A modified USP tablet disintegration tester was used to determine the folding endurance of the membrane. It consisted of fixed and movable jaws that could be moved up and down at the rate of 30 stokes per minute. The distance between 2 jaws at their farthest and closest were 6 centimeter and 0.5 centimeter respectively. The membrane (6cm length) was clamped between the jaws in such a way that the jaws were at their closest, the membrane beats across its middle and when at their farthest, the membrane was in a stretched condition Thus for every stock of the movable jaw the membrane went through one cycle of bending and stretching. The folding endurance is expressed as the number of strokes required to either break or develop visible cracks on the membrane. The test was conducted for 20min equating 600 strokes. The locally fabricated folding endurance tester. 
13 Read more
The transdermal patches of SIT prepared by solvent casting method using a combination of ethylcellulose, eudragit, in various ratios of plasticizers and permeation enhancers were studied. All the formulations showed good physicochemical properties such as thickness, weight variation, drug content and folding endurance. The in vitro release data showed that drug release from the patch has been affected by the type and concentration of the polymer. From this data, optimized formulations were screened. Formulation F3 were considered as the best formulations. Based on the encouraging results, the SIT transdermal patch can be used
All the eight batches were evaluated for thickness by using calibrated Vernier caliper with a least count of 0.01mm. The thickness was measured at three different spots of the films and the average was taken. The results were summarized in results part. Folding endurance:
Selected Dependent Variable: Folding endurance (Y1), Tensile strength (Y2) and % Drug release (Y3) Response Model for Folding Endurance (Y1) The Model F-value of 10.39 for folding endurance implied the model was significant. Values of "Prob > F" was 0.0412 which was less than 0.05 indicated model terms were significant. Adequate Precision measures the signal to noise ratio. A ratio greater than 4 is desirable. Ratio of 9.183 indicated an adequate signal. This model could be used to nevigate the design space shown in table 11.
13 Read more
In the present research Gemifloxacin Mesylate intra-pocket films were developed with combination of chitosan and HPMC. By doing compatibility study, drug was found to be compatible with formulation excipients. The developed formulations showed satisfactory results for physical appearance, % drug content, thickness and weight measurements, percentage moisture loss, folding endurance, surface pH, stability and in vitro drug release. Formulation containing 1% w/w chitosan was considered the best formulation as it gives satisfactory in vitro result which is considered a good candidate for local delivery systems.
13 Read more
Transdermal drug delivery system is a most suitable system for a long-term treatment or for a multi dose treatment, because different transdermal patches are prepared for a long period of time in a suitable dose proving treatment from a day to even up to seven days. In this study Carvedilol transdermal patches were prepared with combination of different polymers such as EC: PVP K-30, EC: HPMC K-15M, EC: Carbopol-934. Total six formulations were selected (F-1 to F-6) for further evaluation such as physicochemical properties, in-vitro drug permeation study and surface pH of the film. From Physicochemical evaluation it is found that thickness, weight variation, moisture content, drug content, folding endurance and flatness were suitable for maximum stability of the prepared transdermal patches. In-vitro drug permeation study, the percent of drug permeated was found to maximum 95.44 and 90.12% from from F-3 and F-5 film respectively. Based on physicochemical and in-vitro permeation studies; F-3 and F-5 were chosen as the best patches among all the
10 Read more
The aim of the present study was to develop site specific drug delivery of ornidazole for the treatment of periodontitis which has excellent activity against anaerobic microorganisms. The formulations were prepared by utilizing polymers such as PEO and gellan gum by solvent technique with the used of plasticizer (PEG-400). The calibration curve of ornidazole was developed in PBS pH 6.8 at 317nm in the range of 2 to 20 µg/ml. Compatibility study were carried out by FT-IR and Differential scanning Colorimetry. The formulations were evaluated for thickness, folding endurance, weight variation, drug content, percent moisture loss, tensile strength, and percent elongation, SEM and in vitro antibacterial activity. In vitro drug release study was also carried out using PBS pH 6.8 and the samples were analyzed by UV-spectrophotometrically at 317nm. FT-IR and DSC study revealed no interaction between drug and polymers. Formulations shown good uniformity of drug content, there is no any kind of effect on moisture loss test. Formulations showed thickness within the range of 0.0417 to 0.0633. Formulations F3, F4, F7 and F8 showed good tensile strength. By increasing the concentration of PEO in the formulation increases the tensile strength, percent elongation and folding endurance. Formulation F3 released 92.44% of drug at the end of three minute and was considered as best formulation. A short-term stability study of the optimized formulation F3 was carried out at 40 0 C for three months. At periodic interval sample were analyzed for drug
11 Read more
of Olanzapine was found to be 226 nm by using U.V. spectrophotometer (Labindia-3000+). The calibration curve of Olanzapine was found to be linear in the concentration range of 5-25µg/ml at 226 nm fig. 2. The general appearance, assay, weight variation and thickness of all the films were within acceptable limits table 2. The results for tensile strength, folding endurance, disintegrating time and % of moisture were shown in table 3. Tensile strength value of optimized formulation (F4) was 1.236±0.045 kg/cm 2 and
Placebo formulations were prepared by using solvent casting technique. The film forming polymers HPMC and PVA were accurately weighed and dispersed in 7:3 ratio of IPA and dichloromethane each and then soaked for 4 hours. To these polymer solutions, glycerol and Mannitol were added with continuous stirring on a magnetic stirrer. The resulting bubble free solution was poured on to a glass plate and was dried at 50˚C in hot air oven for 24hr. Like this many blank films were developed by using polymer (HPMC E5, HPMC E15, PVA) and plasticizer (Glycerol, PEG400) in various combination and concentration, which were carefully removed from glass plate and evaluated for drying time, average weight, thickness, tensile strength, folding endurance and in vitro disintegration time [5,6,7] and the best
