scholarly journals Immediate-Release Formulations Produced via Twin-Screw Melt Granulation: Systematic Evaluation of the Addition of Disintegrants

2021 ◽  
Vol 22 (5) ◽  
Author(s):  
Kristina E. Steffens ◽  
Karl G. Wagner
Keyword(s):  
Immediate Release ◽  
Systematic Evaluation ◽  
Dissolution Profile ◽  
Release Formulation ◽  
Disintegration Time ◽  
Twin Screw ◽  
Total Proportion ◽  
A Minor ◽  
High Plastic ◽  
Melt Granulation

AbstractThe current study evaluated the effect of location and amount of various superdisintegrants on the properties of tablets made by twin-screw melt granulation (TSMG). Sodium-croscarmellose (CCS), crospovidone (CPV), and sodium starch glycolate (SSG) were used in various proportions intra- and extra-granular. Tabletability, compactibility, compressibility as well as friability, disintegration, and dissolution performance were assessed. The extra-granular addition resulted in the fasted disintegration and dissolution. CPV performed superior to CCS and SSG. Even if the solid fraction (SF) of the granules was lower for CPV, only a minor decrease in tabletability was observed, due to the high plastic deformation of the melt granules. The intra-granular addition of CPV resulted in a more prolonged dissolution profile, which could be correlated to a loss in porosity during tableting. The 100% intra-granular addition of the CPV resulted in a distinct decrease of the disintegration efficiency, whereas the performance of SSG was unaffected by the granulation process. CCS was not suitable to be used for the production of an immediate-release formulation, when added in total proportion into the granulation phase, but its efficiency was less impaired compared to CPV. Shortest disintegration (78 s) and dissolution (Q80: 4.2 min) was achieved with CPV extra-granular. Using CPV and CCS intra-granular resulted in increased disintegration time and Q80. However, at a higher level of appx. 500 s and appx. 15 min, only SSG showed a process and location independent disintegration and dissolution performance.

Fast Sleep Onset Pharmaceutical Formulation of the Chronobiotic Hormone Melatonin

2020 ◽  
Vol 12 (3) ◽  
pp. 439-442
Author(s):  
Marilena Vlachou ◽  
Angeliki Siamidi ◽  
Natassa Pippa ◽  
Nikolaos Fikioris
Keyword(s):  
Sleep Onset ◽  
Immediate Release ◽  
Food Supplement ◽  
Sleep Cycle ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Important Amino Acid ◽  
Normal Sleep ◽  
Tablet Formulations ◽  
The Brain

The Sedar, formulation of this investigation is a composition of natural ingredients, which has a relaxant, anxiolytic, and sleep-inducing action. The active ingredients of the formulations are melatonin, L-tryptophan (an important amino acid, which is converted in the brain to serotonin (neurotransmitter that contributes to normal sleep cycle); serotonin is sequentially converted to Melatonin), Pasiflora, valeriana, hawthorn and escholtsia increase GABA levels in the brain. The aim of this investigation is to study the release profile of melatonin from the tablets of the above formulation. This formulation is a unique food supplement, which offers numerous advantages including sleep onset dysfunctions. Tablets' uniformity (in terms of weight and thickness) was achieved and the disintegration time as well as the dissolution profile matched the requirements for immediate release formulations. Tablet formulations are also required to be hard enough such that they do not break up in the packaging (bottle or blister container) but also friable enough to disintegrate in the gastrointestinal tract. The tablets' strength (in terms of friability and hardness) as a consequence of the choice of the appropriate type, but also the quantity of excipients in the tablet formulation, along with the application of the suitable compression force, was evaluated ensuring right handling/packaging, safe transportation and facile release in the gastrointestinal environment.

scholarly journals FORMULATION, DEVELOPMENT AND EVALUATION OF IMMEDIATE RELEASE ROSUVASTATIN CALCIUM TABLET

2021 ◽  
Vol 11 (6) ◽  
pp. 25-30
Author(s):  
Prashant L. Pingale
Keyword(s):  
Research Work ◽  
Flow Characteristics ◽  
Cost Effective ◽  
Immediate Release ◽  
Wet Granulation ◽  
Formulation Development ◽  
Release Formulation ◽  
Disintegration Time ◽  
Rosuvastatin Calcium

Rosuvastatin belongs to the statin medication class, which is used to treat excessive cholesterol and prevent heart disease. The Biopharmaceutical Classification System classifies it as class II. The goal of this project is to create 10 mg Rosuvastatin instant release pills using several types of materials. To boost the drug's bioavailability, superdisintegrants were used to speed up the disintegration and dissolution of Rosuvastatin calcium. Cited research work aims to formulate an immediate release tablet of Rosuvastatin for the treatment of hypercholesterolemia, hypolipoproteinemia, and atherosclerosis. The present work used a cost-effective wet granulation process to create an immediate release formulation of Rosuvastatin calcium. All of the batches were manufactured, and the granules were evaluated for pre-compression properties such as loss on drying, bulk density, tapped density, and compressibility index. Disintegration time and assay were determined to be within acceptable parameters, as were weight fluctuation, thickness, hardness, and friability of tablets. The effect of several superdisintegrants on in vitro dissolutions in 6.8 PH phosphate buffer was investigated. The final formulation was chosen based on the dissolving profile; dissolution studies revealed that formulations F2 and F4 released 80 percent of the medication within 15 minutes. Two different formulations of Rosuvastatin Calcium 5.199 and 10.398 mg employing immediate-release tablets were successfully generated using Crospovidone, Meglumine, and Comprecel 112D+®. The tablets showed complete drug release in 60 minutes and fair flow characteristics when compared to the innovators' product.

