scholarly journals Gellan gum and polyvinylpyrrolidone (PVP) as binding agents in extrusion/spheronization pellet formulations

2019 ◽  
Vol 69 (1) ◽  
pp. 99-109 ◽  
Author(s):  
Eduardo José Barbosa ◽  
Humberto Gomes Ferraz
Keyword(s):  
Aspect Ratio ◽  
Immediate Release ◽  
Gellan Gum ◽  
Pellet Size ◽  
Dissolution Tests ◽  
Binding Agents ◽  
Physical Tests ◽  
Model Drug ◽  
Different Response ◽  
Extrusion Spheronization

Abstract The aim of this work was to evaluate gellan gum as binder in pellet formulations, with theophylline as the model drug, in comparison with polyvinylpyrrolidone (PVP). A full 32 factorial design was realized, with binder and diluent factors at three levels each. Pellets were produced by the extrusion/spheronization technique, and dried in a fluid-ized bed. Physical tests and dissolution tests were conducted. The results showed that the binder factor was not significant for pellet size and granulometry distribution. Rather, trends of a different response of gellan gum were identified, in comparison with PVP, in aspect ratio and dissolution tests: more round pellets were obtained in formulations with gellan gum, and more variable dissolution resulted when this polysaccharide was present. Therefore, if the usage of this compound in immediate release pellet formulations is verified, this justifies the interest in the development of sustained release systems using gellan gum.

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.

scholarly journals Potential and Comparative Tablet Disintegrant Properties of Pectin Obtained from Five Okra Genotypes in Ghana

Scientifica ◽  
2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Frederick William Akuffo Owusu ◽  
Mariam El Boakye-Gyasi ◽  
Jacob Kwaku Agbenorhevi ◽  
Marcel Tunkumgnen Bayor ◽  
Kwabena Ofori-Kwakye
Keyword(s):  
Immediate Release ◽  
Dissolution Profile ◽  
Maize Starch ◽  
Dissolution Tests ◽  
The World ◽  
Weight Test ◽  
Pharmaceutical Industries ◽  
Tablet Formulations ◽  
Low Levels ◽  
Paracetamol Tablet

Okra pectin has been studied as a potential excipient in tablet formulations for pharmaceutical industries. Okra is widely grown and available in Ghana and other parts of the world. The prospective use of pectin from okra genotypes grown in Ghana as tablet disintegrants has not been reported. This study aims to determine the potential and comparative disintegrating properties of pectin from five okra genotypes (Abelmoschus esculentus L.) in Ghana using uncoated immediate release paracetamol tablet formulations. The yield of the pectin from the various genotypes ranged between 6.12 and 18.84% w/w. The extracted pectins had pH ranging from slightly acidic to almost neutral (6.39–6.92). Pectin from the various genotypes exhibited good swelling indexes (˃200%), varying solubility in different solvents, and low moisture content (˂20%). Elemental analysis of the extracted pectin from the various genotypes revealed very low levels of toxic metals and micronutrients. Pectin from the various genotypes was evaluated as disintegrants within concentrations of 5–10% w/w (F1–F18). Their disintegrating properties were compared to that of maize starch BP. All the formulated batches of uncoated immediate release paracetamol tablets (F1–F18) passed the following: uniformity of weight test, uniformity of dimensions, hardness, friability (˂1%), and drug content (95–105%). Significant differences ( p ≤ 0.05 ) were observed between the hardness of the maize starch tablets and tablets formulated from pectin of the various genotypes. Pectin from all genotypes other than PC5 exhibited good disintegrating properties (DT ˂ 15 min) and subsequently passed the dissolution profile test (≥70% release in 45 minutes). Tablets formulated with PC5 as disintegrants at all concentrations (5% w/w (F5), 7.5% w/w (F11), and 10% w/w (F17)) failed the disintegration and dissolution tests. Ultimately, pectins extracted from PC1, PC2, PC3, and PC4 can be commercially exploited as disintegrants in immediate release tablets.

