Displaying publications 101 - 120 of 422 in total

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  1. Kumar P, Chaudhary B, Jain V, Baboota S, Shivanandy P, Alharbi KS, et al.
    Curr Drug Deliv, 2023;20(9):1262-1274.
    PMID: 36380413 DOI: 10.2174/1567201820666221114113637
    Molecular pharmaceutics play a critical role in the drug delivery system, representing the direct interconnection of drug bioavailability with its molecular form. There is a diversity in the molecular structures by which it affects its properties, such as amorphous form, crystalline form, partialamorphous molecular dispersion, and disordered state. The active pharmaceutical ingredient (API) and the excipients utilized in the formulation process contain various divergent modes used in the formulation process. They include better formulations of any type to obtain good quality pharmaceutical products. This review reveals how the molecular states affect the API and are important in maintaining the quality of dosage forms. Furthermore, the physio-chemical properties of the components and various pharmaceutical approaches employed in the formulation of dosage forms are studied from the point of view of molecular pharmaceutics.
    Matched MeSH terms: Solubility
  2. Tsuji T, Ono T, Taguchi H, Leong KH, Hayashi Y, Kumada S, et al.
    Chem Pharm Bull (Tokyo), 2023;71(7):576-583.
    PMID: 37394606 DOI: 10.1248/cpb.c23-00214
    Time-domain NMR (TD-NMR) was used for continuous monitoring of the hydration behavior of hydrophilic matrix tablets. The model matrix tablets comprised high molecular weight polyethylene oxide (PEO), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG). The model tablets were immersed in water. Their T2 relaxation curves were acquired by TD-NMR with solid-echo sequence. A curve-fitting analysis was conducted on the acquired T2 relaxation curves to identify the NMR signals corresponding to the nongelated core remaining in the samples. The amount of nongelated core was estimated from the NMR signal intensity. The estimated values were consistent with the experiment measurement values. Next, the model tablets immersed in water were monitored continuously using TD-NMR. The difference in hydration behaviors of the HPMC and PEO matrix tablets was then characterized fully. The nongelated core of the HPMC matrix tablets disappeared more slowly than that of the PEO matrix tablets. The behavior of HPMC was significantly affected by the PEG content in the tablets. It is suggested that the TD-NMR method has potential to be utilized to evaluate the gel layer properties, upon replacement of the immersion medium: purified (nondeuterated) water is replaced with heavy (deuterated) water. Finally, drug-containing matrix tablets were tested. Diltiazem hydrochloride (a highly water-soluble drug) was employed for this experiment. Reasonable in vitro drug dissolution profiles, which were in accordance with the results from TD-NMR experiments, were observed. We concluded that TD-NMR is a powerful tool to evaluate the hydration properties of hydrophilic matrix tablets.
    Matched MeSH terms: Solubility
  3. Khan AA, Akhtar S, Yadav Y, Atiya A, Alelwani W, Bannunah AM, et al.
    Curr Drug Deliv, 2023;20(10):1474-1486.
    PMID: 35980056 DOI: 10.2174/1567201819666220817111054
    BACKGROUND: The antiretroviral protease inhibitor drug, lopinavir (LPV), is used to treat HIV-1 infection. LPV is known to have limited oral bioavailability, which may be attributed to its poor aqueous solubility, low efficacy and high first-pass metabolism. Self-nanoemulsifying drug delivery systems (SNEDDS) for LPV have been developed and optimised to counter the current issues.

    METHODS: The titration method was used to prepare LPV-loaded SNEDDS (LPV-SNEDDS). Six different pseudo-ternary phase diagrams were constructed to identify the nanoemulsifying region. The developed formulations were chosen in terms of globule size < 100 nm, dispersity ≤ 0.5, dispersibility (Grade A) and% transmittance > 85. Heating-cooling cycle, freeze-thaw cycle, and centrifugation studies were performed to confirm the stability of the developed SNEDDS.

