HPMC K100 Research Articles

Preparation and evaluation of sustained release microspheres for the treatment of diabetic neuropathy

This study aimed to prepare and evaluate sustained release microspheres for the treatment of diabetic neuropathy using Various polymers including sodium alginate, ethyl cellulose, HPMC K100, Carbopol 934, and Eudragit L-100-55. Polymers were employed to assess their impact on several crucial parameter’s entrapment efficiency, production yield Particle size analysis, swelling index, in vitro dissolution, and release kinetics. The production yield of microspheres varied depending on the polymer used, with some polymers performing in advanced yields. Entrapment effectiveness was set up to be optimal with certain polymer combinations. Particle size analysis indicated that the microspheres were within the asked range for controlled release operations. The swelling index showed polymer-dependent lump actions. In vitro dissolution studies demonstrated sustained medicine release over time, with different polymers impacting both the release rate and profile. medicine release kinetics analysis revealed that the release followed specific models, reflecting the commerce between the microsphere matrix and the medicine.

Optimizing Orphan Drug Rucaparib Transdermal Patches for Ovarian Cancer: A Design Expert-Based Strategy for Prolonged Drug Release.

This study aimed to develop and characterize transdermal patches for rucaparib using a Box-Behnken design (BBD), evaluating drug permeation at 8, 12, and 24 hours, with optimization through Design Expert software. The patches were formulated with HPMC K15, ethyl cellulose, and PVP K30. The physicochemical properties and drug infusion were tested and characterized. The transdermal patches developed in this study were found to be soft and flexible, indicating good handling properties and potential for comfortable application. The patches demonstrated sustained drug release, extending beyond 24 hours, which is crucial for preserving consistent beneficial levels of rucaparib in the systemic circulation. The optimal formulation, as identified through the BBD using Design Expert software, included HPMC K15 (100 mg), ethyl cellulose (200 mg), and PVP K30 (40 mg). This combination effectively facilitated prolonged drug penetration while keeping the flexibility and integrity of the patches. The study concludes that the formulated transdermal patches using HPMC K15, ethyl cellulose, and PVP K30 offer an effective means for prolonged delivery of DPZ and MMZ. The optimized patches support sustained discharge for a prolonged time, which can improve patient compliance and therapeutic outcomes in treating ovarian cancer. The use of a systematic design approach, such as the BBD, proved beneficial in optimizing the formulation parameters, ensuring the development of high-quality transdermal patches with desirable properties for clinical application.

Optimizing Transdermal Patch Design: A Quality by Design Approach for Dysmenorrhea Relief.

This study explores the potential of transdermal patches as a systemic delivery system for donepezil (DPZ), aiming to circumvent hepatic first-pass metabolism and mitigate oral administration-associated side effects. DPZ, known for its poor solubility and adverse effects, is formulated into transdermal patches using a matrix-type approach with PVP K30 and HPMC K100 polymers alongside dimethyl sulfoxide as a plasticizer. Through solvent casting on a mercury surface, the patches are prepared and assessed for physical properties and drug-excipient interactions using FTIR analysis. The results demonstrate satisfactory physical characteristics, including appearance, weight variation, and tensile strength. Notably, formulations containing HPMC K100 (400 mg) and PVP K30 (300 mg) exhibit enhanced DPZ discharge, signifying their potential as an effective drug delivery system for mitigating DPZ-associated side effects.

Formulation and Evaluation of Sustained Release Dosage Form of Venlafaxine Hydrochloride for Enhanced Treatment of Neurodisorders

In the present study, we have designed and developed a sustained-release tablet formulation of Venlafaxine Hydrochloride. The optimized formulation was then subjected to various evaluation parameters. The formulation of venlafaxine hydrochloride sustained release tablets with a dosage of 500 mg included the utilization of several hydrophilic polymers, including jackfruit mucilage, HPMC K4, and PVPK30, as release retardants. This was done to extend the duration of drug release to 12 hours. The formulation features, including pre-compression and post-compression investigations, were conducted individually according to established protocols. The tablets were determined to be compliant in terms of weight uniformity, hardness, thickness, diameter, friability, and drug content. Separate in-vitro dissolution studies were done for both tablets. The venlafaxine hydrochloride SR formulation F18 was optimized to provide the desired release profile for up to 12 hours. The Venlafaxine Hydrochloride SR formulation was optimized and exhibited zero-order release kinetics. The stability studies conducted under accelerated conditions at a temperature of 40 ± 2°C and a relative humidity of 75 ± 5% yielded good results. The study indicated that the sustained release administration of Venlafaxine HCl is potentially efficacious. It reduces the frequency at which the patient has to take medication and improves patient adherence. Our objective is to conduct in-vivo pharmacokinetic studies of the formulation to verify the drug’s entry into the systemic circulation.

