scholarly journals Colon Targeted Guar Gum Compression Coated Tablets of Flurbiprofen: Formulation, Development, and Pharmacokinetics

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Sateesh Kumar Vemula ◽  
Vijaya Kumar Bontha
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Area Under The Curve ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Formulation Development ◽  
Colon Targeting ◽  
Resident Time ◽  
Lag Period

The rationale of the present study is to formulate flurbiprofen colon targeted compression coated tablets using guar gum to improve the therapeutic efficacy by increasing drug levels in colon, and also to reduce the side effects in upper gastrointestinal tract. Direct compression method was used to prepare flurbiprofen core tablets, and they were compression coated with guar gum. Then the tablets were optimized with the support ofin vitrodissolution studies, and further it was proved by pharmacokinetic studies. The optimized formulation (F4) showed almost complete drug release in the colon (99.86%) within 24 h without drug loss in the initial lag period of 5 h (only 6.84% drug release was observed during this period). The pharmacokinetic estimations proved the capability of guar gum compression coated tablets to achieve colon targeting. TheCmaxof colon targeted tablets was 11956.15 ng/mL atTmaxof 10 h whereas it was 15677.52 ng/mL at 3 h in case of immediate release tablets. The area under the curve for the immediate release and compression coated tablets was 40385.78 and 78214.50 ng-h/mL and the mean resident time was 3.49 and 10.78 h, respectively. In conclusion, formulation of guar gum compression coated tablets was appropriate for colon targeting of flurbiprofen.

scholarly journals Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 260 ◽  
Author(s):  
Dongwei Wan ◽  
Min Zhao ◽  
Jingjing Zhang ◽  
Libiao Luan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Diffusion Rate ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

scholarly journals PHARMACOKINETIC STUDIES OF A CHRONOTHERAPEUTIC DRUG DELIVERY SYSTEM OF LORNOXICAM BY LC-MS/MS METHOD

2018 ◽  
Vol 10 (6) ◽  
pp. 88
Author(s):  
Sindhu Abraham ◽  
Rajamanickam Deveswaran ◽  
Jayaraman Anbu ◽  
Sharon Furtado ◽  
Bharath Srinivasan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Maximum Concentration ◽  
Area Under The Curve ◽  
Immediate Release ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Elimination Half ◽  
Coated Tablet ◽  
Liquid Chromatography Tandem Mass

Objective: The objective of this study was to investigate differences in pharmacokinetic patterns of immediate release tablet (IR) and compression coated tablet (CCT) of lornoxicam, proposed for the chronotherapeutic treatment of rheumatoid arthritis.Methods: The dosage forms were administered to two groups of white New Zealand rabbits (n=3), and the plasma drug levels were measured by liquid chromatography-tandem mass spectrometry (LC-MS/MS). Pharmacokinetic parameters like maximum concentration (Cmax), time is taken to reach maximum concentration (Tmax), area under the curve (AUC), elimination half-life (t1/2) and Mean Residence Time (MRT) were determined.Results: In the case of IR tablets, the drug was detected within 15 min after oral administration and a Cmax of 1269.57±4.04 ng/ml were attained at 2±0.15 h. With CCT, the drug was detected only after 5 h and a Cmax of 1279.24±12.76 ng/ml were attained at 8±0.10 h. The CCT showed maximum drug release at the eighth hour in comparison to IR tablet which showed maximum release at the second hour of study.Conclusion: The predominant lag time prior to drug release from CCT is an indication that it is consistent with the requirements of chronopharmaceutical drug delivery. The results suggest that the compression coated tablet is a promising approach for chronotherapeutic management of rheumatoid arthritis.

scholarly journals Formulation and Evaluation of Bilayer Matrix Tablets of Nebivolol Hydrochloride and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 82-93
Author(s):  
Selvi Arunkumar ◽  
L. Srinivas ◽  
D. Satyavati ◽  
C. Emmanuel
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Pharmacokinetic Studies ◽  
Drug Content ◽  
Bilayer Tablets ◽  
Nebivolol Hydrochloride

