Formulation and Evaluation of Tablets of Different Drugs

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmaceutical Technology".

Deadline for manuscript submissions: closed (1 July 2022) | Viewed by 22763

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Departamento Ciencias Biomédicas, Facultad de Farmacia, Universidad de Alcalá, Alcalá de Henares, 28871 Madrid, Spain
Interests: drug formulation; pharmaceutical technology; formulation development and characterization
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Special Issue Information

Dear Colleagues,

The galenic developments of tablet formulations currently represent an extraordinary challenge for the pharmaceutical industry. Drugs with a short half-life, with a narrow therapeutic margin, or that degrade in certain circumstances or belonging to biopharmaceutical classifications I and II, that is, with low solubility, form part of these novel pharmaceutical formulations. Many of these challenges are achieved using new release dosage forms. Bilayer tablets, composed of two layers, an immediate release layer and a sustained release layer, anticipating the rapid release of the drug that begins in the stomach to quickly relieve symptoms and continues in the intestine to maintain a prolonged pharmacological effect; mucoadhesive buccal tablets that prevent gastric breakdown and first-pass metabolism, thus increasing the bioavailability of the drug and the onset of action; gastric floating tablets with a lower density than gastric fluid and which consequently can float in the stomach for a prolonged period of time, releasing the drug slowly; or enteric-coated tablets, in which the drug is released into the intestine at a time other than that of administration, but its therapeutic effect is not prolonged are all of interest. This means that one of the paths of current galenic research is directed at the control of drug release kinetics to attain optimal bioavailability and specificity at the site of action, and hence, modern excipients and biopolymers that act by modulating the speed, place, and moment of drug release that ultimately increase the therapeutic effectiveness are of great importance. Biopolymers and their derivatives are remarkably interesting for their renewability, non-toxicity, low cost, biodegradability, and good biological performance. 

We must also point out the importance of manufacturing procedures; they must be reproducible and provide stable, safe, and quality formulations. The physical characteristics of raw materials will determine the performance and results in these pharmaceutical processes. The deformation behavior of powders is particularly complex. The influence of the initial particle size, intermolecular interactions, and porosity on the compressibility and compactability of the starting samples can be extremely complicated, without forgetting their repercussion on the disintegration and dissolution of the final drug. 

This Special Issue is dedicated to the latest advances in the formulation and evaluation of different drug tablets. We invite authors to submit original research or review articles on these topics, including the development of new galenic developments of solid dosage forms targeting a specific patient and pathology. Thus, in addition to improving the therapeutic action of each active ingredient, patient compliance is improved and an essential contribution to the therapeutic success is provided, all representing clear reasons to seek to improve existing dosage forms and to create new ones. 

Prof. Dr. María Ángeles Peña Fernández
Guest Editor

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Keywords

  • formulation
  • tablets
  • release
  • compression
  • polymers
  • drug

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Published Papers (4 papers)