FORMULATION AND EVALUATION COMBINATION OF CARBOPOL/HPMC POLYMER GELS CONTAINING OFLOXACIN FOR OCULAR DRUG DELIVERY SYSTEM

The current research focuses on assessing hydrochloride/HPMC polyethylene blends for uveitis drug delivery. Processes involving polypropylene (PP) matrices have shown similar behavior to solid lipid nanoparticles, with fluid sub-assemblies playing a larger role. Nanoemulsions, with long-chain structures, link drug dispersibility and rheology. The correct combination of polymer matrices is essential for designing an effective ocular drug delivery system.Further studies suggest that polypropylene enhances self-organization, while HPMC K100 improves drug dissolution and viscosity, particularly in formulations involving narcotics. A blend of three polymers has demonstrated effects on drug dissolution, dispersibility, and viscosity.Nanoemulsion-based formulations have shown the best results for drug dissolution and decent rheological properties. Cultured cell investigations indicate that higher levels of specific plastics improve dosage forms. Overall, this research emphasizes the importance of polymer selection and formulation in optimizing drug delivery for uveitis treatment.

Formulation and evaluation of extended-release floating tablets of labetalol hydrochloride 200 mg

The aim of present work is to formulate and evaluate extended-release floating tablets of Labetalol HCL to improve the bioavailability, Patient compliance and solubility on oral floating drug of Labetalol HCL. Labetalol HCL is mainly used in the treatment of hypertension, which is BCS Class Ⅰ drug i.e. Highly soluble and highly permeable. The tablets were prepared by wet granulation method by using different concentrations of HPMC polymer. The tablets were evaluated for Preformulation characteristics, Pre compression parameters and post compression parameters. In-vitro dissolution studies were performed for all prepared formulations by using dissolution test apparatus employing a paddle stirrer at 50 rpm and 37 ± 0.5°C, 0.1N HCL buffer was used as dissolution medium. Samples of 5ml each were withdrawn at different time intervals. Each sample withdrawn was replaced with an equal amount of fresh dissolution medium. Samples were diluted and assayed at 302 nm using Agilent UV Visible double beam spectrophotometer. The increased drug release is due to the presence of low concentration of HPMC K4 m. The drug release kinetics was calculated for all the formulations, among all the formulations F8 was taken as optimized formulation whose percentage drug release was found to be 96%. It indicates the release follows zero order and Hixon kinetics. Hence formulation F8 was Considered as the optimized batch and stability studies were conducted at 40oc±2oc/75±5%RH, Storage condition for 3 months and no change was observed.

Formulation and Evaluation of Bilayered Floating Tablets of Aceclofenac

The objective of this study was to create and assess homogeneous bilayered floating tablets of aceclofenac in order to increase the drug's bioavailability and prolong its stomach release. One of the nonsteroidal anti-inflammatory drugs (NSAID) common side effects is poor solubility and minimal stomach retention, which makes it difficult to treat effectively. As matrix-forming polymers, ten formulations (F1–F10) were made with different amounts of HPMC K15 and additional excipients. Physical properties, buoyancy, in vitro drug release, and kinetic modelling were evaluated for each formulation. With a floating lag time of less than one minute and buoyancy maintained for more than 12 hours, Formulation 5 (F5) showed the most promising findings. With 97.01% of aceclofenac released over 12 hours, it showed a regulated drug release pattern that followed the Korsmeyer-Peppas release model well (R2 = 0.9242). Pre-compression and post-compression values for the optimised formulation F5 were adequate, suggesting good flow characteristics and tablet integrity. FTIR spectroscopy was used to verify the drug-excipient compatibility, guaranteeing stability and the lack of interactions. According to these results, aceclofenac's homogenous bilayered floating tablets, specifically formulation F5, may be able to improve gastric retention time and offer a sustained release profile. This could mean that the medication can be used to treat chronic inflammatory conditions more effectively and with better patient compliance. Keywords: gastric retention, bioavailability, drug excipient compatibility.