    RESULTS: The final LPV-SNEDDS (L-14) droplet size was 58.18 ± 0.62 nm, with polydispersity index, zeta potential, and entrapment efficiency (EE%) values of 0.326 ± 0.005, -22.08 ± 1.2 mV, and 98.93 ± 1.18%, respectively. According to high-resolution transmission electron microscopy (HRTEM) analysis, the droplets in the optimised formulation were < 60 nm in size. The selected SNEDDS released nearly 99% of the LPV within 30 min, which was significantly (p < 0.05) higher than the LPV-suspension in methylcellulose (0.5% w/v). It indicates the potential use of SNEDDS to enhance the solubility of LPV, which eventually could help improve the oral bioavailability of LPV. The Caco-2 cellular uptake study showed a significantly (p < 0.05) higher LPV uptake from the SNEEDS (LPV-SNEDDS-L-14) than the free LPV (LPV-suspension).

    CONCLUSION: The LPV-SNEDDS could be a potential carrier for LPV oral delivery.

    Matched MeSH terms: Solubility
  4. Loke YH, Chew YL, Janakiraman AK, Lee SK, Uddin ABMH, Goh CF, et al.
    Drug Dev Ind Pharm, 2024 Jan;50(1):36-44.
    PMID: 38149637 DOI: 10.1080/03639045.2023.2294095
    INTRODUCTION: Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited.

    OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs.

    METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation.

    RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min.

    CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.

    Matched MeSH terms: Solubility
  5. Senjoti FG, Mahmood S, Jaffri JM, Mandal UK
    Iran J Pharm Res, 2016;15(1):53-70.
    PMID: 27610147
    An oral sustained-release floating tablet formulation of metformin HCl was designed and developed. Effervescence and swelling properties were attributed on the developed tablets by sodium bicarbonate and HPMC-PEO polymer combination, respectively. Tablet composition was optimized by response surface methodology (RSM). Seventeen (17) trial formulations were analyzed according to Box-Behnken design of experiment where polymer content of HPMC and PEO at 1: 4 ratio (A), amount of sodium bi-carbonate (B), and amount of SSG (C) were adopted as independent variables. Floating lag time in sec (Y1), cumulative percent drug released at 1 h (Y2) and 12 h (Y3) were chosen as response variables. Tablets from the optimized formulation were also stored at accelerated stability condition (40°C and 75% RH) for 3 months to assess their stability profile. RSM could efficiently optimize the tablet composition with excellent prediction ability. In-vitro drug release until 12 h, floating lag time, and duration of floating were dependent on the amount of three selected independent variables. Optimized tablets remained floating for more than 24 h with a floating lag time of less than 4 min. Based on best fitting method, optimized formulation was found to follow Korsmeyer-Peppas release kinetic. Accelerated stability study revealed that optimized formulation was stable for three months without any major changes in assay, dissolution profile, floating lag time and other physical properties.
    Matched MeSH terms: Solubility
  6. Mohtar N, A K Khan N, Darwis Y
    Iran J Pharm Res, 2015;14(4):989-1000.
    PMID: 26664366
    Solid lipid nanoparticles of atovaquone (ATQ-SLN) were prepared by high shear homogenization method using tripalmitin, trilaurin, and Compritol 888 ATO as the lipid matrices and Phospholipon 90H, Tween 80, and poloxamer 188 as the surfactants. Optimization of the formulations was conducted using 6 sets of 2(4) full-factorial design based on four independent variables that were the number of homogenizing cycles, concentration of the lipid, concentration of the co-surfactant, and concentration of the main surfactant. The dependent variables were particle size and polydispersity index (PdI). The homogenizing cycles showed a negative influence on the dependent variables which reduced both the particle size and the PdI value. Moreover, a combination of certain percentages of the main surfactant and co-surfactant also showed a negative influence that reduced both the particle size and PdI value. Selected formulations from each design were further characterized for the entrapment efficiency and yield. The optimised formulation of ATQ-SLN consisted of trilaurin, Phospholipon 90H and Tween 80 with a particle size of 89.4 ± 0.2 nm and entrapment efficiency of 83.0 ± 1.7%. The in-vitro release evaluation of the formulation showed a complete and immediate release of ATQ from the SLN that could be a solution to improve the poor aqueous solubility and hence poor bioavailability of the drug.
    Matched MeSH terms: Solubility
  7. Shafie MH, Yusof R, Samsudin D, Gan CY
    Int J Biol Macromol, 2020 Nov 15;163:1276-1282.
    PMID: 32673725 DOI: 10.1016/j.ijbiomac.2020.07.109
    The potential of Averrhoa bilimbi pectin (ABP) as a source of biopolymer for edible film (EF) production was explored, and deep eutectic solvent (DES) (1% w/w) containing choline chloride-citric acid monohydrate at a molar ratio of 1:1 was used as the plasticizer. The EF-ABP3:1, which was produced from ABP with large branch size, showed a higher value of melting temperature (175.30 °C), tensile stress (7.32 MPa) and modulus (33.64 MPa). The EF-ABP3:1 also showed better barrier properties by obtaining the lowest water vapor transmission rates (1.10-1.18 mg/m2.s) and moisture absorption values (2.61-32.13%) depending on the relative humidity compared to other EF-ABPs (1.39-1.83 mg/m2.s and 3.48-51.50%, respectively) that have linear structure with smaller branch size. From these results, it was suggested that the galacturonic acid content, molecular weight, degree of esterification and pectin structure of ABP significantly influenced the properties of EFs. The interaction of highly branched pectin chains was stronger than the linear chains, thus reduced the effect of plasticizer and produced a mechanically stronger EF with better barrier properties. Hence, it was suggested that these EFs could be used as alternative degradable packaging/coating materials.
    Matched MeSH terms: Solubility/drug effects
  8. Gorajana A, Kit WW, Dua K
    Recent Pat Drug Deliv Formul, 2015;9(2):167-82.
    PMID: 25714525
    OBJECTIVE: Norfloxacin has a low aqueous solubility which leads to poor dissolution. Keeping this fact in mind the purpose of the present study is to formulate and evaluate norfloxacin solid dispersion.

