فهرست مطالب

Controlled Release Journal - Volume:1 Issue: 2, 2013

Controlled Release Journal
Volume:1 Issue: 2, 2013

  • تاریخ انتشار: 1392/10/04
  • تعداد عناوین: 4
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  • Nahid Khalili, Elahe Mortazavian Koohkamar, Seyed Sajad Mohseni Salehi Monfared, Farid Abedin Dorkoosh, Morteza Rafiee-Tehrani, Bagher Larijani Page 1
  • Jaleh Varshosaz, Farshid Hassanzadeh, Hojjat Sadeghi, Mostafa Khadem Page 2
    Oral administration of insulin is an interesting route due to the fact that it is more comfortable, and because of intestinal absorption, portal drainage of insulin to liver is more physiologic than subcutaneous injection. This study evaluates the efficacy of three types of SPH polymer-based oral insulin capsules on blood glucose in patients with type I diabetes. The highest bioavailability obtained in our study was for 800 IU core outside insulin capsules in patient #2 that was calculated 1.13%. Patients that had more good response; were younger, and have shorter duration of diabetes but they have light weight and are sensitive to insulin, but patients that were resistant had long duration of diabetes and were older age.
    Keywords: SPH polymer_Oral insulin_Type I diabetes_Glucose level_case series
  • Mirzaagha Babazadeh, Maryam Sheidaei Page 3
    This research work, describes synthesis and in vitro evaluation of a serious of new acrylic type polymeric prodrugs containing 5-aminosalicylic acid (5-ASA), an important drug in the treatment of inflammatory bowel diseases, as colon targeted drug delivery systems. First, 5-ASA reacted with formic acid to obtain 5-formylaminosalicylic acid in the high yield. Reaction of the obtained material with 2-hydroxypropyl methacrylat in the presence of 1,1 carbonyldiimidazole produced methacryloyloxypropyl-5-aminosalicylate (MOPAS), as a acrylic-derivative of 5-ASA, in a one-pot procedure. The resulted MOPAS was then polymerized with hydrophilic and hydrophobic acrylic-monomers such as 2-hydroxyethyl methacrylat, methyl metacrylat or ethylhexyl acrylate by free radical polymerization method to obtain polymeric prodrugs bearing 5-ASA. All compounds were characterized by FT-IR, 1H NMR, elemental analysis and gel permeation chromatography techniques. Also, thermal behavior of the polymeric prodrugs was investigated by differential scanning calorimeter instrument. The release studies of 5-ASA were performed into dialysis bags by hydrolysis buffered solutions (pH 1, 7, 8) at 37°C. Detection of hydrolysis by UV spectroscopy at selected interval showed that the drug can be released by selective hydrolysis of the ester bond at the side of drug moiety. The release profiles indicated that the hydrolytic behavior of polymeric prodrugs is strongly based on the hydrophobicity of polymers and the pH of the hydrolysis media. The results suggested that these systems could be useful in colon targeted drug delivery systems.
    Keywords: 5, aminoslicylic acid, polymeric prodrugs, polymethacrylates, controlled release, in vitro hydrolysis
  • Bharti Sapra, Randeep Kaur, Jatin Sood, Purva Thatai, Ashok K. Tiwary Page 4
    The objective of present investigation was to formulate sustain release (SR) matrix tablets of Glipizide (GLZ) for treating type II Diabetes mellitus (T2DM). Different formulations were prepared by direct compression using Klucel HF (KLU HF) and Kollidon SR (KOL SR). Drug excipient interaction studies confirmed absence of any kind of interaction between the drug and the polymer. The powder blends were evaluated for their flow properties, compressibility, and particle size distribution. The tablets were evaluated for hardness, weight variation, friability and drug content uniformity. In vitro release of glipizide from the formulated tablets was performed in progressive pH media. These tablets were also evaluated for their swelling and erosion behaviour. Pharmacokinetic parameters of optimised formulation were compared with the immediate release and sustained release marketed formulations. Further, the formulations were evaluated for in vitro in vivo correlation and bioequivalence studies. The powder blends possessed good compressibility and flowability. The dissolution release profile demonstrated diffusion controlled release which was depicted from Higuchi and Korsmeyer Peppas model. However, swelling and erosion were also found to play profound role in the release kinetics. The in vivo studies along with in vitro in vivo correlation (IVIVC) elucidated that the optimized formulation was bioequivalent to the marketed formulation.
    Keywords: Glipizide, Klucel HF, Kollidon SR, Direct Compression, In vitro In vivo correlation