Crosslinked carboxymethyl rice starch (CLCMRS), prepared via dual modifications of native rice starch (NRS) with chloroacetic acid and sodium trimetaphosphate, was employed to facilitate the disintegration of hydroxypropylmethylcellulose (HPMC) orodispersible films (ODFs), with or without the addition of glycerol. Fabricated by using the solvent casting method, the composite films, with the HPMC--LCMRS ratios of 9:1, 7:1, 5:1 and 4:1, were then subjected to physicochemical and mechanical evaluations, including weight, thickness, moisture content and moisture absorption, swelling index, transparency, folding endurance, scanning electron microscopy, Fourier transform infrared spectroscopy, tensile strength, elongation at break, and Young’s modulus, as well as the determination of disintegration time by using the Petri dish method (PDM) and slide frame and bead method (SFM). The results showed that HPMC-CLCMRS composite films exhibited good film integrity, uniformity, and transparency with up to 20% CLCMRS incorporation (4:1 ratio). Non-plasticized composite films showed no significant changes in the average weight, thickness, density, folding endurance (96–122), tensile strength (2.01–2.13 MPa) and Young’s modulus (10.28–11.59 MPa) compared to HPMC film (135, 2.24 MPa, 10.67 MPa, respectively). On the other hand, the moisture content and moisture absorption were slightly higher, whereas the elongation at break (EAB; 4.31–5.09%) and the transparency (4.73–6.18) were slightly lowered from that of the HPMC film (6.03% and 7.03%, respectively). With the addition of glycerol as a plasticizer, the average weight and film thickness increased, and the density decreased. The folding endurance was improved (to >300), while the transparency remained in the acceptable range. Although the tensile strength of most composite films decreased (0.66–1.75 MPa), they all exhibited improved flexibility (EAB 7.27–11.07%) while retaining structural integrity. The disintegration times of most composite films (PDM 109–331, SFM 70–214 s) were lower than those of HPMC film (PDM 345, SFM 229 s). In conclusion, the incorporation of CLCMRS significantly improved the disintegration time of the composite films whereas it did not affect or only slightly affected the physicochemical and mechanical characteristics of the films. The 5:1 and 4:1 HPMC:CLCMRS composite films, in particular, showed promising potential application as a film base for the manufacturing of orodispersible film dosage forms.

The rice bran and rice bran wax of the KJ CMU107 rice strain were investigated as potential tablet lubricants in a directly compressed tablet formulation. Stabilized full-fatted rice bran (sFFRB), stabilized defatted rice bran (sDFRB), and rice bran wax (RBW) extracted and purified from crude rice bran oil (cRBO) were tested. Two commercial lubricants, including magnesium stearate (MGS) and hydrogenated cottonseed oil (HVO), were employed as the standards in the formulated mixtures, which contained spray-dried rice starch (SDRS) as a diluent. The tableting was carried out for each formulation, and the obtained tablets were physically and mechanically evaluated. Among the parameters investigated were the general appearance, ejection force, weight variation, hardness, friability, and disintegration time. The powder flow was also determined for each formulation. The results showed that the tablet ejection forces for all the lubricated formulations (58–259 N) were significantly lower than that of the non-lubricated control formulation (349 N). The use of sFFRB as a lubricant at 0.5–2.0% w/w could lower the ejection force up to 78%, but the hardness reduced so drastically that the formulations failed the friability test due to the chipping of the tablets’ edges. Moreover, sDFRB performed significantly better as the use at 0.5–1.0% w/w in the formulation helped to lower the ejection forces by up to 80% while maintaining the changes in the tablet hardness within 10%. RBW functioned effectively as a tablet lubricant at a concentration of 0.5% w/w, yielding tablets with good strength comparable to standard HVO lubricant while helping to reduce the ejection force by 82%. In formulations with good lubrication, i.e., friability < 1%, the powder flow was improved, and the tablet disintegration times were within the same range as the control and HVO formulations. In conclusion, sDFRB displayed a lubricant property at concentrations between 0.5 and 1.0% w/w, with slightly negative effects on the tablet hardness. RBW from KJ CMU107 rice was an effective tablet lubricant at 0.5% w/w, with no effect on tablet hardness. Both materials can be further developed for use as commercial lubricants in direct compression.

This study explored the functional and pharmaceutical properties of native and modified starches derived from rice bean (Vigna umbellata) using physical (pregelatinization) and chemical (phosphorylation, carboxymethylation) modifications. Native starch (NRBS) exhibited a 27.5% amylose content. Modifications significantly influenced physicochemical characteristics. Swelling power increased from 12.25 g/g in NRBS to 16.34 g/g (pregelatinized, PGRBS) and 18.91 g/g (carboxymethylated, CMRBS), while solubility reached 53.12% in CMRBS. X-ray diffraction study estimated degrees of crystallinity of 26.5%, 19.4%, 22.8%, and 14.5% for NRBS, PGRBS, phosphate crosslinked (CLRBS), and CMRBS, respectively. Oil absorption capacity was highest in CMRBS (1.67 g/g), while its free swelling capacity reached 6.12 g/g at 37 °C. In vitro digestibility showed resistant starch (RS) contents of 11.31%, 5.49%, 17.38%, and 21.65% for NRBS, PGRBS, CLRBS, and CMRBS, respectively. Flowability and compressibility analysis demonstrated that CLRBS had the best flow (Carr’s Index: 12.16%, Hausner ratio: 1.14), while CMRBS exhibited superior tablet hardness across compression forces. These findings highlight rice bean starch, particularly in its modified forms, as a sustainable and multifunctional excipient and ingredient for food and pharmaceutical applications.

