dissolution dilution fusion

17 Jan dissolution dilution fusion

As a rule of thumb, higher MDT values indicate slower drug release, and reverse is true for the MDR values. Yuksel N, Kanık AE, Baykara T. Comparison of in vitro dissolution profiles by ANOVA-based, model-dependent and independent methods. Sa va grave m'aider dans mon contrôle :D Arigato!!!!!!! J Pharm Sci. Dumortier G, Grossiord JL, Agnely F, Chaumeil JC. The authors declare that they have no competing interests. From the curves, it was also seen that the crystalline peak for ibuprofen diminished with the increasing polymer content. Introduction. Samples were stirred using a magnetic stirrer at 26 ± 0.5°C for 48 h. After completion, aliquots of samples were centrifuged, filtered, and analyzed spectrophotometrically as described above for saturation solubility studies. Dilution d’une solution Le but de cette opération est de préparer à partir d’une solution mère S 0 (concentration C 0) une nouvelle solution fille S 1 moins concentrée (concentration C 1). Heating rate of 5°C/min from 20 to 120°C and a modulation of ±1.59°C every 60 s was used. Castro SG, Sanchez Bruni SF, Urbizu LP, Confalonieri A, Ceballos L, Lanusse CE, et al. Factors affecting the formation of eutectic solid dispersions and their dissolution behavior. Utilization of hydrophilic gums for the control of drug release from tablet formulations I. Disintegration and dissolution behavior. Il y a dilution de l’avoir des actionnaires lorsqu’une entreprise émet de nouvelles actions aux investisseurs et lorsque les détenteurs d’options d’achat d’actions exercent leur droit d’acheter des actions. Samples were stirred using a magnetic stirrer at a temperature of 26 ± 0.5°C for 48 h and were done in triplicate. Average melting temperatures and change in enthalpy values (ΔHmelt) were evaluated from the thermograms. Pluronic® block copolymers as novel polymer therapeutics for drug and gene delivery. Newa M, Bhandari KH, Li DX, Kwon T-H, Kim JA, Yoo BK, et al. Figure 7a shows the thermograms of drug, polymer, and the PMs while Fig. Tao Q, Chen J-M, Ma L, Lu T-B. La chimie organique, c'est quoi au juste ? Quel volume de solution mère faut-il utiliser€? Figure 9 shows an overlay of FTIR spectra of all samples. Int J Pharm. La dilution est un procédé utilisé pour diminuer la concentration d’une solution en y ajoutant du solvant sans changer la quantité de soluté. ... de fusion - 101 ° C Solubilité dans l’eau 7,3 g / L . Pharm Dev Technol. Volume variation among test samples for different batches was minimized using the split vessel assembly. Estimation of drug–polymer miscibility and solubility in amorphous solid dispersions using experimentally determined interaction parameters. SE is the energy required for the upward clockwise motion of blade in an unconfined low stress environment. En cycle III je souhaiterais que les enfants fassent la différence entre fondre et dissoudre pour que plus tard dans l'année la notion de dissolution soit réutilisée dans les phénomènes de digestion et de respiration. * La dilution au niveau microscopique * Dissolution du sel Distinction entre dissolution, dilution et fusion * Miscibilité des liquides : eau, huile, alcool * Dissolution et masse * Description de la matière * La dissolution du sel par l'eau en vidéo Lorsqu'on mélange un soluté et un solvant, les molécules de soluté se déplacent jusqu'à ce qu'elles soient réparties de manière uniforme dans l'eau. Its average particle size was 1000 μm. La dissolution d'un composé dans l'eau est l'intégration chimique de ce composé dans l'eau tel qu'il en résulte un mélange homogène. Typically, 0.5% Lithium Bromide. CAS  Rutesh H. Dave. 1 values give an idea of approximate value of percent error between dissolution profiles with a value of 0–15 indicating no difference and dissimilarity increasing proportionately with the value. Post-hoc tests were done to compare each sample among themselves individually. Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188. Wath is the difference between dilution, dissolution and fusion ? S0 value was found to be 47.93 μg/ml. Where, n is the number of sample points, i is the sample number, ti is the midpoint time between two samples, ΔMi is additional amount of drug released between ti and ti-1, and Δt is also the time at midpoint. In water, it was a 5-fold increase, and in phosphate buffer, it was mere 1.15-fold. Physical presence of polymer in the PMs also had a similar effect, but it was marginally less than the corresponding FMs. https://doi.org/10.1208/s12249-016-0482-6, DOI: https://doi.org/10.1208/s12249-016-0482-6, Over 10 million scientific documents at your fingertips, Not logged