Preparation and in vitro Release of Ketoprofen/acid-montmorillonite†

doi:10.7503/cjcu20170003

Abstract

Abstract:

With acid-montmorillonite(acid-MMT) as the carrier of ketoprofe(KPF), KPF/acid-MMT composite was prepared by ion-exchange method and characterized by powder XRD, BET, SEM, etc. The effect of the pH of release media on in vitro release of ketoprofen was assessed by the dialysis method. Three models for in vitro drug release were used to simulate the release performance of KPF from the KPF/acid-MMT composite. The results showed that the surface area of acid-MMT increased from 19.66 m²/g to 202.84 m²/g, and the drug-loading increased from 18.09% to 37.24% compared with MMT. In vitro release ability of KPF/acid-MMT composite was affected by pH of the release solution. In the artificial gastric juice(pH=1.2) and in the artificial intestinal juice(pH=6.8), the in vitro cumulative release amounts of the composites were 18.6% and 86.7%, respectively. The zero order kinetics model could be used to describe the variation of in vitro release rate.

Key words: Montmorillonite, Ketoprofen, Acid-treatment, pH-response, Sustained release carrier

CLC Number:

O611.4

TrendMD:

LI Tingting, ZHAO Lele, WANG Ruili, ZHANG Shuqiu. Preparation and in vitro Release of Ketoprofen/acid-montmorillonite^†[J]. Chem. J. Chinese Universities, 2017, 38(5): 722.

Figures/Tables 9

Fig.1 Powder XRD patterns of montmorillonite and its compositesa. MMT; b. acid-MMT; c. KPF/acid-MMT.

Fig.2 N2 adsorption-desorption isotherms of montmorillonite and its compositesa. MMT; b. KPF/acid-MMT; c. acid-MMT.

Table 1 Textural properties of different samples

Sample	S_BET/(m²·g^-1)	V/(cm³·g^-1)	d/nm	w(SiO₂)^*(%)	w(Al₂O₃)^*(%)
MMT	19.66	0.04	3.81	65.1	17.1
Acid-MMT	202.84	0.54	6.19	55.8	12.1
KPF/acid-MMT	98.55	0.29	4.48	56.1	11.9

Fig.3 FTIR spectra of montmorillonite and its compositesa. MMT; b. acid-MMT; c. KPF/acid-MMT.

Fig.4 TG-DTG curves of MMT(A), acid-MMT(B) and KPF/acid-MMT(C)

Fig.5 SEM images of MMT(A), acid-MMT(B) and KPF/acid-MMT(C)

Fig.6 Influence of KPF concentration on drug loading efficiencya. MMT; b. acid-MMT.

Fig.7 Cumulative release amount of KPF/acid-MMT compositea. pH=1.2; b. pH=6.8.

Table 2 Results of mathematical fitting with different equations*

Model	Expression	Equation	R²
Zero-order	Q=Bt+A	Q=16.29+6.41t	0.9745
First-order	ln(100-Q)=Bt+A	ln(100-Q)=4.52-0.14t	0.8731
Higuchi model	Q=Bt¹^/²+A	Q=27.09t¹^/²-7.04	0.9613

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