scholarly journals Impact of Solubility Enhancement Methods on the Dissolution Rate of Valsartan Sachet

2021 ◽  
Vol 11 (1) ◽  
pp. 63-69
Author(s):  
Anjam H. Abdalla ◽  
Anoosh B. Hagop ◽  
Dina A. Boya

The oral drug delivery is the most generally used route of administration that has been explored for the delivery of drugs through various pharmaceutical products. Solubility of drug plays critical role in achieving the optimum therapeutic levels of the drug in blood and thus bioavailability. There are many drugs of various therapeutic categories fall in Biopharmaceutics Classification System Classes II and IV as they lack solubility. For all these drugs, dissolution is the big issue for the absorption process. Valsartan is an effective antihypertensive agent and it can be used for the treatment of hypertension in most cases. The objective of this study is to prepare Valsartan as an oral sachet which can be used as an alternative dosage form after improvement of drug solubility using solubilizing agents such as sodium lauryl sulfate and tween 80. Three different formulas of Valsartan sachet were prepared by conventional technique of wet granulation method named conventional formula (Fc), sodium lauryl sulfate formula (Fs), and tween 80 formula (Ft) then compared with the available marketed product of Valsartan tablet (Fd) as a reference. The preformulations studies were conducted to exclude drug excipients interaction. Evaluation was performed in terms of weight variation, dose content uniformity, and drug release study using dissolution test apparatus. Fourier Transforms Infrared Spectroscopy reveals no drug excipient interaction and the drug release profile for Fs and Ft formulas within 30 min was 100.16% and 104.16%, respectively, while for Fc only 57.55% of the drug was released. This difference in the release profile was statistically significant (P < 0.05) between Fs and Ft with Fc, but a non- significant difference (P > 0.05) was observed between Fs and Ft with the marketed Valsartan tablet (Fd). The results support the possibility of using the prepared formulas Fs and Ft as a Valsartan sachet for the oral administration alternative to conventional Valsartan tablets Fd.

2018 ◽  
Vol 10 (2) ◽  
pp. 20 ◽  
Author(s):  
Noor Mohammed Dawood ◽  
Shaimaa Nazar Abdal-hammid ◽  
Ahmed Abbas Hussien

Objective: The objective of this study was to prepare nanosuspension of a practical water insoluble antiulcer drug which is lafutidine to enhance the solubility, dissolution rate with studying the effect of different formulation variables to obtain the best formula with appropriate physical properties and higher dissolution rate.Methods: Nanosuspension of lafutidine was prepared using solvent anti-solvent precipitation method using Polyvinylpyrrolidone K-90(PVP K-90) as the stabilizer. Ten formulations were prepared to show the effect of different variables in which two formulations showed the effect of stabilizer type, three formulations showed the effect of stabilizer concentration, two formulations showed the effect of combination of polymer with surfactant such as tween 80, three formulations show the effect of stirring speed and three formulations prepare to show the effect of addition of co-surfactant such as tween 20. All these formulations are evaluated for their particle size and entrapment efficiency and in vitro release. The selected one was evaluated for zeta potential, scanning electron microscope, atomic force microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, saturation solubility and stability study.Results: The formulations (F3-F10) were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: polymer: surfactant ratio 1:4:4 and the optimum stirring speed was 1500 rpm. Dramatic effect on the particle size reduction was found by the addition of co-surfactant (tween 20) in formulation F7 that has a particle size 15.89±1.8 nm. The selected formula F7 showed an enhanced dissolution profile (10 min) compared to the pure drug at all-time intervals.Conclusion: The results show that the formulation that contains drug: PVP-K90: tween 80: tween 20 in ratio 1:4:2:2 is the best one and can be utilized to formulate lafutidine nanosuspension. 


2015 ◽  
Vol 26 (1) ◽  
pp. 40-44

The preparation suppositories contain 250 mg of paracetamol on different bases using Novata BD, Novata BCF and composition of Novata BCF/BD (1:1). Suppositories were prepared by the fusion method. The prepared formulations with or without surfactants (Tween 80, Span 60) at concentrations of 2% and 4% (w/w) were tested for hardness, to tal time of de for ma tion, disintegration time, content uniformity and release of the drug. The release of the drug was carried in the apparatus with the stirrer shade in phosphate buffer (pH 7.2) at 100 rpm. The physical properties of the prepared suppositories were according with the requirement of Polish Pharmacopoeia 9th edition. Addition of 4 % Tween 80 to suppository bases significantly increased the drug release from all the investigated formulations. However, incorporation of Span 60 did not result in improvement of the drug release significantly.


