scholarly journals Comparative Study of Antihypertensive Drugs Amlodipine Besylate /Metoprolol Succinate and Nebivolol Hydrochloride /Valsartan Combinations in Bilayer Tablets

2019 ◽  
Vol 9 (4-s) ◽  
pp. 529-539
Author(s):  
Selvi - Arunkumar ◽  
L. Srinivas ◽  
D. Satyavati ◽  
C. Emmanuel
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Antihypertensive Drugs ◽  
Pharmacokinetic Parameters ◽  
Test Drug ◽  
Amlodipine Besylate ◽  
Metoprolol Succinate ◽  
Nebivolol Hydrochloride ◽  
Model Drug

The present research is an approach to develop a formulation platform that shall help in minimizing the time and effort taken to develop a drug delivery system. Taking bilayer tablet technology as a representation for drug delivery system, well accepted antihypertensive drugs, Amlodipine besylate and Metoprolol succinate were considered as model drugs for the study. Initially the process variables like concentration of the disintegrants, Sodium starch Glycolate and cross carmellose sodium, Polymers HPMC K100M and K4M were standardized with these drugs so that the incorporation of a new combination drugs would provide predictable results with a minimal trial runs. Nebivolol hydrochloride and Valsartan were considered as test drugs since they are novel antihypertensive drug combination and their physicochemical and pharmacokinetic parameters were almost similar to that of the model drugs. The r value 0.98943 indicates a good correlation between the release profile of Amlodipine besylate (model drug) and Nebivolol hydrochloride (test drug) from the IR layer. Similarly, the r value in the range of 0.9998 indicates a good correlation between the release profile of Metoprolol succinate (model drug) and Valsartan (test drug) from the SR layer. The comparable experimental results of the model drugs and test drugs considered for this study infer that if two drugs are similar in their physicochemical and pharmacokinetic parameters, their behavior with respect to in vitro parameters will be similar provided formulation variables remains constant. This concept could be productive in developing drug delivery system for new drugs for which extensive research and time are major constraints. Keywords: Bilayer tablets, fixed unit dosage form, Amlodipine besylate, Metoprolol Succinate Nebivolol hydrochloride, Valsartan.

Model drug delivery system based on nanodiamonds

2011 ◽  
Vol 6 (3-4) ◽  
pp. 256-264 ◽  
Author(s):  
K. V. Purtov ◽  
A. I. Petunin ◽  
A. P. Puzyr ◽  
A. E. Burov ◽  
V. S. Bondar
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Model Drug

Investigation of Nanoscale Structure of Self-Emulsifying Drug Delivery System Containing Poorly Water-Soluble Model Drug

2014 ◽  
Vol 970 ◽  
pp. 272-278 ◽  
Author(s):  
Mont Kumpugdee-Vollrath ◽  
Yotsanan Weerapol ◽  
Karin Schrader ◽  
Pornsak Sriamornsak
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Correlation Spectroscopy ◽  
Water Soluble ◽  
Wide Range ◽  
Poorly Water Soluble ◽  
Nanoscale Structure ◽  
Model Drug ◽  
20 Nm

This work has a focus on the self-emulsifying drug delivery system (SEDDS), which can be used in pharmaceutical field for increasing bioavailability of poorly water-soluble drugs. The model drug resveratrol was used because of its poor water-solubility and is of interest because of its wide range of pharmacological effects. It is beneficial to understand the mechanism of SEDDS formation in the human body, therefore, the determination of nanoscale structure was carried out. For this purpose, small angle X-ray scattering (SAXS), photon correlation spectroscopy (PCS), and transmission electron microscopy (TEM) techniques were applied. We have found that the size and size distribution of particles were in nanometers. The inner structure of SEDDS was ordered with the lamellar distances (d-spacing) of < 20 nm. It seems that the prepared SEDDS in water form large oil drops (200-400 nm) in water as well as small micelles with the droplet size of 10-20 nm.