    METHODS: Solid dispersions were prepared using hydrophilic carriers like polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974pNF (CP) in various ratios using solvent evaporation technique. These formulations were evaluated using solubility studies, dissolution studies; Fourier transmitted infrared spectroscopy (FTIR), X-ray diffraction (XRD), and differential scanning calorimetery (DSC). The influence of polymer type and drug to polymer ratio on the solubility and dissolution rate of norfloxacin was also evaluated.

    RESULTS: FTIR analysis showed no interaction of all three polymers with norfloxacin. The results from XRD and DSC analyses of the solid dispersion preparations showed that norfloxacin existsin its amorphous form. Among the Norfloxacin: PEG solid dispersions, Norfloxacin: PEG 1:14 ratio showed the highest dissolution rate at pH 6.8. For norfloxacin: PVP solid dispersions, norfloxacin: PVP 1:10 ratio showed the highest dissolution rate at pH 6.8. For Norfloxacin: CP solid dispersions, norfloxacin: P 1:2 ratio showed the highest dissolution rate at pH 6.8.

    CONCLUSION: The solid dispersion of norfloxacin with polyethylene glycol (PEG) 4000, polyvinylpyrrolidone (PVP) k30 and carbopol 974p NF (CP), lends an ample credence for better therapeutic efficacy.

