Pellet Formulation Research Articles

Utilization of Agricultural Waste as a Total Mixed Ratio Pellet Material for Rex Rabbit Feed

This study aimed to evaluate the quality of Total Mixed Ration (TMR) pellets derived from agricultural waste and assess their potential as feed for Rex rabbits. The research employed an experimental approach, utilizing agricultural and plantation waste to produce TMR pellets. The study was conducted in two stages: pellet production and rabbit feeding trials. Three formulations of TMR pellets were developed with varying concentrations of oil palm empty fruit bunches (EFB): P1 (5% EFB), P2 (10% EFB), and P3 (15% EFB). The optimal formulation was subsequently used for the feeding trials. Rabbit feed treatments included T0 (60% commercial pellet + 40% forage), T1 (40% commercial pellet + 20% TMR pellet + 40% forage), T2 (30% commercial pellet + 30% TMR pellet + 40% forage), and T3 (60% TMR pellet + 40% forage). Results from the pellet analysis indicated no significant differences in organoleptic properties among the formulations. The durability test yielded the highest value of 98.77%, while the proximate analysis of the P1 formulation showed a dry matter content of 85.67%, ash content of 10.35%, organic matter of 89.65%, crude protein of 18.65%, crude fat of 18.72%, and crude fiber of 19.18%. In the rabbit feeding trials, there were no significant differences in rabbit performance when compared to those fed with commercial pellets. Based on these findings, it can be concluded that agricultural waste can be effectively utilized as a raw material for rabbit feed pellets, offering comparable quality to commercial alternatives. This research highlights the potential of agricultural waste in reducing environmental pollution while providing an economically viable alternative for animal feed.

Bioavailability of a novel sustained-release pellet formulation of 5-flucytosine in healthy-fed participants for use in patients with cryptococcal meningitis.

Cryptococcal meningoencephalitis (CM) is an opportunistic fungal infection and a major cause of death among people living with human immunodeficiency virus in sub-Saharan Africa. 5-flucytosine (5-FC) is a unique, brain-permeable antifungal agent used to reduce mortality from CM and to prevent disease in individuals carrying cryptococcal antigen. 5-FC has a short plasma half-life, requiring 6-hourly oral dosing with an immediate-release (IR) formulation, a significant challenge in hospital and outpatient settings, risking a lack of compliance. We recently reported the relative bioavailability in fasting conditions of a sustained release (SR) oral pellet formulation of 5-FC. In this phase I study, we assessed the safety and pharmacokinetic profiles of the new 5-FC SR formulation in a single dose (2 × 3000 mg), relative to 5-FC IR tablets (Ancotil®; 1500 mg b.i.d.) in healthy participants in fed conditions. This randomized, two-period crossover study was conducted in South Africa to confirm the dose of the identified 5-FC SR formulation for a twice-daily 5-FC regimen in patients. Thirty-six healthy participants were included. All treatments were well tolerated and no serious adverse event was reported. Cmax and AUC(0-t) for the SR formulation (49.2 ± 10.49 μg/mL and 640.4 ± 126.4 h.μg/mL, respectively) were significantly higher than for the IR formulation (36.8 ± 7.61 μg/mL and 456.6 ± 72.8 h.μg/mL, respectively). A physiological based pharmacokinetic model (PBPK) predicted that under fasting conditions, 6000 mg SR pellets would show a good overlap with the IR product (3000 mg b.i.d), thus 6000 mg SR 5-FC b.i.d. in fasting conditions is recommended.

