scholarly journals Preparation and In vitro Evaluation of Theophylline Loaded Gastroretentive Floating Tablets of METHOCEL K4M

1970 ◽  
Vol 7 (1) ◽  
pp. 65-70 ◽  
Author(s):  
Ferdous Khan ◽  
Md Shaikhul Millat Ibn Razzak ◽  
Md Ziaur Rahman Khan ◽  
Kazi Rashidul Azam ◽  
Sams Mohammad Anowar Sadat ◽  
...  
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Release Rate ◽  
Lag Time ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Floating Tablets ◽  
Time Required

This investigation describes the preparation and in vitro evaluation of gastroretentive floating tablets of theophylline. Hydrophilic polymer METHOCEL K4M was used for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid), gel forming agent (METHOCEL K4M) and dose variation on drug release profile and floating properties were investigated. It has been observed that in all cases increase of the amount of floating agent caused a decrease of the floating lag time. Increase of theophylline load showed an increase of the floating lag time, which was independent of floating agent content. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixon-Crowell equations. The release rate, extent and mechanisms were found to be governed by the content of polymer and floating agent. The content of active ingredient was also a vital factor in controlling drug release pattern. It was found that polymer content and amount of floating agent significantly affected the time required for 50% of drug release (T50%), percentage drug release after 8 hours, release rate constant, and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed that the drug release mechanism could range from diffusion controlled to case II transport, which was mainly dependent on presence of relative amount of theophylline, polymer and floating agent. Key words: Gastroretention, Floating tablet, Theophylline  DOI = 10.3329/dujps.v7i1.1220 Dhaka Univ. J. Pharm. Sci. 7(1): 65-70, 2008 (June)

scholarly journals Formulation and Evaluation of Gastro Retentive Floating Tablets of Simvastatin using Hydrophilic Rate Retardant

2012 ◽  
Vol 15 (2) ◽  
pp. 119-126 ◽  
Author(s):  
Md Nazmul Hussain ◽  
Md Abdullah Al Masum ◽  
Sharmin Akhter ◽  
Florida Sharmin ◽  
Md Selim Reza
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Release Rate ◽  
Dissolution Time ◽  
Drug Release Profile ◽  
Compression Technique ◽  
Weight Variation ◽  
Gastro Retentive

Gastro retentive floating tablet of Simvastatin was prepared by direct compression technique using Methocel K4M as the rate controlling polymer. The hydrophilic cellulose derivative, Methocel K4M was evaluated for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid) and gel forming agents on drug release profile and floating properties were investigated. The tablets from all formulations were evaluated for thickness, diameter, weight variation, hardness, and friability. The tablets were also tested for the buoyancy studies and in vitro drug release studies. The drug release study was evaluated for eight hours using USP XXII paddle-type dissolution apparatus using 0.1N HCl with 1% Sodium Lauryl Sulphate as dissolution medium. The release mechanisms were explored and explained with zero order, first order, Higuchi, Hixon Crowell and Korsmeyer equations. The release rate, extent and mechanisms were found to be governed by the polymer content. It was found that the mean dissolution time, percentage drug release, release rate constant and diffusion exponent were influenced significantly by the amount of polymer incorporation. DOI: http://dx.doi.org/10.3329/bpj.v15i2.12575 Bangladesh Pharmaceutical Journal 15(2): 119-126, 2012

scholarly journals DEVELOPMENT AND EVALUATION OF GASTRORETENTIVE FLOATING TABLETS OF A QUINAPRIL HCL BY DIRECT COMPRESSION TECHNIQUE

2017 ◽  
Vol 9 (8) ◽  
pp. 35 ◽  
Author(s):  
Audumbar Digambar Mali ◽  
Ritesh Suresh Bathe
Keyword(s):  
Drug Delivery ◽  
Citric Acid ◽  
Drug Release ◽  
Lag Time ◽  
Direct Compression ◽  
Compression Technique ◽  
Floating Tablets ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

Objective: The present study was undertaken with an objective to design, develop and evaluate gastro retentive floating tablets of an antihypertensive drug, quinapril HCl, which release the drug in a sustained manner over a period of 12 h.Methods: In this research work, we used hydrophilic polymer hydroxypropyl methylcellulose (HPMC K4M), the gas generating agent sodium bicarbonate and citric acid at different ratios for the preparation of tablets. A 32 factorial design was applied systematically; the amount of HPMC K4M (X1) and the amount of citric acid (X2) were selected as independent variables. The dependent variables chosen were percentage drug release at 6 h (Q6), percentage drug release at 12 h (Q12) and floating lag time. The high concentration of HPMC K4M and citric acid gives a sustained release for quinapril HCl floating tablets. The tablets were prepared by direct compression technique and evaluated for tablet thickness, hardness, weight variation, friability, floating lag time and In vitro drug release.Results: The In vitro drug release indicated the floating dosage forms showed slower release when the concentration of HPMC K4M increases. Formulation F4 having ratio 25:8 (HPMC K4M: citric acid) was considered as an optimised formulation which shows satisfactory sustained drug release and remained buoyant on the surface of the medium for more than 12 h. It can also conclude that floating drug delivery system of quinapril HCl can be successfully formulated as an approach to increase gastric residence time and thereby improving its bioavailability.Conclusion: The developed effervescent based floating tablets are a promising floating drug delivery system for oral sustained administration of quinapril HCl.