    Matched MeSH terms: Solubility
  9. Rubentheren V, Ward TA, Chee CY, Tang CK
    Carbohydr Polym, 2015 Jan 22;115:379-87.
    PMID: 25439908 DOI: 10.1016/j.carbpol.2014.09.007
    Chitosan film reinforced with nano-sized chitin whiskers and crosslinked using tannic acid was synthesized by the casting-vaporation method. The mechanical and physicochemical properties of several film samples (consisting of different ratio of chitin and tannic acid) were compared with neat chitosan. Tensile tests show that the addition of chitin improves the nanocomposite films mechanical properties up to 137% compared to neat chitosan, but this is slightly degraded when tannic acid is introduced. However, tannic acid and chitin whisker content greatly reduced moisture content by 294% and water solubility by 13%. Transmission electron microscopy (TEM) and Fourier-transform-infrared spectroscopy (FTIR) were used to investigate the morphology and molecular interaction of film. X-ray diffraction results indicated that the samples with chitin whiskers had a more rigid structure. The addition of tannic acid changed the structure into an anhydrous crystalline conformation when compared to neat chitosan film.
    Matched MeSH terms: Solubility
  10. Liew KB, Odeniyi MA, Peh KK
    Pharm Dev Technol, 2016;21(3):346-53.
    PMID: 25597618 DOI: 10.3109/10837450.2014.1003657
    Freeze drying technology has not been maximized and reported in manufacturing orally disintegrating films. The aim of this study was to explore the freeze drying technology in the formulation of sildenafil orally disintegrating films and compare the physical properties with heat-dried orally disintegrating film. Central composite design was used to investigate the effects of three factors, namely concentration of carbopol, wheat starch and polyethylene glycol 400 on the tensile strength and disintegration time of the film. Heat-dried films had higher tensile strength than films prepared using freeze-dried method. For folding endurance, freeze-dried films showed improved endurance than heat-dried films. Moreover, films prepared using freeze-dried methods were thicker and had faster disintegration time. Formulations with higher amount of carbopol and starch showed higher tensile strength and thickness whereas formulations with higher PEG 400 content showed better flexibility. Scanning electron microscopy showed that the freeze-dried films had more porous structure compared to the heat-dried film as a result of the release of water molecule from the frozen structure when it was subjected to freeze drying process. The sildenafil film was palatable. The dissolution profiles of freeze-dried and heat-dried films were similar to Viagra® with f2 of 51.04 and 65.98, respectively.
    Matched MeSH terms: Solubility
  11. Bhat R, Karim AA
    J Food Sci Technol, 2014 Jul;51(7):1326-33.
    PMID: 24966426 DOI: 10.1007/s13197-012-0652-9
    Developing novel fish gelatin films with better mechanical properties than mammalian gelatin is a challenging but promising endeavor. Studies were undertaken to produce fish gelatin films by combining treatments with different sugars (ribose and lactose) followed 'by' 'and' ultraviolet (UV) radiation, as possible cross-linking agents. Increase in tensile strength and percent elongation at break was recorded, which was more significant in films without sugars that were exposed to UV radiation. Films with added ribose showed decreased solubility after UV treatment and exhibited higher swelling percentage than films with added lactose, which readily dissolved in water. FTIR spectra of all the films showed identical patterns, which indicated no major changes to have occurred in the functional groups as a result of interaction between gelatin, sugars and UV irradiation. The results of this study could be explored for commercial use, depending on industrial needs for either production of edible films or for food packaging purposes.
    Matched MeSH terms: Solubility
  12. Moniruzzaman M, Chowdhury MA, Rahman MA, Sulaiman SA, Gan SH
    Biomed Res Int, 2014;2014:359890.
    PMID: 24982869 DOI: 10.1155/2014/359890
