ABSTRACT
OBJECTIVES: To investigate the effects of formulation composition on the physico-chemical and drug release properties of mucoadhesive buccal films prepared by melt extrusion technology, using a response surface methodology. METHODS: Salbutamol sulphate, an antiasthmatic drug was used for this study. Klucel hydroxypropylcellulose (HPC) EF (film-forming polymer), Benecel hydroxypropylmethylcellulose (HPMC) K-15M (drug release retardant) and polyethylene glycol (PEG) 4500 (plasticiser) were the three independent factors utilised for the study. The responses were fitted to a full quadratic model and P-values for each of the factors were used to determine their significance on the film characteristics. KEY FINDINGS: Films were successfully extruded using the corotating twin-screw extruder. The torque during extrusion was found to be significantly affected by all the three factors and no interaction between factors was observed. A significant interaction was observed between HPC and PEG 4500 for stiffness of films. For disintegration time and swelling index, a significant interaction was found between HPC and HPMC. The in vitro % drug release was directly correlated with HPMC content and not with other factors and varied from 69-89% at 4 h. CONCLUSIONS: The influence of extrusion process and formulation parameters on salbutamol sulphate films was elucidated, indicating the use of melt extrusion as a feasible method for film preparation.
Subject(s)
Adhesives/administration & dosage , Adhesives/chemistry , Mouth Mucosa/drug effects , Administration, Buccal , Albuterol/administration & dosage , Albuterol/chemistry , Anti-Asthmatic Agents/administration & dosage , Anti-Asthmatic Agents/chemistry , Cellulose/analogs & derivatives , Cellulose/chemistry , Chemistry, Pharmaceutical/methods , Drug Delivery Systems/methods , Drug Liberation/drug effects , Hot Temperature , Hypromellose Derivatives/chemistry , Plasticizers/chemistry , Polyethylene Glycols/chemistry , Polymers/chemistry , Technology, Pharmaceutical/methods , Tensile Strength/drug effectsABSTRACT
The choice of excipients constitutes a major part of preformulation and formulation studies during the preparation of pharmaceutical dosage forms. The physical, mechanical, and chemical properties of excipients affect various formulation parameters, such as disintegration, dissolution, and shelf life, and significantly influence the final product. Therefore, several studies have been performed to evaluate the effect of drug-excipient interactions on the overall formulation. This article reviews the information available on the physical and chemical instabilities of excipients and their incompatibilities with the active pharmaceutical ingredient in solid oral dosage forms, during various drug-manufacturing processes. The impact of these interactions on the drug formulation process has been discussed in detail. Examples of various excipients used in solid oral dosage forms have been included to elaborate on different drug-excipient interactions.