Formulation and in-vitro anticancer activity of nilotinib immediate release and ibrutinib sustained release pellets

Background: Blood cancer is a significant contributor to mortality rates worldwide, and its prevalence is projected to rise on a global scale. This trend places considerable strain on healthcare systems and necessitates the expedited development of innovative treatments by pharmaceutical firms to remain competitive. Conventional pellets produce rapid plasma drug levels, but they might cause side effects, decrease effectiveness, and lead to poor therapeutic management. Ibrutinib and Nilotinib are employed to treat leukemia patients. Methodology: The current research aims to formulate, characterize, and anticancer effect of Nilotinib immediate release (NIR) and Ibrutinib sustained release (ISR) seal sugar-coated pellets. Micrometric properties estimated the characterization of the drug pellets, and surface morphology was estimated using scanning electron microscopy. Drug excipient compatibility studies, stability studies, and in-vitro drug release were accessed. Result & Discussion: The results of pellet formulations FNI-1 to FNI-5 showed that FNI-5 formulations showed 100±6.0 µm size and possessed excellent mechanical strength for giving pellets a good self-life; also, due to the higher drug content up to 99%, FNI-5 was the best suited for pellet formulation and because NIR showed 99.18 ± 2.12 drug release at 2h and ISR 99.03±3.74% up to 12h so that anticancer concentration maintained for prolonged period. The standard dose for cytotoxicity against the THP-1 cell line of Nilotinib was found to be 200 mg, and the maintenance oral dose of Ibrutinib was 140mg, with four times the intake of the drug up to 560 mg. In an in vitro study in FNI-5 (final formulation), the dose of Ibrutinib was reduced to 420 mg. Conclusion: A synergistic effect of Ibrutinib and nilotinib drugs was observed in the inhibition of cancer cell growth, with an IC50 value of 4.585 µg/mL

Micronutrient Dynamics in Soil under Integrated Thermochemical Organic Fertilizer Pellet Application

A soil incubation study was carried out in the Department of Soil Science and Agricultural Chemistry, to assess dynamics of micronutrient release. Soil pots were filled with 5 kg air-dried, 2 mm sieved soil. The study was laid in Completely Randomized Design with 5 treatments and 4 replications. Treatments were, T1: Pellet formulation 1; T2: Pellet formulation 2; T3: Pellet formulation 3; T4: FYM+NPK (RDF as per POP) and T5: Control (Soil alone). The Fe, Mn, Zn, Cu and B content of soil were 10.14 mg kg-1, 8.59 mg kg-1, 1.90 mg kg-1, 2.50 mg kg-1 and 0.30 mg kg-1, respectively. Three distinct pellet formulations P1, P2 & P3 were used in study based on thermochemical organic fertilizer (TOF). Fe, Mn and Zn exhibited a gradual and progressive release pattern throughout the incubation period. Whereas Cu and B availability showed a decreasing trend from the 15th day onwards. Highest Fe, Mn and Zn availability were observed towards the end of the incubation study. While the Cu and B recorded highest on the initial 15th day of incubation. Hence it can conclude that TOF based pellets significantly impact the micronutrient availability in soil compared to the FYM based and control treatment.

Preparation and evaluation of lipid-based sustained release pellets of chlorpheniramine maleate by the wet extrusion-spheronization method

Introduction: This study aimed to investigate the feasibility of preparation of sustained-release chlorpheniramine maleate (CPM) pellets based on Compritol® as a lipid matrix and evaluation of the affecting factors on pellet properties. Methods: Using the D-optimal experimental design, different pellet formulations containing various amounts of CPM, Compritol® and Avicel were prepared by the wet extrusion-spheronization method. Then the pellets were cured at 40, 65 and 90 ̊C for 4 and 8 h to study the effect of the thermal process. The physicomechanical properties of the pellets were investigated in terms of particle size distribution, pelletization yield, mechanical strength, aspect ratio and sphericity. To investigate the possible interaction of CPM and Compritol®, as well as to evaluate the morphology and surface characteristics of the pellets DSC and SEM were used, respectively. Also, to investigate the drug release rate from pellets the dissolution test was carried out and mean dissolution time (MDT) was calculated to compare different formulations. Results: The results showed that the curing process up to 65 °C improves the strength of the pellets. However, increasing the curing temperature from 65 to 90 °C and also increasing the curing time from 4 to 8 h did not have a significant effect on the strength of the pellets but increased the drug release rate of pellets. Increasing the amount of the drug or decreasing Compritol® in the matrix of pellets leads to a larger particle size with greater mechanical strength. All formulations of the pellets had an aspect ratio and sphericity of about 1.1 and 0.9 respectively, which indicates the spherical shape of the pellets as shown by SEM. DSC thermograms indicate the reduction of the crystallinity or the change of the crystalline form of the drug to amorphous during the pelletization process. Conclusion: The results revealed the feasibility of preparing lipid-based sustained-release matrix pellets using the wet extrusion-spheronization method. The optimal formulation in terms of physicomechanical properties and release rate was the formulation containing 8% CPM, 67% Compritol® and 25% Avicel, which were dried at 40 ° C for 4 h and released about 90% of the drug within 12 h.

