Pellet Formulation Research Articles

CHARACTERISTICS AND SUBSTANTIATION OF THE USE OF PELLETS AS A MODERN DOSAGE FORM ON THE MARKET OF UKRAINE

currently, omeprazole pellets are one of the most common pellet formulations on the pharmaceutical market of Ukraine (Gorobets, Matyash, Pekhenko & Barna, 2019). This medication is available in capsule form. Pellets are multi particular dosage forms that have several advantages over monoparticular dosage forms; therefore, pellets are promising oral delivery systems for active pharmaceutical ingredients (APIs). Pellets are used when the stability of the active substance changes with fluctuations in the pH of the environment, when irritation of the gastric mucosa is possible, to facilitate swallowing (especially important for patients with dysphagia, elderly patients, and children). When using polymers in the shell, it is possible to regulate the release in a certain part of the gastrointestinal tract, this allows you to get a point pharmacological effect. In addition, pellets can be of different sizes (from 0.1 to 2 mm), because of their shape, pellets exhibit abrasion resistance and are more fluid. Omeprazole is a synthetic substance. The active ingredient suppresses gastric acid secretion. In refers to the pharmaceutical group of proton pump inhibitors, it prescribes drugs in this group to treat active duodenal ulcers, gastric ulcers, gastro-oesophageal reflux disease (GERD), severe erosive esophagitis, pathological hypersecretory conditions, for example, Zollinger Ellison syndrome. Among the most commonly used methods for the production of pellets are: stage-by-stage spraying of solutions or suspensions (the second name is stage-by-stage layering); direct pelletization (the second name is extrusion-spheronization); spray drying and spray cooling of melts; agglomeration-spheronization. Unfortunately, at the moment, none of the Ukrainian manufacturers is manufactured enteric pellets on their own (they buy ready-made pellets), while there are medicines of both foreign and Ukrainian origin on the domestic market. The article contains an overview of pharmaceutical preparations as pellets, systematization of information on production methods, a review of omeprazole drugs as pellets, presented on the pharmaceutical market of Ukraine. The purpose of this study was to summarize the cases when the use of such a form as pellets is the most reasonable; make an overview of medicines in Ukraine containing pellets; summarize modern methods of pellet production.

Formulation and In Vitro Evaluation of Pellets Containing Sulfasalazine and Caffeine to Verify Ileo-Colonic Drug Delivery.

The ColoPulse coating is a pH-dependent coating that can be used to target drug release to the ileo-colonic region. ColoPulse coated tablets and capsules have demonstrated their targeting capabilities in vivo in more than 100 volunteers and patients. However, so far the ColoPulse coating has not been used for multi-particulate pellet formulations. The sulfasalazine–caffeine method can be used to confirm ileo-colonic drug delivery in vivo. Caffeine serves as a release marker in this method, while sulfasalazine serves as a marker for colonic arrival. In this study, extrusion–spheronization was used to produce microcrystalline cellulose based pellets containing both caffeine and sulfasalazine. Dissolution tests revealed that a superdisintegrant, i.e., croscarmellose sodium or sodium starch glycolate, should be incorporated in the formulation to achieve acceptable release profiles for both sulfasalazine and caffeine. However, acceptable release profiles were only obtained when the pelletizing liquid consisted of ethanol/water 1/1 (v/v) but not with pure water. This phenomenon was ascribed to the differences in the degree of swelling of the superdisintegrant in the pelletizing liquid during the granulation process. The pellets were coated with the ColoPulse coating and showed the desired pH-dependent pulsatile release profile in vitro. In future clinical studies, ileo-colonic targeting should be verified.

Development and Characterization of Eudragit-RL-100-Based Aceclofenac Sustained-Release Matrix Pellets Prepared via Extrusion/Spheronization.

