scholarly journals FORMULATION OPTIMIZATION AND EVALUATION OF MOUTH DISSOLVING FILM OF APREPITANT

2019 ◽  
pp. 154-163
Author(s):  
ADITI D BAVISKAR ◽  
BARI MM ◽  
BARHATE SD
Keyword(s):  
Nausea And Vomiting ◽  
Compatibility Study ◽  
Scanning Calorimetry ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Peg 400 ◽  
Weight Variation ◽  
Prevention And Treatment ◽  
Post Operative Nausea

Objectives: The aim of the present research is to prepare mouth dissolving film of aprepitant used in the prevention and treatment of post-operative nausea and vomiting. Methods: The MDF was prepared using Kollicoat IR, PEG 400, and spraying technique. Formulation was optimized by central composite design. Compatibility study was carried out using Fourier-transform infrared and differential scanning calorimetry. The films were evaluated for thickness, folding endurance, weight variation, disintegration time, dissolution studies, drug content, and in vitro diffusion test. Results: From the results, it was found that there was no drug excipient interaction. The prepared optimized batch AP2 showed disintegration time 18 sec, highest dissolution rate 101.53%, drug diffused 39.58 mg/cm2 within 10 min and also passes all the physicochemical parameters. It was concluded that plasticizer PEG 400 plays a very much important role in the preparation of aprepitant MDF. Conclusion: MDF of aprepitant was found to be a better option in the prevention and treatment of post-operative nausea and vomiting by the way of fast onset of action for patient convenience and compliance. In the near future, the MDF market will expand very fastly to treat various diseases.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING FILM OF LORNOXICAM

2018 ◽  
Vol 11 (9) ◽  
pp. 217
Author(s):  
Zainab E Jassim ◽  
Mais F Mohammed ◽  
Zainab Ahmed Sadeq
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Compatibility Study ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Weight Variation ◽  
Film Forming ◽  
Folding Endurance

Objective: The aim of the present work was to formulate and evaluate fast dissolving film containing lornoxicam.Materials and Methods: To prepare the film, hydroxypropyl methylcellulose E5 and polyvinyl alcohol (PVA) were used as film-forming polymers by solvent casting method. Glycerine was used as plasticizer, aspartame, and mannitol as sweetener. All prepared films were evaluated for its weight variation, disintegration time, thickness, drug content, pH, dissolution study, and folding endurance. The drug-excipients compatibility study was done using differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR).Results: Satisfactory results obtained when PVA was used as film-forming polymer, and the drug was dispersed in the polymer solution using poloxamer 407 as a solubilizing agent. Formulation F2 is considered as the optimized formulation as it showed good folding endurance (>300), faster disintegration rate (30 s), and maximum in vitro drug release (87%) within 5 min. DSC and FTIR studies showed no interaction between drug and the polymers.Conclusion: It can be concluded from the study that the fast dissolving film can be prepared for poorly water-soluble drug lornoxicam using PVA as a suitable film-forming polymer.

scholarly journals FORMULATION AND EVALUATION OF CHLOROTHALIDONE LOADED MOUTH DISSOLVING FILM-A BIOAVAILABILITY ENHANCEMENT APPROACH USING MULTILEVEL CATEGORIC DESIGN

2020 ◽  
pp. 34-41
Author(s):  
SHUBHAM BIYANI ◽  
SARANG MALGIRWAR ◽  
RAJESHWAR KSHIRSAGAR ◽  
SAGAR KOTHAWADE
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Aqueous Dispersion ◽  
Onset Of Action ◽  
Polyethylene Glycol 400 ◽  
Bioavailability Enhancement ◽  
Disintegration Time ◽  
Peg 400 ◽  
Folding Endurance

