Formulation Development to Enhance the Solubility of Metoclopramide Base Drug by Solid Dispersion and Evaluation of Transdermal Film

  • Goutam Mukhopadhyay Associated Professor, Department of Pharmaceutical Technology, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127
  • Rahul Mukhopadhyay Assistant Professor, Department of Pharmaceutical Technology, Brainware university, 398, Ramkrishnapur Road, Near Jagadighata Market, Barasat, Kolkata, West Bengal 700124
  • Ankita Mukhopadhyay Assistant Professor, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127.
  • Shymodip Kundu Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127
  • Banerjee Shreya Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127
  • Debasmita Manna Student, Department of Pharmacy, NSHM Knowledge campus, 124 BL Saha Road, Kolkata-700053.
  • Argha Sarkar Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127
  • Tarique Nazar Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127
  • Srotoswini Sarkar Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127
  • Sauris Bala Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Abstract

Aims & Objectives: The present work deals with the modification of controlled release dosage form of poorly water soluble drug (Metoclopramide hydrochloride) in order to improve the bioavailability and to control drug release for a longer period of time by the aid of solid dispersion.


Methods: Various binary combination of MET-solid dispersion was prepared with different carriers such as HPβCD, PVP K30 and PLX-188 by solvent evaporation technique and then the aqueous solubility, dissolution study and phase solubility study was performed. DSC analysis is performed to carry out for metoclopramide loaded solid dispersion, physical mixture & also for pure drug to analyze the crystalline and amorphous nature of compounds.


Results and Discussion:  The saturation solubility of Metoclopramide with various carriers at different pH was performed and found that in pH 5.5 (solubility is 5553.2µg/ml), pH 6.8 (3363.3µ/ml), pH 7.4 (1367.3µg/ml) at 37oC. In dissolution study of solid dispersion (5:1) of different carriers in DDW, the Cumulative % dissolution is found in the order of PVP K30>PLX-Met>HPβCD-Met & in pH 7.4, in the order of PLX-Met>PVP K30>HPβCD-Met. DSC thermogram of Metoclopramide base showed a sharp endothermic peak at its melting point (147oC) which exhibits in crystalline form complying with that of Metoclopramide hydrochloride form, melting point was found to be 850C.  In the ex-vivo study of several transdermal patches, patch C [SD of MET: HPβCD (1:5)] showed the controlled release and permeation of drug.


Conclusion: Poor solubility of new chemical entities being a well known problem for past few decades despite the imbalance between significant research efforts & few successful marketed formulations, the solid dispersion proves to hold a key position among all the various formulation strategies to enhance the aqueous solubility & dissolution rate and thereby the bioavailability of  poorly aqueous solubility of drug.


Keywords: Bioavailability,DSC, Metoclopramide hydrochloride, solid dispersion, HPβCD,

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Author Biographies

Goutam Mukhopadhyay, Associated Professor, Department of Pharmaceutical Technology, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Associated Professor, Department of Pharmaceutical Technology, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Rahul Mukhopadhyay, Assistant Professor, Department of Pharmaceutical Technology, Brainware university, 398, Ramkrishnapur Road, Near Jagadighata Market, Barasat, Kolkata, West Bengal 700124

Assistant Professor, Department of Pharmaceutical Technology, Brainware university, 398, Ramkrishnapur Road, Near Jagadighata Market, Barasat, Kolkata, West Bengal 700124

Ankita Mukhopadhyay, Assistant Professor, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127.

Assistant Professor, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127.

Shymodip Kundu, Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Banerjee Shreya, Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Debasmita Manna, Student, Department of Pharmacy, NSHM Knowledge campus, 124 BL Saha Road, Kolkata-700053.

Student, Department of Pharmacy, NSHM Knowledge campus, 124 BL Saha Road, Kolkata-700053.

Argha Sarkar, Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Tarique Nazar, Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Srotoswini Sarkar, Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Sauris Bala, Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

Student, Department of Pharmacy, BCDA College of Pharmacy & Technology, 78, Jessore Road(S), Kolkata-700127

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Mukhopadhyay, G., Mukhopadhyay, R., Mukhopadhyay, A., Kundu, S., Shreya, B., Manna, D., Sarkar, A., Nazar, T., Sarkar, S., & Bala, S. (2018). Formulation Development to Enhance the Solubility of Metoclopramide Base Drug by Solid Dispersion and Evaluation of Transdermal Film. Journal of Drug Delivery and Therapeutics, 8(6), 183-191. https://doi.org/10.22270/jddt.v8i6.2039