in CAS  2002;82(2):189–212. Serajuddin A. PMs were prepared at 1:1, 1:1.5, 1:2, 1:2.5, 1:3, and 1:3.5 w/w ratios of drug and polymer corresponding to 50, 40, 33, 28.57, 25, and 22.22% w/w ibuprofen, respectively. Chemically, it consists of 101 parts of ethylene oxide units (70% w/w) and 56 parts (30% w/w) of propylene oxide units (21). EXERCICES: Réaliser des mélanges peut provoquer des transformations de la matière (dissolution… Animation : Solidification de l'eau pure. Effect of relative humidity on acetaminophen tablet properties prepared by different techniques using polyvinylpyrrolidine derivatives as binder. The time of blending was optimized after preliminary testing. Badawy SIF, Menning MM, Gorko MA, Gilbert DL. In all samples, the characteristic crystalline peaks of ibuprofen were seen although the intensities were lower than the drug. Fusion et dissolution Bonjour. Drug Dev Ind Pharm. In acidic media, almost 58% cumulative drug release for FM 1:0.75 was encountered whereas for drug, it was only 3.67% after 60 min. 20 février 2010 Urbán-Morlán Z, Castro-Ríos R, Chávez-Montes A, Melgoza-Contreras LM, Piñón-Segundo E, Ganem-Quintanar A, et al. 1997;190(2):307–12. Hildebrand-Scott theory of real solutions for liquid solvents and Flory-Huggins model to calculate enthalpy of mixing of drugs in polymer suggests that drugs and polymer mix in a three-step process, and each step is associated with its change in Gibb’s energy which in turn depends on the change in enthalpy and entropy of the process. Un peu plus loin, on peut lire aussi : (B) « chauffer du sucre dans une casserole jusqu'à ce qu'il se caramélise. Linear equation obtained from standard curve was used in the subsequent studies. Modeling and comparison of dissolution profiles. It is a white, coarse prilled powder having waxy consistency with a melting point of 70°C and an average molecular weight of 12,600 g/mol (20). Masse molaire : 70,9 g / mol Masse Volumique : 3,00 kg / m3 Poloxamers are a group of non-ionic block-copolymers consisting of polyethylene oxide (PEO) and polypropylene oxide (PPO) units (-PEO-PPO-PEO-). Enhanced dissolution and systemic availability of albendazole formulated as solid dispersions. Eur J Pharm Biopharm. Figure 6a, b, c shows the in vitro dissolution profiles in de-ionized water, 0.1 N HCl (pH = 1.2) and phosphate buffer (pH = 7.2), respectively. Int J Pharm. Scope of the current study was to prepare and evaluate the potential of Poloxamer 407 (Lutrol® F127 NF Prill) in improving the solubility and dissolution rate of model BCS class II drug ibuprofen. All PMs and FMs showed characteristic crystalline peaks of ibuprofen, but their intensities were lower and that can be due to the dilution effect. Mise en solution d'un solide, d'un liquide ou d'un gaz ; état de ce qui est dissous ; liquide résultant de cette mise en solution. Samples were analyzed using a scanning diffractrometer (Model XI Cupertino, Advanced Diffraction System, Scintag Inc., CA, USA). 2006;23(12):2709–28. J Control Release. J Pharm Sci. The Carr’s indices (24.42 to 17.60), Angle of repose (32.34 to 27.64), and Hausner ratio (1.324 to 1.210) values decreased with the increase in polymer content which were consistent with rheometer results. The enthalpy of solution, enthalpy of dissolution, or heat of solution is the enthalpy change associated with the dissolution of a substance in a solvent at constant pressure resulting in infinite dilution.. Thermal analysis was performed on all the samples using a Q100 (TA instruments, New Castle, DE) instrument with nitrogen (50 ml/min) as a purge gas. 7b shows with the FMs. The characteristic peak seen in the mDSC curves which was lower than the individual melting temperatures of the drug as well as polymer indicated formation of a eutectic for the given ratios (9). FDA recommends f Model independent (time-point and pair-wise approach) and ANOVA based approaches were used to validate the significance of the observed difference in the dissolution profiles for different formulations. Fluid Phase Equilib. En effet, les deux ne correspondent-ils Systemic bioavailability of poorly soluble drugs mainly belonging to the Biopharmaceutics Classification System (BCS) class II category has been a major challenge for the pharmaceutical industry. For saturation solubility studies, excess amount of drug, PMs and FMs of all ratios were placed in beakers containing 40 ml of de-ionized water, 0.1 N HCl (pH = 1.2) and phosphate buffer (pH = 7.2). Melting point of drug and polymer was found to be 76.79 and 57.69°C, respectively. 