scholarly journals Factorial design approach to fabricate and optimize floating tablets based on combination of natural polymer and rice bran wax

2022 ◽  
Vol 11 (1) ◽  
Author(s):  
Vidya P. Sabale ◽  
Gunjan G. Gadge
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Factorial Design ◽  
Rice Bran ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Natural Polymer ◽  
Rice Bran Wax ◽  
The Stability

Abstract Background The aim of the present research work was to fabricate a novel gastroretentive drug delivery system in the form of tablets using a combination of natural polymer and rice bran wax with an intention to control drug delivery and to enhance the gastric residence time of the model drug Famotidine in the gastrointestinal tract. Results The results of the preliminary trial batches prepared by using the hot melt granulation technique resulting in six different formulations showed good physicochemical characteristics and tablets conformed to the Pharmacopoeial specifications. Gastroretentive tablets containing natural polymer showed prolonged drug release comparable to Methocel. The optimized formulation (C3) using 32 factorial design showed FLT 27 ± 2.47 s, SI 92.68 ± 1.36% and % CDR 98.89 ± 0.39% at 12 h. The stability studies indicated the stability of the formulation during storage. Conclusions It was concluded that the release profile fitted best to zero-order equation with non-Fickian diffusion mechanism of drug release which demonstrates swelling-controlled drug release mechanism. Thus, the formulated tablets have the potential for improved release and gastroretentive properties. Graphical Abstract

scholarly journals Fabrication and Characterization of Anticancer Drug Loaded Double Walled Microspheres

2019 ◽  
Vol 9 (4-A) ◽  
pp. 79-85
Author(s):  
Elangovan Nagarajan ◽  
B Rama ◽  
M Swetha ◽  
G.S Sharma ◽  
L Jyothi Rani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Guar Gum ◽  
Diffusion Mechanism ◽  
Polymer Concentration ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Breast Cancer Patients

In the present work, double walled microspheres of Tamoxifen (antiestrogenic drug) using Sodium alginate, Hydroxy propyl methyl cellulose (HPMC) K100,Guar gum, Xanthun gum were formulated to deliver Tamoxifen (TMX) through  oral route to treat breast cancer patients. Details regarding the preparation and evaluation of the formulations have been discussed in results. From the study following conclusions could be drawn. The results of this investigation indicate that Ion gelation method can be successfully employed to fabricate TMX microspheres. FT-IR spectra of the physical mixture revealed that the drug is compatible with the polymers and copolymer used. Microspheres containing sodium alginate along with HPMC in 1:1 ratio had a least size range of 610µm. Increase in the polymer concentration led to increase in % Yield, % Drug entrapment efficiency, Particle size. The  invitro drug release decreased with increase in the polymer and copolymer concentration. Among all formulations F7 shows Maximum drug release in 12 th hr  when compared with other formulations. Analysis of drug release mechanism showed that the drug release from the formulations followed the Non fickian diffusion mechanism and follows zero order kinectics. Based on the results of evaluation tests formulation coded F7 was concluded as best formulation. Keywords : Tamoxifen, sodium alginate, HPMC, Microspheres, Diffusion, Copolymers,  Entrapment efficiency.

scholarly journals Formulation of gastroretentive floating drug delivery system using hydrophilic polymers and its in vitro characterization

2014 ◽  
Vol 50 (2) ◽  
pp. 431-439 ◽  
Author(s):  
Venkata Srikanth Meka ◽  
Senthil Rajan Dharmanlingam ◽  
Venkata Ramana Murthy Kolapalli
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

The aim of the present research is to formulate and evaluate the gastroretentive floating drug delivery system of antihypertensive drug, propranolol HCl. Gastroretentive floating tablets (GRFT) were prepared by using a synthetic hydrophilic polymer polyethylene oxide of different grades such as PEO WSR N-12 K and PEO 18 NF as release retarding polymers and calcium carbonate as gas generating agent. The GRFT were compressed by direct compression strategy and the tablets were evaluated for physico-chemical properties, in vitro buoyancy, swelling studies, in vitro dissolution studies and release mechanism studies. From the dissolution and buoyancy studies, F 9 was selected as an optimized formulation. The optimized formulation followed zero order rate kinetics with non-Fickian diffusion mechanism. The optimized formulation was characterised with FTIR studies and observed no interaction between the drug and the polymers.

scholarly journals DESIGN AND DEVELOPMENT OF LOSARTAN POTASSIUM FLOATING DRUG DELIVERY SYSTEMS