The present study is an attempt to develop bilayer matrix tablets of Nebivolol Hydrochloride and Valsartan with immediate release for Nebivolol Hydrochloride and sustained release for Valsartan. Superdisintegrants such as sodium starch glycolate and Crosscarmellose sodium were evaluated for immediate release of Nebivolol Hydrochloride and polymers HPMC K100M and K4M for sustained release of Valsartan. Preformulation studies were performed prior to compression. The compressed bilayer tablets were evaluated for weight variation, thickness, hardness, friability, drug content and in vitro drug release using USP dissolution apparatus type 2 in 0.01N HCl and phosphate buffer pH 6.8. All the pre and post compression parameters were found to be within the acceptable limits. The results of dissolution show that the formulations B3 was the best of all immediate and sustained release layer batches. The release kinetics of Valsartan was subject to curve fitting analysis in order to identify the best fit kinetic model. The regression analysis proves that the best formulations follow zero order release and drug release by diffusion process based on Fick’s law of diffusion. The data for stability studies infer no considerable change in drug content and dissolution rates as per ICH guidelines. The best formulation B3 was subjected to in vivo pharmacokinetic studies in rabbit model. In vitro, In vivo correlation (IVIVC) showed considerable linearity. Hence a novel bilayer tablet formulation of Nebivolol Hydrochloride and Valsartan was successfully developed by combining both immediate (IR) and sustained (SR) release layers. Keywords: Bilayer tablets, fixed unit dosage form, Nebivolol hydrochloride, Valsartan, LC-MS analysis.

scholarly journals FORMULATION AND IN VITRO EVALUATION OF BILAYER TABLET OF ATENOLOL FOR BIPHASIC DRUG RELEASE

2018 ◽  
Vol 11 (5) ◽  
pp. 114
Author(s):  
Tarun Parashar ◽  
Nardev Singh
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Regression Coefficient ◽  
Release Kinetics ◽  
Immediate Release ◽  
Drug Release Kinetics ◽  
Gum Acacia ◽  
Bilayer Tablet

Objective: In the present research work, the aim was to prepare the bilayer tablet of atenolol for biphasic drug release to improve its bioavailability and absorption in the lower gastrointestinal tract. Methods: In the formulation of immediate release crospovidone, croscarmellose sodium, and sodium starch glycolate was used as super disintegrate and was directly compressed. For a sustained release portion different grade hydroxypropyl methylcellulose (HPMC) K4M, HPMC K15M, gum tragacanth, gum acacia, guar gum, and ethyl cellulose. Preformulation studies were performed before compression. The compressed bilayer tablets were evaluated for weight variation, dimension, hardness, friability, drug content, disintegration time, and in vitro drug release using USP dissolution apparatus type 2 (paddle). Results: The formulation IR3 showed 95% drug release in 30 min, and regression coefficient value (r2) value was found to be 0.994 suggesting first-order drug release kinetics. The F9 formulation using HPMC K15M and gum acacia (1:1) showed 91.20% drug release at the end of 12 h, and regression coefficient value (r2) was 0.992 suggesting zero-order drug release kinetics. Formulation IR3F9 showed faster drug release for bilayer tablet containing 5%w/w crospovidone in immediate release layer and HPMC and guar gum (1:1) in sustained release. Formulation IR3F9 showed swelling index 206%, floating lag time was found to be 2 min and total floating time up to 12 h. Conclusion: The formulation IR3F9 showed a faster drug release profile among the others in the preparation of the atenolol bilayer tablet. Hence, it was considered as an optimized formulation.

scholarly journals SOLUBILITY ENHANCEMENT OF GLIBENCLAMIDE USING MESOPOROUS SILICA

2019 ◽  
pp. 302-314
Author(s):  
Swati Mittal ◽  
AKSHAY SONAWANE ◽  
MANGESH KHUNE
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Drug Loading ◽  
Immediate Release ◽  
Formulation Development ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Drug Precipitation ◽  
Poorly Soluble

Glibenclamide is a BCS Class II drug and poses a major problem during formulation development. In the present study, adsorption onto various carriers was used to enhance the solubility of glibenclamide. It was observed that solubility of glibenclamide was greatly enhanced by adsorbing onto mesoporous silica. The increase in solubility of poorly soluble drugs is often associated with the generation of supersaturation, which results in the risk of drug precipitation. HPMC E5 was used as precipitation inhibitor to maintain sink condition for a longer duration. A 32 full factorial design was adopted to optimize the ratio of glibenclamide (X1) and mesoporous silica as a carrier (X2) and the effect of different ratios was studied on percent yield, percent drug loading, and percent drug release. X-ray powder diffraction (XRPD) and Differential scanning calorimetry studies were performed to investigate any possible interaction in between glibenclamide and mesoporous silica. An optimum batch of drug adsorbate was used to prepare immediate-release tablets. The tablets prepared were evaluated for thickness, uniformity of weight, hardness, friability, in-vitro disintegration time, and in vitro drug release study.

scholarly journals Formulation Development and Evaluation of Doxofylline Sustained-Release Tablets by Using Chitosan and Guar Gum

2021 ◽  
pp. 552-567
Author(s):  
Pawan Avhad ◽  
Revathi Gupta
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Dosage Form ◽  
Guar Gum ◽  
The Body ◽  
Natural Polymer ◽  
Natural Polymers ◽  
Formulation Development ◽  
Sustained Release Tablets

