In the present investigation, an effort was made to design a novel drug delivery system for the treatment of chronic periodontitis for site- specific delivery of Gemifloxacine mesylate which has excellent activity against wide range of microorganisms. The main purpose of formulating intra-pocket films using blend of chitosan and hydroxypropyl methyl cellulose was to extend drug release for prolonged period of time and to minimize frequent dosing of drug which would lead to better patient compliance. FTIR and UV spectroscopic methods revealed that there is no significant interaction between Gemifloxacine mesylate and polymers. The films were then evaluated for various parameters like thickness, foldingendurance, weight variation, content uniformity, stability study and in- vitro drug release study. Formulation MG1 was the best chosen one concerning its high % of drug release 96.18 and retarded drug release as expected from its long T 50% =
Carvedilol is a nonselective beta-adrenergic blocking agent and is employed for the treatment of hypertension. Carvedilol is subjected to considerable first-pass metabolism when it is administered orally. Transdermal preparation of carvedilol was prepared to achieve a sustained effect and to reduce the dose size & dosing frequency as compared to multiple oral dosing and also developed to minimize first pass metabolism. Various polymers such as Ethyl cellulose, PVP K-30, HPMC K15M and Carbopol 934 were selected on the basis of their adhering property and nature of non toxicity, to develop transdermal film of carvedilol. The patches fabricated by EC and Carbopol (F-5 and F-6) were showed very good foldingendurance compared to patches containing PVP K-30 and HPMC K15M. Based on physicochemical and in-vitro permeation studies, F- 3 and F-5 were chosen as the best formulations. Among these two patches, F-5 film was found to have maximum in vitro permeation, maximum steady state flux and maximum permeability coefficient of drug.
The present study was carried out to develop transdermal patches of Rivastigmine with different ratio of HPMC (hydroxyl propyl methyl cellulose) and EC (ethyl cellulose) by solvent casting method. Propylene glycol 3% is used as a plasticizer and Span 80 as permeation enhancer. Formulated transdermal patches were evaluated with regard to physicochemical characteristics (thickness, foldingendurance etc.) and In-vitro permeation studies were performed using Franz diffusion cell. The data obtained from in- vitro permeation studies was treated by various conventional mathematical models (zero order, first order, Higuchi and Korsmeyer- Peppa’s) to determine the release mechanism from the transdermal patches formulations. Selection of a suitable release model was based on the values of R 2 (correlation coefficient), k (release constant) obtained from the curve fitting of release data. It was
In the present research work Frovatriptan drug was formulated as Fast dissolving Thin oral films by solvent casting method. Triptans are a class of anti migraine drugs which are formulated to give rapid relief from migraine attacks. Previously prepared in the form of tablets which has certain disadvantages so are formulated as films which disintegrate rapidly within in seconds in the mouth without need of water. The films were prepared by employing Frovatriptan drug, Hydroxy Proipyl Methyl Cellulose (HPMC E5) as polymer, Isopropyl alcohol was employed as solvent, Propylene glycol as plasticizer, Mannitol as diluents and aspartame as sweetening agent. The films were evaluated for parameters like Weight uniformity, Morphological properties Thickness uniformity, Foldingendurance, Surface pH, Drug content uniformity test, In-vitro disintegration test, In-vitro dissolution studies which were found to be satisfactory. Among all the formulations F8 has found to be the best formulation with a disintegration time of 12sec and 100% of cumulative drug release within in 20min. Thus it indicates that Frovatriptan is highly suitable to be formulated as Fast dissolving thin oral films for their rapid release and immediate treatment of migraine attack.
