DEVELOPMENT AND CHARACTERIZATION OF SUBLINGUAL FILM CONTAINING ROPINIROLE HYDROCHLORIDE

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (07) ◽  
pp. 33-42
Author(s):  
P. B. Patil ◽  
D. A. Patil ◽  
L. R. Zawar ◽  
B. Patil ◽  
G. B. Patil ◽  
...  

In the present work films of ropinirole hydrochloride were prepared by using polymers such as hydroxy propyl methyl cellulose (HPMC E-15) and polyethylene glycol (PEG-400) as plasticizers, by a solvent casting method, for treatment of Parkinson's disease. HPMC E-15 was used as film forming agent in the range of concentration 50 mg – 600 mg and PEG-400 was used as plasticizer in the range of concentration 0.3-1.0 ml for solvent casting method. the optimized concentration of film forming agent was 400 mg and plasticizer concentration was 0.7ml. By using optimized concentration, Ropinirole Hydrochloride mouth dissolving films (MDFs) were prepared by additionof other excipients. The formulated MDFs were evaluated for different physical characteristics like uniformity of weight, thickness, folding endurance, drug content uniformity, percentage elongation, and tensile strength, disintegration, in vitro drug release studies and provided agreeable results. The FTIR and DSC studies confirmed that no physicochemical interaction in between drug and excipients accured. Mouth dissolving film of Ropinirole Hydrochloride containing HPMC E-15 as polymer showed 97.66 % drug release at 30 min. Mouth dissolving films of ropinirole hydrochloride containing HPMC E-15 showed better tensile strength (70.56 ± 0.9 g/mm2), percentage elongation (33.33 ± 2.88 %), folding endurance (168± 2.081 numbers of folds), in vitro disintegration time (35± 3.511 sec.) and thickness (0.4± 0.17 mm).

Author(s):  
SHIFA SHAUKAT HAJU ◽  
SHEELA YADAV

Objective: Buccal drug delivery is the most suited route for local as well as systemic delivery of drugs. Cilnidipine is an L/N type dihydropyridine 4th generation calcium channel blocker (CCB), which decreases hypertension by blocking the N-type calcium channel to attenuate vascular sympathetic neurotransmission. It has high first-pass metabolism leading to low bioavailability. Hence the present research work was undertaken to formulate mucoadhesive buccal film of Cilnidipine with an objective to enhance therapeutic efficacy, bioavailability and was developed to administer into the unconscious and less-co-operative patients. Methods: Cilnidipine buccal films were prepared by a solvent-casting technique using various concentrations of mucoadhesive-polymers such as Hydroxyl propyl methylcellulose (HPMC) E15 and K4M and ethyl-cellulose as backing-layer, which acts like a patch providing unidirectional drug release. Prepared films were evaluated for their weight variation, thickness, surface-pH, swelling-index, drug content uniformity, in vitro residence time, folding endurance, tensile strength, in vitro release and permeability studies. Results: The infra-red (IR) spectra showed no interaction, and Physico-chemical characteristics were found within the limit. Swelling of the film increases with increasing concentration of polymers and %drug content of all formulations found to be in the range of 92.13%±0.94% to 97.92%±0.35%. The formulation F5, showed a promising tensile strength, folding endurance and in vitro drug release of about 95.18±0.03%, thus can be selected as an optimized formulation of mucoadhesive buccal film. Conclusion: The formulation of Cilnidipine mucoadhesive buccal film was found to be satisfactory and reasonable.


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):  
Dillip Kumar Behera ◽  
Kampal Mishra ◽  
Padmolochan Nayak

In this present work, chitosan (CS) crosslink with polyaniline (PANI) with montmorilonite (MMT) called as (CSPANI/MMT) and CS crosslink with PANI without MMT called as (CS-PANI) were prepared by employing the solution casting method. Further the formation of nanocomposites CS-PANI/MMT and CS-PANI were investigated using XRD, FTIR, SEM and tensile strength. Water uptake and swelling ratio of the CS-PANI and CS-PANI/MMT were found to decrease with increase in concentration of clay. Mechanical properties of the CS-PANI and CS-PANI/MMT were assessed in terms of tensile strength and extensibility using texture analyzer. Increase in tensile strength and reduction in extensibility was reported with increase in the nanoclay content. In vitro drug release study on CS-PANI and CS-PANI/MMT indicated pronounced sustained release of doxorubicin by the incorporation of clay particles in the CS polymer matrix. Overall CSPANI/MMT nanocomposite films exhibited improved mechanical and sustained drug release properties than CS-PANI.


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):  
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.


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.


2018 ◽  
Vol 10 (5) ◽  
pp. 235
Author(s):  
Haritha V. Anod ◽  
N. Vishal Gupta ◽  
D. V. Gowda ◽  
Manohar M.