Assessing seed pellet formulations to improve native plant restoration under water‐limited conditions

Water scarcity, a challenge expected to worsen with climate change, significantly hinders native plant community restoration. Enhancing seed‐based restoration requires methods to increase the water availability for seeds and seedlings. Surfactants and superabsorbent polymers (SAPs) can improve soil water‐holding capacity and infiltration, but their use in seed enhancements remains underexplored. We investigated whether pellets containing surfactants or SAPs could improve seedling emergence of two native species (Rytidosperma caespitosum and Chrysocephalum apiculatum) common in temperate grasslands in south‐eastern Australia under different watering treatments. We used a randomized block design with five watering treatments to simulate predicted changes in precipitation for south‐eastern Australia: ambient, two reducing overall water volume, and two reducing watering frequency while increasing watering volume to maintain ambient treatment water volume. We explored four enhanced pellets (two containing surfactants and two containing SAPs) and non‐pelleted seeds. Our results showed that watering events with larger volumes but reduced frequency increased seedling emergence. Under these conditions, block co‐polymer surfactants further increased seedling emergence of C. apiculatum, while synthetic SAP pellets promoted emergence of R. caespitosum. Block co‐polymer surfactants decreased R. caespitosum emergence, and both SAPs reduced C. apiculatum emergence under reduced watering frequency. A 50% reduction in overall water volume significantly reduced seedling emergence for both species, regardless of seed enhancement. These findings suggest that surfactants and SAP pellets can improve the success of seed‐based restoration under ambient conditions and when rainfall events are larger in volume but reduced in frequency, but not when the overall volume of rainfall is reduced.

Preparation and Evaluation of Berberine-Excipient Complexes in Enhancing the Dissolution Rate of Berberine Incorporated into Pellet Formulations

Berberine is used in the treatment of metabolic syndrome and its low solubility and very poor oral bioavailability of berberine was one of the primary hurdles for its market approval. This study aimed to improve the solubility and bioavailability of berberine by preparing pellet formulations containing drug-excipient complex (obtained by solid dispersion). Berberine-excipient solid dispersion complexes were obtained with different ratios by the solvent evaporation method. The maximum saturation solubility test was performed as a key factor for choosing the optimal complex for the drug-excipient. The properties of these complexes were investigated by FTIR, DSC, XRD and dissolution tests. The obtained pellets were evaluated and compared in terms of pelletization efficiency, particle size, mechanical strength, sphericity and drug release profile in simulated media of gastric and intestine. Solid-state analysis showed complex formation between the drug and excipients used in solid dispersion. The optimal berberine-phospholipid complex showed a 2-fold increase and the optimal berberine-gelucire and berberine-citric acid complexes showed more than a 3-fold increase in the solubility of berberine compared to pure berberine powder. The evaluation of pellets from each of the optimal complexes showed that the rate and amount of drug released from all pellet formulations in the simulated gastric medium were significantly lower than in the intestine medium. The results of this study showed that the use of berberine-citric acid or berberine-gelucire complex could be considered a promising technique to increase the saturation solubility and improve the release characteristics of berberine from the pellet formulation.Graphical

