Different Grades Of Hydroxypropyl Methylcellulose Research Articles

Development and characterization of bimodal chrono modulated drug delivery of methylphenidate hydrochloride

The study's goal was to develop chrono modulated pulsatile tablets of methylphenidate hydrochloride with an extended-release pattern in the morning and an immediate burst release in the afternoon for exaggerated symptoms of attention deficit hyperactivity disorder match the circadian rhythm of disease, where high levels of l-3, 4-dihydroxyphenylalanine (DOPA) are observed in the afternoon, necessitating higher drug concentrations. The core tablets were made with Kollidon CL-SF as a super disintegrant at 4% and 8% concentrations, with microcrystalline cellulose PH 102 (Pharma grade) and Ludipress as diluents.The core tablets were then compress coated with a slow-release component blend containing different grades of hydroxypropyl methylcellulose (HPMC) at various concentrations of HPMC E50, HPMC E15M, or HPMC E4M, as well as 4% Ethocel. Among all formulations, the F10 formulation containing HPMC E50 at 70% showed the best drug release, with 60% of the dose released slowly over 4 h, followed by an immediate burst of the remaining 40% at the 5th hour. The effect of different diluents on in vitro drug release kinetics and in vitro dissolution studies were performed for all formulations, and A1 formulation containing Cellactose-80 as a diluent showed the best results, with results matching the circadian variations in the disease condition.

Optimization and Quest of HPMC loaded Stavudine Controlled Release Dosage Development by Central Composite Design utilizing Reduced Factorial Screening Technique

The current research focused on screening and finding the significant independent variables in stavudine loaded tablet, followed by optimizing the best formulation using central composite design. The objective of the study to develop stavudine loaded controlled release tablet utilizing reduced factorial design, followed by optimization technique as well as characterization of prepared tablets. Preliminary trial batches were prepared using different grades of hydroxypropyl methylcellulose. The resolution-IV reduced factorial design was selected to screen the significant independent variables in the dosage form design. A total number of eight runs were prepared and responses were recorded. The signified factors identified by half-normal and Pareto chart. The prepared tablets are evaluated for various physiochemical characterizations. Three dependent responses such as hardness, dissolution at 6 hour and 12 hours are considered in optimization process. Later on, drug-polymer interaction study was carried out. The principal of the study design based on finding the best formulation with prefixed set parameter values utilizing the concept of screening technique. It observed that HPMC K15M (57.18 %), HPMC K100 (66.32 %) and PVP K30 (7.97 %) as best composition in a formulation batch would fulfill the predetermined parameter with specific values.

Hydroxypropyl Methylcellulose E15: A Hydrophilic Polymer for Fabrication of Orodispersible Film Using Syringe Extrusion 3D Printer.

Extrusion-based 3D printing technology is a relatively new technique that has a potential for fabricating pharmaceutical products in various dosage forms. It offers many advantages over conventional manufacturing methods, including more accurate drug dosing, which is especially important for the drugs that require exact tailoring (e.g., narrow therapeutic index drugs). In this work, we have successfully fabricated phenytoin-loaded orodispersible films (ODFs) through a syringe extrusion 3D printing technique. Two different grades of hydroxypropyl methylcellulose (HPMC E5 and HPMC E15) were used as the film-forming polymers, and glycerin and propylene glycol were used as plasticizers. The 3D-printed ODFs were physicochemically characterized and evaluated for their mechanical properties and in vitro disintegration time. Then, the optimum printed ODFs showing good mechanical properties and the fastest disintegration time were selected to evaluate their drug content and dissolution profiles. The results showed that phenytoin-loaded E15 ODFs demonstrated superior properties when compared to E5 films. It demonstrated a fast disintegration time in less than 5 s and rapidly dissolved and reached up to 80% of drug release within 10 min. In addition, it also exhibited drug content uniformity within United States Pharmacopeia (USP) acceptable range and exhibited good mechanical properties and flexibility with low puncture strength, low Young’s modulus and high elongation, which allows ease of handling and application. Furthermore, the HPMC E15 printing dispersions with suitable concentrations at 10% w/v exhibited a non-Newtonian (shear-thinning) pseudoplastic behavior along with good extrudability characteristics through the extrusion nozzle. Thus, HPMC E15 can be applied as a 3D printing polymer for a syringe extrusion 3D printer.

