Controlled Release Formulations Research Articles

Smart and Sustainable Crop Protection: Design and Evaluation of a Novel α-Amylase-Responsive Nanopesticide for Effective Pest Control.

In this study, an α-amylase-responsive controlled-release formulation was developed by capping polydopamine onto β-cyclodextrin-modified abamectin-loaded hollow mesoporous silica nanoparticles. The prepared Aba@HMS@CD@PDA were subjected to characterization using various analytical techniques. The findings revealed that Aba@HMS@CD@PDA, featuring a loading rate of 18.8 wt %, displayed noteworthy release behavior of abamectin in the presence of α-amylase. In comparison to abamectin EC, Aba@HMS@CD@PDA displayed a significantly foliar affinity and improved rainfastness on lotus leaves. The results of field trail demonstrated a significantly higher control efficacy against Spodoptera litura Fabricius compared to abamectin EC at all concentrations after 7, 14, and 21 days of spaying, showcasing the remarkable persistence of Aba@HMS@CD@PDA. These results underscore the potential of Aba@HMS@CD@PDA as a novel and persistently effective strategy for sustainable on-demand crop protection. The application of nanopesticides can enhance the effectiveness and efficiency of pesticide utilization, contributing to more sustainable agricultural practices.

Agar-gelatin-derived hydrogel-based controlled delivery devices for linuron herbicide to prevent environmental hazards

Innovation in agriculture chemicals and delivery systems is essential for the production of food for sustainable development. Herein, natural polymers and agar-gelatin-derived controlled delivery devices for linuron herbicide to prevent environmental and health hazards. These hydrogels were designed by the graft-copolymerization reaction of poly(methacrylamide) [poly(MAAm)] on agar-gelatin for use as controlled-release formulations (CRF). Copolymers were characterized by Copolymers were characterized scanning electron micrographs (SEM), Atomic force microscopy (AFM), X-ray diffraction (XRD) Fourier transform infrared spectroscopy (FTIR), 13C-nuclear magnetic resonance (NMR), and thermogravimetric analysis -differential thermogravimetry (TGA-DTG) techniques. SEM shows the uneven surface morphology, and AFM showed a rough surface with an average roughness value of 137.50 nm in the polymeric matrix. The amorphous nature of the polymer was confirmed with XRD techniques. Grafting of the poly(MAAm) on the agar and gelatin was confirmed by FTIR and 13C NMR spectra. Agar-gelatin-cl-poly(MAAm) hydrogels absorbed water at 4.05 ± 0.32 g per gram, which is useful for soil water retention. Release of the linuron herbicide occurred in a controlled manner during 72 h of observations and followed non-Fickian diffusion mechanism. The slow release of the linuron from the hydrogel is a useful observation for preventing leaching and evaporation loss of herbicide. In the soil column, the release of linuron occurred in a slow and sustained manner for 240 h. A soil adsorption study showed a decrease in ground water ubiquity score (GUS) for linuron-encapsulated hydrogel as compared to commercial formulations. It can reduce groundwater contamination risk due to the leaching of the linuron herbicide. Degradation of CRF may improve micronutrient and soil quality.

Bactericidal Chitosan Derivatives and Their Superabsorbent Blends with ĸ-Carrageenan.

The aim of this work is research dedicated to the search for new bactericidal systems for use in cosmetic formulations, dermocosmetics, or the production of wound dressings. Over the last two decades, chitosan, due to its special biological activity, has become a highly indispensable biopolymer with very wide application possibilities. Reports in the literature on the antibacterial effects of chitosan are very diverse, but our research has shown that they can be successfully improved through chemical modification. Therefore, in this study, results on the synthesis of new chitosan-based Schiff bases, dCsSB-SFD and dCsSB-PCA, are obtained using two aldehydes: sodium 4-formylbenzene-1,3-disulfonate (SFD) and 2-pyridine carboxaldehyde (PCA), respectively. Chitosan derivatives synthesized in this way demonstrate stronger antimicrobial activity. Carrying out the procedure of grafting chitosan with a caproyl chain allowed obtaining compatible blends of chitosan derivatives with κ-carrageenan, which are stable hydrogels with a high swelling coefficient. Furthermore, the covalently bounded poly(ε-caprolactone) (PCL) chain improved the solubility of obtained polymers in organic solvents. In this respect, the Schiff base-containing polymers obtained in this study, with special hydrogel and antimicrobial properties, are very promising materials for potential use as a controlled-release formulation of both hydrophilic and hydrophobic drugs in cosmetic products for skin health.