Aceclofenac (AC) is a nonsteroidal anti-inflammatory drug used in the treatment of chronic pain in conditions such as rheumatoid arthritis, with frequent administration during the day. The formulation of sustained release matrix pellets can provide a promising alternative dosage form that controls the release of the drug, with less blood fluctuation and side effects—especially those related to the gastric system. The extrusion/spheronization technique was used to formulate AC matrix pellets. The response surface methodology (version 17.2.02.; Statgraphics Centurion) was used to study the impacts of Eudragit RL 100 and PVP K90 binder solution concentrations on the pellets’ wet mass peak torque, pellet size, and the release of the drug. Statistically, a significant synergistic effect of PVP K90 concentration on the peak torque and pellet size was observed (p = 0.0156 and 0.031, respectively), while Eudragit RL 100 showed significant antagonistic effects (p = 0.042 and 0.013, respectively). The peak torque decreased from 0.513 ± 0.022 to 0.41 ± 0.021 when increasing the Eudragit RL 100 from 0 to 20%, and the pellet size decreased from 0.914 ± 0.047 to 0.789 ± 0.074 nm. The tested independent factors did not significantly affect the drug release in the acidic medium within 2 h, but these pellet formulae maintained the drug release at less than 10% in the acidic medium (pH 1.2), which may decrease gastric irritation side effects. In contrast, a highly significant synergistic effect of Eudragit and highly antagonistic effect of the PVP solution on drug release in the alkaline-pH medium were observed (p = 0.002 and 0.007, respectively). The optimized pellet formula derived from the statistical program, composed of 3.21% Eudragit and 5% PVP solution, showed peak torque of 0.861 ± 0.056 Nm and pellet size of 1090 ± 85 µm, and resulted in a significant retardation effect on the release after 8 h compared to the untreated drug.

Development and Formulation of Baicalin-loaded Self-nanoemulsifying Matrix Pellets

Development and Formulation of Baicalin-loaded Self-nanoemulsifying Matrix Pellets

FORMULATION, DEVELOPMENT AND OPTIMISATION OF PH. DEPENDENT DRUG DELIVERY SYSTEM CONTAINING PROTON PUMP INHIBITOR

The present study was involving the targeting the Rabeprazole formulation at site specificity. Peptic ulcer mostly occurs in the lower part of the gastrointestinal tract. Proton pump inhibitors category drugs mainly used to cure peptic ulcer. As most of proton pump inhibitors degrades in acidic condition in stomach, the present study mainly focus on targeting site specificity without degradation of drug in stomach. Rabeprazole and selected excipients was tested for reformulation study as well as for analytical techniques like Ultra Violet Visible Spectroscopy, Fourier Transform Infrared Spectroscopy and Differential Scanning Calorimetry. Core pellet formulation of Rabeprazole was formulated using extruder and spheroniser. After core pellet preformulation seal coating of pellet was completed. As seal coating mainly helps the core pellet from interaction between another coating polymer. Seal coating was completed by using Opadry coat. At the top of the pellet polymer coat was applied. Polymer coat was helps to deliver the formulation in appropriate pH only. Polymer coat also protects the formulation from degradation in stomach where acidic condition presents. Evaluation parameters like dissolution test, Ultra Violet Visible Spectroscopy, Fourier Transform Infrared Spectroscopy and Differential Scanning Calorimetry, optimisation parameter applied to optimised formulation. Stability study was performed on optimised formulation.

A systematic approach for assessing the suitability of enteral feeding tubes for the administration of controlled-release pellet formulations

Enteral nutrition plays an important role for patients who are unable to properly swallow food. In such patients, enteral feeding tubes are often used, through which food, but often also oral medications, are administered. However, this can pose the risk of tube clogging. Compared to the administration of crushed tablets, multiparticulate dosage forms are often considered easier to administer and furthermore have the advantage of enabling the administration of even controlled-release preparations. The objective of this systematic study was to identify tube- and formulation-related factors that contribute to successful administration of coated pellet formulations via a variety of commercially available feeding tube devices. The suitability of enteral feeding tubes for the administration of controlled-release pellet formulations that differed in size and type of starter core and functional coating was investigated in a stepwise approach using a novel in vitro setup. Results of the study indicate that pellet diameter and inner diameter of the feeding tube are by no means reliable parameters for estimating the tube’s suitability for pellet administration, but that many other tube and formulation-related factors and combinations thereof must be considered to ensure safe and effective drug administration via enteral feeding tubes.