2014 ◽  
Vol 2014 ◽  
pp. 1-15 ◽  
Author(s):  
Rajni Bala ◽  
Sushil Khanna ◽  
Pravin Pawar

Clobazam orally dissolving strips were prepared by solvent casting method. A full 32 factorial design was applied for optimization using different concentration of film forming polymer and disintegrating agent as independent variable and disintegration time, % cumulative drug release, and tensile strength as dependent variable. In addition the prepared films were also evaluated for surface pH, folding endurance, and content uniformity. The optimized film formulation showing the maximum in vitro drug release, satisfactory in vitro disintegration time, and tensile strength was selected for bioavailability study and compared with a reference marketed product (frisium5 tablets) in rabbits. Formulation (F6) was selected by the Design-expert software which exhibited DT (24 sec), TS (2.85 N/cm2), and in vitro drug release (96.6%). Statistical evaluation revealed no significant difference between the bioavailability parameters of the test film (F6) and the reference product. The mean ratio values (test/reference) of Cmax (95.87%), tmax (71.42%), AUC0−t (98.125%), and AUC0−∞ (99.213%) indicated that the two formulae exhibited comparable plasma level-time profiles.


Author(s):  
C.C. Patil ◽  
J. Vekatesh ◽  
S. R Karajgi ◽  
Vijapure Vitthal ◽  
Ashwini G. ◽  
...  

The aim of this project was to develop sustained release matrix tablets of Repaglinide. Sustained release matrix tablets of Repaglinide were prepared by the wet granulation method using polymers like Hydroxy propyl methyl cellulose, Microcrystalline cellulose, Eudragit RS-100 in different ratios. The matrix tablets of Repaglinide were evaluated for hardness, weight variation, friability, drug content uniformity, and in-vitro drug release. In order to determine the drug release mechanisms and kinetics, the data was subjected to zero order, first order, and higuchi and peppas diffusion model. Twelve batches of sustained release matrix tablets of Repaglinide were developed. Among these formulations F4, F8 and F12 formulation showed satisfactory physicochemical properties and drug content uniformity and sustained release of drug for 12 hours with maximum release of 86.95%, 84.91% and 84.91%. The optimized formulations were characterized for Differential scanning calorimetric analysis; Fourier transforms infrared spectroscopy and scanning electron microscopic studies. IR spectroscopic studies indicated that there were no drug-excipient interactions. The prepared sustained release matrix tablets of Repaglinide were successfully developed and evaluated.


Author(s):  
Bipul Nath ◽  
Tushar Roy

The objectives of present investigation is to evaluate the compatibility of Atorvastatin calcium with immediate release excipients and to optimize the tablet which release is best comparable with innovator product by varying different super disintegrants. Various excipients used were sodium starch glycollate, cross carmellose sodium, cross-povidone, lactose, micro crystalline cellulose, mannitol, sodium lauryl sulfate, magnesium stearate, and stearic acid. Thermal characterization of the drug was done by DSC and FT-IR. From the DSC studies, the excipients such as microcrystalline cellulose (Avicel 101), magnesium stearate, mannitol, sodium lauryl sulfate were found to have physical interactions with Atorvastatin. Immediate release tablet was prepared by direct compression method and its release profile was compared with the marketed IR tablet. The prepared tablet have conform the pharmacopoeial limit for hardness, thickness, friability, weight variation and content uniformity. Formulation F11 containing two super disintegrants have shown the disintegration time less than 25 sec and better dissolution than all other formulations releasing more than 80% of the drug after 20 minutes. Kinetic data reveals that the drug release follows best order by Higuchi model, followed by korsemeyer peppas, zero order and first order mechanisms. The results of accelerated stability studies as per ICH guidelines indicated that the tablet was stable as there were no any significant physical changes after the study.


