scholarly journals Effect of Magnesium Stearate Concentration on Dissolution Properties of Ranitidine Hydrochloride Coated Tablets

2007 ◽  
Vol 7 (3) ◽  
pp. 279-283 ◽  
Author(s):  
Alija Uzunović ◽  
Edina Vranić
Keyword(s):  
Time Course ◽  
Pharmaceutical Formulations ◽  
Magnesium Stearate ◽  
Drug Formulation ◽  
Formulation Development ◽  
Disintegration Time ◽  
Ranitidine Hydrochloride ◽  
Dissolution Properties ◽  
Coated Tablet ◽  
Tablet Formulations

Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates.The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked.During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmaco-peial test for similarity of dissolution profiles (f2 equation), previously proposed by Moore and Flanner.Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

scholarly journals Formulation development and evaluation of Silybum marianum tablets

Rodriguésia ◽  
2020 ◽  
Vol 71 ◽  
Author(s):  
Valeria Andrea Cianchino ◽  
Laura Silvina Favier ◽  
Claudia Alicia Ortega ◽  
Cecilia Peralta ◽  
Diego Alberto Cifuente
Keyword(s):  
Ethanolic Extract ◽  
Soxhlet Extraction ◽  
Pharmaceutical Formulations ◽  
Magnesium Stearate ◽  
Major Constituent ◽  
Active Principle ◽  
Formulation Development ◽  
Silybum Marianum ◽  
Disintegration Time ◽  
Popular Medicine

Abstract In popular medicine Silybum marianum is used as a hepatoprotective agent. Silymarin is the major constituent. The present work deals with the formulation and evaluation of S. marianum tablets from ethanolic extract by direct compression. The ethanolic extract was obtained from seeds by soxhlet extraction. Two pharmaceutical formulations were prepared using fluid extract as an active principle, and Aeroperl® 300 Pharma as a carrier. In order to improve flow ability and compressibility, co-processed excipients MicroceLac® 100 and FlowLac® 90 were employed. Pre-compression and post-compression parameters were evaluated according to USP 34-NF 29. Besides, silymarin was determined by NMR spectral data. Both formulations showed excellent rheological properties and the best biopharmaceutical parameters were observed in F2 (S. marianum ethanolic extract, aeroperl® 300 Pharma, flowLac® 90, glycolate starch and magnesium stearate) in terms of the friability (0.82 %) and the disintegration time (8.05 min).

scholarly journals Formulation development of methylprednisolone dispersible tablets using quality by design approach

2019 ◽  
Vol 9 (1-s) ◽  
pp. 229-239
Author(s):  
J Nandhini ◽  
AN Rajalakshmi
Keyword(s):  
Patient Compliance ◽  
Quality By Design ◽  
Water Solubility ◽  
Magnesium Stearate ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Formulation Development ◽  
Disintegration Time ◽  
Dispersible Tablets

The objective of this study was to enhance the solubility of Methylprednisolone by choosing micronized form of drug and to enhance patient compliance by formulating it as dispersible tablets using quality by design (QbD) approach. Dispersible tablets of Methylprednisolone were developed by 23 factorial design. In this study independent variables were concentrations of MCC 102, CCS and Magnesium stearate and dependent variables were disintegration time, hardness and dissolution. The resulting data was fitted into Design Expert Software (Trial Version) and analyzed statistically using analysis of variance (ANOVA). The response surface plots were generated to determine the influence of concentration of MCC 102, CCS and magnesium stearate on responses. The tablets were prepared by direct compression method by choosing micronized form of drug and formulations were evaluated for the standard of dispersible tablets. Results showed that no significant drug-polymer interactions in FTIR studies. According to QbD suggestion the formulation O1 (Desirability- 0.73) with MCC-38mg, CCS-3.5mg and magnesium stearate-2.5mg was formulated and evaluated. The disintegration time was found to be 69 seconds, hardness was found to be 64N and in vitro dissolution with in 30minutes. Optimized O1 formulation was within the limits of standards of dispersible tablets with increased water solubility and better patient compliance. Stability study on optimized O1 formulation showed that there is no significant changes during study period. Thus, O1 formulation was found to be stable. The study indicates that formulation of Methylprednisolone dispersible tablets by using QbD approach is a promising formulation development method. Keywords: Dispersible tablets, Methylprednisolone, Direct compression, Quality by Design and ANOVA.

scholarly journals Mini-review on Natural Disintegrants in Pharmaceutical Formulations