Recent Advances in Stimulus-Responsive Nanocarriers for Pesticide Delivery.

In an effort to make pesticide use safer, more efficient, and sustainable, micro-/nanocarriers are increasingly being utilized in agriculture to deliver pesticide-active agents, thereby reducing quantities and improving effectiveness. In the use of nanopesticides, the choice to further design and prepare pesticide stimulus-responsive nanocarriers based on changes in the plant growth environment (light, temperature, pH, enzymes, etc.) has received more and more attention from researchers. Based on this, this paper examines recent advancements in nanomaterials for the design of stimulus-responsive micro-/nanocarriers. It delves into the intricacies of preparation methods, material enhancements, in vivo/ex vivo controlled release, and application techniques for controlled release formulations. The aim is to provide a crucial reference for harnessing nanotechnology to pursue reduced pesticide use and increased efficiency.

Alginate- and Chitosan-Modified Gelatin Hydrogel Microbeads for Delivery of E. coli Phages.

Bacterial infections are among the most significant health problems/concerns worldwide. A very critical concern is the rapidly increasing number of antibiotic-resistant bacteria, which requires much more effective countermeasures. As nature's antibacterial entities, bacteriophages shortly ("phages") are very important alternatives to antibiotics, having many superior features compared with antibiotics. The development of phage-carrying controlled-release formulations is still challenging due to the need to protect their activities in preparation, storage, and use, as well as the need to create more user-friendly forms by considering their application area/site/conditions. Here, we prepared gelatin hydrogel microbeads by a two-step process. Sodium alginate was included for modification within the initial recipes, and these composite microbeads were further coated with chitosan. Their swelling ratio, average diameters, and Zeta potentials were determined, and degradations in HCl were demonstrated. The target bacteria Escherichia coli (E.coli) and its specific phage (T4) were obtained from bacterial culture collections and propagated. Phages were loaded within the microbeads with a simple method. The phage release characteristics were investigated comparatively and were demonstrated here. High release rates were observed from the gelatin microbeads. It was possible to reduce the phage release rate using sodium alginate in the recipe and chitosan coating. Using these gelatin-based microbeads as phage carrier matrices-especially in lyophilized forms-significantly improved the phage stability even at room temperature. It was concluded that phage release from gelatin hydrogel microbeads could be further controlled by alginate and chitosan modifications and that user-friendly lyophilized phage formulations with a much longer shelf life could be produced.

Tween–80 Coating in Enhancing Physicochemical Stability, Kinetics and Release Mechanism of Layered Double Hydroxide-Ferulate

This study aims to enhance the targeted delivery of a powerful antioxidant, ferulate (FA), by developing a controlled release formulation (CRF) based on the incorporation of layered double hydroxide and Tween-80 polymeric surfactant. The layered double hydroxide-ferulate (LDH-FA) synthesized by co-precipitation method was homogenously mixed with the Tween-80 coater under continuous stirring. The successful Tween-80 coating was verified with PXRD analysis and supported by FTIR. No changes in interlayer distance between LDH-FA (at 17.4 and 8.7 Å) and LDH-FA-T80 (at 17.6 and 8.6 Å) were observed in the PXRD pattern. TGA/DTG analysis demonstrated good thermal stability of LDH-FA-T80, with the ability to withstand extreme temperatures up to 460 °C. The association of Tween-80 with LDH-FA progressively sustained the release time of FA in each aqueous solution, with a release time of up to 440 min. For both LDH-FA and LDH-FA-T80, the release of FA is through dissolution and anion exchange release mechanism (regulated by pseudo-second-order kinetic model). The study's findings suggest practical applications of FA in the pharmaceutical industry by implying the retarding effect triggered by Tween-80, offering new insights for the application of CRF to enhance the therapeutic effect of FA.

