Formulation, Optimization, in vitro and in-vivo evaluation of levofloxacin hemihydrate Floating Tablets

Abstract The objective of the present investigation was to design, optimize and characterize the gastro retentive floating levofloxacin tablets and perform in-vivo evaluation using radiographic imaging. The floating tablets were prepared by using polymers i.e hydroxy propyl methyl cellulose (HPMC-K4M) and carbopol-940 individually and in combination by nonaquous granulation method. All the Formulations were evaluated for swelling index (S.I), floating behavior and in-vitro drug release kinetics. The compatibility study of levofloxacin with other polymers was investigated by FTIR, DSC, TGA and XRD. Results from FTIR and DSC revealed no chemical interaction amongst the formulation components. The optimized formulation (F11) showed floating lag time (FLT), total floating time (TFT) swelling index (S.I) of 60 sec, >16h and approximately 75 %, respectively. Moreover, F11 showed zero order levofloxacin release in simulated gastric fluid over the period of 6 h. X-ray studies showed that total buoyancy time was able to delay the gastric emptying of levofloxacin floating tablets in rabbits for more than 4 hours. In conclusion the optimized formulation (F11) can be used for the sustained delivery of levofloxacin for the treatment of peptic ulcer.

Formulation Optimization And Evaluation Of Flurbiprofen Emulgel

Objective: The objective of the present study was to formulate flurbiprofen (FLB) emulgel, evaluation of the formulations and the selection of an optimized formulation through in vitro drug release and drug content studies. Flurbiprofen is a non-steroidal anti-inflammatory drug (NSAID) requiring frequent administration and its chronic intake can lead to systemic side effects like gastric irritation and GI bleeding. The development of a dermal drug delivery system can overcome these side effects. Methods: The emulgel formulations were produced using different combinations of oil and emulsifying agents. Carbopol 940 was used as a gelling agent. The prepared emulgels were evaluated for general appearance, pH, spreadability, extrudability, drug content, in vitro drug release, average globule size and viscosity. Results: Optimized formulation F7 showed a better in vitro drug release compared to the marketed gel preparation. The stability study for the optimized formulation was carried out at 25 °C/60 % RH for 3 mo and the emulgel was found to be stable concerning the physical appearance, pH and drug content. Conclusion: The study revolved around the formulation of emulgel containing Flurbiprofen for dermal delivery of the drug. Emulgel was formulated with the purpose to enhance the permeation of poorly water-soluble drug FLB. The study concluded that the optimized emulgel containing FLB exhibited better in vitro drug release profile compared to the marketed formulation.

Development of controlled release dexketoprofen tablets and prediction of drug release using Artificial Neural Network (ANN) modelling

Dexketoprofen trometamol (DT) is an active S (+) enantiomer of ketoprofen, and a non-steroidal anti-inflammatory agent. DT has a short biological half-life and the dosing interval is quite short when there is a need to maintain the desirable effect for longer time periods. Consequently, a controlled release DT tablet was designed for oral administration aiming to minimize the number of doses and the possible side effects. Calculations of the parameters for controlled release DT tablets were shown clearly. Controlled release matrix-type tablet formulations were prepared using hydroxypropyl methylcellulose (HPMC) (low and high viscosity), Eudragit RS and Carbopol, and the effects of different polymers on DT release from the tablet formulations were investigated. The dissolution rate profiles were compared and analyzed kinetically. An Artificial Neural Network (ANN) model was developed to predict drug release and a successful model was obtained. Subsequently, an optimum formulation was selected and evaluated in terms of its analgesic and anti-inflammatory activity. Although the developed controlled release tablets did not have an initial dose, they were found to be as effective as commercially available tablets on the market. Dissolution and in vivo studies have shown that the prepared tablets were able to release DT for longer time periods, making the tablets more effective, convenient and more tolerable.