Proliposomes as a drug delivery system to decrease the hepatic first-pass metabolism: Case study using a model drug

2014 ◽  
Vol 64 ◽  
pp. 26-36 ◽  
Author(s):  
Sarala Yanamandra ◽  
Natarajan Venkatesan ◽  
Veeran Gowda Kadajji ◽  
Zhijun Wang ◽  
Manish Issar ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
First Pass Metabolism ◽  
First Pass ◽  
Model Drug ◽  
Pass Metabolism

scholarly journals ENHANCING OF ORAL BIOAVAILABILITY OF POORLY WATER-SOLUBLE ANTIHYPERTENSIVE DRUGS

2021 ◽  
pp. 42-47
Author(s):  
BITOPAN BAISHYA ◽  
SHEIKH SOFIUR RAHMAN ◽  
DAMANBHALANG RYNJAH ◽  
KAMALLOCHAN BARMAN ◽  
SARANGA SHEKHAR BORDOLOI ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Patient Compliance ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Antihypertensive Drugs ◽  
Polymeric Nanoparticles ◽  
Delivery Systems ◽  
Water Soluble ◽  
Oral Drug

Among various routes of drug delivery, Oral administration is the most convenient route because of its high patient compliance. Although oral drug delivery is effective for drugs with high aqueous solubility and epithelial permeability; however for poorly aqueous soluble drug the membrane permeability, chemical, and enzymatic stability of drugs are the major limitations in successful oral drug delivery. Almost 70% of the new drug candidates which shows poor bioavailability, the antihypertensive drugs are among those. Novel drug delivery systems are available in many areas to overcome the problems associated with hydrophobic drugs and the nanotechnology-based drug delivery system is the most potential to beat the challenges related to the oral route of administration with some important advantages such as the colloidal size, biocompatibility, lowered dose size, reduced toxicity, patient compliance and drug targeting. The foremost common nanotechnology-based strategies utilized in the development of delivery systems are nano-emulsions, nano-suspensions, dendrimers, micelles, liposomes, solid lipid nanoparticles, polymeric nanoparticles, carbon nanotubes, Self-Nano-emulsifying Drug Delivery System, proliposomes, nano-crystals, and so forth, which give controlled, sustained, and targeted drug delivery. The appliance of those systems within the treatment of hypertension continues to broaden. This review focuses on various nano-carriers available in oral drug administration for improving solubility profile, dissolution, and consequently bioavailability of hydrophobic antihypertensive drugs.

Formulation and Evaluation of Pulsatile Drug Delivery System of Atenolol

2020 ◽  
Vol 6 (1) ◽  
pp. 45-49
Author(s):  
Sudipta Das ◽  
Baishali Ghosh ◽  
Surita Basu
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ethyl Cellulose ◽  
Methyl Cellulose ◽  
Burst Release ◽  
Direct Compression ◽  
Optimum Result ◽  
Pulsatile Drug Delivery ◽  
Model Drug

The objective of the present study was formulation and evaluation of pulsatile release tablets of Atenolol. A tablet system consisting of cores which was coated with layers of swelling and rupturable coatings. Cores containing Atenolol as model drug were prepared by direct compression with appropriate ratios of lactose and microcrystalline cellulose and then coated sequentially with different ratios of an inner swelling layer containing HPMC and an outer rupturable layer of Ethyl Cellulose. The effect of level of swelling layer and rupturable coating was investigated. The different formulation press coated by using different weight ratios of Hydroxy Propyl Methyl Cellulose (HPMC) / Ethyl Cellulose (EC) / both HPMC and EC. The optimum result was achieved in formulation containing HPMC: EC weight ratios. The F3 batch achieved a highest burst release after the lag time which is applicable pulsatile drug delivery system of Atenolol.