2021 ◽  
pp. 52-56
Author(s):  
S. U. Kankanamge ◽  
A. G. K. Neranja ◽  
K. D. S. Sandarenu
Keyword(s):  
Pharmaceutical Formulations ◽  
Nutritional Supplement ◽  
Water Soluble ◽  
Aqueous Environment ◽  
Natural Polymers ◽  
Disintegration Time ◽  
Water Soluble Drug ◽  
Tablet Formulations ◽  
Potential Use ◽  
Poorly Water Soluble Drug

Disintegrants are agents which are integrated to tablets and some encapsulated formulations in order to promote the breakup of the tablet and capsule “slugs” into more small fragments in an aqueous environment which thereafter increment the available surface area and promoting a more rapid release of the drug substance.  The development of new excipients for potential use as disintegrant agent in tablet formulations continues to be of interest. This is because different disintegrant agents can be useful in promoting penetration of moisture and dispersion of the tablet matrix and disintegration of tablet has received considerable attention at present as an essential step in obtaining fast drug release. Natural polymers such as starches, gums, mucilage, and dried fruits utilized as binder, diluent, and disintegrants to increase the solubility of poorly water-soluble drug, decrease the disintegration time, and provide nutritional supplement. Natural disintegrants are safe and economical than synthetic disintegrants such as Polyvinylpyrrolidone (PVP). Therefore, in the present review, an attempt has been made to reveal the importance of the natural disintegrants in the pharmaceutical formulations.

scholarly journals Multivariate Statistical Optimization of Tablet Formulations Incorporating High Doses of a Dry Herbal Extract

Pharmaceutics ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 79 ◽  
Author(s):  
Euichaul Oh ◽  
Uijung Kim ◽  
Beom-Jin Lee ◽  
Cheol Moon
Keyword(s):  
Tablet Formulation ◽  
Herbal Extract ◽  
Herbal Extracts ◽  
Formulation Development ◽  
Multivariate Statistical ◽  
Disintegration Time ◽  
Tablet Disintegration ◽  
Tablet Formulations ◽  
High Doses ◽  
Formulation Variables

The development of oral tablet formulation for herbal medicines has been restricted by large drug loadings and the poor physicochemical and mechanical properties of dry herbal extracts (DHEs). Herein, statistical experimental designs were applied to herbal tablet formulation development and optimization using Wuzi Yanzong dry extract (WYE). The tablet disintegration time and hardness were identified as the critical quality attributes (CQAs) of the product. The tablet formulation was designed to achieve a high drug loading (50% or higher of WYE), shorter tablet disintegration time (less than 30 minutes), and suitable hardness (6.0 to 7.5 kp). A D-optimal mixture design was used to evaluate the effects of excipients on CQAs to minimize the risk compression failure and improve the tabletability in formulations containing WYE at 50% and 65% by weight. A partial least squares model was used to elucidate the multivariate relationships between a large number of formulation variables and product CQAs, and determine the maximum possible WYE loading. From overlaid plots of the effects of formulation variables on CQAs, it was found that a maximum WYE loading of 67% in tablet formulation satisfied the acceptance criteria of CQAs. In conclusion, this study shows that multivariate statistical tools are useful for developing tablet formulations containing high doses of herbal extracts and establishing control strategies that ensure product quality.

scholarly journals Tablet Formulation Studies on Recrystallized Active Pharmaceutical Ingredients of Valsartan and Olmesartan Medoxomil

2021 ◽  
Vol 11 (6-S) ◽  
pp. 1-8
Author(s):  
TP. Rao ◽  
Buchi N. Nalluri
Keyword(s):  
Dissolution Rate ◽  
Aqueous Solubility ◽  
Olmesartan Medoxomil ◽  
In Vitro Dissolution ◽  
Content Uniformity ◽  
Type I ◽  
Disintegration Time ◽  
Weight Variation ◽  
Dissolution Properties ◽  
Tablet Formulations