2018 ◽  
Vol 10 (6) ◽  
pp. 168
Author(s):  
Prasanta Kumar Mohapatra ◽  
Ch. Prathibha ◽  
Vivek Tomer ◽  
Mandeep Kumar Gupta ◽  
Satyajit Sahoo
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Angle Of Repose ◽  
Losartan Potassium ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Dissolution Studies

Objective: The current study was projected to prepare a losartan potassium gastroretentive drug delivery system (GRDDS) of floating tablets was planned to enhance the gastric residence time, thus prolong the drug release.Methods: Effervescent floating matrix tablets of losartan potassium were prepared by direct compression technique using polymers like HPMC k4m, guar gum, and gum karaya, with lubricants magnesium stearate and talc. In the present study, sodium bicarbonate was incorporated as a gas generating agent. Total nine formulations were designed and evaluated for pre-compression parameters known as the angle of repose, bulk density, tapped density, Hausner’s ratio, compressibility index, and post-compression parameters are uniformity of weight, hardness, and drug content percentage, variability, in vitro buoyancy, dissolution studies, and Fourier transform infrared spectroscopy (FTIR).Results: An in vitro dissolution study was carried out by using buffer pH 1.2. From in vitro dissolution studies, it has been found that an increase in polymer concentration diminishes the drug release profile. The in vitro drug release percentage from F4-F9 formulations ranged from 60.28%-98.66% at the closing of 12 h and buoyancy found over 12 h.Conclusion: The in vitro drug release from F1-F3 and F7-F9 followed zero-order, F4 followed Higuchi order, F5 and F6 followed Hixon-Crowell release kinetics. The drug release mechanism was set up to be F1-F8 non-Fickian (anomalous behavior) and F9 having Fickian diffusion type.

Development of an In situ Gel Polymer Composite for Local and Sustained Delivery of Drugs in Vaginal Cavity

2019 ◽  
Vol 9 (3) ◽  
pp. 211-221
Author(s):  
Sateesha S. Boregowda ◽  
Sadanand R. Maggidi ◽  
Rajamma A. Jayaramu ◽  
Nethravathi Puttegowda ◽  
Nikhat Parbin
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Polymer Composite ◽  
Diffusion Mechanism ◽  
Fickian Diffusion ◽  
Vaginal Fluid ◽  
Sustained Delivery ◽  
In Situ Gel

Objective: The present research work is aimed at the development of an in situ gel polymer composite to provide local and sustained delivery of therapeutic agents in the vaginal cavity. Administration of medicated gel into a vaginal cavity is very complicated, inconvenient and needs expert assistance. There is a chance of expulsion of liquid formulation from site of application, leads to poor therapeutic efficacy. The effective drug delivery system for the vaginal cavity should be of liquid for application and gel to reside in the cavity. Methods: In situ gel composed of chitosan (0.8%) cross-linked with β-glycerol phosphate (15%) and glutaraldehyde treated guar gum (0.2%) was developed. Gel was characterized for in situ gelling properties. In vitro drug release pattern of the gel was tested on a nutrient agar medium containing attenuated E. coli and B. Subtilis. In vitro diffusion pattern of gel was tested using KC-diffusion cell with Simulated Vaginal Fluid (SVF) (pH 4.2) as the diffusion medium. Results: In situ gel exhibited sharpest sol-gel transition at 35±2°C, at pH 5.4 in 62±1.31sec. The viscosity of polymer composite is 51.25±3.68 CPs at 20±2°C and 328.56±4.16 CPs at 35±2°C. The gelation time of gel was found to be decreasing as the concentration of cross-linking agent β-GP increased. Formulations exhibited a shear thinning property. Drug release from this polymeric composite was found to be highly linear and follows non-fickian diffusion mechanism. Conclusion: This advanced thermosensitive in situ gel is convenient to apply and reside in the vaginal cavity for a prolonged period of time. The gel is mucoadhesive, biodegradable and suitable for controlled drug delivery in the cavity.

scholarly journals FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE SUSTAINED RELEASE MATRIX TABLETS

2021 ◽  
pp. 82-88
Author(s):  
SAHIDUL ALAM ◽  
AMLAN BISHAL ◽  
BRATATI BANDYOPADHYAY
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Metformin Hydrochloride ◽  
Major Advance