2018 ◽  
Vol 10 (1) ◽  
pp. 109
Author(s):  
Musiliu Adedokun ◽  
Clement Nkanta

Objective: The aim of this research work was to comparatively study various proportions of a natural hydrocolloid-Raphia africana, and polyvinylpyrrolidone (PVP) as release sustaining agents in diclofenac sodium tablet formulation.Methods: The purified hydrocolloid (R. africana) was characterized by evaluating its organoleptic, physicochemical and flow properties. Diclofenac-polymer ratios of 1:0, 1:0.2, 1:0.4, 1:0.6, and 1:0.8 were employed to produce different granule batches using wet granulation method (that is, the drug was formulated with 0, 5, 10, 15 and 20 % w/w of either R. africana hydrocolloid or PVP, and coded DWB-00, DRA-05, DRA-10, DRA-15, DRA-20, DPP-05, DPP-10, DPP-15 and DPP-20, respectively). Flow properties of granules were studied by determining bulk density, tapped density, Carr’s index, and Hausner’s ratio for all the formulations. Compressed tablets were evaluated using various parameters as weight variation, friability, hardness, tablet thickness and diameter, content uniformity and in vitro dissolution evaluated in phosphate buffer (pH 7.3).Results: Flowability, mechanical and release parameters determined were within pharmacopoeial limits. Generally, the values of bulk and tapped densities increase as binder concentrations increase for both PVP and R. africana hydrocolloid. The values were significantly different across the batches (p<0.05). Hardness values obtained varied significantly (p<0.05) and were between 5 and 12 KgF which imply that most of the tablet batches are harder than normal depending on the proportion of the polymer used. All the batches exhibited friability within the standard limit without significant difference in values (p>0.05), indicating that tablet formulated with the experimental binders would not undergo surface abrasion. All the formulations exhibited zero order kinetics except batches DPP-10 and DPP-15 which showed Higuchi mechanism. Formulation batches DRA-05 and DRA-10 showed maximum drug release of 98% and 95% respectively after 6 h. A prolonged drug release was observed on increasing polymer ratio. Significantly higher release rates (p<0.05) were observed in the tablets formulated with PVP than those containing R. africana gum. All the batches followed non-fickian diffusion release mechanism.Conclusion: From the study, purified R. africana hydrocolloid generally appeared to perform better than PVP as sustained release agent.


Author(s):  
DIPANJANA ASH ◽  
SUTAPA BISWAS MAJEE ◽  
GOPA ROY BISWAS

Objective: The objective of the present investigation was to develop olive and soybean oil-based oleogels with Span 40 and/or Tween 80 (as gelator and/or surfactant) and determine the critical gelator concentration (CGC), characterise and compare the rheological, thermal properties and drug release profile of the gels formed for topical delivery. Methods: Olive and soybean oil-based Span 40 and Span 40/Tween 80 oleogel formulations were prepared by solid fiber mechanism and subjected to organoleptic evaluation, FT-IR spectroscopy, thermal analysis, rheological study, kinetic modeling of gelation and drug release. Results: The critical gelator (Span 40) concentration was found to be lower for olive oil (12% w/v) and depend on the type of oil. Tween 80 reduced CGC of soybean oleogels only. Soybean oil-based oleogel containing 18% w/v Span 40 was found to form more flexible, less viscous and thermally less stable formulation with better release of paracetamol as evident from lower melt flow index, Tg value, lower β and higher α value compared to olive oil-based oleogel with 12% w/v Span 40 (CGC). Surfactant addition can be assumed to modify the microarchitecture of the oleogels to a great extent to produce more flexible and thermally stable gels with even better drug release profile. Span-Tween based soybean oleogel formed a gel-matrix whereas matrix in olive oil-based oleogels containing Span only became slightly flexible to release the drug in zero-order fashion on the addition of surfactant cogelator. Conclusion: Nature of oil exerts profound influence on the rheological, thermal and release profile of oleogels containing Span 40 as gelator and/or Tween 80 as surfactant cogelator.


2003 ◽  
Vol 66 (8) ◽  
pp. 1462-1464 ◽  
Author(s):  
RENEE M. RAIDEN ◽  
JOEMEL M. QUICHO ◽  
CORYELL J. MAXFIELD ◽  
SUSAN S. SUMNER ◽  
JOSEPH D. EIFERT ◽  
...  

Fresh produce has been implicated in several foodborne disease outbreaks. A primary site of contamination during production and handling is the surface of produce. One approach to reducing contamination is to treat fresh produce with rinsing agents. Studies have examined the efficacies of detergents and other rinses in recovering pathogens from produce surfaces. The determination of how these detergents affect bacterial cells may aid in understanding the mechanisms behind their removal. This study examines the survivability of Salmonella and Shigella in two detergents. A 0.1% sodium lauryl sulfate (SLS) solution, a 0.1% Tween 80 solution, and water were inoculated with a cocktail of stationary-phase organisms (3 log CFU/ml) and incubated for up to 32 h at 22°C and 40°C. Samples were taken over time and plated on tryptic soy agar supplemented with 50 ppm of nalidixic acid. Salmonella survived in all solutions and exhibited significant growth in water (0.8 log CFU/ml at 22°C and 1.9 log CFU/ml at 40°C) and Tween 80 (1.0 log CFU/ml at 40°C). Shigella survived in all solutions at 22°C and exhibited a growth level of 2.0 log CFU/ml in SLS. Shigella also survived in all solutions at 40°C, although its populations decreased significantly in Tween 80 over time. Elevated temperatures may allow Tween 80 to kill Shigella spp. over time. Overall, the detergents tested were not detrimental to the cells; therefore, if these solutions were to be used as produce rinse agents, they would aid in removal of organisms from surfaces rather than kill the cells.


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