1998;55(1):45–55. A review of poloxamer 407 pharmaceutical and pharmacological characteristics. Enough releasing agent is used to be sure the transfer is complete. From the pair-wise analysis, the statistical non-equivalence of the dissolution profiles of formulations when compared to the drug was evident. A method to predict the equilibrium solubility of drugs in solid polymers near room temperature using thermal analysis. 1999;88(10):1058–66. J Pharm Biomed Anal. The apparent stability constant value was found to be 21.95 mM−1. Int J Pharm. le faire passer de l'état solide à l'état liquide. A forty-eight-millimeter stainless steel blade and 50 mm × 160 ml glass vessel was used for testing (n = 3). Int J Pharm. In the pair-wise analysis, f 2013;111:24–9. 2001;13(2):123–33. Eur J Pharm Sci. J Pharm Sci. Standard curve was prepared at the pre-determined λmax using concentrations of 20, 40, 100, 200, 400, 800, and 1000 μg/ml in ethanol, and the test was performed in triplicates. Phase diagram was constructed using the enthalpies of eutectic peaks (ΔH) against the different % w/w ratios of ibuprofen including 1:0.5 w/w ratio (66% w/w ibuprofen). Binary mixtures of ibuprofen and poloxamer were prepared in three different ratios (1:0.25, 1:0.5, and 1:0.75, respectively) using a water-jacketed high shear mixer. There are different grades of Poloxamer available, and they differ in the chain length of PEO and PPO units. Saturation solubility for the drug itself in pH 7.2 was around 4600 μg/ml whereas in pH 1.2, it was 23 μg/ml. AAPS PharmSciTech Guyot M, Fawaz F, Bildet J, Bonini F, Lagueny A-M. Physicochemical characterization and dissolution of norfloxacin/cyclodextrin inclusion compounds and PEG solid dispersions. The characteristic eutectic endotherm with a melting temperature of around 50°C was observed for all PMs as seen in Fig. 2 values of 50–100 ensure dissolution data equivalence with a value of 100 indicating complete similarity and values below 50 suggesting non-equivalence (42). Désoler mais le solide introduit dans le liquide n'a pas "disparu" mais il s'est dissout. La dissolution est un procédé qui consiste à mettre un soluté dans un solvant dans le but de préparer une solution constituée d’une seule phase (mélange homogène). The fused samples are automatically poured into the Teflon beakers containing the dilute acid solution when working in ICP mode. La dissolution est une réaction chimique. Une société régie par la Loi sur les sociétés par actionspeut être dissoute du consentement de ses actionnaires ou du seul consentement de ses administrateurs, ou encore par une déclaration de dissolution faite par l'actionnaire unique de la société. Goud NR, Suresh K, Sanphui P, Nangia A. Mixing was carried out at 200 RPM (Impeller speed) and 950 RPM (Chopper speed) until fusion was completed. CAS  2012;38(8):930–9. There was not much difference in regard to densities (bulk) for the different formulations. All formulations had uniform distribution of drug in each sample. Filter-binding studies on same standard solutions of drug revealed that there was no substantial binding to the filters being used which can be seen by the graph (post-filtration) in Fig. volume 17, pages1428–1440(2016)Cite this article. Pharm Dev Technol. - Q1: Quand le sel est dissous, a-t-il la même masse que quand il ne l'est pas ? Solid state characterization techniques like mDSC suggests the formation of eutectic mixture between drug and polymer. Meltable polymers possess a great challenge when it comes to processing parameters during product development and powder flow properties being one of it. Pharm Res. In case of eutectic mixtures, the melting point of the mixture is less than the individual components which means less energy is required for the first step and hence higher solubility and miscibility. J Colloid Interface Sci. As can be seen, the BFE values decreased with the polymer content and simple explanation for that is the waxy nature of Poloxamer 407 which acts a lubricant (44), and hence, less energy is required for powder flow. 09/02/2017 17:35. & Dave, R.H. Fusion Method for Solubility and Dissolution Rate Enhancement of Ibuprofen Using Block Copolymer Poloxamer 407. Powdered samples having an equivalent weight of 200 mg drug were weighed accurately, and dissolution was performed in triplicates. The PMs were prepared according to the procedure described above. Thermal and physical characterization of samples was done using modulated differential scanning calorimetry (mDSC), X-ray powder diffraction (XRD), and infrared spectroscopy (FTIR). All the samples were collected and stored in tightly sealed containers in a desiccator at a temperature of 25 ± 1.8°C for further analysis. 