Objective: The intension of the present study includes fabrication and optimization of mouth dissolving film loaded with Chlorothalidone by solvent evaporation techniques using two components and their three levels as multilevel Categoric design. Methods: Major problem associated with the development of film loaded with BCS class II drug is to increase its solubility. Here the Chlorothalidone solubility achieved by co-solvents, such as methanol. After dissolving the drug in co-solvent, this drug solution is poured into an aqueous dispersion of Hydroxypropyl Methylcellulose E5 (HPMC E5) and Polyethylene glycol 400 (PEG 400). The two independent variables selected are factor A (concentration of HPMC E5) and factor B (concentration of PEG 400) was selected on the basis of preliminary trials. The percentage drug release (R1), Disintegration time in sec (R2) and folding endurance (R3) were selected as dependent variables. Here HPMC E5 used as a film former, PEG 400 as plasticizer, mannitol as bulking agent, Sodium starch glycolate as a disintegrating agent, tween 80 as the surfactant, tartaric acid as saliva stimulating agent, sodium saccharin as a sweetener and orange flavour etc. These fabricated films were evaluated for physicochemical properties, disintegration time and In vitro drug release study. Results: The formulation F6 has more favorable responses as per multilevel categoric design is % drug release about 98.95 %, average disintegration time about 24.33 second and folding endurance is 117. Thus formulation F6 was preferred as an optimized formulation. Conclusion: The present formulation delivers medicament accurately with good therapeutic efficiency by oral administration, this mouth dissolving films having a rapid onset of action than conventional tablet formulations.

scholarly journals FORMULATION AND EVALUATION OF FUROSEMIDE LIQUISOLID COMPACT

2017 ◽  
Vol 9 (6) ◽  
pp. 39
Author(s):  
Zainab E. Jassim
Keyword(s):  
Dissolution Rate ◽  
Content Uniformity ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 400 ◽  
Coating Materials ◽  
Disintegration Time ◽  
Weight Variation ◽  
R Ratio

Objective: The purpose of this study was to enhance the dissolution pattern of the practically water-insoluble diuretic drug, furosemide through its formulation into liquisolid tablets.Methods: A mathematical model was used to formulate four liquisolid powder systems using polyethylene glycol 400 as a non-volatile water miscible liquid vehicle. The liquid loading factors of the vehicle were used to calculate the optimum quantities of carrier (Avicel PH 102) and coating materials (Aerosil 200) needed to prepare acceptably flowing and compactible powder mixtures and (R) ratio used was 25. The liquisolid tablets were evaluated for weight variation, percent friability, hardness, content uniformity, disintegration time and in vitro drug release profile. Drug and the prepared systems were characterized by fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder x-ray diffraction (PXRD) studies.Results: The enhanced dissolution rate due to the increased wetting properties and the large available surface areas for dissolution were obtained in case of the liquisolid tablets. The selected optimal formulation (F2) of 50% drug concentration released 90% of its content during the first 10 min compared to 65% of DCT. FTIR studies revealed that there was no interaction between drug and polymers. DSC and PXRD indicated conversion of crystalline to amorphous form of furosemide. Conclusion: The dissolution rate of furosemide can be enhanced to a great extent by liquisolid technique.

scholarly journals Development of Tropisetron Hydrochloride Orodispersible Tablet using Natural Superdisintigrants

2021 ◽  
pp. 191-210
Author(s):  
Rupalben K. Jani ◽  
Gohil Krupa ◽  
Aanal Gandhi ◽  
Vijay Upadhye ◽  
Roshani Pragnesh Amin
Keyword(s):  
Drug Candidate ◽  
Antiemetic Drug ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Cassia Tora ◽  
Weight Variation ◽  
Orodispersible Tablet ◽  
Value Loss ◽  
Time Required

The foremost objective of this research was to compare and evaluate natural super disintegrants with synthetic super disintegrants for the preparation of the orodispersible tablet. Tropisetron hydrochloride is widely used as an antiemetic drug, which is a potential drug candidate for developing an orodispersible tablet for quick onset of action. Various formulations were prepared using different concentrations (5%, 7.5%, and 10%) by direct compression method of natural super disintegrants (Banana power and Cassia tora powder) and synthetic super disintegrants (Croscarmellose sodium, Crospovidone, and Sodium starch glycolate). The compatibility studies between the drug and excipients were carried out using FTIR spectroscopy before tablet formulation. The pre-compression parameters were evaluated for additive properties. Standardization of banana powder was done by various parameters like extractive value, ash value, loss on drying, TLC identification test, etc. Post-compression parameters like hardness, weight variation, friability, thickness, the time required for disintegration, wetting time, the release of drug in-vitro, and in-vitro dispersion time of the tablets were evaluated. The disintegration time and in-vitro drug release of optimized formulation (F2) were found to be 4.66±1.15 secs and 99.25±0.15%. The optimized formulation (F2) was subjected to stability studies (40 C& 75 % RH) for one month. The results were shown that natural super disintegrants require less disintegration time as compared to synthetic super disintegrants. Hence present study reveals that the orodispersible tablets prepared using Banana powder and Cassia tora powder is super disintegrants that shown better appearance and rapid disintegration time.

