Hydroxypropyl Methylcellulose Concentration Research Articles

New formulation and approach for mucoadhesive buccal film of rizatriptan benzoate

Mucoadhesive buccal film is developed as a promising dosage form, which has prominent advantages because of drug delivery through buccal mucosa. New formulation of buccal films containing rizatriptan benzoate (RB) was prepared by solvent casting method using various concentrations of hydroxypropyl methylcellulose (HPMC K4M), polyvinyl alcohol (PVA), polyethylene oxide (PEO), glycerol, stevia, and goat buccal mucosa used as a model membrane. In this work, the effect of polymers and plasticizer concentrations on drug release profile, disintegration and dissolution time, mechanical properties, and mucoadhesive characteristics of films was studied. Scanning electron microscopy analysis revealed uniform distribution of RB in film formulations. Chemical compounds and thermal analysis of the films were studied by Fourier transform infrared spectroscopy and differential scanning calorimetry, respectively. The buccal films produced were uniform in drug content and thickness. All formulations have in vitro release of 98–102% between 40 and 80 min. Also ex vivo mucoadhesion strength was in the range of 0.205 ± 0.035 to 0.790 ± 0.014 N for all formulations. A formulation consisting RB (50 mg), HPMC K4M, PVA, and PEO (63 mg), glycerol (1.5 ml), stevia (5 mg) was selected as our optimum composition. More satisfactory results were obtained in terms of disintegration and dissolution time, mechanical properties, and mucoadhesive characteristics. In addition, it showed about 99.89% RB released in 45 min. The results suggest that RB-loaded mucoadhesive buccal films could be a potential candidate to achieve optimum drug release for effective treatment of migraine.

Influence of solution properties and pH on the fabrication of electrospun lentil flour/HPMC blend nanofibers

Electrospinning is a method used in fiber production in which an electric force is applied to create jets of charged polymer solutions. The objective of this study was to obtain homogeneous nanofibers from lentil flour and hydroxypropyl methylcellulose (HPMC) blend by using electrospinning method. Distilled water was used as solvent. The effects of pH (7, 10 and 12), lentil flour concentration (1% and 2% (w/v)) and HPMC concentration (0.25%, 0.5% and 1% (w/v)) on solution properties and fiber morphology were investigated. When the pH was increased, the viscosity of the solutions containing 1% and 2% lentil flour decreased. Increasing the pH values caused an increase in the electrical conductivity. At pH value of 7, homogeneous nanofibers could not be obtained whereas fibers were perfectly homogeneous at alkaline pH values. Nanofiber diameter decreased with increase in pH when 2% lentil flour was used. On the other hand, diameter of fibers did not show any significant change with pH for 1% lentil flour. When the lentil flour concentration was increased, viscosity and fiber diameter increased at pH10. When HPMC concentration was increased, both viscosity and fiber diameter increased but electrical conductivity did not show any significant change. Average fiber diameters ranged between 198±4 and 254±5nm for solutions prepared with different lentil flour and HPMC concentrations at different pH values.

Macro-micro structure characterization and molecular properties of emulsion-templated polysaccharide oleogels

Emulsion and oleogels prepared at a constant xanthan gum (XG) concentration of 0.3 wt%, and varying hydroxypropyl methyl cellulose (HPMC) concentration of 0.2, 0.4, 0.6, 0.8 and 1.0 wt% were evaluated for their macro-micro structure and molecular properties, respectively. Rheological behaviors of the emulsions and oleogels were tested for their gel strength. Oil loss of the oleogel was measured to evaluate their oil binding capacity. Polarizing light microscope (PLM) and scanning electron microscope (SEM) were used to investigate the microstructure of the samples. Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD) measurements were used to further understand the structure of the oleogels. Macro properties and microstructure of the samples were linked with each other, and HPMC concentration had a prominent effect on the microstructure and rheological properties of the emulsions, dried products and oleogels. Higher concentration of HPMC resulted in more stable emulsion with higher mechanical strength, hard dried products with more compact network, and oleogels with higher mechanical strength and better oil binding capacity. The effect of HPMC concentration on the properties of samples was irrelevant to the viscosity of HPMC. The oleogel prepared was a physical gel, and intramolecular or intermolecular hydrogen bonding presented in the oleogel contributed to its relatively orderly structure with liquid oil trapped in it. The oil droplets were coated by the hard layer formed by polysaccharides. This research gave more information about polymer based oleogels and provided a reference for their application.

