Characterization of cellulosic hot-melt extruded films containing lidocaine.

Hot-melt extrusion technology was used to produce thin films containing a model drug, lidocaine, and the cellulosic polymers hydroxypropyl cellulose (HPC) and hydroxypropyl methyl cellulose (HPMC). Two film formulations were extruded and compared, one containing only HPC and the other containing HPC:HPMC (80:20). Thermal analysis of the films using differential scanning calorimetry (DSC) suggested that the drug existed in the amorphous condition, which was confirmed by wide angle X-ray diffractometry. Sustained release of the drug was observed from both of the polymer matrices. Dissolution profiles suggested that HPMC retarded the drug release from HPC:HPMC (80:20) films. However, the mechanism of drug release from both of the films was predominantly diffusion of the drug through the polymer matrices. Incorporation of HPMC also increased both adhesive strength and work of adhesion as compared to the HPC-only films.

[1]  W I Higuchi,et al.  Drug release from wax matrices. I. Analysis of data with first-order kinetics and with the diffusion-controlled model. , 1968, Journal of pharmaceutical sciences.

[2]  S. Agarwal,et al.  PREPARATION AND EVALUATION OF MUCO-ADHESIVE BUCCAL FILMS OF CLOTRIMAZOLE FOR ORAL CANDIDA INFECTIONS , 1997 .

[3]  R. Gurny,et al.  Local delivery of antimicrobial agents for the treatment of periodontal diseases. , 2000, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[4]  S. Agarwal,et al.  Preparation and evaluation of bioerodible buccal tablets containing clotrimazole , 1996 .

[5]  T. Nagai,et al.  Mucosal dosage form of lidocaine for toothache using hydroxypropyl cellulose and carbopol. , 1982, Chemical & pharmaceutical bulletin.

[6]  A. Hussain,et al.  Polymer erosion and drug release characterization of hydroxypropyl methylcellulose matrices. , 1998, Journal of pharmaceutical sciences.

[7]  E. Ibezim,et al.  The release properties of microcapsules prepared with polymerized latex of Landolphia dulcis , 1998 .

[8]  Feng Zhang,et al.  Hot Melt Extrusion of Acrylic Films , 1996, Pharmaceutical Research.

[9]  Guohua Zhang,et al.  Prediction of Drug Release from Hydroxypropyl Methylcellulose (HPMC) Matrices: Effect of Polymer Concentration , 1993, Pharmaceutical Research.

[10]  B. Lippold,et al.  Controlled release of drugs from hydrocolloid embeddings , 1996 .

[11]  G. M. Swallowe.  Mechanical Properties and Testing of Polymers , 1999 .

[12]  C. Wong,et al.  Polymeric films as vehicle for buccal delivery: swelling, mechanical, and bioadhesive properties. , 1999, Journal of pharmacy & pharmaceutical sciences : a publication of the Canadian Society for Pharmaceutical Sciences, Societe canadienne des sciences pharmaceutiques.

[13]  K. Florey,et al.  Analytical profiles of drug substances , 1972 .

[14]  Teruo Okano,et al.  Biorelated Polymers and Gels: Controlled Release and Applications in Biomedical Engineering , 1998 .

[15]  B. Lippold,et al.  Zero-Order Drug Release from Hydrocolloid Matrices , 1993, Pharmaceutical Research.

[16]  P. Sharma,et al.  Formulation and evaluation of buccal mucoadhesive patches of terbutaline sulphate , 2001 .

[17]  R. Jalil,et al.  Effect of Viscosity Increasing Agent and Electrolyte Concentration on the Release Rate of Theophylline from a HPMC Based Sustained Release Capsules , 1993 .

[18]  C. Wong,et al.  An in-vitro method for buccal adhesion studies: importance of instrument variables. , 1999, International journal of pharmaceutics.

[19]  M. Sargon,et al.  Chitosan films and hydrogels of chlorhexidine gluconate for oral mucosal delivery. , 2000, International journal of pharmaceutics.

[20]  J. Perfect,et al.  Diagnosis and treatment of oropharyngeal candidiasis in patients infected with HIV: a critical reassessment. , 1999, AIDS research and human retroviruses.

[21]  Nikolaos A. Peppas,et al.  Surface, interfacial and molecular aspects of polymer bioadhesion on soft tissues , 1985 .

[22]  M. Repka,et al.  Influence of plasticizers and drugs on the physical-mechanical properties of hydroxypropylcellulose films prepared by hot melt extrusion. , 1999, Drug development and industrial pharmacy.

[23]  S. Prodduturi,et al.  Production and Characterization of Hot-Melt Extruded Films Containing Clotrimazole , 2003, Drug development and industrial pharmacy.

[24]  George Zografi,et al.  The molecular basis of moisture effects on the physical and chemical stability of drugs in the solid state , 1990 .

[25]  J. Mcginity,et al.  Influence of Aging on the Physical-Mechanical Properties of Acrylic Resin Films Cast from Aqueous Dispersions and Organic Solutions , 1993 .