scholarly journals DEVELOPMENT, FORMULATION AND EVALUATION OF MECLOFENAMATE FAST DISSOLVING TABLETS

2021 ◽  
Vol 10 (1) ◽  
pp. 59-67
Author(s):  
Mahipal Shakkarwal ◽  
Dr. Mukesh Sharma ◽  
Dr. Ram Garg ◽  
Shankar Lal Soni ◽  
Gopal Kumar Paswan ◽  
...  
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation ◽  
Suitable Treatment ◽  
The Stability

The demands for fast dissolving tablets have received ever increasing day by day during the last 10-15 years for the onset of action. In the present study, the effect of superdisintegrant was compared with synthetic super disintegrants and other conventional super disintegrants in the of fast dissolving tablet formulation of Meclofenamate. Meclofenamate is an antihypertensive drug and in case of hypertension immediate treatment is required so the proposed investigation is totally based to provide the suitable treatment for hypertension. In the present work 9 formulations of Fast dissolving tablets of Cilnidipine were prepared by using Synthesized Co-proceed was evaluated and compiles with the official standards, parameters and specifications. Various formulations were prepared using four different superdisintegrant namely- kyron T-304, sodium starch glycolate, cross carmelose sodium with three concentrations (2%, 4%, 6%) by direct compression method. The blend was evaluated for pre-compression parameters like Angle of repose , bulk density , tapped density , and then tablet  evaluated post-compression parameters like thickness , drug content , hardness , weight variation  , wetting time , friability , disintegration time , dissolution time, drug release study. Formulation A8 showed the lowest disintegration time and in-vitro dissolution studies recorded that formulation A8 showed 98.64% drug release at the end of 3 minutes. The best formulations were also found to be stable and optimized formulations were subjected to the stability studies as per ICH guideline and standards.

scholarly journals Formulation, Evaluation and Optimization of Orodispersible Tablets of Naproxen sodium by using Superdisintegrant

2019 ◽  
Vol 9 (4-s) ◽  
pp. 462-468
Author(s):  
Mohd. Razi Ansari ◽  
Sumer Singh ◽  
M.A. Quazi ◽  
Yaasir Ahmed Ansari ◽  
Jameel Abbas
Keyword(s):  
Patient Compliance ◽  
Naproxen Sodium ◽  
Rapid Onset ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation

Among the different type of route of administration oral route for drug administration is most common route in which Orodispersible tablet is preferred for the patient which are unconscious, week or for immediate control. The tablet gets dispersed in mouth cavity without water, present study deals with formulation of Naproxen sodium mouth dissolving tablets using super disintegrants. Naproxen sodium is analgesic and NSAID, used for the treatment of pain and inflammation caused by different condition such as osteoarthritis, rheumatoid arthritis and menstrual cramps. However gastric discomfort caused by naproxen sodium result in poor patient compliance associated with it conventional doses form but now days Naproxen sodium MDTs produces rapid onset of action and minimise gastric discomfort associated with it. Thus improves patient compliance, enhance bioavailability and reduces the dose of drug. MDTs are formulated by direct compression method using super disintegrants in different proportion. The powder blend is subjected to pre-compression evaluation parameters like bulk density, true density, and tapped density and angle of repose. Formulations are evaluated for weight variation, hardness, wetting time, water absorption time, disintegration time. And in vitro dissolution studies and all formulations complies Pharmacopoeias standards. The tablets are evaluated and result compared for all five formulation the most efficacious super disintegrants for MTDs of Naproxen sodium as suggested by the dispersion time, disintegration time and drug dissolution profiles. Keywords: - MDT, Naproxen Sodium, crosscarmellose Sodium, Sodium starch glycolate, Cross-povidone.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING ORAL FILM OF ANTI-ALLERGIC DRUG

2018 ◽  
Vol 6 (3) ◽  
pp. 5-16 ◽  
Author(s):  
ABRAHAM LINKU ◽  
JOSEPH SIJIMOL
Keyword(s):  
Ex Vivo ◽  
Methyl Cellulose ◽  
Moisture Loss ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Permeation Study ◽  
Weight Variation