Effect Of Different Formulation Variables On Release Characteristics Of Gastro-Floating Microspheres Of Ethyl Cellulose/Carbopol 934p Encapsulating Sorafenib

Objective: The aim of this study is to prepare floating hollow microspheres encapsulating Sorafenib (SFN) to enhance its oral bioavailability.  Methods: Gastro-floating hollow adhesive microspheres containing SFN were produced by using an emulsion solvent evaporation technique with ether and ethanol as solvents. Ethyl cellulose and carbopol 934P were used as the encapsulating carriers. The effects of formulation parameters like, solvent volume ratio, and drug to polymer ratio (D: P ratio), encapsulation efficiency percentage EE%, floating percentage, and release of SFN after 12 h (Rel12) were investigated and analyzed using a (32) full factorial design. Results: The floating percentage of the microspheres was found to be 76.5%. The in vitro drug release from these hollow microspheres followed the Higuchi model equation. The in vivo results showed that approximately 1.96-fold improvement in the relative bioavailability of the microspheres compared with that of the commercial tablet.  Conclusion: The results demonstrate that the hollow microspheres with good gastro-floating ability are a promising delivery system to enhance SFN bioavailability.

Comparison of the Rate of Demineralization of Enamel using Synthetic Polymer Gel / 대한소아치과학회지

Carbopol® 907 used as surface protecting agent in White's method is the one of the artificial caries lesion producing solution was discontinuing of production. New surface protecting material to substitute of Carbopol® 907 was required.The author prepared an artificial caries lesion producing solution as follows White's method with Carbopol® 907 and also another artificial caries lesion producing solution with Carbopol® 2050®.96 flattened and polished enamel samples were immersed in a demineralizing solution of 0.1 mol/L lactic acid, 0.2% carboxyvinylpolymer and 50% saturated hydroxyapatite for 1, 2, 3, 4, 5, 6, 7, 9, 11, 15, 18 and 20 days. All samples from each group were subjected to polarized microscopy observed and image analysis for measuring the lesion depth.From the review of polarized images, the artificial caries lesion producing solution using Carbopol® 907 and Carbopol® 2050 can produced an artificial caries that was very similar to natural caries characters.From the regression analysis of the lesion depth produced by the artificial caries lesion producing solution using Carbopol® 907 and Carbopol® 2050, Carbopol® 2050 estimate as Y = 9.8X + 8.0 and Carbopol® 907 was Y = 8.4X − 0.4. R square value of Carbopol® 2050 and Carbopol® 907 was 0.965 and 0.945 respectively.The rate of demineralization by the artificial caries lesion producing solution using Carbopol® 2050 was faster than that of Carbopol® 907. And R square value of Carbopol® 2050 and Carbopol® 907 were very high and it means that the lesion depth was very high coefficient to demineralization period.

Preparation of Scutellarin Liposomes and Its Pharmacokinetics in Rats / 医药导报

Objective To prepare scutellarin liposomes and to investigate the pharmacokinetics in rats. Methods The liposomes of scutellarin coated with carbopol were prepared with the film dispersion method.Minicolumn centrifugation method was applied to measure the encapsulation efficiency (EE) before and after coating. SD rats were randomly divided into three groups, which were given intragastric administration of scutellarin suspension, scutellarin liposomes, and carbopol-coated scutellarin liposomes, respectively. And then the pharmacokinetic parameters were compared. Results Carbopol-coated scutellarin liposomes after intragastric administration in rats showed pharmacokinetic characteristics of two-compartment model. The main pharmacokinetic parameters of scutellarin suspension,scutellarin liposomes,and carbopol-coated scutellarin liposomes were as follows:AUC0-∞(50.03±13.45) μg?h?mL-1 ,(78.99±20.28) μg?h?mL-1 ,and (107.97±27.26) μg?h?mL-1 , respectively. Conclusion After coated liposomes, the oral bioavailability of scutellarin 1iposomes can be significantly improved,and the maximum drug concentration also increased.

In vitro evaluation of sustained released matrix tablets containing ibuprofen: a model poorly water-soluble drug

ABSTRACT A matrix system was developed that releases ibuprofen (IB) over a 12-hour period and the influence of the polymer type and concentration on the release rate of the drug was evaluated. Tablets containing different concentrations of Carbopol (CP), hydroxypropyl methylcellulose (HPMC), or ethyl cellulose (EC) were prepared using direct compression and the drug content, content uniformity, hardness, friability, dissolution performance, and in vitro release kinetics were examined. Formulated tablets were found to be within acceptable limits for physical and chemical parameters. The release kinetics of the Carbopol(r)971P 8% formulation showed the best linearity (r 2 =0.977) in fitting zero-order kinetics, suggesting the release rate was time independent. The drug release from tablets containing 8% CP was extended over approximately 18 hours and the release kinetics were nearly linear, suggesting that this system has the potential to maintain constant plasma drug concentrations over 12 hours, which could reduce the frequency of administration and the occurrence of adverse effects associated with repeated administration of conventional IB tablets.