scholarly journals Formulation and Evaluation of Gastroretentive Floating Tablets of Quetiapine Fumarate

2021 ◽  
Vol 11 (3-S) ◽  
pp. 65-73
Author(s):  
Keyur S. Patel ◽  
Akshar N. Rao ◽  
Deepa R. Patel ◽  
Dhaval M. Patel ◽  
Advaita B. Patel
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Factorial Design ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Lag Time ◽  
Quetiapine Fumarate ◽  
Floating Tablets ◽  
Vitro Release

The objective of the present study was to develop gastroretentive floating tablets of quetiapine fumarate. The gastroretentive floating tablets of quetiapine fumarate were formulated using natrosol 250 HHX as a sustained release polymer and sodium bicarbonate as a gas forming agents.  A 32 factorial design was employed to study the influence of concentration of natrosol HHX 250 (X1) and concentration of sodium bicarbonate (X2) on the dependent variables % drug release at 1h (Y1), % drug release at 8 h (Y2) and floating lag time (Y3). The optimized formulation (O1) showed floating lag time 49 ± 3 sec and % drug release 99.54± 0.81 at 12 h. The in vitro release of F1-F9 batches were found in between 99.95 ± 1.18 %  to  86.32 ±1.71 % at 12 h. Floating lag time of F1-F9 batches were found to be 25± 2 sec to 178 ± 3 sec. FTIR studies shown that there was no  interaction between quetiapine fumarate and excipients. From the factorial design batches it was found that floating lag time was decreased with increasing the amount of sodium bicarbonate and decreasing the amount of natrosol 250 HHX. Here % release of drug was decreased with increase the extent of natrosol 250 HHX. The in-vitro release kinetics revealed Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion. Keywords: Quetiapine fumarate, Natrosol 250 HHX, Sodium bicarbonate, Gastroretentive floating tablets

Preparation and Evaluation of Gemifloxacin Mesylate Floating Matrix Tablets in Healthy Human Volunteers

2017 ◽  
Vol 10 (1) ◽  
pp. 3623-3630
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Haarika B ◽  
Jyothi Sri S ◽  
K Abbulu
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Physical Parameters ◽  
Drug Bioavailability ◽  
Floating Tablets

The purpose of present investigation was to develop floating matrix tablets of gemifloxacin mesylate, which after oral administration could prolong the gastric residence time, increase the drug bioavailability and diminish the side effects of irritating drugs. Tablets containing drug, various viscosity grades of hydroxypropyl methylcellulose such as HPMC K4M and HPMC K15M as matrix forming agent, Sodium bicarbonate as gas-forming agent and different additives were tested for their usefulness in formulating gastric floating tablets by direct compression method. The physical parameters, in vitro buoyancy, release characteristics and in vivo radiographic study were investigated in this study. The gemifloxacin mesylate floating tablets were prepared using HPMC K4M polymer giving more sustained drug release than the tablet containing HPMC K15M. All these formulations showed floating lag time of 30 to 47 sec and total floating time more than 12 h. The drug release was decreased when polymer concentration increases and gas generating agent decreases. Formulation that contains maximum concen-tration of both HPMC K15M and sodium bicarbonate (F9) showing sufficiently sustained with 99.2% of drug release at 12 h. The drug release from optimized formulation follows Higuchi model that indicates the diffusion controlled release. The best formulation (F9) was selected based on in vitro characteristics and used in vivo radiographic studies by incorporating barium sulphate as a radio-opaque agent and the tablet remained in the stomach for about 6 h.   