Development of a Video-Microscopic Tool To Evaluate the Precipitation Kinetics of Poorly Water Soluble Drugs: A Case Study with Tadalafil and HPMC.

Many drug candidates today have a low aqueous solubility and, hence, may show a low oral bioavailability, presenting a major formulation and drug delivery challenge. One way to increase the bioavailability of these drugs is to use a supersaturating drug delivery strategy. The aim of this study was to develop a video-microscopic method, to evaluate the effect of a precipitation inhibitor on supersaturated solutions of the poorly soluble drug tadalafil, using a novel video-microscopic small scale setup. Based on preliminary studies, a degree of supersaturation of 29 was chosen for the supersaturation studies with tadalafil in FaSSIF. Different amounts of hydroxypropyl methyl cellulose (HPMC) were predissolved in FaSSIF to give four different concentrations, and the supersaturated system was then created using a solvent shift method. Precipitation of tadalafil from the supersaturated solutions was monitored by video-microscopy as a function of time. Single-particle analysis was possible using commercially available software; however, to investigate the entire population of precipitating particles (i.e., their number and area covered in the field of view), an image analysis algorithm was developed (multiparticle analysis). The induction time for precipitation of tadalafil in FaSSIF was significantly prolonged by adding 0.01% (w/v) HPMC to FaSSIF, and the maximum inhibition was reached at 0.1% (w/v) HPMC, after which additional HPMC did not further increase the induction time. The single-particle and multiparticle analyses yielded the same ranking of the HPMC concentrations, regarding the inhibitory effect on precipitation. The developed small scale method to assess the effect of precipitation inhibitors can speed up the process of choosing the right precipitation inhibitor and the concentration to be used.

Design, Preparation and Evaluation of HPMC-Based PAA or SA Freeze-Dried Scaffolds for Vaginal Delivery of Fluconazole.

Aim of this work was preparation of bioadhesive gel formulations based on Hydroxypropyl methylcellulose (HPMC), Poly(acrylic acid) (PAA) or Sodium alginate (SA) loaded with anise/fluconazole β-cyclodextrin inclusion complexes in 1:2 and 1:3 ratios intended for vaginal applications. Freeze-drying method was effectively utilized and superporous morphology was obtained. The superporous morphology of the lyophilized gels, dynamic water vapor sorption measurements, drug release kinetics studies and their antimicrobial activities are presented. HPMC content influences especially the sorption/desorption behaviour of HPMC-based PAA gels and the morphology of the gel formulations with fluconazole/β-cyclodextrin inclusion complexes, due to the interactions among the gel networks absorbing water molecules. It was found that fluconazole release kinetics correspond to quasi-Fickian, Fickian diffusion and non-Fickian mechanisms for the studied hydrogels. The tested vaginal formulations with β-cyclodextrin inclusion complexes exhibited selectivity toward S. aureus ATCC 25923 and all tested Candida strains in comparison with the gel formulation without β-cyclodextrin. The fluconazole/β cyclodextrin inclusion complexes ensure a controlled release of fluconazole over a few days, the highest amount of drug release (92%) being observed after 43h. These bioadhesive gel formulations could be very promising topical alternative for treatment of vaginal fungal infections.

