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5
Advances inPharmaceutical Oral Solid
Dosage Forms
P.Saikiran, T.PawanKumar, ShristiArya, DarshanaTijare,
SohamLoharkar, GopalBajad, DeepankarBahuguna,
PawanDevangan, AtulMourya,
HarithasreeVeerabromma, ChantibabuKatta,
andJitenderMadan
Abstract
The pharmaceutical and healthcare industries are constantly moving through a
period of unmatched changes. Oral administration of solid dosage forms is one
of the most preferred route and is highly patient compliant as well as stable when
compared to other dosage forms. However, the challenge of transition from a
traditional manufacturing approach to continuous automated processing
approach remains unmet. Continuous modications in materials and manufac-
turing technologies are gradually being implemented in the industry to avail the
benets related to process automation, improved quality and reduced costs.
Therefore, it is well accepted that there is a growing demand to discover alterna-
tive processes and design formulation strategies that can signicantly improve
powder processing techniques, granulation methods and equipment to ensure
safe, reproducible and quality products are manufactured. The intended chapter
presents an overview of the state-of-the-art research equipment, material han-
dling techniques, process analytical technique implementation and 3D printing
application strategies. It covers recent advances in techniques and processes at
every stage of pharmaceutical product development and methods employed to
troubleshoot the processing hurdles.
Keywords
Oral route of administration · Solid dosage form · Materials and manufacturing ·
3D printing
P. Saikiran · T. PawanKumar · S. Arya · D. Tijare · S. Loharkar · G. Bajad · D. Bahuguna ·
P. Devangan · A. Mourya · H. Veerabromma · C. Katta · J. Madan (
*)
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research,
Hyderabad, Telangana, India
112
5.1 Introduction
In the vast landscape of pharmaceutical formulations, conventional oral solid dos-
age forms hold a signicant place as one of the most commonly utilised and acces-
sible means of drug administration (Zhang etal. 2004). These solid preparations,
designed to be swallowed and dissolved in the gastrointestinal tract, have played a
crucial role in the treatment of various diseases and ailments. Furthermore, the pop-
ularity of conventional oral solid dosage forms can be attributed to their ease of
administration, allowing patients to self-administer medications conveniently with-
out the need for specialised medical procedures.
Various kinds of oral solid dosage forms such as tablets, capsules, lozenges,
powders, granules and many other formulations are used for the delivery of active
pharmaceutical ingredients (API) (Arshad etal. 2021). Tablets can be further cate-
gorised into immediate release (compressed tablets), extended release, chewable,
effervescent, sublingual, buccal, enteric-coated, dispersible, scored and lm-coated
tablets, each serving specic therapeutic purposes (Lachman et al. 1976). Film-
coated tablets are compressed tablets that are coated with a thin layer of lm. These
coatings have become the rst choice of formulators due to advances in material
science and polymer chemistry (Almoazen and Felton 2013). Enteric-coated/func-
tionalised coated tablets are compressed tablets, coated with substances that resist
dissolution in gastric uid but disintegrate in the intestine (Maderuelo etal. 2019).
A layer or lm made out of water-soluble materials is the main idea behind capsule
development which surrounds drug or active API, hence rendering it odourless,
tasteless, elegant and easy to swallow. There are presently two main types of cap-
sules, viz. hard gelatin and soft gelatin capsules (soft shells) (Hoag 2017). Soft shell
capsules (soft gels) are typically used to encapsulate non aqueous liquid and semi-
solid formulations, and hard shell capsules are used to encapsulate both solid and
nonaqueous formulations (Gullapalli and Mazzitelli 2017). Pellets are dosage forms
similar to tablets and capsule which can be prepared by different types of novel
techniques. They are small solid substances composed of highly puried active
ingredient with or without excipient (Kurbanoglu etal. 2017).
