Effect of API on Powder Flowability, Direct Compression and Properties of Orally Disintegrating Tablets: A Preformulation Study

Abstract Orally disintegrating tablets (ODTs) are dosage forms which disintegrate in mouth within seconds without need of water. This type of quality in dosage form can be attained by addition of different varieties of excipients. Pharmaburst™ 500 is a co-processed excipient system which allows rapid disintegration and low adhesion to punches. The aim of the present study was to develop and evaluate 25 mg diclofenac sodium ODTs (orodispersible tablets) batches by direct compression method at different compression forces 10 kN (F1) and 20 kN (F2) and directly compressible excipients used in different ratio (Avicel PH 102, magnesium stearate and coprocessed excipient Pharmaburst™ 500, 70% and 80% w/w). The obtained batches were analyzed for appearance, tablet thickness, uniformity of weight, hardness, friability, disintegration time, and non-compendial methods (wetting time). Co-processed Pharmaburst™ 500 excipient 70% used for sodium diclofenac ODT obtaining determined good results for quality control tests evaluation.

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Optimization and In Vitro Evaluation of Famotidine Loaded Effervescent Orally Disintegrating Tablets using a Central Composite Design

Current Drug Therapy ◽

10.2174/1574885516666210618094626 ◽

2021 ◽

Vol 16 ◽

Author(s):

Ramesh Kumar ◽

Ravinder Verma ◽

Ritu Kaushik ◽

Prerna Kaushik ◽

Parijat Pandey ◽

...

Keyword(s):

Citric Acid ◽

Drug Release ◽

Sodium Bicarbonate ◽

Central Composite Design ◽

Pediatric Population ◽

Direct Compression ◽

Disintegration Time ◽

Orally Disintegrating Tablets ◽

Swallowing Problems ◽

Central Composite

Background: Over the years, effervescent orally disintegrating tablets (ODTs) have proved their worth over conventional tablets in overcoming the swallowing problems associated with the geriatric and pediatric population. The addition of effervescent agents in ODT provides a rapid disintegration along with masking of the slightly bitter taste of drugs and is worth exploring. Objective: The present research investigation deals with the preparation of effervescent ODTs by direct compression with rapid disintegration and adequate hardness using the central composite design response surface methodology. Method: Central composite design was used to study the effect of concentration of crospovidone (X1) and concentration of citric acid and sodium bicarbonate (X2) as independent factors on the two responses: disintegration time (Y1) and drug release (Y2). The tablets were prepared by direct compression approach using directly compressible mannitol. Results: Central composite design was used to study the effect of concentration of crospovidone (X1) and concentration of citric acid and sodium bicarbonate (X2) as independent factors on the two responses: disintegration time (Y1) and drug release (Y2). The tablets were prepared by direct compression approach using directly compressible mannitol. Conclusion: The results obtained in the present investigation revealed a successful development of famotidine effervescent ODTs with a better release profile compared to marketed formulation.

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FORMULATION OF ORALLY DISINTEGRATING TABLETS OF CINNARIZINE BY USING DIRECT COMPRESSION METHOD

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i1.29599 ◽

2019 ◽

Vol 11 (1) ◽

pp. 117

Author(s):

Rasha Khalid Al-dhahir ◽

Myasar Al-kotaji

Keyword(s):

Evaluation Studies ◽

Spectroscopic Studies ◽

Stability Study ◽

Compatibility Study ◽

Direct Compression ◽

Dissolution Profile ◽

Compression Method ◽

Orally Disintegrating Tablets ◽

Different Types ◽

Rapid Dissolution

Objective: The aim of this work was to formulate and evaluate orally disintegrating tablets of cinnarizine that were prepared by direct compression method using different types of diluents and super disintegrants. The rationale behind this work was to accelerate the disintegration of the tablet to provide rapid dissolution, quick action and enhanced bioavailability of the drug.Methods: The tablets were prepared by direct compression method using different types of diluents as mannitol, microcrystalline cellulose (MCC), and lactose. Different super disintegrants were used such as crospovidone (CP), sodium starch glycolate (SSG) and Kyron T-314; Kyron T-314 was used in different concentrations of 5%, 6%, 7%, and 8%. The prepared formulae (F1-F9c) were subjected to flowability studies and post-compression evaluation studies. The optimized formula was selected depending on the time of disintegration and dissolution; then it was subjected to drug-excipient compatibility study and stability study.Results: Flowability results were ranging from excellent, excellent to good, and good to fair according to the type of the diluent used. All of the prepared tablets showed acceptable hardness, friability, drug content, and disintegration. A rapid disintegration of 11.66±2.25 s with the highest percentage 2 min-drug release of 74.55±3.01% was obtained by using the diluent lactose and the super disintegrant Kyron T-314 (8%) in the formula F9c. The infrared spectroscopic studies of the formula F9c showed no drug-excipient interaction. In addition, the stability study indicated that the optimized formula is a stable formula.Conclusion: Formula F9c of a rapidly disintegrating tablet was easy to be manufactured, and the results showed that this formula had a rapid disintegration, high dissolution profile, no noticeable chemical incompatibility and it was stable upon storage.

