DESIGN DEVELOPMENT AND EVALUATION OF FAST DISSOLVING ORAL FILMS OF RANITIDINE HYDROCHLORIDE

INDIAN DRUGS ◽  
2014 ◽  
Vol 51 (06) ◽  
pp. 27-36
Author(s):  
B.V. Ramana ◽  
◽  
C Triveni ◽  
G Nagarajan ◽  
T.E.G.K. Murthy
Keyword(s):  
Polyvinyl Alcohol ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Design Development ◽  
Drug Release Profile ◽  
Film Forming ◽  
Film Formulation ◽  
Oral Films

The aim of this study was to develop an innovative fast dissolving oral film of Ranitidine HCl based on polymers such as Hydroxy Propyl Methyl Cellulose-E6, Hypromellose-E3 LV, and Polyvinyl alcohol. Trials on various concentrations of polymers were conducted in order to optimize polymer concentration and develop the films with best suitability and acceptability. The various concentrations of super disintegrating agents like Crospovidone, Croscarmellose sodium and Sodium Starch Glycolate were evaluated. The fast dissolving oral films were characterized for weight, thickness, folding endurance, disintegration and dissolution using in vitro experimentations. The effect of super disintegrating agents on drug release profile and film forming properties was investigated. The prepared films exhibited satisfactory physicochemical characteristics. Finally, it is concluded that Ranitidine can be formulated with Hydroxy Propyl Methyl Cellulose-E6, Hypromellose-E3 LV, and Polyvinyl Alcohol polymers to achieve oral film formulation by using solvent casting method.

FORMULATION AND EVALUATION OF FAST DISSOLVING ORAL FILMS OF PROCHLORPERAZINE MALEATE

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (12) ◽  
pp. 23-33
Author(s):  
R. Kanekar ◽  
◽  
P. M. Dandagi ◽  
A. P. Gadad
Keyword(s):  
Ex Vivo ◽  
Rapid Onset ◽  
Drug Release Profile ◽  
Onset Of Action ◽  
In Vitro Drug Release ◽  
Physico Chemical ◽  
Film Forming ◽  
Oral Films ◽  
Ex Vivo Study

The objective of the present study was to prepare and evaluate fast-dissolving oral films of prochlorperazine maleate (PCM), in order to enhance the bioavailability of the drug and to provide rapid onset of action thereby improving patient compliance. The solubility of the drug was increased by preparing inclusion complex with 2-hydroxypropyl-β-cyclodextrin (2HPβCD) and then incorporating it into the fast dissolving films. The fast-dissolving films of PCM were prepared by solvent casting method using different film forming polymers such as HPMC E15 and HPMC E5, either as single polymer or combination of the two. The film formulations were evaluated for various physico-chemical parameters. All formulations released more than 85% of the drug within 15 minutes. Formulation F4 showed best in vitro drug release profile. From the ex vivo study it was found that 94.79% of drug permeated through the porcine oral mucosa from the optimized formulation F4 within 60 mins.

scholarly journals Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

2021 ◽  
Vol 4 (2) ◽  
pp. 99-109
Author(s):  
Priyanka Singh ◽  
Amit Kumar Shrivastava ◽  
Sachin Kumar ◽  
Manish Dhar Dwivedi
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Study Results

This study aimed to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets were prepared by direct compression method, using hydrophilic polymers (HPMC/guar gum). Matrix tablets were prepared by wet granulation method using different hydrophilic polymers (HPMC/guar gum). Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 6.8 (without enzymes). The thickness and hardness of prepared tablets were 3.23 ± 0.035 to 3.28 ± 0.008 mm and 3.26 ± 0.115 to 3.60 ± 0.200 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopoeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. Drug release was retarded with an increase in polymer concentration due to the gelling property of polymers. The in vitro drug release from the proposed system was best explained by Higuchi’s model, indicating that drug release from tablets displayed a diffusion-controlled mechanism. The results clearly indicate that guar gum could be a potential hydrophilic carrier in developing oral controlled drug delivery systems. Based on the study results, formulations F8 was selected as the best formulation.