Background: Large porous particles (LPPs) offer significant potential in drug delivery due to their porous structure and suitable particle size and shape, which can improve powder dispersibility and control drug release. Methods: In this study, sustained-release large porous microparticles of mannitol, PVA, and diclofenac sodium (MPDs) were developed using a spray drying technique. The influence of PVA co-spray drying and its concentration (0–40%) on the characteristics of the spray-dried particles was investigated. Results: Co-spray drying with PVA enhanced particle morphology, producing MPDs with a spherical shape and smooth surface, which minimized particle adhesion. This improvement correlated with a low Carr’s Index value (17.56%), indicating favorable particle dispersibility and aerosol performance. The large geometric diameter (>5 μm) of the MPDs, coupled with their low bulk density (<0.1 g/cm³), suggested potential for inhalation use. FTIR, XRD, and DSC analyses revealed that PVA altered the polymorphic form of mannitol, with the MPDs exhibiting a mixture of the α and δ forms. In vitro dissolution tests demonstrated that PVA co-spray drying effectively prolonged drug release, with the formulation containing 40% PVA (MPD-4) showing an optimal release profile. The release kinetics followed first-order Higuchi models, suggesting drug release occurred through a matrix diffusion mechanism facilitated by the porous structure. Conclusions: These findings demonstrate the feasibility of engineering large porous microparticles with tailored release characteristics and physicochemical properties suitable for further development in inhalable or other controlled-release dosage forms.

In recent years, pediatric medicine has shifted towards solid oral dosage forms, moving away from liquid formulations to create tailored platforms for children. Orally disintegrating mini-tablets (ODMTs), with a diameter below 3 mm, dissolve rapidly in the mouth and represent a promising option. This study aimed to develop ODMTs using various co-process excipients, assessing their suitability with the Sediment Delivery Model-Orally Disintegrating Tablet (SeDeM-ODT) expert system. Favorable Index of Good Compressibility and Bucodispersibility (IGCB) values (> 5) were found for F-MELT® and co-process rice starch (CR), utilizing for ODMT formulation. Cetirizine dihydrochloride (CET) was evaluated for direct compression suitability, revealing flowability deficiencies. Therefore, co-process excipient quantities were adjusted based on flowability compensation. CET-ODMTs containing F-MELT® exhibited higher drug loading capacity than CR (5 and 2.5 mg/table, respectively). Uniformity of mass, content uniformity, and friability met acceptance criteria with no significant differences between formulations. F-MELT®-based CET-ODMTs showed slower wettability due to magnesium stearate lubrication. Ultimately, the SeDeM-ODT expert system facilitated the excipient selection and formulation development, resulting in ODMTs meeting requirements with minimal experimentation.

Background/Objectives: Direct compression offers a cost-effective route for tablet manufacturing but is often limited by poor powder flow and compressibility. This study reported the development of a co-processed excipient comprising 98% mannitol and 2% pregelatinized rice starch (PRS) using spray drying with ammonium bicarbonate as a pore-forming agent. Methods: This optimized excipient demonstrated balanced powder flow and enhanced compressibility suitable for direct compression applications. The SeDeM expert system guided the optimization process by evaluating raw and spray-dried components. PRS exhibited excellent flowability that decreased after spray drying but displayed significantly enhanced compressibility, whereas mannitol maintained superior flow but continued to show limited compressibility post-drying. Scanning electron microscopy, differential scanning calorimetry, Fourier-transform infrared spectroscopy, and X-ray powder diffraction confirmed the absence of chemical interactions and unchanged wettability during co-processing. Results: The resulting excipient combined the favorable flow characteristics of mannitol with the improved compressibility of PRS, rendering it suitable for direct compression. Cetirizine dihydrochloride (CET) tablets were formulated via exponential curve fitting within the SeDeM framework, yielding an optimal CET-to-excipient ratio of 13:87. The tablets met all pharmacopeial physicochemical requirements, including uniform mass, adequate tensile strength, rapid disintegration, and dissolution profiles comparable to a reference product, with dissimilarity (f₁ = 4.28) and similarity (f₂ = 64.03) factors within regulatory acceptance limits. Conclusions: These findings represented the first application of SeDeM methodology to a co-processed mannitol–pregelatinized rice starch system, enabling predictive optimization of powder flow and compressibility in direct compression formulations.