    The present study was undertaken to determine the content of six minerals, five trace elements, and ten pesticide residues in honeys originating from different regions of Malaysia. Calcium (Ca), magnesium (Mg), iron (Fe), and zinc (Zn) were analyzed by flame atomic absorption spectrometry (FAAS), while sodium (Na) and potassium (K) were analyzed by flame emission spectrometry (FAES). Trace elements such as arsenic (As), lead (Pb), cadmium (Cd), copper (Cu), and cobalt (Co) were analyzed by graphite furnace atomic absorption spectrometry (GFAAS) following the microwave digestion of honey. High mineral contents were observed in the investigated honeys with K, Na, Ca, and Fe being the most abundant elements (mean concentrations of 1349.34, 236.80, 183.67, and 162.31 mg/kg, resp.). The concentrations of the trace elements were within the recommended limits, indicating that the honeys were of good quality. Principal component analysis reveals good discrimination between the different honey samples. The pesticide analysis for the presence of organophosphorus and carbamates was performed by high performance liquid chromatography (HPLC). No pesticide residues were detected in any of the investigated honey samples, indicating that the honeys were pure. Our study reveals that Malaysian honeys are rich sources of minerals with trace elements present within permissible limits and that they are free from pesticide contamination.
    Matched MeSH terms: Solubility
  13. Habibi N, Mohd Hashim SZ, Norouzi A, Samian MR
    BMC Bioinformatics, 2014;15:134.
    PMID: 24885721 DOI: 10.1186/1471-2105-15-134
    Over the last 20 years in biotechnology, the production of recombinant proteins has been a crucial bioprocess in both biopharmaceutical and research arena in terms of human health, scientific impact and economic volume. Although logical strategies of genetic engineering have been established, protein overexpression is still an art. In particular, heterologous expression is often hindered by low level of production and frequent fail due to opaque reasons. The problem is accentuated because there is no generic solution available to enhance heterologous overexpression. For a given protein, the extent of its solubility can indicate the quality of its function. Over 30% of synthesized proteins are not soluble. In certain experimental circumstances, including temperature, expression host, etc., protein solubility is a feature eventually defined by its sequence. Until now, numerous methods based on machine learning are proposed to predict the solubility of protein merely from its amino acid sequence. In spite of the 20 years of research on the matter, no comprehensive review is available on the published methods.
    Matched MeSH terms: Solubility
  14. Loh GO, Tan YT, Peh KK
    Carbohydr Polym, 2014 Jan 30;101:505-10.
    PMID: 24299805 DOI: 10.1016/j.carbpol.2013.09.084
    The effect of hydroxypropyl methylcellulose (HPMC) concentration on β-cyclodextrin (β-CD) solubilization of norfloxacin was examined. The solubility and dissolution of norfloxacin/β-CD and norfloxacin/β-CD/HPMC inclusion complexes were studied. The presence of β-CD increased significantly the solubility and dissolution of norfloxacin. The addition of HPMC until 5% (w/w) improved the solubilization of norfloxacin but further addition above 5% (w/w), decreased norfloxacin solubilization. Fourier transformed Infra-red (FTIR) showed that norfloxacin was successfully included into β-CD. Differential scanning calorimetry (DSC) showed that the norfloxacin endothermic peak shifted to a lower temperature with reduced intensity indicating the formation of inclusion complex. The addition of HPMC reduced further the intensity of norfloxacin endothermic peak. Most of the sharp and intense peaks of norfloxacin disappeared with the addition of HPMC. In conclusion, the concentration of hydrophilic polymer used to enhance β-CD solubilization of poorly soluble drugs is very critical.
    Matched MeSH terms: Solubility
  15. Nopianti R, Huda N, Ismail N, Ariffin F, Easa AM
    J Food Sci Technol, 2013 Aug;50(4):739-46.
    PMID: 24425976 DOI: 10.1007/s13197-011-0394-0
    Physicochemical properties of threadfin bream surimi with different levels of polydextrose (3%, 6%, 9% and 12%), raw surimi, raw surimi with addition sodium tripolyphosphate and commercial surimi (sucrose) during 6 months of frozen storage were investigated. The analyses included the measurement of Ca(2+)-ATPase, sulfhydryl contents, protein solubility, sodium dodecyl sulfate polyacrylamide gel electrophoresis, differential scanning calorimetry and scanning electron microscopy. The Ca(2+)-ATPase, sulfhydryl content and protein solubility levels added with 3%, 6%, 9% and 12% polydextrose can be maintained until the 6 months of storage by 47.33%, 41.60% and 51.41%, respectively. Differential scanning calorimetry showed decreases in thermal stabilization of myosin with regard to transition termperature. Analysis by scanning electron microscopy demonstrated that the number of pores formed was increased after storage. This study suggested that surimi stored with the polydextrose as a cryoprotectant was able to maintain physicochemical of surimi better compared to raw surimi with no additives or raw surimi with sodium tripolyphosphate.
