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Evaluation of orally disintegrating tablets (ODTs) containing microspheres with losartan potassium
1
Katedra i Zakład Technologii Postaci Leku, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej w Sosnowcu, Śląski Uniwersytet Medyczny w Katowicach
2
Wydział Ochrony Zdrowia, Śląska Wyższa Szkoła Medyczna w Katowicach
Corresponding author
Beata Sarecka-Hujar
Katedra i Zakład Technologii Postaci Leku, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej w Sosnowcu, Śląski Uniwersytet Medyczny w Katowicach, ul. Kasztanowa 3, 41-200 Sosnowiec
Katedra i Zakład Technologii Postaci Leku, Wydział Farmaceutyczny z Oddziałem Medycyny Laboratoryjnej w Sosnowcu, Śląski Uniwersytet Medyczny w Katowicach, ul. Kasztanowa 3, 41-200 Sosnowiec
Ann. Acad. Med. Siles. 2019;73:36-42
KEYWORDS
multicompartment systemsmicrospherespotassium losartanprolonged releasetablets disintegrating in the oral cavity
TOPICS
ABSTRACT
Introduction:
Multicompartment systems containing an active substance distributed among carriers (i.e. liposomes, microspheres, microcapsules, nanocapsules) open new possibilities for sustained or controlled drug release. Microspheres are monolithic, porous or smooth spherical particles, sized 1–500 μm, in which the drug substance is suspended, incorporated or emulsified in a polymer matrix. The aim of the study was to prepare microspheres containing losartan potassium and Eudragit L 100-55 as the matrix and then orally disintegrating tablets (ODTs) with the obtained microspheres.
Methods:
Microspheres with drug:polymer ratios of 1:1 and 1:2 were obtained by the spray drying method under the following conditions: inlet temperature – 150°C, aspirator efficiency – 80% and pump efficiency – 10%. The morphology and microsphere size were evaluated microscopically. Orally disintegrating tablets containing microspheres with losartan potassium were prepared by direct compression. The obtained tablets were evaluated according to the Farmakopea Polska X (FPX) requirements for this drug form. Statistical analysis was performed using Statistica 10.1.
Results:
The ODTs met the appearance, size and mass uniformity standards. The disintegration time of the obtained ODTs did not exceed the required 3 minutes. The release analysis of losartan potassium from the microspheres with the drug:polymer ratio of 1:1 in 0.1 M hydrochloric acid (HCl) showed that the largest amount of losartan (21%) was released in 60 minutes. After 120 minutes, the process was continued in artificial intestinal juice (pH = 6.8), in which losartan was completely released within 270 minutes. For the microspheres with the 1:2 ratio, we observed that the largest amount of losartan (36%) was released in 90 minutes in 0.1 M HCl and further release in artificial intestinal juice showed a release of 99.43% of the active substance up to 300 minutes.
Conclusions:
The model microspheres containing losartan potassium can be used as an intermediate form of a drug to obtain ODTs.
Multicompartment systems containing an active substance distributed among carriers (i.e. liposomes, microspheres, microcapsules, nanocapsules) open new possibilities for sustained or controlled drug release. Microspheres are monolithic, porous or smooth spherical particles, sized 1–500 μm, in which the drug substance is suspended, incorporated or emulsified in a polymer matrix. The aim of the study was to prepare microspheres containing losartan potassium and Eudragit L 100-55 as the matrix and then orally disintegrating tablets (ODTs) with the obtained microspheres.
Methods:
Microspheres with drug:polymer ratios of 1:1 and 1:2 were obtained by the spray drying method under the following conditions: inlet temperature – 150°C, aspirator efficiency – 80% and pump efficiency – 10%. The morphology and microsphere size were evaluated microscopically. Orally disintegrating tablets containing microspheres with losartan potassium were prepared by direct compression. The obtained tablets were evaluated according to the Farmakopea Polska X (FPX) requirements for this drug form. Statistical analysis was performed using Statistica 10.1.
Results:
The ODTs met the appearance, size and mass uniformity standards. The disintegration time of the obtained ODTs did not exceed the required 3 minutes. The release analysis of losartan potassium from the microspheres with the drug:polymer ratio of 1:1 in 0.1 M hydrochloric acid (HCl) showed that the largest amount of losartan (21%) was released in 60 minutes. After 120 minutes, the process was continued in artificial intestinal juice (pH = 6.8), in which losartan was completely released within 270 minutes. For the microspheres with the 1:2 ratio, we observed that the largest amount of losartan (36%) was released in 90 minutes in 0.1 M HCl and further release in artificial intestinal juice showed a release of 99.43% of the active substance up to 300 minutes.
Conclusions:
The model microspheres containing losartan potassium can be used as an intermediate form of a drug to obtain ODTs.
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