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.

Naturally Derived Matrix for Controlled Selenium Nanoparticles Delivery

2016 ◽  
Vol 695 ◽  
pp. 284-288 ◽  
Author(s):  
Simona Cavalu ◽  
Vasile Laslo ◽  
Florin Banica ◽  
Simona Ioana Vicas
Keyword(s):  
Gastric Fluid ◽  
Point Of View ◽  
Matrix Composition ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Elemental Selenium ◽  
Simulated Intestinal Fluid ◽  
Advantages And Disadvantages ◽  
Probiotic Lactic Acid Bacteria

The aim of this study is to develop a lyophilized matrix (microspheres) as a controlled delivery system for nanoselenium particles, using different formulation based on alginate or agar. Elemental selenium is considered as the least toxic of all selenium forms and in the same time supplementation with its nanosize particles has the same or better bioavailability compared to its salts. In our study, nanosized elemental selenium was obtained by fermentation technology using probiotic lactic acid bacteria (Lactobacillus casei). The microspheres have been characterized from structural point of view by using different techniques: FTIR spectroscopy, X-ray Diffraction and SEM. Each individual natural polymer has its own characteristic advantages and disadvantages; it is commonly accepted that naturally derived matrix often show an excellent balance between the mechanical properties, swelling and dissolution capacity. The optimized formulation was proposed upon in vitro dissolution study using Diferential Pulsed Voltammetry in order to measure the concentration of selenium released in simulated gastric fluid (pH=1.2) and simulated intestinal fluid (pH=8.1). The cumulative release of selenium from different formulations showed large differences with respect to matrix composition. We demonstrated that both alginate and agarose-based formulations are suitable to be used in basic environment such as small or large intestine. The results might be of high importance as absorption of selenium occurs mainly in the duodenum, caecum and colon (more than 85%).

Comparative In vitro Bioequivalence Evaluation of Different Brands of Amoxicillin Capsules Marketed in Tigray, Ethiopia

2013 ◽  
Vol 6 (1) ◽  
pp. 1966-1971
Author(s):  
Gebremedhin Solomon Hailu ◽  
Girma Belachew Gutema ◽  
Hailemichael Zeru Hishe ◽  
Yimer Said Ali ◽  
Adissu Alemayehu Asfaw
Keyword(s):  
In Vitro Dissolution ◽  
In Vitro Tests ◽  
Dissolution Profile ◽  
Difficult Situation ◽  
Similarity Factor ◽  
Regulatory Bodies ◽  
Monitoring And Surveillance ◽  
Dunnett's Test ◽  
Dissolution Efficiency

The availability of multisource generic brands of amoxicillin in the market today places health professionals and patients in a difficult situation about the choice of a suitable product among numerous generic brands. The purpose of this study was to estimate the bioequivalence of amoxicillin capsules marketed in Ethiopia using in vitro tests in order to determine their interchangeability. The in vitro dissolution study was carried out on the six brands of amoxicillin capsules according to USP guidelines. To compare the dissolution profiles, a difference factor (f1), similarity factor (f2), dissolution efficiency (DE) and statistical methods were employed. Results have shown significant differences in the dissolution profiles of the brands based on the statistical analysis (p<0.0001). Pair-wise comparisons using Dunnett’s test indicated that the innovator brand has a significantly faster dissolution than the generic brands, except brand D. According to f1, f2 and DE calculations, only brand D was found to have similar dissolution profile with the innovator. Based on the in vitro studies, only brand D may be considered bioequivalent and interchangeable, while the other brands may not be considered bioequivalent and interchangeable with the innovator brand. This research highlights among other things the need for constant monitoring and surveillance on the marketed drugs by regulatory bodies to ascertain bioequivalence and quality medicines, especially for drugs like amoxicillin for which there exists evidence of non-bioequivalence from different firms, resulting in efficacy issues.  

scholarly journals In Vitro Dissolution Evidence for Delivering Multiple Vitamin-Mineral Ingredients past the Stomach by Novel Capsule Delivery System (P24-009-19)

2019 ◽  
Vol 3 (Supplement_1) ◽  
Author(s):  
Luke Bucci ◽  
Mastaneh Sharafi ◽  
Nima Alamdari
Keyword(s):  
Absorption Spectrometry ◽  
Gastric Fluid ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Magnesium Concentration ◽  
Simulated Gastric Fluid ◽  
Lauryl Sulfate ◽  
Simulated Intestinal Fluid ◽  
Tablet Disintegration

