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Journal of Excipients and Food Chemicals
  This is an Open Access Journal Open Access journal
     ISSN (Print) 21502668
     Published by International Pharmaceutical Excipients Council Homepage  [1 journal]
  • An alternative approach to adjustment of the level of incorporation of
           boundary lubricants to accommodate changes in granule or blend

    • Authors: Richard Christian Moreton
      Abstract: A method is proposed whereby the determination of the level of incorporation of a boundary lubricant is based on the surface area of the blend or granulation and the shape of the lubricant particles. This is a more logical approach to the lubrication of blends and granulations for the manufacture of solid oral dosage forms than the percentage by weight approach that has traditionally been used. Equations are provided to allow the adjustment of the level of incorporation of the boundary lubricant based on the variation in the surface area of the granulation or blend. This method has potential application in the manufacture of solid oral dosage forms by both batch and continuous processing. The concept of lubricant coverage is relevant to the development of solid oral dosage forms using Quality by Design principles, since certain changes in the granulation or blend characteristics on scale-up would be compensated for, and the use of grade bracketing strategies would be facilitated.
      PubDate: 2014-03-31
      Issue No: Vol. 5 (2014)
  • Future of Tableting Technology

    • Authors: Abu T. M. Serajuddin
      PubDate: 2014-03-31
      Issue No: Vol. 5 (2014)
  • Quantification of clarithromycin polymorphs in presence of tablet

    • Authors: Swathi Kuncham, Ganesh Shete, Arvind Kumar Bansal
      Abstract: Characterization of solid form of API in presence of excipients offers considerable challenge. Aim of the present study was to quantify polymorphs of clarithromycin (CAM) in a commercial tablet in the presence of excipients, by powder X-ray diffraction (PXRD) method. Polymorphic Form I (CAM-1), Form II (CAM-2) and amorphous phase of CAM were characterized using thermal and crystallographic tools. CAM-1 and CAM-2 were found to be monotropically related, with CAM-2 being the stable form. PXRD instrument related parameters were optimized for characterization of CAM polymorphic forms in a mixture of excipients. Calibration curves for CAM-1 and CAM-2 were prepared in a mixture with excipients. Analytical method based on differences in diffraction pattern of CAM-1, CAM-2 and excipients was developed. Sodium methyl paraben, sodium propyl paraben, microcrystalline cellulose and magnesium stearate were crystalline and exhibited characteristic diffraction pattern. Starch, croscarmellose sodium, talc and sodium starch glycolate were found to be semicrystalline in nature while colloidal silicon dioxide was amorphous material. Diffraction peak at 8.7° 2θ value allowed quantification of CAM-2 in the presence of excipients. The analytical method was evaluated and validated for accuracy, precision, inter and intraday variation, variability due to sample repacking and instrument reproducibility. The method for quantification of CAM-2 in the range of 80 to 100% w/w was found to be linear with R2 = 0.998.  Relative standard deviation (RSD) due to sample repacking was 2.77% indicating good homogeneity of mixing of samples. RSD due to all assay errors was found to be 1.66%. PXRD analysis of commercial tablet revealed presence of CAM-2 as major polymorph and it was found to be 98% of the overall content of API. CAM-1 was found to be present as an impurity in trace amount as evidenced by peaks at 2θ values of 5.2° and 6.7°. This method allows characterization of polymorphic forms of CAM in presence of common tablet excipients. It can be a useful tool for monitoring solid form behavior during product development and stability studies. 
      PubDate: 2014-03-31
      Issue No: Vol. 5 (2014)
  • Investigation of thermal and viscoelastic properties of polymers relevant
           to hot melt extrusion, II: Cellulosic polymers

    • Authors: Anuprabha Meena, Tapan Parikh, Simerdeep Singh Gupta, Abu T. M. Serajuddin
      Abstract: The purpose of the study was to evaluate the thermal and viscoelastic properties of cellulosic polymers commonly used in hot melt extrusion (HME). Cellulose ethers of different molecular weight (MW) with varied degree of substitution and functional groups were analyzed using modulated differential scanning calorimetry (MDSC), thermogravimetric analysis (TGA) and oscillatory rheometry. The results indicate that glass transition temperature (Tg) and viscoelastic characteristics of polymers strongly depend on their chain length, MW, and degree and type of substitutions in the main chain. In general, an increase in chain length or MW was found to increase Tg as well as the viscosity (HPMC, MW10000 < MW 25000 < MW 150000). Also, substitutions with bulkier groups decrease the Tg and viscosity of the polymer. Most of the cellulosics were found to have high viscosity between their Tg and degradation temperature (Td), and thus cannot be extruded by themselves. The thermal properties in combination with polymer viscosity at different temperature will help formulators determine processability using HME.
      PubDate: 2014-03-31
      Issue No: Vol. 5 (2014)
  • Investigation of thermal and viscoelastic properties of polymers relevant
           to hot melt extrusion, III: polymethacrylates and polymethacrylic acid
           based polymers