Despite many advantages offered by conventional dosage forms, they often suf-
fer from some major limitations like low bioavailability, repeated dosing, peripheral
adverse effects and lack of patient compliance (Lafeur and Keckeis 2020). Lack of
targeted action, premature decomposition of drugs and uctuations in plasma drug
concentrations are the extended limitations of oral solid dosage forms. For very
potent medicines, the precise dosing may be difcult or impossible with conven-
tional dosage forms (Adepu and Ramakrishna 2021). Solubility, which ultimately
affects the bioavailability of the medicinal product and results in less effective
action, is a major problem associated with oral solid dosage forms. A complex chain
of physicochemical, biological, physiological and anatomical factors acting inde-
pendently and in concert with each other to limit drug bioavailability is a major
obstacle to successful oral administration (Boyd etal. 2019). Another barrier to the
administration of medicinal products orally is inadequate absorption and rst-pass
P. Saikiran etal.
113
metabolism, which has an effect on the amount of drugs reaching systemic circula-
tion necessary for their therapeutic efcacy (Devadasu etal. 2018).
To overcome the limitations associated with conventional dosage form, we need
advanced technologies. The major aim of the drug delivery system is to liberate the
substance at the correct time in an adequate concentration on a target site (Lafeur
and Keckeis 2020). In addition, novel raw materials have been used to improve
manufacturability and functionality. The development of additive manufacturing
technology, 3D printing medical devices, which offer key advantages over tradi-
tional drug delivery systems, has gained increasing popularity. The ability to pro-
duce 3D structures that are custom designed and have a complex architecture is of
paramount importance, as well as easy access to personalised medicines (Wang
etal. 2021a). Automated medication system helps to minimise errors in drug admin-
istration process, and along with this it is cost-effective (Risør etal. 2017). Articial
intelligence (AI), which helps to increase the quality of a product and assist in its
optimisation, is emerging as an important tool for pharmaceutical industry (Khanna
etal. 2020). Process analytical technology (PAT) is an indispensable tool for imple-
menting quality by design (QbD), enabling effective process parameter monitoring
and the fabrication of nished pharmaceuticals of the highest standard. The devel-
opment of analytical QbD techniques facilitates the development of an appropriate
control plan to govern the analytical method, hence reducing variability and enhanc-
ing robustness in method performance with exceptional quality (Haneef and Beg
2021). Real-time release testing (RTRt) of the product is made possible when a
thorough understanding of the process is combined with the application of quick
and precise analytical sensors. To do this, identify the product’s critical quality attri-
butes (CQA), followed by the critical process parameters (CPP) and the critical
material attributes (CMA), all of which have a big impact on the CQAs (Galata
etal. 2021).
Progress of machine design over the years has led to the development of continu-
ous manufacturing technologies which increases productivity by application of
PAT.The intended chapter aims to summarise recent advances in the eld of oral
solid dosage forms highlighting key aspects of novel excipients used in its manufac-
turing. It throws light upon the utilisation of AI and 3D printing in solid oral dos-
age form.
5.2 Novel Excipients Involved inManufacturing ofOral
Solid Dosage Form
Pharmaceutical excipients are components used in the manufacturing process or
included in the dosage form of a nal pharmaceutical product but are not pharma-
cologically active drugs or prodrugs. The word excipient is derived from the Latin
word excipere, meaning ‘to except’, which is simply described as ‘other than’ (van
der Merwe etal. 2020). Excipients can make up to 80–90% of the formulation of a
drug product and are vital to the formulation of drug products because they provide
for the efcient distribution of therapeutic ingredients. A pharmaceutical excipient
5 Advances inPharmaceutical Oral Solid Dosage Forms
114
being inert offers many functions and is used to increase the bulk of medicament
during its formulation, improve product’s precision as well as API dose accuracy,
increase bioavailability and nally produce a more palatable nal pharmaceutical
form, with increased patient acceptance (Fig.5.1) (Abrantes etal. 2016).
Chemically modied excipients are categorised as novel excipients which can be
listed in inactive ingredient database (IID). Single-component excipients may not
always offer the necessary performance to enhance the formulation characteristics
for proper manufacturing of some active pharmaceutical compounds (Chaudhari
et al. 2012). Formulation scientists have an increasing number of co-processed
excipients introduced into the market. New approaches for enhancing excipient
functionality include new combinations of presently used excipients (van der Merwe
et al. 2020), e.g. binders, disintegrants, sweeteners, colorants and co-processed
excipients.