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Formulation and Development of Taste Masked Orally Disintegrating Tablets of Perindopril Erbumine by Direct Compression Method

Pharmaceutica Analytica Acta ◽

10.4172/2153-2435.1000162 ◽

2012 ◽

Vol 03 (06) ◽

Cited By ~ 1

Author(s):

Mukesh P Ratnaparkhi

Keyword(s):

Direct Compression ◽

Compression Method ◽

Perindopril Erbumine ◽

Orally Disintegrating Tablets

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Studies on Orally Disintegrating Tablets Prepared by Using Natural and Synthetic Superdisintegrants

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v8i2.13869 ◽

2018 ◽

Vol 8 (2) ◽

Author(s):

Piplani Mona ◽

Diwedi Rohini ◽

Bhagwat Deepak Prabhakar ◽

Pahwa Rakesh

Keyword(s):

Direct Compression ◽

Dissolution Test ◽

Plantago Ovata ◽

Compression Technique ◽

Disintegration Time ◽

Weight Variation ◽

Orally Disintegrating Tablets ◽

Metoclopramide Hydrochloride ◽

Wetting Time ◽

Croscarmellose Sodium

The objective of present study was to compare the disintegration efficiency of mucilage isolated from Plantago ovata with commonly used synthetic superdisintegrant, croscarmellose sodium in the formulation of orally disintegrating tablets. Effects of varying concentration of both superdisintegrants on disintegration time were studied. Orally disintegrating tablets of metoclopramide hydrochloride were prepared using selected superdisintegrants by direct compression technique. Prepared tablets were evaluated for weight variation, thickness, hardness, friability, disintegration time, wetting time, water absorption ratio and dissolution test. Swelling index was also investigated for comparing the swelling property of croscarmellose sodium with mucilage of Plantago ovata. Swelling index of mucilage isolated from Plantago ovata was found to be greater (94 ± 2.5% v/v) when compared with croscarmellose sodium (85 ± 1.5% v/v). The present study indicated that mucilage isolated from natural source proved to be more effective for their disintegrating property than the most commonly used synthetic superdisintegrant, croscarmellose sodium.

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Comparison of Flow and Compression Properties of Four Lactose-Based Co-Processed Excipients: Cellactose® 80, CombiLac®, MicroceLac® 100, and StarLac®

Pharmaceutics ◽

10.3390/pharmaceutics13091486 ◽

2021 ◽

Vol 13 (9) ◽

pp. 1486

Author(s):

Martin Dominik ◽

Barbora Vraníková ◽

Petra Svačinová ◽

Jan Elbl ◽

Sylvie Pavloková ◽

...

Keyword(s):

Mechanical Resistance ◽

Direct Compression ◽

Preparation Technique ◽

Flow Properties ◽

Compression Pressure ◽

Compression Properties ◽

Novel Approach ◽

Ejection Force ◽

Orally Disintegrating Tablets ◽

Consolidation Behavior

The utilization of co-processed excipients (CPEs) represents a novel approach to the preparation of orally disintegrating tablets by direct compression. Flow, consolidation, and compression properties of four lactose-based CPEs—Cellactose® 80, CombiLac®, MicroceLac® 100, and StarLac®—were investigated using different methods, including granulometry, powder rheometry, and tablet compaction under three pressures. Due to the similar composition and the same preparation technique (spray drying), the properties of CPEs and their compacts were generally comparable. The most pronounced differences were observed in flowability, undissolved fraction after 3 min and 24 h, energy of plastic deformation (E2), ejection force, consolidation behavior, and compact friability. Cellactose® 80 exhibited the most pronounced consolidation behavior, the lowest values of ejection force, and high friability of compacts. CombiLac® showed excellent flow properties but insufficient friability, except for compacts prepared at the highest compression pressure (182 MPa). MicroceLac® 100 displayed the poorest flow properties, lower ejection forces, and the best mechanical resistance of compacts. StarLac® showed excellent flow properties, the lowest amounts of undissolved fraction, the highest ejection force values, and the worst compact mechanical resistance. The obtained results revealed that higher compression pressures need to be used or further excipients have to be added to all tested materials in order to improve the friability and tensile strength of formed tablets, except for MicroceLac® 100.

