Formulations 2019: Statistical Optimization & In-Vitro Evaluation of Beta Cyclodextrin Complexed Oral Matrix Tablet of Class-II Drug Glipizide for the treatment of Diabetes mellitus - Rajesh Jagtap - Annasaheb Dange College of B. Pharmacy

Glipizide, an oral hy-poglycemic agent used in the treatment of non-insulin established diabetes mellitus which belongs to Class II of BCS changed into complexed with HP-β-CD so as to enhance its solubility. Glipizide is a short-acting, second-era sulfonylurea with hypoglycemic activity.  Glipizide is swiftly absorbed, has a very quick onset of movement and a brief half-existence. Glipizide is white in colour, odourless powder having a pKa of 5.9.   It is insoluble in water and alcohols and soluble in 0.1 N NaOH. It is freely soluble in dimethylformamide. This agent is drastically metabolized in the liver and the metabolites as well as the unchanged form are excreted within the urine. Glipizide is an N-sulfonylurea this is glyburide wherein the (5-chloro-2-methoxybenzoyl group is replaced through a (5-methylpyrazin-2-yl)carbonyl group. An oral hypoglycemic agent, it's far used inside the treatment of kind 2 diabetes mellitus. It has a role as a hypoglycemic agent, an EC (pantothenate kinase) inhibitor and an insulin secretagogue. It is a N-sulfonylurea, a member of pyrazines, an aromatic amide and a monocarboxylic acid amide.

According to the 2018 Clinical Practice Guidelines by way of Diabetes Canada, sulfonylurea tablets are taken into consideration a second-line glucose-decreasing remedy following  Because sulfonylureas require practical pancreatic beta cells for their healing effectiveness, sulfonylureas are extra usually used for early-stage type 2 diabetes while there can be no progressed pancreatic compared to the first-era sulfonylureas, which includes tolbutamide and chlorpropamide, second-technology sulfonylureas incorporate a more non-polar factor chain of their chemical structure, which   Compared to special participants of the sulfonylurea drug group, glipizide presentations fast absorption and onset of movement with the shortest half-existence and length of movement, decreasing the danger for long-lasting hypoglycemia this is often observed with blood glucose-reducing Glipizide became first approved by way of the usage of the FDA in 1994 and is available in extended-launch  tablets below the logo call Glucotrol®, as well as in aggregate with metformin under the brand  The complexes of glipizide with HP-β-CD were prepared by using Physical mixing, Co-grinding and kneading strategies and had been characterized and evaluated to take a look at the effect of complexation on dissolution Fourier redesign infrared spectroscopy, X-ray diffraction, Differential scanning calorimetry, and Scanning electron microscopy indicated stronger drug amorphization and entrapment in   Phase solubility studies have been labeled as AL type characterized with the aid of apparent 1:1 stability regular that had a cost 582.forty eight M-1 in Fourier remodel infrared spectroscopy, X-ray diffraction, Differential scanning calorimetry, and Scanning electron microscopy indicated stronger drug amorphization and entrapment in HP-β-CD.

Phase solubility research have been performed according to technique reported by using Higuchi and Connors which become labelled as AL kind characterized by obvious 1:1 stability regular that had a price 582.48 eight phosphate buffer by means of dissolving 28.20 g of disodium hydrogen phosphate and 11.forty five g of potassium dihydrogen phosphate in sufficient water to provide a thousand ml to present 6.eight PH. Remarkable improvement turned into observed within the In-vitro drug release profiles in 0.1N HCl and phosphate buffer pH 6.8 with all complexes. 

Fourier-transform infrared spectroscopy (FTIR) is an method used to obtain an IR spectrum of absorption or emission of a solid, liquid or gases samples.  An FTIR spectrometer concurrently collects high-spectral-resolution data over a wide spectral range.  DSC is a thermal analysis technique wherein the warmness flow into or out of a pattern is measured as a feature of temperature or time, while the pattern is uncovered to a managed temperature program.  DSC may be Power-compensated DSC in which energy supply remains consistent or Heat-flux DSC wherein warmness flux remains steady. FTIR and DSC studies showed the formation of inclusion complex. The basic principle underlying this technique is that after the sample undergoes a bodily transformation such as section transitions, more or less warmth will need to glide to it than the reference to maintain both at the same temperature.  Whether much less or more warmth have to glide to the pattern depends on whether the system is exothermic or endothermic.


 Dissolution study of inclusion complex confirmed that β-cyclodextrin is useful for enhancing the solubility and drug dissolution. A 32 full factorial design was employed to prepare HPMC K100 M and Xanthan Gum matrix tablet containing inclusion complex equivalent to 10 mg Glipizide. Swelling study of tablet shows that, water uptake was continuously increasing with time and the radial and axial expansion was almost constant after 12 hour. The curve-fitting data indicated that the possible mechanism of drug release would be diffusion, as most of the batches produced yielded quality adjustment with the Higuchi model (average R2=0.9732). However, the best fit model was found to be the Korsmeyer-Peppas model (average R2 =0.9912), suggesting that the mechanism of drug release was combination of diffusion and erosion. The mathematical models generated employing regression analysis and ANOVA were found to be valid, these studies showed that complexation was found to exert a significant effect (P <0.05) on drug release (Y1, Y2 and Y3) as well as the release mechanism (Y4). The variables X1, X2 and X1X2 were found to be significant for Y1, Y2 , Y3 and Y4.



Rajesh Jagtap has completed his M. Pharmacy from Department of Pharmaceutics, Poona District Education Association’s, Seth Govind Raghunath Sable college of Pharmacy, Saswad Savitribai Phule University of Pune and registered for Ph D at Shivaji University Kolhapur under faculty of Engineering and Technology (Pharmacy). He is working as an Assistant Professor at Annasaheb Dange college of Pharmacy Saswad & he is having 10 year teaching experience. He has published more than 15 papers in reputed national & international journals and also presented more than 10 papers in national & international conference.

Author(s): Rajesh Jagtap

Abstract | PDF

Share this  Facebook  Twitter  LinkedIn  Google+
Flyer image
Abstracted/Indexed in
  • Google Scholar
  • The Global Impact Factor (GIF)
  • China National Knowledge Infrastructure (CNKI)
  • CiteFactor
  • Open Academic Journals Index (OAJI)
  • Directory of Research Journal Indexing (DRJI)
  • Publons
  • Secret Search Engine Labs