Gastroretentive Tablets Research Articles

Quality and Release Profile of Captopril from Mucoadhesive Gastroretentive Tablet by Using Matrix Sodium Carboxymethyl Cellulose and Carbopol 934P

Captopril have good absorption in gastric pH and ionized on intestinal pH. It is necessary to keep the drug in the form of molecules in the area of the absoption. The mucoadhesive gastroretensive drug delivery system provides the possibility of controlled release in stomach in a certain amount of time. Research has been conducted to assess the quality and profile of captopril release in of a mucoadhesive gastroretensive tablet. Mucoadhesive tablets (MK) were made in 5 formulas by wet granulation method using carbopol 934P and sodium carboxymethyl cellulose as matrix with ratio 10: 0 (MK1), 0: 10 (MK2), 5: 5 (MK3), 7: 3 (MK4), and 3: 7 (MK5). The parameters which was evaluate were characteristics of granules and tablets and kinetics model of captopril release from tablets in 0,01 N HCl medium. Mucoadhesive tablets had different characteristics for each formula. Mucoadhesive tablets that had good quality and release profile were shown by MK4 and MK5 formula. They had controlled drug release profiles accorded to the Korsmeyer-Peppas and Higuchi kinetics models, respectively.

Investigation of cannabidiol gastro retentive tablets based on regional absorption of cannabinoids in rats

The cannabis plant has been widely researched for many therapeutic indications and found to be effective in many chronic conditions such as epilepsy, neuropathic or chronic pain and more. However, biased opinion against compounds of the plant, regulatory as well as compounding challenges have led to very few approved cannabinoid medicinal products. Those formulations which are approved are dosed several times a day, creating an unmet need for controlled release (CR) formulations of cannabinoids. Conventional CR formulations rely on prolonged absorption of the drug, including absorption from the colon. The purpose of this work is to investigate regional absorption of major cannabinoids THC and CBD from the colon and develop a suitable CR formulation.As hypothesized by researchers, THC and CBD have poor absorption from the colon compared to small intestine, suggesting that these compounds have a narrow absorption window. The suggested CR formulation examined in-vitro was a floating gastro retentive tablet based on egg albumin matrix, gas generating agents and surfactants. In-vivo investigation of CBD containing formulation in the freely moving rat model proved a prolonged absorption phase with a substantial increase in bioavailability compared to CBD solution.The findings of this paper answer a crucial question regarding potential application of CR dosage forms for cannabinoids and shed light on the regional intestinal absorption of these compounds. Ultimately, these results cement the way for future development of cannabinoid gastro retentive dosage forms.

Formulation and <i>In Vitro </i>Evaluation of Gastroretentive Theophylline Floating Tablets

The main aim of the present investigation was to formulate and evaluate gastroretentive floating tablets of theophylline. Theophylline, a brochodialator, used in the treatment of asthma, has good absorption at the gastric pH. Therefore, a floating drug delivery system in a gastric pH could deliver the drug in a slow and sustained manner which could be a useful for broncho dilation in the treatment of asthma. The formulated gastroretentive tablets of theophylline were evaluated for various parameters such as weight variation, hardnesss, friability, drug content, swelling index, buoyancy time and drug release studies. Among the different formulations, formulation F7 prepared using HPMC:Carbopol (1:1 ratio) exhibited better release profile (93.36%) for 8 hours and this batch was selected as an ideal batch. The release of theophylline from the ideal batch was found to follow diffusion mechanism.

Artificial membranes in combination with selected natural oils for in vitro drug passive diffusion screening in Ussing type chamber apparatus applied to gastro-retentive systems

This study aimed at developing an effective in vitro technique for the screening of drug passive diffusion utilising artificial membranes in combination with three selected oils (i.e. cognac, emu, and olive oil). Artificial membranes of varying chemical composition and characteristics have been investigated individually and in combination with the selected oils in terms of the passive diffusion of a fluorescent probe (i.e. Rhodamine 6G or R6G), in a diffusion apparatus as compared to excised pig intestinal tissues. In general, the permeation results showed that the rate and extent of R6G permeation were dependent on the membrane composition as well as the type of oil used. The apparent permeability coefficient (Papp) value for R6G across the cellulose nitrate membrane (0.197 × 10−7 ± 0.069 cm/s) was the closest to the Papp of R6G across the excised pig intestinal tissue (0.210 × 10−7 ± 0.080 cm/s). The cellulose acetate-nitrate mixture membrane impregnated with emu oil also produced a Papp value (0.191 × 10−7 ± 0.010 cm/s) that was relatively close to that of R6G across the excised pig intestinal tissue. The delivery of R6G from gastro-retentive matrix type tablets correlated with the release of R6G from the gastro-retentive tablets.

FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF TRAZODONE HYDROCHLORIDE

FORMULATION DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF TRAZODONE HYDROCHLORIDE Vivek Jain1, Halki Kushwah*1, Anwar Iqbal Khan1, Geeta Parkhe2 NRI Institute of Pharmacy, Bhopal, Madhya Pradesh, India. ABSTRACT Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design).Floating drug delivery systems are the gastro retentive forms that precisely control the release rate of target drug to a specific site which facilitate an enormous impact on health care. This can be achieved by use of various polymeric substances. Trazodone Hydrochloride (TRZ), is a well-known chemical compound that is used as an antidepressant that belongs to a selective serotonin reuptake inhibitors (SARI). TRZ is used as anti-anxiety and sleep-inducing agent. The tablets of TRZ were prepared by direct compression method using gas generating agent and different polymer combinations. The prepared tablets of TRZ were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, swelling index, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. The varying concentration of gas generating agent and polymers was found to effect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of TRZ shown that the formulation F9 was found to be the best formulation as it releases 97.98% TRZ in a controlled manner for an extended period of time (up to 12 hours). The release data was fitted to various mathematical models such as higuchi, Korsmeyer-Peppas, first order and zero order to evaluate the kinetics and mechanism of the drug release. Prepared floating tablets of TRZ may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Trazodone Hydrochloride, Gastro retentive, floating tablet, Total floating time. Full Text Article

Development of novel bilayer gastroretentive tablets based on hydrophobic polymers.

This study aimed to develop a bilayer gastroretentive (GR) tablet containing an insoluble drug and ascertain the potential of using hydrophobic polymers in GR matrix systems. Highly porous tablets were prepared using a camphor-based sublimation technique. After the screening of several commonly used polymers, two types of GR layers, a conventional hydrophilic GR layer and a hydrophobic GR layer, were designed. The optimal drug layer comprising Metolose® 90SH-100SR and dicalcium phosphate provided not only a gradual matrix erosion but also high strength after hydration. Regarding the GR layers, the hydrophobic layer based on Kollidon® SR was superior to the hydrophilic layer made of PEO 7M in terms of wet strength, implying a higher resistance to mechanical stresses upon water absorption. Also, the excellent tableting properties of Kollidon® SR and the effects of curing in improving its matrix hardness resulted in porous tablets with better mechanical strength. Moreover, good flowability and low cohesion of Kollidon® SR formulation were advantageous in direct compression. In conclusion, novel bilayer GR tablets were successfully developed, indicating the potential for widening the application of GR systems to insoluble drugs. The results also suggested numerous advantages of incorporating Kollidon® SR into the production of GR tablets.

Design and Optimization of Bilayer Floating Gastroretentive Tablets of Metoprolol

Objectives: We aimed to formulate and optimize bilayer tablets of metoprolol tartrate consisting of both immediate and sustained release layer. Methods: A 23 factorial design was employed in formulating the GFDDS in which parameters, such as amount of HPMC (X1), sodium bicarbonate + citric acid (X2), and crospovidone (X3) were characterized as independent variables, whereas percent metoprolol release at 30 min (Y1), 4 hr (Y2), 8 hr (Y3), floating lag time (Y4), and total floating time (Y5) were considered as dependent variables. Findings: The formulations showed the biphasic release of metoprolol, where the immediate layer was completely disintegrated within 30 min and the release of the sustained layer was extended to 8 hr. Prompt disintegration of the immediate layer was facilitated by the combined effects of sodium starch glycolate and sodium bicarbonate + citric acid, whereas the extended release was assisted by HPMC. Formulations, where HPMC played the major role, were considered the best formulations. A good correlation was displayed between the experimental and predicted values that confirm the practicability of the model. Application/improvements: This study shows the effect of various variables in the release of metoprolol tartrate and formulates the bilayer tablets of metoprolol tartrate for the immediate and sustained drug release.Keywords: Metoprolol, Floating Drug Delivery System, Bilayer, Immediate Release Layer, Sustained Release Layer