Lysozyme Mucoadhesive Tablets Obtained by Freeze-Drying

Lysozyme is particularly attractive for the local treatment of oral pathologies related to microbiological infections. However, the requirement of a prolonged release is difficult to achieve because of saliva swallowing and of the protein denaturation which can occur during production and storage of a dosage form. This work demonstrates the feasibility to prepare lysozyme mucoadhesive tablets by freeze-drying. Tablets were prepared by using alginate (ALG) physically “cross-linked” with calcium ion and different grades of hydroxypropyl methylcellulose (HPMC) (i.e., E5, E50, or K100). The tablets were characterized in terms of swelling or erosion behavior, in vitro mucoadhesive properties, lysozyme activity (Micrococcus lysodeikticus), drug release and ability to inactivate Staphylococcus aureus. The formulations prepared with HPMC K100 were discarded because of the fast erosion. All other formulations allowed a sustained release over at least 6 h. Independently of composition, lysozyme activity (78,311 ± 1873 Units/mg) significantly decreased in the case of tablets containing 5% and 10% w/w of protein (55,000 Units/mg and 33,000 Units/mg, respectively). Conversely, no modifications occurred in the case of tablets containing 1% w/w lysozyme. The formulation prepared by ALG/HPMC E5 7/3 ratio was efficacious against S. aureus. After 3 months of storage at 5 ± 3°C, no significant decrease in lysozyme activity was observed.

Development and radiographical evaluation of floating tablets with combination of Amoxicillin Trihydrate and Ranitidine Hydrochloride

Stomach Specific Floating Tablets (SSFT) with a combination of Amoxicillin-Trihydrate (AT) and Ranitidine Hydrochloride (RH) were developed by using different grades of Hydroxypropylmethylcellulose (HPMCK) (i.e.HPMCK 100M, HPMCK4M and HPMCK15M), to treat patients with H. pylori-infected duodenal ulcer. Floating tablets were prepared by direct compression method, developed formulations were evaluated for different pre-compression and post-compression parameters like angle of repose, compressibility index, hardness, weight variation, floating lag time, content uniformity, and in-vitro drug release. In-Vitro release of two drugs (Amoxicillin-Trihydrate and Ranitidine hydrochloride) from the developed formulation was estimated by the Simultaneous Estimation method (Vierordt's Method). The optimized formulation was subjected to Radio graphical evaluation by incorporating the BaSO4, a radio-opaque substance by replacing a part of the drug from the optimized formulation of into the formulation and then it was administered to the healthy human volunteers to find out the in-vivo residence time. In-vivo X-ray studies were conducted both in fed condition, as well as fasted condition the optimized formulation showed a gastric residence time of more in fed state than that of fasting state. From these studies it was clearly observed that the floating tablets should be given to patients after a standard food and with frequent intake of water.

DEVELOPMENT AND IN VITRO–IN VIVO EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF AN ANTIRETROVIRAL AGENT RITONAVIR

Objective: The present research work concerns the development of the extended release of Ritonavir floating matrix tablets, designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects of irritating drugs.
 Methods: The floating tablets of Ritonavir were prepared by direct compression method using different grades of hydroxypropyl methylcellulose (HPMC), crospovidone, Polyox WSR 303, and sodium bicarbonate, as gas generating agent. Evaluation parameters and in vivo radiographic studies were conducted in suitable model.
 Results: Among all formulations, F21 was chosen as optimized formulation based on evaluation parameters such as floating lag time (33 s), total floating time (>24 h), and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product were shown 98.67% and 91.46±5.02% of drug release, respectively. The main appliance of medication discharge follows zero-order kinetics and non- Fickian transport by coupled diffusion and erosion. In vivo experiments maintained the potentials in extending the gastric residence time in the fasted state in beagle dogs. The mean gastric residence time of the optimized formulation found to be 330 min±40 in the stomach, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for enhanced bioavailability.
 Conclusion: From in vitro and in vivo radiographic studies, Ritonavir floating tablets estimated to provide novel choice for harmless, inexpensive, and extended release for the effective management of AIDS.

