Pharmaceutical evaluation of Levofloxacin orally disintegrating tablet formulation using low frequency Raman spectroscopy
We evaluated the pharmaceutical properties of levofloxacin (LV) in the form of an orally disintegrating tablet (LVODT) to find a new usefulness of low frequency (LF) Raman spectroscopy. LVODT contained dispersed granules with diameters in the order of several hundred micrometers, which were composed of the active pharmaceutical ingredient (API), as confirmed by infrared (IR) microspectroscopy. On the contrary, the API and inactive pharmaceutical ingredients (non-APIs) were homogeneously distributed in LV tablet (LVT) formulations. Microscopic IR spectroscopy and thermal analyses showed that LVODT and LVT contained the API in different crystalline forms or environment around the API each other.
Furthermore, powder X-ray diffraction showed that LVT contained a hemihydrate of the API, while LVODT showed a partial transition to the monohydrate form. This result was confirmed by microscopic LF Raman spectroscopy. Moreover, this method confirmed the presence of thin layers coating the outer edges of the granules that contained the API. Spectra obtained from these thin layers indicated the presence of titanium dioxide, suggesting that the layers coexisted with a polymer that masks the bitterness of API. The microscopic LF Raman
spectroscopy results in this study indicated new applications of this method in pharmaceutical science.
Table 1. Nonactive pharmaceutical ingredients of LVODT and LVT formulations.
| Formulations | Non-APIs* |
|---|---|
| LV ODT | MCC**, Carmellose sodium, Hydroxypropyl cellulose, Sucralose, Aminoalkyl methacrylate copolymer E, Talc, Titanium dioxide, Yellow ferric oxide, D-Mannitol, MCC**, Light anhydrous silicic acid, Fragrance, Magnesium stearate, other 3 components |
| LV T_CRAVIT | MCC**, Carmellose, Hydroxypropyl cellulose, Stearyl sodium fumarate, Hypromellose, Titanium dioxide, Talc, Macrogol 6000, Yellow ferric oxide, Carnauba wax |
| LV T_NIPRO | MCC**, Hydroxypropyl cellulose, Carmellose, Stearyl sodium fumarate, Hypromellose, Macrogol, Talc, Titanium dioxide, Yellow ferric oxide, Carnauba wax |
| LV T_SAWAI | Carnauba wax, Carmellose, MCC**, Titanium dioxide, Ferric oxide, Talc, Hydroxypropyl cellulose, Hypromellose, Stearyl sodium fumarate, Macrogol 6000 |
| LV T_TOWA | MCC**, Carmellose, Hydroxypropyl cellulose, Cros-carmellose sodium, Magnesium stearate, Hypromellose, Macrogol 6000, Talc, Titanium dioxide, Yellow ferric oxide |
* These inactive pharmaceutical ingredients (non-APIs) have been cited from manufacturer’s forms [9–12].
** MCC: Microcrystalline cellulose
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Materials
LVODT (250 mg “Towa,” lot. B0048) was purchased from Towa Pharmaceutical Co., Ltd. (Osaka, Japan). Cravat tablets (250 mg, lot. QUA1173, Daiichi Sankyo Co. Ltd, Tokyo, Japan; LVT_CRABIT), 250 mg levofloxacin tablets “Nipro” (lot. 20L031, Nipro, Osaka, Japan; LVT_NIPRO), 250 mg levofloxacin tablets “Sawai” (lot. 420502, Sawai Pharmaceutical Co., Ltd, Osaka, Japan; LVT_SAWAI), and 250 mg levofloxacin tablets “Towa” (lot. B0023, Towa Pharmaceutical Co., Ltd, Osaka, Japan; LVT_TOWA) were analyzed. The non-API formulations for all tablets are shown in Table 1 [9–12]. LV was purchased from Tokyo Chemical Industry Co. Ltd. ( L0193, Tokyo, Japan) and Dadipharm (Lot. HBW211015-7, Jiangxi, China). Both were commercially available levofloxacin hemihydrate (LV0.5) reagents, which is stable under ambient conditions. Microcrystalline cellulose (MCC; CEOLUS® UF-702) was purchased from Asahi Kasei Chemicals (Tokyo, Japan).
Yamamoto, Y.; Kajita, M.; Hirose, Y.; Shimada, N.; Fukami, T.; Koide, T. Pharmaceutical Evaluation of Levofloxacin Orally Disintegrating Tablet Formulation Using Low Frequency Raman Spectroscopy. Preprints.org 2023, 2023060130. https://doi.org/10.20944/preprints202306.0130.v1
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