Displaying publications 1 - 20 of 38 in total

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  1. Fulltext Preparation of astaxanthin nanodispersions using gelatin-based stabilizer systems
    Anarjan N, Nehdi IA, Sbihi HM, Al-Resayes SI, Malmiri HJ, Tan CP
    Molecules, 2014 Sep 10;19(9):14257-65.
    PMID: 25211006 DOI: 10.3390/molecules190914257
    The incorporation of lipophilic nutrients, such as astaxanthin (a fat soluble carotenoid) in nanodispersion systems can either increase the water solubility, stability and bioavailability or widen their applications in aqueous food and pharmaceutical formulations. In this research, gelatin and its combinations with sucrose oleate as a small molecular emulsifier, sodium caseinate (SC) as a protein and gum Arabic as a polysaccharide were used as stabilizer systems in the formation of astaxanthin nanodispersions via an emulsification-evaporation process. The results indicated that the addition of SC to gelatin in the stabilizer system could increase the chemical stability of astaxanthin nanodispersions significantly, while using a mixture of gelatin and sucrose oleate as a stabilizer led to production of nanodispersions with the smallest particle size (121.4±8.6 nm). It was also shown that a combination of gelatin and gum Arabic could produce optimal astaxanthin nanodispersions in terms of physical stability (minimum polydispersity index (PDI) and maximum zeta-potential). This study demonstrated that the mixture of surface active compounds showed higher emulsifying and stabilizing functionality compared to using them individually in the preparation of astaxanthin nanodispersions.
    Matched MeSH terms: Excipients/chemistry*
  2. Promises of Molecular Pharmaceutics in the Development of Novel Drug Delivery Formulations
    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: Excipients/chemistry
  3. QbD Assisted Systematic Review for Optimizing the Selection of PVP as a Ternary Substance in Enhancing the Complexation Efficiency of Cyclodextrins: a Pilot Study
    Mulenga G, Alahmed TAA, Sami F, Majeed S, Ali MS, Le JLJ, et al.
    AAPS PharmSciTech, 2024 Jun 11;25(5):134.
    PMID: 38862663 DOI: 10.1208/s12249-024-02845-3
    Inclusion complexes require higher concentration of Beta cyclodextrins (βCD) resulting in increased formulation bulk, toxicity, and production costs. This systematic review offers a comprehensive analysis using Quality by design (QbD) as a tool to predict potential applications of Polyvinylpyrrolidone (PVP) as a ternary substance to address issues of inclusion complexes. We reviewed 623 documents from 2013 to 2023 and Eighteen (18) research papers were selected for statistical and meta-analysis using the QbD concept to identify the most critical factors for selecting drugs and effect of PVP on inclusion complexes. The QbD analysis revealed that Molecular weight (MW), Partition coefficient (Log P), and the auxiliary substance ratio directly affected complexation efficiency (CE), thermodynamic stability in terms of Gibbs free energy (ΔG), and percent drug release. However, Stability constant (Ks) remained unaffected by any of these parameters. The results showed that low MW (250), median Log P (6), and a βCD: PVP ratio of 2:3 would result in higher CE, lower G, and improved drug release. PVP improves drug solubility, enhances delivery and therapeutic outcomes, and counteracts increased drug ionization due to decreased pH. In certain cases, its bulky nature and hydrogen bonding with CD molecules can form non-inclusion complexes. The findings of the study shows that there is potential molecular interaction between PVP and β-cyclodextrins, which possibly enhances the stability of inclusion complexes for drug with low MW and log P values less than 9. The systematic review shows a comprehensive methodology based on QbD offers a replicable template for future investigations into drug formulation research.
    Matched MeSH terms: Excipients/chemistry
  4. Fulltext Effects of using pozzolan and Portland cement in the treatment of dispersive clay
    Vakili AH, Selamat MR, Moayedi H
    ScientificWorldJournal, 2013;2013:547615.