Formulation and Evaluation of Transdermal Patches of Metformin Hydrochloride using HPMC K100 as Release Retarding Agent

Formulation and Evaluation of Transdermal Patches of Metformin Hydrochloride using HPMC K100 as Release Retarding Agent

Development of a simple and rapid Formulation and evaluation of Metformin HCl extended-release tablets in comparison with Glucophage® XR

Metformin HCl is the first-line therapy for type 2 diabetes. It is available in both immediate-release and extended-release tablet forms, with the extended-release tablet being more beneficial. In this study, 34 formulations using five sustained-release agents, alone or in combination, were evaluated. The granular flowability, angle of repose, bulk Density, tapped Density, compressibility index, and Hausner ratio were assessed. Furthermore, the compressed tablets were tested for appearance, hardness, friability, and in-vitro drug release. Eleven formulations were evaluated for dissolution profiles according to the standards specified in the United States Pharmacopeia. After calculating the similarity factor (f1) and difference factor (f2), eight formulations were identified for further investigation. The combination of xanthan gum and hypromellose (HPMC K100) demonstrated superior results regarding the sustained-release agent amount and tablet appearance. This noteworthy finding led to continuing the study to explore further formulations with different amounts of xanthan gum and Hypromellose K100. As a result, formulation F34 was identified as the optimal choice because of its higher drug-to-polymer ratio. In conclusion, the final formulation is a rapid, cost-effective, and straightforward method due to the less time required for drying, the amount of sustained-release agents, and the number of components.

To Formulate and Evaluate the Metformin Hydrochloride Floating Tablet

The aim of the research was to create a gastro retentive system for prolonged release of metformin HCl in the proximal part of the gastrointestinal tract (GIT) in the form of an oral floating tablet. Metformin HCl is an antidiabetic biguanide with poor bioavailability and an absorption window in the upper GIT. Floating tablets were prepared using a wet granulation method containing the natural polymers guar gum and kcarrageenan and the synthetic polymer HPMC K100 (HPMC) either alone or in combination. Sodium bicarbonate and citric acid were used as gas generators. Floating tablets were evaluated for weight variation, hardness and friability, drug content, swelling index, in vitro buoyancy and in vitro drug release. The formulation is optimized based on buoyancy, matrix integrity and in vitro drug release in simulated gastric fluid at pH 1.2. A formulation formulated with a combination of 6 wt. % k-carrageenan and 11 wt. % guar gum showed good gel strength, stable and continuous buoyancy for 12 hours, minimal buoyancy delay of 58 seconds, and good matrix integrity during dissolution period. The drug release of the optimized formulation followed the Korsmeyer- Peppas model and the mechanism was non-Fickian/divergent. PXRD and DSC studies showed partial amorphization of the drug. The mechanism of drug release appeared to be a diffusion mechanism. Stability studies have shown that the drug does not degrade when stored for 3 months at 40˚C.

Design of advanced buccal films with kiwiberry extract to prevent oral mucositis: From in vitro buccal models to ex vivo studies

Oral mucositis (OM) is a common side effect of cancer treatments characterized by disruption of the oral mucosa integrity, inflammation, and pain. The treatment strategies to prevent and treat OM are still unsatisfactory, leading to the search of new active compounds, particularly from natural sources, such as Actinidia arguta fruits. A. arguta is a perennial vine and its fruit, commonly known as kiwiberry, has been associated with different therapeutic properties and pro-healthy benefits, particularly antioxidant, anti-inflammatory and anticancer effects. These bioactive properties are due to the fruit outstanding content in phenolic compounds, vitamins, and organic acids, which attracted the researcher's attention for potential application in pharmaceutical industry. The aim of this study is to develop buccal films with A. arguta fruit extract as active ingredient to prevent OM symptoms. The films were prepared by solvent casting after placing 50 g of a buccal film mixture prepared with 1% of HPMC K100 LV EP, 2.5% glycerin, and 100 mL of A. arguta extract as solvent. Different films parameters were assessed, namely physical features (weight: 194.8 mg; thickness: 0.37 mm; disintegration time: 15.05 min; moisture content: 10.53%; swelling capacity: 55.95%), mechanical properties (resistance to extension: 10.11 N; percent of elongation: 36.10%; Young's modulus: 0.0034 MPa) and antioxidant/antiradical activities (TPC = 6.46 mg GAE/g film; FRAP = 49.45 μmol FSE/g film; ABTS = 3.74 mg AAE/g film; DPPH = 4.90 mg TE/g film). In vitro cell assays attested the absence of negative effects on HSC-3 and TR146 oral cell lines. Most important, the compounds release profile were assessed through in vitro and ex vivo models coupled to LC/DAD-ESI-MS quantification and the results revealed high permeation of rutin, quercetin-3-O-glucoside and catechin. Overall, these results highlight the significant potential of buccal films with A. arguta fruit extract to prevent OM condition.