Formulation and Evaluation of Nelfinavir Extended Release Trilayer Matrix Tablets by Design of Experiment

The present study was aimed to develop once-daily controlled release trilayer matrix tablets of nelfinavir to achieve zero-order drug release for sustained plasma concentration. Nelfinavir trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVP (Polyvinyl Pyrrolidine) K-30 and MCC (Micro Crystalline Cellulose). Barrier layers were prepared with Polyox WSR-303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 were found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the zero-order and best fitted to Higuchi model. FT-IR studies confirmed that there were no chemical interactions between drug and excipients used in the formulation. These results indicate that the approach used could lead to a successful development of a controlled release formulation of nelfinavir in the management of AIDS.

DESIGN AND IN VIVO EVALUATION OF CONTROLLED RELEASE GLICLAZIDE TRILAYER MATRIX TABLETS IN THE MANAGEMENT OF DIABETES MELLITUS

The purpose of the present study was to develop and optimize multi-layered matrix tablets of Gliclazide trilayer tablets to achieve zero-order drug release for sustained plasma concentration. Gliclazide tablets were prepared by direct compression and consist of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC K 4M, K 15M and K100M), Guar gum and Eudragit L 100. The tablets were also evaluated for physicochemical characteristics and release kinetics. The physicochemical characteristics of the prepared tablets were satisfactory. The developed drug delivery systems showed prolonged drug release rates over a period of 24 h. In vivo bioavailability studies were carried out on the optimized formulation (EF14), mean time to attain peak drug concentration (Tmax) was 6.00 ± 0.14 and 4.02 ± 0.12 h for the optimized and marketed product respectively, while mean maximum drug concentration (Cmax) was 124.80 ± 1.02 ng/ml and 95.12 ± 1.05 ng/ml respectively. AUC0-α and AUC0-t for optimized formulation was significantly higher (p<0.05) as compared to marketed product. A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a controlled release formulation of the drug. The EF14 was shown significant plasma concentration with controlled release and maintained for 24 hours with patient compliance by reducing the dosage frequency, when compared with marketed product in the efficient management of Diabetes mellitus.

GASTRO-FLOATING TABLETS OF REPAGLINIDE: PREPARATION AND IN VIVO EVALUATION

Objective: Current research concerns the expansion of repaglinide matrix floating tablets, which are designed to prolong the gastric residence time, increase the drug bioavailability, and diminish the side effects.Methods: Different formulations of repaglinide floating tablets were prepared with different grades of hydroxypropyl methylcellulose (HPMC) and other agents. Evaluation parameters and in vivo bioavailability studies were conducted in the suitable model.Results: Among all the formulations, F21 containing HPMC K1500 PH PRM, Polyox WSR 303, and sodium bicarbonate, as gas generating agent was selected as optimized formulation based on physicochemical properties, floating lag time (36 s), and total floating time (>24 h). From in vitro dissolution studies, the optimized formulation F21 showed drug release of 98.92±5.19% within 24 h whereas 95.09±5.01% of the drug was released from the marketed product within 1 h.Conclusion: From in vitro and in vivo bioavailability studies repaglinide floating tablets expected to give a new choice for safe, economical, and increased bioavailability for effective management of diabetes mellitus.

DEVELOPMENT AND IN VIVO EVALUATION OF NELFINAVIR EXTENDED RELEASE TRILAYER MATRIX TABLETS IN THE MANAGEMENT OF AIDS

The purpose of this investigation was to design and develop trilayer matrix tablets of Nelfinavir prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropyl methylcellulose (HPMC), PVK K 30 and MCC. Barrier layers are prepared with Polyox WSR 303, Xanthan gum, microcrystalline cellulose and magnesium stearate. Based on the evaluation parameters, drug dissolution profile and release drug kinetics DF8 was found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (DF8) was described by the Zero-order and best fitted to Higuchi model. From in vivo bioavailability studies the extended release of Nelfinavir from trilayer matrix tablets also provides for higher plasma drug content and improved bioavailability. The results indicate that the approach used could lead to a successful development of low biological half life Nelfinavir with controlled drug release in the effective management of AIDS.

