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An excipient intended for direct compression in pharmaceutical tableting must show important features of flowability and compactibility. This study investigated pregelatinised sago starch as an excipient for direct compression tablets. Pregelatinised sago starch was prepared and characterised. Its powder bulk properties and performance in the tablet formulations with paracetamol as a model drug were compared against two commercial, directly compressible excipients, namely Avicel® PH 101 and Spress® B820. The results showed that pregelatinisation did not affect the chemical structure of sago starch, but its degree of crystallinity reduced, and X-ray diffraction pattern changed from C-type to A-type. Powder bulk properties of pregelatinised sago starch and Spress® B820 were comparable, exhibiting better flowability but lower compactibility than Avicel® PH 101. In the formulation of paracetamol tablets, pregelatinised sago starch and Spress® B820 performed equally well, followed by Avicel® PH 101 as indicated in Formulations 3, 2 and 1, respectively.

Hypromellose, a widely used polymer in the pharmaceutical industry, is available in several grades, depending on the percentage of substitution of the methoxyl and hydroxypropyl groups and molecular weight, and in various functional forms (e.g., suitable for direct compression tableting). These differences can affect their physicomechanical properties, and so this study aims to characterise the particle size and mechanical properties of HPMC K100M polymer grades from four different vendors. Eight polymers (CR and DC grades) were analysed using scanning electron microscopy (SEM) and light microscopy automated image analysis particle characterisation to examine the powder’s particle morphology and particle size distribution. Bulk density, tapped density, and true density of the materials were also analysed. Flow was determined using a shear cell tester. Flat-faced polymer compacts were made at five different compression forces and the mechanical properties of the compacts were evaluated to give an indication of the powder’s capacity to form a tablet with desirable strength under specific pressures. The results indicated that the CR grades of the polymers displayed a smaller particle size and better mechanical properties compared to the DC grade HPMC K100M polymers. The DC grades, however, had better flow properties than their CR counterparts. The results also suggested some similarities and differences between some of the polymers from the different vendors despite the similarity in substitution level, reminding the user that care and consideration should be given when substitution is required.

The aim of this study was to improve flowability and compressibility characteristics of starch to use as a suitable excipient in direct compression tabletting. Quasi-emulsion solvent diffusion was used as a crystal modification method. Corn starch was dissolved in hydrochloric acid at 80°C and then ethanol as a non-solvent was added with lowering temperature until the formation of a precipitate of modified starch. Flow parameters, particle size and thermal behavior of the treated powders were compared with the native starch. Finally, the 1:1 mixture of naproxen and each excipient was tabletted, and hardness and friability of different tablets were evaluated. Larger and well shaped agglomerates were formed which showed different thermal behavior. Treated starch exhibited suitable flow properties and tablets made by the treated powder had relatively high hardness. It was found that recrystallization of corn starch by quasi emulsion solvent diffusion method could improve its flowability and compressibility characteristics.

Obtaining orodispersible tablets (ODT) containing substances from the second Biopharmaceutical Class has raised concerns as the dissolution test is challenging. This study aimed to select suitable excipients for developing orodispersible tablets containing cannabidiol (CBD) by direct compression method. No similar studies were found in the literature. Excipients from different classes were characterized using the SeDeM-ODT tool: fillers – lactose (LCT) and microcrystalline cellulose (CelMC), sweeteners – sorbitol (SRB) and mannitol (MNT), disintegrants – sodium starch glycolate (SSG), sodium croscarmellose (CCS), soy polysaccharides (Emcosoy® – EMCS) and two co-processed excipients (Prosolv®-ODT G2 – PODTG2 and Prosolv® EasyTab sp – PETsp). Drug compatibility with excipients in binary mixtures (1:1) was verified by Differential Scanning Calorimetry (DSC) and Fourier Transform-Infrared (FTIR) spectroscopy. Using the SeDeM-ODT expert system, the fillers and the co-processed excipients showed good properties regarding compressibility and disintegration behavior. Also, the DSC and FTIR results showed that small or no interactions between the CBD and the excipients took place.

