scholarly journals Formulation and Evaluation of Biphasic Gastro Floating Tablets of Nateglinide and Atenolol

2020 ◽  
Vol 11 (3) ◽  
pp. 10906-10922
Keyword(s):  
Sustained Release ◽  
Low Cost ◽  
Diffusion Mechanism ◽  
Amorphous State ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Fixed Dose ◽  
Floating Tablets ◽  
Model Drug

The aim was to design, formulate, and evaluate bilayer gastro floating tablets of an antidiabetic agent, nateglinide (immediate-release layer), and antihypertensive agent, atenolol (sustained-release layer). The solubility of model drug nateglinide was enhanced by using cremophor RH 40 and characterized by FTIR, DSC, XRD, SEM, and in vitro dissolution. It was found that selected ingredients were compatible, and crystalline nateglinide transits to an amorphous state. The gastro-bilayer tablets were directly compressed using the optimized nateglinide (solid dispersion equivalent to 60 mg of nateglinide) immediate-release layer (IRL2) containing different percentage of F-Melt type C and crospovidone and atenolol (50 mg) sustained-release layer (SRL6) using different percentage of HPMC K15, sodium bicarbonate, and MCC. Developed tablets were evaluated and found within the acceptance range as per the guidelines. The release of nateglinide and atenolol from an optimized bilayer tablet (BLT3) was 100 % within 60 min and 12 h, respectively. The floating lag time and total floating time were 2 min and 12 h, respectively. The atenolol sustained-release followed the diffusion mechanism. The combination of nateglinide and atenolol was successfully showed a biphasic release pattern. This formulation may strengthen the fixed-dose combination therapy for diabetes and hypertension at a low cost.

scholarly journals Electrospun Janus Beads-On-A-String Structures for Different Types of Controlled Release Profiles of Double Drugs

Biomolecules ◽  
2021 ◽  
Vol 11 (5) ◽  
pp. 635
Author(s):  
Ding Li ◽  
Menglong Wang ◽  
Wen-Liang Song ◽  
Deng-Guang Yu ◽  
Sim Wan Annie Bligh
Keyword(s):  
Controlled Release ◽  
Combined Therapy ◽  
Diffusion Mechanism ◽  
Amorphous State ◽  
Electrospinning Process ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Sem Images ◽  
Release Profiles

A side-by-side electrospinning process characterized by a home-made eccentric spinneret was established to produce the Janus beads-on-a-string products. In this study, ketoprofen (KET) and methylene blue (MB) were used as model drugs, which loaded in Janus beads-on-a-string products, in which polyvinylpyrrolidone K90 (PVP K90) and ethyl cellulose (EC) were exploited as the polymer matrices. From SEM images, distinct nanofibers and microparticles in the Janus beads-on-a-string structures could be observed clearly. X-ray diffraction demonstrated that all crystalline drugs loaded in Janus beads-on-a-string products were transferred into the amorphous state. ATR-FTIR revealed that the components of prepared Janus nanostructures were compatibility. In vitro dissolution tests showed that Janus beads-on-a-string products could provide typical double drugs controlled-release profiles, which provided a faster immediate release of MB and a slower sustained release of KET than the electrospun Janus nanofibers. Drug releases from the Janus beads-on-a-string products were controlled through a combination of erosion mechanism (linear MB-PVP sides) and a typical Fickian diffusion mechanism (bead KET-EC sides). This work developed a brand-new approach for the preparation of the Janus beads-on-a-string nanostructures using side-by-side electrospinning, and also provided a fresh idea for double drugs controlled release and the potential combined therapy.

scholarly journals Formulation and evaluation of bi-layer floating tablets of ziprasidone HCl and trihexyphenidyl HCl

2011 ◽  
Vol 47 (3) ◽  
pp. 545-553 ◽  
Author(s):  
Sathis Kumar Dinakaran ◽  
Santhos Kumar ◽  
David Banji ◽  
Harani Avasarala ◽  
Venkateshwar Rao
Keyword(s):  
Sustained Release ◽  
In Vitro Release ◽  
Chemical Properties ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Floating Tablets ◽  
Ir Studies ◽  
Weight Variation ◽  
The Matrix