Investigate the effect of solvents on wet granulation of microcrystalline cellulose using hydroxypropyl methylcellulose as a binder and evaluation of rheological and thermal characteristics of granules

Wet granulation is the most commonly used technique in the pharmaceutical industry for delivering oral solid dosage forms. In wet granulation, the binder solvent is one of the critical factors affecting granule properties. In the current study, an attempt was made to investigate the effect of solvents (aqueous and hydro-alcoholic) on thermal and flow properties of Microcrystalline Cellulose (MCC) granules prepared using two different grades of Hydroxypropyl Methylcellulose (HPMC), which served as an effective binder. The granulation endpoint was evaluated using thermal effusivity sensor. Rheometer and Modulated Differential Scanning Calorimetry (mDSC) was used to study the flow and thermal properties of wet and dried granules. Furthermore, physical characterization was carried out by granule strength, particle size distribution and tablet hardness for all granules under the study. Thermal effusivity sensor results indicate 55% w/w concentration of binder solution as the endpoint by measuring thermal effusivity for both binders. Additionally, powder rheometer results show that the wet granules of hydro-alcoholic batches show greater resistance to flow whereas the dried granules display excellent flow characteristics as evident from Basic flowability energy values and specific energy values. Permeability results suggest that the granules formed with hydro-alcoholic binder solvent exhibit better porosity and permeability. Tablet hardness data showed that tablets formulated using hydro-alcoholic solvent granules have greater hardness than tablets formulated using water based solvent granules. The granule strength for water based granules is relatively higher than that of hydro-alcoholic based granules. mDSC thermograms show a sharp rise in enthalpy value at 55% w/w binder solution which is indicative of a more significant amount of solvent being present on the surface of granules and formation of optimal granules. To summarize, we have determined a technique to measure endpoint determination and simultaneously investigate the role of solvent systems on the rheology of MCC granules, which could assist in selecting an appropriate solvent system for granulation.

Physicochemical characterisation and in vitro evaluation of modified release matrix tablets: The role of different grades of hydroxypropylmethyl cellulose

The purpose of this work was to formulate prolonged release matrix tablets with water soluble opioid drug (API) using different types of hydroxypropylmethyl cellulose (Methocel) as controlled release polymers. Methocel K100M was incorporated as intra-granular polymer (sample 1) along with Methocel K4M (sample 2) or Methocel K15M (sample 3) as extra-granular polymers. The final blends and tablets prepared by wet granulation process were fully characterized. Results showed that the polymer used extra-granularly significantly affects the tablet properties. By incorporation of Methocel extra granularly (samples 2 and 3), the hardness and tensile strength of the tablets increased and the total tablet porosity decreased. Sample 1, containing only Methocel K100M (intra granularly) has the lowest index of swelling and the fastest release of API probably due to the cross-linking of the polymer chains during the process of wet granulation. Also, the type of Methocel used extra-granularly (with different viscosity grade) was found to significantly affect the swelling ratio of the designed matrix systems and the drug release behavior. Sample 2 containing Methocel K4M extra-granularly has a lower index of swelling and faster release of API compared to sample 3. Considering the release mechanism, release data showed best fitting to the heuristic model proposed by Korsmeyer-Peppas. Two additional approaches were used for mathematical modeling of the release data in order to make them directly applicable for our experimental results. Keywords: matrix tablet, water soluble opioid drug, prolonged release, HPMC (Methocel)

Formulation And In Vitro/In Vivo Evaluation Of Olmesartan Medoxomil Solid Dispersions Incorporated E/R Trilayer Matrix Tablets By Geomatrix

<p>An attempt has been made to develop and optimize an novel anti hypertensive trilayered controlled release matrix tablets incorporated with Olmesartan medoxomil solid dispersion prepared by direct compression and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), guar gum, ethyl cellulose. Upper and lower layers are prepared with Carnauba wax, guar gum and sodium CMC. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo bioavailability studies were carried out with the optimized formulation (HF14) and reference standard A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a trilayer extended release formulation up to 24h. These results also demonstrated that the Olmesartan solid dispersion incorporated trilayer tablets shown more bioavailability because of its conversion from crystalline to amorphous form.</p>

In Vitro - In Vivo Evaluation Of E/R Trilayer Matrix Tablets Containing Solid Dispersion Of Atorvastatin