2004;56(12):1527–35. - 88.208.193.166. In the current study, maximum solubility enhancement was observed in acidic media, and this was critical because ibuprofen, being a weak acidic drug, remains mostly unionized in acidic pH which is the insoluble form. (1) Lots of techniques have been employed in the past for solubility enhancement like solid dispersions (2), nanosizing and micronization (3), eutectic mixtures (4), co-crystals and salt formation (5), polymorphs (6), complexation (7), surfactants and other hydrophilic polymers (8). 2012;101(9):3019–32. 1980;69(6):659–61. Loftsson T, Brewster ME. The percent recoveries for PMs (1:0.25, 1:0.5, and 1:0.75) were 99.8, 99.4, and 97.5% respectively whereas for FMs, they were 97.1, 104.2, and 98.4% respectively. Adv Drug Deliv Rev. 2012;101(12):4549–58. Fiche méthode - Démarche d'investigation. Modulated differential scanning calorimetry (mDSC), X-ray powder diffraction studies (XRD), and Fourier transform infrared spectroscopy (FTIR) analysis were carried out to investigate the interaction of drug and polymer at a molecular level. critical for all samples. A trend of decreasing f 1990;63(3):259–66. Ibuprofen solubility in pure organic solvents and aqueous mixtures of cosolvents: interactions and thermodynamic parameters relating to the solvation process. The solution was passed through 0.45-μm syringe filters and analyzed spectrophotometrically at a λmax of 264 nm. Murdande SB, Shah DA, Dave RH. A lab-scale high shear mixer (GMX-LAB Micro®, Freund-Vector Corporation, IA, USA) was used for carrying out the fusion process in a 1-L jacketed bowl. 2007;14(7):413–26. Int J Pharm. Huber HE, Dale LB, Christenson GL. Expérience du programme de physique chimie de cinquième. Jacket temperature was maintained at 75°C using an external water circulator (Model F25-MA, Julabo Inc., PA, USA), and fusion was carried until a product temperature of 70 ± 1.2°C was attained. Table 2. In vitro dissolution studies showed dissolution rate enhancement for physical mixtures and the formulations in all three media. La fusion est aussi appelée fusion alors que la dissolution est aussi appelée dissolution. The effect was most pronounced in acidic media where, solubility enhancement was 18-fold for FM 1:0.75 as compared to ibuprofen. Özdemir N, Erkin J. Enhancement of dissolution rate and bioavailability of sulfamethoxazole by complexation with β-cyclodextrin. 2. Thermal analysis showed a characteristic behavior of the drug and polymer mixture. Binary mixtures of ibuprofen and poloxamer were prepared in three different ratios (1:0.25, 1:0.5, and 1:0.75, respectively) using a water-jacketed high shear mixer. Enhanced dissolution of the PMs and FMs as compared to the drug was observed. Pharm Res. These studies prove that the observed dissolution rate enhancement might not be due to any changes in the crystallinity of ibuprofen which means the drug dissolution was enhanced when the drug was in more stable crystalline form. Eur J Pharm Sci. Stock solution of the drug was prepared in ethanol (100 μg/ml), and the solution was scanned through a wavelength of 200–400 nm to determine the λmax using a UV–VIS spectrophotometer (Model # 1800, Shimadzu Scientific Instruments Inc., NJ, USA). Physical mixtures were prepared for all the ratios in a turbula blender (Turbula® T2C, Glen Mills Inc., NJ, USA) at a constant speed for 10 min. Colloids Surf B: Biointerfaces. In vitro dissolution studies for ibuprofen, physical mixtures (PM), and fusion mixtures (FM) in a de-ionized water; b 0.1 N HCl (pH = 1.2), and c phosphate buffer (pH = 7.2). Analysis was done in the range of 50 ≤ 2θ ≤ 400 at a scan step of 0.020° and time for each step being 0.5 s. FTIR spectroscopy was done for all samples including ibuprofen, Poloxamer 407 and formulations using a Nicolet iS5 FTIR spectrophotometer with iD5 ATR diamond accessory (Thermo Fisher Scientific Inc., Madison, WI, USA). Effect of process parameters on compressibility of granulation manufactured in a high-shear mixer. With this ratio, delivery of 200 mg ibuprofen would end up having a formulation weight of 700 mg without excipients which is not feasible. Mixture was cooled down in the bowl itself by rapidly circulating water at 25.0 ± 1.0°C through the jacket. Int J Pharm. 2007;343(1–2):228–37. To study the effects of solvent and relative humidity on rheological and thermal properties of microcrystalline cellulose granules using hydroxypropyl methylcellulose as binder. The first step is the melting of drug and polymer at their respective melting points. AAPS PharmSciTech 17, 1428–1440 (2016). Phenazopyridine cocrystal and salts that exhibit enhanced solubility and stability. Dissolution avec liquidation : les protagonistes Que ce soit pour la dissolution ou la liquidation, la décision des associés est un facteur clé de la fermeture de la société. Assay of the prepared PMs and FMs was done to see if the blending parameters used and the conditions used to carry out the fusion process were optimal to have acceptable content uniformity. Standard curve for ibuprofen using UV spectrsoscopy. Stability of formulations and miscibility of drug and polymer can be predicted with these calculations. 