Objective: The objective of the study was to prepare simvastatin transdermal films for the treatment of atherosclerosis and to evaluate the effect of concentration of polymer on penetration enhancement.Methods: Solvent evaporation technique was employed for the preparation of films and the prepared films were evaluated for various physicochemical properties of films such as tensile strength, thickness, surface pH, swellability, drug content, moisture content and folding endurance. In vitro drug, release study and release kinetics were also studied.Results: Tensile strength ranged from 3.56±0.343 to 4.56±0.12 (N/mm²). The films were of uniform weight. Thickness varied from 0.2±0.3 mm to 0.2±0.8 mm. Surface pH ranged from 6.6±0.14 to 6.9±0.16. Percentage swellability ranged from12.1±0.36 to 16.3±0.22. Percentage drug content ranged from 88.4±0.7% to 90.5±0.6% in all the formulation. Percentage moisture content ranged from 0.864 to 1.03%. Moisture uptake was from 2.6±0.24 to 2.9±0.072. The folding endurance test gave satisfactory results and F3 formulation showed maximum drug release.Conclusion: From the study, it was concluded that out of various formulations, the F3 formulation was found to be the optimum formulation with 88% drug release at the fourteenth hour.Keywords: Simvastatin, Transdermal film, Solvent evaporation, Penetration enhancer, Swellability


Author(s):  
Hir. R. Mehta ◽  
Vijay K. Patel

The present invention was aimed to formulate and evaluate Lafutidine gastro retentive films. The films were prepared by solvent casting technique using different film forming polymers like HPMC and Ethyl cellulose. PEG 400 used as a plastsizer. The prepared films were evaluated for number of parameters like Physical appearance, Weight variation, Thickness, Folding endurance, Tensile strength, unfolding behavior, floating properties, drug content and In vitro drug release studies. From the trial batches the best release for gastroretentive film was shown by formulation T5 (Ethyl cellulose and PEG 400). Formulation T5 exhibited good appearance, better mechanical strength with acceptable flexibility. Also, formulation T5 was given more than 90 % drug released after 12 hr and 97.56 % Drug content.  For optimization of formulation, 32 factorial design was applied by taking Ethyl cellulose and PEG 400 as an independent variables. Drug release at 8 hour and folding endurance selected as dependent variables. Based on drug release study, L8 batch found most satisfactory in all formulation and the effect of Ethyl cellulose and PEG 400 found significant. L8 batch found stable during stability study. Key words: Lafutidine, Floating Films, Ethyl Cellulose.


Author(s):  
ZANKAHANA PATEL ◽  
RAHIL BHURA ◽  
SAMIR SHAH

Objective: Ramosetron Hydrochloride is found to be more potent and having a longer duration of action with the least side effects, but the major drawback is it undergoes hepatic first-pass metabolism so our aim is to prepare mouth dissolving film (MDF) of Ramosetron hydrochloride for rapid relief in emesis. Methods: The mouth dissolving films of Ramosetron Hydrochloride were prepared by using the solvent casting method. Films were formulated using HPMC E5 (Hydroxy Propyl Methyl Cellulose) as a film-forming agent, PEG400 (Polyethylene glycol) as a plasticizer and Aspartame as the sweetening agent. A 32 full factorial design was applied considering the concentration of HPMC E5 (X1) and concentration of PEG400 (X2) as independent variables and % cumulative drug release (Y1) (CDR), disintegration time (Y2) (DT) and tensile strength (Y3) (TS) as dependent variables. The prepared films were evaluated for thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and taste masking by E-tongue. The results indicated that factors X1 and X2 were found to be having a positive effect on DT and TS and negative effects on CDR. Results: The optimized formulation was found to be the best with 94.00±0.85% in vitro drug release, 33.22±0.75 sec DT and 1.359±0.005 g/mm2 tensile strength. Concentration of aspartame was optimized with E-tongue taking into consideration increased electric potential with decreasing bitterness. Conclusion: Thus, a rapidly dissolving oral film of Ramosetron Hydrochloride with successful taste masking and immediate in vitro drug release was prepared using a solvent casting technique.


INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (06) ◽  
pp. 23-30
Author(s):  
S. Patha ◽  
◽  
P. Dara ◽  
S. K Yamsani ◽  
R Thadkapally ◽  
...  

The objective of the present study was to develop a sustained release once a day oral elementary osmotic tablet for ropinirole hydrochloride and evaluate its in vivo performance. The core of elementary osmotic tablet of ropinirole hydrochloride was prepared by compression of mixture consisting of drug,different concentrations of osmogens, and other tablet material. Core tablets were then coated with different concentrations of cellulose acetate and PEG-400. FTIR was used to identify if the excipients are compatible with the drug. All the tablets that were prepared were evaluated for drug release and based on the results an optimum and ideal osmotic pump composition with a zero-order drug release extended for 24 h was proposed and this was considered the optimized formulation. Surface morphology of coated formulation was studied by scanning electron microscopy. The drug release was determined in different pH media and different agitation speeds. The pharmacokinetics of the drug after oral administration of optimized osmotic pump was investigated in rabbits and the data were compared with that of a conventional tablet. In vitro in vivo correlation was determined for the optimized formulation. A suitable and simple sustained release elementary osmotic pump for ropinirole hydrochloride was developed. The release rate was independent of the pH of the dissolution medium and the agitation speeds. In vivo studies with optimized osmotic tablet formulation demonstrated that drug concentration in plasma was maintained for prolonged period and minimized fluctuation. A better in vitro in vivo correlation was achieved with the osmotic tablet. A simple once a day elementary osmotic tablet is feasible for ropinirole hydrochloride.


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