Formulation and Characterization of Ketoprofen Emulgels.

The present study was intended to formulate the ketoprofen emulgels using different viscosity grades of hydroxypropyl methylcellulose and carbopol as gelling agents. All the prepared emulgels were shown acceptable physical properties concerning colour, homogeneity, consistency, and pH value. Emulgels containing hydroxypropyl methylcellulose were poor in clarity when compared to carbopol formulations. The influence of the type of gelling agent on the drug release from the prepared emulgels was investigated and carbopol 934 showed good results not only in the drug release but also in physical evaluation parameters. From the drug release studies, F3 formulation showed 98.46±2.05% drug release in 8 h with good clarity and physical appearance. The T10% and T80% values of best formulation F3 was found to be 0.9 h and 6.6 h respectively. The T10% and T80% was higher for formulations with carbopol in low concentration when compared to hydroxypropyl methylcellulose K 4M and K 15M in high concentrations, indicating better controlled release. FTIR studies proved the compatibility between drug and carbopol. From the stability studies, similarity index value between dissolution profiles of F3 formulation before and after storage was found to be 87.16. Hence the development of ketoprofen emulgels is a suitable way for topical administration.

Study on modeling process for golden gel / 中草药

Objective: To study the preparation process of golden gel. Methods: Taking the gel forming properties, stability, water loss rate, and pH value as investigation indexes, the influences of gel matrix, humectants, and binder dosage on gel forming were studied by single factor experiments. Results: The optimal conditions of preparation process were as follows: 1 g carbopol static swelling for 4 h, adding 10 g glycerol and 4 g drug powder, stirring after adding 1 g triethanolamine, adding water to 100 g, stirring well to obtain the gel. Conclusion: The method provides the evaluation criterion and basis for the further optimization of the golden gel forming process.

Simple Controlled Release Delivery System for an Anti-hypertensive Drug via Buccal Route.

Objective: This study aims to develop controlled release buccal tablets of losartan potassium based on bioadhesion using direct compression technique. Materials and Methods: The bioadhesive buccal tablets of losartan potassium were prepared after preliminary drug-excipients compatibility studies and micromeretics study for powder blends. The tablets were prepared by direct compression utilizing carbopol 934LR as a primary bioadhesive polymer either with or without chitosan or hydroxypropyl methylcellulose E15LV as secondary polymers. Other excipients included PVP K30 as a binder, magnesium stearate as a lubricant and mannitol as a diluent. The tablets were evaluated for weight variation, thickness and diameter, hardness, friability, drug content, surface pH, Ex-vivo residence time and bioadhesion force, In-vitro swelling and drug release study. The analysis of the release profiles in the light of distinct kinetic models (zero order, first order, Higuchi, Hixson-Crowell and Korsmeyer–Peppas) was carried out. Results and Discussion: The formula containing 40% w/w bioadhesive polymers of carbopol 934LR and chitosan (1:2) was selected as the optimum one based on a ranking methodology and then, it was subjected to Ex-vivo permeation and physical stability study in human saliva. Swelling index was 78.32±1.84% after 7h and tablets showed a neutral surface pH. Ex-vivo residence time was long enough for more than 10h. Ex-vivo bioadhesion force was 0.38±0.01N. Drug release was 57.64±3.43% after 8h following zero order kinetics with a steady state permeation flux of 0.959mg/cm2h. Tablets were physically stable in human saliva. Conclusion: These formulae improved, controlled and prolonged the release of losartan potassium from a buccal bioadhesive system for at least 8h in a simple way which can achieve a high patient compliance.

Effect of formulation parameters on Sumatriptan succinate Buccal Mucoadhesive Tablet: Quality by Design approach.