    PMID: 23864828 DOI: 10.1155/2013/547615
    Use of dispersive clay as construction material requires treatment such as by chemical addition. Treatments to dispersive clay using pozzolan and Portland cement, singly and simultaneously, were carried out in this study. When used alone, the optimum amount of pozzolan required to treat a fully dispersive clay sample was 5%, but the curing time to reduce dispersion potential, from 100% to 30% or less, was 3 month long. On the other hand, also when used alone, a 3% cement content was capable of reducing dispersion potential to almost zero percent in only 7 days; and a 2% cement content was capable of achieving similar result in 14 days. However, treatment by cement alone is costly and could jeopardize the long term performance. Thus, a combined 5% pozzolan and 1.5% cement content was found capable of reducing dispersion potential from 100% to zero percent in 14 days. The results indicate that although simultaneous treatment with pozzolan and cement would extend the required curing time in comparison to treatment by cement alone of a higher content, the task could still be carried out in a reasonable period of curing time while avoiding the drawbacks of using either pozzolan or cement alone.
    Matched MeSH terms: Excipients/chemistry*
  5. Use of microwave in processing of drug delivery systems
    Wong TW
    Curr Drug Deliv, 2008 Apr;5(2):77-84.
    PMID: 18393808
    Microwave has received a widespread application in pharmaceuticals and food processing, microbial sterilization, biomedical therapy, scientific and biomedical analysis, as well as, drug synthesis. This paper reviews the basis of application of microwave to prepare pharmaceutical dosage forms such as agglomerates, gel beads, microspheres, nanomatrix, solid dispersion, tablets and film coat. The microwave could induce drying, polymeric crosslinkages as well as drug-polymer interaction, and modify the structure of drug crystallites via its effects of heating and/or electromagnetic field on the dosage forms. The use of microwave opens a new approach to control the physicochemical properties and drug delivery profiles of pharmaceutical dosage forms without the need for excessive heat, lengthy process or toxic reactants. Alternatively, the microwave can be utilized to process excipients prior to their use in the formulation of drug delivery systems. The intended release characteristics of drugs in dosage forms can be met through modifying the physicochemical properties of excipients using the microwave.
    Matched MeSH terms: Excipients/chemistry
  6. Interfacial elastic relaxation during the ejection of bi-layered tablets
    Anuar MS, Briscoe BJ
    Int J Pharm, 2010 Mar 15;387(1-2):42-7.
    PMID: 19963050 DOI: 10.1016/j.ijpharm.2009.11.031
    The predilection of a bi-layered tablet to fail in the interface region after its initial formation in the compaction process reduces its practicality as a choice for controlled release solid drug delivery system. Hence, a fundamental appreciation of the governing mechanism that causes the weakening of the interfacial bonds within the bi-layered tablet is crucial in order to improve the overall bi-layered tablet mechanical integrity. This work has shown that the occurrence of the elastic relaxation in the interface region during the ejection stage of the compaction process decreases with the increase in the bi-layered tablet interface strength. This is believed to be due to the increase in the plastic bonding in the interface region. The tablet diametrical elastic relaxation affects the tablet height elastic relaxation, where the impediment of the tablet height expansion is observed when the interface region experiences a diametrical expansion.
    Matched MeSH terms: Excipients/chemistry*
  7. Hydrophobic kenaf nanocrystalline cellulose for the binding of curcumin
    Zainuddin N, Ahmad I, Kargarzadeh H, Ramli S
    Carbohydr Polym, 2017 May 01;163:261-269.
    PMID: 28267505 DOI: 10.1016/j.carbpol.2017.01.036
    Nanocrystalline cellulose (NCC) extracted from lignocellulosic materials has been actively investigated as a drug delivery excipients due to its large surface area, high aspect ratio, and biodegradability. In this study, the hydrophobically modified NCC was used as a drug delivery excipient of hydrophobic drug curcumin. The modification of NCC with a cationic surfactant, cetyl trimethylammonium bromide (CTAB) was used to modulate the loading of hydrophobic drugs that would not normally bind to NCC. The FTIR, Elemental analysis, XRD, TGA, and TEM were used to confirm the modification of NCC with CTAB. The effect of concentration of CTAB on the binding efficiency of hydrophobic drug curcumin was investigated. The amounts of curcumin bound onto the CTAB-NCC nanoparticles were analyzed by UV-vis Spectrophotometric. The result showed that the modified CTAB-NCC bound a significant amount of curcumin, in a range from 80% to 96% curcumin added. Nevertheless, at higher concentration of CTAB resulted in lower binding efficiency.
