scholarly journals Effects of Magnesium Hydroxide on Disintegration Time and Dissolution Rate of Diclofenac Sodium Plain Tablet

1970 ◽  
Vol 2 ◽  
pp. 42-48
Author(s):  
Md Mosharaf Miazi ◽  
M Mohiuddinn A Choudhury ◽  
M Habibur Rahman ◽  
Abedur Rahman
Keyword(s):  
Dissolution Rate ◽  
Magnesium Hydroxide ◽  
Diclofenac Sodium ◽  
Gastric Fluid ◽  
Simulated Gastric Fluid ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Standard Specification ◽  
Disintegration Time ◽  
Investigational Agent

The objective of this study was to evaluate the effects of magnesium hydroxide (MH) on disintegration time (DT) and dissolution profile of diclofenac sodium (DS) plain tablet. The tablets of DS were formulated with conventionally used excipients and investigational agent Mg [OH]2. Different parameters of tablets like hardness, thickness, friability, and disintegration time and dissolution rate were determined to assess the effects of MH on these parameters. The physical resistance against abrasion or shock of DS-MH tablets had been noticed by the results of hardness and friability test which were within the limits of standard specification. The disintegration times of tablets of the experimental batches except one, found 2.0 to 25 minutes were also within the limits of standard specification. The release rates of DS in simulated gastric fluid (SGF) at 30 minutes were inspiring about batches FO3: 84.78% and FO4: 90.38%. A positive correlation of coefficient determined between quantity of Mg(OH)2 in different batches of tablets and their effects on dissolution rate was found statistically significant (r = 0.66). The tmax of DS was not affected by the presence or increment of MH as evident in rtmax= 0.50. The overall study indicated that Magnesium hydroxide didn't affect the different physical parameters of plain tablet rather it in certain quantity while present in some batches assisted rapid disintegration and release profile of active content Diclofenac sodium. The DS-MH plain tablet to provide rapid disintegration, dissolution and absorption hence fastest anti-inflammatory action with acid neutralizing benefits by MH, might be considered sincerely Key words: Diclofenac Sodium; Magnesium Hydroxide; Disintegration; Dissolution DOI:10.3329/jbsp.v2i0.984 J Bangladesh Soc Physiol. 2007 Dec;(2): 42-48.    

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>

Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-Soluble Drug (Curcurmin)

2011 ◽  
Vol 393-395 ◽  
pp. 119-122
Author(s):  
Dong Hua Wan ◽  
Fen Lin ◽  
Qu Xiang Liao
Keyword(s):  
Dissolution Rate ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Gastric Fluid ◽  
Molecular State ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Simulated Gastric Fluid ◽  
Scanning Calorimetry ◽  
Rate Improvement

It’s well known that curcumin is practically insoluble in water. Therefore, to improve the drug dissolution rate, fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads. The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid. The concentration of the dissolved drug in the medium was determined by HPLC. The dissolution rates of the formulations were dependent on the drug loading in SDs. 92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load, whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads, respectively. The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier. Furthermore, their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction. In the dispersions containing 8.97% CUR, the drug was in the molecular state. At a composition of approximately 18.9%, CUR was dispersed as micro-fine crystals. These interesting results indicate that the physical states of the drug in the carrier, which are governed by the drug loading, can affect the dissolution rate improvement.

scholarly journals Eight enteric-coated 50 mg diclofenac sodium tablet formulations marketed in Saudi Arabia: in vitro quality evaluation

2020 ◽  
Vol 13 (1) ◽  
Author(s):  
Muhammad M. Hammami ◽  
Rajaa F. Hussein ◽  
Reem AlSwayeh ◽  
Syed N. Alvi
Keyword(s):  
Quality Evaluation ◽  
Diclofenac Sodium ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
United States Pharmacopoeia ◽  
Weight Variation ◽  
Tablet Formulations ◽  
Enteric Coated