Nitrogen Use Efficiency and Yield Levels Using Soluble and Controlled-release Urea Formulations in Tomato Production

This research study evaluated the suitability of controlled-release urea (CRU) as an alternate nitrogen (N) fertilizer source to conventional soluble urea (U) for tomato production under a humid, warm climate in coastal plain soils. Tomatoes are typically produced on raised plastic-mulched beds, where U is fertigated through multiple applications. On the other hand, CRU is applied once at planting, incorporated into soil before the raised beds are covered with plastic mulch. N source and management will likely impact tomato yield, N use efficiency (NUE), and apparent recovery of N fertilizer (APR). A 2-year field study was conducted on fall and spring tomato crops in north Florida to determine the crop N requirement and NUE in tomatoes (var. HM 1823) grown in sandy soils under a plastic-mulched bed system. In addition to a no N fertilizer treatment, three urea N sources [one soluble source and two polymer-coated CRU sources with different N release durations of 60 (CRU-60) and 75 (CRU-75) days] were applied at three N rates (140, 168, and 224 kg⋅ha−1). Across all N sources and N rates, fall yields were at least 20% higher than spring seasons. At the 140 kg⋅ha−1 N rate, APR and NUE were improved, especially when U was applied in fall tomato, whereas preplant CRUs improved N efficiency in spring tomato. Based on the lower APR values found in spring production seasons (0% to 16%) when compared with fall (57.1% to 72.6%), it can be concluded that residual soil N was an important source for tomatoes. In addition, the mean whole-plant N accumulation of tomato was 102.5 kg⋅ha−1, further indicating that reducing the N rate closer to crop N demand would greatly improve conventional vegetable production systems on sandy soils in north Florida. In conclusion, polymer-coated CRU and fertigation U applications were able to supply the N requirement of spring and fall tomato at a 38% reduction of the recommended N rate for tomato in Florida (224 kg⋅ha−1). Preliminary results show that adoption of CRU fertilizers can be considered a low-risk alternative N source for tomato production and the ease of applying CRU once during the bed preparation period for tomato may be an additional incentive.

The impact of tightened prescribing restrictions for PBS-subsidised opioid medicines and the introduction of half-pack sizes, Australia, 2020-21: an interrupted time series analysis.

To evaluate the impact of the tightened Pharmaceutical Benefits Scheme (PBS) prescribing rules for immediate release (IR) and controlled release (CR) opioid medicines (1 June 2020), which also eliminated repeat dispensing without authorisation for codeine/paracetamol and tramadol IR and introduced half-pack size item codes for IR formulations. Population-based interrupted time series analysis of PBS dispensing data claims for a 10% sample of PBS-eligible residents and IQVIA national opioid medicine sales data (PBS-subsidised and private prescriptions), 28 May 2018 - 6 June 2021. Mean amount of PBS-subsidised opioid medicines dispensed per day and mean overall amount sold per day- each expressed as oral morphine equivalent milligrams (OME) - overall, by formulation type (IR, CR), and by specific formulation. During the twelve months following the PBS changes, daily PBS-subsidised opioid medicine dispensing was 81 565 OME lower (95% CI, -106 146 to -56 984 OME) than the mean daily level for 2018-20, a decline of 3.8% after adjusting for the pre-intervention trend; the relative reduction was greater for IR (8.4%) than CR formulations (2.6%). Total daily sales of all, IR formulation, and CR formulation opioid medicines did not change significantly after the PBS changes. Repeat dispensing of prescriptions comprised 7.4% of PBS-subsidised opioid dispensing before 1 June 2020, and 1.3% after the changes. Half-pack sizes comprised 8.4% of PBS-subsidised IR opioid medicine dispensing and 2.8% of all opioid medicines sold in the twelve months after the PBS changes. The introduction of new PBS rules for subsidised opioid medicines was followed by a decline in PBS-subsidised dispensing. Some people may have bypassed the new restrictions by switching to private prescriptions, but our findings suggest that opioid medicine use in Australia declined as a result of the new restrictions.