<p>Investigation of <em>in vitro/in vivo</em> behaviour of extended release tablets containing solid dispersions of Atorvastatin is the focus of the present research work. Atorvastatin trilayer matrix tablets were prepared by direct compression method and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), ethyl cellulose and Carbopol 934P. Barrier layers are prepared with hydrophobic polymers carnauba wax and xanthan gum. Based on the evaluation parameters, drug dissolution profile and release order kinetics HF16 was found to be optimized formulation. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF16) was described by the Zero-order and best fitted to Higuchi model. FTIR confirmed that there was no chemical interaction between drug and excipients used in the formulation. . In vivo bioavailability studies were conducted for optimized formulation HF16 and reference standard. The optimized formulation of Atorvastatin trilayer matrix tablet was shown significant plasma concentration with extended release and maintained for 24 hrs with patient compliance by reducing the dosage frequency, when compared with reference standard. </p>

Hydroxypropylmethyl cellulose‐based sponges loaded self‐microemulsifying curcumin: Preparation, characterization, and in vivo oral absorption studies

ABSTRACTNovel hydroxypropylmethyl cellulose (HPMC)‐based sponges containing self‐microemulsifying curcumin (SME‐Cur) were prepared by a freeze drying method using different grades of HPMC (E5 LV, E15 LV, E50 LV, A15 LV, and A4C). The physical properties and drug release from these carriers were characterized and compared among the different formulations. The mean pore size values of the sponges from image analysis ranged from 43.36 ± 4.54 to 123.22 ± 8.19 nm. An increase in the concentration or viscosity of the HPMC, resulted in denser sponges and a slower drug release. The average microemulsion droplet size from the optimal sponge formulation was 34.80 ± 0.1 nm, and the curcumin was almost completely released within 120 min. The AUC after oral administration of the liquid and solid SME‐Cur were 7‐ and 5‐fold greater than that of the curcumin powder in the rabbit, respectively. The results demonstrated that the HPMC‐based sponges loaded with SME‐Cur could be efficiently used to enhance the oral bioavailability and might be useful as they could be administered at a lower dose compared to normal curcumin powder. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2016, 133, 42966.

Formulation and optimization of mucoadhesive buccal patches of losartan potassium by using response surface methodology.

Background:This study was undertaken with an aim to systematically design a model of factors that would yield an optimized sustained release dosage form of an anti-hypertensive agent, losartan potassium, using response surface methodology (RSM) by employing 32 full factorial design.Materials and Methods:Mucoadhesive buccal patches were prepared using different grades of hydroxypropyl methylcellulose (HPMC) (K4M and K100M) and polyvinylpyrrolidone-K30 by solvent casting method. The amount of the release retardant polymers – HPMC K4M (X1) and HPMC K100M (X2) was taken as an independent variable. The dependent variables were the burst release in 30 min (Y1), cumulative percentage release of drug after 8 h (Y2) and swelling index (Y3) of the patches. In vitro release and swelling studies were carried out and the data were fitted to kinetic equations.Results:The physicochemical, bioadhesive, and swelling properties of patches were found to vary significantly depending on the viscosity of the polymers and their combination. Patches showed an initial burst release preceding a more gradual sustained release phase following a nonfickian diffusion process.Discussion:The results indicate that suitable bioadhesive buccal patches with desired permeability could be prepared, facilitated with the RSM.

Novel sustained release and swellable gastroretentive dosage form for ciprofloxacin hydrochloride.

Introduction:The present study aims at developing a gastroretentive swellable and floating matrix tablet formulation of ciprofloxacin hydrochloride (HCl) for the effective treatment of infections caused by susceptible organisms. Ciprofloxacin HCl is a fluoroquinoline antibiotic drug. Ciprofloxacin HCl is more stable in acidic medium and it has a narrow absorption window which is sited at the stomach and proximal portions of the small intestine, so it covers the required criteria for selection of drug for gastroretentive dosage form.Materials and Methods:Ciprofloxacin HCl gastroretentive tablets were formulated by using direct compression method and different grades of hydroxypropyl methylcellulose as suspending and stabilizing agent (polymer), sodium starch glycolate (SSG), crospovidone as disintegrates, sodium bicarbonate as alkalizing agent and magnesium stearate as lubricant.Results:The tablets were evaluated for post compression parameters. All the parameters were within the pharmacopoeial limits.Conclusion:The in vitro dissolution studies showed that the drug release was fast in formulations F2, F4 and F6 containing SSG as super disintegrant when compared with all other formulations. In SEM study of F2 formulation shows maximum swelling and porosity observed after 12 h. Hence, formulation F2 shows the best formulation among the six formulations containing different binders and super disintegrants.