The aim of present work was the development of fast dissolving oral film of Loratadine to overcome the limitations of current routes of administration, to provide immediate action and increase the patient compliance. To improve the bioavailability of the drug, fast dissolving oral film were formulated using different grades of Hydroxy Propyl Methyl Cellulose(HPMC) and various plasticizers like Polyethylene Glycol(PEG) 400, glycerol, Propylene glycol(PG) by solvent casting method. The formulated films were evaluated for film thickness, surface pH, folding endurance, weight variation, % moisture loss, exvivo permeation study, tensile strength, % elongation, drug content uniformity, in vitro dissolution studies,in vitro disintegration test and in vivo study. The optimized formulation (F9) containing HPMC E5 and glycerol showed minimum disintegration time (10.5 s), highest in vitrodissolution (92.5%) and satisfactory stability. Ex vivo permeation study of optimized formulation showed a drug release of 80.6% within 10 min. The milk induced leucocytosis inrat proved that fast dissolving oral films of Loratadine produced a faster onset of action compared to the conventional tablets. These findings suggest that fast dissolving oral film of Loratadine could be potentially useful for treatment of allergy where quick onset of action is required.

scholarly journals Development and Optimization of Quinapril Fast Dissolving Oral Films

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
P. Vamsee Kumar ◽  
Y. Shravan Kumar
Keyword(s):  
In Vitro Dissolution ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Efficient Management ◽  
Weight Variation ◽  
Drug Polymer Interaction ◽  
Oral Films ◽  
Evaluation Parameters ◽  
Polymer Interaction

In current investigation an attempt has been made to formulate and evaluate Quinapril mouth dissolving films using HPMC 50cps, E5, E15 and in combination of Pullulan by Solvent evaporation method. Sodium starch glycolate acts as a super disintegrating agent and it is shown that as the concentration of the super disintegrates increases the disintegration time decreases. The films were evaluated for weight variation, surface pH, folding endurance, drug content, dissolving time, disintegration time, and in-vitro dissolution studies. Based on the evaluation parameters F17 was to be optimized formulation. The optimized film (F17) showed the more drug release i.e 99.40 ± 5.30% within 7 min, lowest in vitro disintegration time 10 sec. FTIR studies proved no drug polymer interaction takes place. These results revealed that fast dissolving films of Quinapril could be formulated for quick onset of action which is required in the efficient management of hypertension.

Formulation and Evaluation of Oro Dispersible Tablets of Ondansetron Hydrochloride by Direct Compression using Superdisintegrants

1970 ◽  
Vol 1 (1) ◽  
pp. 106-111
Author(s):  
Avani R. Gosai ◽  
Sanjay B. Patil ◽  
Krutika K. Sawant
Keyword(s):  
Mechanical Strength ◽  
Direct Compression ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Weight Variation ◽  
Ondansetron Hydrochloride ◽  
Dispersible Tablets ◽  
In Vitro Disintegration

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

scholarly journals CINNARIZINE LIQUID SOLID COMPACTS: PREPARATION EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 150
Author(s):  
Sreenivas Patro Sisinthy ◽  
Shubbaneswarei Selladurai
Keyword(s):  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Dsc Studies ◽  
Weight Variation ◽  
Drug Concentrations ◽  
R Value

Objective: The objective of this research was to formulate cinnarizine tablets using the liquid-solid compact technique to enhance its solubility and dissolution rate.Methods: Cinnarizine liquid-solid compacts were formulated using propylene glycol as the non-volatile solvent, Neusilin US2 as the carrier material, Aerosil 200 as the coating material and croscarmellose sodium as the disintegrant. The interaction between drug and excipients were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies. Different batches of liquid, solid compacts were prepared by using varying carrier-coating excipient ratio and different concentration of liquid medication. Flow parameters such as bulk density, tapped density, Carr’s Index, Hausner’s Ratio as well as an angle of repose were used to test the flowability of the powder blend. The liquid-solid compacts were produced by direct compression method and were evaluated for tests such as weight variation, drug content, hardness, thickness, friability, wetting time, disintegration time as well as the in vitro dissolution studies.Results: The results of the preformulation studies of liquisolid compacts showed acceptable flow properties. The results of FTIR and DSC studies showed that there is no drug-excipient interactions. The different R values and concentrations were found to have a marked effect on the dissolution profile. Formulations with higher carrier: coating ratio (R-value) and lower drug concentrations displayed a better dissolution profile. The percentage of drug release of F3 with an R-value of 20 and a drug concentration of 10% was found to be 88.11% when compared to the conventional marketed tablet which released only 44.07% at the end of 2 h.Conclusion: From this research, it is inferred that liquid-solid technique is a promising and effective approach that can be used to enhance the dissolution rate of cinnarizine.

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