Background:
Diabetes mellitus (DM) is a disorder of carbohydrate metabolism characterised
by chronic hyperglycemia, although lipid and protein metabolism are also
affected. Underlying its pathophysiology is a deficit in insulin secretion or
action, or there may be a simultaneous deficit in both insulin secretion and
activity. Diabetes represents a global health challenge. In 2021, it was
estimated that 536.6 million people suffered from this disease. Today, a wide
range of drugs is available for the treatment of Type 2 Diabetes Mellitus. In
2022, in Mexico, the most cost-effective intervention for Type 2 Diabetes was a
combined oral treatment of metformin and glibenclamide, with a total cost of
USD 951.75, an effectiveness rate of 42.30%, and an effectiveness coefficient
of 2.25. Osmotic systems offer clear advantages over conventional
pharmaceutical forms, as they allow for the maintenance of constant plasma
concentrations over long periods.
Aims: This study
aims to target the improvement of the treatment of people suffering from
Diabetes. Rather than using multiple doses and dosage forms for effective
treatment, the author provides a robust solution in the form of a combination
of drugs as an osmotic capsule, which has a controlled release pattern and aims
at treating the disease effectively. This study also presents, for the first time,
a compatibility study using a non-destructive methodology with a Raman
spectrometer, which can be considered as the article’s novelty.
Methodology: A
compatibility drug-excipient with Raman spectroscopy study at 50°C for four
weeks was conducted. A 32 experimental design was successfully developed to
obtain controlled-release osmotic capsules containing metformin/Glibenclamide.
Pharmaceutical Technology Laboratory, College of Pharmacy, Universidad Autonoma
del Estado de Morelos. 2013-2015. Compatibility study between Metformin and
Glibenclamide with 15 excipients using Raman spectrofotometer during 4 weeks at
50C, then manual encapsulation of the 9 formulations and coating with cellulose
acetate in acetone and finally release study in two steps: 2.5 hours in gastric
medium and ten hours in enteric medium for a total of 12.5 hrs of release
study.
Results: Capsules
free of excipient incompatibilities, with a constant release rate over 12.5
hours, independent of pH and stirring speed. These controlled-release osmotic
capsules were sealed and coated with a cellulose acetate membrane, with a
weight gain of 3% and a release hole of 635 μm. The best formulation exhibited
lag times of 2.09 hours for metformin and 0.18 hours for glibenclamide. The 1:1
Mannitol-Sorbitol mixture in this study showed a reduction in osmotic
potential, with Mannitol exhibiting lower osmotic potential and Sorbitol
providing the highest osmotic potential. The most important findings indicate
that the release rate for both drugs remained linear for 12.5 hours, with the
lag time being close to zero. The lag time in the systems was better when the
highest level of osmotic agent (sorbitol) and the highest amount of the osmotic
agent (100 mg) were present in the osmotic system.
Conclusion: For
the first time presented a compatibility study was presented using a
nondestructive methodology with a Raman spectrometer. The capsules presented
constant release for 12.5 hours; the best lag time was 2.09 hours for metformin
and 0.18 hours for Glibenclamide. the mixture 1:1 sorbitol– mannitol presented
a reduction in osmotic potential. The limited release rate of glibenclamide may
be attributed to its solubility constraints. The combination of a high amount
of sorbitol as the osmotic agent, along with the use of non-disintegrating
capsules, effectively reduced the system's lag time. The manuscript compares
the pharmacological agents used by diabetes patients, and they have to take
multiple doses for the efficacy of the treatment with an osmotic system, improving
treatment adherence through controlled release, easier and more effective with
a lower number of administrations.
Author(s) Details :-
Raúl Pineda-Santiago
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos,
Cuernavaca, Morelos, México.
Luz María
Melgoza-Contreras
Departamento de Ciencias Biológicas, Universidad Autónoma
Metropolitana-Xochimilco, México.
Jessica
Espinosa-Garcia
Thermo Fisher, CDMX, México.
Enrique
Amador-Gonzalez
Facultad de Química, Universidad Nacional Autónoma de México, CDMX, México.
Efrén
Hernandez-Baltazar
Facultad de Farmacia, Universidad Autónoma del Estado de Morelos,
Cuernavaca, Morelos, México.
Please see the book
here :- https://doi.org/10.9734/bpi/psnid/v9/6466
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