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Journal of Excipients and Food Chemicals
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  This is an Open Access Journal Open Access journal
     ISSN (Print) 21502668
     Published by International Pharmaceutical Excipients Council Homepage  [1 journal]
  • The variation of the activity of Xenobiotic metabolizing enzymes with
           latitude as a potential factor in determining the course of history.

    • Authors: Shireesh Apte
      Abstract: None
      PubDate: 2014-06-25
      Issue No: Vol. 5 (2014)
       
  • Decreasing the rate of delamination of pharmaceutical glass containers

    • Authors: Shireesh Apte
      Abstract: None
      PubDate: 2014-06-25
      Issue No: Vol. 5 (2014)
       
  • Understanding interactions of oleic acid with basic drugs in solid lipids
           on different biopharmaceutical levels

    • Authors: Zdravka Misic, Dubravka Šišak Jung, Georg Sydow, Martin Kuentz
      Abstract: Recently, the impact of intestinal supersaturation on absorption of poorly water-soluble drugs has raised much interest among researchers. A focus has been mostly to study excipient effects on maintenance of drug supersaturation. The aim of the present study was to better understand the effects of drug-excipient interactions on the level of the anhydrous formulation, upon dispersion in simple buffer media and, in particular, regarding precipitation kinetics. A solid lipid-based formulation comprising PEG-32 stearate and oleic acid (OA) (8:2 w/w) was developed as a model. Loratadine (pKa = 4.33) and carvedilol (pKa = 8.74) were chosen as basic drugs. UV/FTIR spectroscopy and viscometry were used to characterize drug-OA molecular interactions in solution, while solid formulations were studied using x-ray diffraction, thermal analysis and van’t Hoff solubility-temperature plots. Precipitation kinetics of drug formulations was real-time monitored in phosphate buffer (pH = 6.5) by focused beam reflectance measurements. It was found that the addition of OA in the formulations resulted in substantial drug solubility increase. Although the drug-OA interactions appeared to be partially lost upon formulation dispersion, the extent of precipitation was markedly lowered compared to the formulations without OA. A Precipitation number (Pnc) was introduced as a ratio of a relevant residence time of drug in the gastrointestinal tract (GIT) to the induction time (the onset time of crystalline precipitation). Without OA, Pnc was already taking critical values (>1), while the anhydrous formulation was still below saturation for both model drugs. Interestingly, the addition of OA resulted in amorphous instead of crystalline precipitates, which is advantageous for drug re-dissolution and absorption. In conclusion, this study provides an improved understanding of OA and basic drug interactions on different levels of in vitro performance for more rational oral formulation development.
      PubDate: 2014-06-25
      Issue No: Vol. 5 (2014)
       
  • Evaluation of new aroma substances for feline minitablet formulation

    • Authors: Jaana Hautala, Sari Airaksinen, Noora Naukkarinen, Outi Vainio, Anne Mari Juppo
      Abstract: Despite the global interest in companion animal pharmaceuticals, feline peroral medication still lacks tailor-made, palatable and voluntarily accepted pharmaceuticals with suitable size and attractive taste. As a consequence, treating cats with canine and even human pharmaceuticals has weakened patient compliance and treatment commitment, and has even left many pet cats untreated. In future, the companion animal pharmaceutical business will therefore particularly concentrate on cats and the rapid and economic development of palatable feline medication. Following this goal, the overall aim of this study was to facilitate voluntary drug administration to felines. Specifically we aimed to develop sophisticated and tailor-made feline pharmaceuticals, with the focus on flavours in minitablets. Since excipients should be easily obtained and suitable for formulation, we conducted rapid preformulation compatibility and stability screening tests of synthetic flavours with commonly used tableting excipients. On the basis of the feline carnivorous diet, L-methionine, L-leucine, L-proline and thiamine hydrochloride were presented as new aroma substances for the improvement of feline medication palatability. These flavours and a model substance for a bitter taste, denatonium benzoate, were systematically evaluated for their physicochemical properties, stability and physical compatibility. This was done with substances alone and in binary combinations of flavours and excipients. Stability and compatibility were examined employing DSC and XRPD. The results showed that L-proline and denatonium benzoate anhydrate were hygroscopic. Thiamine hydrochloride was incompatible with talc and sodium stearyl fumarate. The known incompatibility between the amines contained in aromas, and α-lactose monohydrate was used in assessing method sensitivity. Overall, the study provided new information on the compatibility of novel aromas with the tableting excipients. The study also demonstrated the applicability of XRPD and DSC in the rapid evaluation of instability and incompatibility.
      PubDate: 2014-06-25
      Issue No: Vol. 5 (2014)
       
  • Absorption Enhancing Excipients in Systemic Nasal Drug Delivery

    • Authors: Edward T. Maggio
      Abstract: Intranasal drug delivery is becoming an increasingly important form of drug administration for chronic and chronic-intermittent diseases. Important new applications in development include drugs for diabetes, osteoporosis, obesity, certain types of convulsive disorders, migraine headaches, symptomatic pain relief, nausea, and anxiety, among others. Transmucosal absorption across the nasal mucosa is generally limited to molecules under 1,000 Da in size. Systemic delivery of molecules larger than this requires formulation with a suitable transmucosal absorption enhancer. More than one hundred potential transmucosal absorption enhancing excipients have been tested to date.  Nearly all have failed to be practical due to poor effectiveness or unacceptable toxicity to mucosal tissue. Alkylsaccharides, cyclodextrins, and chitosan's have emerged as the leading candidates for potential broad clinical applications and are allowing development of convenient, patient-friendly, needle free formulations of small molecule drugs, as well as peptide and protein drugs that can be administered at home, at work, or in other public and private settings outside of the doctor’s office or hospital environment.
      PubDate: 2014-06-25
      Issue No: Vol. 5 (2014)
       
  • Chitosan and Xanthan Gum Mixtures as Excipient for Controlled Release of
           Ambroxol HCl: In- vitro drug Release and Swelling Behavior

    • Authors: Faisal Al-Akayleh, Mayyas Al Remawi, Mutaz S. Salem, Adnan Badwan
      Abstract: Abstract   Directly compressed matrices were produced using binary mixture of different chitosan (CH) and xanthan gum (XG) ratios. These hydrophilic excipients were used to control the release of ambroxol HCl. Three CH to XG ratios were investigated namely: 1:1, 1:4 and 4:1. Mucosolvan LA® was used as a reference commercial product.  The optimal CH to XG ratio was 1:1 and the optimal drug to polymer mixture ratio was 1:3. Matrix erosion, hydration and drug release study were carried out using a dissolution apparatus (basket method). The mechanism of release was discussed.
      PubDate: 2014-06-25
      Issue No: Vol. 5 (2014)
       
 
 
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