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

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 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.

Oral Disintegrating Tablets – An Updated Patent Perspective

2020 ◽  
Vol 14 ◽  
Author(s):  
Shailesh Sharma ◽  
Kuljit Singh
Keyword(s):  
Dosage Form ◽  
Rapid Onset ◽  
Wet Granulation ◽  
Patent Citations ◽  
Onset Of Action ◽  
Solid Dosage ◽  
Alternative Approach ◽  
Cotton Candy ◽  
Improve Patient ◽  
Advantageous Effect

Abstract:: Current development in drug delivery system has been employed with an endeavour of enhancing the bioavailability, mask the taste of drug, rapid onset of action and improve patient compliance. An alternative approach of conventional dosage form is being employed to triumph over all these issues named as Orodispersible system. Over past three decades this novel dosage form gain a considerable attention as compared to other conventional solid dosage form such as tablet and capsules. ODTs dissolved or disintegrate within few seconds to a minute when put on the tongue, without need of water. ODT has an advantageous effect on paediatrics and geriatrics patients with dysphagia. Over the last decade, widespread advances in the formulation of ODTs have been executed in academia and industry that resulted in the emerging of a large number of patents. Products developed from ODT mechanics launched in the market in the 1980s, have grown bit by bit in demand and their product are rapidly escalating. Expanding in the technology forum for industrialized these systems include the use of lyophilization, cotton candy, sublimation, melt extrusion and direct compression in addition the conventional wet granulation processes and patent techniques. The present study focused on non-patent and patent citations concerning to ODT along with active ingredients, technique used and results of the innovations.

Formulation and Evaluation of Salbutamol Sulphate Sublingual Films

2017 ◽  
Vol 10 (5) ◽  
pp. 3836-3843
Author(s):  
Y Shravan Kumar ◽  
Deepthi B ◽  
Mounika M
Keyword(s):  
In Vitro Dissolution ◽  
Casting Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Salbutamol Sulphate ◽  
Weight Variation ◽  
Film Forming ◽  
Adrenergic Receptor Agonist ◽  
Polymer Ratio

Salbutamol is a short-acting, selective beta-2-adrenergic receptor agonist used in treatment of asthma and COPD. In the present work, sublingual films of Salbutamol sulphate were developed with a view to enhance the patient compliance and provide quick onset of action. Salbutamol has a bioavailability of 53 - 60%. The goal of the study was to formulate sublingual films of Salbutamol sulphate to achieve a better dissolution rate and further improving the bioavailability of the drug. Sublingual films prepared by solvent casting method using film forming polymers HPMC-E5, HPMC-E15 and Maltodextrin in different ratios. The prepared batches of films were evaluated for the drug content, weight variation, film thickness, disintegration time and in vitro dissolution studies. Among all, the formulation B1 containing HPMC-E15 with a drug: polymer ratio (1:6) was found to be the best formulation which showed 98.36% of the drug release within 15 minutes and disintegration time 18 sec. This study shows the viability of developing sublingual films of salbutamol.    

scholarly journals AN OVERVIEW ON MOUTH DISSOLVING FILM

2018 ◽  
Vol 11 ◽  
Author(s):  
Raykar Meghana
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Dosage Form ◽  
Active Drug ◽  
Transdermal Patch ◽  
Therapeutic Action ◽  
Improve Patient Compliance ◽  
Systemic Delivery ◽  
Onset Of Action ◽  
Improve Patient

Context: Mouth dissolving film (MDF) is an innovative approach for systemic delivery of therapeutically/ medicinally active drug substance(s). Objective: The main objectives of Oral mouth dissolving films is to provide better bioavailability of drug, to have improved permeability, quick onset of action as well as improve patient compliance Method: Preparation of films is similar to that of transdermal patch. Film when placed in mouth it get dissolve rapidly due to salivary fluid then it releases medicament(s), It will get absorbed within blood to show therapeutic action. Results: This overview provides information about formulation, technologies used in making mouth dissolving film formulations and evaluation tests carried out for the same. Conclusion: Mouth dissolving film formulations are innovative dosage form to improve the drug delivery, onset of action as well as improve patient compliance

scholarly journals Research Paper DESIGN, OPTIMIZATION AND EVALUATION OF EMPAGLIFLOZIN ORODISPERSIBLE TABLETS USING DIFFERENT SUPERDISINTEGRANTS

2019 ◽  
pp. 32-41
Author(s):  
AKANKSHA DWIVEDI ◽  
G. N. DARWHEKAR
Keyword(s):  
Drug Release ◽  
Rapid Onset ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Dependent Variables ◽  
Tablet Properties ◽  
Croscarmellose Sodium ◽  
Experimental Trials ◽  
Different Levels