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Research

18 pages, 4748 KiB  
Article
Study of Orally Disintegrating Tablets Using Erythritol as an Excipient Produced by Moisture-Activated Dry Granulation (MADG)
by Mizuki Yamada, Agata Ishikawa, Shun Muramatsu, Takayuki Furuishi, Yoshinori Onuki, Kaori Fukuzawa and Etsuo Yonemochi
Pharmaceuticals 2022, 15(8), 1004; https://doi.org/10.3390/ph15081004 - 15 Aug 2022
Cited by 3 | Viewed by 3184
Abstract
Moisture-activated dry granulation (MADG) is an eco-friendly granulation method that uses a small amount of water and insoluble excipients to absorb moisture. MADG is expected to improve productivity and reduce costs. Erythritol, an excipient used for preparing orally disintegrating tablets (ODTs), has poor [...] Read more.
Moisture-activated dry granulation (MADG) is an eco-friendly granulation method that uses a small amount of water and insoluble excipients to absorb moisture. MADG is expected to improve productivity and reduce costs. Erythritol, an excipient used for preparing orally disintegrating tablets (ODTs), has poor tabletability and is difficult to form into tablets by conventional methods, such as high-shear granulation (HSG) and direct compression. In this study, we optimized the manufacturing conditions for ODTs to improve the tabletability of erythritol using MADG. The disintegration time of tablets made using the MADG method was approximately one-tenth that of those made using the HSG method, and the hardness was approximately 1.4 times higher. Moreover, MADG could delay disintegration and improve tabletability. We further attempted to optimize the manufacturing conditions using MADG, particularly in terms of the amount of water used. The disintegration time increased as the amount of added water increased. Moreover, water absorption tests revealed that capillary wetting decreased as the amount of water added increased, but the initial wetting did not change. These results suggested that the disintegration time was prolonged because of the increase in granule density and decrease in capillary wetting with the increase in the amount of added water. The hardness of the tablets increased because of the easy deformation of the granules after the addition of up to 3% water; however, when more than 3% water was added, the hardness decreased because of the aggregation of the granules with the excess water. Finally, two-dimensional maps of the effect of the amount of added water and water activity indicated that tablets with a hardness of ≥80 N and a disintegration time of ≤15 s could be produced by adjusting the amount of added water to within the range of 2.2–3.3% and water activity to 0.3–0.53. These results indicate that MADG can improve the tabletability of erythritol and be used for the granulation of ODTs. Tablets with appropriate hardness and disintegration properties can be produced by adjusting the water content to approximately 2.7% and the water activity to approximately 0.4 when producing ODTs with MADG. Full article
(This article belongs to the Special Issue Formulation and Evaluation of Tablets of Different Drugs)
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14 pages, 1572 KiB  
Article
Development of 3D-Printed, Liquisolid and Directly Compressed Glimepiride Tablets, Loaded with Black Seed Oil Self-Nanoemulsifying Drug Delivery System: In Vitro and In Vivo Characterization
by Tarek A. Ahmed, Hanadi A. Alotaibi, Waleed S. Alharbi, Martin K. Safo and Khalid M. El-Say
Pharmaceuticals 2022, 15(1), 68; https://doi.org/10.3390/ph15010068 - 5 Jan 2022
Cited by 12 | Viewed by 3124
Abstract
Glimepiride is characterized by an inconsistent dissolution and absorption profile due to its limited aqueous solubility. The aim of this study was to develop glimepiride tablets using three different manufacturing techniques, as well as to study their quality attributes and pharmacokinetics behavior. Black [...] Read more.
Glimepiride is characterized by an inconsistent dissolution and absorption profile due to its limited aqueous solubility. The aim of this study was to develop glimepiride tablets using three different manufacturing techniques, as well as to study their quality attributes and pharmacokinetics behavior. Black seed oil based self-nanoemulsifying drug delivery system (SNEDDS) formulation was developed and characterized. Glimepiride liquisolid and directly compressed tablets were prepared and their pre-compression and post-compression characteristics were evaluated. Semi-solid pastes loaded with SNEDDS were prepared and used to develop three-dimensional printing tablets utilizing the extrusion technique. In vivo comparative pharmacokinetics study was conducted on Male Wistar rats using a single dose one-period parallel design. The developed SNEDDS formulation showed a particle size of 45.607 ± 4.404 nm, and a glimepiride solubility of 25.002 ± 0.273 mg/mL. All the studied tablet formulations showed acceptable pre-compression and post-compression characteristics and a difference in their in vitro drug release behavior. The surface of the liquisolid and directly compressed tablets was smooth and non-porous, while the three-dimensional printing tablets showed a few porous surfaces. The inner structure of the liquisolid tablets showed some cracks and voids between the incorporated tablet ingredients while that of the three-dimensional printing tablets displayed some tortuosity and a gel porous-like structure. Most of the computed pharmacokinetic parameters improved with the liquisolid and three-dimensional printed tablets. The relative bioavailabilities of the three-dimensional printed and liquisolid tablets compared to commercial product were 121.68% and 113.86%, respectively. Therefore, the liquisolid and three-dimensional printed tablets are promising techniques for modifying glimepiride release and improving in vivo performance but more clinical investigations are required. Full article
(This article belongs to the Special Issue Formulation and Evaluation of Tablets of Different Drugs)
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22 pages, 3127 KiB  
Article
Formulation and Characterization of an Effervescent Hydrogen-Generating Tablet
by Moritz Rosch, Kurt Lucas, Jozef Al-Gousous, Ulrich Pöschl and Peter Langguth
Pharmaceuticals 2021, 14(12), 1327; https://doi.org/10.3390/ph14121327 - 18 Dec 2021
Cited by 9 | Viewed by 7430
Abstract
Hydrogen, as a medical gas, is a promising emerging treatment for many diseases related to inflammation and oxidative stress. Molecular hydrogen can be generated through hydrogen ion reduction by a metal, and magnesium-containing effervescent tablets constitute an attractive formulation strategy for oral delivery. [...] Read more.
Hydrogen, as a medical gas, is a promising emerging treatment for many diseases related to inflammation and oxidative stress. Molecular hydrogen can be generated through hydrogen ion reduction by a metal, and magnesium-containing effervescent tablets constitute an attractive formulation strategy for oral delivery. In this regard, saccharide-based excipients represent an important class of potential fillers with high water solubility and sweet taste. In this study, we investigated the effect of different saccharides on the morphological and mechanical properties and the disintegration of hydrogen-generating effervescent tablets prepared by dry granulation. Mannitol was found to be superior to other investigated saccharides and promoted far more rapid hydrogen generation combined with acceptable mechanical properties. In further product optimization involving investigation of lubricant effects, adipic acid was selected for the optimized tablet, due to regulatory considerations. Full article
(This article belongs to the Special Issue Formulation and Evaluation of Tablets of Different Drugs)
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20 pages, 11500 KiB  
Article
Formulation Study of a Co-Processed, Rice Starch-Based, All-in-One Excipient for Direct Compression Using the SeDeM-ODT Expert System
by Karnkamol Trisopon, Nisit Kittipongpatana, Phanphen Wattanaarsakit and Ornanong Suwannapakul Kittipongpatana
Pharmaceuticals 2021, 14(10), 1047; https://doi.org/10.3390/ph14101047 - 14 Oct 2021
Cited by 5 | Viewed by 4715
Abstract
A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the formulation containing CS, in comparison with those containing the [...] Read more.
A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the formulation containing CS, in comparison with those containing the physical mixture and the commercial DC excipients. The results revealed that CS showed acceptable values in all six incidence factors of the SeDeM-ODT diagram. In addition, the comprehensive indices (IGC and IGCB) were higher than 5.0, which indicated that CS could be compressed with DC technique without additional blending with a disintegrant in tablet formulation. The formulation study suggested that CS can be diluted up to 60% in the formulation to compensate for unsatisfactory properties of paracetamol. At this percentage, CS-containing tablets exhibited narrow weight variation (1.5%), low friability (0.43%), acceptable drug content (98%), and rapid disintegration (10 s). The dissolution profile of CS displayed that more than 80% of the drug content was released within 2 min. The functionality of CS was comparable to that of high functionality excipient composite (HFEC), whereas other excipients were unsuccessful in formulating the tablets. These results indicated that CS was a suitable all-in-one excipient for application in DC of tablets. Full article
(This article belongs to the Special Issue Formulation and Evaluation of Tablets of Different Drugs)
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