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Microwave-Assisted Development of Orally Disintegrating Tablets by Direct Compression

AAPS PharmSciTech ◽

10.1208/s12249-016-0683-z ◽

2016 ◽

Vol 18 (6) ◽

pp. 2055-2066 ◽

Cited By ~ 4

Author(s):

Kishor V. Kande ◽

Darsheen J. Kotak ◽

Mariam S. Degani ◽

Dmitry Kirsanov ◽

Andrey Legin ◽

...

Keyword(s):

Direct Compression ◽

Microwave Assisted ◽

Orally Disintegrating Tablets

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Development and Evaluation of Astaxanthin Orally Disintegrating Tablets Prepared from Coprocessed Excipients for Use in the Elderly

Key Engineering Materials ◽

10.4028/www.scientific.net/kem.859.295 ◽

2020 ◽

Vol 859 ◽

pp. 295-300

Author(s):

Tanikan Sangnim ◽

Kampanart Huanbutta

Keyword(s):

Mechanical Properties ◽

Age Groups ◽

The Elderly ◽

Dosage Forms ◽

Direct Compression ◽

Compression Method ◽

Pharmaceutical Dosage Forms ◽

Orally Disintegrating Tablets ◽

Type C ◽

Tablet Hardness

The world’s population is aging; therefore, conventional pharmaceutical dosage forms designed for adult are not suitable. Orally disintegrating tablets (ODTs) are innovative dosage forms designed to overcome the problem of difficulty in swallowing or dysphagia, which is a common problem among all age groups, especially the elderly. This study aimed to develop and assess ODTs loaded with astaxanthin and manufactured by direct compression method using different coprocessed pharmaceutical excipients, including F-Melt® Type C, F-Melt® Type M, and Pearlitol Flash®. The results found that the ODTs prepared from F-Melt® Type C and F-Melt® Type M offered better mechanical properties. An astaxanthin concentration of 20–40 mg in the tablets did not retard the disintegration mechanism. From the taste modified formulation, the tablets disintegrated within 82 seconds. The tablet hardness was higher than 35.33 N and its friability was less than 0.5%. Lastly, active ingredient dissolved more than 80% in 2 minutes.

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Evaluation of co-processed excipients used for direct compression of orally disintegrating tablets (ODT) using novel disintegration apparatus

Pharmaceutical Development and Technology ◽

10.3109/10837450.2012.710238 ◽

2012 ◽

Vol 18 (2) ◽

pp. 464-474 ◽

Cited By ~ 16

Author(s):

Witold Brniak ◽

Renata Jachowicz ◽

Anna Krupa ◽

Tomasz Skorka ◽

Krzysztof Niwinski

Keyword(s):

Direct Compression ◽

Orally Disintegrating Tablets

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The technologies used for developing orally disintegrating tablets: A review

Acta Pharmaceutica ◽

10.2478/v10007-011-0020-8 ◽

2011 ◽

Vol 61 (2) ◽

pp. 117-139 ◽

Cited By ~ 49

Author(s):

Bhatu Badgujar ◽

Atish Mundada

Keyword(s):

Freeze Drying ◽

Unique Property ◽

Wet Granulation ◽

Pharmaceutical Companies ◽

Direct Compression ◽

Improve Patient Compliance ◽

Advanced Technologies ◽

Orally Disintegrating Tablets ◽

Improve Patient ◽

Insight Into

The technologies used for developing orally disintegrating tablets: A reviewOrally disintegrating tablets (ODTs), also known as fast melts, quick melts, fast disintegrating and orodispersible systems, have the unique property of disintegrating in the mouth in seconds without chewing and the need of water and are thus assumed to improve patient compliance. Conventional methods like direct compression, wet granulation, moulding, spray-drying, freeze-drying and sublimation were used to prepare ODTs. New advanced technologies like Orasolv®, Durasolv®, Wowtab®, Flashtab®, Zydis®, Flashdose®, Oraquick®, Lyoc®, Advatab®, Frosta®, Quick-Disc® and Nanomelt® have been introduced by some pharmaceutical companies for the production of ODTs. The main objective of this review is to give a comprehensive insight into conventional and recent technologies used for the preparation of ODTs.

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