Formulation and optimization of mesoporous silica loaded gel containing extract of Rosmarinus officinalis for treatment of acute wound healing

This study investigate the development and optimization of a mesoporous silica-loaded gel formulated with Rosmarinus officinalis extract, aiming to amplify wound healing capabilities by harnessing the plant's known therapeutic properties alongside the sophisticated drug delivery advantages of mesoporous silica. The formulation process entailed encapsulating the Rosmarinus officinalis extract within mesoporous silica particles before their incorporation into a gel matrix, with particular attention paid to the variable concentrations of Poloxamer 407 and HPMC K15 M to evaluate their effect on the gel's Spreadability and drug release profile. Employing a comprehensive full factorial experimental design analyzed through Design-Expert software, inclusive of ANOVA and 3D surface plotting, the investigation identified batch RF7 as the prime formulation, composed of 14 % w/v Poloxamer 407 and 1 % w/v HPMC K15 M. RF7 precisely matched the predicted Spreadability with an experimental value of 13.6 gm.cm/sec and showcased a promising Cumulative % drug release at 10 h of 87.93 %, closely aligning with a predicted 89.94 %, marking a minimal percentage error of −2.01 %. The study further validated RF7 efficacy through stability and in-vitro antibacterial activity assessments, where it demonstrated significant zones of inhibition against E. coli (22.5 ± 0.87 mm) and S. Aureus (23.4 ± 1.15 mm), nearly paralleling or outperforming the Rosmarinus officinalis extract itself and a marketed standard, Candiderma Plus. These findings, supported by rigorous statistical validation, underscore RF7 enhanced wound healing potential, marrying natural therapeutic virtues with cutting-edge drug delivery technology for a promising advancement in wound care solutions.

Formulation and Evaluation of Verapamil Hydrochloride Sustain Release Tablet

Verapamil hydrochloride, a calcium channel blocker, is used to treat hypertension, supraventricular arrhythmia and myocardial infarction Verapamil hydrochloride (VPH) sustain release tablets were developed for this study in order to maintain plasma concentrations, enhance bioavailability, and avoid repeated dosing. Materials and procedures Tablets containing a fixed amount of VPH were made using the direct compression method and various combinations and ratios of the polymers hydroxypropyl methyl cellulose (HPMC K15) and ethyl cellulose. The tablets were then tested for thickness, weight variation, hardness, uniformity of the drug content, drug release, and potential ingredient interactions. Regarding thickness, weight variation, hardness, and medication content, all tablets were satisfactory. It may be determined from formulations comprising HPMCK15 and ethyl cellulose that the two polymers functioned well together, controlling the first burst and improving the drug's release throughout the first three hours. A study of in vitro drug release followed the formulation of the 32 factorial planned batches. The formulations F5, F6, and F8 demonstrated better drug release up to 24hours and minimal burst release with more than 80% release in 24hours. They were composed of HPMC K15 60mg, 60 mg, and 75mg, respectively, and ethyl cellulose 30mg, 45mg, and 30mg, respectively. Thus, the F5 formulation with somewhat lower polymer content was chosen as the optimal formulation and they contained HPMC K15 60mg and ethyl cellulose 30mg.

DEVELOPMENT, CHARACTERIZATION AND PHARMACOKINETIC EVALUATION OF OPTIMIZED VILDAGLIPTIN SUSTAINED RELEASE MATRIX TABLET USING BOX-BEHNKEN DESIGN