Swelling and mass transport properties of nanocellulose-HPMC composite films

Composite films were sprayed from mixtures of water soluble hydroxypropyl methylcellulose (HPMC) and either nanofibrillated cellulose (NFC) or cellulose nanocrystals (CNC). Fiber diameter was similar for both nanocelluloses but fiber length was several μm for NFC and about 200nm for CNC. Films were characterized for morphology, swelling, mass loss and transport properties. NFC-HPMC films swelled less than CNC-HPMC films; with a HPMC content of 20wt% NFC-HPMC and CNC-HPMC films presented swelling of 7 and 75g/g, respectively. The swelling strongly influenced water transport across the films, with slower transport for CNC-based materials compared to NFC-based materials. The properties of NFC-based films were comparable to previous results using microfibrillated cellulose (MFC) with heterogeneous structural content and fiber lengths of ~10μm. The findings have implications for using nanocellulose to modulate material properties in wet-state applications, with effects being in strong contrast when using as a hardening filler in dry materials.

In Vitro and In Vivo Modeling of Hydroxypropyl Methylcellulose (HPMC) Matrix Tablet Erosion Under Fasting and Postprandial Status

PurposeTo develop a model linking in vitro and in vivo erosion of extended release tablets under fasting and postprandial status.MethodsA nonlinear mixed-effects model was developed from the in vitro erosion profiles of four hydroxypropyl methylcellulose (HPMC) matrix tablets studied under a range of experimental conditions. The model was used to predict in vivo erosion of the HPMC matrix tablets in different locations of the gastrointestinal tract, determined by magnetic marker monitoring. In each gastrointestinal segment the pH was set to physiological values and mechanical stress was estimated in USP2 apparatus rotation speed equivalent.ResultsErosion was best described by a Michaelis–Menten type model. The maximal HPMC release rate (VMAX) was affected by pH, mechanical stress, HPMC and calcium hydrogen phosphate content. The amount of HPMC left at which the release rate is half of VMAX depended on pH and calcium hydrogen phosphate. Mechanical stress was estimated for stomach (39.5 rpm), proximal (93.3 rpm) and distal (31.1 rpm) small intestine and colon (9.99 rpm).ConclusionsThe in silico model accurately predicted the erosion profiles of HPMC matrix tablets under fasting and postprandial status and can be used to facilitate future development of extended release tablets.

Characterization of oral disintegrating film of peanut skin extract—Potential route for buccal delivery of phenolic compounds

This paper aimed to develop and characterize oral disintegrating films (ODF) based on gelatin and hydroxypropyl methylcellulose (HPMC) incorporated with peanut skin extract (PSE) as phenolic compounds vehicle. Films were prepared by casting technique varying the polymer ratio (GEL:HPMC 100:0, 25:75, 50:50, 75:25, 0:100) and PSE concentration (20 and 30g/100g film-forming solution). Formulations with high content of gelatin presented insoluble complex possibly due to cross-linking between gelatin and polyphenols. For formulations which gelatin was in a minority or equal concentration of HPMC, the increase in the PSE concentration favored the association of rich phases in gelatin and HPMC. This also increased inter- and intramolecular bonding which led to a more compact matrix and reduction of films elongation and tensile strength around 45%. The HPMC film with PSE (20%) presented tensile strength of 26.63±1.89MPa, elongation of 4.97±0.41%, contact angle of 67.17±0.41° and disintegration time of 17.87±1.77s. In the in vitro release profile, 80% of phenolics were released in 5min, and in accelerated stability test the films retained 60% of the total phenolic compounds. HPMC-based film can be a good alternative to vehicle the active compounds present in peanut skin.

Poly vinyl acetate and ammonio methacrylate copolymer as unconventional polymer blends increase the mechanical robustness of HPMC matrix tablets