Preparation and evaluation of lipid-based sustained release pellets of chlorpheniramine maleate by the wet extrusion-spheronization method

Background: This study aimed to investigate the feasibility of preparation of sustained-release chlorpheniramine maleate (CPM) pellets based on Compritol® as a lipid matrix and evaluation of the affecting factors on pellet properties. Method: Using the D-optimal experimental design, different pellet formulations containing various amounts of CPM, Compritol® and Avicel were prepared by the wet extrusion-spheronization method. Then the pellets were cured at 40, 65 and 90 ̊C for 4 and 8 h to study the effect of the thermal process. The physicomechanical properties of the pellets were investigated in terms of particle size distribution, pelletization yield, mechanical strength, aspect ratio and sphericity. To investigate the possible interaction of CPM and Compritol®, as well as to evaluate the morphology and surface characteristics of the pellets DSC and SEM were used, respectively. Also, to investigate the drug release rate from pellets the dissolution test was carried out and mean dissolution time (MDT) was calculated to compare different formulations. Results: The results showed that the curing process up to 65 °C improves the strength of the pellets. However, increasing the curing temperature from 65 to 90 °C and also increasing the curing time from 4 to 8 h did not have a significant effect on the strength of the pellets but increased the drug release rate of pellets. Increasing the amount of the drug or decreasing Compritol® in the matrix of pellets leads to a larger particle size with greater mechanical strength. All formulations of the pellets had an aspect ratio and sphericity of about 1.1 and 0.9 respectively, which indicates the spherical shape of the pellets as shown by SEM. DSC thermograms indicate the reduction of the crystallinity or the change of the crystalline form of the drug to amorphous during the pelletization process. Conclusion: The results revealed the feasibility of preparing lipid-based sustained-release matrix pellets using the wet extrusion-spheronization method. The optimal formulation in terms of physicomechanical properties and release rate was the formulation containing 8% CPM, 67% Compritol® and 25% Avicel, which were dried at 40 ° C for 4h and released about 90% of the drug within 12 h.

Calcium-carbonate and phytoelements to improve egg production in backyard laying hens under heat stress

Calcium-carbonate and phytoelements to improve egg production in backyard laying hens under heat stress

A mono-layer matrix for pelleting marigold (Tagetes erecta) seeds

Marigold growers in Thailand face challenges in the cultivation from seeds of marigold owing to the elongated, slender and sometimes fragile shape of the seeds. These characteristics often result in a high number of seedlings with abnormal traits, making them susceptible to diseases and insects. The objective of this study was to develop a pellet formulation for marigold seeds to increase their size and facilitate cultivation from seeds. Seven pellet matrices, including a commercial product (pre-pelleted seeds), were assessed for integrity, including friability, dissolution period germination, shoot length, and root length under both laboratory and greenhouse conditions. Methylhydroxyethyl cellulose (MHEC) was used as the binding agent for each pellet matrix. Seeds pelleted with MHEC-bentonite and MHEC-zeolite resulted in irregularly shaped pellets, whereas the other matrices appeared smoother and more similar to commercially-pelleted seeds. CaCO3 and talc-pelleted seeds had a high friability, whereas CaSO4 -, pumice- and bentonite-pelleted seeds had friability values similar to those of the commercially- pelleted seeds. CaSO4 -pelleted seeds exhibited germination rates that were the closest to those of non-pelleted and commercially-pelleted seeds under both laboratory and greenhouse conditions. In conclusion, the MHEC- CaSO4 matrix is the most suitable choice for pelleting marigold seeds.