Advances in Periodontal Drug Delivery Systems and the Role of Probiotics in Periodontitis Treatment

Periodontitis is a group of inflammatory diseases which results the destruction of tooth-supporting tissues and affects 20-50% of the global population. Different bacterial enzymes are released into the periodontal pockets as a result of the proliferation of varied microflora, particularly anaerobes, which affect the body's immune response. A key component of treating periodontitis is mounting along with routing. Soluble at the site of infection, nonoperative controlled-release formulations reduce the requirement for systemic dosage by providing an affordable, non-toxic, biocompatible, and long-term therapeutic alternative. To successfully deliver a drug variety, several polymer-based systems can be used, i.e., strips, microparticles, fibers, nanoparticles, films, and nanofibers. This paper reviews the potential benefits and limits of using periodontal pockets as a medication delivery platform to create an appropriate dental localized dose form. The microorganisms called probiotics are present in the human body's alimentary canal and saliva. Recent studies on the usage of these organisms in treating periodontitis have substantially sparked the interest of researchers due to the positive metabolic effects of these organisms. Therefore, more study is needed to understand better how probiotics function physiologically and to manage periodontal disease over the long term.

Pimobendan controlled release guar gum printlets: Tailoring drug doses for personalised veterinary medicines

Treating chronic heart diseases in dogs is challenging due to variations in mass within and between species. Pimobendan (PBD), a veterinary drug only, is prescribed in specific cases of chronic heart disease in dogs and is available on the market in only a few different doses. Furthermore, the therapy itself is challenging due to the large size of the chewable tablets and the requirement for twice-daily administration. The development of customised and on-demand PBD medicines by three-dimensional (3D) printing has been proposed to circumvent these disadvantages. In this study, we designed controlled-release flavoured printlets containing PBD. We evaluated the use of two natural polymers, guar or xanthan gums, as the main component of the printing inks. Guar gum showed the better rheological behavior and printability by semisolid extrusion. The printlets were produced in three different shapes and sizes to allow dose customisation. Guar gum printlets showed a PBD controlled release profile, regardless of their shape or size. Therefore, we have demonstrated a novel approach for controlling PBD drug release and tailoring the dose by employing a natural polymer to produce 3D-printed tablets. This study represents a significant step towards the development of 3D-printed guar gum controlled-release formulations for veterinary applications.

Innovations and Future Trends in Storage Pest Management

Current innovations and future trends in storage pest management, with a specific focus on the Indian context. The critical role of effective pest management in agriculture and food security is underscored, considering its impact on economic stability and public health. It begins by detailing the challenges faced in storage pest management, including the variety of pests like insects and rodents, and the damage they inflict on stored agricultural products. It critiques the limitations of traditional pest management methods, particularly chemical control, and highlights emerging issues such as climate change effects and pesticide resistance. The core examines the latest innovations in storage pest management. Advanced chemical approaches like novel pesticides and controlled release formulations are discussed, alongside the rise of nanotechnology applications in pest control, including nano-pesticides and smart delivery systems. The emergence of biological control innovations, particularly new biocontrol agents, and genetic control strategies like the sterile insect technique, marks a significant shift towards more sustainable pest management methods. Additionally, It explores developments in physical and mechanical control methods, emphasizing improved storage facilities and environmental control techniques. Integrated Pest Management (IPM) approaches are identified as a key future trend, promoting holistic and sustainable strategies, with case studies underscoring their success and practical application. It also addresses the vital role of policy and regulatory developments, considering the impact of global regulations and the importance of international cooperation and standards in shaping pest management practices in India. Ethical and environmental considerations form a crucial part of the discourse, focusing on the ecological impact of pest management and the balance between control measures and conservation efforts. It concludes with an examination of practical applications and case studies, providing insights into real-world challenges and the strategies employed to overcome them. Overall, It offers a thorough analysis of the state-of-the-art in storage pest management, highlighting the intersection of innovation, sustainability, and practicality. It aims to provide valuable guidance for researchers, policymakers, and practitioners in the field, contributing to the advancement of more effective, environmentally responsible, and sustainable pest management strategies in India.