2) factors were calculated using the Eqs. 2 and 3, respectively. A linear trend (pre-filtration and post-filtration) was seen at the selected λ Table II shows the results from one-way ANOVA and post-hoc t test done between different pairs of formulations. Effect of the polymer present physically as well as when molecularly dispersed on saturation solubility of ibuprofen was evaluated in the saturation solubility studies. One-way ANOVA was done for each time point for all the dissolution data (p < 0.05) followed by post-hoc t test to compare two groups at a time (36). Pandey P, Tao J, Chaudhury A, Ramachandran R, Gao JZ, Bindra DS. Pour être informé des derniers articles, inscrivez vous : Aparté : notations pour les équations de réaction. Hermetically sealed aluminum pans were used with pin hole on the lid to maintain a constant pressure for analysis, and a sample weight of 10 ± 3 mg was maintained (n = 3). 1986;12(7):969–92. PubMed  Int J Pharm. From these studies, it can be concluded that the saturation solubility of the drug was enhanced mainly due to the Poloxamer 407 presence in the micellar form and the fusion process gave it a marginal boost. The SE values were similar for all formulations. Figure 5 shows the linear plot of total drug solubility with increasing surfactant concentration. Singhal D, Curatolo W. Drug polymorphism and dosage form design: a practical perspective. Google Scholar. On in Lors d’une dilution, il y a conservation de la quantité de matière de soluté … Mauger JW, Chilko D, Howard S. On the analysis of dissolution data. Int J Pharm. Savić R, Eisenberg A, Maysinger D. Block copolymer micelles as delivery vehicles of hydrophobic drugs: micelle–cell interactions. The most pronounced effect was seen for formulation (1:0.75) in acidic media where the cumulative drug release was 58.27% while for drug, it was 3.67%. Similarly, in de-ionized water, a cumulative release of 44% for FM 1:0.75 was seen whereas for drug, it was 8% after 60 min. A combined experimental and modeling approach to study the effects of high-shear wet granulation process parameters on granule characteristics. 2 value of 0.9997. 4 and 5, respectively, as outlined in the SUPAC and IVIVC guidelines (34,35). Au cours de la dissolution, ... - Calculer le facteur de dilution. En effet, si la quantité de solvant augmente et que la quantité de soluté demeure la même, le volume de la solution totale augmentera alors que sa concentration diminue. Dilution: 1:4 (0.4 g sample for 1.6 g flux) 4 - 8 minutes dissolution in a beaker containing about 90 ml of 5% HNO 3 w/v. Marques HC, Hadgraft J, Kellaway I. Drug Deliv. 1995;123(1):53–63. Article  2. The solidified mixture was scrapped out, then powdered with a mill (Model L1A, FitzPatrick®, IL, USA) using a mesh of 1680 μm opening (US mesh #12). Cyclodextrins as functional excipients: methods to enhance complexation efficiency. Passerini N, Albertini B, González-Rodríguez ML, Cavallari C, Rodriguez L. Preparation and characterisation of ibuprofen–poloxamer 188 granules obtained by melt granulation. 2013;18(2):434–42. The calculated F values were greater than F 2.11.1) recommends the abbreviations sol and dil for these processes. max of 264 nm as seen in Fig. Similar observations were made by the Carr’s index and angle of repose values. Overlay of modulated differential scanning calorimeter thermograms between a ibuprofen and physical mixtures (PM); b ibuprofen and fusion mixtures (FM); c ibuprofen and physical mixtures (PM) for eutectic composition study; d phase diagram for ibuprofen/poloxamer 407 binary mixtures. From the dissolution data, it was noticed that though there was not much difference in saturation solubility values between PMs and FMs seen previously, there was significant difference in their dissolution profiles. Hu L, Tang X, Cui F. Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs. Diffraction studies were performed to check the sustainability of crystalline nature of the drug after the fusion process.

Rassurer Un Homme Qui Manque De Confiance En Lui, Cours De Théâtre Paris Gratuit, Gaston Bachelard Le Droit De Rêver, Châssis 4l Occasion, Gestion Du Stress Exercices, Télétravail Un Jour Sur Deux, Clothilde De Bernardi,