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A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (20 February 2023) | Viewed by 38445

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Prof. Dr. Jelena Djuris

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Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia
Interests: quality by design; oral drug delivery; solid dosage forms; artificial intelligence; modified drug release; multiparticulates; process optimization
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Dr. Ivana Aleksić

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Guest Editor

Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia
Interests: liquisolid systems; co-processed excipients; melt granulation; hot melt coating; multiparticulates; fluid bed; solid dosage forms
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Solid dosage forms are still the golden standard for patients and the pharmaceutical industry in terms of convenience and versatility. The current research interest in the field of solid dosage forms spans from formulation development of delivery systems for improved bioavailability of poorly soluble drugs (e.g., solid dispersions, liquisolid systems) to conversion of complex colloidal formulations, including biologics, into solid dosage forms for oral administration. Specific dosage forms for intraoral administration, such as orally disintegrating tablets, mucoadhesive tablets, and films, as well as multiparticulate systems that can be formulated as sprinkle products, have received great interest due to the potential for improved patient compliance. Furthermore, novel additive manufacturing technologies for 2D and 3D printing are allowing a patient-centric approach to drug delivery. From the perspective of the pharmaceutical industry, key enabling technologies are continuous processing, modeling, and simulation tools and process analytical technologies.

This Special Issue has the aim of highlighting recent advances in solid dosage forms, in terms of both formulation and processing aspects.

Dr. Jelena Djuris
Dr. Ivana Aleksić
Guest Editors

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Keywords

solid dosage forms
oral drug delivery
bioavailability
mesoporous materials
excipients
patient-focused formulation development
continuous processing
machine learning
quality by design

Published Papers (9 papers)

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Research

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22 pages, 6497 KiB

Open AccessEditor’s ChoiceArticle

Development of Simvastatin-Loaded Particles Using Spray Drying Method for Ex Tempore Preparation of Cartridges for 2D Printing Technology

by Barbara Sterle Zorec and Rok Dreu

Pharmaceutics 2023, 15(9), 2221; https://doi.org/10.3390/pharmaceutics15092221 - 28 Aug 2023

Viewed by 760

Abstract

In this work, a spray drying method was developed to produce drug/polymer (simvastatin/polycaprolactone) microparticles that have the potential to be used as a pre-formulation for ex tempore preparation of 2D printing cartridges. An experimental model was designed with the process parameters set to predict the smallest particle size required for successful 2D printing. Three different types of particles (lactose, nanocellulose/lactose, calcium silicate) were produced, and the average size of the dry particles varied depending on the sampling location (cyclone, collection vessel). The encapsulation efficiency of simvastatin was highest with nanocellulose/lactose from the collection vessel. The one-month stability of simvastatin in the particles showed low content, but the addition of ascorbic acid as an antioxidant increased the chemical stability of the drug. Interestingly, the addition of antioxidants decreased the stability of simvastatin in the calcium silicate particles from the collection vessel. Dispersion of the particles in three different propylene glycol and water mixtures (10/90, 50/50, and 90/10% (v/v)), representing a printable ink medium with three different viscosity and surface tension properties, showed that nanocellulose/lactose was the most suitable antiadhesive in terms of dispersed particle size (˂1 µm). After one month of storage, the dispersed particles remained in the same size range without undesirable particle agglomeration. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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19 pages, 2980 KiB

Open AccessArticle

Application of Machine-Learning Algorithms for Better Understanding the Properties of Liquisolid Systems Prepared with Three Mesoporous Silica Based Carriers

by Teodora Glišić, Jelena Djuriš, Ivana Vasiljević, Jelena Parojčić and Ivana Aleksić

Pharmaceutics 2023, 15(3), 741; https://doi.org/10.3390/pharmaceutics15030741 - 23 Feb 2023

Viewed by 1261

Abstract

The processing of liquisolid systems (LSS), which are considered a promising approach to improving the oral bioavailability of poorly soluble drugs, has proven challenging due to the relatively high amount of liquid phase incorporated within them. The objective of this study was to apply machine-learning tools to better understand the effects of formulation factors and/or tableting process parameters on the flowability and compaction properties of LSS with silica-based mesoporous excipients as carriers. In addition, the results of the flowability testing and dynamic compaction analysis of liquisolid admixtures were used to build data sets and develop predictive multivariate models. In the regression analysis, six different algorithms were used to model the relationship between tensile strength (TS), the target variable, and eight other input variables. The AdaBoost algorithm provided the best-fit model for predicting TS (coefficient of determination = 0.94), with ejection stress (ES), compaction pressure, and carrier type being the parameters that influenced its performance the most. The same algorithm was best for classification (precision = 0.90), depending on the type of carrier used, with detachment stress, ES, and TS as variables affecting the performance of the model. Furthermore, the formulations with Neusilin^® US2 were able to maintain good flowability and satisfactory values of TS despite having a higher liquid load compared to the other two carriers. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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30 pages, 3848 KiB