Extruded seed pelleting offers an alternative direct seeding option to rehabilitate forested ecosystems impacted by a soil‐borne plant pathogen

SummaryThe high cost of native seeds and low seedling establishment percentages after seed broadcasting are major constraints for seed‐based rehabilitation. This study examines whether extruded seed pelleting can be used as a tool to distribute seeds more effectively (e.g. distribute small seeds in a precise manner) while maintaining or enhancing seedling emergence and establishment of Australian shrub species used in the rehabilitation of Phytophthora cinnamomi infested Jarrah (Eucalyptus marginata) forest sites. Pellet formulation was first tested using five different formulations of dry ingredients and the addition of seeds from four Phytophthora‐resistant species under glasshouse conditions. The best performing formulation from this work was then adopted to compare laboratory‐produced and field‐deployed pellets. Seedling emergence of the larger seeded species, Raspberry Jam Wattle (Acacia acuminata) and Pin‐cushion Hakea (Hakea laurina), was highest using field‐deployed pellets and emergence was statistically similar to the non‐pelleted seeds. Seedling emergence reached 100% for the small seeded species, Silky‐leaved Bold Flower (Calothamnus sanguineus) and Melaleuca seriata, from laboratory‐produced pellets and was significantly higher than non‐pelleted seeds. These results indicate that extruded pelleting offers an alternative direct seeding option that can result in greater or equal seedling emergence than that observed with non‐pelleted seeds, yet the responses are species‐specific. These species‐specific pelleting techniques must now be tested under field conditions to confirm whether pellet production method and delivery improve seedling establishment under field conditions.

Development and Characterization of Pectin-Based Colon Targeted Pellets Containing Lactobacillus Plantarum FNCC-0461

Lactobacillus plantarum FNCC-0461 is a lactic acid bacteria isolated from "dadih" a traditional Indonesian food that has potential as a probiotic. Probiotics can show health benefits if they can maintain cell viability of at least 7 log CFU in the distal ileum and colon. However, most probiotics are not resistant to the extreme conditions of the gastrointestinal tract. Probiotic encapsulation in the form of pectin-based colon targeted pellets is a promising delivery system to overcome probiotic viability problems due to the gastrointestinal tract extreme conditions and can assist release to specific target site in colon. Pellets was produced by extrusion-spheronization method using microcrystalline cellulose (MCC), lactose and pectin. Optimization of spheronization process was carried out by varying the spheronization speed and time while the optimization of pellets formula was carried out by varying the concentration of total pectin and the type of coating polymer (cellulose acetate phthalate (CAP) or shellac). The morphology, particle size, moisture content, micromeritic properties, process yield and viability of pellets were evaluated. Release of probiotics on coated and uncoated pellets were examined at pH 1.2, 6.8 and 7.4 under simulated colon fluid for 24 hours. The formula containing MCC, lactose and pectin (5:4:1) with spheronization speed at 1500 rpm for 15 minutes showed the best pellets characteristic and cell viability. The pellets obtained were spherical, with particle size distribution of 913.57±8.28 μm, process yield of 88.71±1.04 % and viability of 7.50 x 107 cfu/g. Pellets coated with CAP showed the highest cell release in simulated colon fluid of 1.38 x 107 CFU/g at 24 hours. This research proved that CAP coated pellet formulation has promising potential for colon targeted delivery of L. plantarum as well as to protect the viability of probiotics for colon-targeted delivery.

Design and Development of Immediate Release Pellets Formulation Containing Co Amorphous Mixture of Aceclofenac: In-Vitro and In-Vivo Study

Design and Development of Immediate Release Pellets Formulation Containing Co Amorphous Mixture of Aceclofenac: In-Vitro and In-Vivo Study