PurposeAlthough the mechanical properties of paracetamol and MCC are extensively described in literature, there still is a need for a better understanding of the material properties impacting them. Thus, this study systematically analyzed material properties of paracetamol-MCC blends to elucidate their influence on the mechanical tablet properties in roller compaction and direct compression with special focus on surface properties.MethodsMultiple material characteristics of binary mixtures of paracetamol and MCC with varying drug loads were analyzed, with particular emphasis on specific surface area and surface energy. Subsequently, mechanical tablet properties of the materials in direct compression and after roller compaction were examined.ResultsIt was demonstrated that the impact of the initial material properties on mechanical tablet properties prevailed over the impact of processing route for paracetamol-MCC blends, underlining the importance of material characterization for tabletability of oral solid dosage forms. By applying bivariate as well as multivariate analysis, key material properties influencing the tabletability of paracetamol, MCC and its mixtures such as surface area, surface energy, effective angle of internal friction and density descriptors were identified.ConclusionsThis study highlighted the importance of comprehensive assessment of different material characteristics leading to a deeper understanding of underlying factors impacting mechanical tablet properties in direct compression and after roller compaction by the example of paracetamol-MCC mixtures with varying drug loads. Furthermore, it was shown that multivariate analysis could be a valuable extension to common bivariate analysis to reveal underlying correlations of material properties.

Orally disintegrating tablets (ODTs) are one of the drug delivery systems with high acceptance and compliances. The major advantage of ODTs is drug administration any time without water; self-medication and stability compared to parenteral which increased patient compliances. Orally disintegrating tablets (ODTs) which have ideal properties and desired characteristics have remarkable impact on the patient compliance. The main characteristics required for ODTs to be successful are that they don't require water for oral administration, dissolve, disperse, or disintegrate in the mouth in a matter of seconds, have a high bioavailability, start working therapeutically quickly, are less sensitive to temperature and humidity to maintain stability, and use an economical production process that includes packaging. Furthermore, desirable properties for ODTs include swallowability, drug dissolving in saliva, high drug loading, and prevention of tablet size growth. Leaves of Piper betel possess several bioactivities and are used in traditional medicinal systems. The goal is to demonstrate the potential impact of this plant on the creation of herbal medications with therapeutic effects. Phenolic compounds present in the Piper betel inhibit the lipid peroxidation and had the ability to prevent oxidative DNA damage. The hydrophobic parts of the compound may enable them to partition the lipids of the bacterial cell membrane, thereby disturbing the structures and rendering them more permeable. According to the study's findings, direct compression has a major impact on the drug's release, disintegration time, and % friability. It is thus concluded that direct compression is a better option for the formulation of Oral disintegrating tablet (ODT).

The study aimed to formulate DFX disintegrating tablets using different types of ready-to-use excipients using the direct compression method and evaluate the powder and tablet properties of the ready-to-use excipients. Ready-to-use excipients, including Parteck® ODT, Kollitab™ DC 87 L, Ludiflash®, Ludipress® LCE, Parteck® M 200, Parteck® SI 150, Parteck® LUB MST were blended with Deferasirox. The blend consisting of eight different formulations was evaluated for powder properties, including angle of repose, bulk density, tapped density, Hausner's ratio, and compressibility index. The produced tablets were evaluated for tablet properties, including weight variation, breaking force, thickness, friability, disintegration test, and dissolution test. According to all the obtained results, none of the prepared formulations could fulfill the requirements needed to be applicable as an individual excipient of ODT. The formulations that could pass all the tests except the dissolution test were formulation (F5) Ludiflash® and formulation (F4) Kollitab™ DC 87 L. Ludiflash® could provide a drug release after 30 minutes of (45.62%) which was more than Kollitab™ DC 87 L which provides (35.32%). These excipients can not be used alone for ODTs. Further study is needed to optimize the formulations.