Open AccessArticle

Using a Material Library to Understand the Change of Tabletability by High Shear Wet Granulation

by Yawen Wang, Junjie Cao, Xiaoqing Zhao, Zichen Liang, Yanjiang Qiao, Gan Luo and Bing Xu

Pharmaceutics 2022, 14(12), 2631; https://doi.org/10.3390/pharmaceutics14122631 - 28 Nov 2022

Cited by 4 | Viewed by 2193

Abstract

Understanding the tabletability change of materials after granulation is critical for the formulation and process design in tablet development. In this paper, a material library consisting of 30 pharmaceutical materials was used to summarize the pattern of change of tabletability during high shear wet granulation and tableting (HSWGT). Each powdered material and the corresponding granules were characterized by 19 physical properties and nine compression behavior classification system (CBCS) parameters. Principal component analysis (PCA) was used to compare the physical properties and compression behaviors of ungranulated powders and granules. A new index, namely the relative change of tabletability (CoT_r), was proposed to quantify the tabletability change, and its advantages over the reworking potential were demonstrated. On the basis of CoT_r values, the tabletability change classification system (TCCS) was established. It was found that approximately 40% of materials in the material library presented a loss of tabletability (i.e., Type I), 50% of materials had nearly unchanged tabletability (i.e., Type II), and 10% of materials suffered from increased tabletability (i.e., Type III). With the help of tensile strength (TS) vs. compression pressure curves implemented on both powders and granules, a data fusion method and the PLS2 algorithm were further applied to identify the differences in material properties requirements for direct compression (DC) and HSWGT. Results indicated that increasing the plasticity or porosity of the starting materials was beneficial to acquiring high TS of tablets made by HSWGT. In conclusion, the presented TCCS provided a means for the initial risk assessment of materials in tablet formulation design and the data modeling method helped to predict the impact of formulation ingredients on the strength of compacts. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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12 pages, 7175 KiB

Open AccessArticle

Drug Physicochemical Properties and Capsule Fill Determine Extent of Premature Gastric Release from Enteric Capsules

by Fouad S. Moghrabi and Hala M. Fadda

Pharmaceutics 2022, 14(11), 2505; https://doi.org/10.3390/pharmaceutics14112505 - 18 Nov 2022

Cited by 4 | Viewed by 2204

Abstract

Intrinsically, enteric capsule shells offer several advantages compared to coating of dosage forms with enteric polymers. We undertook a systematic investigation to elucidate capsule-fill parameters that may result in premature gastric drug release from Vcaps^® Enteric capsules (Lonza CHI, Morristown, NJ, USA). Four model drugs with different ionization and solubility profiles were investigated: acetaminophen, ketoprofen, trimethoprim and atenolol. Different fill loads, diluents and drug-to-diluent ratios were explored. Enteric capsules were filled with drug or drug and diluent powder mix and underwent USP II dissolution testing using mini-vessels and paddles. Capsules were tested in pH 2 (0.01 M HCl) or pH 4.5 (3.2 × 10⁻⁵ M HCl) 200 mL acid media to simulate normal, fasted or hypochlorhydric gastric pH, respectively. Acetaminophen, trimethoprim and atenolol displayed premature gastric drug release from enteric capsules. The extent of premature release was dependent on drug solubility, ionization profile and capsule-fill level. At 100 mg drug-fill level, acetaminophen, trimethoprim and atenolol gave rise to 10.6, 12.2 and 83.1% drug release, respectively, in normal, fasted, gastric fluids. Diffusion layer pH of trimethoprim and atenolol in pH 2 media was determined to be pH 6.3 and 10.3, respectively. Upon increasing capsule-fill load using microcrystalline cellulose as a diluent, a significant reduction in premature gastric release was observed. However, including mannitol as a diluent was only effective at decreasing premature drug release at a low drug-to-diluent ratio. Systematic in vitro screening of enteric capsule fills needs to be conducted to ensure that drug product performance is not compromised. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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26 pages, 5712 KiB

Open AccessArticle

Itraconazole Amorphous Solid Dispersion Tablets: Formulation and Compaction Process Optimization Using Quality by Design Principles and Tools

by Hetvi Triboandas, Kendal Pitt, Mariana Bezerra, Delphine Ach-Hubert and Walkiria Schlindwein

Pharmaceutics 2022, 14(11), 2398; https://doi.org/10.3390/pharmaceutics14112398 - 07 Nov 2022