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 Development and Optimization of Gastro-Retentive Formulation of Hydralazine HCl

2016 ◽  
Vol 8 (05) ◽  
Author(s):  
Himanshu Acharya ◽  
Rakesh Patel
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Methyl Cellulose ◽  
Optimization Procedure ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Hydralazine Hydrochloride ◽  
Predicted Values

Hydralazine hydrochloride has a half-life of 2 to 4 hours with an oral bioavailability of 26-50%. Since hydralazine has a demethylating effect on various suppressor genes, it can be used in various types of cancer to support chemotherapy. The purpose of this study was to optimize and evaluate floating tablets of hydralazine hydrochloride designed to prolong the gastric residence time and to provide controlled release of the drug for 24 h. The floating tablets of hydralazine hydrochloride were prepared by the wet granulation method. Polymers of hydroxy propyl methyl cellulose (HPMC K100M), HPMC K15M, carbopol 940 and sodium bicarbonate were used as the release retarding agents. This study investigated utility of a 3-factor, 3-level Box-Behnken design and optimization process for floating tablet of Hydralazine with 5 replicates of center points. Amount of HPMC K4 (Hydroxy Propyl Methyl cellulose), amount of sodium bicarbonate were selected as the independent variables whereas total floating time (TFT), T90, % cumulative drug release at 24 hours, and T20, Q1 were selected as dependent variables. Non-Fickian diffusion release transport was confirmed as the release mechanism for the optimized formulation and the predicted values agreed well with the experimental values. Drug excipient compatibility studies were investigated by FTIR, DSC and XRD. The produced tablets exhibited good floating time and controlled drug release over a period of 24 h. The resultant data were critically analyzed to locate the composition of optimum formulations. All predicted values of response variables of optimized formulation demonstrated close agreement with the experimental data during optimization procedure.

scholarly journals Formulation and Evaluation of Colchicine Sustained release tablet by using factorial designs

2021 ◽  
Vol 11 (5-S) ◽  
pp. 100-107
Author(s):  
M. Pradeep Kumar ◽  
Goparaju Suryanarayana Murthy ◽  
Annamdasu Lakshmi Poojitha ◽  
P. Sindhuri ◽  
A Sreekanth ◽  
...  
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Similarity Factor ◽  
Time Required ◽  
Full Factorial

The study on the effect of polymer concentration on in vitro drug release profile revealed that there is a change in vitro drug release parameters (t50, t80, and MDT) with a change in polymer concentration. Fraction of HPMC K4M, HPMC K 100 M, and Ethyl Cellulose were required to be 15, 10, and 7 mg respectively for designing optimized batch F7. The release rate of Colchicine decreased proportionally with an increase in the concentration of ethyl Cellulose and HPMC K100 M. Also the high amount of HPMC K4M leads to the less initial release and sustain effect. A theoretical drug release profile was generated using pharmacokinetic parameters of Colchicine. The value of t50 and t80 of theoretical drug release profile was found to be 242 min and 529 min respectively. The similarity factor f2 was applied between the in vitro drug release profile of optimizing batches and theoretical profile, which indicate a decent similarity between all in vitro drug release profiles (f2 = 68.28 for F7). All the batches except F1shows the value of f2 value within a range. Batch F7 showed the highest f2 (f2 = 68.28) among all the batches and this similarity was also reflected in t50 (≈ 256 min) and t80 (≈ 554 min) values. A 23 full factorial design was applied to systemically optimize in vitro drug release profile. The HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) were selected as independent variables. The time required for 50% drug released (t50), the time required for 80% drug release (t80), similarity factor f2, and mean dissolution time (MDT) were selected as dependent variables. The results of full factorial design indicate that the HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) have a significant effect on in vitro drug release profile. To find out the release mechanism the in vitro release data were fitted in the Korsmeyer-Peppas equation. All Batches except F1 and F3 show Anomalous diffusion-controlled release (combined mechanism of diffusion and case II transport).  

scholarly journals Formulation and Evaluation of Floating Matrix Tablets of Sacubitril and Valsartan

2019 ◽  
Vol 9 (4-s) ◽  
pp. 298-309
Author(s):  
Sudhakar Pathak ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Potential Candidate ◽  
In Vitro Drug Release ◽  
Gastric Emptying Rate ◽  
Floating Tablets

Floating Drug Delivery Systems (FDDS) have a bulk density lower than gastric fluids and thus remain buoyant in the stomach for a prolonged period of time, without affecting the gastric emptying rate. While the system is floating on the gastric contents, the drug is released slowly at a desired rate from the system. These floating tablets mainly prepared for reduction of lag time and release the drug up to 12 hours and may also increase the bioavailability of the drugs by utilizing the drug to full extent avoiding unnecessary frequency of dosing. The purpose of this research was to develop and evaluated floating matrix tablets of sacubitril and valsartan. The floating matrix tablets of sacubitril and valsartan were prepared by direct compression method using altered concentrations of HPMC K4M, HPMC K100M, sodium alginate as polymers and sodium bicarbonate, citric acid as gas generating agent. FTIR, DSC studies conformed that there was no incompatibility between the polymers and the drug. Tablet preformulation parameters were within the pharmacopoeias limit. Tablets were evaluated by different parameters such as weight uniformity, content uniformity, thickness, hardness, in vitro release studies, buoyancy determination and kinetic analysis of dissolution data. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. Tablet showed ≤ 1min lag time, continuance of buoyancy for >12 h. The in-vitro drug release pattern of sacubitril and valsartan optimized floating tablets (F16) was fitted to different kinetic models which showed highest regression (r2 = 0.9838) for Higuchi model. The Optimized formulation (F16) 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 sacubitril and valsartan 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.  

