Formulation and evaluation of mucoadhesive glipizide films

被引:16
作者
Rajput, Ganesh [1 ]
Majmudar, Falguni [2 ]
Patel, Jayvadan [1 ]
机构
[1] SP Vidyadham, Nootan Pharm Coll, Visnagar 384315, India
[2] NHL Municipal Med Coll, Ahmadabad, Gujarat, India
关键词
glipizide; mucoadhesive film; factorial design; desirability function; hypoglycemic effect; FLOATING MATRIX TABLETS; RELEASE FORMULATION; DRUG-DELIVERY; OPTIMIZATION;
D O I
10.2478/v10007-011-0017-3
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Glipizide is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. Increase in hydroxypropyl cellulose concentration resulted in a higher tensile strength and elongation at break, while increase in concentration of PEG 400 was reflected in a decrease in tensile strength and increase of elongation at break. Glipizide/hydroxypropyl cellulose/PEG 400 (2.5:1:0.5) (GF5) was found to be the optimal composition for a novel mucoadhesive stomach formulation that showed good peelability, relatively high swelling index, moderate tensile strength, and stayed on rat stomach mucosa up to 8 h. In vivo testing of the mucoadhesive films with glipizide demonstrated a potential hypoglycemic effect.
引用
收藏
页码:203 / 216
页数:14
相关论文
共 18 条
[1]   Development and Evaluation of Acid-buffering Bioadhesive Vaginal Tablet for Mixed Vaginal Infections [J].
Alam, Mohd Aftab ;
Ahmad, Farhan Jalees ;
Khan, Zeenat Iqbal ;
Khar, Roop Krishen ;
Ali, Mushir .
AAPS PHARMSCITECH, 2007, 8 (04)
[2]   Optimisation of floating matrix tablets and evaluation of their gastric residence time [J].
Baumgartner, S ;
Kristl, J ;
Vrecer, F ;
Vodopivec, P ;
Zorko, B .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 195 (1-2) :125-135
[3]   COMPARATIVE EFFICACY OF A ONCE-DAILY CONTROLLED-RELEASE FORMULATION OF GLIPIZIDE AND IMMEDIATE-RELEASE GLIPIZIDE IN PATIENTS WITH NIDDM [J].
BERELOWITZ, M ;
FISCHETTE, C ;
CEFALU, W ;
SCHADE, DS ;
SUTFIN, T ;
KOURIDES, IA .
DIABETES CARE, 1994, 17 (12) :1460-1464
[4]   OPTIMIZATION OF SOTALOL FLOATING AND BIOADHESIVE EXTENDED-RELEASE TABLET FORMULATIONS [J].
CHUEH, HR ;
ZIA, H ;
RHODES, CT .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1995, 21 (15) :1725-1747
[5]  
Dokoumetzidis A, 2006, PHARM RES-DORDR, V23, P256, DOI 10.1007/s11095-006-9093-3
[6]   Glipizide - A review of the pharmacoeconomic implications of the extended-release formulation in Type 2 diabetes mellitus [J].
Foster, RH ;
Plosker, GL .
PHARMACOECONOMICS, 2000, 18 (03) :289-306
[7]   Development and characterization of bioadhesive vaginal films of sodium polystyrene sulfonate (PSS), a novel contraceptive antimicrobial agent [J].
Garg, S ;
Vermani, K ;
Garg, A ;
Anderson, RA ;
Rencher, WB ;
Zaneveld, LJD .
PHARMACEUTICAL RESEARCH, 2005, 22 (04) :584-595
[8]  
KAHN CR, 1991, GOODMAN GILMANS PHAR, P1712
[9]   MECHANISMS OF SOLUTE RELEASE FROM POROUS HYDROPHILIC POLYMERS [J].
KORSMEYER, RW ;
GURNY, R ;
DOELKER, E ;
BURI, P ;
PEPPAS, NA .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1983, 15 (01) :25-35
[10]   Effect of formulation variables on the floating properties of gastric floating drug delivery system [J].
Li, SF ;
Lin, SS ;
Daggy, BP ;
Mirchandani, HL ;
Chien, YW .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2002, 28 (07) :783-793