Transdermal drug delivery systems are becoming more popular in the field of modern pharmaceutics because it has many advantages over traditional drug delivery system and mostly used to overcome the problems associated with conventional delivery system of drugs. it is self-contained, non-invasive, painless, user- friendly and discrete dosage form. The main objective of transdermal drug delivery system is to deliver drugs into targeted organ or parts through skin at predetermined rate with minimal inter and intra patient variation. The present study was carried out to develop transdermal patches of atenolol with different ratio of HPMC (hydroxyl propyl methyl cellulose), EC (ethyl cellulose) and PVP (polyvinyl pyrrolidine) by solvent casting method. Propylene glycol 3% is used as a plasticizer and Span 80 as permeation enhancer. The identification of drug and the possible drug polymer interactions were studied by FTIR spectroscopy. Formulated transdermal patches were evaluated with regard to physicochemical characteristics (thickness, foldingendurance etc.) and In-vitro permeation studies were performed using Franz diffusion cell. The data obtained from in- vitro permeation studies was treated by various conventional mathematical models (zero order, first order, Higuchi and Korsmeyer- peppa’s) to determine the release mechanism from the transdermal patches formulations. Selection of a suitable release model was based on the values of R 2
The conventional multidose antiparkinsons therapy leads to re-emergence of Parkinson’s symptoms, due to fluctuations in serum levels of drug. The rational strategy to overcome this drawback is to minimize the fluctuations by fabricating sustained release formulations. Ropinirole HCl is a drug used to treat Parkinson’s disorder and it is suitable drug candidate for transdermal delivery due to its small molecular size, optimum log P and low oral bioavailability due to first pass metabolism. Hence the present study was aimed at preparation of transdermal patch of Ropinirole HCl to show its prolonged release. HPMC K4M and Sodium alginate were used as a polymer matrix to control the release of Ropinirole HCl up to 24 hrs. The transdermal patches were prepared by solvent casting method. All the patches were evaluated for the weight variation, thickness, foldingendurance, drug content, percentage of moisture content and percentage of moisture uptake, tensile strength and In-vitro diffusion study. The results of physical parameters ensured integrity and applicability of the patches. The highest diffusion was found to be more than 93 % in 24 hours and kinetic model application confirmed that the release of Ropinirole HCl follows zero order as well as higuchi model. The stability study was carried out on optimized batch under accelerated condition for 1 month.. The objectives are:Preliminary compatibility study between drug and excipients, To prepare drug loaded transdermal patch, To evaluate the prepared transdermal patch, Conduct Stability study.
The present study was aimed to formulate site- specific controlled release dental strips for the treatment of periodontal diseases. The various pharmaceutical parameters like thickness, compatibility studies, tensile strength, uniformity, weight, content uniformity, percentage elongation, foldingendurance, DSC, percent moisture loss and SEM. In vitro antibacterial activity and stability studies were performed on optimized formulation.
In case of psychiatric treatment immediate release of drug from the dosage form is required. Fast dissolving dosage forms are gaining popularity in recent time, as this dosage forms requires no water for administration. Oral films dissolve rapidly along with drug in mouth and majority of the drug is absorbed through buccal/oral mucosa in to systemic circulation avoiding first pass metabolism. Olanzapine is a thienobenzodiazepine class of drugs, which has been approved by the FDA, for the treatment of schizophrenia, depressive episodes associated with bipolar disorder, acute manic episodes and maintenance treatment in bipolar disorder. The absolute bioavailability is only approximately 31.5% due to extensive hepatic metabolism. Thus the objective of the present study was to formulate and evaluate fast dissolving oral films of Olanzapine to improve water solubility, dissolution rate, oral bioavailability and reduction of first pass metabolism and increase patient’s compliance. Oral fast dissolving films prepared by solvent casting method using water and 95% ethanol as solvents and HPMC as film forming polymer. PEG 400 was the selected plasticizers, Superdisintegrants such as croscarmellose sodium (CCS) and sodium starch glycolate (SSG) alone and also in combinations was incorporated to achieve the aim. The prepared films were evaluated for the drug content, weight variation, film thickness, disintegration time, foldingendurance, percentage of moisture content and in vitro dissolution studies. Among all, the formulation F4 was found to be best formulation which releases 98.78 % of the drug within 15 min and disintegration time is 42 sec. which was significantly high when compared to other formulation. The data obtained from In-vitro release were fitted into the various kinetic models such as Zero Order, Higuchi, First Order and Korsmeyer–Peppas Model in order to determine the mechanism of drug release. When the regression coefficient values compared, it was observed that ‘r’ values of formulation F4 was maximum i.e 0.974 hence indicating drug release from formulations was found to follow first order drug release kinetics.
The present research work is to develop mouth dissolving film of Fexofenadine Hydrochloride by solvent casting method using different concentration of HPMC 5cps as film former & Polyethylene glycol 400 as plasticizer. Drug – Excipient compatibility study by FTIR shows no interaction between drug and excipients. The films were characterized for various physic-chemical parameters such as film weight, thickness, foldingendurance, surface pH, tensile strength, % elongation, drug content, disintegration time, in vitro drug release studies. A 3 2 full factorial design was applied to study the combined effect of HPMC 5cps and Polyethylene glycol 400. The formulation containing combination of two independent variables such as concentration of HPMC 5cps (X 1 ) and Concentration of polyethylene glycol 400 (X 2 ). Tensile strength (Y 1 ), Disintegration
The purpose of the present investigation was to prepare Glibenclamide transdermal patches and to study the effect of different polymer combination and polymer ratios on physiochemical parameters including in-vitro drug release profile. Matrix type Glibenclamide transdermal patches were prepared using Ethyl Cellulose (EC) and Hydroxy propyl methyl cellulose (HPMC) in different ratios. Propylene glycol was used as a plasticizer and tween 80 used as permeation enhancers which were prepared by solvent casting method. The prepared formulations were evaluated for various parameters like Thickness, Weight variation, Foldingendurance, Moisture absorption, Moisture loss, Drug content, Drug permeation, Drug–polymer interactions. In- vitro drug release studies were performed by using Franz diffusion cells. Variations in drug release profile were observed among various formulations. The FT-IR studies revealed no interaction between drug and polymers. The present work also concentrates on comparision between the effect of hydrophillic and hydrophobic polymers on the physicochemical parameters of the transdermal patches.