5.2.1 Binders
Pharmaceutical binders are designed to produce a product with the appropriate ow
qualities. These components employed to give the powder ingredients a specic
shape and size (Kar etal. 2019). Binders are applied to the powders to improve the
ow qualities of the powdered raw material by reducing surface area and increasing
cohesiveness (Allenspach et al. 2020). They are obtained from natural origin
(starch), semisynthetic origin (hydroxyl ethyl cellulose) and synthetic origin (povi-
done). Now a days, different grades of binders are introduced that have more
advanced properties such as better drug release and controlled pharmacokinetics
than conventional forms.
Fig. 5.1 Conventional excipients used in the manufacture of pharmaceutical solid oral dosage form
P. Saikiran etal.
115
5.2.1.1 Hydroxy Propyl Methyl Cellulose (HPMC)
HPMC is used in a direct compression process or for continuous production. HPMC
exhibits poor ow for which new grades of direct compression HPMC have been
created. Three distinct novel direct compression (DC) grades of HPMC were used
to improve ow properties (K4M, K15M and K100M). Physical characteristics,
bioadhesive strength, buoyancy lag time, swelling index and invitro drug release
studies were assessed for the prepared tablets (Pittu and Sharma 2013).
5.2.1.2 LYCATA B
These are pregelatinised starches, which are often analysed with around 30% cws.
Conventionally, starch has limitations of low cold water solubility (Elballa and
Salih 2022). Pregelatinised starch obtained from Roquette is water dispersible and
acts as suitable binder.
5.2.1.3 GalenIQ (Isomalt)
GalenIQ (isomalt) is one of the most multi-functional water-soluble ller and binder
that has low hygroscopicity and is available in different pharmaceutical grades
based on solubility. It can be milled to desired particle size for preparing solid oral
dosage forms. It can be a mixture of D-sorbitol and D-mannitol suitable for a direct
compression process. It possesses excellent owability, negligible sticking to tablet-
ing tools and a very good compatibility. It is widely used in pharmaceutical prepara-
tions for coating of oral dispersible tablets and capsules.
5.2.2 Disintegrants
Disintegrants are chemical substances or mixtures of chemicals that are added to a
drug formulation to help break down or disintegrate the contents of tablets or cap-
sules into smaller pieces which would likely dissolve more quickly than they would
otherwise. Superdisintegrants are a new class of agents that are added to improve
dissolution and disintegration properties of dosage form in less than 30s, thereby
enhancing drug release absorption (e.g. croscarmellose, sodium starch glycolate)
(Desai etal. 2016).
Modied nanocrystalline cellulose (NCC) is a novel pharmaceutical excipient
which acts as a super disintegrant. It has been derivatised from microcrystalline cel-
lulose (MCC) via cross-linking process. Structural characteristics, such as low
porosity, cause unnecessary swelling, which restricts pharmaceutical applications
of MCC. However, NCC has better biocompatibility, biodegradability, low cost,
nontoxic and possesses characteristics such as large specic surface area, high ten-
sile strength, stiffness and lightweight (Sheikhy etal. 2021). Malic acid used as a
cross-linking agent reacts with NCC polymer to form double bond cross-linker. In
the graft copolymer nanocrystalline cellulose-poly (2-hydroxyethyl methacrylate-
co- itaconic acid) as modied NCC, it was hypothesised that adding hydrophilic
itaconic acid (IA) and relatively more hydrophobic poly (2-hydroxy-ethyl
5 Advances inPharmaceutical Oral Solid Dosage Forms
116
methacrylate) (PHEMA), HEMA, as co-monomers, may improve the HLB and
increase swelling property.
5.2.3 Lubricants
Lubricants are used to attain uniform tableting force distribution and tablet density
distribution. These are utilised to reduce friction between the particles or tablets and
the die-hole wall (Miller and York 1988). This allows the compressed tablet to be
pushed out of the die-hole smoothly while also requiring lesser force and wearing
down less frequently. Sodium stearyl fumarate is a relatively new lubricant and
comparatively less hydrophobic than stearic acid. It imparts lesser effect on tablet
disintegration and has higher ability to lessen friction and adhesion to the punches.