Objective: Now a days as very few antidiabetic drugs are coming out of research and development and some existing drugs are showing several side effects when administered orally, multiple times in a day, hence change in the operation is a suitable and optimized way to make some drug more effective by slight alteration in the drug delivery. Matrix type drug delivery systems of an antidiabetic drug like Metformin Hydrochloride, is an interesting and promising option when developing an oral sustained release system Methods: An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug to a specific organ or tissue and controlling the rate of drug delivery to the target sites. This research work is made in designing of sustained release dosage form of Metformin Hydrochloride by wet granulation method employing both Xanthan Gum and Hydroxy Propyl Methyl Cellulose (HPMC K4M) as a rate controlling polymer. Results: The development of oral sustained release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. From all the formulation trial batches, formulation F7 shows the best results. It has been observed that HPMC K4M alone cannot give satisfactory drug release profile but the blend of HPMC K4M and Xanthan gum together give the best drug release kinetics. Conclusion: The drug release mechanism from the matrix tablets follows Fickian diffusion with first order kinetics. Thus, sustained release matrix tablets of metformin hydrochloride can be expected to reduce the frequency of administration and decrease the dose dependent side effects

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

Nanostructured Ketorolac-Tromethamine/MCF: Synthesis, Characterization and Application in Drug Release System

2018 ◽  
Vol 14 (5) ◽  
pp. 432-439 ◽  
Author(s):  
Juliana M. Juarez ◽  
Jorgelina Cussa ◽  
Marcos B. Gomez Costa ◽  
Oscar A. Anunziata
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Therapeutic Efficacy ◽  
Drug Delivery Systems ◽  
Controlled Drug Release ◽  
Delivery Systems ◽  
The Body ◽  
Fickian Diffusion ◽  
Ketorolac Tromethamine

Background: Controlled drug delivery systems can maintain the concentration of drugs in the exact sites of the body within the optimum range and below the toxicity threshold, improving therapeutic efficacy and reducing toxicity. Mesostructured Cellular Foam (MCF) material is a new promising host for drug delivery systems due to high biocompatibility, in vivo biodegradability and low toxicity. Methods: Ketorolac-Tromethamine/MCF composite was synthesized. The material synthesis and loading of ketorolac-tromethamine into MCF pores were successful as shown by XRD, FTIR, TGA, TEM and textural analyses. Results: We obtained promising results for controlled drug release using the novel MCF material. The application of these materials in KETO release is innovative, achieving an initial high release rate and then maintaining a constant rate at high times. This allows keeping drug concentration within the range of therapeutic efficacy, being highly applicable for the treatment of diseases that need a rapid response. The release of KETO/MCF was compared with other containers of KETO (KETO/SBA-15) and commercial tablets. Conclusion: The best model to fit experimental data was Ritger-Peppas equation. Other models used in this work could not properly explain the controlled drug release of this material. The predominant release of KETO from MCF was non-Fickian diffusion.

scholarly journals Polymer-Drug Conjugates as Nanotheranostic Agents

2021 ◽  
Vol 2 (1) ◽  
pp. 63-81
Author(s):  
Sajana Manandhar ◽  
Erica Sjöholm ◽  
Johan Bobacka ◽  
Jessica M. Rosenholm ◽  
Kuldeep K. Bansal
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Treatment Options ◽  
The Body ◽  
Drug Conjugates ◽  
Imaging Characteristics ◽  
Wide Range ◽  
Systemic Side Effects ◽  
Theranostic Agents ◽  
The Stability

Since the last decade, the polymer-drug conjugate (PDC) approach has emerged as one of the most promising drug-delivery technologies owing to several benefits like circumventing premature drug release, offering controlled and targeted drug delivery, improving the stability, safety, and kinetics of conjugated drugs, and so forth. In recent years, PDC technology has advanced with the objective to further enhance the treatment outcomes by integrating nanotechnology and multifunctional characteristics into these systems. One such development is the ability of PDCs to act as theranostic agents, permitting simultaneous diagnosis and treatment options. Theranostic nanocarriers offer the opportunity to track the distribution of PDCs within the body and help to localize the diseased site. This characteristic is of particular interest, especially among those therapeutic approaches where external stimuli are supposed to be applied for abrupt drug release at the target site for localized delivery to avoid systemic side effects (e.g., Visudyne®). Thus, with the help of this review article, we are presenting the most recent updates in the domain of PDCs as nanotheranostic agents. Different methodologies utilized to design PDCs along with imaging characteristics and their applicability in a wide range of diseases, have been summarized in this article.

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

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (11) ◽  
pp. 71-73
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
J Vijaya Ratna ◽  
R. B. Srinivasa
Keyword(s):  
Drug Release ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Gastric Residence Time ◽  
Drug Release Mechanism ◽  
The Matrix ◽  
Gastro Retentive

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.

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.

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