Co-pelletization of pine sawdust and refused derived fuel (RDF) to high-quality waste-derived pellets

Energy generation from non-hazardous waste streams, which are unfeasible to be reused or recycled, can help overcome some of the problems related to fossil fuel depletion, global increase in energy demand and waste generation management under restricted landfilling. One of the main drawbacks of waste-to-energy strategies is the poor combustion properties of waste, which densification could help to circumvent. This work studies the co-pelletization of refused derived fuel (RDF) and pine sawdust (PIN) in a continuous pilot pellet mill that resembles industrial pelletization. The effect of RDF contents up to 90 wt% on a set of parameters has been assessed: pelletization energy consumption, physical properties (durability, particle and bulk densities), net calorific value and energy density of the obtained pellets. In addition, slagging, fouling and corrosion, phenomena associated with combustion, were estimated from the ash composition. Results showed that obtaining pellets with a low RDF loading (2–9 wt%) was feasible. They accomplished ISO 17225-2 solid biofuels standard for industrial use, and presented low deposition and corrosion risks. On the other hand, pellets with 30–90 wt% RDF were also manufactured and complied with the UNE-EN 15359:2012 solid recovered-fuel standard for energy recovery in incineration and co-incineration plants. All the produced pellets presented durability and net calorific value above 96.9% and 10.7 MJ/kg, respectively. Energy density higher than 10.6 GJ/m3 was obtained for pellet formulations with RDF content up to 50 wt%. It was demonstrated that the blends of RDF and PIN can provide high-quality pellets with a high load of waste material, under the same operational conditions required for PIN pelletization. It is a versatile process that can be tailored to different product requirements depending on the end-use. It promotes energy recovery and generates value out of a waste fraction with no relevant use, adding economic and environmental benefits.

Development and characterization of multiparticulate system as an alternative to unit dosage forms containing drugs with diverse release profiles

BackgroundCurrently, the Bilayer tablets, Tablet in tablet and Inlay tablets composed of Glimepiride (GMP) and Pioglitazone (PGH) as immediate release part, and Metformin (MFH) as sustained-release part are available for the treatment of type II diabetes mellitus (T2DM). In these products, there is a possibility of the incomplete release of immediate release part (GMP and PGH) due to their entrapment into high viscosity gel barrier of MFH sustained-release part when drug product comes in contact with media. Therefore, the present study was aimed to deliver the above combination drugs in the form of hard gelatin capsules (as unit dosage form) containing MFH sustained-release (MFH-SR) pellets and immediate release pellets of PGH and GMP (PG-IR).ResultsThe MFH-SR and GP-IR pellets, prepared by extrusion and spheronization technique, were optimized based on the drug content and % cumulative drug release. The MFH-SR pellets formulation (batch A6) has shown maximum drug content, and sustained-release of MFH similar to marketed glucophage tablet while, the GP-IR pellets formulation (batch B5) has displayed maximum drug contents and immediate release of GMP and PGH; thus, these batches were considered for further characterizations. The optimized MFH-SR and GP-IR formulations have shown particle sizes of 0.23 ± 0.0010 mm and 0.35 ± 0.0018 mm, respectively. Besides, the formulations exhibited good micromeritics properties. The in vivo pharmacokinetic study in rabbits has demonstrated comparable bioavailability of the drugs from pellets and the marketed formulations following oral administration. Further, the pellets were found to be stable for 6 months at 40 ± 2 °C/75% ± 5%RH.ConclusionsThe study results revealed that the multiparticulate systems with varied release profiles could be a promising approach to overcome drug release issues associated with the unit dosage forms.

Formulation Development and Evaluation of Multiple Unit Pellet System of Tamsulosin Hydrochloride