Abstract Objectives The ability of a novel beadlet-in-oil, gastric-resistant, vegetarian capsule containing a multiple vitamin-mineral (MVM) composition to deliver capsule contents past the stomach was tested by standard in vitro tablet disintegration procedures using magnesium as the marker of capsule contents dissolution. Methods A novel capsule design using a gastric-resistant vegetarian hypromellose/gellan gum capsule (DRcaps®, Capsugel®) was tested for disintegration in a standard tablet disintegration apparatus according to compendial United States Pharmacopeia methods, as per Good Manufacturing Practices for dietary supplements. The MVM ingredients were encapsulated into size 0 Vcaps® (hypromellose with no gastric acid resistance) and DRcaps®. Individual capsules were placed into chambers containing simulated gastric fluid (0.1 M HCl) for 120 minutes then changed to simulated intestinal fluid (buffered 2% sodium lauryl sulfate, pH 6.0) for an additional 300 minutes. Aliquots were tested for magnesium concentration at ten time points by atomic absorption spectrometry. Results Magnesium was contained inside coated beadlets along with ferrous bisglycinate, methylcobalamin, 5-methyltetrahydrofolate, calcium fructoborate and cellulose. Vcaps® released 50% of the magnesium between 30–45 minutes and all by 60 minutes in the acid phase. DRcaps® released 25% of the magnesium at 45 minutes, and 43% at 120 minutes, followed by slow, steady release of the remaining magnesium by 420 minutes. Conclusions These dissolution profiles reproduce the known, rapid disintegration profile of Vcaps® when wetted. DRcaps® released the majority of their contents after the pH was changed to intestinal conditions, and then the beadlets released the water-soluble ingredients (magnesium) in a linear manner over a two hour period. Since normal stomach emptying of DRcaps® without a meal is less than 20–30 minutes (previously shown), DRcap® MVMs bypass the stomach almost completely to release ingredients in the small intestine. Thus, a novel, beadlet-in-oil, gastric-resistant capsule delivered its contents past the stomach. These properties have the ability to improve tolerability and thus, compliance with users. Funding Sources Capsugel®, Greenwood, SC, conducted this study for Ritual. Supporting Tables, Images and/or Graphs

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.

Development of Pulsatile Drug Delivery for Chronotherapeutics of Hypertension

2017 ◽  
Vol 7 (03) ◽  
Author(s):  
A. Y. Kanugo ◽  
N. I. Kochar ◽  
A. V. Chandewar
Keyword(s):  
Ethyl Cellulose ◽  
Candesartan Cilexetil ◽  
Gastric Fluid ◽  
In Vitro Dissolution ◽  
Simulated Gastric Fluid ◽  
Dissolution Studies ◽  
Coating Method ◽  
Pulsatile Drug Delivery ◽  
Compression Coating

The goal of present work was to investigate the effects of rupturable material ethyl cellulose combines with erodible material Klucel EXF on the pulsatile release pattern of Candesartan cilexetil in order to prevent morning rise in blood pressure. A tablet prepared by compression coating method contains core and coat components. Core consists of active ingredients with its various superdisintegrants where as coat contains different grades of ethyl cellulose and Klucel HXF in various combinations. All these tablets were evaluated for its micromeritics, weight variations, hardness, friability and in vitro dissolution testing. Drug-excipients interactions were carried out by FTIR. Dissolution studies were carried out in simulated gastric fluid followed by phosphate buffer of pH 6.5. The optimized formulation PT6 which give lag time of 6 hrs and released 99.10 % within 7 hr, as well as found to be stable in ICH stability testing guidelines.

PERILAKU DISOLUSI KETOPROFEN DAN INDOMETASIN FARNESIL TERSALUT GEL KITOSAN-GOM GUAR

2012 ◽  
Vol 12 (1) ◽  
Author(s):  
Purwantiningsih Sugita ◽  
Bambang Srijanto ◽  
Budi Arifin ◽  
Fithri Amelia ◽  
Mahdi Mubarok
Keyword(s):  
Room Temperature ◽  
Guar Gum ◽  
Tween 80 ◽  
Chitosan Solution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Magnetic Stirrer ◽  
Dissolution Behaviour ◽  
Shrimp Shell Waste