Cited by 10 | Viewed by 3301

Abstract

BCS Class II drugs, such as itraconazole (ITZ), exhibit poor solubility (1–4 ng/mL) and so require solubility enhancement. Therefore, ITZ and Kollidon^® VA64 (KOL) amorphous solid dispersions (ASDs) were produced using hot-melt extrusion (HME) to improve ITZ’s poor solubility. A novel strategy for tablet formulations using five inorganic salts was investigated (KCl, NaCl, KBr, KHCO₃ and KH₂PO₄). These kosmotopric salts are thought to compete for water hydration near the polymer chain, hence, preventing polymer gelation and, therefore, facilitating disintegration and dissolution. Out of all the formulations, the KCl containing one demonstrated acceptable tensile strength (above 1.7 MPa), whilst providing a quick disintegration time (less than 15 min) and so was selected for further formulation development through a design of the experiment approach. Seven ITZ-KOL-ASD formulations with KCl were compacted using round and oblong punches. Round tablets were found to disintegrate under 20 min, whereas oblong tablets disintegrated within 10 min. The round tablets achieved over 80% ITZ release within 15 min, with six out of seven formulations achieving 100% ITZ release by 30 min. It was found that tablets comprising high levels of Avicel^® pH 102 (30%) and low levels of KCl (5%) tend to fail the disintegration target due to the strong bonding capacity of Avicel^® pH 102. The disintegration time and tensile strength responses were modeled to obtain design spaces (DSs) relevant to both round and oblong tablets. Within the DS, several formulations can be chosen, which meet the Quality Target Product Profile (QTPP) requirements for immediate-release round and oblong tablets and allow for flexibility to compact in different tablet shape to accommodate patients’ needs. It was concluded that the use of inorganic salts, such as KCl, is the key to producing tablets of ITZ ASDs with fast disintegration and enhanced dissolution. Overall, ITZ-KOL-ASD tablet formulations, which meet the QTPP, were achieved in this study with the aid of Quality by Design (QbD) principles for formulation and compaction process development and optimization. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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16 pages, 2739 KiB

Open AccessEditor’s ChoiceArticle

Novel Esomeprazole Magnesium-Loaded Dual-Release Mini-Tablet Polycap: Formulation, Optimization, Characterization, and In Vivo Evaluation in Beagle Dogs

by Taek Kwan Kwon, Ji-Hyun Kang, Sang-Beom Na, Jae Ho Kim, Yong-Il Kim, Dong-Wook Kim and Chun-Woong Park

Pharmaceutics 2022, 14(7), 1411; https://doi.org/10.3390/pharmaceutics14071411 - 05 Jul 2022

Cited by 4 | Viewed by 4500

Abstract

Esomeprazole magnesium (EMP) is a proton pump inhibitor (PPI) that reduces acid secretion. EMP has a short plasma half-life (approximately 1.3 h); hence, nocturnal acid breakthrough (NAB) frequently occurs, disturbing the patient’s nighttime comfort and sleep. We aimed to develop a novel esomeprazole magnesium-loaded dual-release mini-tablet polycap (DR polycap) with a prolonged onset time and improved bioavailability to prevent NAB. The formulation of the EPM mini-tablet core resulted in rapid drug release. The core was coated with an inner coating and an Eudragit^® L30D-55 aqueous dispersion coating to prepare the first-release mini-tablet. In addition, the core was coated with an inner coating and an aqueous dispersion of Eudragit^® S100 and Eudragit^® L100 coating to prepare the second-release mini-tablet. Each mini-tablet type was characterized using an in vitro dissolution test and microscopic examination. After testing, 10 of each mini-tablets were placed together in hard capsules to form DR polycaps. The combination of mini-tablets was optimized via in vitro release testing and in vivo pharmacokinetic studies. The AUC_0–24h of the DR polycap was similar to that of a comparable commercial product (Nexium^®); C_max was lower by approximately 50%, and T_max was extended by approximately 1.7-fold. In conclusion, DR polycap is an alternative to commercial products with improved NAB and dosing compliance because of its dual-release characteristics. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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Review

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23 pages, 4978 KiB

Open AccessReview

3D Printing Technology as a Promising Tool to Design Nanomedicine-Based Solid Dosage Forms: Contemporary Research and Future Scope

by Javed Ahmad, Anuj Garg, Gulam Mustafa, Abdul Aleem Mohammed and Mohammad Zaki Ahmad

Pharmaceutics 2023, 15(5), 1448; https://doi.org/10.3390/pharmaceutics15051448 - 10 May 2023

