scholarly journals FORMULATION DEVELOPMENT OF ORAL FAST-DISSOLVING FILMS OF RUPATADINE FUMARATE

2020 ◽  
pp. 67-72
Author(s):  
ABHIBRATA ROY ◽  
REEGAN AREES ◽  
MADHAVI BLR
Keyword(s):  
Drug Release ◽  
Inclusion Complex ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Solvent Casting ◽  
Formulation Development ◽  
Casting Method ◽  
Disintegration Time ◽  
Low Viscosity

Objective: Rupatadine fumarate (RF) is an anti-allergic drug indicated for the treatment of allergic rhinitis. It has low oral bioavailability due to its poor aqueous solubility and extensive hepatic first pass metabolism. In the present work, oral fast-dissolving films (OFDF) have been formulated and evaluated to facilitate dissolution in the oral cavity itself. Methods: Pullulan and HPMC (5, 15 cps) were employed as film formers and six formulations were tried. The physicochemical compatibility between drug and the polymers was studied by FTIR spectroscopy. RF-beta-cyclodextrin (BCD) inclusion complex was initially prepared and evaluated. The inclusion complex was incorporated into the film. OFDF were formulated and prepared by solvent casting method. The film size for one dose was 2 × 2 cm. The films were evaluated for various film parameters including disintegration time and drug release. Results: Preliminary film studies indicated % of film former solution to be between 3 and 5% for good appearance, mechanical strength, and quick disintegration. Solubility enhancement of RF is almost 40-fold from its BCD inclusion complex. Drug content in the films ranged between 83 and 90%. The pH ranged between 6 and 7 for all the formulations. All OFDF of RF disintegrated within one minute. With higher viscosity grade of HPMC, disintegration was comparatively slower and so was the drug release. Pullulan based films also showed desirable properties. F3 had disintegration time was 28 s and % drug release was 92% in 180 s. Conclusion: OFDF of RF could be formulated employing pullulan and HPMC low viscosity grades by solvent casting method. F3 containing HPMC E5 at 37% by weight of dry film showed desirable film properties. Stability studies indicated that there was no significant change in the films with respect to physicochemical properties and in vitro release.

scholarly journals Formulation Development and Evaluation of Fast Dissolving Oral Film of Midodrine Hydrochloride

2020 ◽  
Vol 10 (3-s) ◽  
pp. 107-110
Author(s):  
Aashish Marskole ◽  
Sailesh Kumar Ghatuary ◽  
Abhishek Parwari ◽  
Geeta Parkhe
Keyword(s):  
Systemic Circulation ◽  
In Vitro Dissolution ◽  
Systemic Availability ◽  
Solvent Casting ◽  
Formulation Development ◽  
Casting Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Dissolution Tests

Oral fast dissolving midodrine hydrochloride films prepared by solvent casting method, PEG 400 was the selected plasticizers, incorporating superdisintegrants such as croscarmellose sodium (CCS) and sodium starch glycolate (SSG) to achieve the goal. Drug content, weight variability, film thickness, disintegration time, endurance, percentage of moisture content, and in vitro dissolution tests were analyzed for the prepared films. In all formulations, the tensile strength value was found from 0.965±0.045 and 1.256±0.032 and the folding capacity was over 100. The assay values ranged from 97.98±0.25 to 99.89±0.36 percent for all formulations. The disintegration time was ranging between 55±9 to 120±6 sec, the minimum time for disintegration was found in formulation F5 (55±9). The prepared F5 formulation shows greater release of the drug (99.25±0.41 percent) within 15 min relative to other formulations. As the drug having low solubility, fast disintegration may leads to more drug availability for dissolution, resulting in faster absorption in systemic circulation increased systemic availability of drug leads to quick onset of action which is prerequisite for hypertension. Keywords: Midodrine hydrochloride, Fast dissolving films, Solvent casting method, Superdisintegrants.