An emerging terpolymeric nanoparticle pore former as an internal recrystallization inhibitor of celecoxib in controlled release amorphous solid dispersion beads: Experimental studies and molecular dynamics analysis

Solid oral controlled release formulations feature numerous clinical advantages for drug candidates with adequate solubility and dissolution rate. However, most new chemical entities exhibit poor water solubility, and hence are exempt from such benefits. Although combining drug amorphization with controlled release formulation is promising to elevate drug solubility, like other supersaturating systems, the problem of drug recrystallization has yet to be resolved, particularly within the dosage form. Here, we explored the potential of an emerging, non-leachable terpolymer nanoparticle (TPN) pore former as an internal recrystallization inhibitor within controlled release amorphous solid dispersion (CRASD) beads comprising a poorly soluble drug (celecoxib) reservoir and insoluble polymer (ethylcellulose) membrane. Compared to conventional pore former, polyvinylpyrrolidone (PVP), TPN-containing membranes exhibited superior structural integrity, less crystal formation at the CRASD bead surface, and greater extent of celecoxib release. All-atom molecular dynamics analyses revealed that in the presence of TPN, intra-molecular bonding, crystal formation tendency, diffusion coefficient, and molecular flexibility of celecoxib were reduced, while intermolecular H-bonding was increased as compared to PVP. This work suggests that selection of a pore former that promotes prolonged molecular separation within a nanoporous controlled release membrane structure may serve as an effective strategy to enhance amorphicity preservation inside CRASD.

Immune Potentiation of PLGA Controlled-Release Vaccines for Improved Immunological Outcomes.

With the emergence of SARS-CoV-2 and the continued emergence of new infectious diseases, there is a need to improve and expand current vaccine technology. Controlled-release subunit vaccines provide several benefits over current vaccines on the market, including the use of less antigen and fewer boost doses. Previously, our group reported molecules that alter NF-κB signaling improved the vaccine's performance and improved adjuvant-related tolerability. In this report, we test how these immune potentiators will influence responses when included as part of a controlled-release poly(lactic-co-glycolic) vaccine formulation. Murine in vivo studies revealed that SN50 and honokiol improved antibody levels at early vaccine time points. Microparticles with SN50 produced strong antibody levels over a longer period compared to microparticles without SN50. The same particles also increased T-cell activity. All of the immune potentiators tested further promoted Th2 humoral responses already exhibited by the control CpG OVA microparticle formulation. Overall, under controlled-release conditions, immune potentiators enhance the existing effects of controlled-release formulations, making it a potentially beneficial additive for controlled-release vaccine formulations.

Studying the API Distribution of Controlled Release Formulations Produced via Continuous Twin-Screw Wet Granulation: Influence of Matrix Former, Filler and Process Parameters.

Hydroxypropyl methylcellulose (HPMC) is a preferred hydrophilic matrix former for controlled release formulations produced through continuous twin-screw wet granulation. However, a non-homogeneous API distribution over sieve fractions with underdosing in the fines fraction (<150 µm) was previously reported. This could result in content uniformity issues during downstream processing. Therefore, the current study investigated the root cause of the non-homogeneous theophylline distribution. The effect of process parameters (L/S-ratio and screw configuration) and formulation parameters (matrix former and filler type) on content uniformity was studied. Next, the influence of the formulation parameters on tableting and dissolution behavior was investigated. Altering the L/S-ratio or using a more aggressive screw configuration did not result in a homogeneous API distribution over the granule sieve fractions. Using microcrystalline cellulose (MCC) as filler improved the API distribution due to its similar behavior as HPMC. As excluding HPMC or including a hydrophobic matrix former (Kollidon SR) yielded granules with a homogeneous API distribution, HPMC was identified as the root cause of the non-homogeneous API distribution. This was linked to its fast hydration and swelling (irrespective of the HPMC grade) upon addition of the granulation liquid.