The aim of current work was to grow extended release multiple unit pellets of Tamsulosin Hydrochloride, is an alpha-blocker, used for the healing of the symptoms of a prostate gland condition called BPH (benign prostatic hyperplasia) by extrusion- spheronization (E/S) and solution/suspension layering (S/S) method. In the Extrusion-Spheronization, A ratio of 75:25, 67:33, 64:36 Tamsulosin Hydrochloride and Microcrystalline cellulose were mixed for making drug pellets and extended release (ER) coating was performed in fluidized bed processor (FBP) by solution/suspension layering with Ethyl cellulose (aqueous. dispersion, 4 cps and 7 cps) and Hypromellose (5cps) with different ratios % weight buildups accordingly. In the Solution/suspension layering (S/S) method, Tamsulosin Hydrochloride drug pellets were prepared by layering onto MCC spheres in FBP. These drug pellets were further coated for extended release with HPMC, 5cps and EC, 7cps. In drug coating stage, drug and different binder (Hypromellose, 5 cps) concentrations 8, 10, 12, 14 mg/unit were coated onto the cores for optimization of binder concentration. The weight of MCC spheres were optimized for further formulations. For all the drug coated pellets, ER coating was given with EC, 7cps and HPMC, 5 cps at a coating level of 8% weight by weight. In the extrusion- spheronization (E/S) Optimization of Drug pellets: Among the trials TD3 (Tamsulosin HCl and MCC) showed good mechanical strength with better yield due to increased MCC concentration. Optimization of Extended Release Coating: Optimized TD3 drug pellets were coated with ER coating using water insoluble polymer (Aq.EC 25% dispersion/ EC, 4cps/ EC, 7cps) and water soluble polymer (HPMC, 5cps). Among these polymers, extended release coating was optimized (TD3E14) with the combination of EC, 7cps and HPMC, 5cps at 8% weight build up. In the Solution/Suspension layering: Optimization of binder concentration in drug coating stage: HPMC, 5cps with 12 mg/unit for TF7 was optimized based on %yield. Optimization of MCC spheres in drug coating stage in formulation of ER pellets with different weight drug pellets: The weight of MCC spheres (160, 170, 180, 190 mg/unit) used in the drug coating stage with binder HPMC, 5cps (12 mg/unit). These drug pellets were given with ER coating at 8% weight buildup by using EC, 7cps and HPMC, 5cps. Among these trials, TF7E7 was optimized. Based on the investigations of the present study, conclusions was. formulating low dose, high soluble, BCS class I drug- Tamsulosin Hydrochloride ER formulation by extrusion-spheronization showed flexibility for batch processing and cost effectiveness while solution/suspension layering was process feasible but time consuming due to high drug loading.

Design of Experiment Approach to Assess the Effect of Formulation Variables on Extrusion and Spheronization of Telmisartan and Cilostazol Loaded Pellets and its Pharmacokinetic Study

Background: Solubility is an important parameter that affects the availability of drug in systemic circulation. Drugs having poor solubility belonging to BCS class II eventually result in lower dissolution and bioavailability. Hence, improvement of solubility is a challenging task. Hence the present work focuses on using solid dispersion and inclusion complex approach for both telmisartan and cilostazol belonging to BCS Class II drugs. Objective: The present study was carried out to improve apparent solubility of telmisartan and cilostazol (BCS-Class II drugs) and optimization as pellets along with its pharmacokinetic study. Methods: Phase solubility study was carried out to screen the excipients such as, PVPK30, PVA, HPMC E5 and β-CD. Solvent evaporation method was adopted to prepare the solid dispersions and inclusion complex of both drugs. Pellets were optimized by extrusion spheronization method using 32 factorial design and characterized by morphology, drug content, DSC, FTIR, XRD, SEM, in- -vitro studies and drug content study. Results: Phase solubility study showed improved apparent solubility of telmisartan with HPMC E5 (1:3) by solid dispersion and cilostazol with β-CD (1:3) using inclusion complexation method. Drug characterization did not reveal any incompatibility. Formulation was optimized on the basis of acceptable pellet properties, including acceptable spherical shape and micromeritics properties. The percent friability of all batches was found to be less than 1%. The optimized pellets of both drugs prepared with micro crystalline cellulose provided desirable maximum release with acceptable release profile. Conclusion: The formulated pellets when studied in vivo showed superior pharmacokinetic profile. The drawback associated with apparent solubility and bioavailability of both drugs can thus be alleviated by use of novel pellet formulation.

Design, development and QbD based optimization of double coated spheronized aceclofenac pellets for effective palliative care in rheumatoid arthritis

ObjectiveDesign, develop, optimize and validate a chronotherapeutic double coated aceclofenac pellet formulation prepared using extrusion-spheronization technique for effective palliative action of RA symptoms. SignificanceRA is a chronic systemic autoimmune disease leading to pain in joints, connective/fibrous tissues, cartilages, ligaments, muscles and tendons. RA mostly prevails at productive age of human life and its chronic effect may lead to deformity or disability thereby resulting in substantial socioeconomic burden. Early morning circadian manifestations of symptoms in RA are due to night time activation of inflammatory responses. Chronotherapeutic double coated pellet formulation can deliver aceclofenac according to circadian rhythm of RA symptoms leading to effective palliative action. MethodsCore aceclofenac pellets were prepared and double coated with inner swellable HPMC and outer erodible ethylcellulose layers to achieve desired lag time in ACE release. Formulation and process parameters of double coating process were optimized by QbD approach. Drug release lag time, production yield and pellet morphology were identified as CQAs. ResultsIn vitro drug release and in vivo pharmacokinetic studies revealed that optimized pellet formulation with 15% weight gain due to swellable layer, 1.6% weight gain due to erodible layer and 5% of pore forming agent exhibited highest desirability indices with drug release lag time of 5h, production yield of 79 ± 2%, 1.05 ± 0.04 aspect ratio, 88.1% ± 1.25% roundness and.1.22 ± 0.2 mm pellet size. ConclusionDesired ACE release lag time required to match the circadian rhythm of RA was achieved through double coated spheronized pellets, without any associated drawback of dose dumping.