Rheological and textural analysis as tools for investigation of drug-polymer and polymer–polymer interactions on the example of low-acyl gellan gum and mesalazine

2022 ◽  
pp. 088532822110527
Author(s):  
Piotr Gadziński ◽  
Tomasz Zbigniew Osmałek ◽  
Anna Froelich ◽  
Oliwia Wilmańska ◽  
Agata Nowak ◽  
...  
Keyword(s):  
Profile Analysis ◽  
Polymer Network ◽  
Crosslinking Agent ◽  
Gellan Gum ◽  
Hydroxyethyl Cellulose ◽  
Rheological Analysis ◽  
Gelling Agents ◽  
Texture Profile ◽  
Ionic Crosslinking ◽  
Model Drug

Purpose. In the performed study, the rheological and textural parameters of gellan-based hydrogels were investigated and their dependence on three factors was taken into consideration: ( i) The presence of the model drug, ( ii) The presence and type of the ionic crosslinking agent, and ( iii) the composition of the polymer network. The objective was to compare two analytical methods, regarded as complementary, and define to what extent the obtained results correlate with each other. Methods. The hydrogels contained low-acyl gellan gum or its mixtures with hydroxyethyl cellulose or κ-carrageenan. CaCl2 and MgCl2 were used as gelling agents. Mesalazine was used as a model drug. The rheological analysis included oscillatory stress and frequency sweeping. The texture profile analysis was performed to calculate texture parameters. Results. Placebo gels without the addition of gelling agents had the weakest structure. The drug had the strongest ability to increase the stiffness of the polymer network. The weakest structure revealed the placebo samples without the addition of gelling agents. Texture analysis revealed no significant influence of the drug on the strength of the gels, while rheological measurements indicated clear differences. Conclusions. It can be concluded that in the case of some parameters methods correlate, that is, the effect related to gelling ions. However, the rheological analysis seems to be more precise and sensitive to some changes in the mechanical properties of the gels.

Impact of pharmaceutical dosage form on stability and dissolution of roxithromycin

Open Medicine ◽  
2010 ◽  
Vol 5 (1) ◽  
pp. 83-90 ◽  
Author(s):  
Michał Ostrowski ◽  
Ewa Wilkowska ◽  
Tomasz Bączek
Keyword(s):  
High Performance ◽  
Bitter Taste ◽  
Immediate Release ◽  
Oral Suspension ◽  
Pharmaceutical Dosage Form ◽  
Dissolution Tests ◽  
Ph Conditions ◽  
Dispersible Tablets ◽  
Enteric Coated

AbstractThe behavior of dispersible tablets containing enteric-coated pellets and oral suspension, both containing roxithromycin, was investigated using dissolution tests in different media. The dissolution test was performed under different pH conditions. For both dosage forms investigated, the test was conducted at pH 1.2, 4.5, and 6.8. Additionally, for dispersible tablets, the test involving increasing pH was performed at pH 1.2 (acid stage) and afterwards at pH 6.8 (buffer stage). The extent of dissolution was measured using high-performance liquid chromatography (HPLC). In all cases tested, roxithromycin underwent rapid degradation at pH 1.2. Dispersible tablets displayed the features of modified release preparations with a non-complete dissolution during the test times in all media. Conversely, the oral suspension behaved as an immediate release preparation, with degradation at pH 1.2. However, the dissolution of the oral suspension at pH 4.5 and 6.8 was rapid and complete. The role of enteric-coated pellets is to mask the bitter taste of the active substance upon administration. However, the coating showed lack of resistance to media at pH 1.2. Therefore, dispersible tablets containing enteric-coated pellets are not pharmaceutically equivalent to the immediate-release oral suspension.

scholarly journals Utilization of Pectin from Okra as Binding Agent in Immediate Release Tablets

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Frederick W. A. Owusu ◽  
Mariam E. Boakye-Gyasi ◽  
Philomena Entsie ◽  
Marcel T. Bayor ◽  
Kwabena Ofori-Kwakye
Keyword(s):  
Polymeric Materials ◽  
Immediate Release ◽  
Binding Agent ◽  
Crushing Strength ◽  
Binding Characteristics ◽  
Dissolution Tests ◽  
Potential Binding ◽  
Pharmaceutical Industries ◽  
Tablet Formulations ◽  
Paracetamol Tablet

