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
Which of the following business challenge poses the greatest threat to your company?
Building a sustainable pipeline of products
Attracting a skilled workforce
Obtaining/maintaining adequate financing
Regulatory compliance
Building a sustainable pipeline of products
25%
Attracting a skilled workforce
31%
Obtaining/maintaining adequate financing
13%
Regulatory compliance
31%
View Results
Eric Langer Outsourcing Outlook Eric LangerBiopharma Outsourcing Activities Update
Cynthia Challener, PhD Ingredients Insider Cynthia Challener, PhDAppropriate Process Design Critical for Commercial Manufacture of Highly Potent APIs
Jill Wechsler Regulatory Watch Jill Wechsler FDA and Manufacturers Seek a More Secure Drug Supply Chain
Sean Milmo European Regulatory WatcchSean MilmoQuality by Design?Bridging the Gap between Concept and Implementation
Medicare Payment Data Raises Questions About Drug Costs
FDA Wants You!
A New Strategy to Tackle Antibiotic Resistance
Drug-Diagnostic Development Stymied by Payer Concerns
Obama Administration Halts Attack on Medicare Drug Plans
Source: Pharmaceutical Technology,
Click here