Both the Valsartan (VAL) and Olmesartan medoxomil (OLM) are widely prescribed anti-hypertensive agents with angiotensin II type I receptor antagonistic activity. Both VAL and OLM are type of BCS class II drugs and having a low and variable oral bioavailability.  Recrystallization of VAL and OLM from different organic solvents improved its aqueous solubility and thereby in vitro dissolution properties. In the present investigation, tablets containing Valsartan (VAL), Olmesartan medoxomil (OLM and)  recrystallized products were prepared by  direct compression method and evaluated for drug content, uniformity of weight, hardness, friability, disintegration time and dissolution properties. All the tablets fulfilled the compendial requirements with regarding to weight variation, friability and disintegration time etc for immediate release tablets.  The DP15 (drug percent dissolved at 15 min) values for V-1 (tablets of VAL), V-4 (tablets of methanol recrystallized product with crospovidone as disintegrant) and DIOVAN™ 40mg tablet formulations are 45.97,  98.95 and 82.65 respectively and V-4 formulation showed higher dissolution rate when compared to other formulations. The DP15 values of O-1(tablets of OLM), O-4 (tablets of acetonitrile recrystallized product with crospovidone as disintegrant and OLMY™ (20mg) tablet formulations are 29.25, 99.93 and 84.82 respectively. O-4 tablet formulations showed higher dissolution rate when compared to other tablet formulations. Keywords: Valsartan, Olmesartan medoxomil, Recrystallization, Aqueous solubility

scholarly journals Aceclofenac Fast Dispersible Tablet Formulations: Effect of different concentration levels of Avicel PH102 on the compactional, mechanical and drug release characteristics

2019 ◽  
Author(s):  
Riffat Yasmin ◽  
Muhammad Harris Shoaib ◽  
Farrukh Rafiq Ahmed ◽  
Faaiza Qazi ◽  
Huma Ali ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Hydraulic Press ◽  
Formulation Development ◽  
Disintegration Time ◽  
Dispersible Tablet ◽  
Material Formulation ◽  
Tablet Formulations ◽  
Central Composite

ABSTRACTObjective of this study was based on the formulation development of fast dispersible Aceclofenac tablets (100mg) and to evaluate the influence of pharmaceutical mixtures of directly compressible Avicel PH102 with Mannitol and Acdisol on the compressional, mechanical characteristics and drug release properties. Fifteen different aceclofenac formulations were developed by central composite rotatable design (CCRD). Among them best possible formulations (FA–FH) were selected on the basis of micromeritic properties, appropriate tablet weight and disintegration time for further study. Tablets were compressed by direct compression method using hand held hydraulic press with a compressional force ranging from 8 to 80 MN/m2 (MPa). Pre and post compression studies were performed and the compressed formulations (FA-FH) were assessed for different quality tests. The Heckel and Kawakita equations were applied for determination of compressional behavior of formulations. The quality attributes suggested that formulation (FB) containing avicel PH 102 (20%), mannitol (25%) and ac-di-sol (3%) as best optimized formulation showing better mechanical strength i.e. hardness 37.75 ± 0.14N, tensile strength 5.67MN/m2 and friability 0.34%. Furthermore, compressional analysis of FB showed lowest PY value 59.52 MN/m2 and Pk value 1.040 MN/m indicating plasticity of the material. Formulation FB disintegrated rapidly within 21 seconds and released 99.92 % drug after 45min in phosphate buffer pH 6.8. Results of drug release kinetics showed that formulations FA-FH followed Weibull and First-order models in three different dissolution media. Avicel based formulation mixture exhibit excellent compactional strength with rapid disintegration and drug release.

scholarly journals Studies on Fruit Pectin in the Development of Tablet Formulations of Ibuprofen

2021 ◽  
Vol 8 (4) ◽  
Author(s):  
Nausheen Tariq Siddiqui ◽  
Ramla Binte Baber ◽  
Rsfi Akhtar Sultan ◽  
Iqbal Azhar ◽  
Waseemuddin Ahmed ◽  
...  
Keyword(s):  
Pharmaceutical Formulations ◽  
Gelling Agent ◽  
Wet Granulation ◽  
Binding Agent ◽  
Disintegration Time ◽  
Compression Properties ◽  
Naturally Occurring ◽  
Manufacture Process ◽  
Tablet Formulations ◽  
Tablet Manufacture

Background: Pectin, a naturally occurring polysaccharide is more than a food additive and has got amazing properties as a gelling agent and as a binder. Objective: The current research entails the extraction and identification of pectin from peels of selected fruits mango (Magnifera indica) and banana (Musa paradisiaca) by direct heating and using alcohol as precipitating agent. The potential of pectin as a binding agent in tablet formulation was evaluated by screening its micromeritics and post compression properties. Method: quadruple formulations of ibuprofen with crude peel pectin extracted from mango and banana in concentration of 50, 75, 100 and 125 mg respectively were employed in the tablet manufacture process by wet granulation method. Results: Successful formulation of tablet was done with the extracted pectin from the two fruit peels. The micromeritics properties showed good binding and flowing properties. An increase in concentration of pectin increased the hardness and also the dissolution of tablets up to a certain extent. The disintegration time was suitable for all formulations. Conclusion: It was concluded that pectin extracted from mango and banana peels can be used as a super disintegrating agent in pharmaceutical formulations, where needed.