Polymeric materials from plants continue to be of interest to pharmaceutical scientists as potential binders in immediate release tablets due to availability, sustainability, and constant supply to feed local pharmaceutical industries. Paracetamol tablet formulations were utilized in investigating the potential binding characteristics of pectin harnessed from various okra genotypes (PC1-PC5) in Ghana. The pectin yields from the different genotypes ranged from 6.12 to 18.84%w/w. The pH of extracted pectin ranged from 6.39 to 6.92, and it had good swelling indices and a low moisture content. Pectin extracted from all genotypes were evaluated as binders (10, 15, and 20%w/v) and compared to tragacanth BP. All formulated tablets (F1-F18) passed the weight uniformity, drug content, hardness, and friability tests. Based on their crushing strength, tablets prepared with pectin from the various genotypes were relatively harder ( P ≤ 0.05 ) than tablets prepared with tragacanth BP. Tablets prepared with pectins as binders at 10%w/v and 15%w/v passed the disintegration and dissolution tests with the exception of PC4 at 15%w/v. Incorporation of pectin from all genotypes (excluding PC5) as a binder at concentrations above 15%w/v (F13, F16, F14, and F15) produced tablets which failed the disintegration test and showed poor dissolution profiles. Thus, pectin from these genotypes can be industrially commodified as binders in immediate release tablets using varying concentrations.

scholarly journals Enteric Hard Capsules for Targeting the Small Intestine: Positive Correlation between In Vitro Disintegration and Dissolution Times

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 123 ◽  
Author(s):  
Maoqi Fu ◽  
Jozef Al-Gousous ◽  
Johannes Andreas Blechar ◽  
Peter Langguth
Keyword(s):  
Immediate Release ◽  
Dosage Forms ◽  
Type I ◽  
Type Ii ◽  
Hard Shell ◽  
Model Drug ◽  
Enteric Coated ◽  
In Vitro Disintegration ◽  
Paddle Apparatus

In this study, the potential for correlation between disintegration and dissolution performance of enteric-coated (EC) dosage forms was investigated. Different enteric hard shell capsule formulations containing caffeine as model drug were tested for disintegration (in a compendial disintegration tester) and for dissolution in both USP type I (basket) and type II (paddle) apparatuses using different media. Overall, good correlations were obtained. This was observed for both the basket and the paddle apparatus, indicating that the use of disintegration testing as a surrogate for dissolution testing (allowed by International Conference on Harmonization (ICH) for immediate release dosage forms in case, in addition to other conditions, a correlation between disintegration and dissolution is proven) could be extended to include delayed release dosage forms.

scholarly journals FORMULATION OPTIMIZATION OF PROMETHAZINE THEOCLATE IMMEDIATE RELEASE PELLETS BY USING EXTRUSION-SPHERONIZATION TECHNIQUE

2018 ◽  
Vol 10 (1) ◽  
pp. 30
Author(s):  
Shelar Vishwas S. ◽  
Shirolkar Satish V. ◽  
Kale Rupali N.
Keyword(s):  
Drug Release ◽  
Motion Sickness ◽  
Dosage Form ◽  
Corn Starch ◽  
Research Work ◽  
Immediate Release ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Extrusion Spheronization ◽  
Pellet Formulation

Objective: Promethazine theoclate is a BCS Class II drug having anti-histaminic property and mainly used for the treatment of motion sickness and postoperative emesis. The main objective of the research work was to formulate and optimize immediate release pellets of promethazine theoclate by using the extrusion-spheronization technique to offer immediate release dosage form suitable for treatment of nausea and vomiting associated with motion sickness and post-operative conditions.Methods: Immediate release pellets of promethazine theoclate were prepared by using microcrystalline cellulose (MCC) and corn starch as filler and disintegrant respectively along with other excipients. Pellet formulation was further optimized for bulk density, disintegration time and percent drug release after 10 min. using 32 factorial design. Formulations were also characterized for drug-polymer interactions using Differential Scanning Calorimetry (DSC), surface morphology by Scanning Electron Microscopy (SEM) and other physicochemical properties.Results: Optimised pellet formulation contains 2.5:4.5:1 ratio of MCC: Corn Starch: Drug and spheronization time of 60 seconds showing highest percent yield of 78% and immediate drug release of 100.52±0.65% after 10 min.Conclusion: Promethazine theoclate pellets formulated in this study can serve as an alternative to tablet dosage form which can give immediate drug release for treatment of motion sickness and postoperative emesis.