The particle size of sodium stearyl fumarate was more important, as it is an alterna-
tive to magnesium stearate. It is generally nontoxic and nonirritant material and can
be included in IID in a concentration range of 0.2–0.5% (de Backere etal. 2022).
5.2.4 Co-processed Excipients
Co-processing is an appealing method for enhancing the material properties of
APIs, which can be done at the point of API isolation. The pharmaceutical industry
is becoming more and more interested in continuous manufacturing techniques
(Stocker etal. 2023).
5.2.4.1 Kollitab™ DC 87L
It is a new all-in-one tableting excipient material with four characteristics such as
binder, ller, disintegrant and lubricant. It enables quick tablet disintegration, offers
greater owability and produces high tablet strength while using a wide range of
compression strengths (both low and high), eases formulation procedures and
decreases the complexity of production.
5.2.4.2 COMBILOSE
Lactose is the primary pharmaceutical diluent in solid oral dosage forms. Hence,
lactose’s inadequate compressibility and ow characteristics prevent it from being
used as a direct compressible ller and binder (Somnache etal. 2023). Maltose
monohydrate 10%, maize starch and lactose monohydrate 20:1 were all processed
together using co-freezing and co-drying techniques which has the potential to offer
improved dilution capability and compressibility with less susceptibility to
lubricants.
5.2.4.3 PEARLITOL CR-H
PEARLITOL formulations are used for modern direct compression techniques.
PEARLITOL
®
CR-H is a co-processed blend of hydroxypropyl methylcellulose
(HPMCK4M) (70%) and D-mannitol (30%) that enables the controlled release of
P. Saikiran etal.
117
active medicinal ingredients, with excellent functional characteristics that improve
tablet processibility, such as owability (Jin etal. 2023).
5.2.4.4 PROSOLV EASYtab SP (Silicified Microcrystalline Cellulose)
It is a multifunctional homogenous lubricant-coated co-processed excipient com-
posite. It is ready-to-use material comprising of four individual components such as
silicied MCC, colloidal silicon dioxide, sodium starch glycolate and sodium stea-
ryl fumarate which is a binder-ller, glidant, super disintegrant and a lubricant,
respectively (Darzuli etal. 2019). These components maintain their chemical identi-
ties while synergistically providing increased functional performance (Buckton
etal. 1999). Utilisation of PROSOLV EASYtab SP has the potential of increasing
protability through cost savings brought by increased productivity, less setup and
cleaning costs, improved yield and reduced loss.
5.3 New-Age Material Handling Techniques Developed
In the pharmaceutical sector, particularly when producing solid oral dosage forms,
material management is crucial (American Society of Health-System Pharmacists
2006). Throughout the production process, material handling comprises transpor-
tation, storage, management and protection of raw materials, completed items and
other things (Steenweg etal. 2021). The efcacy and efciency of material han-
dling operations signicantly affect the cost, lead time and quality of the nal
product (Jagtap et al. 2022). New-generation material handling solutions have
emerged in recent years as a result of technological breakthroughs in material han-
dling, offering various advantages over conventional methods (Arshad etal. 2021).
Oral solid dosage forms are taken orally and then absorbed in gastrointestinal tract
to provide a localised therapeutic impact in the mouth, throat, digestive tract or
systemic action in the body (Goodin etal. 2011). APIs and acceptable excipients
can be milled, dried, encapsulated, mixed, granulated or tableted to create oral
solid dosage forms. Due to its simplicity and resulting patient compliance, a vari-
ety of solid oral dosage forms, including tablets, capsules, lozenges, powders and
granules, have already been used effectively for conveying API (Ng etal. 2022).
Some of the most well- liked and thoroughly researched areas of oral solid dosage
form development include tablet formulations that offer a unit dose which is either
immediate drug release, modulated release or taste-masked (Finke and Kwade
2021). In order to create durable tablet dosage forms, quality by design (QBD)-
based formulation methodological approaches are often used to decrease variation
in processes. In order to enhance the functioning and manufacturability of tablet
formulations, new raw ingredients were also used (Jagtap etal. 2022). New Age
Material Handling Methods 1. Automated dispensing systems, 2. Vacuum convey-
ing systems, 3. Flexible screw conveyors.
5 Advances inPharmaceutical Oral Solid Dosage Forms