Displaying publications 1 - 20 of 151 in total

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  1. Sengupta P, Chatterjee B, Tekade RK
    Int J Pharm, 2018 May 30;543(1-2):328-344.
    PMID: 29635054 DOI: 10.1016/j.ijpharm.2018.04.007
    Different regulatory guidelines recommend establishing stability profile of pharmaceuticals at the time of drug development. The expiry date, retesting period and storage conditions of active drugs or products are established through stability analysis. Several regulatory guidelines exist for stability testing of pharmaceuticals. Mostly, ICH stability guidelines are followed in practice. This guideline recommends to validate stability indicating method using forced degradation samples that contains all possible degradation impurities. ICH guidelines provide general recommendations for inclusion of stability indicating parameters in a stability testing protocol. However, those guidelines do not provide specific requirements and experimental methodology to be followed for stability studies. Due to this gap, often confusion arises in the scientific community in designing stability testing protocol. Therefore, significant variations are observed in reported literature in selection of stability indicating parameters. Procedural dissimilarity amongst reported stability studies is also evident. This review discusses the regulatory guidelines and procedures to follow in performing stability testing of pharmaceuticals. Scope of this review also includes recommendations on practical approaches for designing stability testing protocol to fulfill current regulatory requirements for drug substances and their formulations.
    Matched MeSH terms: Chemistry, Pharmaceutical/legislation & jurisprudence*; Chemistry, Pharmaceutical/methods
  2. Ramli Musa, Mat Aris MA, Draman S, Abdullah K, Bujang MA
    MyJurnal
    All available family scales are designed for western countries and there is no validated
    family scale which is specifically devised for Asian population. The difference in culture and family values warrants the formulation of a specific Asian family scale to cater the regional needs. The objectives are to devise and validate a new family scale and eventually to validate it for Malaysian population.
    Matched MeSH terms: Chemistry, Pharmaceutical
  3. Meka VS, Gorajana A, Dharmanlingam SR, Kolapalli VR
    Invest Clin, 2013 Dec;54(4):347-59.
    PMID: 24502177
    The aim of the present research was to prepare and evaluate a gastroretentive drug delivery system for metformin HCl, using synthetic and semi-synthetic polymers. The floating approach was applied for preparing gastroretentive tablets (GRT) and these tablets were manufactured by the direct compression method. The drug delivery system comprises of synthetic and semi-synthetic polymers such as polyethylene oxide and Carboxymethyl ethyl cellulose (CMEC) as release-retarding polymers. GRT were evaluated for physico-chemical properties like weight variation, hardness, assay friability, in vitro floating behaviour, swelling studies, in vitro dissolution studies and rate order kinetics. Based upon the drug release and floating properties, two formulations (MP04 & MC03) were selected as optimized formulations. The optimized formulations MP04 and MC03 followed zero order rate kinetics, with non-Fickian diffusion and first order rate kinetics with erosion mechanism, respectively. The optimized formulation was characterised with FTIR studies and it was observed that there was no interaction between the drug and polymers.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  4. Meka VS, Songa AS, Nali SR, Battu JR, Kukati L, Kolapalli VR
    Invest Clin, 2012 Sep;53(3):223-36.
    PMID: 23248967
    The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50 degrees C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods*
  5. Nakanishi K, Sasaki S, Kiang AK, Goh J, Kakisawa H, Ohashi M, et al.
    Chem Pharm Bull (Tokyo), 1965 Jul;13(7):882-90.
    PMID: 5867816
    Matched MeSH terms: Chemistry, Pharmaceutical*
  6. Kue CS, Kamkaew A, Burgess K, Kiew LV, Chung LY, Lee HB
    Med Res Rev, 2016 Apr;36(3):494-575.