Objective: The principal objective of this research was to develop and optimize cost-effective sustained-release Vildagliptin (VLN) tablets using the wet granulation method. Methods: The tablets were prepared by the non-aqueous wet granulation method. A Box-Behnken design was used to study the effect of the independent variables, i.e., HPMC K100 M, Eudragit RSPO and PVP K30, on the dependent variables swelling index, in vitro drug release at 8 and 12 h. The drug's physiochemical properties were investigated using ultraviolet (UV), Fourier transform infrared (FTIR) and differential scanning calorimetry (DSC). The hardness, thickness, weight variation, content uniformity, swelling index, and in vitro drug release study of the formulated tablets were all evaluated. The optimized formulation Opt-VLD-SR was evaluated for pharmacokinetic parameters like AUC, Cmax, tmax and MRT. Results: The FTIR and DSC studies confirmed that no interaction occurred between the drug, polymers and excipients. The crystalline nature of VLN remained unchanged in the optimised formulation tablet, according to DSC studies. With the optimal concentration of both polymers, formulation Opt-VLN delayed drug release for up to 12 h. The formulated Optimized Sustained-release tablets (Opt-VLD-SR) showed significantly lower Cmax±3.01ng/ml) than conventional IR tablets (256.17±8.02ng/ml). In the pharmacokinetic study, the MRT for Optimized-VLD-SR is (7.40h) showed a better result than the Vildagliptin IR marketed product (3.70 h.), which leads to higher bioavailability of Vildagliptin. Conclusion: Sustained release tablets of VLN with a combination of diffusion and erosion-controlled drug release mechanisms have been successfully developed.

Formulation and Evaluation of Linagliptin Buccal Films

Achieving steady concentration levels of drugs in the plasma for diabetics is important for an extended period. Thestudy focussed on developing mucoadhesive buccal films incorporating linagliptin, aiming to achieve controlled drug delivery foreffective type 2 diabetes management towards steady level plasma concentration. The research utilizes various mucoadhesivepolymers, specifically HPMC K100, HPMC E5LV, and Eudragit RL100, exploring their potential in formulating optimized filmsthrough solvent casting technique. Our primary aim was to identify the most effective formulation, that would ensure controlleddrug release over an extended period. We formulated various formulations and evaluated drug content, swelling index, in-vitrodrug discharge, and ex-vivo mucoadhesive strength. The formulation, incorporated linagliptin, HPMC E5LV, HPMC K100,Eudragit RL100, glycerol, and polyethylene glycol. Results from our comprehensive evaluations showcased favorable dissolutiontime, robust mechanical properties, and impressive mucoadhesive characteristics in the buccal films. The sustained drugdischarge and mucoadhesive strength exhibited by formulation F7 indicate its potential for effective type 2 diabetes managementwith a single film administration lasting up to 8 hours. This research represents a significant step forward in the field ofpharmaceuticals, offering a promising avenue for developing mucoadhesive buccal films to control drug delivery precisely forenhanced therapeutic outcomes in the management of type 2 diabetes.

Design, optimization, and characterization of an in-situ pore-forming system for controlled delivery of paliperidone

The purpose of the current investigation was to develop a pharmaceutical equivalent osmotic drug delivery formulation of Paliperidone (PLD) in the form of controlled porosity osmotic pump tablets (CPOT) in order to keep the drug's steady state concentration in the body. This helps to achieve the greatest therapeutic benefit with the fewest side effects. For the purpose of identifying various formulation attributes, preliminary trials were conducted. Taguchi design was used to study the influence of seven input factors namely drug to polymer ratio, polymer 1(HPMC K100 M) to polymer 2 (HPMC K15 ​M), drug to total osmogens, coating level, amount of pore former, concentration of ethyl cellulose and amount of plasticizer on dependent variable similarity factor (f2). Utilizing the Minitab 17, data analysis was done. The similarity factor (f2) was computed using the osmotic tablet reference product INVEGA®. The findings demonstrate that each of the seven independent variables significantly affects the similarity factor. For optimized batch, both core and coated tablets showed acceptable pharmaco-technical parameters. The release profile of the optimized batch tablets was found to be similar to that of reference product with good zero-order release pattern. Drug release was observed through the channels formed by in-situ pores on tablet surface performed using SEM. From the results it can be concluded that prepared CPOT of PLD was found pharmaceutical equivalent with commercial product which is cost effective and fully compliance with cGMP.

Design and Characterization of Oral Mucoadhesive Buccal Films of Empagliflozin

An anti-diabetic drug called Empagliflozin is used to control blood glucose levels in type 2 diabetics. Due to the high rate of hepatic first pass metabolism, it exhibits limited bioavailability. The current study was done to create Mucoadhesive buccal films of Empagliflozin with the aim of increasing bioavailability, patient compliance, and therapeutic efficacy. The solvent casting process used for the preparation of Empagliflozin Mucoadhesive buccal films by using the Mucoadhesive polymers like HPMC K100 and HEC. The prepared films' evaluated for weight variation, thickness, surface pH, uniformity of the drug content, in-vitro residence time, folding durability, in-vitro release, and permeation investigations were all assessed. Formulations (F1-F4) were created by altering the concentrations of various polymers, with F2 and F4 formulations having the highest polymer ratios and the longest-lasting drug release rates. According to characterization results such as in-vitro dissolution experiments, the sustained release formulation F2, F4 shows the best drug release rate, the order of drug release is F1>F3>F2>F4. It was determined that the films could be chosen for the development of buccal films for effective therapeutic applications because they exhibited effective enlargement, a practicable residence duration, and promising controlled drug release.