The objective was to investigate poly vinyl acetate (Kollicoat® SR 30 D) and ammonio methacrylate copolymer (Eudragit® RL 30 D) blends as coatings to increase the mechanical robustness of hydroxypropyl methylcellulose (HPMC) matrix tablets. Poly vinyl acetate (Kollicoat® SR 30 D – KSR) was selected for its flexibility and ammonio methacrylate copolymer (Eudragit® RL 30 D – ERL) because of its high permeability. Films based on KSR:ERL blends were prepared by casting or spraying aqueous dispersions of these polymers and were characterized by water uptake, dry mass loss and mechanical properties. KSR:ERL blends were investigated as coating materials to improve the robustness, mechanical strength and drug release from the HPMC matrix tablets containing propranolol HCl, caffeine and carbamazepine as model drugs. Both HPMC and the polymer coating affected the propranolol release. The release and the mechanical properties could be easily adjusted by varying the polymer blend ratio. The flexibility increased with increasing KSR content. At an 8% w/w coating level, a force of 3.2N was required to rupture the coating of the swollen tablet after 16h in the release medium; the coated tablets were thus robust to withstand gastrointestinal forces. The coating level (6%–10%, w/w) and dissolution agitation rate (50rpm to 150rpm) had no effect on the drug release. The water-insoluble carbamazepine was not released from the coated tablets as HPMC erosion, which is necessary for the release of a poorly water-soluble drug was hindered by the coating. The release of the water-soluble propranolol increased with increasing drug content and decreased with increasing HPMC content. ConclusionPoly vinyl acetate and ammonio methacrylate copolymer could be a proper polymer blend for coating HPMC matrix tablets to increase mechanical robustness, which characterized by its flexibility and permeability.

Assessment of Photodynamic Inactivation against Periodontal Bacteria Mediated by a Chitosan Hydrogel in a 3D Gingival Model.

Chitosan hydrogels containing hydroxypropyl methylcellulose (HPMC) and toluidine blue O were prepared and assessed for their mucoadhesive property and antimicrobial efficacy of photodynamic inactivation (PDI). Increased HPMC content in the hydrogels resulted in increased mucoadhesiveness. Furthermore, we developed a simple In Vitro 3D gingival model resembling the oral periodontal pocket to culture the biofilms of Staphylococcus aureus (S. aureus), Aggregatibacter actinomycetemcomitans (A. actinomycetemcomitans), and Porphyromonas gingivalis (P. gingivalis). The PDI efficacy of chitosan hydrogel was examined against periodontal biofilms cultured in this 3D gingival model. We found that the PDI effectiveness was limited due to leaving some of the innermost bacteria alive at the non-illuminated site. Using this 3D gingival model, we further optimized PDI procedures with various adjustments of light energy and irradiation sites. The PDI efficacy of the chitosan hydrogel against periodontal biofilms can significantly improve via four sides of irradiation. In conclusion, this study not only showed the clinical applicability of this chitosan hydrogel but also the importance of the light irradiation pattern in performing PDI for periodontal disease.

Development and optimization of pluronic® F127 and HPMC based thermosensitive gel for the skin delivery of metoprolol succinate

The aim of the present investigation was to prepare and optimize suitable combination of polymers hydroxypropyl methylcellulose (HPMC) and pluronic® F127 (PN F127) for the development of thermosensitive gel of Metoprolol succinate (MS) using central composite design (CCD). The effect of formulation factors (concentration of HPMC and PN F127) on responses such as cumulative percentage release (CPR) of MS, bioadhesive force (BF) and viscosity was measured statistically. Quadratic model was found to be best fit model among different models used in the study. The optimum conditions were found to be 0.92% of HPMC and 15% of PN F127. Under these conditions, the predicted CPR, BF and viscosity were found to be 84.94 μg/cm2, 41.56 gf and 48.94 Pa s, respectively. Ex vivo permeation of MS from optimized thermosensitive gel across abdominal skin of rat demonstrated highest flux (64.35 μg/cm2/h) for the gel formulation containing 1,8-cineole (5% w/w). The hypotensive activity was performed on normotensive rabbits and the results showed that the optimized formulation prolonged the activity up to 12 h. The above findings indicated that thermosensitive gel of MS for skin application exhibited strong potential against hypertension and expected to provide a better alternative to oral MS formulations.

Development and In vitro Evaluation of Mucoadhesive Buccal Films of Nebivolol.