Abstract Objective To evaluate in vitro quality of enteric-coated 50 mg diclofenac sodium tablet formulations on Saudi market. Results A reference and seven generic (G1-7) formulations were commercially available in December 2019/January 2020 and were assessed within 25–75% of manufacture-expiration period. Weight variation (range as% difference from mean, n = 20), active substance content (ASC, mean (SD) as% difference from label, n = 20), hardness (mean (SD), n = 10), and friability (% weight loss, n = 20) were 97–103%, 102.0% (3.4%), 15.4 (1.1) kg, and 0.24%, respectively, for the reference. For G2-7, they were ≤ ±5%, 98.6% (4.0%) to 109.9% (1.8%), 11.9 (0.9) to 18.3 (0.8) kg, and ≤ 0.00 to 0.75%, respectively. G1 ASC, hardness, and friability were 111.3% (1.7%), 20.1 (1.7) kg, and 1.10%, respectively. Disintegration time (n = 6) and dissolution profile (n = 8) were also determined. No formulation disintegrated or released ˃ 0.1% of label ASC in 0.1 N HCl for 2 h. The reference disintegrated in 15:00 min:seconds and released a mean (range) of 100% (99–103%) of label ASC by 45 min in phosphate buffer (pH = 6.8). G1-7 disintegrated in 8:53 to 20:37 min:seconds and released 81% (69–90%) (G1) to 109%. Except for borderline performance of G1, all formulations passed in vitro quality tests according to United States Pharmacopoeia.

scholarly journals In Vitro Dissolution Profile of Dapagliflozin: Development, Method Validation, and Analysis of Commercial Tablets

2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Rafaela Zielinski Cavalheiro de Meira ◽  
Aline Biggi Maciel ◽  
Fabio Seigi Murakami ◽  
Paulo Renato de Oliveira ◽  
Larissa Sakis Bernardi
Keyword(s):  
Quality Evaluation ◽  
Systematic Approach ◽  
Gastric Fluid ◽  
Scientific Basis ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Dissolution Profile ◽  
Sodium Glucose Cotransporter ◽  
Dissolution Efficiency

Dapagliflozin was the first of its class (inhibitors of sodium-glucose cotransporter) to be approved in Europe, USA, and Brazil. As the drug was recently approved, there is the need for research on analytical methods, including dissolution studies for the quality evaluation and assurance of tablets. The dissolution methodology was developed with apparatus II (paddle) in 900 mL of medium (simulated gastric fluid, pH 1.2), temperature set at 37±0.5°C, and stirring speed of 50 rpm. For the quantification, a spectrophotometric (λ=224 nm) method was developed and validated. In validation studies, the method proved to be specific and linear in the range from 0.5 to 15 μg·mL−1 (r2=0.998). The precision showed results with RSD values lower than 2%. The recovery of 80.72, 98.47, and 119.41% proved the accuracy of the method. Through a systematic approach by applying Factorial 23, the robustness of the method was confirmed (p>0.05). The studies of commercial tablets containing 5 or 10 mg demonstrated that they could be considered similar through f1, f2, and dissolution efficiency analyses. Also, the developed method can be used for the quality evaluation of dapagliflozin tablets and can be considered as a scientific basis for future official pharmacopoeial methods.

scholarly journals pH-Sensitive Alginate/Carboxymethyl Chitosan/Aminated Chitosan Microcapsules for Efficient Encapsulation and Delivery of Diclofenac Sodium

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 338
Author(s):  
Ahmed M. Omer ◽  
Maha S. Ahmed ◽  
Gehan M. El-Subruiti ◽  
Randa E. Khalifa ◽  
Abdelazeem S. Eltaweil
Keyword(s):  
Drug Carrier ◽  
Diclofenac Sodium ◽  
Gastric Fluid ◽  
Carboxymethyl Chitosan ◽  
Ph Sensitive ◽  
Simulated Gastric Fluid ◽  
Burst Release ◽  
Polyelectrolyte Complexes ◽  
Thermogravimetric Analyzer ◽  
Ft Ir

To develop an effective pH-sensitive drug carrier, alginate (Alg), carboxymethyl chitosan (CMCs), and aminated chitosan (AmCs) derivatives were employed in this study. A simple ionic gelation technique was employed to formulate Alg-CMCs@AmCs dual polyelectrolyte complexes (PECs) microcapsules as a pH-sensitive carrier for efficient encapsulation and release of diclofenac sodium (DS) drug. The developed microcapsules were characterized by Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analyzer (TGA), and scanning electron microscope (SEM). The results clarified that formation of dual PECs significantly protected Alg microcapsules from rapid disintegration at colon conditions (pH 7.4), and greatly reduced their porosity. In addition, the dual PECs microcapsules can effectively encapsulate 95.4% of DS-drug compared to 86.3 and 68.6% for Alg and Alg-CMCs microcapsules, respectively. Higher DS-release values were achieved in simulated colonic fluid [SCF; pH 7.4] compared to those obtained in simulated gastric fluid [SGF; pH 1.2]. Moreover, the drug burst release was prevented and a sustained DS-release was achieved as the AmCs concentration increased. The results confirmed also that the developed microcapsules were biodegradable in the presence of the lysozyme enzyme. These findings emphasize that the formulated pH-sensitive microcapsules could be applied for the delivery of diclofenac sodium.

