Synthesis and in-vivo taste assessment of meloxicam pivalate

Bandoo C Chatale1, Mariam S Degani1

  • 1Department of Pharmaceutical Sciences & Technology, Institute of Chemical Technology , Mumbai , India.

Insights

Meloxicam pivalate (MXP) was synthesized to mask the bitter taste of meloxicam (MX), a common arthritis medication. Taste tests in rats showed MXP significantly improved palatability compared to MX.

Area of Science:

  • Pharmaceutical Chemistry
  • Drug Development
  • Sensory Science

Background:

  • Meloxicam (MX) is a widely prescribed nonsteroidal anti-inflammatory drug for arthritis.
  • A significant drawback of meloxicam is its pronounced bitter taste, limiting patient compliance.
  • Prodrug strategies are employed to improve drug palatability and delivery.

Purpose of the Study:

  • To synthesize a prodrug of meloxicam to improve its taste profile.
  • To evaluate the palatability of the novel meloxicam prodrug in a preclinical model.

Main Methods:

  • Chemical synthesis of meloxicam pivalate (MXP) from meloxicam.
  • Taste evaluation using a single bottle-test rat model.
  • Comparative palatability assessment between MXP and MX solutions.

Main Results:

  • Successful synthesis of meloxicam pivalate (MXP).
  • The rat model demonstrated a significant improvement in the palatability of MXP compared to MX.
  • The chemical modification effectively masked the bitter taste of the parent drug.

Conclusions:

  • Meloxicam pivalate (MXP) represents a promising strategy to overcome the bitter taste of meloxicam.
  • This prodrug approach could enhance patient adherence to meloxicam therapy.
  • Further investigation into MXP for clinical use is warranted.

Related Concept Videos

The Physiology of Taste01:24

The Physiology of Taste

The perception of a salty flavor is facilitated by sodium ions within the oral salivary fluid. Upon consumption of a salty substance, salt crystals disassemble, leading to the liberation of its constituents—Na+ and Cl- ions. These ions subsequently dissolve into the salivary fluid present in the oral cavity. The external environment of the gustatory cells experiences an elevation in Na+ concentration, thereby establishing a potent concentration gradient. This gradient propels the...
7.3K
The Tongue and Taste Buds00:49

The Tongue and Taste Buds

The surface of the tongue is covered with various small bumps called papillae, which either distribute what has been ingested (filiform papillae) or contain the sensory taste (or gustatory) receptor cells (fungiform, circumvallate, and foliate papillae). Embedded within each taste-related papilla are the taste buds—clusters of 30 to 100 gustatory receptor cells.
40.8K
Taste Buds and Receptors01:20

Taste Buds and Receptors

Gustation, or the sense of taste, is intrinsically linked to the anatomical structures located on the tongue. This organ's surface, along with the entirety of the oral cavity, is adorned with stratified squamous epithelium. Evident on the tongue are elevated structures known as papillae (singular = papilla), which house the mechanisms for the transduction of gustatory stimuli. Four distinct types of papillae exist, each identified by their unique morphological attributes: the circumvallate,...
4.7K
Conditioned Taste Aversion01:14

Conditioned Taste Aversion

Conditioned taste aversion, also known as sauce béarnaise syndrome, is a phenomenon in which an individual develops an aversion to a certain food taste following a negative experience, typically illness. This form of aversion is a type of classical conditioning in which the taste of the food (conditioned stimulus, CS) is associated with the experience of illness (unconditioned stimulus, UCS).
A notable characteristic of conditioned taste aversion is that it often requires only a single...
559
Dehydration Synthesis01:15

Dehydration Synthesis

Overview
Dehydration synthesis (also called a condensation reaction) is the chemical process in which two molecules covalently link together to form a new molecule, along with the release of a water molecule. Many physiologically important compounds form by dehydration synthesis reactions, such as complex carbohydrates, proteins, DNA, and RNA.
Synthesis of carbohydrates
Sugar molecules are covalently linked together by dehydration synthesis. During the reaction, the hydroxyl (-OH) group from...
148.9K
Synthesis and Decomposition Reactions02:17

Synthesis and Decomposition Reactions

Synthesis and decomposition are two types of redox reactions. Synthesis means to make something, whereas decomposition means to break something. The reactions are accompanied by chemical and energy changes. 
38.1K