmellose as superdisintegrants, as the combination of these two agents gives better disintegration of the tablet. Microcrystalline cellulose was used as diluent and mannitol, mint flavor, sodium saccharine to enhance the organoleptic properties of tablets. The tablets were evaluated for weight variation, mechanical strength, in vitro disintegration time, in vivo disintegration time, wetting time, and drug release characteristics. Hardness and friability data indicated good mechanical strength of tablets.  The results of in vitro disintegration time and in vivo disintegration time indicated that the tablets dispersed rapidly in mouth within 3 to 5 seconds. Dissolution study revealed faster release rate of ondansetron hydrochloride from the tablets as compared to pure drug and marketed conventional tablet formulation of ondansetron hydrochloride. It was concluded that superdisintegrants addition technique is a useful method for preparing oro dispersible tablets by direct compression method


Author(s):  
Rina G. Maskare ◽  
Nitin H. Indurwade ◽  
Aparna O. Yadav ◽  
Ajita S. Kesharwani ◽  
Aishwarya A. Jain ◽  
...  

The present work concerned with formulation and evaluation of fast disintegrating tablet of Topiramate by using natural superdisintegrants like Trigonellafoenum graceum (fenugreek) powder, Plantago ovata powder, dehydrated banana powder, soy polysaccharide, linseed powder. Topiramate is an antiepileptic drug and also used in migraine. Preformulation studies like solubility, melting point were studied. Five formulations were prepared using different natural superdisintegrant with same concentrations by using direct compression method. All the formulations were evaluated for precompression parameters and all the parameters were found to be within the pharmacopoeial limits. Post compression parameters like hardness of the tablet, thickness of the tablet, friability test, weight variation, disintegration test, in-vitro dissolution test, drug content were performed. The formulation F-5 containing Trigonellafoenum-graceum (fenugreek) powder shown disintegration time of 12sec. Rapid disintegration of the Trigonellafoenum-graceum due to its rapid water absorbency swells in water to the extent of 200–300% disintegrates rapidly for quick and complete disintegration of the tablet. An accelerated stability study on optimized formulation was performed and it was found to be stable. It can be concluded that Trigonellafoenum-graceum (fenugreek) powder as Superdisintegrant showed better release than soy polysaccharide, plantago ovata powder, dehydrated banana powder and linseed powder.


2019 ◽  
Vol 9 (6) ◽  
pp. 110-115
Author(s):  
Rajat Pawar ◽  
Ravi Sharma ◽  
Gajanan Darwhekar

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


Author(s):  
Dharmik M Mehta ◽  
P K Shelat ◽  
P B Parejiya ◽  
A J Patel ◽  
B Barot

 The main objective of this study is to explore development of pharmaceutical excipients from the husk obtained from the seeds of Plantago ovata. Husk shows very good swelling property in water due to the major part of mucilage in it. Since swelling is one of the mechanisms of action of some tablet disintegrants, it is thought that the husk powder of Plantago ovata would be able to act as a tablet disintegrant. The powder obtained from the Plantago ovata husk was characterized for micromeritical properties, swelling capacity, hydration capacity, LOD, pH, particle size, foreign particles, ash value and microbial limit tests. Its disintegrant ability in comparison with maize starch was investigated by preparing famotidine tablets via the direct compression method. It was also compared with three marketed tablets of famotidine. The Plantago ovata husk powder, however, showed superior flow, swelling capacity as well as water retention capacity than maize starch. The tablets were characterized for hardness, friability, weight variation, in vitro disintegration study and in vitro dissolution study. The optimized batch F2C comprising of 10% of the Plantago ovata husk powder showed a 15 seconds disintegration time, which was significantly less than tablets prepared from maize starch as well as all three market preparations. Tablets from batch F2C were submitted for short term stability studies and exhibited stable characteristics.


Author(s):  
SHEEBA F. R. ◽  
KUNDAN CHAUDHARY

Objective: In the present study, the effects of a natural superdisintegrant gellan gum, karya synthetic gum superdisintegrants like sodium starch glycolate, crospovidone and combination of natural and synthetic superdisintegrant were compared in the formulations of rizatriptan benzoate oral dispersible tablets. Methods: This oral dispersible tablets were prepared by direct compression method and evaluated for weight variation, hardness, disintegration time, drug content, friability and dissolution. Drug compatibility with excipients was checked by FTIR studies. Stability study of the prepared tablets was done at 40±2°/75%±5% RH for a period of 1 mo. Results: FTIR studies showed that no any chemical interaction between drugs and excipients. The in vitro drug release study revealed that formulation F9 combination of both crospovidone and karya gum was the most successful formulation and disintegrate time within 13 seconds and drug release within 10 min. The drug release from the best formulations followed first-order kinetics, which is concentration-dependent. Short terms stability studies of the tablet for three months showed non-significant drug loss. Conclusion: The formulation containing a combination of natural and synthetic superdisintegrant was found to be the best results. Apart from fulfilling all official and other specifications, the tablets exhibited a higher rate of drug release.