Resveratrol Nanocrystal Loaded Orodispersible Films: Formulation Development and In Vitro Characterization

2021 ◽  
Author(s):  
Samet Ozdemir ◽  
Burcu Uner ◽  
Alptug Karakucuk
Keyword(s):  
Physical Stability ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Formulation Development ◽  
Disintegration Time ◽  
Orodispersible Films ◽  
Antisolvent Precipitation ◽  
In Vitro Characterization ◽  
Poorly Soluble

Abstract Nanocrystals are a feasible system to improve the aqueous solubility of poorly soluble compounds. Orodispersible films (ODFs) offer a rapid release of the drug in the mouth and are preferred for patients with dysphagia or paediatrics. The objective of the current study was to develop resveratrol (RES) nanocrystal-loaded ODFs. RES nanocrystals were prepared by antisolvent precipitation in the existence of Poloxamer 188 as a polymeric stabilizer. Polyvinyl alcohol was used for the preparation of the ODFs by using the solvent casting method. Then, RES nanocrystals were incorporated into the films. Particle size (PS), polydispersity index (PDI), and zeta potential (ZP) values were measured for nanocrystals. ODFs were characterized, and bioadhesion, disintegration, and in vitro release studies were performed. RES nanocrystals were obtained with 631 nm PS, 0.314 PDI and − 14.3 ZP values. Over 90% of RES nanocrystals were loaded in ODFs, which were approximately 75 µm in thickness. The thermal and crystal properties of nanocrystals in ODFs were preserved regarding DSC and FTIR analyses. Homogenous distribution in smooth films was observed on SEM. Mechanical properties and bioadhesion forces were found to be appropriate for ODFs. The disintegration time was found below 30 seconds for nanocrystal loaded films. RES nanocrystal loaded film formulations showed > 85% release in 5 minutes, significantly higher (p < 0.05) than those prepared with coarse RES. Novel RES nanocrystal-loaded ODFs can be a promising delivery system for use as an antioxidant with improved patient compliance by increasing solubility and physical stability of RES.

Formulation and Evaluation of Transdermal patch of Methimazole

2021 ◽  
pp. 4667-4672
Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Patch ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Percent Moisture ◽  
Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING FILMS OF ELETRIPTAN HYDROBROMIDE

2017 ◽  
Vol 9 (2) ◽  
pp. 59
Author(s):  
K. Pallavi ◽  
T. Pallavi
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Guar Gum ◽  
Methyl Cellulose ◽  
Synthetic Polymers ◽  
Locust Bean Gum ◽  
Solvent Casting ◽  
Casting Method ◽  
Disintegration Time ◽  
Locust Bean

Objective: The main aim of the present research was to develop an oral fast dissolving polymeric film (FDF) with good mechanical properties, faster disintegration and dissolution when placed on the tongue.Methods: Eletriptan hydrobromide is prescribed for the treatment of mild to a moderate migraine. The polymers selected for preparing films were Pullulan, Maltodextrin (MDX), Acacia, Sodium alginate (SA), Locust bean gum (LBG), Guar gum (GG), Xanthan gum (XG), Polyvinyl alcohol (PVA), Polyvinyl pyrrolidine (PVP), Hydroxyl propyl methyl cellulose (HPMC) E5, and HPMC E15. Twelve sets of films FN1–FN12 were prepared by solvent casting method with Pullulan and combination of Acacia, MDX, SA, LBG, GG, XG, PVA, PVP, HPMC E5 and HPMC E15. Five sets of films FS1–FS5 were prepared using synthetic polymers like PVA, PVP, HPMC E5 and HPMC E15.Results: From all the prepared polymer formulations, FN2, FN8, and FS3 were selected based on disintegration time, and drug release and amongst this three FN2 was optimised based on its disintegration time (D. T). The percent drug release of the optimised film was compared with the percent release of the pure drug.Conclusion: The optimised formulation had a D. T of 16 s and a percent drug release of 97.5% in 10 min in pH 6.8 phosphate buffer and 100.6% drug release in 10 min in 0.1N HCl.

scholarly journals Formulation Development and Evaluation of Mouth Dissolving Tablet of Aspirin by Using QbD Approach