    Matched MeSH terms: Excipients/chemistry*
  8. Alginate graft copolymers and alginate-co-excipient physical mixture in oral drug delivery
    Wong TW
    J Pharm Pharmacol, 2011 Dec;63(12):1497-512.
    PMID: 22060280 DOI: 10.1111/j.2042-7158.2011.01347.x
    Use of alginate graft copolymers in oral drug delivery reduces dosage form manufacture complexity with reference to mixing or coating processes. It is deemed to give constant or approximately steady weight ratio of alginate to covalently attached co-excipient in copolymers, thereby leading to controllable matrix processing and drug release. This review describes various grafting approaches and their outcome on oral drug release behaviour of alginate graft copolymeric matrices. It examines drug release modulation mechanism of alginate graft copolymers against that of co-excipients in non-grafted formulations.
    Matched MeSH terms: Excipients/chemistry*
  9. Investigation on Secondary Structure Perturbations of Proteins Embedded in Solid Lipid Matrices as a Novel Indicator of their Biological Activity upon In Vitro Release
    Zeeshan F, Tabbassum M, Jorgensen L, Medlicott NJ
    AAPS PharmSciTech, 2018 Feb;19(2):769-782.
    PMID: 29134579 DOI: 10.1208/s12249-017-0883-1
    Protein biologics are prone to conformational changes during formulation development. Limited methods are available for conformational analysis of proteins in solid state and in the presences of formulation excipients. The aim of this study was to investigate the secondary structures of proteins encased in solid lipid matrices as a novel indicator of their stability upon in vitro release. Model proteins namely catalase and lysozyme were incorporated into lipid namely Precirol® AT05 (glycerol palmitostearate, melting point 58°C) at 30% w/w loading using melting and mixing and wet granulation methods. Attenuated total reflectance (ATR-FTIR) spectroscopy, size-exclusion chromatography (SEC) and biological activity analyses were performed. The information about secondary structure was acquired using second derivative analysis of amide-I band (1600-1700 cm-1). ATR analysis demonstrated interference of lipid spectrum with protein amide-I band which was subsequently subtracted to allow the analysis of the secondary structure. ATR spectra amide-I bands showed shifts peak band positions compared to native protein for matrices prepared using wet granulation. SEC analysis gave evidence of protein aggregation for catalase which was increased using wet granulation. The biological activity of catalase was statistically different from that of control and was affected by the incorporation method and was found to be in alignment with ATR spectral changes and extent of aggregation. In conclusion, ATR spectroscopy could analyze protein secondary structure in lipid matrices provided lipid interference was minimized. The ATR spectral changes and formation of aggregates can indicate the loss in biological activity of protein released from solid lipid matrices.
    Matched MeSH terms: Excipients/chemistry
  10. Fulltext Green synthesis and characterization of gelatin-based and sugar-reduced silver nanoparticles
    Darroudi M, Ahmad MB, Abdullah AH, Ibrahim NA
    Int J Nanomedicine, 2011;6:569-74.
    PMID: 21674013 DOI: 10.2147/IJN.S16867
    Silver nanoparticles (Ag-NPs) have been successfully prepared with simple and "green" synthesis method by reducing Ag(+) ions in aqueous gelatin media with and in the absence of glucose as a reducing agent. In this study, gelatin was used for the first time as a reducing and stabilizing agent. The effect of temperature on particle size of Ag-NPs was also studied. It was found that with increasing temperature the size of nanoparticles is decreased. It was found that the particle size of Ag-NPs obtained in gelatin solutions is smaller than in gelatin-glucose solutions, which can be related to the rate of reduction reaction. X-ray diffraction, ultraviolet-visible spectra, transmission electron microscopy, and atomic force microscopy revealed the formation of monodispersed Ag-NPs with a narrow particle size distribution.
    Matched MeSH terms: Excipients/chemistry
  11. Formulation and optimization of orally disintegrating tablets of sumatriptan succinate
    Sheshala R, Khan N, Darwis Y
    Chem Pharm Bull (Tokyo), 2011;59(8):920-8.