Evaluation of Native and Pregelatinized Arrowroot (Maranta Arundinacea) Starches as Disintegrant in Tablet Formulation

2011 ◽  
Vol 197-198 ◽  
pp. 127-130 ◽  
Author(s):  
Vipaluk Patomchaiviwat ◽  
Piriyaprasarth Suchada ◽  
Koorattanasiri Popporn ◽  
Kanoknirumdom Supaporn ◽  
Rattanasiha Achara
Keyword(s):  
Corn Starch ◽  
Magnesium Stearate ◽  
Tablet Formulation ◽  
Direct Compression ◽  
Disintegration Time ◽  
Native Starch ◽  
Sodium Starch Glycolate ◽  
Tablet Formulations ◽  
Swelling Volume ◽  
Arrowroot Starch

The purpose of this study was to investigate the disintegrating properties of native arrowroot starch and pregelatinized arrowroot starch in comparison with corn starch and sodium starch glycolate (Explotab®). Tablets were prepared by direct compression. The tablet formulations contained dibasic calcium phosphate as filler and magnesium stearate as lubricant. Each starch at various concentrations between 2-10 % w/w was used in formulation as disintegrant. The swelling volume and weight of starches and disintegration time of tablets were evaluated. At 2% w/w concentration of starch, the pregelatinizaed starch provided disintegration time faster than the native starch (2.5 times). The disintegration time of 2% w/w pregelatinized arrowroot starch was comparable to Explotab and faster than that of native starch. The disintegration time of native starch at the concentration of 4, 6 and 10 %w/w was comparable to that of corn starch and Explotab®. Native arrowroot starch and pregelatinized arrowroot starch could be used as effective disintegrants in tablet formulation.

scholarly journals Development and Evaluation of Fluoxetine Fast Dissolving Films: An Alternative for Noncompliance in Pediatric Patients

Processes ◽  
2021 ◽  
Vol 9 (5) ◽  
pp. 778
Author(s):  
Emőke-Margit Rédai ◽  
Paula Antonoaea ◽  
Nicoleta Todoran ◽  
Robert Alexandru Vlad ◽  
Magdalena Bîrsan ◽  
...  
Keyword(s):  
Pediatric Patients ◽  
Hydroxypropyl Methylcellulose ◽  
Pharmaceutical Formulations ◽  
Release Kinetic ◽  
Disintegration Time ◽  
Casting Technique ◽  
First Order ◽  
Orodispersible Films ◽  
Folding Endurance

The most used pharmaceutical formulations for children are syrups, suppositories, soft chewable capsules, and mini-tablets. Administrating them might create an administration discomfort. This study aimed to develop and evaluate orodispersible films (ODFs) for pediatric patients in which the fluoxetine (FX) is formulated in the polymeric matrix. Six FX fast dissolving films (10 mg FX/ODF), FX1, FX2, FX3, FX4, FX5, and FX6, were prepared by solvent casting technique. In the composition of the ODFs, the concentration of the hydroxypropyl methylcellulose and the concentration of the propylene glycol were varied. Each formulation of fluoxetine ODF was evaluated by determining the tensile strength, folding endurance, disintegration, behavior in the controlled humidity and temperature conditions, and adhesiveness. All the obtained results were compared with the results obtained for six ODFs prepared without FX. The disintegration time of the FX ODFs was of maximum 88 s for FX2. Via the in vitro releasing study of the FX from the ODFs it was noticed that FX1 and FX2 allow a better release of the drug 99.98 ± 3.81% and 97.67 ± 3.85% being released within 15 min. From the obtained results it was also confirmed that FX ODFs were found to follow first-order release kinetic.

Machine learning directed drug formulation development

2021 ◽  
Author(s):  
Pauric Bannigan ◽  
Matteo Aldeghi ◽  
Zeqing Bao ◽  
Florian Häse ◽  
Alán Aspuru-Guzik ◽  
...  
Keyword(s):  
Machine Learning ◽  
Drug Formulation ◽  
Formulation Development
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