Steam and supercritical water gasification of densified canola meal fuel pellets

In this research, canola meal was densified using bio-additives including alkali lignin, glycerol, and l-proline. The fuel pellet's formulation was optimized. The best fuel pellet demonstrated relaxed density and mechanical durability of 1015 kg/m3 and 99.0%, respectively. Synchrotron-based computer tomography technique indicated that lack of water in pellet formulation resulted in a twofold increase in pellet porosity. Thermogravimetric analysis showed that ignition temperature (240 °C) and burn-out temperature (640 °C) for fuel pellet were smaller than those for coal. Impacts of process parameters were evaluated on the quality of the gas product obtained from pellet's steam gasification and hydrothermal gasification. The gasification experiments showed production of untreated syngas with a suitable range of H2/CO molar ratio (1.3–1.6) using steam gasification. Hydro-thermal gasification produced a larger molar ratio of H2/CO (1.8–51.2) for the gas product. Modeling of pellet's steam gasification showed an excellent agreement with experimental results of steam gasification.

Formulation and Evaluation of Sustained Release Floating Pellets of Amlodipine Besylate

The aim of the present study is to design and develop sustained release pellets formulations for Amlodipine besylate. Amlodipine is an oral antihypertensive agent, commonly used as calcium channel blocker for treating high blood pressure. It is frequently used to treat heart diseases like angina pectoris. The dose of Amlodipine in case of hypertension or angina initially 5 mg daily later adjusted to 10 mg daily by oral route. Amlodipine has a maximum solubility in acidic pH. Amlodipine has a high bioavailability ranging from 60 to 80 % and slow rate of elimination. Amlodipine besylate at different drug to polymer ratios were prepared by extrusion and spheronization technique. The influence of the proportion of the polymer on the release rate of the drug from the pellets was studied. The in-vitro release studies of pellets were carried out in 0.1N HCl for 12 hours. The studies indicated that the drug release can be modulated by varying the concentration of the polymer. Pellets were prepared and evaluated for loose bulk density, tapped bulk density, compressibility index and angle of repose, shows satisfactory results. Formulation was optimized on the basis of acceptable pellet properties and in-vitro drug release. The resulting formulation produced robust pellets with acceptable drug content and low friability. The release data was fitted to various mathematical models such as, Higuchi, Korsmeyer- Peppas, First-order and Zero-order to evaluate the kinetics and mechanism of the drug release. Keywords: Sustained release, Ethyl cellulose, HPMC, Pellets, Amlodipine besylate

New glyoxalated pre-gelatinized starch as release retardant for extended release pellets containing zaltoprofen: statistical optimization, in-vitro and in-vivo evaluation

The aim of the present investigation is to develop zaltoprofen-loaded extended-release (ER) pellets formulation by an extrusion-spheronization technique using glyoxalated pre-gelatinized starch (GPS) complex as a novel matrix-forming polymer. The prime objective was to prepare an efficient and robust ER drug delivery system of zaltoprofen. Pellets were characterized by physicochemical, morphological, and solid-state characterization. The formulation was also analyzed for in-vitro drug release and in-vivo pharmacokinetic parameters. The FTIR analysis confirmed the GPS complex formation through the formation of the hemiacetal group while the ketone groups of glyoxal are abolished. Optimized formulation G5 containing 5:8 ratio of GPS complex and MCC showed 99.03 ± 2.12 percent cumulative drug releases in 14 h. The in-vivo study showed decreased C max and increased t 1/2 compared to bulk zaltoprofen, and hence would be a viable alternative for ER-type formulations. In the author’s opinion, the GPS-based ER pellet formulation would be an excellent delivery system for zaltoprofen.

