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Novel patchouli alcohol ternary solid dispersion pellets prepared by poloxamers.

Jin-Bin Liao1, Yong-Zhuo Liang2, Yun-Long Chen2

  • 1School of Chinese Materia Medica, Guangzhou University of Chinese Medicine, Guangzhou 510006, PR China. ; Guangdong Second Province Hospital of Traditional Chinese Medicine, Guangzhou 510095, P. R. China.

Iranian Journal of Pharmaceutical Research : IJPR
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Summary

Poloxamers significantly enhance the dissolution of patchouli alcohol (PA) in solid dispersions (SDs), improving drug release by approximately 16 times. This study presents a scalable method for preparing PA-loaded pellets for immediate release formulations.

Keywords:
Closed in-vitro dissolution test methodEutectic mixturesPatchouli alcoholPoloxamersTernary solid dispersion pellets

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Materials Science

Background:

  • Poorly water-soluble drugs present challenges in formulation development, limiting bioavailability.
  • Patchouli alcohol (PA) is a bioactive constituent with low water solubility, hindering its therapeutic application.
  • Poloxamers are versatile excipients with potential for enhancing drug solubility and dissolution.

Purpose of the Study:

  • To evaluate poloxamers (188 and 407) as solubility and dissolution rate enhancers for patchouli alcohol (PA).
  • To prepare and characterize immediate-release pellets using PA-loaded solid dispersions (SDs).
  • To establish a simple, accurate in-vitro dissolution method for volatile drugs like PA.

Main Methods:

  • Preparation of binary solid dispersions (bSDs) and ternary solid dispersions (tSDs) of PA with poloxamer 188 (P 188) and poloxamer 407 (P 407) using a low-temperature melting method.
  • Rapid solidification of SDs by dropping into a cold condensing agent.
  • Characterization of PA-SD pellets using Differential Scanning Calorimetry (DSC) and Fourier-Transform Infrared Spectroscopy (FTIR).
  • In-vitro dissolution testing to assess drug release rates.

Main Results:

  • Both PA/P 188 and PA/P 407 bSDs significantly increased PA dissolution rate by approximately 16-fold compared to pure PA within 180 minutes.
  • P 188 demonstrated a faster dissolution rate, while P 407 exhibited better solubility.
  • Incorporating P 188 into PA/P 407 bSD pellets further enhanced PA dissolution.
  • The enhanced dissolution is attributed to particle size reduction of crystalline PA due to eutectic system formation with poloxamers.

Conclusions:

  • Poloxamers are effective agents for enhancing the solubility and dissolution rate of patchouli alcohol.
  • The developed low-temperature melting method for preparing PA-loaded solid dispersion pellets is simple, rapid, cost-effective, and potentially scalable.
  • The study established a suitable in-vitro dissolution method for volatile drugs, facilitating formulation development.