Author(s):  
Deborah Ejiogu Chioma ◽  
Felix Sunday Yusuf

Metoclopramide hydrochloride is a dopamine receptor antagonist, used mostly for stomach and esophageal problems as it is a prokinetic agent. The aim of the present study was to design and evaluate the suppositories of Metoclopramide HCl.  Six different, rectal suppositories were developed by fusion (pour-moulding) method by employing various hydrophilic and hydrophobic polymeric bases like gelatin, PEG-400 and hydrogenated vegetable oil using propylene glycol as plasticizer and beeswax as hardening agent.  Metoclopramide HCl suppositories were evaluated for appearance, weight variation, drug content uniformity, liquefaction time and temperature, micro-melting range, disintegration and in-vitro release study.  The in-vitro release rate data was evaluated statistically and was found that from all the formulations the drug release is by diffusion mechanism. Optimum formulation of batch S1 has shown 83.427% Metoclopramide HCl in a study of 2 hrs. These drug release results are supported by the disintegration time of suppositories. Lesser the disintegration time faster the drug release. All formulations has shown zero, first and Higuchi release kinetics. The result suggests that the Metoclopramide HCl suppositories can be prepared by employing hydrophilic and hydrophobic polymers.


Author(s):  
P. Srinivasa Rao ◽  
T. Rama Mohan Reddy

The current investigation was aimed with the objective of formulating Selegiline fast dissolving oral thin films allowing fast reproducible drug dissolution in oral cavity thus bypassing the first pass metabolism to enhance the patient convenience and compliance in the effective treatment of Parkinson's disease. Oral thin films of Selegiline were prepared by solvent casting method with using different film forming agents like HPMC5LV, HPMC 15LV, HPMC50LV and HPMC K4M. Propylene glycol, Sucrose, Vanillin is used as a plasticizer, sweetening agent, flavouring agent respectively and citric acid as saliva stimulating agent. FDOFs were evaluated for physical characteristics, Surface pH, weight variation, thickness, folding endurance, percent drug content, percentage elongation, disintegration time, in vitro dissolution studies. Based on all the evaluation studies F18 is selected as optimized formulation and in vitro disintegration time and amount of drug release from the film was 9 seconds and 99.68% within 7 min respectively


Author(s):  
SANJEEV KUMAR ◽  
AMIN MIR M ◽  
SARVESH KUMAR ◽  
ANUJ KUMAR

Objective: The main focus of the study was to investigate the marketed formulations of cinnarizine and it is marketed analogous. Methods: The study involved the analysis of basic pre-formulation studies, namely, physical properties, melting point, Fourier-transform infrared, loss on drying, assay of cinnarizine, standard curve, and partition co-efficient of various marketed tablets of cinnarizine. Results: Cinnarizine is an H1-receptor antagonist drug which is widely used for the treatment of dynamical sickness, vomiting, and vertigo. In this study, five known marketed formulations of cinnarizine were evaluated for weight variation, hardness, drug content, friability, disintegration time, and in vitro dissolution as well as the drug release kinetics of the tablets. As per the study, the drugs show low disintegration time and good hardness, also in vitro dissolution studies have shown near about 90% drug release at the end of the first 10 min and then cumulative drug release of not less than 92% in the nearby 10 min. Hence, these formulations show lower friability, acceptable taste, and shorter disintegration time which make them suitable to be accepted. Thus, the tablets are good for the use, so allow them to be marketed for the wellbeing of humans. Conclusion: It had been found that all the tablets show acceptable limits for various parameters of analysis, in a sustained manner. Thus, all the tablets are effective for usage under standard conditions.


Author(s):  
Sudarshan Singh ◽  
S S Shyale ◽  
P Karade

The aim of this study was to design orally disintegrating tablet (ODT) of Lamotrigine. It is an Antiepileptic drug which is widely used in epilepsy. It is also used in simple and complex partial seizures and secondary generalized tonic-clonic seizures. It is poorly water soluble drug (0.46 mg/ml). Thus, an attempt was made to enhance the water solubility by complexation with β-cyclodextrin (1:1 molar ratios). The orally disintegrating tablet of lamotrigine was prepared by direct compression method using different concentration of superdisintegrants such as Sodium starch glycollate, croscarmellose sodium by sublimating agent such as camphor. The formulations were evaluated for weight variation, hardness, friability, drug content, wetting time, in vitro disintegration time and in vitro dissolution studies. The prepared tablets were characterized by Fourier transform infrared spectroscopy and differential scanning calorimetry. The disintegration time for the complexed tablets prepared by different concentration of superdisintegrants was found to be in range of 32.54 ± 0.50 to 55.12 ± 0.57 sec and wetting time of the formulations was found to be in range of 28.47 ± 0.67 to 52.19 ± 0.72 sec. All the formulation showed almost 100 percent of drug release within 15 min. Among all the formulation F6 and F7 prepared with 18% croscarmellose sodium and camphor shows faster drug release, respectively 10 min, F6 gives good result for disintegration time, drug release, wetting time and friability. Further formulations were subjected to stability testing for 30 days at temperature of 40 ± 5 ºC/75 ± 5 %RH. Tablets showed no appreciable changes with respect to physical appearance, drug content, disintegration time and dissolution profiles. Results were statistically analyzed by one-way ANOVA at a p < 0.05. It was found that, the data at any point of time are significant at p < 0.05.


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