A formulation approach for development of HPMC-based sustained release tablets for tolterodine tartrate with a low release variation

Objective: The purpose of this study was to develop hydroxypropylmethylcellulose (HPMC)-based sustained release (SR) tablets for tolterodine tartrate with a low drug release variation.Methods: The SR tablets were prepared by formulating a combination of different grades of HPMC as the gelling agents. The comparative dissolution study for the HPMC-based SR tablet as a test and Detrusitol® SR capsule as a reference was carried out, and the bioequivalence study of the two products was also conducted in human volunteers.Results: The amount of HPMC, the grade of HPMC and the combination ratio of different grades of HPMC had remarkable effects on drug release from the SR tablets. Both the test and reference products had no significant difference in terms of comparative dissolution patterns in four different media (f2 > 50). Furthermore, the dissolution method and rotation speed showed no effects on the drug release from the two products. The 90% confidence intervals of the AUC0–36 and Cmax ratios for the test and reference products were within the acceptable bioequivalence intervals of log0.8–log1.25.Conclusions: A HPMC-based SR tablet for tolterodine tartrate with a low release variation was successfully developed, which was bioequivalent to Detrusitol® SR capsule.

Statistical design of experiments on fabrication of bilayer tablet of narrow absorption window drug: Development and In vitro characterisation

The current study involves the fabrication of oral bioadhesive bilayer matrices of narrow absorption window drug baclofen and the optimisation of their in vitro drug release and characterisation. Statistical design of experiments, a computer-aided optimisation technique, was used to identify critical factors, their interactions and ideal process conditions that accomplish the targeted response(s). A central composite design was employed to systematically optimise the drug delivery containing a polymer, filler and compression force. The values of ratio of different grades of hydroxypropyl methylcellulose, microcrystalline cellulose and compression force were varied to be fitted in design. Drug release at 1 h (Q1), 4 h (Q4), 8 h (Q8), 12 h (Q12), and hardness were taken as responses. Tablets were prepared by direct compression methods. The compressed tablets were evaluated for their hardness, weight variation, friability, content uniformity and diameter. Counter plots were drawn and optimum formulation was selected by desirability function. The formulations were checked for their ex vivo mucoadhesion. The experimental value of Q1, Q4, Q8, Q12 and hardness for check-point batch was found to be 31.64, 45.82, 73.27, 98.95% and 4.4 kg/cm2, respectively. The release profile indicates Highuchi kinetics (Fickian transport) mechanism. The results of the statistical analysis of the data demonstrated significant interactions amongst the formulation variables, and the desirability function was demonstrated to be a powerful tool to predict the optimal formulation for the bilayer tablet.

Mucoadhesive buccal films of glibenclamide: Development and evaluation

Background:Glibenclamide is an oral hypoglycemic drug completely metabolized in the liver, the principal metabolite being very weakly active, buccal delivery may be useful for the treatment of diabetes more effectively. The aim of the present study was to design formulations and systematically evaluate in vitro and ex vivo performances of buccal films of glibenclamide so that the required therapeutic plasma concentrations can possibly be achieved more rapidly using the different grades of hydroxypropyl methyl cellulose (HPMC) as the base matrix.Materials and Methods:Mucoadhesive buccal films of glibenclamide were prepared by solvent casting technique using different grades of HPMC with different ratios. Prepared films were evaluated for weight, thickness, surface pH, swelling index (SI), folding endurance, drug content uniformity, in vitro release, and ex vivo permeation studies.Results:The film thickness and weight were in the range of 0.213–0.4892mm and 22.25–39.83 mg, respectively. The films exhibited controlled release over more than 6 h. HPMC, HPMCK100, and HPMC3000 films exhibited satisfactory swelling. Surface pH of buccal films was found to be 6.4–6.8. SI observed to be highest for GF12 (275.3 ± 12.17) and lowest for GF1 (173.5 ± 5.65). The films exhibited controlled release over more than 6 h. HPMC exhibited satisfactory swelling, an optimum residence time, and promising drug release. The Higuchi plots were found to be linear with correlation coefficient values of 0.8933, 0.9138, and 0.9947 for GF4, GF8, and GF9, respectively.Conclusions:Among all the formulations, GF9 shows good controlled release results correlated with ex vivo permeation studies.