Nebivolol, a cardioselective β-blocker undergoes extensive metabolism in the liver after its oral administration resulting in low bioavailability. Oral administration of nebivolol also causes gastrointestinal disturbances characterised by stomach ache. To overcome these short comings, mucoadhesive buccal films of nebivolol were prepared using different concentrations of hydroxypropyl methylcellulose and hydroxyl ethylcellulose in the ratios of 2:1, 4:1 and 6:1 and hydroxypropyl methylcellulose and methylcellulose in the ratio of 2:2, 4:3 and 6:4 by solvent casting technique. All the prepared films were found to be smooth, elegant and uniform in thickness and weight. Among the three polymer combinations used, 6:4 (BFN6) showed increased in vitro residence time, which appeared to be mainly due to mucoadhesive nature of hydroxylpropyl methylcellulose and methylcellulose. Evaluation of the films showed uniform dispersion of the drug throughout the formulation (96.21±0.71 to 97.02±0.12%). In vitro drug release studies showed better results at the end of 8 h. The release profile of all the formulations was subjected to kinetic analyses, which suggested that the drug was released by diffusion mechanism following super case-II transport.

A study on the effect of the polymeric additive HPMC on morphology and polymorphism of ortho-aminobenzoic acid crystals

In the present study, the effect of Hydroxy Propyl Methyl Cellulose (HPMC) on the crystallization of ortho-aminobenzoic acid (OABA) was investigated by seeded and unseeded cooling crystallization experiments. The influence of HPMC on the induction time, crystal shape of Forms I and II of OABA and the polymorphic transformation time was studied. Furthermore, the capability of HPMC to inhibit growth of Form I was evaluated quantitatively and modeled using population balance equations (PBE) solved with the method of moments. The additive was found to strongly inhibit nucleation and growth of Form I as well as to increase the time for the polymorphic transformation from Form II to I. Solvent was also found to influence the shape of Form I crystals at equal concentrations of HPMC. In situ process analytical technology (PAT) tools, including Raman spectroscopy, focused beam reflectance measurement (FBRM) and attenuated total reflectance (ATR) UV–vis spectroscopy were used in combination with off-line techniques, such as optical microscopy, scanning electron microscopy (SEM), Raman spectroscopy, Malvern Mastersizer and differential scanning calorimetry (DSC) to study the crystals produced. The results illustrate how shape, size and stability of the two polymorphs of OABA can be controlled and tailored using a polymeric additive.

Gelatin-hydroxypropyl methylcellulose water-in-water emulsions as a new bio-based packaging material

Gelatin and hydroxypropyl methylcellulose (HPMC) are two incompatible and immiscible biopolymers which cannot form homogeneous composite films using usual methods. In this study, to prevent phase separation, gelatin-HPMC water-in-water (W/W) emulsion was utilized to from transparent composite films by entrapment the HPMC dispersed droplets in gelatin continuous network. The physicochemical and mechanical properties of emulsion-based films containing different amounts (5–30%) of dispersed phase were determined and compared with those of individual polymer-based films. Incorporating HPMC into W/W emulsion-based films had no significant effect on the tensile strength. The flexibility of composite films decreased at HPMC concentrations below 20%. The depletion layer at the droplets interface reduced the diffusion of water vapor molecules because of its hydrophobic nature, so the water vapor permeability remained constant. Increasing the HPMC content in the emulsion films increased the swelling and decreased the transparency. The entrapment of HPMC in continuous gelatin phase decreased its solubility. Therefore, W/W emulsions are capable of holding two incompatible polymers alongside each other within a homogeneous film network without weakening the physical properties.