    PMID: 26992114 DOI: 10.1002/med.21387
    For the purpose of this review, active targeting in cancer research encompasses strategies wherein a ligand for a cell surface receptor expressed on tumor cells is used to deliver a cytotoxic or imaging cargo. This area of research is more than two decades old, but in those 20 and more years, how many receptors have been studied extensively? What kinds of the ligands are used for active targeting? Are they mostly naturally occurring molecules such as folic acid, or synthetic substances developed in campaigns for medicinal chemistry efforts? This review outlines the most important receptor or ligand combinations that have been used in active targeting to answer these questions, and therefore to address the most important one of all: is research in active targeting affording diminishing returns, or is this an area for which the potential far exceeds progress made so far?
    Matched MeSH terms: Chemistry, Pharmaceutical
  7. Ismail, S., Mohd Atan, K.A.
    MyJurnal
    This paper is concerned with the existence, types and the cardinality of the integral solutions for
    diophantine equation
    4 4 3
    x y z + = where x , y and z are integers. The aim of this paper was to
    develop methods to be used in finding all solutions to this equation. Results of the study show the
    existence of infinitely many solutions to this type of diophantine equation in the ring of integers
    for both cases, x y = and x y ¹ . For the case when x y = , the form of solutions is given by
    3 3 4
    ( , , ) (4 , 4 ,8 ) x y z n n n = , while for the case when x y ¹ , the form of solutions is given by
    3 1 3 1 4 1
    ( , , ) ( , , )
    k k k
    x y z un vn n
    - - -
    = . The main result obtained is a formulation of a generalized method to find
    all the solutions for both types of diophantine equations.
    Matched MeSH terms: Chemistry, Pharmaceutical
  8. Soo HL, Quah SY, Sulaiman I, Sagineedu SR, Lim JCW, Stanslas J
    Drug Discov Today, 2019 09;24(9):1890-1898.
    PMID: 31154065 DOI: 10.1016/j.drudis.2019.05.017
    Andrographolide (AGP), a naturally occurring bioactive compound, has been investigated as a lead compound in cancer drug development. Its multidimensional therapeutic effects have raised interest among medicinal chemists, which has led to extensive structural modification of the compound, resulting in analogues with improved pharmacological and pharmaceutical properties. Nevertheless, the analogues with the improved properties need to be rigorously studied to identify drug-like lead compounds. We scrutinised articles published from 2012 to 2018, to objectively provide opinions on the mechanisms of action of AGP and its analogues, as well as their potential as viable anticancer drugs. Preclinical and clinical data, along with the extensive medicinal chemistry efforts, indicate the compounds are potential anticancer agents with specific value in treating recalcitrant cancers such as pancreatic and lung cancers.
    Matched MeSH terms: Chemistry, Pharmaceutical
  9. Sivakumar M, Tang SY, Tan KW
    Ultrason Sonochem, 2014 Nov;21(6):2069-83.
    PMID: 24755340 DOI: 10.1016/j.ultsonch.2014.03.025
    Novel nanoemulsion-based drug delivery systems (DDS) have been proposed as alternative and effective approach for the delivery of various types of poorly water-soluble drugs in the last decade. This nanoformulation strategy significantly improves the cell uptake and bioavailability of numerous hydrophobic drugs by increasing their solubility and dissolution rate, maintaining drug concentration within the therapeutic range by controlling the drug release rate, and reducing systemic side effects by targeting to specific disease site, thus offering a better patient compliance. To date, cavitation technology has emerged to be an energy-efficient and promising technique to generate such nanoscale emulsions encapsulating a variety of highly potent pharmaceutical agents that are water-insoluble. The micro-turbulent implosions of cavitation bubbles tear-off primary giant oily emulsion droplets to nano-scale, spontaneously leading to the formation of highly uniform drug contained nanodroplets. A substantial body of recent literatures in the field of nanoemulsions suggests that cavitation is a facile, cost-reducing yet safer generation tool, remarkably highlighting its industrial commercial viability in the development of designing novel nanocarriers or enhancing the properties of existing pharmaceutical products. In this review, the fundamentals of nanoemulsion and the principles involved in their formation are presented. The underlying mechanisms in the generation of pharmaceutical nanoemulsion under acoustic field as well as the advantages of using cavitation compared to the conventional techniques are also highlighted. This review focuses on recent nanoemulsion-based DDS development and how cavitation through ultrasound and hydrodynamic means is useful to generate the pharmaceutical grade nanoemulsions including the complex double or submicron multiple emulsions.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods*
  10. Al-Amiery AA, Musa AY, Kadhum AA, Mohamad AB
    Molecules, 2011 Aug 10;16(8):6833-43.