The purpose of this research study was to establish ziprasidone HCl NR 40 mg and trihexyphenidyl HCl SR 4mg in the form of bi-layer sustained release floating tablets. The tablets were prepared using sodium HPMC K4M / HPMC K15M as bio-adhesive polymers and sodium bicarbonate acting as a floating layer. Tablets were evaluated based on different parameters such as thickness, hardness, friability, weight variation, in vitro dissolution studies, content of active ingredient and IR studies. The physico-chemical properties of the finished product complied with the specifications. In vitro release from the formulation was studied as per the USP XXIII dissolution procedure. The formulations gave a normal release effect followed by sustained release for 12 h which indicates bimodal release of ziprasidone HCl from the matrix tablets. The data obtained was fitted to Peppas models. Analysis of n values of the Korsmeyer equation indicated that the drug release involved non-diffusional mechanisms. By the present study, it can be concluded that bi-layer tablets of ziprasidone HCl and trihexyphenidyl HCl will be a useful strategy for extending the metabolism and improving the bioavailability of Ziprasidone HCl and Trihexyphenidyl HCl.

scholarly journals FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

2017 ◽  
Vol 10 (5) ◽  
pp. 285
Author(s):  
S Shanmugam
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Kinetic ◽  
Natural Polymers ◽  
In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 

scholarly journals Formulation and in vitro Evaluation of Glimepiride Sustained Release Tablets: Comparison with Immediate Release Tablets

2015 ◽  
Vol 18 (2) ◽  
pp. 157-162
Author(s):  
Samira Karim ◽  
Mohiuddin Ahmed Bhuiyan ◽  
Md Sohel Rana
Keyword(s):  
Sustained Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Zero Order Kinetics ◽  
Weight Variation ◽  
Sustained Release Tablets

This work aims at the design of a sustained release formulation of glimepiride which is currently available in the treatment of type 2 diabetes mellitus and to investigate the effect of polymers on the release profile of glimepiride. Glimepiride sustained release tablets were prepared by direct compression method using different ratios of various release retarding polymers such as carbopol, ethyl cellulose, methocel K4 MCR, methocel K15 MCR, methocel K100 MCR and xanthum gum. These formulations were also compared with glimepiride immediate release tablets. The prepared tablets were subjected to various physical parameter tests including weight variation, friability, hardness, thickness, diameter, etc. In vitro dissolution studies of the formulations were done at pH 6.8 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. The percent releases of all the formulations (30) were 73.11%- 98.76% after 8 hours. The release pattern followed zero order kinetics and the release of the drug was hindered by the polymers used in the study. On the other hand, 100% drug was released within 1 hour from the immediate release tablet of glimepiride. The study reveals that the polymers used have the capacity to retard the release of the drug from the sustained release tablets and the more is the amount of the polymer in the formulation the less is the release of drug showing more retardation of drug release.Bangladesh Pharmaceutical Journal 18(2): 157-162, 2015

Electrospun Ketoprofen Sustained Release Nanofibers Prepared Using Coaxial Electrospinning

2013 ◽  
Vol 395-396 ◽  
pp. 138-143 ◽  
Author(s):  
Deng Guang Yu ◽  
Min Hao Hu ◽  
Wen Zhou ◽  
Bi Yu Chen ◽  
Xia Wang
Keyword(s):  
Sustained Release ◽  
Diffusion Mechanism ◽  
Electrospinning Process ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Coaxial Electrospinning ◽  
Electron Microscopic ◽  
Sheath Fluid ◽  
Release Drug

The present study investigates the preparation of sustained release drug-loaded nanofibers using a modified coaxial electrospinning process where only solvent is exploited as sheath fluid. Drug-loaded ethyl cellulose (EC) nanofibers are successfully generated smoothly and continuously without any clogging through the coaxial process, in which ethanol is used as sheath fluid and EC and ketoprofen (KET) are taken as the filament-forming matrix and active pharmaceutical ingredient, respectively. Field-emission scanning electron microscopic observations demonstrated that the nanofibers diameter can be manipulated through the sheath fluid flow rate. The composite nanofibers are in essential a molecular solid dispersion of EC and KET based on the hydrogen bonding between them, as verified by XRD and ATR-FTIR results. In vitro dissolution tests show that KET in the nanofibers has a fine sustained release profile via a typical Fickian diffusion mechanism. The modified coaxial electrospinning with solvent as sheath fluid can be a useful tool for developing novel sustained release drug delivery nanofibers.

scholarly journals Formulation of Lipid-Based Tableted Spray-Congealed Microparticles for Sustained Release of Vildagliptin: In Vitro and In Vivo Studies