    PMID: 21804234
    The aims of the present research were to mask the intensely bitter taste of sumatriptan succinate and to formulate orally disintegrating tablets (ODTs) of the taste masked drug. Taste masking was performed by coating sumatriptan succinate with Eudragit EPO using spray drying technique. The resultant microspheres were evaluated for thermal analysis, yield, particle size, entrapment efficiency and in vitro taste masking. The tablets were formulated by mixing the taste masked microspheres with different types and concentrations of superdisintegrants and compressed using direct compression method followed by sublimation technique. The prepared tablets were evaluated for weight variation, thickness, hardness, friability, drug content, water content, in vitro disintegration time and in vitro drug release. All the tablet formulations disintegrated in vitro within 37-410 s. The optimized formulation containing 5% Kollidon CL-SF released more than 90% of the drug within 15 min and the release was comparable to that of commercial product (Suminat®). In human volunteers, the optimized formulation was found to have a pleasant taste and mouth feel and disintegrated in the oral cavity within 41 s. The optimized formulation was found to be stable and bioequivalent with Suminat®.
    Matched MeSH terms: Excipients/chemistry
  12. The effect of oleic acid stabilizer on the surface properties of bimetallic PtNi catalysts
    Abu Bakar NH, Abu Bakar M, Bettahar MM, Ismail J, Monteverdi S
    J Nanosci Nanotechnol, 2013 Jul;13(7):5034-43.
    PMID: 23901527
    A detailed study on the surface properties of oleic acid-stabilized PtNi nanoparticles supported on silica is reported. The oleic acid-stabilized PtNi nanoparticles were synthesized using NaBH4 as the reducing agent at various temperatures and oleic acid concentrations, prior to incorporation onto the silica support. X-ray diffraction studies of the unsupported oleic acid-stabilized PtNi particles revealed that the PtNi existed as alloys. Upon incorporation onto silica support, surface properties of the catalysts were investigated using H2-temperature reduction (H2-TPR), H2-temperature desorption (H2-TPD) and H2-chemisorption techniques. It was found that for the bimetallic catalysts, no oxides or very little oxidation occurred. Furthermore, these catalysts exhibited both Pt and Ni active sites on its surface though the availability of Ni active sites was dominant. A comparison of the surface properties of these materials with those prepared without oleic acid in our previous work [N. H. H. Abu Bakar et al., J. Catal. 265, 63 (2009)] and how they affect the hydrogenation of benzene is also discussed.
    Matched MeSH terms: Excipients/chemistry
  13. Centrifugal air-assisted melt agglomeration for fast-release "granulet" design
    Wong TW, Musa N
    Int J Pharm, 2012 Jul 1;430(1-2):184-96.
    PMID: 22531845 DOI: 10.1016/j.ijpharm.2012.04.026
    Conventional melt pelletization and granulation processes produce round and dense, and irregularly shaped but porous agglomerates respectively. This study aimed to design centrifugal air-assisted melt agglomeration technology for manufacture of spherical and yet porous "granulets" for ease of downstream manufacturing and enhancing drug release. A bladeless agglomerator, which utilized shear-free air stream to mass the powder mixture of lactose filler, polyethylene glycol binder and poorly water-soluble tolbutamide drug into "granulets", was developed. The inclination angle and number of vane, air-impermeable surface area of air guide, processing temperature, binder content and molecular weight were investigated with reference to "granulet" size, shape, texture and drug release properties. Unlike fluid-bed melt agglomeration with vertical processing air flow, the air stream in the present technology moved centrifugally to roll the processing mass into spherical but porous "granulets" with a drug release propensity higher than physical powder mixture, unprocessed drug and dense pellets prepared using high shear mixer. The fast-release attribute of "granulets" was ascribed to porous matrix formed with a high level of polyethylene glycol as solubilizer. The agglomeration and drug release outcomes of centrifugal air-assisted technology are unmet by the existing high shear and fluid-bed melt agglomeration techniques.
    Matched MeSH terms: Excipients/chemistry*
  14. Use of artificial neural networks to predict drug dissolution profiles and evaluation of network performance using similarity factor
    Peh KK, Lim CP, Quek SS, Khoh KH
    Pharm Res, 2000 Nov;17(11):1384-8.
    PMID: 11205731
    PURPOSE: To use artificial neural networks for predicting dissolution profiles of matrix-controlled release theophylline pellet preparation, and to evaluate the network performance by comparing the predicted dissolution profiles with those obtained from physical experiments using similarity factor.