The optimum loading for better, flexible films was found to be 15% or less than that. For the present investigation, chitosan films containing moxifloxacin with three different concentrations, that is 5,10, and 15% to the weight of the polymer of single layer as well as bilayer with 5% and trilayer with 10% of drug were prepared using solvent casting technique. The prepared films containing moxifloxacin trilayer with 15% drug concentration has shown the extended drug release for 12 days. The FTIR studies from the spectra [Figure 1] confirmed the absence of any chemical interaction between the drug and the polymer. Macroscopical features revealed that the drug had dissolved in the polymer matrix rather than dispersing. The physicochemical evaluation data presented in [Table 1] showed that the average weight of the films ranged from 0.989 to 3.176 mg. The maximum weight was observed with trilayer with 10% drug loaded films. The thickness of the films ranged from 0.101 to 3.01 mm. The thickness was observed more with the trilayer 10%.The tensile strength of the films ranged from 1.35 to 3.25 kg/sq.mm, tensile strength was minimum for plain films and maximum for trilayer film containing 10% of moxifloxacin. The folding endurance studies showed that plain inserts exhibited maximum folding endurance followed by drug loaded inserts respectively. All the films were found to contain an almost uniform quantity of the drug, as per content uniformity studies [table 2] indicating reproducibility of the technique. The percentage moisture loss between 18.01 to 42.75 and the percentage moisture absorption was found to be in the range of 22.21 to 33.75.
From the above physicochemical evaluation and in vitro studies it was concluded that preformulation studies of glibenclamide were found in accordance with the reported literature limits. The formulated transdermal patches of combinations of HPMC and EC showed good physical properties Thickness, folding endurance and drug content were found to be uniform and reproducible with low SD values compared to patches with hydrophillic and hydrophobic polymers alone. All the optimized patches formulated were stable at room temperature. F4 showed highest release during in vitro drug permeation studies through dialysis membrane. The release of glibenclamide appears to be dependent on hydrophilicity of the matrix. Moderately hydrophilic matrices showed best release. The predominant release mechanism of drug through the fabricated matrices was believed to be by diffusion mechanism. The release of glibenclamide from the optimized formulation F4 follows zero order kinetics and the mechanism of drug release was concluded as diffusion controlled.
Transdermal patches folding endurance was estimated by frequently double over at the same place till it broke. The number of times the film could be folded at the same place without breaking is the folding endurance. This was restating on all the films for three times and the mean values plus standard deviation was calculated.
Hence, it is commonly employed in formulation of patch. The physico-chemical characteristics such as thickness of the patch, folding endurance, percentage of moisture absorbed, percentage of moisture lost, and drug content analysis were found to be within the acceptable limits. The patches were found to be stable to withstand the stress. In vitro Diffusion studies of Transdermal patches: The study of in-vitro diffusion is carried out by using Franz Diffusion Cell.
14 Read more
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, folding endurance 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
12 Read more
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, folding endurance, 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.
The main objective of the present study was to formulate and evaluate matrix type Pioglitazone transdermal patches and to determine the drug release. Firstly, characterization of the drug was done by performing FTIR compatibility studies and found that there was no interaction between the drug and polymers under study. Formulations (F1 to F6) were prepared using different ratios of HPMC E15 and Eudragit L 100 and penetration enhancer DMSO was incorporated to the above formulations (F7 to F12).These formulations were evaluated for weight variation, thickness variation, folding endurance, %moisture content, %moisture absorption studies, drug content, mechanical properties and exvivo permeation studies. In formulations F1 to F12, the drug permeation was maximum for F4 and F10 (ratio 10:2 HPMC E15: Eudragit L100). Among these, formulations F10 is exhibited the required flux.
10 Read more
The purpose of this work was to develop an ocular insert for the treatment of glaucoma with α- agonist Brimonidine tartrate. Nine such ocular inserts were prepared by solvent casting method using polymers Hydroxyethyl methacrylate (HEMA), EUDRAGITRL-100,EUDRAGIT RS-100, plasticizers, Dibutyl phthalate(DBP), PEG 400 and Propylene glycol and water as solvent. These formulations were evaluated for mechanical properties like tensile strength, % elongation at break, strain, folding endurance, physicochemical properties like thickness, weight variation, surface pH, %moisture absorption, compatibility, and drug content. In vitro drug release was carried out and the release kinetics was studied which revealed case II transport. All the formulations were taken for sterilization and subjected to eye irritancy test on Rabbits. Inserts containing HEMA plasticized with DBP showed better shape retaining properties and more controlled release of drug. On the basis of evaluation it was found that tensile strength and folding endurance of the inserts prepared with plasticizer DBP was high compared to inserts prepared with other plasticizer and inserts containing HEMA showed good shape retaining properties than other polymers used in the study.
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, folding endurance 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.
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, folding endurance, 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
12 Read more
A modified USP tablet disintegrating tester was used to determine the folding endurance of the membranes. It consisted of fixed and movable jaw that could move up and down at the rate of 30 strokes per minute. The distance between the two jaws at their farthest and closest was 6cm. The membrane 6cm length was clamped between the jaws in such a way that when the jaws were at the closest, the membrane folds across its middle and when the jaw was at its farthest, the