Feed preference in lactating dairy cows for different pellet formulations

Two taste preference experiments were conducted with the same 8 multiparous lactating Jersey cattle (100 ± 7.1 DIM, 30.5 ± 4 0.06 kg of milk yield, 18.8 ± 2.52 kg of DMI in experiment 1; and 215 ± 7.1 DIM, 27.6 ± 3.98 kg of milk yield, 19.6 ± 3.03 kg of DMI in experiment 2). In experiment 1, 4 pellets were formulated and manufactured into 4.0-mm pellets. These were as follows: 45.7% alfalfa meal, 45.7% corn grain, and 8.57% wheat middlings (ALFC); 72.3% corn grain, 18.5% wheat middlings, and 9.25% dried distillers grains and solubles (ENG); a pellet containing 100% dehydrated alfalfa meal (DALF); and a pellet containing a mixture of concentrate ingredients (GMIX; 43.1% corn grain, 26.3% dried distillers grains and solubles, 13.8% wheat middlings, 7.10% dry molasses, 3.18% soybean meal, 0.93% corn oil, and 5.6% minor constituents). Cows were offered 0.50 kg of pellets in a randomized arrangement within the feed bunk. Feed preference was ranked from 1 to 4 with 1 being the most preferred and 4 the least. The resulting preference rankings were averaged (± SE) resulting in a highest (closest to 1) to lowest (furthest from 1) ranking as follows of ALFC (1.38 ± 0.164), ENG (2.13 ± 0.327), GMIX (2.88 ± 0.375), and DALF (3.13 ± 0.350). The probabilities of first choice were 70.6 ± 0.55% ALFC, 16.5 ± 0.46% ENG, 5.50 ± 0.475% DALF, and 7.48 ± 0.455% GMIX. A Z-test was conducted to determine the percentage a treatment would be chosen first differed from the value of no preference at 25%; ALFC and DALF differed from the mean value, whereas no difference was observed for ENG and GMIX. The most preferred pellet (ALFC) was used in a second study and compared against 3 other treatments in which different flavoring agents were added. In this study, 4 pellets were manufactured with ALFC: 45.7% alfalfa meal, 45.7% corn grain, 6.76% wheat middlings, and 1.81% oregano leaf (ALFCO); 45.7% alfalfa meal, 45.7% corn grain, 8.22% wheat middlings, 0.10% melon flavoring, and 0.25% BitterOff (ALFCM); and 45.7% alfalfa meal, 45.7% corn grain, 8.47% wheat middlings, and 0.10% licorice flavoring (ALFCL). The resulting preference rankings were averaged resulting in a highest to lowest ranking as follows: ALFC (1.25 ± 0.164), ALFCO (2.38 ± 0.263), ALFCM (2.63 ± 0.375), and ALFCL (3.25 ± 0.164). The probabilities of first choice were 81.9 ± 0.65% ALFC, 8.49 ± 0.46% ALFCO, 6.50 ± 0.481% ALFCM, and 3.12 ± 0.491% ALFCL. Of the pellet choices, ALFC and ALFCL differed from the mean value of no choice, whereas no difference was observed for ALFCO and ALFCM. Mixtures of corn grain and dehydrated alfalfa meal bound by wheat middlings may serve as a feeding strategy that is preferred by the animals and may be an effective reward to cows entering an automated milk system, and we were unable to improve preference by adding flavoring agents.

Population Pharmacokinetics of Pediatric Lopinavir/Ritonavir Oral Pellets in Children Living with HIV in Africa.

Antiretroviral therapy for children living with HIV (CLHIV) under 3 years of age commonly includes lopinavir/ritonavir (LPV/r). However, the original liquid LPV/r formulation has taste and cold storage difficulties. To address these challenges, LPV/r oral pellets have been developed. These pellets can be mixed with milk or food for administration and do not require refrigeration. We developed the population pharmacokinetic (PK) model and assessed drug exposure of LPV/r oral pellets administered twice daily to CLHIV per World Health Organization (WHO) weight bands. The PK analysis included Kenyan and Ugandan children participating in the LIVING studies (NCT02346487) receiving LPV/r pellets (40/10 mg) and ABC/3TC (60/30 mg) dispersible tablets. Population PK models were developed for lopinavir (LPV) and ritonavir (RTV) to evaluate the impact of RTV on the oral clearance (CL/F) of LPV. The data obtained from the study were analyzed using nonlinear mixed-effects modeling approach. Data from 514 children, comprising a total of 2,998 plasma concentrations of LPV/r were included in the analysis. The LPV and RTV concentrations were accurately represented by a one-compartment model with first-order absorption (incorporating a lag-time) and elimination. Body weight influenced LPV and RTV PK parameters. The impact of RTV concentrations on the CL/F of LPV was characterized using a maximum effect model. Simulation-predicted target LPV exposures were achieved in children with this pellet formulation across the WHO weight bands. The LPV/r pellets dosed in accordance with WHO weight bands provide adequate LPV exposures in Kenyan and Ugandan children weighing 3.0 to 24.9 kg.