    PMID: 21832973 DOI: 10.3390/molecules16086833
    New coumarin derivatives, namely 7-[(5-amino-1,3,4-thiadiazol-2-yl)methoxy]-2H-chromen-2-one, 5-[(2-oxo-2H-chromen-7-yloxy)methyl]-1,3,4-thiadiazol-2(3H)-one, 2-[2-(2-oxo-2H-chromen-7-yloxy)acetyl]-N-phenylhydrazinecarbothioamide, 7-[(5-(phenylamino)-1,3,4-thiadiazol-2-yl)methoxy]-2H-chromen-2-one and 7-[(5-mercapto-4-phenyl-4H-1,2,4-triazol-3-yl)methoxy]-2H-chromen-2-one were prepared starting from the natural compound umbelliferone. The newly synthesized compounds were characterized by elemental analysis and spectral studies (IR, ¹H-NMR and ¹³C-NMR).
    Matched MeSH terms: Chemistry, Pharmaceutical/methods*
  11. 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: Chemistry, Pharmaceutical/methods
  12. Kam TS, Lim KH
    Alkaloids Chem Biol, 2008;66:1-111.
    PMID: 19025097
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  13. Oladzadabbasabadi N, Ebadi S, Mohammadi Nafchi A, Karim AA, Kiahosseini SR
    Carbohydr Polym, 2017 Mar 15;160:43-51.
    PMID: 28115099 DOI: 10.1016/j.carbpol.2016.12.042
    The aim of this study was development a composite film based on sago starch and κ-carrageenan to find a gelatin alternative in the pharmaceutical capsules processing. Hydrolyzed-Hydroxypropylated (dually modified) sago starch was mixed with κ-carrageenan (0.25, 0.5, 0.75, and 1%). The drying kinetics, thermomechanical, physicochemical, and barrier properties of composite films were estimated and compared with bovine gelatin. Results show that drying kinetics and mechanical properties of the composite films were comparable to those of gelatin. The water vapor permeability and moisture content of the composite films were lower than those of gelatin. The solubility of the composite films was higher than that of gelatin, and the composite films were more stable at higher relative humidity than were the gelatin films. These results show that dually modified sago starch in combination with κ-carrageenan has properties similar to those of gelatin, thus proposed system can be used in pharmaceutical capsules processes.
    Matched MeSH terms: Chemistry, Pharmaceutical*
  14. Mahesparan VA, Bin Abd Razak FS, Ming LC, Uddin AH, Sarker MZI, Bin LK
    Int J Pharm Compd, 2020 3 21;24(2):148-155.
    PMID: 32196477
    Orodispersible tablets disintegrate rapidly (within 3 minutes) in the oral cavity and release the medicament before swallowing. The mode of disintegrant addition might affect the properties of orodispersible tablets. The objective of this study was to formulate and evaluate orodispersible tablets by studying different modes of disintegration addition with varying concentrations of disintegrants. The wet granulation method was used to produce the orodispersible tablets. Two methods of disintegration addition were compared (i.e., intragranular, extragranular). Three disintegrants (i.e., cornstarch, sodium starch glycolate, crospovidone) were used at three levels (5%, 10%, and 15%) in the study. The formulations were tested for the powder flowability (angle of repose) and characterized physically (hardness, weight, thickness, friability, disintegration time). The mangosteen pericarp extract was used as a model active pharmaceutical ingredient to be incorporated into the optimum formulation. It was observed that the extragranular method produced granules with better flowability compared to that of the intragranular method. Crospovidone was found as the most efficient disintegrant among the three. The optimum formulation selected was one with the highest concentration of crospovidone (15%), which showed the fastest disintegration time. The mode of disintegrant addition into the orodispersible tablets formulation was found to show a marked difference in the disintegration, as well as other physical characteristics of the orodispersible tablets where the extragranular mode of addition showed better property, which caused the orodispersible tablets to disintegrate the fastest.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  15. Samiun WS, Ashari SE, Salim N, Ahmad S
    Int J Nanomedicine, 2020;15:1585-1594.
