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Dissolution Profile of Mefenamic Acid Solid Dosage Forms in Two Compendial and Biorelevant (FaSSIF) Media

Wilda Nurhikmah1, Yeyet Cahyati Sumirtapura1, Jessie Sofia Pamudji1

  • 1School of Pharmacy Bandung Institute of Technology, Ganesha 10, 40132, Bandung, Indonesia.

Scientia Pharmaceutica
|April 26, 2016
PubMed

Insights

Mefenamic acid dissolution testing revealed significant differences between compendial and biorelevant media. While USP and PPRC methods showed high drug release, biorelevant fasted simulated small intestinal fluid (FaSSIF) demonstrated limited mefenamic acid solubility and dissolution.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery and Formulation
  • Analytical Chemistry

Background:

  • Mefenamic acid, a non-steroidal anti-inflammatory drug (NSAID), is classified as a Biopharmaceutical Classification System (BCS) class II drug, characterized by low water solubility and high permeability.
  • Existing compendial methods for dissolution testing, such as those from the United States Pharmacopeia (USP) and the Pharmacopoeia of the People's Republic of China (PPRC), are used for mefenamic acid solid dosage forms.
  • There is growing interest in utilizing 'biorelevant' media to develop more physiologically relevant dissolution test methods.

Purpose of the Study:

  • To investigate the dissolution profiles of mefenamic acid from solid dosage forms (caplets and capsules) available in the Indonesian market.
  • To compare the dissolution performance of mefenamic acid in three different media: USP, PPRC, and biorelevant fasted simulated small intestinal fluid (FaSSIF).
  • To assess the impact of different dissolution media on the solubility and release rate of mefenamic acid.

Main Methods:

  • Dissolution tests were conducted on mefenamic acid caplets and capsules using USP, PPRC, and FaSSIF media.
  • Standard dissolution apparatus (Apparatus II - paddle, or Apparatus I - basket) was employed at 37°C with specified rotation speeds.
  • Solubility of mefenamic acid was determined in each of the three dissolution media at 37°C.

Main Results:

  • Mefenamic acid exhibited the highest solubility in USP medium (~2 mg/mL), followed by PPRC medium (~0.5 mg/mL), and FaSSIF medium (~0.06 mg/mL).
  • Dissolution in USP and PPRC media generally exceeded 75% drug release within 45 minutes for most products, with one exception (PN caplet in USP medium).
  • In contrast, dissolution in the biorelevant FaSSIF medium was significantly lower, with less than 16% of the drug dissolved for all products within the tested timeframe. Capsule dosage forms consistently showed higher dissolution rates across all media.

Conclusions:

  • The choice of dissolution medium significantly impacts the observed dissolution profile of mefenamic acid.
  • Compendial media (USP, PPRC) may overestimate drug release compared to biorelevant FaSSIF, potentially leading to different conclusions about product performance.
  • Biorelevant media like FaSSIF provide a more discriminating assessment of mefenamic acid dissolution, which is crucial given its low solubility (BCS Class II).
Keywords:
Biorelevant mediumDissolution TestingIndonesian PharmacopoeiaMefenamic acidPharmacopoeia of the People’s Republic of ChinaUnited States Pharmacopoeia

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