The effects of feeding liquid or pelleted formulations of Asparagopsis armata to lactating dairy cows on methane production, dry matter intake, milk production and milk composition

Asparagopsis armata has been reported to have strong antimethanogenic effects when fed to dairy cows. The aim of this study was to evaluate the effect of a liquid and a pelleted formulation of A. armata when fed to lactating dairy cows as a supplemental feed twice daily at milking on i) enteric methane emissions, milk yield and dry matter intake (DMI), and ii) presence of halogenated compounds in milk, urine, faeces, and blood. Forty lactating, multiparous, Holstein-Friesian cows (117 ± 20.2 days in milk) were randomly allocated one of four treatments; 1) CON1: basal diet plus liquid supplement without A. armata, 2) AA1: basal diet plus liquid supplement with A. armata, 3) CON2: basal diet plus pellet supplement without A. armata, and 4) AA2: basal diet plus pellet supplement with A. armata. The liquid and pelleted supplements were offered twice daily for 34 days. Supplements were offered with a grain mix during each milking. The basal diet consisted of vetch hay ad libitum and 6.15 kg dry matter (DM)/d of a grain mix fed as 3.07 kg DM in the dairy per milking. Cows given the AA1 treatment received 298 mg bromoform per day while cows on the AA2 treatment received 293 mg bromoform per day. Individual forage DMI were measured daily via electronic monitoring of individual cows at the feed bins. Methane emissions were measured using the modified sulphur hexafluoride tracer technique on the last 5 days of the experiment. Feeding the A. armata formulations showed no effect on total DMI, forage DMI, concentrate DMI or milk yield. Methane production (g CH4/d), methane yield (g CH4/kg DMI) and methane intensity (g CH4/kg energy corrected milk) were reduced by about 20 % for both the liquid and the pelleted A. armata formulations. Feeding the A. armata formulations led to increased bromoform concentrations in milk (∼2.0 µg/L) but were well below the limit for safe consumption (100 µg/L). It is concluded that both formulations were effective in reducing enteric methane emissions and that milk from cows fed these A. armata formulations is safe for human consumption.

FORMULATION AND BIOPHARMACEUTICAL EVALUATION OF SUSTAINED RELEASE PELLETS OF BOSENTAN BY PANCOATING METHOD

Objective: The aim of the present study was to formulate sustained-release pellets of bosentan by eudragit RL 100 and RS 100, which are the polymers used in the pan coating technique. Methods: The sustained release pellets of bosentan were formulated by pan coating method. The drug was coated on nonpareil seeds along with EudragitRL100 by solution layering technique. Drug-loaded pellets were coated with EudragitRS100. The prepared pellets were evaluated for moisture content, drug content, particle size, and in vitro drug release. Stability studies were carried out on the optimised formulations for a period of 6 mo. Results: The drug content was in the range of 98.89±0.32. The mean particle size of the drug-loaded pellets was in the range of 835 μm. The drug release rate decreased as the concentration of eudragit increased in the pellet formulations. Among the prepared formulations, PC 4 showed 89.35±0.52 drug release in 12 h from a good linear relationship was established between model-independent approaches (T25%, T50%, and T100%) and weight gain in coating. This indicated the possibility of extending the drug release by increasing the weight gain in the coating, and hence, it was proposed to extend the drug release for 24 h. From the prepared pellets, the optimised formulation PC 12 showed a 100.02±0.03 drug release in 24 h. Furthermore, these pellets were filled into capsules and compared the dissolution studies. The compatibility between drugs and polymers in the drug-loaded pellets was confirmed by DSC and FTIR studies. Stability studies indicated that the pellets were stable. Conclusion: The prepared pellets were capable of releasing the drug for 24 h to treat the Pulmonary Arterial Hypertension.