COMPARATIVE EVALUATION OF POLYMER COMBINATION IN THE DESIGN OF BRIMONIDINE TARTRATE OCULAR INSERTS

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (07) ◽  
pp. 30-35
Author(s):  
P Goudanavar ◽  
◽  
N Ambhore ◽  
D. Hiremath ◽  
R Udupi
Keyword(s):  
Polymer Concentration ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Carboxymethyl Chitosan ◽  
Moisture Loss ◽  
In Vivo Release ◽  
Weight Variation ◽  
Brimonidine Tartrate

Brimonidine is an anti-glaucoma agent useful in treatment of intraocular pressure. In the present study an attempt was made to formulate ophthalmic inserts of brimonidine tartrate (BT) in combination with polymers like methylcellulose, carboxymethyl chitosan and HPMC. Prepared ocular films were evaluated for uniformity in thickness, weight variation, % moisture absorption, % moisture loss, in vitro and in vivo release studies. The physical characteristics of the films were found to be within acceptable limits. The study confirmed that brimonidine tartrate can be delivered through films made of methyl cellulose, carboxymethyl chitosan and HPMC combination matrix cast with ethyl cellulose (EC). In vitro release study revealed that increasing the proportion of polymer concentration decreased the rate of release of brimonidine tartrate. In vivo release profile of ocular inserts revealed controlled release of drug over a period of 24 h. Optimized formulation CH3 was evaluated for in vivo release characteristics using rabbits as animal model. The optimized formulation CH3 was found to be stable at accelerated storage condition of 40/75 % RH.

scholarly journals Formulation and Evaluation of Colchicine Sustained release tablet by using factorial designs

2021 ◽  
Vol 11 (5-S) ◽  
pp. 100-107
Author(s):  
M. Pradeep Kumar ◽  
Goparaju Suryanarayana Murthy ◽  
Annamdasu Lakshmi Poojitha ◽  
P. Sindhuri ◽  
A Sreekanth ◽  
...  
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Similarity Factor ◽  
Time Required ◽  
Full Factorial

The study on the effect of polymer concentration on in vitro drug release profile revealed that there is a change in vitro drug release parameters (t50, t80, and MDT) with a change in polymer concentration. Fraction of HPMC K4M, HPMC K 100 M, and Ethyl Cellulose were required to be 15, 10, and 7 mg respectively for designing optimized batch F7. The release rate of Colchicine decreased proportionally with an increase in the concentration of ethyl Cellulose and HPMC K100 M. Also the high amount of HPMC K4M leads to the less initial release and sustain effect. A theoretical drug release profile was generated using pharmacokinetic parameters of Colchicine. The value of t50 and t80 of theoretical drug release profile was found to be 242 min and 529 min respectively. The similarity factor f2 was applied between the in vitro drug release profile of optimizing batches and theoretical profile, which indicate a decent similarity between all in vitro drug release profiles (f2 = 68.28 for F7). All the batches except F1shows the value of f2 value within a range. Batch F7 showed the highest f2 (f2 = 68.28) among all the batches and this similarity was also reflected in t50 (≈ 256 min) and t80 (≈ 554 min) values. A 23 full factorial design was applied to systemically optimize in vitro drug release profile. The HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) were selected as independent variables. The time required for 50% drug released (t50), the time required for 80% drug release (t80), similarity factor f2, and mean dissolution time (MDT) were selected as dependent variables. The results of full factorial design indicate that the HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) have a significant effect on in vitro drug release profile. To find out the release mechanism the in vitro release data were fitted in the Korsmeyer-Peppas equation. All Batches except F1 and F3 show Anomalous diffusion-controlled release (combined mechanism of diffusion and case II transport).  

scholarly journals PLGA NANOPARTICLES LOADED MUCOADHESIVE AND THERMOSENSITIVE HYDROGEL AS A POTENTIAL PLATFORM FOR THE TREATMENT OF ORAL MUCOSITIS