Aqueous tape casting of B4C ceramics

B4C green tapes are prepared by aqueous tape casting and a spark plasma sintering (SPS) process using polyethylenimine (PEI) as dispersant, hydroxypropyl methyl cellulose (HPMC) as binder and polyethylene glycol (PEG) as plasticiser. The influences of solid content, dispersant content, mass ratio of plasticiser to binder (R value) and milling time on the slurry viscosity are studied. The samples are characterised by means of hardness tester, universal testing machine and scanning electron microscopy. The results indicate that the solid content of B4C slurry achieves 47.5 wt-% with milling time of 12 h when the content of PEI, HPMC and PEG is 1.5, 5 and 5 wt-%, respectively. The relative density of B4C ceramics subject to SPS at 1600°C and 50 MPa for 8 min is up to 97.2%. The Vickers hardness, flexural strength and fracture toughness of B4C ceramics reach 36.5 ± 0.7 GPa, 510.3 ± 19.4 MPa and 5.04 ± 0.29 MPa m−1/2, respectively.

Formulation and Evaluation of Dexibuprofen Transdermal Films in Rabbits

Dexibuprofen is a practically water-insoluble nonsterodial anti-inflammatory drug. Following previous experience on enhancing the solubility of the drug, a mixed hydrotropic solubilization technique was here applied in order to improve the aqueous solubility of the drug so that a soluble form of dexibuprofen was prepared and then could be used as a main active ingredient in transdermal films. Nine formulae were prepared applying 32 full factorial design using different amounts of hydroxypropylmethylcellulose (HPMC) and polyvinylpyrrolidone K30 (PVP K30). The prepared formulae were evaluated for their physical properties, loading efficacy and In-vitro dissolution studies adopting the USP XXII dissolution method type V paddle over disk apparatus method. Permeation studies were done for best three films showing higher dissolution rate using Franz cell apparatus and also bioavailability study was carried out on the best formula to compare the absorption of dexibuprofen from the prepared film (treatment A) to commercial tablets (treatment B) following administration of a single dose to rabbits. The prepared films were off-white color, opaque, smooth, moist and non-sticky. Increasing the amounts of HPMC and PVP K30 lead to increasing weight, folding endurance, tensile strength, moisture content and moisture absorption. Transdermal films containing higher concentrations of PVP K30 and lower concentration of HPMC showed higher rate and amount of dexibuprofen released from dissolution medium and Franz cell. The bioavailability study showed that (Tmax) in treatments A and B is 3 hours and 2 hours respectively. The average peak plasma concentration values (Cmax) were 28.98±3.36 and 34.67±0.61 ug/mL, respectively and the AUC0-∞ values were 145.82±13.09 and 117.44±3.15 µg·h/mL, respectively. There were significant differences between treatments A and B in Cmax, t(1/2)ab, Kel, t(1/2)el, TCR, AUC0-8, AUC0-∞, AUMC0-8, AUMC0-∞, and MRT. While the difference was insignificant in Kab.

Design and Evaluation of Buccal Patch Containing Combination of Hydrochlorothiazide and Lisinopril

Purpose: The objective of the present study was to formulate and evaluate buccal patches containing combination of lisinopril (LP) and hydrochlorothiazide (HCZ). Approach: Films were fabricated by solvent casting method, using combination of mucoadhesive polymers such as hydroxypropylmethyl cellulose (HPMC), hydroxypropyl cellulose (HPC), polyvinyl alcohol (PVA) and polyvinyl pyrolidone (PVP) and ethyl cellulose (EC) as backing layer. The patches were evaluated for physicochemical characteristics such as weight, thickness, surface pH, folding endurance, bioadhesive strength, swelling index, drug content, tensile strength, elongation at break, mucoadhesion time, in vitro and ex vivo drug permeation. Results: The IR spectra showed no interaction between drug and polymer. Physicochemical characteristics of all the samples were found to be satisfactory. Swelling of the films increased with increasing content of HPMC or HPC and PVP. Bioadhesive force, tensile strength, percentage elongation and mucoadhesion time increased with higher proportions of HPMC, HPC and PVA. In vitro drug release studies demonstrated slower release of both drugs in formulations with higher amount of HPMC, HPC and PVA. The in vitro drug release data of most formulations best fitted first order model, except for the formulations FA3 and FC. Ex vivo drug permeation studies of formulations through porcine buccal mucosa showed similar results as in vitro. Conclusion: Buccal delivery of this combination can resolve the drawbacks like incomplete absorption in the gut thereby possible improvement in bioavailability, apart from controlled release of the drugs.