scholarly journals IN VITRO-IN VIVO BIO-EQUIVALENCE CORRELATION STUDY OF ATENOLOL, AND ITS BRANDS OF IMMEDIATE RELEASE TABLET UNDER BIO-WAIVER CONDITIONS

2020 ◽  
Author(s):  
Ahmed EM ◽  
Ibrahim ME ◽  
Magbool FF
Keyword(s):  
Drug Delivery ◽  
Peer Review ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Class Iii ◽  
Release Formulation ◽  
E Mail

The aim of present study is to examine the in-vitro-in-vivo correlation (IVIVC) of immediate release product. Atenolol 100mg and its brands of immediate release dosage forms. Atenolol is clearly classified into BCS class III, and could be evaluated under bio waiver conditions. The in vitro parameters employed were hardness, weight uniformity, friability, disintegration time, absolute drug content, dissolution rate (in 0.1 N Hydrochloric acid, phosphate buffer and acetate buffer at 37ºC), and dissolution efficiencies were also analyzed. The in-vitro dissolution study was performed on the brands, according to FDA,USP  dissolution profile in three different PH (1.2),(4.5), and (6.8) at 37ºC, using the USP apparatus II,  then f1, f2 were determined for the time intervals of 10, 15, 30, 45 and 60 minutes, and dissolution efficiencies were calculated.  MINITAB 14 statistical program used for in vitro-in vivo correlation, level A was done for reference product. A non linear relation was established which is typical for immediate release formulation, of class III. Peer Review History: UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file Average Peer review marks at initial stage: 3.0/10 Average Peer review marks at publication stage: 7.0/10 Reviewer(s) detail: Name: Dr. Hayriye Eda Şatana Kara   Affiliation: Gazi University, Turkey E-mail: [email protected]   Name: Dr. Nicola Micale   Affiliation: University of Messina, Italy E-mail: [email protected]   Comments of reviewer(s): Similar Articles: FAST DISSOLVING DRUG DELIVERY SYSTEMS: FORMULATION, PREPARATION TECHNIQUES AND EVALUATION FAST DISSOLVING TABLETS: A PROMISING APPROACH FOR DRUG DELIVERY DEVELOPMENT AND EVALUATION OF FAST DISSOLVING THIN FILMS OF ARIPIPRAZOLE TABLET GRANULATION: CURRENT SCENARIO AND RECENT ADVANCES  

Vitamin C Fast Action Tablets by Doctor's Formulas' Food Supplements: Evaluation of Matrix Properties

2019 ◽  
Vol 11 (11) ◽  
pp. 1111-1114
Author(s):  
Marilena Vlachou ◽  
Angeliki Siamidi ◽  
Natassa Pippa ◽  
Nikolaos Fikioris
Keyword(s):  
Ascorbic Acid ◽  
Vitamin C ◽  
Corn Starch ◽  
Radical Scavenging ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
Food Supplements ◽  
Dissolution Profile ◽  
Onset Of Action ◽  
Disintegration Time

Vitamin C (ascorbic acid) is a diet dependent vitamin that promotes antioxidation though free radical scavenging and electron donation, has anti-inflammatory properties, supports growth of healthy immune cells and enhances bioavailability of iron in hemoglobin. Vitamin C as a food supplement is commercially available in many forms like immediate/extended release, effervescent and chewable tablets. Its absorption from a solid dosage form after oral administration depends on the release of the active ingredient from the product under physiological conditions and the permeability across the gastrointestinal tract. Generally, immediate release formulations provide rapid drug absorption and consequently a quick onset of the therapeutic effect. The aim of this study was to examine whether the physicochemical properties of the excipients, present in the solid pharmaceutical formulation under study, promote a synergistic interaction with the stereoelectronic features of ascorbic acid, so that the latter is released into the gastric-like dissolution environment in 30 minutes, thus ensuring fast onset of action. Vitamin C fast action tablets by Doctor's Formulas' Food Supplements were evaluated regarding their tablets' properties. Uniformity of tablets regarding their weight, thickness, friability, hardness, disintegration and dissolution was achieved. The careful choice of the appropriate type and quantity of excipients (calcium phosphate, corn starch, silicon dioxide, maltodextrin and magnesium stearate) in the tablet formulation, along with the application of the suitable compression force, ensures right handling/packaging and safe transportation. Moreover the disintegration time as well as the dissolution profile matched the requirements needed for immediate release formulations.

scholarly journals Production of Itraconazole Nanocrystal-Based Polymeric Film Formulations for Immediate Drug Release

Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 960
Author(s):  
Anna Karagianni ◽  
Leena Peltonen
Keyword(s):  
Drug Release ◽  
Physicochemical Characterization ◽  
Methyl Cellulose ◽  
Immediate Release ◽  
Polymeric Film ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Weight Variation ◽  
Film Forming

In order to improve the solubility properties of BCS class II drug itraconazole, fast dissolving oral polymeric film formulations based on itraconazole nanocrystals were produced. Drug nanocrystals were manufactured by the wet pearl milling technique. In polymeric film formulations, hydroxypropyl methyl cellulose (HPMC) was used as a film forming polymer, and glycerin was used as a plasticizer. For nanocrystal suspensions and film formulations, thorough physicochemical characterization was performed, including particle sizing and size deviation, film appearance, weight variation, thickness, folding endurance, drug content uniformity, disintegration time, and dissolution profile. After milling, the nanoparticles were 369 nm in size with a PI value of 0.20. Nanoparticles were stable and after redispersion from film formulations, the particle size remained almost the same (330 nm and PI 0.16). The produced films were flexible, homogeneous, fast disintegrating, and drug release rate from both the nanosuspension and film formulations showed immediate release behavior. Based on the study, the film casting method for production of itraconazole nanocrystal based immediate release formulations is a good option for improved solubility.

scholarly journals Assessment of physicochemical properties and comparison of the dissolution profile of amoxicillin caplets

2020 ◽  
Vol 16 (2) ◽  
pp. 118-129
Author(s):  
Een Widiyasari ◽  
Teuku Nanda Saifullah Sulaiman
Keyword(s):  
Physicochemical Properties ◽  
Product Quality ◽  
Dosage Form ◽  
Reference Product ◽  
Immediate Release ◽  
Dissolution Profile ◽  
Type Ii ◽  
Dissolution Test ◽  
Disintegration Time ◽  
Similarity Factor

Background: Marketed drugs must meet the required standards to guarantee product quality. Amoxicillin is a generic compound marketed under various trademarks as copy drugs. Amoxicillin caplets are an immediate release dosage form of BCS class I. An essential aspect of evaluating copy drugs is to assess the equivalence for their treatment to the innovator drugs to ensure the safety and effectiveness of the circulating copy drugs. Objective: The study aims to evaluate the physicochemical properties and compare the dissolution profile of amoxicillin caplets available in the market. Methods: Five amoxicillin caplet products, four test products, and one reference product were tested for their physicochemical properties and dissolution. The dissolution test was carried out with a type II device at a speed of 75 rpm in 900 mL of media buffered at pH 1.2, 4.5, and 6.8 and at a temperature of 37 +/- 0.5degrees celcius. The dissolution profile was analyzed by comparing it with the similarity factor (f2) parameters. Results: Two of the four amoxicillin caplet products had a similar dissolution profile to the reference products, namely products A and B. Products C and D were dissimilar because f2 was lower than 50 at pH 4.5. The caplets tested had almost the same dimensions, and all caplets met the requirements for uniformity of content, hardness, disintegration time, and dissolution. Conclusion: Not all of the amoxicillin caplets in the market have a similar dissolution profile to the reference products. Keywords: caplets, amoxicillin, dissolution, similarity factor

Formulation and Optimization of Immediate Release Pellets of Antiplatelet Drugs Using Design of Experimentation

2017 ◽  
Vol 7 (04) ◽  
Author(s):  
Deshkar S. S. ◽  
Pore A. R.
Keyword(s):  
Platelet Aggregation ◽  
Drug Release ◽  
Peripheral Arterial Disease ◽  
Tissue Injury ◽  
Immediate Release ◽  
Arterial Disease ◽  
Fixed Dose ◽  
Disintegration Time ◽  
Peripheral Arterial ◽  
Pvp K30

Platelets play an important role in hemostasis during tissue injury, which blocks the defect and terminates blood loss. Platelet aggregation inhibitors are widely used in treatment of cardiovascular disorders and Peripheral arterial disease. Clopidogrel bisulphate and Cilostazol, are FDA approved BCS class II drugs, used in treatment of Platelet aggregation, peripheral arterial disease and intermittent claudication. The aim of the present study was to develop an immediate release pellets for combination of Clopidogrel bisulphate and Cilostazol using extrusion spheronization technique. The effects of spheronization speed(X1) and binder concentration (PVP K30) (X2), on size of pellets, disintegration time and drug release were studied using 32 full factorial design. The surface response and counter plot were drawn to facilitate an understanding of the contribution of the variables and their interaction. From the results, speed of spheronization of 1100 rpm and 5% concentration of PVP K30, were selected. In vitro drug release studies revealed more than 80% of clopidogrel bisulphate release and more than 75% of cilostazol release within 30 min of dissolution which complied with the pharmacopoeal limits. Film coated pellets did not show significant change in the drug release. DSC and FTIR studies revealed no interaction of drugs and excipient during pellet formulation. The pellet formulations of clopidogrel and cilostazol were found to be stable when stored at 40ºC±2ºC/ 75%RH±5%RH for 2 months. Conclusively, clopidogrel bisulphate and cilostazol pellet fixed dose combination could be successfully developed by design of experimentation and complied with pharmacopoeal limits.

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.  

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