Formulation, optimization and evaluation of pellets loaded glipizide co amorphous mixture using central composite design to enhance solubility

Formulation, optimization and evaluation of pellets loaded glipizide co amorphous mixture using central composite design to enhance solubility

Design, Synthesis, Evaluation, and Molecular Docking Study of Ascorbic Acid Dual-Coated Omeprazole Pellets and the Antioxidative Effect of Ascorbic Acid on Omeprazole-Induced Renal Injury in an Animal Model.

The present study was carried out to investigate the antioxidant effect of ascorbic acid on omeprazole (O.P.)-induced acute kidney infection (AKI). Design of experiment (DoE) was employed to fabricate formulations (P1-P8) by the extrusion spheronization technique, and they were evaluated using various analytical techniques. P1-P8 formulations have % drug loading ranging from 56.34 ± 1.10 to 98.67 ± 1.05%, encapsulation efficiency from 70.98 ± 0.96 to 98.67 ± 1.05%, percentage drug release varying from 36.56 ± 1.34 to 93.45 ± 1.45%, Hausner's ratio ranging from 1.026 ± 0.05 to 1.065 ± 0.02%, and Carr's index varying from 2.3 ± 0.07 to 6.1 ± 0.06 g/mL. The optimized formulation (P6) was dual-coated with Eudragit L-100 (5% w/v) and ascorbic acid (2% w/v). A smooth uniform morphology was found after coating, and particle size nonsignificantly changed from 85.31 ± 77.43 to 101.99 ± 65.56 μm. IR spectra showed omeprazole characteristic peaks confirming drug loading, and peaks at 1747.40 and 1611.51 cm-1 confirmed ascorbic acid and Eudragit L-100 coating. X-ray diffraction (XRD) analysis confirmed the crystalline nature, and thermal degradation studies until 500 °C demonstrated increased stability after coating. Cytotoxicity analysis with 97% cell viability revealed the nontoxic behavior of pellets. In vitro dissolution studies of coated pellets showed <20% drug release at pH 1.2 and 99.54% at pH 6.8. Animal studies showed that pure omeprazole showed a nonsignificant decrease in weight, urine output, and fecal output compared to rodents on ascorbic acid pellets. Increased uric acid and creatinine levels in the group on pure omeprazole indicated AKI. Histopathological studies of renal cells also supported these results. The integration of experimental pellet formulation with molecular docking simulations has unveiled the potential of ascorbic acid and omeprazole as highly promising therapeutic agents for addressing oxidative stress and inflammation.

IADVL SIG Recalcitrant Dermatophytosis Position Statement on Super Bioavailable Itraconazole.

Itraconazole (ITZ) has been the mainstay of oral antifungal treatment for the current epidemic of recalcitrant dermatophytosis (RD) in India. Recently, a newer formulation of ITZ, super bioavailable itraconazole (SUBA-ITZ), is made available in the market by many pharmaceutical companies. It is important for dermatologists to understand the pharmacokinetic properties of SUBA-ITZ vis-a-vis conventional pellet formulation to use it effectively and safely. Indian Association of Dermatologists, Venereologists and Leprologists (IADVL) has established a special interest group for recalcitrant dermatophytosis (SIG-RD) to strengthen research, continuing medical education, and industry collaboration on the subject. This position statement on SUBA-ITZ by SIG-RD is an attempt to address current pieces of evidence and the position of this new formulation in the management of RD.