Design, Formulation and Evaluation of Atenolol Gastro Retentive Floating Tablets

The main objective of present research work is to formulate the floating tablets of atenolol using 32 factorial design. Atenolol, β-blocker belongs to Biopharmaceutical Classification System Class-III. The floating tablets of atenolol were prepared employing different concentrations of hydroxypropyl methylcellulose (HPMC) K15M and sodium bicarbonate in different combinations by direct compression technique using 32 factorial design. The concentration of HPMC K15M and sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2, respectively, whereas time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%), and 90% (t90%) were selected as dependent variables. Totally, nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, floating lag time, in vitro drug release. From the results, concluded that all the formulation were found to be within the pharmacopoeial limits and the in vitro dissolution profiles of all formulations were fitted into different Kinetic models, the statistical parameters like intercept (a), slope (b) and regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations was verified by designing 2 checkpoint formulations (C1, C2). According to SUPAC guidelines the formulation (F8) containing combination of 25% HPMC K15M and 3.75% sodium bicarbonate, is the most similar formulation (similarity factor f2 = 87.797, dissimilarity factor f1 = 2.248 and no significant difference, t = 0.098) to marketed product (BETACARD). The selected formulation (F8) follows Higuchi’s kinetics, and the mechanism of drug release was found to be non-Fickian diffusion (n = 1.029, Super Case-II transport).

Development and Optimization of the Reservoir-type Oral Multiparticulate Drug Delivery Systems of Galantamine Hydrobromide

This study is focused on the development and optimization of the reservoir-type oral multiparticulate drug delivery systems loaded with galantamine hydrobromide. For this purpose, the process of applying of the drug onto sugar pellets through the medium of a hydroxypropyl methylcellulose-based suspension was investigated. A substantial part of the study was to refine the layering process in respect to the influence of critical process parameters on the formation of agglomerates between the pellets. This outcome is related to some critical coating factors, such as: spray rate, product temperature, airflow, concentration of hydroxypropyl methylcellulose in the coating suspension and spray pressure. In this study design of experiments was used as a statistical method for assessing the influence of critical process parameters on the agglomeration. For this purpose full factorial design of five factors at two levels was built. The effect of the main factors and their interaction on the response was evaluated using regression analysis, analysis of variance and graphical analysis of the experimental design. The results showed that the airflow and the concentration of hydroxypropyl methylcellulose in the coating suspension have the most significant effect on the formation of agglomerates during the drug layering process.

Development and Characterization of Novel Floating-Mucoadhesive Tablets Bearing Venlafaxine Hydrochloride.

The present investigation is concerned about the development of floating bioadhesive drug delivery system of venlafaxine hydrochloride which after oral administration exhibits a unique combination of floating and bioadhesion to prolong gastric residence time and increase drug bioavailability within the stomach. The floating bioadhesive tablets were prepared by the wet granulation method using different ratios of hydroxypropyl methyl cellulose (HPMC K4MCR) and Carbopol 934PNF as polymers. Sodium bicarbonate (NaHCO3) and citric acid were used as gas (CO2) generating agents. Tablets were characterized for floating properties, in vitro drug release, detachment force, and swelling index. The concentration of hydroxypropyl methyl cellulose and Carbopol 934PNF significantly affects the in vitro drug release, floating properties, detachment force, and swelling properties of the tablets. The optimized formulation showed the floating lag time 72 ± 2.49 seconds and duration of floating 24.50 ± 0.74 hr. The in vitro release studies and floating behavior were studied in simulated gastric fluid (SGF) at pH 1.2. Different drug release kinetics models were also applied. The in vitro drug release from tablets was sufficiently sustained (more than 18 hr) and the Fickian transports of the drug from the tablets were confirmed. The radiological evidence suggests that the tablets remained buoyant and altered position in the stomach of albino rabbit and mean gastric residence time was prolonged (more than > 6 hr).