Effect of preparation methods on tosufloxacin tosylate/ hydroxypropyl-β-cyclodextrin inclusion complex

Sun, Jianfei; Hong, Hailong; Zhu, Ning; Han, Limin; Suo, Quanling

doi:10.1590/s2175-97902022e18650

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Brazilian Journal of Pharmaceutical Sciences

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Article • Braz. J. Pharm. Sci. 58 • 2022 • https://doi.org/10.1590/s2175-97902022e18650 copy

Effect of preparation methods on tosufloxacin tosylate/ hydroxypropyl-β-cyclodextrin inclusion complex

Authorship SCIMAGO INSTITUTIONS RANKINGS

Abstract

The main purpose of this work was to compare the effects of the four preparation methods on the TFLX/HP-β-CD inclusion complex. The effects of different preparation methods on the inclusion complex were investigated by SEM, DSC, PXRD, FT-IR and ¹H NMR. All the characterization information indicated that the four preparation methods could cause interaction between TFLX and HP-β-CD, but the inclusion complex prepared by solvent evaporation has more reaction sites. Phase solubility experiments demonstrated that the inclusion reaction was spontaneous. In vitro dissolution experiments showed that the dissolution of the inclusion complex in water was: solvent evaporation method (64.39%) > grinding method (42.37%) > ultrasonic method (40.00%) > freezing method (36.08%), and all higher than pure TFLX and physical mixture. These results suggest that the solvent evaporation is the most suitable method for preparing TFLX/HP-β-CD inclusion complexes.

Keywords:
Tosufloxacin tosylate; Hydroxypropyl-β-cyclodextrin; Methods; Inclusion complex

Number	Factors				Embedding efficiency (%)
Number	A	B	C	D(Empty column)	Embedding efficiency (%)
1	1 (1:1)	1 (40 °C)	1 (30 min)	1	52.40
2	1	2 (50 °C)	2 (60 min)	2	47.23
3	1	3 (60 °C)	3 (120 min)	3	33.78
4	2 (1:2)	1	2	3	47.14
5	2	2	3	1	50.44
6	2	3	1	2	27.52
7	3 (2:1)	1	3	2	28.74
8	3	2	1	3	35.45
9	3	3	2	1	42.08
K₁	133.41	128.28	115.37	144.92	C_T=14784.94
K₂	125.1	133.12	136.45	103.49
K₃	106.27	103.38	112.96	116.37
R	9.05	9.91	7.83	13.81

Number	Factors				Embedding efficiency (%)
Number	A	B	C	D(Empty column)	Embedding efficiency (%)
1	1 (1:1)	1 (30 min)	1 (0.5 mL)	1	32.79
2	1	2 (1 h)	2 (1 mL)	2	58.98
3	1	3 (2 h)	3 (1.5 mL)	3	49.83
4	2 (1:2)	1	2	3	51.61
5	2	2	3	1	44.29
6	2	3	1	2	34.35
7	3 (2:1)	1	3	2	61.02
8	3	2	1	3	39.25
9	3	3	2	1	43.70
K₁	141.60	145.42	106.39	120.78	C_T=19211.81
K₂	130.25	142.52	154.29	154.35
K₃	143.97	127.88	155.14	140.69
R	13.72	17.54	48.75	33.57

Number	Factors				Embedding efficiency (%)
Number	A	B	C	D	Embedding efficiency (%)
1	1 (1:1)	1 (40 °C)	1 (15 min)	1 (100 W)	66.77
2	1	2 (50 °C)	2 (30 min)	2 (150 W)	57.41
3	1	3 (60 °C)	3 (60 min)	3 (200 W)	46.76
4	2 (1:2)	1	2	3	12.98
5	2	2	3	1	16.03
6	2	3	1	2	30.36
7	3 (2:1)	1	3	2	23.22
8	3	2	1	3	20.71
9	3	3	2	1	18.45
K₁	170.94	102.97	117.84	101.25	C_T=9518.60
K₂	59.37	94.15	88.84	119.99
K₃	62.38	95.57	86.01	89.45
R	111.57	8.82	31.83	30.54

Number	Factors				Embedding efficiency (%)
Number	A	B	C	D(Empty column)	Embedding efficiency (%)
1	1 (1:1)	1 (0 °C)	1 (6 h)	1	13.68
2	1	2 (2 °C)	2 (12 h)	2	16.50
3	1	3 (4 °C)	3 (18 h)	3	15.53
4	2 (1:2)	1	2	3	11.09
5	2	2	3	1	19.38
6	2	3	1	2	18.25
7	3 (2:1)	1	3	2	33.50
8	3	2	1	3	42.90
9	3	3	2	1	41.99
K₁	45.71	58.27	74.83	75.05	C_T=6258.03
K₂	48.72	78.78	69.58	68.25
K₃	118.39	75.77	68.41	68.61
R	72.68	20.51	6.42	6.8

T (°C)	Equations	R²	K (L/mol)	∆G (KJ/mol)	∆H (KJ/mol)	∆S (J/mol*K)
30	$Y = 0.0936 X + 1.0141$	0.9960	101.83	-10.27	7.32	60.15
40	$Y = 0.1055 X + 1.1324$	0.9916	104.15	-12.10
50	$Y = 0.1305 X + 1.2367$	0.9815	121.36	-12.89
60	$Y = 0.1148 X + 1.7057$	0.9856	76.03	-12.00

Universidade de São Paulo, Faculdade de Ciências Farmacêuticas Av. Prof. Lineu Prestes, n. 580, 05508-000 S. Paulo/SP Brasil, Tel.: (55 11) 3091-3824 - São Paulo - SP - Brazil
E-mail: bjps@usp.br

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[1] *Correspondence: H. L. Hong. College of Chemical Engineering. Inner Mongolia University of Technology. Hohhot 010051, China. Phone: +86-471-6575722. Fax: +86-471-6575722. E-mail:honghailong_1979@163.com