scholarly journals IMPROVEMENT OF THE DISSOLUTION PROFILE OF SIMVASTATIN TABLETS WITH THE ADDITION OF CREMOPHOR-EL USING WET GRANULATION METHOD

2021 ◽  
pp. 244-246
Author(s):  
FIRMAN GUSTAMAN ◽  
KENI IDACAHYATI ◽  
WINDA TRISNA WULANDARI ◽  
FAJAR SETIAWAN ◽  
INDRA INDRA
Keyword(s):  
Phosphate Buffer ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Dissolution Test ◽  
Cremophor El ◽  
Dissolution Medium ◽  
First Line ◽  
Drug Levels ◽  
P Glycoprotein ◽  
Low Solubility

Objective: Simvastatin is a drug used as a first-line anti-cholesterol in the treatment of dyslipidemia. Low solubility will affect its ability to penetrate the digestive tract membrane and will affect the amount of drug levels in the plasma. The use of Cremophor-EL as a surfactant has been shown to inhibit the action of P-glycoprotein so that it can increase the bioavailability of a drug and can increase the effect of a drug. Methods: The preparation of simvastatin tablets was carried out using the wet granulation method. The dissolution test used the paddle method, a speed of 50 rpm at a temperature of 37±0.5 ° C with a phosphate buffer pH 7.0 as the dissolution medium. Results: The results showed that at 30 min the generic simvastatin tablets had 81.52% dissolution and the Simvastatin Tablets with Cremophor-EL were 85.520%. Conclusion: Simvastatin cremophor-EL tablets are more dissolved than generic simvastatin at 30 min so that cremophor-EL simvastatin tablets have a better dissolution rate than generic simvastatin tablets.

scholarly journals DISSOLUTION IMPROVEMENT OF KETOPROFEN THROUGH POLYMER MATRIX COMPOSITE POVIDONE K-30/TiO2

2021 ◽  
Vol 9 (Spl-2-ICOPMES_2020) ◽  
pp. S234-S240
Author(s):  
Aliyah . ◽  
◽  
Eka Tri Saputri ◽  
Diana Fitriah ◽  
Andi Arjuna ◽  
...  
Keyword(s):  
Matrix Composite ◽  
Polymer Matrix ◽  
Phosphate Buffer ◽  
Release Profile ◽  
Polymer Matrix Composite ◽  
Composite Particles ◽  
Coating Process ◽  
Dissolution Profile ◽  
Low Solubility ◽  
Biopharmaceutics Classification

Ketoprofen is a nonsteroidal anti-inflammatory drug that has been classified into Class II as per the Biopharmaceutics Classification System. This substance has low solubility i.e. only 51 mg/L at 22℃. Therefore, a study of ketoprofen modification prepared in Polymer Matrix Composite (PMC) using Povidone K-30, coated with TiO2 as an effort to improve its dissolution profile, had been conducted. Composite particles were prepared through a dissolving method with a ratio of ketoprofen: Povidone K30 i.e. 1: 1 (F1), 1: 2 (F2), and 1: 4 (F3). They were evaluated and continued on the coating process using TiO2 30%, 40%, and 50%. Results of the study revealed that the PMC provides an absence of chemical intervention against ketoprofen. All the used combination ratios improved the dissolution profile by using phosphate buffer media pH 7.5 for 60 minutes. After coating, a release profile was obtained by running it on phosphate buffer media at pH 6.8 for 8 hours, this showing a sustained release profile.

scholarly journals Development of a dissolution test for lamotrigine in tablet form using an ultraviolet method

2010 ◽  
Vol 46 (2) ◽  
pp. 179-186 ◽  
Author(s):  
Magda Targa Martins ◽  
Clésio Soldatelli Paim ◽  
Martin Steppe
Keyword(s):  
Hydrochloric Acid ◽  
Reference Product ◽  
Single Point ◽  
Analysis Procedure ◽  
Dissolution Profile ◽  
Dissolution Test ◽  
Dissolution Medium ◽  
Tablet Form

A dissolution test for tablets containing 100 mg of lamotrigine was developed and validated. The dissolution test was applied to compare the dissolution profile of Neural® with the reference product Lamictal®. The analysis procedure was carried out using a simple ultraviolet method at 267 nm. After the determination of solubility and sink conditions, the parameters selected were paddles at 50 rpm, 900 mL of 0.01 M hydrochloric acid, and 30 minutes duration (single point). This method was validated for specificity, linearity, accuracy, precision and robustness. Lamotrigine stability was also evaluated in dissolution medium.

Formulation and Evaluation of Microbially- triggered tablets of Valdecoxib

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma
Keyword(s):  
Phosphate Buffer ◽  
Guar Gum ◽  
Oral Route ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Study ◽  
Caecal Content ◽  
Model Drug

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.