Unveiling the potential of microsponges: Enhancing oral bioavailability

Oral medication administration is widely recognized as the most practical and widely used method. Medications with a short half-life and easy absorption in the gastrointestinal tract are quickly removed by the bloodstream. To avoid these issues, oral controlled-release formulations have been created. There are a ton of novel formulation approaches in the realm of medication delivery systems. One new novel approach that is becoming increasingly well-liked these days is the usage of microsponges. A wide variety of active chemicals can be entrapped by the highly cross-linked, porous, polymeric structure that makes up the Microsponges Delivery System (MDS). Various polymers like ethyl cellulose, polystyrene, etc., have been utilized in forming microsponges and these active microsponges can be incorporated into formulations, such as capsules, gel, and powders, and have a broad package of benefits. The microsponges have satisfactory stability over pH values ranging from 1 to 11, they exhibit reasonable stability at temperatures as high as 130, and entrapment efficiency is great, reaching 50–60%. The preparation of microsponges involves the Quasi-emulsion solvent method, and the emulsion solvent diffusion method the release of drug through microsponges increases with increasing drug-polymer ratio and lowering polymer wall thickness. The microsponges are characterized for visual characterization, zeta potential, entrapment efficiency, and drug content. This review is focused on their advantages over other dosage forms, methods of preparation, characterization, and application of microsponges.

A Comprehensive Review on Floating Drug Delivery System

The category of gastroretentive drug delivery systems (GRDDS) includes floating drug delivery systems (FDDS). These dose formulations are intended to extend the duration of the stomach's residence period by a sustained release technique. Drugs which are harder to dissolve in high pH environments have improved bioavailability and solubility when incorporated into GRDDS. Reduced intestinal absorption of solid dose forms can be accomplished by the flotation mechanism. The novel fusion of bilayer and floating mechanism is demonstrated by the bilayer floating drug delivery device. It demonstrates the effective creation of a controlled release formulation. Bilayer floating tablets offer a sustained release layer formulation in addition to an immediate release. A attempt was made to explain the mechanism of FDDS, or floating bilayer, in the review. In order to accomplish regulated administration of various medications with predetermined release profiles, bi-layer tablets were developed. The pharmaceutical industry has been more interested in creating bilayer tablets over the past ten years as a way to improve patient compliance and convenience by combining two or more API in a single dose form.

Controlled release herbicide formulation for effective weed control efficacy

Controlled release formulation (CRF) of herbicide is an effective weed management technique with less eco-toxicity than other available commercial formulations. To maximise the effectiveness of CRFs however, it is crucial to understand the herbicide-releasing behaviour at play, which predominately depends on the interaction mechanisms between active ingredients and carrier materials during adsorption. In this study, we investigated and modelled the adsorption characteristics of model herbicide 2,4-D onto two organo-montmorillonites (octadecylamine- and aminopropyltriethoxysilane-modified) to synthesise polymer-based CRFs. Herbicide-releasing behaviour of the synthesised CRF microbeads was then analysed under various experimental conditions, and weed control efficacy determined under glasshouse conditions. Results revealed that adsorption of 2,4-D onto both organo-montmorillonites follows the pseudo-second-order kinetics model and is predominately controlled by the chemisorption process. However, multi-step mechanisms were detected in the adsorption on both organoclays, hence intra-particle diffusion is not the sole rate-limiting step for the adsorption process. Both organoclays followed the Elovich model, suggesting they have energetically heterogeneous surfaces. Herbicide-releasing behaviours of synthesised beads were investigated at various pH temperatures and ionic strengths under laboratory and glasshouse conditions. Furthermore, weed control efficacy of synthesised beads were investigated using pot studies under glasshouse condition. Desorption studies revealed that both synthesised microbeads have slow releasing behaviour at a wide range of pHs (5–9), temperatures (25–45 °C), and ionic strengths. The results also revealed that synthesised microbeads have excellent weed control efficacy on different broad-leaf weed species under glasshouse conditions.