    PMID: 32210553 DOI: 10.2147/IJN.S198914
    Background: Aripiprazole, which is a quinolinone derivative, has been widely used to treat schizophrenia, major depressive disorder, and bipolar disorder.

    Purpose: A Central Composite Rotatable Design (CCRD) of Response Surface Methodology (RSM) was used purposely to optimize process parameters conditions for formulating nanoemulsion containing aripiprazole using high emulsification methods.

    Methods: This design is used to investigate the influences of four independent variables (overhead stirring time (A), shear rate (B), shear time (C), and the cycle of high-pressure homogenizer (D)) on the response variable namely, a droplet size (Y) of nanoemulsion containing aripiprazole.

    Results: The optimum conditions suggested by the predicted model were: 120 min of overhead stirring time, 15 min of high shear homogenizer time, 4400 rpm of high shear homogenizer rate and 11 cycles of high-pressure homogenizer, giving a desirable droplet size of nanoemulsion containing aripiprazole of 64.52 nm for experimental value and 62.59 nm for predicted value. The analysis of variance (ANOVA) showed the quadratic polynomial fitted the experimental values with F-value (9.53), a low p-value (0.0003) and a non-significant lack of-fit. It proved that the models were adequate to predict the relevance response. The optimized formulation with a viscosity value of 3.72 mPa.s and pH value of 7.4 showed good osmolality value (297 mOsm/kg) and remained stable for three months in three different temperatures (4°C, 25°C, and 45°C).

    Conclusion: This proven that response surface methodology is an efficient tool to produce desirable droplet size of nanoemulsion containing aripiprazole for parenteral delivery application.

    Matched MeSH terms: Chemistry, Pharmaceutical/methods
  16. 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: Chemistry, Pharmaceutical/methods
  17. Saiful Bahri, S., Wan Rosli, W. l.
    MyJurnal
    The influence of oyster mushroom (pleurotus sajor-caju, PSC) powder on the physical
    properties of herbal seasoning (HS) was investigated. The pH, total solid, viscosity, rheology
    and texture of semi solid HS containing different PSC powder level (0%, 20%, 40%, 60%,
    8%, 100% w/w) of coconut milk powder were measured. The pH of the products were in the
    range of 4.05 - 4.15. Rheological behavior was characterized by oscillatory rheometry. Stress
    sweep, frequency sweep and steady stress experiments were conducted to study the behavior
    of the products. The products showed non Newtonian characteristic or shear thinning. All
    samples were G’> G’’ showed the gel like network. In addition, the back extrusion rig texture
    analysis showed the correlation among the samples were also studied. Total substitution of PSC
    powder (100% w/w) in the formulation resulted more viscous product and the combination
    of the coconut milk powder and PSC powder showed the best spreadability and flow to the
    product characteristics. No added PSC powder (0% w/w) showed the least viscous products
    and the less moduli among the samples studied. The present study suggested the incorporation
    of more than 40% PSC powder to replace coconut milk powder give better flowability and not
    affect the viscosity of the products.
    Matched MeSH terms: Chemistry, Pharmaceutical
  18. Muniroh, M.F., Ismail, N., Lazim, M.A.
    MyJurnal
    Combining forecast values based on simple univariate models may produce more favourable results than complex models. In this study, the results of combining the forecast values of Naïve model, Single Exponential Smoothing Model, The Autoregressive Moving Average (ARIMA) model, and Holt Method are shown to be superior to that of the Error Correction Model (ECM).Malaysia’s unemployment rates data are used in this study. The independent variable used in the ECM formulation is the industrial production index. Both data sets were collected for the months of January 2004 to December 2010. The selection criteria used to determine the best model, is the Mean Square Error (MSE), Root Mean Squared Error (RMSE) and Mean Absolute Percentage Error (MAPE). Initial findings showed that both time series data sets were not influenced by the seasonality effect.