scholarly journals DESIGN EXPERT SUPPORTED FORMULATION DEVELOPMENT, MATHEMATICAL OPTIMIZATION AND PREDICTABILITY STUDY OF FLOATING TABLETS OF BISOPROLOL FUMARATE

2021 ◽  
pp. 242-248
Author(s):  
SHAIKH SHAOOR AHMAD ◽  
SHAIKH SIRAJ N. ◽  
PATEL M. SIDDIK ◽  
KHALIFA MAHMADASIF YUNUS ◽  
MAKRANI SHAHARUKH I. ◽  
...  
Keyword(s):  
Drug Release ◽  
Scale Up ◽  
Mathematical Optimization ◽  
Lag Time ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Floating Tablets ◽  
Design Expert

Objective: Focus of the study was to formulate Design expert Software assisted floating tablet of Bisoprolol Fumarate. Bisoprolol Fumarate is a Beta adrenergic blocking agent, used to treat cardiac diseases favorable characters to be formulated as sustained release Gastro retentive floating tablets. Methods: Floating Tablets of Bisoprolol Fumarate were prepared by using polymers such as Polyox N 12 K and Carbapol 940 P. Formulations were prepared by using direct compression method and evaluated for various parameters like Hradness, thickness, weight variations, Floating lag time Total floating time,% drug release and Stability Study etc. Results: FTIR spectroscopic study indicates no drug-excipients interaction in the prepared formulations. Hardness or crushing strength of the tablets of all the formulation was found between 5.8 and 6.5 kg/cm2. Floating lag time of all batches is in range of 1.18±2.0 to 2.43±1.6 (minutes). All other parameters of all batches are within an acceptable range. The polymer Carbopol 940 P had the significant negative effect of on the floating lag times. The In vitro dissolution profiles of optimized A3 Floating formulation of Bisoprolol Fumarate were found to sustain drug release 99.25 % up to 12 h with floating lag time of 1.45 min; Designed formulation was stable after Stability study. Optimization study was carried out by using 32 factorial designs to fabricate formulations. Conclusion: It can be conclude that reproducible results of various parameters in this developed formulation can easily scale up. Furthermore designed formulation will be very effective for controlling blood pressure.

The Measurement and Mathematical Analysis of 5-Fu Release from Magnetic Polymeric Nanocapsules, following the Application of Ultrasound

2018 ◽  
Vol 18 (3) ◽  
pp. 438-449 ◽  
Author(s):  
Ziaeddin Abed ◽  
Samideh Khoei ◽  
Behafarid Ghalandari ◽  
Jaber Beik ◽  
Ali Shakeri-Zadeh ◽  
...  
Keyword(s):  
Drug Release ◽  
Mathematical Analysis ◽  
Ultrasound Irradiation ◽  
Controlled Drug Release ◽  
Release Profile ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Ultrasound Intensity ◽  
Dialysis Bag

Objective: To study the effects of ultrasound irradiation on the release profile of 5-fluorouracil (5-Fu) loaded magnetic poly lactic co-glycolic acid (PLGA) nanocapsules. Also, the controlled drug-release behaviour of the nanocapsules was mathematically investigated. Methods: The nanocapsules were synthesized, dispersed in phosphate buffered saline (PBS), transferred to a dialysis bag, and finally, irradiated by various ultrasound parameters (1 or 3MHz; 0.3-1W/cm2; 5-10 minutes). The release profile of the irradiated nanocapsules was recorded for 14 days. To find the in vitro drug release mechanism in the absence and presence of various intensities of ultrasound, the obtained data were fitted in various kinetic models for drug release. Results: The results demonstrated that the ultrasound speeded up the rate of drug release from the nanocapsules. The mathematical analysis illustrated that when the ultrasound intensity is increased, the probability of controlled release behaviour of the nanocapsules is raised. We found that drug release from the irradiated nanocapsules follows an erosion-controlled mechanism with the decrease in the velocity of diffusion. Conclusion: In conclusion, to attain a controlled drug-delivery strategy in the area of cancer therapy, the drug release profile of the nano-carriers may be well-controlled by ultrasound.

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