Chitosan, a modification of shrimp-shell waste, has been utilized as microcapsule. However, it’s fragile gel property needs to be strengthened by adding glutaraldehyde (glu) and natural hydrocolloid guar gum (gg). This research’s purposes were to study dissolution behaviour of ketoprofen and infar through optimum chitosan-guar gum microcapsule. Into 228.6 mL of 1.75% (w/v) chitosan solution in 1% (v/v) acetic acid,38.1 mL of gg solution was added with concentration variation of 0.35, 0.55, and 0.75% (w/v) for ketoprofen microcapsules and 0.05, 0.19, and 0.33% (w/v) for infar microcapsules, and stirred with magnetic stirrer until homogenous. Afterwards, 7.62mL of glu was added slowly under stirring, with concentrations varied: 3, 3.5, and 4% (v/v) for ketoprofen microcapsules, and 4, 4.5, and 5% (v/v) for infar microcapsules. All mixtures were shaked for 20 minutes for homogenization. All mixtures wereshaked for 20 minutes for homogenization. Into each  microcapsule mixture for ketoprofen, a solution of 2 g of ketoprofen in 250 mL of 96% ethanol was added, whereas solution of 100 mg of in 250 mL of 96% ethanol was added into each microcapsule mixture for infar. Every mixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Everymixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Conversion of suspension into fine powders/granules (microcapsules) was done by using spray dryer. The data of [gg], [glu], and medicine’s content from each microcapsule were treated with Minitab 14 software to obtain optimum [gg] and [glu] for microencapsulation. The dissolution behaviour of optimum ketoprofen and infar microcapsules were investigated. The result of optimization by using Minitab Release 14 software showed that among the microcapsule compositions of [gg] and [glu] were 0.35% (w/v) and 3.75% (v/v), respectively, optimum to coat ketoprofen, whereas [gg] and [glu] of 0.05% (w/v) and4.00% (v/v), respectively, optimum to coat infar, at constant chitosan concentration (1.75% [w/v]). In vitro dissolution profile showed that chitosan-guar gum gel microcapsule was more resistant in intestinal pH condition (rather basic) compared with that in gastric pH (very acidic).

scholarly journals Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 449
Author(s):  
Ahmed M. Omer ◽  
Zyta M. Ziora ◽  
Tamer M. Tamer ◽  
Randa E. Khalifa ◽  
Mohamed A. Hassan ◽  
...  
Keyword(s):  
Slow Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Gastric Fluid ◽  
Release Profile ◽  
Simulated Gastric Fluid ◽  
Maximum Value ◽  
Structure Surface ◽  
Drug Encapsulation Efficiency

An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

scholarly journals In Silico Prediction of Plasma Concentrations of Fluconazole Capsules with Different Dissolution Profiles and Bioequivalence Study Using Population Simulation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 215 ◽  
Author(s):  
Marcelo Dutra Duque ◽  
Daniela Amaral Silva ◽  
Michele Georges Issa ◽  
Valentina Porta ◽  
Raimar Löbenberg ◽  
...  
Keyword(s):  
Reference Product ◽  
Plasma Concentrations ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Dissolution Profile ◽  
Time Data ◽  
Simulation Results ◽  
Population Simulation

A biowaiver is accepted by the Brazilian Health Surveillance Agency (ANVISA) for immediate-release solid oral products containing Biopharmaceutics Classification System (BCS) class I drugs showing rapid drug dissolution. This study aimed to simulate plasma concentrations of fluconazole capsules with different dissolution profiles and run population simulation to evaluate their bioequivalence. The dissolution profiles of two batches of the reference product Zoltec® 150 mg capsules, A1 and A2, and two batches of other products (B1 and B2; C1 and C2), as well as plasma concentration–time data of the reference product from the literature, were used for the simulations. Although products C1 and C2 had drug dissolutions < 85% in 30 min at 0.1 M HCl, simulation results demonstrated that these products would show the same in vivo performance as products A1, A2, B1, and B2. Population simulation results of the ln-transformed 90% confidence interval for the ratio of Cmax and AUC0–t values for all products were within the 80–125% interval, showing to be bioequivalent. Thus, even though the in vitro dissolution behavior of products C1 and C2 was not equivalent to a rapid dissolution profile, the computer simulations proved to be an important tool to show the possibility of bioequivalence for these products.

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 FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 10 (5) ◽  
pp. 131-136
Author(s):  
Asim pasha ◽  
C N Somashekhar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

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