Preparation and Characterization of Meloxicam–Myrj-52 Granules Obtained by Melt Granulation - Pharmaceutical Technology

Latest Issue
PharmTech

Latest Issue
PharmTech Europe

Preparation and Characterization of Meloxicam–Myrj-52 Granules Obtained by Melt Granulation
Various manufacturing techniques can improve a drug's solubility, thus increasing its bioavailability. The authors examined whether melt granulation can enhance drug solubility using meloxicam as the drug substance and myrj-52 as the binder.


Pharmaceutical Technology


Tablet-dissolution studies were performed in triplicate. Dissolution was achieved in a 900-mL phosphate butter (pH 7.4) using a USP 24 Type II dissolution apparatus (Veego Scientific). The dissolution medium was stirred at 100 rpm and maintained at 37 0.5 C. Drug release was determined using an ultraviolet spectrophotometer (UV-1700, Shimadzu) at 363.5 nm. For comparison, a commercial tablet (Metflam, Unichem Laboratories, Mumbai, India) was also studied. Data obtained from the dissolution studies were analyzed using PCP Disso software (PCP, Pune, India).

Results and discussion

Drug-content estimation. The granules and solid dispersion showed less variation in percentage drug content. The percentage drug content was between 96.82 0.75% and 101.39 1.18%. These values indicate a uniform distribution of drug in the granules and solid dispersion obtained using myrj-52.


Figure 1: Saturation solubility of melt granulation (MG), physical mixture (PM), and solid dispersion (SD) of meloxicam with myrj-52 in an aqueous solution at room temperature.
Saturation solubility. All of the test samples showed an increase in drug solubility (see Figure 1). The physical mixture, solid dispersion, and granules prepared by melt granulation showed higher saturation solubility compared with pure meloxicam. This result might arise from an improvement in the wetting of drug particles and localized solubilization by myrj-52.

An increase in a drug's saturation solubility can explain the improved dissolution of melt granulation, physical mixture, and solid dispersions, according to the Noyes–Whitney equation, because the saturation solubility of a compound depends on particle size. Thus, one can improve meloxicam's saturation solubility by reducing its particle size through various approaches. The saturation solubility of pure meloxicam was 23 μg/mL. Melt granulation, physical mixture, and solid dispersion exhibited improved solubility.

The saturation solubility of solid dispersion prepared with myrj-52 increased to 1.2 mg/mL. Solubility is increased almost 52.17 times with myrj-52.


Figure 2: Solubility of meloxicam in an aqueous solution of myrj-52.
Solubilization effect of myrj-52. The results from the current study showed that myrj-52 has a significant solubilizing effect on meloxicam. Figure 2 shows the phase-solubility curve of meloxicam in the presence of myrj-52. Meloxicam's solubility increased when the concentration of myrj-52 in the water increased. The solubility enhancement may result from the improved dissolution of meloxicam particles in the water by myrj-52.

The process of the transfer of meloxicam from the pure water to the aqueous solution of myrj-52 was obtained using the values of Gibb's free-energy change. The Gibb's free energy of transfer (Gtr) of meloxicam from the pure water to aqueous solution of myrj-52 was calculated using the following equation:





ADVERTISEMENT

blog comments powered by Disqus
LCGC E-mail Newsletters

Subscribe: Click to learn more about the newsletter
| Weekly
| Monthly
|Monthly
| Weekly

Survey
What role should the US government play in the current Ebola outbreak?
Finance development of drugs to treat/prevent disease.
Oversee medical treatment of patients in the US.
Provide treatment for patients globally.
All of the above.
No government involvement in patient treatment or drug development.
Finance development of drugs to treat/prevent disease.
30%
Oversee medical treatment of patients in the US.
9%
Provide treatment for patients globally.
8%
All of the above.
45%
No government involvement in patient treatment or drug development.
8%
Jim Miller Outsourcing Outlook Jim MillerCMO Industry Thins Out
Cynthia Challener, PhD Ingredients Insider Cynthia ChallenerFluorination Remains Key Challenge in API Synthesis
Marilyn E. Morris Guest EditorialMarilyn E. MorrisBolstering Graduate Education and Research Programs
Jill Wechsler Regulatory Watch Jill Wechsler Biopharma Manufacturers Respond to Ebola Crisis
Sean Milmo European Regulatory WatchSean MilmoHarmonizing Marketing Approval of Generic Drugs in Europe
Legislators Urge Added Incentives for Ebola Drug Development
FDA Reorganization to Promote Drug Quality
FDA Readies Quality Metrics Measures
New FDA Team to Spur Modern Drug Manufacturing
From Generics to Supergenerics
Source: Pharmaceutical Technology,
Click here