Pharmaceutical studies on and clinical application of olanzapine suppositories prepared as a hospital preparation.
BACKGROUND
A new formulation of olanzapine available for terminally ill patients is needed. Rectal administration using suppositories is an alternative for patients for whom administration via the oral route is not feasible. In the present study, we prepared olanzapine suppositories, and confirmed using pharmaceutical tests. Furthermore, we demonstrated the efficacy and safety of olanzapine suppositories in terminally ill patients.


METHODS
We prepared olanzapine suppositories using bases consisting of different compositions of Witepsol H-15, Witepsol S-55, and Witepsol E-75. The suppository release test was performed, and the olanzapine suppository with the best dissolution rate was selected. The suppository was assessed using the content uniformity test, content test in suppositories, hardness test, stability test, and clinical efficacy and safety.


RESULTS
The dissolution rate at 360 min of olanzapine suppositories with Witepsol H-15 was the best (77.0 ± 3.3 %). The suppositories prepared had a uniform weight (2.47 ± 0.02 g) and content (2.11 ± 0.07 mg). The power required to break suppositories was 7.96 ± 0.55 kgf. When olanzapine suppositories were stored with protection from light, their contents were maintained regardless of whether the temperature was at 4 °C or room temperature. The numbers of patients administered 2.5 mg, 5 mg, and 10 mg of olanzapine suppositories were 4, 19, and 1. The percentages of patients with delirium or nausea and vomiting cured with olanzapine suppositories were 82 and 57 %, respectively.


CONCLUSIONS
We suggest that olanzapine suppositories prepared in the hospital by pharmacists will improve the quality of life of terminally ill patients.


BACKGROUND
UMIN000022172. May 2, 2016 retrospectively registered.
Division of Practical Pharmacy, Keio University Faculty of Pharmacy, 1-5-30 Shibakoen, Minato-ku, Tokyo, 105-8512 Japan.
Kazuaki
K
Matsumoto
Division of Practical Pharmacy, Keio University Faculty of Pharmacy, 1-5-30 Shibakoen, Minato-ku, Tokyo, 105-8512 Japan.
Satoru
S
Kimura
Division of Practical Pharmacy, Keio University Faculty of Pharmacy, 1-5-30 Shibakoen, Minato-ku, Tokyo, 105-8512 Japan.
Kenichi
K
Takahashi
Division of Practical Pharmacy, Keio University Faculty of Pharmacy, 1-5-30 Shibakoen, Minato-ku, Tokyo, 105-8512 Japan.
Yuta
Y
Yokoyama
Department of Pharmacy, Shonan Central Hospital, 1-3-43 Hatori, Fujisawa-shi, Kanagawa 251-0056 Japan.
Masayuki
M
Miyazawa
Department of Pharmacy, Shonan Central Hospital, 1-3-43 Hatori, Fujisawa-shi, Kanagawa 251-0056 Japan.
Satoko
S
Kushibiki
Department of Palliative Care, Shonan Central Hospital, 1-3-43 Hatori, Fujisawa-shi, Kanagawa 251-0056 Japan.
Morio
M
Katamachi
Division of Practical Pharmacy, Keio University Faculty of Pharmacy, 1-5-30 Shibakoen, Minato-ku, Tokyo, 105-8512 Japan.
Junko
J
Kizu
Delirium; Nausea and vomiting; Olanzapine; Suppository; Terminally ill patients; Witepsol H-15
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