The Effect of Different Superdisintegrants and their Concentrations on the Dissolution of Topiramate Immediate Release Tablets

2009 ◽  
Vol 2 (2) ◽  
pp. 531-5366
Author(s):  
V A. Vamshi Priya ◽  
G. Chandra Sekhara Rao ◽  
D. Srinivas Reddy ◽  
V. Prabhakar Reddy
Keyword(s):  
Immediate Release ◽  
Drug Dissolution ◽  
Dissolution Profile ◽  
Dissolution Medium ◽  
Lactose Monohydrate ◽  
Sodium Starch Glycolate ◽  
Tablet Disintegration ◽  
Croscarmellose Sodium ◽  
Model Drug ◽  
Usp Apparatus

The purpose of this study was to investigate the efficiency of superdisintegrants: sodium starch glycolate, croscarmellose sodium and crospovidone in promoting tablet disintegration and drug dissolution of Topiramate immediate release tablets. The efficiency of superdisintegrants was tested, by considering four concentrations, viz., like 2%, 3%, 4% and 5% in the formulations. The dissolution was carried out in USP apparatus II at 50 rpm with distilled water as a dissolution medium. The dissolution rate of the model drug topiramate was found highly dependent on the tablet disintegration, on the particle size of the superdisintegrant, on the solubility of the drug and also on the type of superdisintegrant in the dissolution medium. There was no effect of the diluent (Lactose monohydrate) on the disintegration of different concentrations of superdisintegrants. These results suggest that, as determined by the f2 metric (similarity factor), the dissolution profile of the formulation containing 4% sodium starch glycolate and lactose monohydrate as a diluent was similar to that of a marketed product.

Formulation and Evaluation of Immediate Release Bilayer Tablets of Telmisartan and Hydrochlorothiazide

2011 ◽  
Vol 4 (3) ◽  
pp. 1477-1483
Author(s):  
Natarajan R ◽  
N Patel ◽  
Rajendran N N ◽  
M Rangapriya
Keyword(s):  
Antihypertensive Drugs ◽  
In Vitro Release ◽  
Immediate Release ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Sodium Starch Glycolate ◽  
Bilayer Tablets

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.  

scholarly journals Developing methods to compare tablet formulations of atorvastatin

2012 ◽  
Vol 48 (4) ◽  
pp. 801-810 ◽  
Author(s):  
Marcelo Antonio de Oliveira ◽  
Caroline Dutra Lacerda ◽  
André Fazôlo Bonella
Keyword(s):  
Rotation Speed ◽  
Pharmaceutical Formulations ◽  
Generic Product ◽  
Dissolution Test ◽  
Dissolution Medium ◽  
Differential Dissolution ◽  
Tablet Formulations ◽  
Biopharmaceutical Classification System ◽  
Paddle Apparatus ◽  
The Ideal

Atorvastatin (ATV) is an antilipemic drug of great interest to the pharmaceutical industry. ATV does not appear in the monographs of Brazilian pharmacopoeia, and analytical methodologies for its determination have been validated. The chromatographic conditions used included: RP-18 column-octadecylsilane (250 x 4.6 mm, 5 mm), detection at 238 nm, mobile phase containing 0.1% phosphoric acid and acetonitrile (35:65% v/v), flow at 1.5 mL min-1, oven temperature at 30ºC, and injection volume of 10 mL. ATV is classified as a class II product, according to the biopharmaceutical classification system. As such, a dissolution test was proposed to evaluate pharmaceutical formulations on the market today, under the following conditions: water as a dissolution medium, 1000 mL as a volume, paddle apparatus at a rotation speed of 50 rpm, 80% (Q) in 15 minutes with UV spectrophotometer readings at 238 nm. In the pattern condition proposed as the ideal dissolution test, which appropriately differentiates amongst formulations, the generic product was not considered pharmaceutically equivalent; however, in other less differential dissolution methods, which also fall within appropriate legal parameters, this product could come to be regarded as generic.

scholarly journals EFFECT OF SELECTED POLYMERS ON DISSOLUTION AND STABILIZATION OF AMORPHOUS FORM OF MELOXICAM

2017 ◽  
Vol 9 (9) ◽  
pp. 33
Author(s):  
Rana Obaidat ◽  
Bashar Al-taani ◽  
Hanan Al-quraan
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersions ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 4000 ◽  
Amorphous Form ◽  
Molecular Weights ◽  
Low Solubility ◽  
Reproducible Manner

Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release.Conclusion: The dissolution profile of meloxicam has been increased successfully in a reproducible manner.

scholarly journals Assessment of physical and dissolution characteristics of various itraconazole capsule formulations: a comparative analysis

2019 ◽  
Vol 5 (4) ◽  
pp. 765
Author(s):  
Rajan Verma ◽  
Shrikant Hodge ◽  
Chandrashekhar Gargote ◽  
Prakash Modi ◽  
Naresh Upreti ◽  
...  
Keyword(s):  
Size Distribution ◽  
Phosphate Buffer ◽  
Acetate Buffer ◽  
Simulated Gastric Fluid ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Lauryl Sulfate ◽  
Complete Dissolution ◽  
Innovator Product