Objective: The objective of this study was to formulate orodispersible tablets containing empagliflozin by direct compression method with sufficient hardness and rapid disintegration time and to study the effect of functionality differences of super-disintegrants on the tablet properties. Methods: A two factor three level factorial design (32) was used for the formulation optimization of orodispersible tablets of Empagliflozin and experimental trials were performed on all possible formulations, in which the amount of β-cyclodextrin, crospovidone and croscarmellose sodium were selected as independent variables (factor) varied at three different levels: low (-1), medium (0), and high (+1) levels. The drug release and disintegration time were used as dependent variables (response). All formulations were characterized for parameters such as diameter, hardness, weight, thickness, friability, disintegration time, drug release. Results: Formulation FD6 having 30 sec disintegration time, 98.84% drug release after 30 min, 2.8 kg/cm2 hardness and 0.292% friability was found best among all formulations and selected as an optimized formulation with rapid onset of action and enhanced bioavailability (more than 98% drug release within 30 min.) as compared to the oral empagliflozin tablet. Conclusion: Empagliflozin orodispersible tablets with different superdisintegrants were successfully prepared and formulation containing highest percentage of crospovidone was found best among all other formulations in terms of bioavailability and rapid onset of action.

scholarly journals Development and Evaluation of Mouth Dissolving Films Containing Selegiline

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
P. Srinivasa Rao ◽  
T. Rama Mohan Reddy
Keyword(s):  
Thin Films ◽  
Evaluation Studies ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Weight Variation ◽  
Film Forming ◽  
In Vitro Disintegration ◽  
Pass Metabolism

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

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 PREPARATION AND EVALUATION OF MEFENAMIC ACID AND DICYCLOMINE HYDROCHLORIDE AS ORAL DISINTEGRATING TABLET BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 10 (4) ◽  
pp. 94-101
Author(s):  
Ranjitha M T ◽  
C N Somashekhar
Keyword(s):  
Mefenamic Acid ◽  
Dosage Form ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Direct Compression ◽  
Compression Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Improved Stability ◽  
Oral Disintegrating Tablet

A new dosage form, Oral disintegrating tablets (ODT’s) as a replacement to conventional oral dosage forms. ODT’s are dosage forms they disintegrate in mouth offering various advantages such as better mouth feel, dose accuracy, improved stability and convenient dosing as compared to oral liquids. So, there is need to designed oral disintegrating tablet to release the medicaments with an enhanced rate. Mefenamic acid is an anti- inflammatory drug while Dicyclomine HCl is anti-cholinergic drug. The combination of Mefenamic acid & Dicyclomine HCl controls pain very effectively, also relaxes bodily spasm which commonly arises during menstruation or intestinal colic spasm. This combination gives the quick onset of action and fast relief than conventional dosage form. For preparation of oral disintegrating tablet nine formulations were designed using Croscarmellose sodium and Crospovidone as superdisintegrants in varying concentration. All the formulations were prepared by direct compression method. Thus, all the formulations of Mefenamic acid and Dicyclomine HCl oral disintegrating tablets were investigated, in which F9 formulation was optimized. The % drug release of, Oral disintegrating tablet batch F9 has shown 96.98% of Mefenamic acid and 94.02 % of Dicyclomine HCl in 18 min, disintegration time in 40 sec and wetting time in 25sec.

Pharmacokinetic peculiarities of drugs used in the form of rapidly dispersible tablets (oral delivery system)

2020 ◽  
pp. 7-24
Author(s):  
Zhanna Kozlova ◽  
Ivan Krasnyuk ◽  
Yuliya Lebedeva ◽  
Ekaterina Odintsova
Keyword(s):  
Oral Mucosa ◽  
Oral Delivery ◽  
Chemical Properties ◽  
Rapid Onset ◽  
Systemic Circulation ◽  
Systemic Delivery ◽  
Onset Of Action ◽  
Mucosal Drug Delivery ◽  
Physical And Chemical ◽  
Pass Metabolism

Oral mucosal drug delivery is an alternative method of systemic delivery with several advantages over both injectable and enteral methods. Drugs that are absorbed through the oral mucosa directly enter the systemic circulation, passing through the gastrointestinal tract and first-pass metabolism in the liver due to oral mucosa being highly vascularised. This results in rapid onset of action for some drugs because of a more comfortable and convenient way of delivery than the intravenous one. But not all drugs can be administered through the oral mucosa due to characteristics of the oral mucosa and physical and chemical properties of the drug.

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