2019 ◽  
Vol 11 (1) ◽  
pp. 106
Author(s):  
Gina S. El-feky ◽  
Gamal M. Zayed
Keyword(s):  
Oral Mucositis ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Plga Nanoparticles ◽  
Complete Healing ◽  
Drug Release Profile ◽  
Thermosensitive Hydrogel ◽  
Hydrogel Matrix

Objective: The objective of this study was to design an effective topical treatment for oral mucositis.Methods: Poly-(DL-lactide-co-glycolide) (PLGA) nanoparticles (NPs) and Poloxamer407 (PLX)/Hydroxy propyl methyl cellulose (HPMC) hydrogel matrix (HG) were used as combined carriers for benzydamine HCL (BNZ). BNZ loaded PLGA nanoparticles were assessed for their particle size, PDI, zeta potential and entrapment efficiency. Scanning electron microscopy, thermosensitivity study, mucoadhesion study, in vitro release and in vivo investigation were used to characterize the combined BZN loaded PLGA NPs HG.Results: Negatively charged NPs with an average diameter of 139±4.92 nm were incorporated into PLX/HPMC HG bases. The gelation temperature of BZN-PLGA-NPs-HGs ranged between 31°C and 36.5°C. When diluted with saliva simulated fluid, BZN-PLGA-NPs-HGs preserved their gelation properties. Mucoadhesion was found lower for formulations prepared with PLX without HPMC. An increase in the concentrations of PLX from 10 to 30% resulted in an increase in adhesion. Both PLGA-NPs and PLGA-NPs-HG provided a biphasic drug release profile while BZN-HG provided monophasic zero order release pattern. The in vivo study showed that animal groups treated with BZN-HG and BZN-PLGA-NPs-HG showed a significantly higher reduction percentage in ulcer surface area compared to those treated with BZN-PLGA-NPs. BZN-PLGA-NPs-HG group needed 10 d of treatment to complete healing versus 16 d, 14 d and 12 d for the complete healing of groups with no treatment, treated with BZN-PLGA-NPs and treated with BZN-HG, respectively.Conclusion: BZN-PLGA-NPs-HG could represent a promising mean for the effective treatment of oral mucositis induced by cancer therapy.

scholarly journals FORMULATION AND EVALUATION OF ORAL DISINTEGRATING FILM OF ATENOLOL

2018 ◽  
Vol 11 (8) ◽  
pp. 312
Author(s):  
Sanjay P ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Praveen Sivadasu
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
In Vitro Dissolution ◽  
Surface Ph ◽  
Morphological Evaluation ◽  
Weight Variation ◽  
Film Forming ◽  
Folding Endurance ◽  
Drug Polymer Interaction ◽  
Oral Films

Objective: The main objective of the study was to formulate the oral disintegrating films loaded with atenolol by solvent-casting method and to carry out its evaluation studies.Methods: The films were prepared using the film-forming hydrophilic polymer like hydroxypropyl methylcellulose (E-5) and super disintegrant like pectin in various proportions.The formulated oral films were characterized for Fourier transform infrared (FTIR) and morphological evaluations. Various physicochemical parameters such as weight variation, folding endurance, surface pH, in vitro disintegration, and in vitro dissolution studies were carried out.Results: FTIR studies revealed that there was no drug-polymer interaction. The morphological evaluation of films showed that all the films were homogenous and transparent. The folding endurance test ensured that the films had sufficient brittleness and by weight variation test, it was inferred that all the films were within the deviation. The surface pH study showed the pH of the films was around neutral pH. The drug was well distributed in all the films. The films disintegrated within 120 s and the fastest being disintegrated in 30 s. Based on all the evaluation parameters, F6 had shown optimal performance and remarkable increase in drug release of 94.38% in 2 min.Conclusion: Thus, formulated oral disintegrating films can be termed as an alternative approach to deliver atenolol.