<p class="abstract"><strong>Background:</strong> This <em>in vitro</em> study compared physical parameters and the dissolution profile of innovator itraconazole capsule formulation, i-Tyza, and 5 other generic capsule formulations available in the Indian market.</p><p class="abstract"><strong>Methods:</strong> The number of pellets and size distribution were determined using naked eye examination and sieving method, respectively. Dissolution profile of formulations was done at 15, 30, 45, and 60 minutes, using a United States Pharmacopeia type II Paddle apparatus in simulated gastric fluid (SGF, pH 1.2) without enzymes, acetate buffer (pH 4.5) with 0.5% sodium lauryl sulfate (SLS), and phosphate buffer (pH 6.8) with 0.5% SLS.<strong></strong></p><p class="abstract"><strong>Results:</strong> All formulations had capsule size 0. Capsule fill weight (~335 to ~510 mg) and total pellet number (127 to 810) varied across formulation, with the innovator brand having the highest number of pellets. Innovator product and i-Tyza had similar fill weight (~460 mg). Pellet size distribution of the innovator product, brand 2, brand 3, and i-Tyza was relatively narrow. In SGF, except brand 1 (84% dissolved) and brand 5 (80% dissolved), all the formulations had near-complete (&gt;85% drug dissolved) or complete dissolution (&gt;90% drug dissolved) at 60 minutes. In acetate buffer, pH 4.5 with 0.5% SLS and phosphate buffer, pH 6.8 with 0.5% SLS, only the innovator product and i-Tyza demonstrated near-complete to complete dissolution at 60 minutes (96% and 90% dissolved).</p><p class="abstract"><strong>Conclusions:</strong> Across all the itraconazole generic formulations evaluated, i-Tyza had comparable physical characteristics and dissolution profile to the innovator product. The <em>in vitro</em> dissolution profile of i-Tyza may indicate adequate <em>in vivo</em> performance.</p>

scholarly journals Evaluation of pharmacokinetic properties of isobornylphenols in silico

2020 ◽  
Vol 35 (4) ◽  
pp. 79-86
Author(s):  
O. I. Ostrikova ◽  
O. E. Vaizova ◽  
O. I. Aliev ◽  
E. V. Buravlev ◽  
I. Yu. Chukicheva ◽  
...  
Keyword(s):  
Toxicity Assessment ◽  
Pharmacokinetic Parameters ◽  
Structure Property ◽  
Solubility In Water ◽  
Virtual Tools ◽  
Internet Resources ◽  
P Glycoprotein ◽  
Pharmacokinetic Properties ◽  
Low Toxicity ◽  
Low Solubility

Introduction. The potential of a new compound in the ongoing drugs discovery process is initially explored using virtual instruments, where its activity is predicted based on its molecular structure.Aim. This study aimed to evaluate the pharmacokinetic parameters and possible toxicity of isobornyl compounds based on virtual tools.Material and Methods. Several free Internet resources were used to assess the absorption, distribution, metabolism, excretion (ADME), and toxicity (T) of 2,6-diisobornyl-4-methylphenol (1, Dibornol), 2-hydroxy-3-isobornyl-5-methylbenzaldehyde (2), and 2-((di-n-butylamino) methyl)-6-isobornyl-4-methylphenol (3). Pharmacokinetic properties were calculated on ADMETlab platform. Toxicity and physical properties were evaluated using TEST software based on the structure-property quantification models of organic substances according to structure–property principle. Web server ProTox_II was used for acute toxicity assessment.Results. Plasma protein binding degrees were 76,9% for (1), 85,9% for (2), and 91,8% for (3). All three compounds were capable of penetrating the blood-brain barrier. Dibornol was identified neither as a substrate nor as an inhibitor of P-glycoprotein unlike (2) and (3). The half-life of all compounds was short (about 2 hours); the clearance was slow (about 2 mL/min*kg). The study showed that (2) and (3) potentially exert the toxic effects during the developmental stage of the organism, while ADMETlab showed potential cardio- and hepatotoxicity for (2) and (3), respectively. All compounds had extremely low solubility in water, which affected the assessments of other indicators by TEST software. The ProTox_II server showed the extremely low toxicity LD50 for all compounds (toxicity class 5).

Formulation and Evaluation of Immediate Release Tablets of Etizolam

2021 ◽  
pp. 281-284
Author(s):  
Abhishek Kumar Singh ◽  
Kasif Shakeel
Keyword(s):  
Immediate Release ◽  
Magnesium Stearate ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Compressibility Index ◽  
Tablet Hardness ◽  
In Vitro Disintegration

In the present investigation, immediate release tablet formulation of etizolam was developed for management of insomnia and anxiety using different Superdisintegrants (Sodium Starch Glycolate, Croscarmellose, Crospovidone), Povidone K-30 and Magnesium stearate by wet granulation method. The drug-excipients interaction was investigated by UV spectrophotometer. The granules and tablets of Etizolam were evaluated for various pre and post compression parameters like angle of repose, compressibility index, hausners ratio, tablet hardness, friability and in vitro disintegration and dissolution studies and their results were found to be satisfactory. These results suggest that maximum in vitro dissolution profile of formulation F6 were found to have equivalent percentage of drug release and concluded that F6 is better and similar to innovator product.

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