FORMULATION DEVELOPMENT AND EVALUATION OF GASTRO RETENTIVE FLOATING TABLET OF ATORVASTATIN USING STATISTICAL DESIGN (JMP SOFTWARE)

More complications and cost of promoting of imaginative drugs are more prominent consideration to the improvement of controlled release (CR) drug delivery systems. Sustained release or controlled release drug delivery system helps to reduced toxicity of drug and more patient compliant drug delivery system. The aim of this study is to have efficient means of manufacturirng of Gastro retentive floating tablet of Atorvastatin Calcium. Atorvastatin is used in the treatment of hyperlipidaemia. Oral bioavailability of atorvastatin calcium is less than 12% due to instability and in complete absorption. It also undergoes high first pass metabolism. It is absorbed more in the upper part of the GIT. Gastro retentive drug delivery system of Atorvastatin enhanced the bioavailability by retaining the drug in upper part of GIT and by preventing the first pass metabolism of the drug. The objective of present work was to create and assessed oral extended release gastro retentive tablet dosage form of Atorvastatin by using direct compression method using Methocel K4MDC2, Methocel K100MDC2 and Glyceryl behenate using Statistical design (JMP software). Sodium bicarbonate and Citric Acid is used as gas generating agent which helps to float the tablet.

Formulation Development and Evaluation of Sustain Release Gastroretentive Floating Tablets of Prochlorperazine Dimaleate

Floating drug delivery systems are the gastroretentive forms that precisely control the release rate of target drug to a specific site which facilitate an enormous impact on health care. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of Prochlorperazine dimaleate (PCZ) were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of PCZ were evaluated for hardness, thickness, friability, weight variation, drug content uniformity, buoyancy lag time, total floating time, in-vitro dissolution study, etc. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of PCZ shown that the formulation F9 was found to be the best formulation as it releases 98.89% in a controlled manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. The optimized formulation (F9) showed no significant change in physical appearance, drug content, floating lag time, in vitro dissolution studies after 75%±5% RH at 40±20C relative humidity for 6 months. Prepared floating tablets of PCZ may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.
 Keywords: Prochlorperazine dimaleate, Floating tablet, Gastro retentive, Total floating time.

Preparation and In-Vitro Evaluation as an Oral Microsponge Tablet of Baclofen

The aim of the present study is to formulate floating effervescent microsponge tablet of the narrow absorption window drug, Baclofen (BFN) for controlling drug release and thereby decrease the side effect of the drug. The microsponges of BFN were prepared by non-aqueous emulsion solvent diffusion method (oil in oil emulsion method). The effects of drug: polymer ratio, stirring time and type of Eudragit polymer on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selected microsponge formula was incorporated into the floating effervescent gastro-retentive tablet. The prepared floating microsponge tablet was evaluated for tablet hardness, friability, swelling in addition to in vitro drug release. The results showed that the microsponge formula with Eudragit RS100 had optimum physical properties and controlled drug release (75% of drug release in 8 hr.) when compared with other formulas and pure baclofen. The oil in oil emulsion method is a promising method to produce baclofen microsponge.

Gastroretentive Floating-Bioadhesive Drug Delivery System for Rebamipide: Design, In vitro and In vivo Evaluation