Solvent influence on manufacturability, phase behavior and morphology of amorphous solid dispersions prepared via bead coating

Bead coating or fluid-bed coating serves as an auspicious solvent-based amorphous solid dispersion (ASD) manufacturing technique in respect of minimization of potential physical stability issues. However, the impact of solvent selection on the bead coating process and its resulting pellet formulation is, to the best of our knowledge, never investigated before. This study therefore aims to investigate the influence of the solvent on the bead coating process itself (i.e. manufacturability) and on solid-state characteristics of the resulting ASDs coated onto beads. For this purpose, the drug-polymer system felodipine (FEL)-poly(vinylpyrrolidone-co-vinyl acetate) (PVP-VA) was coated onto microcrystalline cellulose (MCC) beads from acetonitrile (ACN), methanol (MeOH), ethanol (EtOH), acetone (Ac), 2-propanol (PrOH), dichloromethane (DCM) and ethyl acetate (EthAc). A drug loading screening approach with bead coating revealed analogous ability to manufacture high drug-loaded ASDs from the different organic solvents. The results show no correlation with crystallization tendency or with equilibrium solubility of the drug in the different solvents, nor with the solvent-dependent drug-polymer miscibility obtained from film casting experiments. Distinct coating morphologies were however observed for PVP-VA and FEL-PVP-VA ASDs deposited onto beads from the various solvents, which is attributed to differences in solvent evaporation kinetics.

FORMULATION AND EVALUATION OF BUDESONIDE PELLETS CONTAINING NATURAL GUMS FOR COLON TARGETING

Pellets formulation with natural gums. The formulation of an enzyme as well as pH dependant pellets containing natural gums such as Mornings oleifera gum Lam. (MOG) and Cyamopsis tetragonolobus gum Taub. (CTG) were used for enzyme dependant release and further coating is provided to shows colon-specific delivery. Extrusion and spheronization techniques were used for the preparation of pellets. Pellets of budesonide evaluated for various properties such as flow behavior, physical properties such as sphericity, roundness, aspect ratio, hardness, and friability also investigated in vitro and in vivo targeting in rabbit. Preparation of pellets was done by using extrusion and spheronization method with the use of optimized concentration of gums those were 7.5% and 10% for CTG and MOG respectively and proportion of solvent mixture of water and Isopropyl alcohol in the ratio of 80:20. Pellets of budesonide evaluated for various properties includes flow behavior, physical properties such as sphericity, roundness, aspect ratio, hardness, and friability and found that all properties as per official limit also in vitro release study found that release of uncoated pellets in a sustained manner in 0.1N HCl for 2h due to swelling of natural gum, therefore further step of the coating was done in fluidized bed coater to prevent the release of drug in the upper part of GIT and after coating found that In vitro release of drug at the colonic environment and it confirmed with in vivo investigation in rabbit with X-ray examination of targeting and found that pellets reach at colonic part without disintegration. The use of natural gums for preparation of pellets in optimized concentration and wetting agent produce a formulation with all required chemical and physical properties and it gives effective in vitro release and also shows In vivo targeting in rabbit and due to use of natural gum for preparation of pellets also reduce some problems of metabolism of synthetic excipients.

Inclusion of Spirulina in Floating Fish Feed Production: Protein and Physical Quality

The objective of this study was to investigate effects of Spirulina meal (SM) inclusion in fish feed formulations on their physical and protein content. Four formulations of fish feed were carried out i.e. a control diet with fishmeal (FM) as the single protein source and three others formulations containing Spirulina meal (SM) ingredient in different ratios of FM: SM (w/w) namely 75:25; 50:50 and 25:75 (w/w). All the formulations were processed into pellets using an extruder with a 600 rpm screw speed, 100 °C barrel temperature, and 3 mm diameter of dies. The dried pellets were then evaluated with respect to the protein content and physical properties i.e. expansion ratio, unit density, floatability and hardness. In general, the most optimum pellet formulation was found at the ratio of 25:75 (FM: SM) ingredients resulted in pellet with higher protein (38.89%) and expand ratio (1.65 fold), the lowest unit density (0.473 mg/mm3), the highest floatability (100%) and less hardness (32.53 N). Therefore, formulation of floating fish feed included with Spirulina are an option for improving its protein content and physical properties.