Biopolymer Packaging Materials in the Pharmaceutical Industry

Biopolymer packaging materials are gaining prominence in the pharmaceutical industry due to environmental concerns. Derived from renewable sources, these biopolymers offer biodegradability, biocompatibility, and non-toxicity, making them ideal for various pharmaceutical applications. In drug delivery, biopolymers play a crucial role in controlled release formulations, especially for personalized medicines and biopharmaceutical products. Hydrogels, three-dimensional polymer networks, are key in mimicking living tissues and facilitating stimuli-responsive drug release with minimal toxic effects. The formulation strategies involve diffusion-controlled, degradation-controlled, or environmentally triggered release. Biodegradable systems, using polymers like poly(lactic acid) and poly(glycolic acid), contribute to sustainable drug delivery by undergoing controlled degradation. Osmotic delivery systems leverage osmotic pressure for controlled drug release, while stimuli-responsive designs respond to environmental changes. Biopolymer integration in pharmaceutical packaging aligns with eco-friendly practices, addressing challenges posed by traditional petroleum-based materials. This shift signifies a sustainable and innovative approach to pharmaceutical packaging in harmony with environmental preservation.

P534 The preference for controlled-release mesalazine formulation of 2 g-granule sachet in patients already experienced 1 g-tablet

Abstract Background The important factor is a good adherence in the treatment of inflammatory bowel disease (IBD) and the major guidelines recommend that the choice of formulation of mesalazine should consider patient preference and likely adherence. This study was to evaluate the preference for controlled-release (CR) mesalazine 2 g-granule sachet in patients who have been already experienced CR mesalazine 1 g-tablet and its related clinical factors. Methods First was treatment with 4 g CR mesalazine a day as two 2 g-granule sachets for 2 weeks in patients with IBD in remission who have already taken 4 g CR mesalazine a day as four 1 g-tablets for more than 3 months in Kosin University Gospel Hospital, Korea. The patients were consecutively enrolled. Second were the patients’ survey with 10 questionnaires about preferences (Table 1) after the 2 week-treatment and medical review of clinical information of patients. Results A total of 80 patients (46 in ulcerative colitis and 34 in Crohn’s disease, and 54 of male) were enrolled. Previous use of CR mesalazine four 1 g-tablets a day more than 1 year was in 88.6% of patients. In preference of formulation by ease to swallow, 70.0% of patients answered 2 g-granule sachet was better but just 20.0% of patients answered 1 g-tablet was better. In preference of formulation by next prescription, that is about overall preference, 63.8% of patients answered granule was better but 30.0% for tablet. In the number of 1 g-tablet or 2 g-granule sachet able to be swallowed at once, 46.9% of patients could swallow one or less tablet (1 g or less) and 96.1% of patients could swallow one or two sachets (2 g or more) (Fig. 1). When the patients who chose ‘granule was much better or better in overall preference' are classified as granule preference group and the remaining as others group. Number of tablet able to be swallowed at once in the medication before the granule trial was significantly less in granule preference group compared to others group (1.6 tablet vs. 2.0 tablet) (Fig. 2). However, the other factors including age, sex, body weight, height, body mass index, type of disease, concomitant oral medications, previous duration of 1 g-tablet use, were not associated with the overall preference. Conclusion In patients already experienced CR mesalazine 1 g-tablet for a long time, two-thirds of the patients more preferred to be prescribed 2 g-granule sachet and the preference was associated with the ability to swallow 1 g-tablets at once. Not only CR mesalazine 1 g-tablet but also 2 g-granule sachet can be an excellent choice for improving adherence of mesalazine treatment in IBD, especially when it comes to patients who can't take two or more 1 g-tablets at once.

Development of Ethylcellulose Microparticles for Taste Masking of Fexofenadine.

For taste masking of fexofenadine hydrochloride (FXD), ethylcellulose (EC) microparticles with FXD were developed. The amounts of EC, Tween 80, and polyvinyl alcohol (PVA) in the composition had little effect on initial drug release properties. Based on the results of the drug recovery and the drug release properties, FXD(EC200) was the optimal FXD microparticle formulation. From the results of Fourier transform infrared spectroscopy spectra and X-ray diffraction patterns of FXD(EC200), FXD amorphization in the microparticles and interaction between FXD and other components were suggested, and the formation of a solid dispersion of FXD was suggested. Because the possibility of the complex of PVA and FXD on the particle surface was suggested, sodium lauryl sulfate (SLS) was added to the composition. The initial drug release from FXD microparticles with SLS was further suppressed compared with FXD(EC200). From these results, FXD microparticles with SLS can be prepared as a controlled-release formulation and are expected to be useful for masking the bitter tasting particulates.