scholarly journals Evaluation of Prunus domestica gum as a novel tablet binder

2014 ◽  
Vol 50 (1) ◽  
pp. 195-202 ◽  
Author(s):  
Haroon Rahim ◽  
Mir Azam Khan ◽  
Amin Badshah ◽  
Kamran Ahmad Chishti ◽  
Salimullah Khan ◽  
...  
Keyword(s):  
Magnesium Stearate ◽  
Angle Of Repose ◽  
Binding Potential ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Prunus Domestica ◽  
Disintegration Time ◽  
Model Drug ◽  
Pvp K30

To evaluate binding potential of Prunus domestica gum in tablets formulations. Six tablet batches (F-1B to F-6B) were prepared by wet granulation method, containing Avicel pH 101 as diluent, sodium diclofenac as model drug using 10, 15 and 20 mg of Prunus domestica gum as binder and PVP K30 was used as standard binder. Magnesium stearate was used as lubricant. Flow properties of granules like bulk density, tapped density, Carr index, Hausner’s ratio, angle of repose as well as physical parameters of the compressed tablets including hardness, friability, thickness and disintegration time were determined and found to be satisfactory. The FTIR spectroscopic analysis showed that the formulation containing plant gum is compatible with the drug and other excipients used in tablets formulation. Hence the plant gum has role as a potential binder in tablets formulations. The dissolution profile showed that tablets formulations containing Prunus domestica gum 15 mg/200 mg of total weight of tablet as binder showed better results as compared to PVP K30.

scholarly journals Design of Catalase Monolithic Tablets for Intestinal Targeted Delivery

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 69
Author(s):  
Mirna Alothman ◽  
Pompilia Ispas-Szabo ◽  
Mircea Alexandru Mateescu
Keyword(s):  
Targeted Delivery ◽  
Intestinal Inflammation ◽  
Gastric Fluid ◽  
Oral Dosage ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Dissolution Profile ◽  
Negative Effects ◽  
Simulated Intestinal Fluid

Several studies confirmed a correlation between elevated hydrogen peroxide (H2O2) levels in patients with intestinal bowel diseases (IBD) and the negative effects caused by its presence. The objective of this study was to explore the potential use of catalase (CAT) to diminish the level of H2O2 and its deleterious action on intestinal mucosa. Oral dosage forms of a CAT bioactive agent targeted to the intestines were designed and tested in various simulated gastric and intestinal media. Monolithic tablets (30% loading) were prepared using commercial CarboxyMethylCellulose (CMC) or synthesized CarboxyMethylStarch (CMS) and TriMethylAmineCarboxyMethylStarch (TMACMS) as matrix-forming excipients. For starch derivatives, the presence of the ionic groups (carboxymethyl and trimethylamine) was validated by spectral analysis. In vitro studies have shown that tablets formulated with TMACMS and 30% CAT resisted the acidity of the simulated gastric fluid and gradually released the enzyme into the simulated intestinal fluid. The investigation of the CAT release mechanism revealed the role of anionic and cationic groups of polymeric excipients and their involvement in the modulation of the CAT dissolution profile. The proposed drug delivery system can be considered an efficient solution to target CAT release in the intestine and contribute to the reduction of H2O2 associated with intestinal inflammation.

Quality and Safety Evaluation of Commercial Mangosteen (Garcinia mangostana Linn.) Capsule

10.17158/333 ◽  
2014 ◽  
Vol 18 (2) ◽  
Author(s):  
Ma. Eva C. San Juan ◽  
Razle R. Alagos ◽  
Ruiza R. Alocelja ◽  
Ruel S. Manluyang Jr.
Keyword(s):  
Normal Limit ◽  
Safety Evaluation ◽  
Gastric Fluid ◽  
Plate Count ◽  
Simulated Gastric Fluid ◽  
Human Consumption ◽  
Garcinia Mangostana ◽  
Disintegration Time ◽  
Quality Control Standard ◽  
Aerobic Plate Count