scholarly journals Mechanistic PBPK Modelling to Predict the Advantage of the Salt Form of a Drug When Dosed with Acid Reducing Agents

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1169
Author(s):  
Siri Kalyan Chirumamilla ◽  
Venkatesh Teja Banala ◽  
Masoud Jamei ◽  
David B. Turner
Keyword(s):  
Pbpk Model ◽  
Immediate Release ◽  
Reducing Agents ◽  
Free Base ◽  
Salt Form ◽  
Pbpk Modelling ◽  
Release Formulation ◽  
Drug Products ◽  
Model Drug ◽  
The Impact

Acid reducing agents (ARAs) reduce the dissolution rate of weakly basic drugs in the stomach potentially leading to lower bioavailability. Formulating the API as a rapidly dissolving salt is one strategy employed to reduce the impact of ARAs on dissolution of such drugs. In the present work, a model drug was selected with an immediate release formulation of the free base dosed in both the absence and presence of the ARA famotidine. In the latter case, bioavailability is restricted and several salt formulations were investigated. To simulate these drug products a mechanistic physiologically based pharmacokinetic (PBPK) model was built using the Simcyp Simulator, which illustrates the advantage of formulating an API as a salt compared to the free base form. The simulations use a mechanistic salt model utilising knowledge of the solubility product which was applied to predict the salt advantage. The developed PBPK model exemplifies that it can be critical to account for the surface pH and solubility when modelling the dissolution of low pKa bases and their salts in the gastric environment. In particular, the mechanistic salt model can be used to aid in screening and salt form selection where the aim is to mitigate effects of ARAs.

scholarly journals LIQUISOLID-PELLETS TECHNIQUE: A RECENT TECHNIQUE FOR ENHANCING SOLUBILITY AND BIOAVAILABILITY OF DRUGS

2020 ◽  
pp. 34-40
Author(s):  
ABHISHEK KANUGO
Keyword(s):  
Scale Up ◽  
Immediate Release ◽  
Powdered Material ◽  
Spherical Particles ◽  
Pilot Plant Scale ◽  
Current Article ◽  
Dose Accuracy ◽  
Coating Agents ◽  
Extrusion Spheronization ◽  
Biopharmaceutical Classification System

The current article aims with the introduction of newer solubility enhancing technique as Liquisolid-pellet. The majority of newly invented molecules comes under the biopharmaceutical classification system (BCS) Class II, IV indicating poor solubility and thereby poor bioavailability. Liquisolid Compaq is one of the solubility enhancement techniques used for improving solubility and dissolution of the molecule by incorporating non-volatile solvent followed by carrier and coating agents. However, this technique is only applicable to potent molecules as a higher dose resulted in inconvenience to the patient and difficult to swallow. Another drawback of this method is not suitable for pilot plant scale-up. Liquisolid pellet technique overcoming all limitations of Liquisolid Compaq and offers good compaction, flowability, dose accuracy, less gastric irritations, and better bioavailability. In the Liquisolid-Pellet technique, powdered material received from Liquisolid Compaq is further moistened with granulating fluid to provide enough plasticity. The material is subjected to extrusion using an extruder to generate extrudates. The extrudates are placed under the spheronizer to form spherical particles as Pellets. The pellets are mainly prepared by extrusion-spheronization and hence, articles elaborate details of extruders and spheronizers, their specifications as well as factors, which strongly impart processing. These pellets are filled in capsules according to their dose and utilized as an immediate release or sustained release. The literature related to this review was collected from Science Direct, PubMed, Google Scholar, Google, USPTO, etc. from 1998 to 2020 with the following key-words.

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