Rebamipide is an amino acid analog of 2-(1H)-quinolinone used in the treatment of peptic ulcer. Here we sought to formulate and evaluate gastroretentive floating-bioadhesive tablets of rebamipide to increase the gastric residence time and further compare their pharmacokinetics with conventional immediate release tablets. Floating-bioadhesive tablets of rebamipide were prepared with combination of Polyox WSR 303 and CP 971P/HPMC K4M and Sodium CMC by direct compression method. The prepared formulations were evaluated for hardness, thickness, weight variation, friability, drug content, in vitro buoyancy and drug release. The optimized formulation (RBF12) floated with a lag time of 28.3 ± 3.2 sec, duration of floating 12 h and released about 99.91 ± 1.84% of drug in 12 h, and then followed non-Fickian diffusion release mechanism with n value of 0.635. The RBF12 tablets with BaSO4 remained in stomach for 5.13 ± 0.64 h (n=3) in radiological studies. The formulation, RBF12 exhibited maximum bioadhesive strength (1.346 ± 0.110 N) than other formulations. The bioavailability studies were carried out for the optimized formulation (RBF12) and compared with that of reference IR tablets “Rebagen” in nine healthy human volunteers. Based on in vivo performance significant difference was observed between Cmax, tmax, t1/2, AUC0–∞, and MRT of RBF12 and IR tablets. The increase in relative bioavailability of RBF12 was 1.7-fold when compared to reference IR tablets. The increased relative oral bioavailability may be due to the floating-bioadhesive mechanism of dosage form, which is desirable for drugs absorbed from the upper part of gastrointestinal tract.

Improved bioavailability of Azelnidipine gastro retentive tablets-optimization and in-vivo assessment

Azelnidipine, dihydropyridine based calcium channel blocker has been used for treating ischemic heart disease and cardiac remodeling after myocardial infarction but it is having a low bioavailability due to its poor solubility. The present study is to investigate the formulation and evaluation of floating tablets of Azelnidipine for controlled release and to increase bioavailability by increasing the gastrointestinal transit time and mucoadhesion of drug. The gastro retentive tablets were prepared by direct compression method using different concentrations of combination of Polyoxyethylene oxide WSR 303 as hydrophilic polymer and Potassium bicarbonate as gas generating agent. Main effects of the formulation variables were evaluated quantitatively using design approach showing that both independent variables have significant effects on floating lag time, % drug release at 1 h (D1 h) and time required to release 90% of the drug (t90). The statistically optimized formulation (F3) released 95.11 ± 1.43% drug for 12 h followed K-Peppas drug release kinetics indicating release of drug by diffusion and erosion mechanism. Evaluation of the optimized formulation in vivo in human volunteers showed that the GFT was buoyant in gastric fluid and that its gastric residence time was enhanced. Pharmacokinetics studies carried out revealed significant (P < 0.05) equivalent Cmax, longer Tmax and higher AUC values for the optimized formula compared to the marketed oral product. From the results obtained it can be concluded that Azelnidipine Gastro retentive tablets with enhanced bioavailability and better release pattern is suitable for more effective treatment compared to marketed conventional tablets.

Formulation and evaluation sustained release mucoadhesive gastroretentive pantoprazole sodium sesquihydrate tablets for anti–ulcer

Objective: The objective of this research work is to develop and evaluate the mucoadhesive gastroretentive tablets of an anti – ulcer drug for sustain release. Materials and Methods: Mucoadhesive tablets were prepared by direct compression method using Hydroxy propyl methyl cellulose K4M, Carbopol 940 NF and Guar gum in the various drug – polymer ratios. The prepared tablets were evaluated for their pre and post compression parameters. In this study the optimized formulation was obtained within the specified limits. Results: The final optimized formulation was showed mucoadhesion time 12 h, mucoadhesive strength of tablets were ready with HPMC K4M, Carbopol 940 NF and gum were found to be 45 g and the extreme proportion of drug release was obtained 97.11% at the completion of 12 h. The drug release mechanism for optimized formulations of pantoprazole mucoadhesive sustain release tablets was observed to be zero order kinetic model. Conclusion: The formulation of hydroxy propyl methyl cellulose showed excellent mucoadhesive ability and a suitable drug release pattern.&#x0D; Keywords: Pantoprazole sodium sesquihydrate, Gastroretentive, mucoadhesive polymers

Development of stability-indicating HPLC method and accelerated stability studies for osmotic and pulsatile tablet formulations of Clopidogrel Bisulfate