2021 ◽  
Vol 20 (1) ◽  
pp. 19-29
Author(s):  
Nilima A Thombre ◽  
Pradeep S Ahire ◽  
Sanjay J Kshirsagar
Keyword(s):  
Drug Release ◽  
Quality By Design ◽  
Formulation Development ◽  
Compression Method ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Design Expert ◽  
32 Factorial Design ◽  
Mouth Dissolving Tablet

In the current investigations, mouth dissolving tablets (MDT) were developed by applying quality by design (QbD) approach. Direct compression method was applied for the preparation of MDT containing aspirin using 32 factorial design with quantity of drug, microcrystalline cellulose (MCC) and crosscarmellose sodium (CCS) as dependant variables. MCC and CCS were used as superdisintegrants. Sodium stearyl fumarate was used as lubricant. Developed MDT were evaluated for characteristics like hardness, friability, disintegration time (DT) and in vitro drug release . Design Expert 11.0 described adequately impact of selected variables (MCC and CCS) at various levels for response under study (DT and friability). The optimized batch showed disintegration time of 15-28 secs, friability within 1% and in vitro drug release of 75-98% after 30 mins, respectively. The present study of experimental design revealed that MCC and CCS are fruitful at low concentration to develop the optimized formulation. As per the results obtained from the experiments, it can be concluded that QbD is an effective and efficient approach for the development of quality into MDT with the application of QTPP, risk assessment and critical quality attributes (CQA). Dhaka Univ. J. Pharm. Sci. 20(1): 19-29, 2021 (June)

scholarly journals ENHANCEMENT OF SOLUBILITY AND OPTIMIZATION OF ORALLY DISINTEGRATING FILMS OF ACYCLOVIR

2018 ◽  
Vol 11 (9) ◽  
pp. 280 ◽  
Author(s):  
Bikash Pandey ◽  
Arshad Bashir Khan
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Antiviral Agent ◽  
Disintegration Time ◽  
Casting Technique ◽  
Accelerated Stability ◽  
Full Factorial

Objective: The objective of this work was to prepare and optimize orally disintegrating films of acyclovir (ACV), which is a known antiviral agent. To enhance the solubility of ACV, solid dispersions of ACV were made.Methods: The films were prepared using a solvent casting technique. Full factorial design was utilized for the optimization of the effect of independent variables such as the amount of hydroxypropyl methylcellulose 5 cps, sodium starch glycolate, and propylene glycol on the disintegration time. Other evaluation tests such as drug release, drug content, thickness, and folding endurance of film were also conducted.Results: Compatibility studies by Fourier transform infrared showed that there was no significant interaction between the drug and excipients used. Disintegration time was found to be 43 s for the optimized batch. The in vitro release profile of formulation response disintegrating time in phosphate buffer pH 6.8 revealed that there was a significant increment in drug release of the optimized batch in comparison to the screening batches. Further, short-term accelerated stability studies carried out for 4 weeks for the optimized formulation which proved that the formulated films were stable at the accelerated conditions of temperature and humidity (40±2°C/75±5% RH).Conclusions: It was concluded that such ACV solid dispersion films could be beneficial in enhancement of dissolution and consequently the oral bioavailability of ACV.

scholarly journals In vitro Studies on Sustained Release Suppository Formulations of Tiaprofenic Acid with Sucrose Fattv Acid Ester

2003 ◽  
Vol 71 (4) ◽  
pp. 357-364
Author(s):  
Sevgi Gūngör ◽  
Mine Orlu ◽  
Yildiz Özsoy ◽  
Ahmet Araman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Tiaprofenic Acid ◽  
In Vitro Release ◽  
Content Uniformity ◽  
Sugar Ester ◽  
Disintegration Time ◽  
Suppository Base ◽  
Vitro Release

The objective of this study was to evaluate the performance of Sucro Ester 7 (sucrose distearate) as additive for preparing sustained release suppositories of tiaprofenic acid. Suppocire AIM (semi-synthetic glycerides) was used as suppository base and formulations were prepared containing different ratios of sugar ester: Suppocire AIM. Content uniformity, disintegration time and in vitro release characteristics of suppositories were investigated. Significant decrease in the extent of drug release was observed with the increase in the content of sugar ester, which was due to the longer disintegration time of suppositories.