Cited by 9 | Viewed by 2612

Abstract

3D printing technology in medicine is gaining great attention from researchers since the FDA approved the first 3D-printed tablet (Spritam^®) on the market. This technique permits the fabrication of various types of dosage forms with different geometries and designs. Its feasibility in the design of different types of pharmaceutical dosage forms is very promising for making quick prototypes because it is flexible and does not require expensive equipment or molds. However, the development of multi-functional drug delivery systems, specifically as solid dosage forms loaded with nanopharmaceuticals, has received attention in recent years, although it is challenging for formulators to convert them into a successful solid dosage form. The combination of nanotechnology with the 3D printing technique in the field of medicine has provided a platform to overcome the challenges associated with the fabrication of nanomedicine-based solid dosage forms. Therefore, the major focus of the present manuscript is to review the recent research developments that involved the formulation design of nanomedicine-based solid dosage forms utilizing 3D printing technology. Utilization of 3D printing techniques in the field of nanopharmaceuticals achieved the successful transformation of liquid polymeric nanocapsules and liquid self-nanoemulsifying drug delivery systems (SNEDDS) to solid dosage forms such as tablets and suppositories easily with customized doses as per the needs of the individual patient (personalized medicine). Furthermore, the present review also highlights the utility of extrusion-based 3D printing techniques (Pressure-Assisted Microsyringe—PAM; Fused Deposition Modeling—FDM) to produce tablets and suppositories containing polymeric nanocapsule systems and SNEDDS for oral and rectal administration. The manuscript critically analyzes contemporary research related to the impact of various process parameters on the performance of 3D-printed solid dosage forms. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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26 pages, 3976 KiB

Open AccessEditor’s ChoiceReview

Emerging Artificial Intelligence (AI) Technologies Used in the Development of Solid Dosage Forms

by Junhuang Jiang, Xiangyu Ma, Defang Ouyang and Robert O. Williams III

Pharmaceutics 2022, 14(11), 2257; https://doi.org/10.3390/pharmaceutics14112257 - 22 Oct 2022

Cited by 17 | Viewed by 7781

Abstract

Artificial Intelligence (AI)-based formulation development is a promising approach for facilitating the drug product development process. AI is a versatile tool that contains multiple algorithms that can be applied in various circumstances. Solid dosage forms, represented by tablets, capsules, powder, granules, etc., are among the most widely used administration methods. During the product development process, multiple factors including critical material attributes (CMAs) and processing parameters can affect product properties, such as dissolution rates, physical and chemical stabilities, particle size distribution, and the aerosol performance of the dry powder. However, the conventional trial-and-error approach for product development is inefficient, laborious, and time-consuming. AI has been recently recognized as an emerging and cutting-edge tool for pharmaceutical formulation development which has gained much attention. This review provides the following insights: (1) a general introduction of AI in the pharmaceutical sciences and principal guidance from the regulatory agencies, (2) approaches to generating a database for solid dosage formulations, (3) insight on data preparation and processing, (4) a brief introduction to and comparisons of AI algorithms, and (5) information on applications and case studies of AI as applied to solid dosage forms. In addition, the powerful technique known as deep learning-based image analytics will be discussed along with its pharmaceutical applications. By applying emerging AI technology, scientists and researchers can better understand and predict the properties of drug formulations to facilitate more efficient drug product development processes. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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73 pages, 1350 KiB

Open AccessEditor’s ChoiceReview

Formulation of Dosage Forms with Proton Pump Inhibitors: State of the Art, Challenges and Future Perspectives

by Justyna Srebro, Witold Brniak and Aleksander Mendyk

Pharmaceutics 2022, 14(10), 2043; https://doi.org/10.3390/pharmaceutics14102043 - 25 Sep 2022

Cited by 10 | Viewed by 11295

Abstract

Since their introduction to pharmacotherapy, proton pump inhibitors (PPIs) have been widely used in the treatment of numerous diseases manifested by excessive secretion of gastric acid. Despite that, there are still unmet needs regarding their availability for patients of all age groups. Their poor stability hinders the development of formulations in which dose can be easily adjusted. The aim of this review is to describe the discovery and development of PPIs, discuss formulation issues, and present the contemporary solutions, possibilities, and challenges in formulation development. The review outlines the physicochemical characteristics of PPIs, connects them with pharmacokinetic and pharmacodynamic properties, and describes the stability of PPIs, including the identification of the most important factors affecting them. Moreover, the possibilities for qualitative and quantitative analysis of PPIs are briefly depicted. This review also characterizes commercial preparations with PPIs available in the US and EU. The major part of the review is focused on the presentation of the state of the art in the development of novel formulations with PPIs covering various approaches employed in this process: nanoparticles, microparticles, minitablets, pellets, bilayer, floating, and mucoadhesive tablets, as well as parenteral, transdermal, and rectal preparations. It also anticipates further possibilities in the development of PPIs dosage forms. It is especially addressed to the researchers developing new formulations containing PPIs, since it covers the most important formulary issues that need to be considered before a decision on the selection of the formula is made. It may help in avoiding unnecessary efforts in this process and choosing the best approach. The review also presents an up-to-date database of publications focused on the pharmaceutical technology of formulations with PPIs. Full article

(This article belongs to the Special Issue Recent Advances in Solid Dosage Form)

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