原辅料相容性研究.pdfVIP

Review Paper Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review. Sonali S. Bharate,a* Sandip B. Bharateb and Amrita N. Bajajc a P.E. Society’s Modern College of Pharmacy (For Ladies), Borhadewadi, At/Post- Moshi, Tal-Haweli, Dist- Pune, Maharashtra – 412105, India b STES’s Sinhgad College of Pharmacy, Off Sinhgad Road, Vadgaon (Budruk), Pune-411041, India c C.U. Shah College of Pharmacy, S.N.D.T. Women’s University, Juhu Tara Road, Santacruz (E), Mumbai, Maharashtra-400049, India Received: 05 March 2010; Acc epted: 03 November 2010 ABSTRACT Studies of active drug/excipient compatibility represent an important phase in the preformulation stage of the development of all dosage forms. The potential physical and chemical interactions between drugs and excipients can affect the chemical nature, the stability and bioavailability of drugs and, consequently, their therapeutic efficacy and safety. The present review covers the literature reports of interaction and incompatibilities of commonly used pharmaceutical excipients with different active pharmaceutical ingredients in solid dosage forms. Examples of active drug/excipient interactions, such as transacylation, the Maillard browning reaction, acid base reactions and physical changes are discussed for different active pharmaceutical ingredients belonging to different thera- peutic categories viz antiviral, anti-inflammatory, antidiabetic, antihypertensive, anti-convulsant, an- tibiotic, bronchodialator, antimalarial, antiemetic, antiamoebic, antipsychotic, antidepressant, anti- cancer, anticoagulant and sedative/hypnotic drugs and vitamins. Once the solid-state reactions of a pha