The present investigation was focused on application of QbD approach to see the effect of formulation variables on buccal mucoadhesive tablets containing anti migraine drug, Sumatriptan succinate to circumvent the first pass effect and to provide sustained release. Risk assessment of critical material and process parameters are linked to critical quality attributes (CQAs) of the product with respect to obtain total quality product profile (TQPP). The effect of critical parameters (polymer: drug ratio, carbopol: HPMC E5 ratio and diluent quantity) were investigated by executing design of experimentation (DoE) using Box-Behnken statistical model. DR10 hr (drug release after 10 hrs), mucoadhesive strength and mucoadhesion time were considered critical quality attributes (CQAs). Sumatriptan succinate buccal mucoadhesive (SBM) tablets were prepared by direct compression method and were evaluated as per pharmacopoeia procedure. Multiple regression analysis and ANOVA were employed to identify and estimate the effect of important parameters and establish their relationship with CQAs and to obtain design space for optimization purpose. The best in-vitro drug release profile, mucoadhesive strength, mucoadhesion time and desired product quality was achieved with the formulation prepared in the region of design space. FDS graph, 3D response graph and Overlay plot were successfully implemented to interpret effects and selection of significant parameters on CQAs. Hence, it can be concluded that formulation parameters affects the SBM tablet and can be successfully optimized using the QbD a novel approach resulting into the SBM tablets which could provide sustained effect and avoid first pass effect.

pH-induced in situ gelling system of an anti-infective drug for sustained ocular delivery.

Recently, in situ gel formation has been extensively studied to enhance ocular bioavailability and the duration of drug activity. Poor ocular bioavailability of drugs (<1%) from conventional eye drops is mainly due to the precorneal loss factors that include rapid tear turnover, nonproductive absorption, transient residence time in the cul-de-sac, and the relative impermeability of the drugs to corneal epithelial membrane. These problems may overcome by the use of in situ gel-forming systems that are instilled as drops into the eye and undergoes sol-gel transition in the cul-de-sac. In this study, in situ gelling system of Gatifloxacin were prepared using polymers carbopol 940 (0.1% to 0.5% w/v) and HPMC E4M (0.2% to 0.6% w/v). The developed formulation was characterized for various in vitro parameters such as clarity, temperature, pH, tonicity, sterility, rheological behavior, drug release profile, transcorneal permeation profile, and ocular irritation. Developed formulation was clear isotonic solution, converted into gel at temperatures above 35 °C and pH 6.9–7.0. The results demonstrated that the carbopol/ HPMC mixture can be used as an in situ gelling vehicle to enhance the ocular bioavailability of Gatifloxacin. The developed system is a viable alternative to conventional eye drops for the treatment of Bacterial conjunctivitis and various other ocular infections.

Mucoadhesive Polymeric Hydrogels for Nasal Delivery of Penciclovir.

The study evaluated different mucoadhesive polymeric hydrogels for nasal delivery of penciclovir . Gels containing poly-N-vinyl-2-pyrrolidone (PVP) were prepared with crosslinking achieved by irradiation with a radiation dose of 15 kGy being as efficient as 20 kGy. Gels containing chitosan and carbopol were also evaluated. The mucoadhesive properties of gels were measured by a modification of a classical tensile experiment, employing a tensile tester and using freshly excised sheep nasal mucosa. Considering the mucoadhesive force, chitosan gel and gel prepared with 3% PVP in presence of polyethylene glycol (PEG) 600 were the most efficient. The in vitro drug release depended on the gel composition. Higher release rates were obtained from PVP gels compared to chitosan or carbopol gels. The release rate of drug from PVP gels was increased further in presence of PEG or glycerol. Histopathological investigations proved that the PVP was a safe hydrogel to be used for mucosal delivery. The PEG in gel formulations caused less damages to the nasal mucosal compared to formulation containing glycerol.

Formulation and evaluation of colon specific microbial degradable matrix tablet using sterculia gum as carrier.

