scholarly journals Overcoming Poor Solubility of Dimenhydrinate: Development, Optimization and Evaluation of Fast Dissolving Oral Film

2018 ◽  
Vol 8 (4) ◽  
pp. 721-725 ◽  
Author(s):  
Yuvraj Govindrao Jadhav ◽  
Upendra Chandrakant Galgatte ◽  
Pravin Digambar Chaudhari

Purpose: To develop fast dissolving oral film to address vomiting and nausea in pediatric population. Methods: Oral films of Dimenhydrinate were prepared by solvent casting method by using hydroxypropylmethyl cellulose E5 (HPMC E5), polyethylene glycol 400 (PEG 400) and croscarmellose sodium. Solubility of dimenhydrinate was enhanced by ethanol as a co-solvent. To make dimenhydrinate palatable sodium saccharin and peppermint oil were used. All films were evaluated for mechanical parameters, surface pH, morphology, disintegration time and percent dissolution. Results: Films were smooth, acceptable and white in colour. For optimized batch, drug content (99.106%), disintegration time (25 sec), dissolution (99.10% in 210 sec), surface pH (6.81) were acceptable. Conclusion: Optimized batch, due to its potential to deliver through fast dissolving film, can be developed for clinical use.

Author(s):  
S. Jyothi Sri ◽  
D.V. R.N Bhikshapathi

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.


Author(s):  
Sudhakar Kancharla ◽  
Prachetha Kolli ◽  
Dr.K.Venkata Gopaiah

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.


2019 ◽  
Vol 9 (4-A) ◽  
pp. 122-125
Author(s):  
Yadagiri Phalguna ◽  
Haritha Pasupulati ◽  
Sandhya Rudra

The predominant goal of this work is to formulate and evaluate Cetirizine HCl ODF’s the usage of Sodium starch glycolate (SSG) as superdisintegrant, Sodium alginate as polymer and Glycerol as plasticizer. Films were prepared by way of Solvent casting method and evaluated for thickness, folding endurance, percentage elongation, floor pH and disintegration time. The consequences indicate that method prepared with 17.5% combo of polymer and plasticizer was determined to be optimized. The three special formulations F1, F2 and F3 of CTZ motion pictures were organized via solvent casting technique the usage of sodium alginate as polymer, SSG as disintegrant and glycerol as plasticizer. Menthol was once used as cooling agent along with aspartame as sweetener and citric acid as a style overlaying agent. The formulation (F3) with presence of superdisintegrant and combo of polymer, plasticizer confirmed first-rate results. Keywords: Cetirizine HCl, Oral thin film, superdisintegrant, polymer, plasticizer


Author(s):  
SHUBHAM BIYANI ◽  
SARANG MALGIRWAR ◽  
RAJESHWAR KSHIRSAGAR ◽  
SAGAR KOTHAWADE

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.


Author(s):  
K. Pallavi ◽  
T. Pallavi

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.


Author(s):  
ABHIBRATA ROY ◽  
REEGAN AREES ◽  
MADHAVI BLR

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.


2020 ◽  
Vol 10 (3-s) ◽  
pp. 107-110
Author(s):  
Aashish Marskole ◽  
Sailesh Kumar Ghatuary ◽  
Abhishek Parwari ◽  
Geeta Parkhe

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.


INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (09) ◽  
pp. 34-41
Author(s):  
M. R Andrea ◽  
◽  
P. M. Dandagi ◽  
A. P. Gadad

The aim of the present study was to develop a fast dissolving buccal film of dimenhydrinate with good mechanical properties and fast disintegration, producing an acceptable taste when placed in the mouth. The formulations were developed by solvent casting method by using HPMC E5 and HPMC E15 as film formers in different concentrations, propylene glycol as plasticizer and Poloxamer 407 as solubiliser. The resultant films were evaluated for various parameters. the films were found to be satisfactory for all the parameters. All formulations released more than 85% of the drug within 15 minutes. Formulation F7 (1% HPMC E5: 1% HPMC E15) was selected as the optimized formulation based upon the least disintegration time (24.3sec), optimum mechanical properties, percentage drug content (94.96%) and in vitro drug release (95.20%). The ex vivo release was found to be acceptable. Stability studies revealed that the formulation was stable on storage for two months.


2019 ◽  
Vol 819 ◽  
pp. 51-56
Author(s):  
Wipada Samprasit ◽  
Benchawan Chamsai ◽  
Praneet Opanasopit

Polymethacrylates polymeric film formation in patches containing α-mangostin and resveratrol were developed using solvent casting method. Eudragit® E100 (E) and Eudragit® L100 (L) were dissolved in ethanol and the plasticizer (propylene glycol (PG) and polyethylene glycol (PEG) 400) was individual added and followed with the drying process. The dried films were evaluated for the morphology and flexibility. After the stable film was achieved, the α-mangostin and resveratrol were incorporated into the film. The variation of weight and thickness, swelling property, pH surface, mechanical properties and drug content of patches was evaluated. Fourier transform infrared spectrophotometry (FT-IR) was also conducted to confirm that drugs were qualitatively loaded into the patches. The results indicated that patch of L and PG was found to be stable. PG enhanced the flexibility of patch. The patches were less variation in weight and thickness. This patch did not effect to the physiological pH in the human body. In addition, patch had a tensile strength high enough to withstand tearing during handing. The qualitative and quantitative analysis indicated the α-mangostin and resveratrol was well incorporated in this patch. These results suggest that polymethacrylate polymer could be a promising polymeric film formation in patches for drug delivery.


Sign in / Sign up

Export Citation Format

Share Document