Dental caries poses a widespread oral health challenge demanding effective treatments that patients find agreeable. Our research zeroes in on crafting and assessing eugenol-infused herbal chewable tablets to combat tooth decay. Eugenol, a substance drawn from clove oil, boasts pain-relieving, germ-fighting, and swelling-reducing qualities - a perfect fit for dental use. We fashioned these herbal chew tablets via direct compression throwing in suitable additives to nail down key tablet traits like toughness, crumbliness, and how fast they break down. Due to excellent to good flow property and compression ability of powder blend, direct compression method was used for the formulation of chewable tablets. They checked weight changes, thickness, hardness, crumbliness, and drug spread and found satisfactory results. Lab tests revealed how fast eugenol released from the tablets. The team also studied how well these eugenol-packed tablets fought common mouth germs that rot teeth, like Streptococcus mutans and concluded that it has good antibacterial effect. With the help of findings, formulation 8 (F-8) was determined as optimized batch among all the batches. The results showed the chewable tablets had good physical and chemical qualities. Eugenol left the tablets at a proper rate. Antibacterial tests proved the tablets packed a punch against bacteria that cause tooth decay. People find it easier to take chewable tablets kids and older folks.

Metronidazole has the potential to produce local stomach specific action in order to treat Helicobacter pylori induced peptic ulcer disease. The current project executes the development of osmotically controlled bioadhesive metronidazole loaded effervescent floating tablets with optimized floating and swelling behavior. Direct compression technique was used to prepare the tablets. The designed formulations exhibited physico-chemical properties within acceptable optimum limits as per pharmacopeial requirements. The results of tablet floating studies revealed that all formulations, except F1 and F5, had good buoyancy characteristics (TFT > 12 h except F2 and F8 with TFT of 6 h). Formulation F2 containing guar gum in higher concentration with carbopol and formulation F8 containing guar gum in 50% decreased concentration in combination with HPMC and carbopol had enhanced FLT appreciably, with least TFT as compared to formulations F3, F4, and F6 (ANOVA; p ≤ 0.05). Formulation batches of F3, F4, and F6 exhibited appreciable FLT as well as TFT and were optimized formulations. Out of the above mentioned optimized batches, F4 and F6 formulations showed low FLT (4 and 5 s respectively). The results of the swelling study indicated a proportionate increase in the swelling index with increase in time. A significantly higher swelling ratio was found with formulation F6 and F4 compared with that of F7 and F8 (ANOVA; p ≤ 0.05). Additionally, the impact of pH change, agitational intensity, as well as increasing concentration of NaCl was investigated on drug release. It was observed that agitational intensity had no effect on drug release rate while increasing concentration of NaCl produced an increased drug release from the dosage form as compared to the drug release exhibited by the formulations in the absence of NaCl. Overall, this project could have valuable contribution in the fabrication of metronidazole loaded effervescent floating tablets. Gastro-retentive systems are expected to enhance local stomach specific action of anti H. pylori agents based on their buoyancy and swelling behavior.

PurposeOrodispersible tablets (orally disintegrating tablets, ODTs) have been used in pharmacotherapy for over 20 years since they overcome the problems with swallowing solid dosage forms. The successful formula manufactured by direct compression shall ensure acceptable mechanical strength and short disintegration time. Our research aimed to develop ODTs containing bromhexine hydrochloride suitable for registration in accordance with EMA requirements.MethodsWe examined the performance of five multifunctional co-processed excipients, i.e., F-Melt® C, F-Melt® M, Ludiflash®, Pharmaburst® 500 and Prosolv® ODT G2 as well as self-prepared physical blend of directly compressible excipients. We tested powder flow, true density, compaction characteristics and tableting speed sensitivity.ResultsThe manufacturability studies confirmed that all the co-processed excipients are very effective as the ODT formula constituents. We noticed superior properties of both F-Melt’s®, expressed by good mechanical strength of tablets and short disintegration time. Ludiflash® showed excellent performance due to low works of plastic deformation, elastic recovery and ejection. However, the tablets released less than 30% of the drug. Also, the self-prepared blend of excipients was found sufficient for ODT application and successfully transferred to production scale. Outcome of the scale-up trial revealed that the tablets complied with compendial requirements for orodispersible tablets.ConclusionsWe proved that the active ingredient cannot be absorbed in oral cavity and its dissolution profiles in media representing upper part of gastrointestinal tract are similar to marketed immediate release drug product. In our opinion, the developed formula is suitable for registration within the well-established use procedure without necessity of bioequivalence testing.