The sustained-release dosage form is a well-characterized and reproducible dosage form that is designed to control drug release profile at a certain rate to reach desired drug concentration in blood plasma or at the target site. There is immense demand in the market for new sustained-release formulations used for new drug molecules which release the drug at a sustained rate. Doxofylline is one of the widely useful drugs in the market and needs to be given in a single dose for a long duration of time. For the same, we have prepared a sustained released Doxofylline tablet. Aim: This research was done to design, formulate and evaluate Doxofylline sustained-release tablets by using different concentrations of Chitosan and Guar Gum.  Methods: The factorial design was used to prepare Doxofylline sustained-release tablet. Doxofylline sustained-release tablets were prepared to employ different concentrations of Chitosan, Guar Gum, Lactose, and Magnesium Stearate in different combinations by wet granulation technique. Total 9 formulations were designed, formulated, and evaluated for the hardness, thickness, friability, % drug content, and in-vitro drug release. Results: A study of the release of drug by in-vitro found that F8 is to be the best efficient formulation which consists of both Chitosan and Guar Gum helped in delayed the release of drug up to 24 hours and performs excellent release of drug in starting hours of drug release in the body. The drug released from the F8 formulation indicates the kinetic model of First Order, by anomalous diffusion. The formulation F8 shows optimum thickness, hardness and at 40ºC±2 99.35% drug release after 24 hours shows optimum formulation.  Conclusion: This study concludes that better drug release was observed by using natural polymers.  Doxofylline with natural polymer shows good release and better dissolution rate as compared with a single synthetic polymer. Synthetic drug with natural polymer shows more future scope and this work will help the researcher in the future.

scholarly journals Formulation and Pharmacokinetics of Flurbiprofen Sublimated Fast Dissolving Tablets#

2015 ◽  
Vol 2 (1) ◽  
pp. 56-65 ◽  
Author(s):  
Sateesh K. Vemula ◽  
Santhosh G. Reddy
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Area Under The Curve ◽  
Physical Parameters ◽  
Pharmacokinetic Studies ◽  
Disintegration Time ◽  
Sublimation Method

Present study efforts are focusing to develop the flurbiprofen fast dissolving tablets using sublimation method to enhance the dissolution rate. In this study an attempt was made to fasten the drug release from the oral tablets by incorporating the sublimating agents in the presence of crosspovidone as superdisintegrant and studied the effect on dissolution rate when compared to conventional tablets. In the present study, sublimated fast dissolving tablets were prepared by direct compression method. The prepared tablets were characterized for physical parameters and drug release behavior and the best formulation was subjected to pharmacokinetic studies. From in vitro drug release studies, the formulation F2 showed fast drug release of about 99.94±0.26% in 30 min, and disintegration time 34.42 ± 0.74 sec. The percent drug release in 15 min (Q15) and initial dissolution rate for formulation F2 was 91.46±1.42%, 6.10%/min. The dissolution efficiency was found to be 53.44 and it is increased by 4.5 fold with F2 sublimated tablets. From the pharmacokinetic evaluation, the conventional tablets producing peak plasma concentration (Cmax) was 9023.68±561.83 ng/ml at 3 h Tmax and F2 sublimated tablets showed Cmax 11126.71±123.56 ng/ml at 2 h Tmax. The area under the curve for the conventional and F2 tablets was 30968.42±541.52 and 42973.66±568.13 ng h/ml. Hence, the development of flurbiprofen fast dissolving tablets by sublimation method is a right way to enhance not only the dissolution rate but also the absorption rate.

Characterization and Screening of a Novel Multiparticulate Pulsatile Delivery of Aceclofenac

2016 ◽  
Vol 9 (5) ◽  
pp. 3494-3501
Author(s):  
Bipul Nath ◽  
Santimoni Saikia
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Alginate Beads ◽  
In Vitro Drug Release ◽  
Dsc Studies ◽  
Ft Ir ◽  
Lag Period ◽  
Pulsatile Delivery ◽  
Ca Alginate

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.

Formulation and Evaluation of Immediate Release Bilayer Tablets of Telmisartan and Hydrochlorothiazide

2011 ◽  
Vol 4 (3) ◽  
pp. 1477-1483
Author(s):  
Natarajan R ◽  
N Patel ◽  
Rajendran N N ◽  
M Rangapriya
Keyword(s):  
Antihypertensive Drugs ◽  
In Vitro Release ◽  
Immediate Release ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Sodium Starch Glycolate ◽  
Bilayer Tablets

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.  

Formulation and Evaluation of Transdermal patch of Methimazole

2021 ◽  
pp. 4667-4672
Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Patch ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Percent Moisture ◽  
Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

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