Current study is to develop the colon targeted matrix tablet using the natural polysaccharide sterculia gum as carrier and model drug ciprofloxacin HCl. The matrix tablets were prepared by wet granulation technology using the various proportions of sterculia gum with carbopol 934 P, sterculia gum and ethyl cellulose polymer blends. Gra-nules of all formulations were evaluated for rheological, post compressional properties and in vitro dissolution study in different pH buffers of pH 1.2 , pH 7.4 , pH 6.8 (saline phosphate buffer) without and with 4% rat cecal content in order to mimic GIT condition . Formulation SGC2 to SGC4 and SGE7 to SGE9 has released 13.6% to 38.9% in the initial 5h and released more amount of drug in stomach and small intestine than colon. Formulation SGC5 containing 45% of sterculia gum and 25% carbopol 934 p and Formulation SGE10 containing 45% of sterculia gum and 25% ethyl cellulose has released minimum 10.91 % to 13.04 % in the initial 5h and sustained the drug release up to 24 h and at the end of study released 75% to 79.99%. Formulations with 4% rat cecal content at the end of 24 h study drug released is 90.44% to 95.33% indicating higher amount of drug release is due to enzymatic break down of sterculia gum in the matrix tablet. Hence the above results conclude that the formulation SGC5 and SGE10 are potential in targeting the drug to colon to treat irritable bowel disease.

Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin.

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavaila-bility and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance.

Formulation and In-Vivo Study of Diltiazem Hydrochloride Tablets Prepared Using Interpolymer Complexes.

Aim: To investigate interpolymer complexes (IPCs) formation between carbopol and cationic polymers such as chitosan and Eudragit E for oral controlled drug delivery systems. Methodology: The prepared IPCs were investigated using Fourier transform infra-red spectroscopy (FT-IR) and differential scanning calorimetry (DSC). Chitosan-carbopol and Eudragit E-carbopol IPCs loaded with diltiazem hydrochloride (DTZ HCl) with different drug:polymer ratios were also prepared. Diltiazem hydrochloride tablets were prepared using polymers alone, physical mixtures of chitosan or Eudragit E with carbopol and the corresponding drug loaded IPCs. In-vitro release studies were carried out in two dissolution media; 0.1 NHCl of pH 1.2 and phosphate buffer of pH 7.4. Results: The dissolution rate of DTZ HCl from the prepared tablets were found to be dependant on the interaction between chitosan or Eudragit E with carbopol in the physical mixture, drug:polymer ratio and pH of the dissolution medium. Tablets prepared using chitosan – carbopol IPC, Eudragit E – carbopol IPC, and Eudragit E – carbopol physical mixture of drug:polymer ratio 1:5 were selected for the in-vivo study using rabbits. The results showed a lower peak plasma concentration and marked prolonged release effect of tablets containing Eudragit E – carbopol IPC and the corresponding physical mixture compared to that of commercial Altiazem tablets. Conclusion: Tablets containing Eudragit E – carbopol or chitosan – carbopol physical mixtures showed prolonged drug release compared to that containing the corresponding IPCs, Furthermore, Eudragit E- carbopol matrix tablets showed slower drug release than that of chitosan – carbopol

Formulation and evaluation of colon specific microbial degradable matrix tablet using sterculia gum as carrier.

Current study is to develop the colon targeted matrix tablet using the natural polysaccharide sterculia gum as carrier and model drug ciprofloxacin HCl. The matrix tablets were prepared by wet granulation technology using the various proportions of sterculia gum with carbopol 934 P, sterculia gum and ethyl cellulose polymer blends. Gra-nules of all formulations were evaluated for rheological, post compressional properties and in vitro dissolution study in different pH buffers of pH 1.2 , pH 7.4 , pH 6.8 (saline phosphate buffer) without and with 4% rat cecal content in order to mimic GIT condition . Formulation SGC2 to SGC4 and SGE7 to SGE9 has released 13.6% to 38.9% in the initial 5h and released more amount of drug in stomach and small intestine than colon. Formulation SGC5 containing 45% of sterculia gum and 25% carbopol 934 p and Formulation SGE10 containing 45% of sterculia gum and 25% ethyl cellulose has released minimum 10.91 % to 13.04 % in the initial 5h and sustained the drug release up to 24 h and at the end of study released 75% to 79.99%. Formulations with 4% rat cecal content at the end of 24 h study drug released is 90.44% to 95.33% indicating higher amount of drug release is due to enzymatic break down of sterculia gum in the matrix tablet. Hence the above results conclude that the formulation SGC5 and SGE10 are potential in targeting the drug to colon to treat irritable bowel disease.

Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin.