Cetrizine dihydrochloride belongs to the category of anti histamines used in treatment of various allergic conditions. Administration of these agents via transdermal route can bypass various disadvantages caused by oral administration and may maintain relatively consistent plasma drug level for long time therapy .The present study attempts for preparation of matrix monolithic transdermal system of Cetrizine dihydrochloride. Different polymers like hydroxy propyl methyl cellulose (HPMC), polyvinyl pyrrolidine (PVP), ethyl cellulose (EC) and methyl cellulose (MC) either individually or in combination have been tried. All the patches were prepared by adding glycerin as plasticizer. Methanol is used as a common solvent. The prepared patches were evaluated for physicochemical parameters like thickness, weight variation, foldingendurance, water absorption capacity, moisture content, tensile strength, percentage elongation, drug content, in vitro and in vivo drug permeation studies. From all the patches, F7 containing 2.25%w/v of hydroxy propyl methyl cellulose and 7.5%w/v of Polyvinyl Pyrrolidone had shown good physical properties. In vitro studies indicated a drug permeation of 90.51% and in vivo studies indicated drug permeation of 85.21% in 24 hours. The in vitro and in vivo pharmacokinetic data had shown first order drug release and they followed non fickian diffusion mechanism of drug permeation. Keywords: Cetrizine Dihydrochloride, Matrix Transdermal system, Transdermal drug delivery system.
The study was to formulate and evaluate chitosan film containing tobramycin which will give local action for the treatment of periodontitis. Chitosan film containing tobramycin was prepared by solvent casting method. IR studies were done to determine the compatibility of drug with the polymer. Minimum inhibitory concentration of tobramycin was done by cup-plate method. The films were evaluated for their physicochemical properties like weight variation, thickness, drug content uniformity, foldingendurance, % moisture loss, tensile strength and stability. Drug content uniformity was performed on Staphylococcus aureus. Scanning electron microscope (SEM) studies were done to determine the surface characteristics of the film.IR studies revealed that there is compatibility of drug with the polymer. Minimum inhibitory concentration of tobramycin was found to be 1 µg/ml. The physiochemical properties of the film showed good results.
The Aim of the present study is to design and evaluate fast dissolving Oral thin films (OTF) of Alendronate drug. The bisphosphonate called alendronate used for osteoporosis and several other bone diseases. Sixteen Formulations (F1–F16) of OTF were prepared by casting method using different concentrations of polymer increased tensile strength and foldingendurance were improved with more dissolution time. 0.3% and above concentration of polymer showed good physical and rheological properties. Optimized formulation among OTF was an F4 with 1.5% Sodium alginate showing good foldingendurance, t ensile strength, disintegration time and 98.9% drug release with no casting problem and appearance.
Fast dissolving films are playing an important role in the current pharmaceutical drug delivery systems. They have convenience and ease of use over solid and liquid dosage forms. In the present research, fast dissolving oral film of terbutaline sulphate were developed for treatment of asthma in pediatric and geriatrics using HPMC K15 LV as film forming polymer, SSG as superdisintegrant and PEG-400 as plasticizer. The films were prepared by solvent casting method. Optimization of HPMC E15 LV, SSG and PEG-400 was carried out using 3 2 full factorial designs. The formulated films of terbutaline sulphate were evaluated for their physic-mechanical parameters like disintegration time, tensile strength, percent elongation, foldingendurance and In-vitro drug release. Estimation of drug content uniformity of terbutaline sulphate films was performed and the results were satisfactory. Optimized batch F 3 has thickness (0.188±0.001mm), disintegration time
The main objective of the study was to formulate and evaluate fast dissolving film containing Loratidine. The fast dissolving films can be easily formulated by solvent casting method by using polymers such as HPMC, HPC and EC in different ratios with suitable plasticizer like glycerin and Tween-80 and sweetener like aspartame. It was observed that the physicochemical characteristics such as uniformity of weight, thickness, foldingendurance, surface pH, and uniformity of drug content of all the film samples showed satisfactory results with respect to variation of these parameters between films of same formulation. Based on the physicochemical parameters and in vitro drug release studies, formulation F4 considered as the best formulation which exhibited the drug release of 98.49%. At the end of 10 min. Present study reveals that all the five formulated films showed satisfactory film parameters. From the present investigation it can be conclude that fast dissolving film formulation can be a potential novel drug dosage form for paediatric, geriatric and also for general population. Finally formulation 4 was considered as optimized formula for preparing FDF of Loratidine, where it shown best drug release profile.