Drug Excipient Compatibility, Development and Preliminary Clinical Studies of Tizanidine Hydrochloride Floating Drug Delivery System

2021 ◽  
Vol 14 (1) ◽  
pp. 5334-5342
Author(s):  
Kishan V ◽  
Swathi Yambadi ◽  
Ramesh Bomma
Keyword(s):  
Clinical Studies ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Visual Observation ◽  
Matrix Tablets ◽  
Gastric Retention ◽  
Clinical Effects ◽  
Floating Tablets

The objective of this investigation was to develop formulation of floating matrix tablets of tizanidine HCl to prolong the gastric residence time by using hydroxy propyl methyl cellulose (HPMC K15M) or xanthan gum as sole release retardant and to check the clinical response. The drug-excipients compatibility studies were conducted using DSC and also by visual observation. Incorporation of NaHCO3 in the formulation resulted incompatibility with drug and therefore, the composition was modified by replacing NaHCO3 with CaCO3 in remaining formulations. Floating matrix tablets of tizanidine were developed by direct compression method and the developed ten formulations exhibited satisfactory physicochemical characteristics and in-vitro buoyancy. Formulation (F9) was selected as optimized formulation based on physicochemical characters, in-vitro buoyancy and drug release, and was used in in-vivo radiographic studies in human volunteers by incorporating BaSO4. In radiographic studies, the gastric retention time of floating tablets was found to be 4 ± 0.86 h (n=3). Optimized floating tablets (F9) were used to know the clinical effects in patients suffering from spasticity under the observation of clinician. The optimized tizanidine HCl floating matrix tablets were developed and found to have gastric retention behaviour in stomach and further were found to have good clinical effects in patients suffering from spasticity during preliminary clinical studies.

scholarly journals PREPARATION AND CHARACTERIZATION OF LAFUTIDINE AS IMMEDIATE RELEASE ORAL STRIP USING DIFFERENT TYPE OF WATER-SOLUBLE POLYMER

2018 ◽  
Vol 10 (5) ◽  
pp. 249 ◽  
Author(s):  
Saba Abdulhadee Jabir ◽  
Halah Talal Sulaiman
Keyword(s):  
Drug Release ◽  
Methyl Cellulose ◽  
Water Soluble ◽  
Low Grade ◽  
Disintegration Time ◽  
Water Soluble Polymer ◽  
Surface Ph ◽  
Drug Content ◽  
Film Forming

Objective: The objective of the present study was to design and optimize oral fast dissolving film (OFDF) of practically insoluble drug lafutidine in order to enhance bioavailability and patient compliance especially for a geriatric and unconscious patient who are suffering from difficulty in swallowing.Methods: The films were prepared by a solvent casting method using low-grade hydroxyl propyl methyl cellulose (HPMC E5), polyvinyl alcohol (PVA), and sodium carboxymethyl cellulose (SCMC) as film forming polymers. Polyethylene glycol 400 (PEG400), propylene glycol (PG) and glycerin were used as a plasticizer to enhance the film forming properties of the polymer. Tween 80 (1% solution) and poloxamer407 were used as a surfactant, citric acid as a saliva stimulating agent, and croscarmellose as a super disintegrant. Films were then tested for both physical (weight variation, thickness, surface pH, drug content) and mechanical (folding endurance, tensile strength, percent elongation, Young's modulus) characteristics. In vitro disintegration, time and drug release profile were also determined for each formula.Results: Films were found to be satisfactory when evaluated for both physical and mechanical characterizations. The surface pH of all the films was found to be within the range of salivary pH 6.8. The USP dissolution apparatus type II (paddle type) was used for in vitro drug release studies. The optimized formulation F13 gave 100 % of drug released at 2 min. It also showed satisfactory surface pH (6.2±0.2), drug content (100.1±0.01%), the disintegration time of (7.0±0.5) seconds and the time needed for 80% of medication to be released (T80%) was 0.96 min.Conclusion: Lafutidine OFDF was formulated using HPMC E5 as film-forming a polymer with PEG400 as a plasticizer. Combination of tween80 (1% solution) and poloxamer407 as a surfactant were used in the presence of croscarmellose as a super disintegrant. The chosen OFDF disintegrates within seven seconds, releases the drug rapidly and gives an action.