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2158
Author(s):  
Khaled H. Al Zahabi ◽  
Hind Ben tkhayat ◽  
Ehab Abu-Basha ◽  
Al Sayed Sallam ◽  
Husam M. Younes
Keyword(s):  
Sustained Release ◽  
Oral Drug Delivery ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Oral Drug ◽  
Once Daily ◽  
Significant Difference ◽  
In Vivo Pharmacokinetics

Spray-congealing (SPC) technology was utilized to prepare lipid-based microparticles (MP) capable of sustaining the release of Vildagliptin (VG) for use as a once-daily treatment for type 2 diabetes mellitus. VG microparticles were prepared using Compritol® and Gelucire®50/13 as lipid carriers in the presence of various amounts of Carbomer 934 NF. The lipid carriers were heated to 10 °C above their melting points, and VG was dispersed in the lipid melt and sprayed through the heated two-fluid nozzle of the spray congealer to prepare the VG-loaded MP (VGMP). The microparticles produced were then compressed into tablets and characterized for their morphological and physicochemical characteristics, content analysis, in vitro dissolution, and in vivo bioavailability studies in mixed-breed dogs. The VGMP were spherical with a yield of 76% of the total amount. VG was found to be in its semicrystalline form, with a drug content of 11.11% per tablet and a percentage drug recovery reaching 98.8%. The in vitro dissolution studies showed that VG was released from the tableted particles in a sustained-release fashion for up to 24 h compared with the immediate-release marketed tablets from which VG was completely released within 30 min. The in vivo pharmacokinetics studies reported a Cmax, Tmax, T1/2, and MRT of 118 ng/mL, 3.4 h, 5.27 h, and 9.8 h, respectively, for the SPC formulations, showing a significant difference (p < 0.05)) from the pk parameters of the immediate-release marketed drug (147 ng/mL, 1 h, 2.16 h, and 2.8 h, respectively). The area under the peak (AUC) of both the reference and tested formulations was comparable to indicate similar bioavailabilities. The in vitro–in vivo correlation (IVIVC) studies using multiple level C correlations showed a linear correlation between in vivo pharmacokinetics and dissolution parameters. In conclusion, SPC was successfully utilized to prepare a once-daily sustained-release VG oral drug delivery system.

scholarly journals Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1073
Author(s):  
Ki Hyun Kim ◽  
Minju Jun ◽  
Mi-Kyung Lee
Keyword(s):  
Oral Administration ◽  
Geometric Mean ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Fixed Dose ◽  
Chlorpheniramine Maleate ◽  
Patient Centered ◽  
Dose Combination

Jellies for oral administration have been suggested as alternative dosage forms to conventional tablets for improved palatability and compliances for pediatric and geriatric patients. To evaluate the effect of jelly formulation on the bioavailability of cold medicines, two types of jellies were prepared for a fixed-dose combination of acetaminophen (AAP), chlorpheniramine maleate (CPM), dextromethorphan hydrobromide (DMH), and dl-methylephedrine hydrochloride (MEH). Jelly-S and Jelly-H were fabricated using carrageenan and locust bean gum in the absence and presence of xanthan gum, respectively. In vitro dissolution and in vivo absorption of the four drugs in the jellies were compared with other conventional formulations, a syrup and two types of immediate-release (IR) tablets with different hardness, Tablet-S (15 kPa) and Tablet-H (20 kPa). All the formulations exhibited more than 80% dissolution rate within 2 h even though the syrup, Jelly-S, and Tablet-S showed higher 30-min dissolution compared to Jelly-H and Tablet-H. The dissolution rates from the jellies decreased with increasing pH, which resulted in the slowest dissolution in pH 6.8 compared to the syrup and IR tablets. When administered orally to beagle dogs, all five formulations were determined not to be bioequivalent. However, Jelly-S and Jelly-H showed 0.82–1.05 of the geometric mean ratios (GMRs) of AUC0-t for all four drugs compared to the syrup suggesting comparable absorption. In two IR tablets, GMRs of AUC0-t were in a range of 0.55–0.95 indicating a tendency of lower absorption than the syrup and jellies. In conclusion, jelly can be a patient-centered formulation with comparable bioavailability to syrup.

scholarly journals FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE AND GLICLAZIDE SUSTAINED RELEASE BILAYER TABLETS: A COMBINATION THERAPY IN MANAGEMENT OF DIABETES