    METHODS: The Multi-Layered Perceptron (MLP) neural network was used to predict the dissolution profiles of theophylline pellets containing different ratios of microcrystalline cellulose (MCC) and glyceryl monostearate (GMS). The concepts of leave-one-out as well as a time-point by time-point estimation basis were used to predict the rate of drug release for each matrix ratio. All the data were used for training, except for one set which was selected to compare with the predicted output. The closeness between the predicted and the reference dissolution profiles was investigated using similarity factor (f2).

    RESULTS: The f2 values were all above 60, indicating that the predicted dissolution profiles were closely similar to the dissolution profiles obtained from physical experiments.

    CONCLUSION: The MLP network could be used as a model for predicting the dissolution profiles of matrix-controlled release theophylline pellet preparation in product development.

    Matched MeSH terms: Excipients/chemistry
  15. Diclofenac release from eudragit-containing matrices and effects of thermal treatment
    Billa N, Yuen KH, Peh KK
    Drug Dev Ind Pharm, 1998 Jan;24(1):45-50.
    PMID: 15605596
    Ethyl acrylate-methyl methacrylate copolymer (Eudragit NE40D) was evaluated as matrix material for preparing controlled-release tablets of diclofenac sodium. Drug release could be modified in a predictable manner by varying the Eudragit NE40D content, but was pH dependent, being markedly reduced at lower pH. This could be attributed to the low solubility of the drug at these pH values. Thermal treatment of the tablets at 60 degrees C was also found to affect the rate of drug release, which was found to decrease with an increase in the treatment duration, but could be stabilized after 96 hr of treatment. This was also associated with a corresponding increase in the tablet tensile strength. However, treatment of the granules for 5 hr prior to compaction into tablets could shorten the stabilizing time of the drug release to 48 hr and that of the tensile strength to 24 hr. The effect of thermal treatment may be ascribed to better coalescence of the Eudragit particles to form a fine network, resulting in matrix of higher tortuosity and lower porosity.
    Matched MeSH terms: Excipients/chemistry*
  16. Comparison studies on the percolation thresholds of binary mixture tablets containing excipients of plastic/brittle and plastic/plastic deformation properties
    Amin MC, Fell JT
    Drug Dev Ind Pharm, 2004;30(9):937-45.
    PMID: 15554218
    Percolation theory has been used with great interest in understanding the design and characterization of dosage forms. In this study, work has been carried out to investigate the behavior of binary mixture tablets containing excipients of similar and different deformation properties. The binary mixture tablets were prepared by direct compression using lactose, polyvinyl chloride (PVC), Eudragit RS 100, and microcrystalline cellulose (MCC). The application of percolation theory on the relationships between compactibility, Pmax, or compression susceptibility (compressibility), gamma, and mixture compositions reveals the presence of percolation thresholds even for mixtures of similar deformation properties. The results showed that all mixture compositions exhibited at least one discreet change in the slope, which was referred to as the percolation threshold. The PVC/Eudragit RS100 mixture compositions showed significant percolation threshold at 80% (w/w) PVC loading. Two percolation thresholds were observed from a series of binary mixtures containing similar plastic deformation materials (PVC/MCC). The percolation thresholds were determined at 20% (w/w) and 80% (w/w) PVC loading. These are areas where one of the components percolates throughout the system and the properties of the tablets are expected to experience a sudden change. Experimental results, however, showed that total disruption of the tablet physical properties at the specified percolation thresholds can be observed for PVC/lactose mixtures at 20-30% (w/w) loading while only minor changes in the tablets' strength for PVC/MCC or PVC/Eudragit RS 100 mixtures were observed.
    Matched MeSH terms: Excipients/chemistry*
  17. Design of a 24-hour controlled porosity osmotic pump system containing PVP: formulation variables
    Yakubu R, Peh KK, Tan YT
    Drug Dev Ind Pharm, 2009 Dec;35(12):1430-8.
    PMID: 19929202 DOI: 10.3109/03639040902988566
    The purpose of this study was to design a 24-hour controlled porosity osmotic pump system that utilizes polyvinyl pyrrolidone (PVP) as an osmotic-suspending/release retarding agent of drugs.