The objective of the present study was to formulate and evaluate controlled and prolonged release transdermal drug delivery system of atenolol for effective management of hypertension. The administration of atenolol via transdermal patch facilitates a direct entry of drug molecules into the systemic circulation, avoiding the first-pass metabolism and drug degradation in the harsh gastrointestinal environment, which are often associated with oral administration. To fulfill above objective transdermal patches of atenolol were prepared by solvent evaporation method using combinations of Eudragit RL100, Ethyl cellulose and PVP in different proportions. Various physicomechanical parameters like weight variation, thickness, foldingendurance, drug content, water vapour transmission and tensile strength were evaluated. In-vitro Diffusion Study, skin irritation test and stability studies were also performed. In PVA and Eudragit RL 100 patches the water vapor transmission rate was found to be higher at 75% RH, RT conditions. Therefore at both % RH, RT conditions the PVA and Eudragit RL 100 patches provide the best resistance to water vapor.
Eletriptan, an anti migraine agent is selected for the preparation of transdermal delivery system as it complies with physicochemical properties required to permeate through skin. The preformulation studies involving melting point, partition coefficient of the drug were found to be suitable when compared with the standard. The patches were prepared by solvent evaporation method. The patches were subjected for following evaluation parameters such as physical appearance, weight variation, thickness, foldingendurance, drug content, percentage moisture absorption, percentage moisture loss, tensile strength, diffusion studies and skin irritation studies. All the parameters shows were within the limits. In- vitro drug release the formulations F 1- F 5 , which is
In the present work efforts have been made to prepare transdermal drug delivery system of Nisoldipine, EC and PVP, using polyethylene glycol as a plasticizer by solvent casting technique. The selection of polymer combinations produces clear, smooth, uniform, substantive, flexible and desired thickness film for the transdermal drug delivery systems of Nisoldipine. The prepared formulation were evaluated for different physico- chemical characteristics such as thickness, foldingendurance, drug content, percent moisture absorption, percentage moisture loss and weight uniformity. The release characteristics of the formulation were studied in in-vitro conditions. In vitro permeation studies were carried out in phosphate buffer (pH 7.4) for 24 hours. The partition coefficient of the Nisoldipine was found to be 3.87, After 24 hrs. 71.25 % drug was permeated through skin. The thickness of the patches varied from 52 to 65μm. The minimum standard deviation values assumed that the process used for preparing the drug delivery system is capable of giving reproducible result. As the concentration of PVP and Ethyl cellulose increase, moisture content of patches was also increase. Formulation F5 (1.481±0.24) absorbed highest amount of moisture which also revealed its high hydrophilicity and formulation F1 (1.096±0.14) absorb least amount of moisture. The foldingendurance was measured manually; films were folded 59 times maximum in formulation F1and if the film shows any cracks it was taken as end point. The foldingendurance was better in F1 formulation. As the concentration of PVP and Ethyl cellulose increase, moisture uptake of patches was also increase. The highest moisture absorption was found in the formulation F5 and lowest value of moisture absorption was found in the formulation F1. The drug content uniformity of the prepared formulation have
Transdermal patches are innovative drug delivery systems and can be used for achieving efficient systemic effect by passing hepatic first pass metabolism and increasing the fraction absorbed. Transdermal patches of Promethazine hydrochloride (PMZ) were prepared by the solvent casting evaporation technique using ethyl cellulose: HPMC, Eudragit RSPO, propylene glycol and permeation enhancer using different ratios. The physicochemical parameters such as flexibility, thickness, smoothness, weight variation, moisture content, hardness, foldingendurance and tensile strength were evaluated for the prepared patches. The formulation exhibited flexibility, uniform thickness and weight, smoothness, good drug content (91.65 to 96.36%), and little moisture content. The in vitro diffusion studies were carried out using modified Franz diffusion cell using egg membrane as the diffusion membrane and the formulation followed the Korsmeyer-Peppas diffusion mechanism. The formulation containing ethyl cellulose: HPMC as polymers showed faster release rate compared to Eudragit: HPMC. The stability studies indicated that all the patches maintained good physicochemical properties and drug content after storing the patches in different storage conditions. Compatibility studies indicated that there was no interaction between the drug and polymers. Hence, the aim of the present study was to prepare the sustained release formulation (Transdermal patches) of the drug using different blend of polymers.