    • Authors: Tapan Parikh, Simerdeep Singh Gupta, Anuprabha Meena, Abu T. M. Serajuddin
      Abstract: Polymers serve as major constituents of drug products prepared by hot melt extrusion (HME) and hence it is necessary to understand their behavior under heat and mechanical stress for the development of successful HME processes. The aim of this work was to generate a database of physicochemical properties for polymethacrylates and polymethacrylic acid based polymers relevant to HME. Only neat polymers were used and no drug or plasticizers were added. All six polymers used were amorphous and had < 2% moisture.  In differential scanning calorimetric (DSC) studies, the three homo block copolymers, Eudragit® E PO, Eudragit® RL PO and Eudragit® RS PO, had glass transition temperatures (Tg) of 57 °C, 63 °C and 64 °C respectively, and in thermogravimetric analysis (TGA) they showed weight loss due to thermal degradation at 250 °C, 166 °C and 170 °C, respectively. Thermomechanical analysis was conducted to investigate rheological properties of the polymers, which predicted their melt extrusion ranges to be 127-150 °C, 165-170 °C, and 142-167 °C respectively. In contrast, the hetero block copolymers: Eudragit® L 100, Eudragit® S 100 and Eudragit® L 100-55 had Tg of 195 °C, 173 °C, and 111 °C, respectively, and onsets of their degradation, as measured by TGA, were in the range of 173-176 °C. The predicted HME processing temperatures of Eudragit® L 100, Eudragit® S 100 and Eudragit® L 100-55 were greater than 200 °C and hence these polymers should not be processed as it is.
      PubDate: 2014-03-31
      Issue No: Vol. 5 (2014)
  • Moisture Adsorption and Desorption Properties of Colloidal Silicon Dioxide
           and Its Impact on Layer Adhesion of a Bilayer Tablet Formulation

    • Authors: Jennifer Wang
      Abstract: A bilayer tablet formulation approach was used to develop a fixed dose combination tablet formulation of drugs Y & Z.  The weight of Layer-I containing Drug Y and the weight of Layer -II A or II B containing Drug Z were 250 mg and 1280 mg, respectively.  While layer-I was manufactured using the dry granulation method, Layer -II A and II B were manufactured using the moisture activated dry granulation (MADG) process. Layer II A and Layer II B contained 3% w/w colloidal silicon dioxide with the surface area of 300 m2/g (Aeroperl® -300) and  200 m2/g (Aerosil® -200), respectively, as moisture scavenger , and the rest of the common excipients. Both grades of silicon dioxide were amorphous. The change in grade of silicon dioxide did not alter the compaction behavior of the tablet formulation. When exposed to open 40°C/75%RH for 72 hours, the bilayer tablet consisting of Layers I/Layer II A (containing Aeroperl-300) showed a clear layer separation while tablet consisting of Layers I/Layer II B (containing Aerosil-200) did not. When the individual layer was exposed to similar condition, the water absorption for Layer I, Layer II A, and Layer II B, was 345% w/w, 107% w/w, and 184% w/w, respectively. Thus, the difference in water absorption was higher between Layer I/ Layer II A (containing Aeroperl-300) than Layer I/Layer II B (containing Aerosil-200) leading to more significant shear stress at the layer interface.  The moisture adsorption-desorption isotherms, pore size distributions, mercury intrusion porosimetry (MIP) and scanning electron microscopy (SEM) for both grades of silicon dioxide suggested that Aeroperl 300 containing small pores (Layer II A) did not retain water while Aerosil 200 (Layer II B) containing large pores did.  It is hypothesized that in spite of its lower surface area, the retained water of Aerosil 200 provided better binding and cohesion to layers, thus minimizing the layer separation.
      PubDate: 2014-03-31
      Issue No: Vol. 5 (2014)
  • Investigation of thermal and viscoelastic properties of polymers relevant
           to hot melt extrusion, I: Polyvinylpyrrolidone and related polymers

    • Authors: Simerdeep Singh Gupta, Anuprabha Meena, Tapan Parikh, Abu T. M. Serajuddin
      Abstract: Polymers are essential components of melt extruded products. The objective of the paper was to generate physicochemical data on polyvinylpyrrolidone-based polymers and copolymers that are relevant to hot melt extrusion (HME). It also highlights the importance of viscoelastic analysis to predict HME processing conditions. Powder X-ray diffraction (XRD) patterns of polymers were recorded to determine the physical nature of polymers. Differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) were conducted to determine their glass transition temperature (Tg) and weight loss due to degradation (Td) respectively. Rheological studies were conducted to quantitate storage modulus (G´), loss modulus (G˝), tan δ and complex viscosity (η) of the polymers at various temperatures. Powder XRD analyses showed that all polymers were amorphous in nature, with distinct single or dual halos. DSC ascertained that the amorphous polymers had single Tg values. The conversion of the polymers from solid to liquid forms with an increase in temperature was established by the tan δ = 1 values. The overall complex viscosity for all polymers decreased with an increase in temperature. The complex viscosity of one of the polymers, Soluplus®, was correlated with torque analysis by HME to establish an extrudable temperature range. The results will help the selection of polyvinylpyrrolidone-based polymers for HME.
      PubDate: 2014-03-31
      Issue No: Vol. 5 (2014)
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