    Matched MeSH terms: Excipients/chemistry*
  18. Effect of storage temperature on the stability of spray dried bacteriophage powders
    Leung SSY, Parumasivam T, Nguyen A, Gengenbach T, Carter EA, Carrigy NB, et al.
    Eur J Pharm Biopharm, 2018 Jun;127:213-222.
    PMID: 29486303 DOI: 10.1016/j.ejpb.2018.02.033
    This study aimed to assess the robustness of using a spray drying approach and formulation design in producing inhalable phage powders. Two types of Pseudomonas phages, PEV2 (Podovirus) and PEV40 (Myovirus) in two formulations containing different amounts of trehalose (70% and 60%) and leucine (30% and 40%) were studied. Most of the surface of the produced powders was found to be covered in crystalline leucine. The powders were stored at 4 °C and 20 °C under vacuum. The phage stability and in vitro aerosol performance of the phage powders were examined on the day of production and after 1, 3 and 12 months of storage. A minor titer loss during production was observed for both phages (0.2-0.8 log10 pfu/ml). The storage stability of the produced phage powders was found to be phage and formulation dependent. No further reduction in titer occurred for PEV2 powders stored at 4 °C across the study. The formulation containing 30% leucine maintained the viability of PEV2 at 20 °C, while the formulation containing 40% leucine gradually lost titer over time with a storage reduction of ∼0.9 log10 pfu/ml measured after 12 months. In comparison, the PEV40 phage powders generally had a ∼ 0.5 log10 pfu/ml loss upon storage regardless of temperature. When aerosolized, the total in vitro lung doses of PEV2 were of the order of 107 pfu, except the formulation containing 40% leucine stored at 20 °C which had a lower lung dose. The PEV40 powders also had lung doses of 106-107 pfu. The results demonstrate that spray dried Myoviridae and Podoviridae phage in a simple formulation of leucine and trehalose can be successfully stored for one year at 4 °C and 20 °C with vacuum packaging.
    Matched MeSH terms: Excipients/chemistry
  19. Microwave modified non-crosslinked pectin films with modulated drug release
    Anuar NK, Wong TW, Taib MN
    Pharm Dev Technol, 2012 Jan-Feb;17(1):110-7.
    PMID: 20958167 DOI: 10.3109/10837450.2010.522584
    The effects of microwave on drug release properties of pectin films carrying sulfanilamide (SN-P), sulfathiazole (ST-P) and sulfamerazine (SM-P) of high to low aqueous solubilities were investigated. These films were prepared by solvent evaporation technique and treated by microwave at 80 W for 5-40 min. Their profiles of drug dissolution, drug content, matrix interaction and matrix crystallinity were determined by drug dissolution testing, drug content assay, differential scanning calorimetry, X-ray diffractometry and scanning electron microscopy techniques. Microwave induced an increase in matrix amorphousness but lower drug release propensity with a greater retardation extent in SN-P films, following a rise in strength of matrix interaction. A gain in amorphous structure does not necessarily increase the drug release of film. Microwave can possibly retard drug release of pectin film carrying water-soluble drug through modulating its state of matrix interaction.
    Matched MeSH terms: Excipients/chemistry*
  20. Fulltext Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits
    Razavi M, Karimian H, Yeong CH, Chung LY, Nyamathulla S, Noordin MI
    Drug Des Devel Ther, 2015;9:4373-86.
    PMID: 26273196 DOI: 10.2147/DDDT.S86263
    The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1-F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (palmate tubers of Orchis morio), and xanthan. Post-compression studies showed that there were no interactions between the active drug and the polymers. Results of in vitro drug-release studies indicated that the F10 formulation which contained 5 mg of tamarind kernel powder, 33.33 mg of xanthan, and 61.67 mg of salep could sustain a 95% release in 12 hours. The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models. The in vivo study was performed in New Zealand White rabbits by gamma scintigraphy; the F10 formulation was radiolabeled using samarium (III) oxide ((153)Sm2O3) to trace transit of the tablets in the gastrointestinal tract. The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours. In conclusion, the use of a combination of polymers in this study helped to develop an optimal gastroretentive drug-delivery system with improved bioavailability, swelling, and floating characteristics.
    Matched MeSH terms: Excipients/chemistry*
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