Physical properties of lansoprazole orally disintegrating tablets

Introduction

Orally disintegrating (OD) tablets are rapidly dissolved or disintegrated in the oral cavity, ¹ and patients can take them with or without water. Thus, OD tablets are highly convenient for patients in any situation, including in patients with limited water intake, those who have difficulty obtaining water because of a busy lifestyle, and those with decreased deglutition function. ² Various OD tablets, including the generic ones, are now being clinically used. OD tablets help reducing the swallowing burden and improve medication compliance. When patients with prostatic hypertrophy were switched from tamusulosin capsules (used for dysuria treatment) to OD tablets, more elderly patients preferred the OD tablets and equivalent efficacy was obtained before and after the switch. ³ Similarly, during the switch from conventional voglibose tablets (used for diabetic postcibal hyperglycemia inhibition) to OD tablets, the medication compliance improved and therapeutic efficacy increased. ⁴

OD tablets are required to immediately disintegrate in the oral cavity but possess a tablet strength that can endure impact and vibration. In addition, elderly and incapacitated patients should be able to easily push out the OD tablets from the press through package (PTP). Therefore, it is very important that pharmacists know the characteristics of OD tablets, including their hydrophilia, tablet strength, and PTP pushing out strength for patient compliance instructions. However, there is limited information available regarding these physical properties.

In this study, one branded and five generic lansoprazole OD tablets, used frequently in clinical situations, were chosen for evaluation. We examined each formulation for its physical properties, including their hydrophilia, tablet strength, and PTP pushing out strength.

Materials and methods

Materials

The tested lansoprazole OD tablets are presented in Table 1.

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Table 1.

Lansoprazole OD tablets

	OD tablets (manufacturer)	Lot No.
A	Takepron® OD Tablets 15 mg (Takeda Pharmaceutical Company Ltd, Osaka, Japan)	OJ344
B	Lansoprazole OD Tablets 15 mg “JG” (Nihon Generic Co., Ltd., Tokyo, Japan)	203840
C	Lansoprazole OD Tablets 15 mg “DK” (Daiko Pharmaceutical Co., Ltd., Kawagoe, Japan)	AR01
D	Lansoprazole OD Tablets 15 mg “Taiyo” (Teva Pharma Japan Inc., Nagoya, Japan) a	AY1305
E	Lansoprazole OD Tablets 15 mg “TOWA” (Towa Pharmaceutical Co., Ltd., Osaka, Japan)	A057
F	Lansoprazole OD Tablets 15 mg “Nichi-Iko” (Nichi-Iko Pharmaceutical Co., Ltd., Toyama, Japan)	GI1401

a

Current name is Lansoprazole OD Tablets 15 mg “Teva.”

Results

Hydrophilia

Wetting times of the OD tablets are shown in Figure 1. Wetting times of formulations A, B, C, D, E, and F were 25 ± 2, 14 ± 1, 14 ± 1, 16 ± 1, 22 ± 1, and 38 ± 4 s, respectively.

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Figure 1.

Wetting time of OD tablets. (a) p < 0.05 vs. A; (b) p < 0.05 vs. B; (c) p < 0.05 vs. C; (d) p < 0.05 vs. D; (e) p < 0.05 vs. E; (f) p < 0.05 vs. F. Data presented are mean ± standard deviation (S.D.; n = 6).

Tablet strength

Hardness and friability of the OD tablets are shown in Figure 2 and Table 2. Hardness of formulations A, B, C, D, E, and F were 2.1 ± 0.5, 7.5 ± 1.1, 7.2 ± 1.0, 8.0 ± 1.3, 3.5 ± 0.5, and 3.3 ± 0.2 kgf, respectively (Figure 2). Friability of formulations A, B, C, D, E, and F were less than 1% (Table 2).

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Figure 2.

Hardness of OD tablets. (a) p < 0.05 vs. A; (b) p < 0.05 vs. B; (c) p < 0.05 vs. C; (d) p < 0.05 vs. D; (e) p < 0.05 vs. E; (f) p < 0.05 vs. F. Data presented are mean ± S.D. (n = 10).

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Table 2.

Friability of OD tablets

Friability (%)
A	B	C	D	E	F
0.74	0.02	0.05	0.05	0.07	0.15

Pushing out from PTP

PTP pushing out strengths of the OD tablets are shown in Figure 3. The PTP pushing out strengths of formulations A, B, C, D, E, and F were 20.1 ± 1.8, 29.7 ± 1.3, 34.4 ± 3.0, 28.0 ± 1.8, 22.3 ± 2.3, and 24.2 ± 2.1 N, respectively.

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Figure 3.

Strength required for pushing out OD tablets from a PTP. (a) p < 0.05 vs. A; (b) p < 0.05 vs. B; (c) p < 0.05 vs. C; (d) p < 0.05 vs. D; (e) p < 0.05 vs. E; (f) p < 0.05 vs. F. Data presented are mean ± S.D. (n = 4).

Discussion

Immersion wetting is a widely demonstrated approach for determining the solid hydrophilia of drug formulations. ⁹ In the present study, the immersion wetting rate of formulation F was significantly longer than that of other formulations (Figure 1), presumably reflecting differences in the additives and compression pressure. These findings indicate that the time required for the oral disintegration of formulation F in the oral cavity may be longer than that required for the oral disintegration of other formulations.

Formulations A, B, C, D, and E had hardness (>3 kgf) ¹⁰ and friability (<1%)^7,8 that could endure impact and vibration of the manufacturing process and transporting. However, formulation A did not have enough strength for impact because its hardness was 2.1 ± 0.5 kgf. Differences in hardness and friability between formulations reflect the differences in the additives and compression pressure.

PTP requiring pushing out strengths of 20–30 N are reportedly easy to open.^6,11 The strength required for pushing out from a PTP for formulations A, B, D, E, and F was approximately 20–30 N (Figure 1), confirming the ease of pushing the tablets out. However, PTP pushing out strength of formulation C was 34.4 ± 3.0 N, which indicates that patients may feel pain on their fingertips upon pushing out the tablets of formulation C. Differences in PTP pushing out strengths between formulations are based on differences in PTP materials and thicknesses.

Conclusion

In this study, we examined hydrophilia, tablet strength, and pushing out by PTP to evaluate the physical properties of each lansoprazole OD tablet formulations. This study indicated that the physical properties of lansoprazole OD tablets, such as their hydrophilia, tablet strength, and PTP pushing out strength, differ between formulations. Again, this study provides useful information for selecting lansoprazole OD tablets individually suitable for each patient.