<p>Many herbal food supplements today are being sold in market and most popular among them is the commercial mangosteen (Garcinia mangostana Linn.) capsule. With the present scenario, this study focused on ensuring the quality of commercial mangosteen (Garcinia mangostana Linn.) capsule being sold in the market for consumer’s safety. Based on results of experimentations, the sample of commercial mangosteen capsule passed all the tests conducted. The disintegration time using water and simulated gastric fluid as a solvent was within the 30 minutes specification set by 22nd edition of USP XXII/ NF XVII, which was at 21.88 minutes and 10.83 minutes, respectively. Result also revealed that commercial mangosteen capsule was more soluble in simulated gastric fluid when compared to water since, in the first test, all the capsule disintegrated completely within 30 minutes at a lower mean disintegration time and the residue left after the experimentation was lesser. For microbial limit tests, the Aerobic Plate Count (CFU/g) was 540 (normal limit - 104), Yeast (CFU/g) at 135 (normal limit -103), and Molds (CFU/g) at 10 (normal limit- 103). Lastly, for heavy metal load, Cadmium (ug/g) has &lt;0.05 (normal limit - 0.3) and Lead (ug/g) has 2.73 (normal limit – 10). All results conformed to FDA Guidelines. Therefore, commercial mangosteen capsule has met the minimum quality control standard and is safe for human consumption based on the 22nd edition of USP XXII/NF XVII specifications and FDA Guidelines.</p>

scholarly journals Comparative Physicochemical Evaluation of Selective Brands of Diclofenac Potassium Tablets Available in Pakistan

2020 ◽  
pp. 90-97
Author(s):  
Jabbar Abbas ◽  
Arslan Ahmer ◽  
Muhammad Yousuf ◽  
Shaib Muhammad ◽  
Durr-e-Shahwar Malik ◽  
...  
Keyword(s):  
Spectrophotometric Analysis ◽  
Local Market ◽  
Dissolution Profile ◽  
Standard Specification ◽  
Disintegration Time ◽  
Physicochemical Evaluation ◽  
Rate Profile ◽  
Unites States ◽  
Present Effort ◽  
Good Agreement

The purpose of present effort was to conduct physiochemical evaluation of miscellaneous commercially available diclofenac potassium 75 mg tablets in the local market of Sindh, Pakistan. Further comparison was made among their different parameters. In study seven brands tagged as RB1 to RB7 were evaluated for diameter, thickness, disintegration time, and assay content and dissolution profile. Obtained results of all brands conformed to the official standard specification for disintegration test, Assay Content. The attained release rate profile during dissolution study revealed that all brands achieved more than 80% in sixty minutes. The spectrophotometric analysis for assay content of all brands was within 90%-110% which in good agreement with specified in the Unites States Pharmacopoeia. In the current study all the assessed products could be regarded as being chemically similar, while no product is found as a false product, these all brands can be used alternatively. The used spectrophotometric evaluation is very simple, reasonable, and easy to adopt for analysis and could be used in routine analysis of diclofenac potassium tablets, particularly in the unavailability of advanced equipment’s just like HPLC, LCMS & GC etc. which is not easily available and accusable in many institutions.

scholarly journals Design, Development, and Characterization of Amorphous Rosuvastatin Calcium Tablets

2021 ◽  
Author(s):  
Rocío González ◽  
Mª Ángeles Peña ◽  
Norma Sofía Torres ◽  
Guillermo Torrado
Keyword(s):  
Dissolution Rate ◽  
Active Ingredient ◽  
Cost Effective ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Design Development ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Rosuvastatin Calcium

This work proposes a methodology for the design, development, optimisation, and evaluation of amorphous rosuvastatin calcium tablets (BCS class II drug). The main goal was to ensure rapid disintegration and high dissolution rate of the active ingredient, thus enhancing its bioavailability. The design started from a careful selection of excipients, which due to their characteristics and proportions within the formulation allowed the use of their properties such as fluidity or granulometric distribution. The formulation was characterised using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermogravimetry (TGA), Fourier transform infrared spectroscopy (FT-IR) and powder X-ray diffraction (PXRD) methods. The galenic SeDeM methodology was used to establish the profile of the active ingredient-excipient mixture and guarantee its suitability for producing tablets by the direct compression method. The results demonstrate that the amorphous rosuvastatin calcium tablets formulation developed made it possible to obtain cost-effective tablets by direct compression with optimal pharmacotechnical characteristics that showed a remarkable disintegration and dissolution rate. The manufactured tablets complied with the pharmacopoeia guidelines regarding uniformity of weight, tablet hardness, thickness, friability, in vitro disintegration time and dissolution profile.

Sign in / Sign up

Export Citation Format

Share Document