scholarly journals Development and Optimization of Fast Dissolving Oral Film Containing Aripiprazole

2017 ◽  
Vol 9 (06) ◽  
Author(s):  
S. Jyothi Sri ◽  
D.V. R.N Bhikshapathi
Keyword(s):  
Good Alternative ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Solvent Casting ◽  
Casting Method ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Folding Endurance ◽  
Oral Films

The present investigation was aimed with the objective of developing fast dissolving oral films of Aripiprazole to attain quick onset of action for the better management of Schizophrenia. Fourteen formulations (F1-F14) of Aripiprazole mouth dissolving films by solvent-casting method using HPMC E5, HPMC E15, Maltodextrin, PG and PVA. Formulations were evaluated for their physical characteristics, thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and drug release characteristics and found to be within the limits. Among the prepared formulations F13 showed minimum disintegration time 10 sec, maximum drug was released i.e. 99.49 ± 0.36% of drug within 8 min when compared to the other formulations and finalized as optimized formulation. FTIR data revealed that no interactions take place between the drug and polymers used in the optimized formulation. The in vitro dissolution profiles of marketed product and optimized formulation was compared and found to be the drug released was 20.73 ± 0.25 after 8 min. Therefore, it can be a good alternative to conventional Aripiprazole for immediate action. In vitro evaluation of the Aripiprazole fast dissolving oral films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Aripiprazole. The mouth dissolving film is potentially useful for the treatment of Schizophrenia where the quick onset of action is desired.

scholarly journals Formulation development and evaluation of Luliconazole Topical Emulgel

2021 ◽  
pp. 79-87
Author(s):  
Naga sai divya K ◽  
T Malyadri ◽  
Ch.saibabu
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Formulation Development ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Zero Order Kinetics ◽  
Diffusion Controlled ◽  
Carbopol 940 ◽  
Vitro Release

The purpose of the present study was to develop and optimize the emulgel system for Luliconazole using different types of gelling agents: HPMCK15M, Carbopol 940, and Xanthan Gum. The prepared emulgels were evaluated in terms of appearance, pH, spreadability, viscosity, drug content, and in-vitro drug release. In-vitro release study demonstrated diffusion-controlled release of Luliconazole from formulation up to 12 hours. The drug release profile exhibited zero-order kinetics. All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and higher drug release. In the case of all evaluation parameters, carbopol based formulation showed better properties so, as a general conclusion, it was suggested that the Luliconazole emulgel formulation prepared with carbopol (F6) was the formula of choice.

scholarly journals Formulation Development and Evaluation of Liposphere of Poor Water Soluble Drug for Hyperlipidemia

2021 ◽  
Vol 11 (2) ◽  
pp. 23-30
Author(s):  
Anil Kumar ◽  
Umesh K. Jain ◽  
Ajay Patel
Keyword(s):  
Drug Release ◽  
Stearic Acid ◽  
Aqueous Solubility ◽  
Class Ii ◽  
Water Soluble ◽  
Fibric Acid Derivative ◽  
Formulation Development ◽  
Bcs Class Ii ◽  
Paraffin Oil

Lipospheres offer a new approach to improve an aqueous solubility of BCS class-II drugs. Simvastatin is a third generation fibric acid derivative belonging to this class, employed clinically as a hypolipidemic agent to lessen the risk caused by atherosclerosis. An attempt was made to improve aqueous solubility of Simvastatin by aid of stearic acid and Paraffin oil. The factorial batches of the Simvastatin lipospheres were formulated by melt dispersion technique using 32 factorial design with variables X1- concentration of stearic acid and X2- concentration of paraffin oil and responses Y1 - % Drug Entrapment (% DE) and Y2 - % Drug Release (% DR). From the surface response graphs the optimized batch was formulated and evaluated for saturation solubility, in-vitro drug release studies. Significant improvement in the aqueous solubility of the drug in the Simvastatin lipospheres supports the applicability of lipospheres as a tool for improving aqueous solubility of the BCS class-II drugs. Keywords: Linospheres; Simvastatin; Drug release; Hyperlipidemic; Drug entrapment.

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