    Matched MeSH terms: Solubility
  16. Tan ES, Ying-Yuan N, Gan CY
    Food Chem, 2014;152:447-55.
    PMID: 24444960 DOI: 10.1016/j.foodchem.2013.12.008
    Optimisation of protein extraction yield from pinto bean was investigated using response surface methodology. The maximum protein yield of 54.8 mg/g was obtained with the optimal conditions of: temperature=25 °C, time=1 h and buffer-to-sample ratio=20 ml/g. PBPI was found to obtain high amount of essential amino acids such as leucine, lysine, and phenylalanine compared to SPI. The predominant proteins of PBPI were vicilin and phytohemagglutinins whereas the predominant proteins of SPI were glycinin and conglycinins. Significantly higher emulsifying capacity was found in PBPI (84.8%) compared to SPI (61.9%). Different isoelectric points were found in both PBPI (4.0-5.5) and SPI (4.0-5.0). Also, it was found that PBPI obtained a much higher denaturation temperature of 110.2 °C compared to SPI (92.5 °C). Other properties such as structural information, gelling capacity, water- and oil-holding capacities, emulsion stability as well as digestibility were also reported.
    Matched MeSH terms: Solubility
  17. Oladebeye AO, Oshodi AA, Amoo IA, Karim AA
    Food Chem, 2013 Nov 15;141(2):1416-23.
    PMID: 23790933 DOI: 10.1016/j.foodchem.2013.04.080
    Ozone-oxidised starches were prepared from the native starches isolated from white and red cocoyam, and white and yellow yam cultivars. The native and oxidised starches were evaluated for functional, thermal and molecular properties. The correlations between the amount of reacted ozone and carbonyl and carboxyl contents of the starches were positive, as ozone generation time (OGT) increased. Significant differences were obtained in terms of swelling power, solubility, pasting properties and textural properties of the native starches upon oxidation. The DSC data showed lower transition temperatures and enthalpies for retrograded gels compared to the gelatinized gels of the same starch types. The native starches showed CB-type XRD patterns while the oxidised starches resembled the CA-type pattern. As amylose content increased, amylopectin contents of the starches decreased upon oxidation. Similarly, an increase in Mw values were observed with a corresponding decrease in Mn values upon oxidation.
    Matched MeSH terms: Solubility
  18. Mirhosseini H, Amid BT
    Molecules, 2012 May 29;17(6):6465-80.
    PMID: 22643356 DOI: 10.3390/molecules17066465
    Durian seed is an agricultural biomass waste of durian fruit. It can be a natural plant source of non-starch polysaccharide gum with potential functional properties. The main goal of the present study was to investigate the effect of chemical extraction variables (i.e., the decolouring time, soaking temperature and soaking time) on the physicochemical properties of durian seed gum. The physicochemical and functional properties of chemically-extracted durian seed gum were assessed by determining the particle size and distribution, solubility and the water- and oil-holding capacity (WHC and OHC). The present work revealed that the soaking time should be considered as the most critical extraction variable affecting the physicochemical properties of crude durian seed gum.
    Matched MeSH terms: Solubility
  19. Rahim TN, Mohamad D, Md Akil H, Ab Rahman I
    Dent Mater, 2012 Jun;28(6):e63-70.
    PMID: 22480722 DOI: 10.1016/j.dental.2012.03.011
    To determine the diffusion coefficient, water sorption and solubility of various types of restorative dental composites and to evaluate the effect of acidic media (orange juice and coke) on their characteristics.
    Matched MeSH terms: Solubility
  20. Mahdi ES, Sakeena MH, Abdulkarim MF, Abdullah GZ, Sattar MA, Noor AM
    Drug Des Devel Ther, 2011;5:311-23.
    PMID: 21792294 DOI: 10.2147/DDDT.S15698
    The purpose of this study was to select appropriate surfactants or blends of surfactants to study the ternary phase diagram behavior of newly introduced palm kernel oil esters.
    Matched MeSH terms: Solubility
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