The purpose of the present study is to develop a simple, rapid and sensitive stability-indicating high-performance liquid chromatography (HPLC) method for Clopidogrel Bisulfate (CBS) and further extending it for assessment of CBS stability in osmotic and pulsatile tablet formulations tested under accelerated conditions. A stability-indicating HPLC method for quantitative determination of CBS in gastro-retentive formulations is developed by using a C18 HPLC column, acetonitrile and 0.1% formic acid (60:40 v/v) as mobile phase, with a flow rate of 0.9 mL/min, UV detection at 222 nm and subsequently validated. The key objective was to analyze the stability profile of formulations under accelerated conditions. The retention time (Rt) of CBS was observed as 5.9 min with the linearity range between 0.06–1.95 μg/mL. Forced degradation studies were performed on bulk samples of CBS using acidic, basic, oxidative, thermal (80 °C) and photolytic (under sunlight) conditions. The resulting method was validated as per ICH Q2(R1) guidelines. Moreover, an attempt has been made to identify the degradation products by Liquid chromatography-mass spectrometry (LC–MS) analysis. The proposed method was successfully applied to novel gastro-retentive tablet formulations (osmotic tablet and pulsatile tablet) for assessment of stability under accelerated conditions.

DESIGN AND CHARACTERIZATION OF ALFUZOSIN HCL GASTRORETENTIVE FLOATING MATRIX TABLETS EMPLOYING HPMC K 100M

The present investigation involves developing gastro retentive drug delivery systems (GFDDS) of alfuzosin HCl using HPMCK100M a is the matrixing agent and floating enhancer. Sodium bicarbonate in the acidic environment reacts with the acid and produces carbon dioxide. The gastro retentive tablets can be formulated to increase the gastric residence time and thereby increase the oral bioavailability. From the drug release study, it was concluded that the AFTB4 formula of HPMC K 100 M matrix tablets gives the controlled release up to 12 hours by showing increased release with floating lag time 24 seconds. Non – Fickian diffusion was the drug release mechanism from the matrix tablets formulated employing HPMC K 100 M. The matrix tablets (AFTB4) formulated employing 40 % HPMC K 100 M are best suited to be used for gastro retentive dosage form of alfuzosin HCl. Finally, it can be concluded that good candidates for the preparation of gastro retentive dosage forms due its gastric stability, gastric absorption and better bioavailability.

Formulation and Pharmacokinetic Evaluation of Ritonavir Floating Tablets in the Management of AIDS

In the current study, gastro-retentive tablets of Ritonavir was developed to increase its oral bioavailability using hydrophilic polymers HPMC K 4M, K 15M, and K 100M as release retarding agents. Polyox WSR 303 was chosen as resin, sodium bicarbonate was used as effervescent agents. The tablets were prepared by direct compression method and FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. Among all the formulations F21 containing HPMC K 100M, Crospovidone, Polyox WSR 303 and sodium bicarbonate, as gas generating agent was choosen as optimized formulation based on the evaluation parameters, floating lag time (33 sec) and total floating time (&gt;24 h) and in vitro dissolution studies. From in vitro dissolution studies, the optimized formulation F21 and marketed product was shown 98.67% and 95.09 ± 5.01% of drug release respectively. From in vivo bioavailability studies, after oral administration of floating tablet containing 100 mg Ritonavir, the Cmax, Tmax, and AUC0–∞ of optimized gastroretentive formulation were found to be 30.11 ± 1.16μg/mL, 8.00±1.23 h and 173 ± 26.34μg*h/ml, respectively. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product, where longer gastric residence time is an important condition for prolonged or controlled drug release and also for improved bioavailability.

Preparation and evaluation of non-effervescent gastroretentive tablets containing pregabalin for once-daily administration and dose proportional pharmacokinetics

The main purpose of this study was to develop gastroretentive tablets with floating and swelling properties for once-daily administration of pregabalin. The non-effervescent floating and swelling tablets were prepared using wet granulation and compaction, which are widely used and easily accessible. All formulations showed sustained release patterns and maintained buoyancy for over 24 h. The amount of hydroxypropyl methylcellulose and crospovidone were found to be critical factors affecting in vitro dissolution and floating properties of the prepared tablets. The optimized tablets containing 300 mg of pregabalin started to float within 3 min and swelled above 12.8 mm, the reported pyloric sphincter diameter during the fed state, in all dimensions including length, width, and thickness. In vivo results in beagle dogs indicated that the optimized formulations are suitable as once-daily dosage forms, and dose proportionality was observed in doses ranging from 75 to 300 mg. Additionally, the dogs administered with the formulation having poor in vitro gastroretentive properties showed highly variable and reduced extent of absorption, signifying the necessity of the gastroretentive drug delivery system. In conclusion, the developed non-effervescent floating tablets are promising candidates for once-daily delivery of pregabalin.