Preparation and Physical Properties of PCL-Metoprolol Tartrate Electrospun Nanofibers as Drug Delivery System

2021 ◽  
Vol 886 ◽  
pp. 183-188
Author(s):  
Saja A. Moosa ◽  
Akram R. Jabur ◽  
Emad S. Al-Hassani
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Electrospun Nanofibers ◽  
Metoprolol Tartrate ◽  
Water Contact ◽  
High Fiber ◽  
Good Potential ◽  
Span 80 ◽  
Model Drug

Electrospinning is considered a promising technology for encapsulating and loading various drugs into nanofibers. Metoprolol tartrate (MPT), hydrophilic therapy, was used as model drug. Metoprolol tartrate was loaded into poly(ɛ-caprolactone) (PCL) via blend and emulsion electospinning. The preparation processes, morphology, chemical structure thermal properties were evaluated. FESEM showed that emulsion electospinning produce larger fiber diameters(301.775nm) when compared to fibers produced by blend electrospinning(112.463, 249.34)nm, the PCL/ span 80 and MPT-PCL by emulsion method which have high fiber diameter than pure PCL and MPT-PCL by blend method and the Tm of pure PCL nanofibers and all drug loaded scaffolds are around 60°C from DSC test, water contact angle to pure PCL electrospun mats hydrophobic character (126.2°), while PCL/span 80, and PCL-drug nanofiber mats showed hydrophilic character. Our study demonstrated the possibility of using electrospinning with a promising good potential toward sustained and controlled drug delivery system.

scholarly journals Enhanced Dissolution and Oral Bioavailability of Cyclosporine A: Microspheres Based on αβ-Cyclodextrins Polymers

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 285 ◽  
Author(s):  
Malika Lahiani-Skiba ◽  
Francois Hallouard ◽  
Frederic Bounoure ◽  
Nicolas Milon ◽  
Youness Karrout ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Secondary Structure ◽  
Oral Administration ◽  
Drug Delivery System ◽  
Delivery System ◽  
Cyclosporine A ◽  
Polymer Mixture ◽  
Pharmacokinetic Parameters

Cyclosporine (CsA) has a selective property of suppressing various T-lymphocyte functions. This is of utmost importance in preventing allograft rejection by several organ transplantations, as well as in the treatment of systemic and local autoimmune disorders. However, the poor water solubility of CsA can be a major hurdle for its absorption into the blood stream, which leads to low bioavailability and thus less efficacy. The aim of this study was to prepare, characterize, and evaluate in vitro as well as in vivo, the potential of the innovative CsA drug delivery system. The latter contains CsA in spherical amorphous solid dispersion (SASD) which is embedded in an original α-cyclodextrin and β-cyclodextrin polymer mixture (Poly-αβ-CD) as a multifunctional amorphous carrier. The new developed SASD formulation showed that CsA was molecularly dispersed in αβ-cyclodextrins in an amorphous form, as was confirmed by physicochemical characterization studies. Interestingly, the peptide secondary structure, and thus, the drug activity was not impacted by the preparation of SASD as was shown by circular dichroism. Furthermore, the in vitro CsA release profile kinetics was almost identical to the commercially available product Neoral®. This study presents the first in vivo proof-of-concept for a novel drug delivery system based on Poly-αβ-CD containing CsA, with SASD allowing for increased bioavailibility. The pharmacokinetic parameters of cyclosporine A from the spherical spray-dried dispersion formulation was demonstrated in a “rat” animal model. For comparison, the commercially available Neoral® was studied. Importantly, the pharmacokinetic parameters were improved by extending Tmax from 2 to 3 h after the oral administration in rats, and eventually preventing the enterohepatic circulation. All these results clearly demonstrate the improved pharmacokinetic parameters and enhanced bioavailability of CsA in the new developed drug delivery system. These data demonstrated the superiority of the newly developed Poly-αβ-CD formulation for oral administration of the poorly soluble CsA in vivo without altering its secondary structure. Poly-αβ-CD can be a very useful tool for the oral administration of poorly water-soluble drugs.

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