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavaila-bility and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance.

Transdermal iontophoretic delivery of timolol maleate

Transdermal iontophoresis would be a promising method for the systemic delivery of water soluble and ionic drugs of relatively high molecular size, including peptides. The objective of the present study was to investigate the effect of biological variable such as guinea pig and human cadaver skin and other variables like drug concentration, current density on the transdermal iontophoretic transport of timolol maleate. The permeation profile of drug using solution and gel formulation was studied and compared. For better bioavailability, better patient compliance, and enhanced delivery, an iontophoretic drug delivery system of a timolol maleate matrix gel was formulated using Carbopol 974P. The study was conducted using silver-silver chloride electrodes across the guinea pig and human cadaver skin. Viscosity measurements and flux calculations indicated the suitability of the Carbopol 974P gel for transdermal iontophoretic delivery of timolol maleate. Anodal iontophoresis with silver-silver chloride electrode significantly increased the timolol maleate skin permeation as compared with the passive permeation study. The amount of timolol maleate transported during iontophoresis was significantly different among the different skins. However, iontophoretic gel formulations provided required flux of drug through human cadaver skin.

A iontoforese transdérmica seria um método promissor para a liberação sistêmica de fármacos solúveis em água e iônicos de relativamente elevado tamanho molecular, incluindo peptídeos. O objetivo do presente estudo foi investigar o efeito da variável biológica, tais como cobaia e pele de cadáver humano, e outras variáveis como concentração do fármaco, densidade de corrente sobre o transporte transdérmico iontoforético de maleato de timolol. Comparou-se o perfil de permeação do fármaco usando a formulação de solução e de gel. Para melhor biodisponibilidade, melhor adesão do paciente e liberação aprimorada, formulou-se sistema de liberação iontoforética gel de maleato de timolol usando Carbopol 974P. O estudo foi conduzido usando eletrodos de prata-cloreto de prata na cobaia e na pele de cadáver humano. Medidas de viscosidade e de fluxo indicaram a adequação do gel Carbopol 974 P para liberação iontoforética transdérmica do maleato de timolol. A iontoforese anódica com eletrodo de prata-cloreto de prata aumentou significativamente a permeação dérmica do maleato de timolol, comparativamente à permeação passiva. A quantidade de maleato de timolol transportado durante a iontoforese foi significativamente diferente entre as diferentes peles . No entanto, as formulações iontoforéticas de gel forneceram o fluxo necessário do fármaco através da pele de cadáver humano.

Gastro-Retentive Floating Matrix Tablets of Cefpodoxime Proxetil.

The present work aims at the development and evaluation of Floating matrix tablets of Cefpodoxime Proxetil were undertaken to prolong gastric residence time. A visible Spectrophotometric method has been employed for the estimation of Cefpodoxime Proxetil at 263 nm and Beer’s law is obeyed in the concentration range of 5-40 μg/ml. Total 7 formulations (B1-B7) were prepared using guargum with carbopol 934P was used in different concentrations. Fourier transform Infrared spectroscopy confirmed the absence of any drug/polymers/excipients interactions. The tablets were prepared by direct compression technique, using polymer such as hydroxy propyl methyl cellulose (HPMC K4M), guargum and carbopol 934P in different combinations with other standard excipients like sodium bicarbonate and lactose. Tablets were evaluated for physical characterization viz. hardness, friability, swelling index, floating capacity, thickness and weight variation. Further tablets were evaluated in-vitro drug release for 12 hr. The effect of polymer concentrations on buoyancy and drug release pattern was also studied. In-vitro drug release mechanism was evaluated by PCP V-3 software. Carbopol 934P had a negative effect on the floating properties also decreased the drug release. A lesser FLT and a prolonged floating duration could be achieved by varying the amount of effervescent and using different polymer concentrations. The entire matrix tablets showed significantly greater swelling index, exhibited controlled and prolonged drug release profiles and some floated over the dissolution medium for more than12 hr. The paddle speed affected the floating lag time and floating duration it had a negative effect on the floating properties. The optimized formulation followed the higuchi release model and showed non-fickian diffusion mechanism. It also showed no significant change in physical appearance, drug content, floatability or in-vitro dissolution pattern after storage at 45 oC at 75 % RH for three months.