Formulation and Evaluation of Pellets of natural Okra gum prepared by Extrusion and Spheronization

The aim of the current study was to explore the possibility of preparing pellets of okra gum using extrusion and spheronization technique. Different formulations were prepared by altering the concentration of okra gum. Metronidazole was chosen as a model drug. The pellets were smooth and spherical in shape. FTIR and DSC spectra’s confirmed that there was no interaction between drug and polymer. The pellets were free-flowing and exhibited satisfactory flow characteristics along with good mechanical strength. Okra gum was able to control the drug release and around 90% drug was released in 8hrs. Pellets showed increase in swelling as the concentration of gum was increased. Mucoadhesion study exhibited that the prepared pellets had good mucoadhesive strength.

Development of Gelucire® 48/16 and TPGS Mixed Micelles and Its Pellet Formulation by Extrusion Spheronization Technique for Dissolution Rate Enhancement of Curcumin.

The oral bioavailability of curcumin is limited, attributed to its low solubility or dissolution and poor absorption. Herein, the study describes formulation of curcumin-loaded mixed micelles of Gelucire® 48/16 and TPGS for its dissolution rate enhancement. Curcumin was dispersed in these molten lipidic surfactants which was then adsorbed on carrier and formulated as pellets by extrusion spheronization. Critical micelle concentration (CMC) of binary mixture of Gelucire® 48/16 and TPGS was lower than their individual CMC demonstrating the synergistic behavior of mixture. Thermodynamic parameters like partition coefficient and Gibbs free energy of solubilization indicated that mixed micelles were more efficient than micelles of its individual components in curcumin solubilization. Dynamic light scattering (DLS) suggested slight increase in micellar size of mixed micelles than its components suggesting curcumin loading in mixed micelles. Fourier transform infrared spectroscopy (FTIR) revealed that phenolic hydroxyl group interacts with lipids which contribute to its enhanced solubility. Furthermore, the differential scanning calorimetry (DSC) and X-ray diffraction (XRD) study indicated the conversion of crystalline curcumin into amorphous form. In the pellet formulation, Gelucire® 48/16 acted as a binder and eliminated the requirement of additional binder. Microcrystalline cellulose (MCC) forms wet mass and retards the release of curcumin from pellets. Increase in concentration of water-soluble diluent increased drug release. The optimized formulation released more than 90% drug and maintains supersaturation level of curcumin for 2 h. Thus, mixed micellar system was effective delivery system for curcumin while pellet formulation is an interesting formulation strategy consisting semi-solid lipids.

Preparation and Characterization of Novel Self Nano Emulsifying Drug Delivery System of Allopurinol

The aim of research was to develop self nanoemulsifying drug delivery technology containing low aqueous soluble drug allopurinol for improving solubility, dissolution and bioavaibility. Preliminary screening were carried on the basis of maximum solubility of allopurinol in oil, surfactant, co-surfactant and pseudo-ternary phase diagram was constructed to identify the ratio of surfactant and co-surfactant for nanoemulsion formulation using water titration method. Based on the solubility study, Labrafil M 1944 CS, Cremophor RH 40, Transcutol used as oil, surfactant, and co-surfactant respectively. Pseudo-ternary phase diagram was constructed to identify the ratio of surfactant and co-surfactant for nanoemulsion formation by water titration method. As per the ternary phase diagram ratio of Smix in 2:1 was identified with maximum emulsification area. SNEDDS composed of 35 % Labrafil M 1944 CS, 43.34% Cremophor RH 40, 21.66% Transcutol. Globule size was found to be 25.42 nm, and zeta potential value was -9.26 mV. Prepared SNEDDS were evaluated for globule size, viscosity, emulsification time, cloud point, dilution test and thermodynamic stability study. Prepared liquid SNEDDS then converted into solid SNEDDS via extrusion/spheronization technique using Aerosil 200, lactose monohydrate and Croscarmellose sodium. The pellets containing SNEDDS possessed good flow properties and mechanical strength and other rheological parameters. Self nanoemulsifying pellet exhibited uniform size and shape. Friability, dissolution time and disintegration of pellets formulation shown promising results. Time required for 80% drug release of self nanoemulsifying pellet was found to be 26 min, which was significantly lower than liquid SNEDDS, plain drug containing pellet and marketed preparation of Allopurinol (ZYRIK).