    Matched MeSH terms: Chemistry, Pharmaceutical
  19. Hand RM, Senarathna SMDKG, Page-Sharp M, Gray K, Sika-Paotonu D, Sheel M, et al.
    Pharmacol Res Perspect, 2020 12;8(6):e00668.
    PMID: 33090729 DOI: 10.1002/prp2.668
    Benzathine penicillin G (BPG) is used as first-line treatment for most forms of syphilis and as secondary prophylaxis against rheumatic heart disease (RHD). Perceptions that poor quality of BPG is linked to reported adverse effects and therapeutic failure may impact syphilis and RHD control programs. Clinical networks and web-based advertising were used to obtain vials of BPG from a wide range of countries. The quality of BPG was assessed using a high performance liquid chromatography assay capable of detecting relevant impurities and degradation products. Tests for water content, presence of heavy metals and physical characteristics of BPG, including particle size analysis and optical microscopy, also were conducted. Thirty-five batches of BPG were sourced from 16 countries across 4 WHO regions. All batches passed the US Pharmacopeia requirements for BPG injection (content), with no evidence of breakdown products or other detected contaminants. Water content and heavy metal analysis (n = 11) indicated adherence to regulatory standards and Good Manufacturing Practice. Particle size analysis (n = 20) found two batches with aggregated particles (>400 µm) that were dispersed following sonication. Current batches of BPG were of satisfactory pharmaceutical quality but aggregated particles were found in a modest proportion of samples. Future studies should focus on the physical characteristics of BPG which may contribute to variations in plasma penicillin concentrations an observed needle blockages in clinical practice. Pharmacopeial monographs could be revised to include standards on particle size and crystal morphology of BPG.
    Matched MeSH terms: Chemistry, Pharmaceutical/methods; Chemistry, Pharmaceutical/standards*
  20. Karim S, Baie SH, Hay YK, Bukhari NI
    Pak J Pharm Sci, 2014 May;27(3):425-38.
    PMID: 24811797
    Pelletized dosage forms can be prepared by different methods which, in general, are time consuming and labor intensive. The current study was carried out to investigate the feasibility of preparing the spherical pellets of omeprazole by sieving-spheronization. An optimized formulation was also prepared by extrusion-spheronization process to compare the physical parameters between these two methods. The omeprazole pellets were consisted of microcrystalline cellulose, polyvinylpyrrolidone K 30, sodium lauryl sulphate and polyethylene glycol 6000. The omeprazole delay release system was developed by coating the prepared pellets with aqueous dispersion of Kollicoat 30 DP. The moisture content, spheronization speed and residence time found to influence the final properties of omeprazole pellets prepared by extrusion-spheronization and sieving-spheronization. The Mann-Whitney test revealed that both methods produced closely similar characteristics of the pellets in terms of, friability (p=0.553), flowability (p=0.677), hardness (p=0.103) and density (bulk, p=0.514, tapped, p=0.149) except particle size distribution (p=0.004). The percent drug release from the coated formulation prepared by sieving-spheronization and extrusion spheronization was observed to be 84.12 ± 1.10% and 82.67 ± 0.96%, respectively. Dissolution profiles of both formulations were similar as indicated by values of f1 and f2, 1.52 and 89.38, respectively. The coated formulation prepared by sieving-spheronization and commercial reference product, Zimore ® also showed similar dissolution profiles (f1=1.22, f2=91.52). The pellets could be prepared using sieving-spheronization. The process is simple, easy, less time- and labor-consuming and economical as compared to extrusion-spheronization process.
    Matched MeSH terms: Chemistry, Pharmaceutical
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