Formulation Development and In-Vitro Evaluation of Transferosomal Gel of Mometasone Furoate

The main aim of the study is to formulate and evaluate transferosomal gel formulation for effective topical delivery of Mometasone furoate. The transferosomes was prepared using thin film hydration technique by various proportions of Soya phosphatidylcholine, tween 80. The drug was encapsulated into eight different Transferosomal formulations from F1-F8. The optimized formulation F4 showed small particle size (152.48 nm), entrapment efficiency % EE of 87.16%, zeta potential of -32mV, 0.252 PDI and % Cumulative Drug Release of (97.14%). SEM of optimized Transferosome appeared as spherical, well identified, Unilamellar vesicles. The optimized formulation of Transferosomes was further formulated to transferosomal gel with Carbopol-940 (0.2 to 0.8% w/w), HPMC k15 (0.2 to 0.8% w/w), Propylene glycol, Triethanolamine and Isopropyl alcohol. Among these, F4 formulation with Carbopol-940 0.8%w/w transferosomal gel is the optimized transferosomal gel and showed Spreadability value 0.229±0.01gm.cm/sec, pH value 5.8. The actual drug content of the Transferosomal gel was found to be 98.90%, which represents good content uniformity. The viscosity of optimized Transferosomal gel was found to 55417cps. The percentage drug release for Transferosomal gel was 98.22%. And the formulation was stable throughout the stability studies. This research suggests that Mometasone Furoate loaded transferosomal gel can be potentially used as a transdermal drug delivery system for effective topical delivery.
 Keywords: Mometasone Furoate, Transfersomes, Soya phosphatidyl choline and Tween 80.

Effect of Croscormellose Sodium in Sustained Release Layer of Valsartan in Bilayer Tablet with Clopidogrel as Immediate Drug Release and Valsartan as Sustained Drug Release

The aim of the study was to design and evaluate bilayer tablets of clopidogrel as immediate release and quick relief and valsartan for sustained release and check the effect of croscarmellose sodium (2%) in Carbopol for sustained release action. Bilayer tablets was prepared using direct compression method. Super disintegrants such as Crospovidone, Croscarmellose sodium were evaluated for immediate release of clopidogrel. Polymers HPMC K4, guar gum, ethyl cellulose and carbopol for controlling release of Valsartan. The compressed bilayer tablets were evaluated for weight variation, thickness, hardness, friability, drug content and in vitro drug release in 0.1N HCl and phosphate buffer pH 6.8. All the pre and post compression parameters were found to be within the acceptable limits. The formulations were optimized based on results of dissolution and formulations CF5 for immediate release & VF11 for sustained release. VF11 was formulated with addition of superdisentigrant and showed better controlled release and dissolution similar to VF8. The release kinetics of Valsartan was subject to curve fitting analysis in order to identify the best fit kinetic model. The regression analysis proves that VF11 follow first order release and drug release by diffusion process based on Fick’s law of diffusion. The data for stability studies infer no considerable change in drug content, dissolution rates and other quality control test were within limits.
 Keywords: Bilayer tablets, clopidogrel, valsartan, direct compression method.

Formulation and evaluation of buccal film of an antihypertensive drug

The aim of the study was to formulate and evaluate Losartan potassium buccal films, an angiotensin receptor blocker and is used to treat hypertension. Losartan potassium is having less bioavailability (33%), so the buccal films are expected to increase the bioavailability by avoiding hepatic metabolism. Ten formulations of buccal films were prepared by solvent casting method using HPMC K15 M as the main film-forming polymer in various proportions with various co-polymers such as Eudragit RL. 100, Carbopol 940, Ethyl cellulose. Physicochemical characteristics,in vitro buccal permeation, in vitro release study and residence time were evaluated. In vitro studies revealed that the release rate of Losartan potassium was higher for films containing HPMC K15 M and Eudragit RL100 in 3:1 ratio. The result of stability study indicated that no significant changes have occurredduring the period of study.