Formulation and evaluation of gastro retentive tablets of clarithromycin prepared by using novel polymer blend

Clarithromycin is a semi synthetic macrolide antibiotic that is proved to be extremely effective mono therapy in treating H. pylori infection. One of the various reasons reported for partial eradication of H. pylori infection is that the short dwelling time of antimicrobial agents in the stomach. Hence the principal object of the present work was to design and develop floating and swellable gastro retentive tablet of clarithromycin to obtain its prolonged release in the stomach. HPMC K 100LV was blended in the present study with the Gel isolated from the seeds of Ocimum basilicum to overcome the drawback of time dependent erosion of former. This novel polymer blend was investigated and exploited as a matrix material for the development of gastro retentive tablets of clarithromycin as drug delivery system. Hydrogen bonding between the Glucomannan – a component of the Gel and HPMC K100LV was envisaged and further confirmed by ATR-FTIR. Tablets of clarithromycin prepared by using the polymer blend of Gel and HPMC K100LV exhibited fast swelling with almost instantaneous buoyancy followed by prolonged release of drug from the swollen, floating dosage form. The retention of the optimized tablet formulation of clarithromycin in the stomach was confirmed by γ scintigraphy.

FORMULATION OPTIMIZATION AND EVALUATION OF GASTRORETENTIVE TABLETS OF ONDANSETRON HCL

The aim of the work is to design Gastroretentive tablets of Ondansetron HCl for gastric retention by using 32 factorial designs. Floating tablets of Ondansetron HCl were prepared by direct compression method using polymers, sodium alginate and excipient. Gastroretentive tablets of Ondansetron HCl were successfully prepared by effervescent technique using different gel forming polymers- HPMC K200M, and sodium alginate. Formulation was optimized by design expert software. Floating tablets were evaluated for floating time, floating lag time, drug content, raft measurement and in vitro dissolution profile. The lag time is between 17-22 sec and floating time of the formulations for 12 hrs. The best fit model is Korsemeyer Peppas Model. From the study it is proof that the sustain release by floating tablets of Ondansetron HCl can be develop. Optimized batch selected was A3, The prepared gastroretentive test formulation was found to exhibit satisfactory physico-chemical characteristics at the end of 3 months, during the stability studies. The optimized formulation A3 was found to be stable at 400C/ 75% RH. Keywords: Gastric retention time, Ondansetron HCl, HPMC, sodium alginate, measurement of raft, Factorial design, stability studies.Â

Design and Preclinical Evaluation of Gastroretentive Floating Tablets of Quetiapine Fumerate

The present study was focused on gastro-retentive tablets of quetiapine fumarate using hydrophilic polymers HPMC K250 PH PRM, HPMC K750 PH PRM and HPMC K1500 PH PRM as release retarding agents. WSR 301 was chosen as resin, sodium bicarbonate was used as effervescent agents. FTIR studies revealed that there is no interaction between the drug and polymers used for the formulation. The tablets were prepared by direct compression method and the release rate was found to decrease with proportional increase in the ratio of polymer to drug. Quetiapine fumarate is absorbed well from stomach and therefore is a very good drug to be formulated into gastro retentive floating dosage form. In-vitro release profile of quetiapine fumarate and marketed product when compared, the optimized formulation F19 showed drug release of 98.65% within 24 h whereas 96.78% of the drug was released from the marketed product within 1h. The optimized formulation remained stable when subjected to accelerated stability studies. In vivo radiographic studies of quetiapine fumarate optimized formulation (F19) supported the expectations in prolonging the gastric residence time in the fasted state in beagle dogs. Cmax and AUC values of optimized formulation were found to be significantly higher than of marketed product. In conclusion, gastro-retention can be a promising approach to enhance bioavailability of quetiapine fumarate with narrow absorption window in upper GIT.