2021 ◽  
pp. 343-350
Author(s):  
RAJESWARI ALETI ◽  
SRINIVASA RAO BARATAM ◽  
BANGARUTHALLI JAGIRAPU ◽  
SRAVYA KUDAMALA
Keyword(s):  
Combination Therapy ◽  
Sustained Release ◽  
Diffusion Mechanism ◽  
Research Work ◽  
In Vitro Dissolution ◽  
Metformin Hydrochloride ◽  
Dissolution Profile ◽  
Sustained Release Formulation ◽  
Bilayer Tablets

Objective: The main objective of the present investigation is to develop a sustained-release (SR) formulation to optimize the postprandial elevation of glucose level in type 2 Diabetic subjects using combination therapy. In the present research work, bilayer sustained release formulation of metformin hydrochloride (MFH) and gliclazide (GLZ), based on monolithic-matrix technology was developed and evaluated. Methods: The formulations of metformin hydrochloride layer and gliclazide layer that contain polyox WSR coagulant and different viscosity grades of hydroxyl propyl methylcellulose (HPMC) as sustained-release matrix were prepared by direct compression and wet granulation method respectively. The bilayer tablets were prepared after carrying out the optimization of metformin layer and evaluated for various pre-compression and post-compression parameters. For the best formulation selected on basis of in vitro evaluation of tablets, Fourier-transform infrared spectroscopy (FT-IR) studies and comparison of in vitro dissolution profile of developed formulation with the innovator were performed. Results: Metformin hydrochloride and gliclazide showed sustained release of drug by diffusion mechanism and followed first-order kinetics. The best formulation of metformin hydrochloride (M7) and gliclazide (G8) show 99.93% and 99.65% of drug release in 24 h respectively. The similarity factor (f2) was 79.95 for metformin hydrochloride and 73.62 for gliclazide when compared with the innovator. Conclusion: The monolith diffusion-controlled bilayer tablets of metformin hydrochloride and gliclazide offer improved patient compliance and convenience with better postprandial hyperglycemic control with once-a-day dosing. The sustained release of the drug up to 24 h regulate antidiabetic activity round the clock with minimal side effects.

scholarly journals Formulation and Evaluation of Fixed-Dose Combination Immediate Release Tablets of Ibuprofen and Famotidine through Quality by Design Approach

2021 ◽  
Vol 24 (2) ◽  
pp. 133-148
Author(s):  
Md Mahbubul Alam ◽  
Md Shahidul Islam ◽  
KM Yasif Kayes Sikdar ◽  
ASM Monjur Al Hossain
Keyword(s):  
Immediate Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Fixed Dose ◽  
Compatibility Study ◽  
Compression Technique ◽  
Disintegration Time ◽  
Independent Variables ◽  
Anti Inflammatory

Nonsteroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed by the physicians for the management of pain due to their anti-inflammatory and analgesic properties. Long term use of NSAIDs causes gastrointestinal (GI) toxicity and the common GI disorders are indigestion, ulcers or bleeding. Therefore, the production of local oral tablets containing NSAIDs and gastro-protectant is inevitable. In this experiment, combination of ibuprofen 600 mg and famotidine 20 mg tablets were prepared by direct compression technique, which is unique in Bangladesh. To pursue the study Design of Experiments (DoE) approach was implemented to create fifteen trial formulations where Polyvinylpyrrolidone (PVPK30) 1%-3%, Microcrystalline Cellulose (Avicel PH-102) 1%-7% and Starch-1500 1%-13% were considered as independent variables and the responses were depicted in friability and disintegration time which were found 0.21–0.45% and 1.8–20.5 minutes respectively. Out of fifteen formulation trials (F-1 to F-15), seven formulations (F-3, F-6, F-8, F-9, F-10, F-13 and F-14) had met the acceptable criteria and one formulation (F-9) with independent variables PVP-K30 2.00%, Avicel PH-102 4.75% and Starch-1500 6.5% was selected because of its better disintegration, dissolution and friability profile. Data obtained from in-vitro dissolution tests were fitted to different kinetic models such as zero order, first order, Higuchi, Hixson-Crowell and Korsmeyer-Peppas models. Also, a compatibility study was conducted using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA) and X-Ray Diffraction (XRD). Furthermore, Scanning Electron Microscopy (SEM) was performed to analyze surface morphology. Finally, the selected formulation was compared to FDA regulated QC parameters and proved its superiority over conventional market products. Bangladesh Pharmaceutical Journal 24(2): 133-148, 2021

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