scholarly journals Pre-Formulation Studies: Physicochemical Characteristics and In Vitro Release Kinetics of Insulin from Selected Hydrogels

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1215
Author(s):  
Aneta Ostróżka-Cieślik ◽  
Małgorzata Maciążek-Jurczyk ◽  
Jadwiga Pożycka ◽  
Barbara Dolińska
Keyword(s):  
Release Kinetics ◽  
Polymer Network ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Physicochemical Characteristics ◽  
Diabetic Patients ◽  
Tertiary Structures ◽  
Duration Of Action ◽  
The Stability

Insulin loaded to the polymer network of hydrogels may affect the speed and the quality of wound healing in diabetic patients. The aim of our research was to develop a formulation of insulin that could be applied to the skin. We chose hydrogels commonly used for pharmaceutical compounding, which can provide a form of therapy available to every patient. We prepared different gel formulations using Carbopol® UltrezTM 10, Carbopol® UltrezTM 30, methyl cellulose, and glycerin ointment. The hormone concentration was 1 mg/g of the hydrogel. We assessed the influence of model hydrogels on the pharmaceutical availability of insulin in vitro, and we examined the rheological and the texture parameters of the prepared formulations. Based on spectroscopic methods, we evaluated the influence of model hydrogels on secondary and tertiary structures of insulin. The analysis of rheograms showed that hydrogels are typical of shear-thinning non-Newtonian thixotropic fluids. Insulin release from the formulations occurs in a prolonged manner, providing a longer duration of action of the hormone. The stability of insulin in hydrogels was confirmed. The presence of model hydrogel carriers affects the secondary and the tertiary structures of insulin. The obtained results indicate that hydrogels are promising carriers in the treatment of diabetic foot ulcers. The most effective treatment can be achieved with a methyl cellulose-based insulin preparation.

scholarly journals FORMULATION AND EVALUATION OF FLOATING ORAL IN SITU GEL OF DILTIAZEM HYDROCHLORIDE

2016 ◽  
Vol 9 (1) ◽  
pp. 50
Author(s):  
A. Maheswaran ◽  
J. Padmavathy ◽  
V. Nandhini ◽  
D. Saravanan ◽  
P. Angel
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Diltiazem Hydrochloride ◽  
Release Formulation ◽  
Gelling Properties ◽  
In Situ Gelling

Objective: The objective of the present study was to formulate and evaluate the floating in-situ gelling system of diltiazem hydrochloride.Methods: Sodium alginate based diltiazem hydrochloride floating in situ gelling systems were prepared by dissolving hydroxyl propyl methyl cellulose (HPMC) in 25% of water, to which calcium carbonate and diltiazem hydrochloride were added with stirring to form, a proper and a homogenous dispersion of diltiazem hydrochloride. Meanwhile, 30% of water was heated to 60 ˚C on a hot plate to dissolve sodium alginate and cooled to 40 ˚C. The resulting solution was added to HPMC solution and mixed well. To 5% of water at 60 ˚C, sodium methyl paraben was added and dissolved and cooled to 40 ˚C and was added to the above mixture and mixed well. The volume was adjusted finally to 100% with distilled water. Prepared formulae were evaluated for physicochemical properties, drug content, pH, in vitro gelling capacity, in vitro buoyancy, viscosity, water uptake and in vitro drug release.Results: Formulation variables such as type and concentration of viscosity enhancing polymer (sodium alginate) and HPMC affected the formulation viscosity, gelling properties, floating behavior, and in vitro drug release. Formulation F5 and F6 showed the floating time of 5 min and more than 20 h respectively. A significant decrease in the rate and extent of the drug release was observed with the increase in polymer concentration in in-situ gelling preparation. Formulation F4, F5, F6 were shown to have extended drug release until the end of 7 h.Conclusion: The prepared in situ gelling formulations of diltiazem hydrochloride could float in the gastric conditions and released the drug in a sustained manner. The present formulation was non-irritant, easy to administer along with good retention properties, better patient compliant and with greater efficacy of the drug.

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