Drug excipient interaction pdf

Unintended physicochemical interaction of an excipient with a drug substance in a dosage form can result in the complexation or binding of the drug, resulting in slow andor incomplete drug release in a dissolution medium. Pdf drugexcipient interaction and its importance in dosage form. Loratadine and carvedilol were chosen as model basic drugs. Drugexcipient interaction and its importance in dosage form development nishath fathima, tirunagari mamatha, husna kanwal qureshi, nandagopal anitha and jangala venkateswara rao excipients are included in dosage forms to aid manufacture, administration or absorption. Pdf drugexcipient interaction and incompatibilities. Although technically inactive from a therapeutic sense, pharmaceutical excipients are critical and essential components of a modern drug product. Mixture should be examined under n 2 to eliminate oxidative and pyrrolytic effects at heating rate 2, 5 or 100 c min on dsc apparatus. Drugexcipient compatibility studies study of drug excipient compatibility is an important phase in the preformulation stage of drug development. Drugexcipient compatibility studies have been used as an approach for acceptingrejecting excipients for use in pharmaceutical formulations, thus allowing the rapid optimization of a dosage form with respect to patentability, processing, drug release, elegance.

The samples are then visually observed for any changes in color or physical characteristics, and the drug. Pdf on jan 1, 2018, bapi gorain and others published drugexcipient interaction and incompatibilities find, read and cite all the research. Such interactions generally cause loss of product quality. A number of techniques can be used to indicate the drug excipient interaction. The preformulation screening of drug excipient interaction requires 1. Pdf drugexcipient interaction and its importance in.

Pharm pharmaceutics qis college of pharmacy ongole, andhra pradesh 1 pharmacylectures. These interactions adversely affect the therapeutic efficacy, safety, and appearance of the active constituent tekade et al. Identification, characterization and drugexcipient. However, unfavourable combinations of drug drug and drug excipient may result in interaction and rises the safety concern. Drug excipient compatibility testing at an early stage helps in the selection of excipient that increases the probability of developing a stable dosage form. Some specific examples of drugexcipient impurity interaction from. The potential physical and chemical interactions between drugs and excipients can affect the chemical, physical, therapeutical properties and stability of the dosage form. Introduction excipients are considered as pharmacologically inert but can initiate, propagate or participate in chemical or physical interactions with drug components, which may. Excipients interactions and drug degradation due to flavors, lactose. Dissolution stability studies of suspensions of prolonged. Drugexcipient compatibility studies creative biolabs.

Kuwata 2, raj suryanarayanan 1 department of pharmaceutics, university of minnesota, minneapolis, minnesota 55455, usa 2 department of chemistry, macalester college, saint paul, minnesota. Packageexcipient interactions these interactions are discussed in detail as follows. We apply a range of techniques thermal methods, microscopy, xray diffraction, ir spectroscopy to characterize a drug atenolol, several excipients pvppolyvinylpyrrolidone, mgstmagnesium stearate, avicel and drug excipients mixtures either as. Interactions and incompatibilities of pharmaceutical. In addition to that, several degradation products of the 32 6aminocaproic acid reacting with itself, e. Pharmpharmaceutics 1st semester, assam downtown university, guwahati guided by. Maillard reaction is one of the most important and well known drug excipient interactions which is studied by many researchers in drugs containing at least one amine functional group.

The potential physical and chemical interactions between drugs and excipients can affect the chemical, physical, therapeutical properties and. Compatibility study of metformin with pharmaceutical. Interaction between drugs and excipients can alter stability and bioavailability of drugs, thereby, affecting its safety andor efficacy 1. Although considered pharmacologically inert, excipients can initiate, propagate or participate in chemical or physical interactions with drug compounds, which may compromise the effectiveness of a medication. Drugs may trigger the appearance of hypohydration by means of the increase of water elimination through either diarrhea, urine or sweat. Drug excipient incompatibility drug excipient interaction incompatibilitygeneral aspects. Although considered pharmacologically inert, excipients can initiate. In academic and industrial research, there is a huge interest in understanding the different mechanisms of drug excipient interactions with regards to formulation processes or with respect to dissolution and absorption. Effect on molecular mobility and physical stability of ketoconazoleorganic acid coamorphous systems. Drugdrugdrugexcipient compatibility studies on curcumin. Thermal analysis, tga, dta and dsc, has been used extensively for chemical stability and compatibility studies59. Drugexcipient interaction and its importance in dosage form. Studies of active drugexcipient compatibility represent an important phase in the. Characterization of drugexcipient compatibility christin t.

Mixture should be examined under n 2 to eliminate oxidative and pyrrolytic effects at heating rate 2, 5 or 100c min on dsc apparatus. Excipients are included in dosage forms to aid manufacture administration or absorption. Different tablet formulations with or without excipients tested were prepared, and assessed for drug dissolution and permeability. Inactive ingredients are added during the manufacturing process of pharmaceutical products such as tablets, capsules, suppositories, and injections. Excipient applications in formulation design and drug. Excipient development for pharmaceutical, biotechnology. The interaction between celecoxib and magnesium stearate or colloidal silicon dioxide were determined in the aqueous dispersions by ftir. Cyclodextrin interaction inferred that there was no physical and chemical interaction between drug and. Inactive ingredients are components of a drug product that do not increase or affect the therapeutic action of the active ingredient, which is usually the active drug. Abstract in recent years there has been an increasing interest in the study of drug excipient interactions in pharmaceutical dosage forms. Case studies and overview of drug degradation pathways, authorkishore kumar hotha and swapan roychowdhury and veerappan subramanian, year2016 kishore kumar hotha, swapan roychowdhury, veerappan subramanian the. The information on excipient performance can be used, as appropriate, to justify the choice and quality attributes of the excipient, and to support the justification of the drug product specification 3. This paper discusses mechanistic basis of known drug excipient interactions with case studies and provides an overview of common underlying themes in solid, semisolid and parenteral dosage forms. Excipients are included in dosage forms to aid manufacture, administration or absorption.

Pdf drugexcipient interaction and incompatibilities researchgate. Ist involves storage of drug excipient blends with, or without moisture, at elevated tempertures for a specific period of time typically 34 weeks to accelerate drug degradation and interaction with excipients. The preformulation screening of drug excipient interaction requires 5 mg of drug, in 50% mixture 1. Study of drugexcipient interactions regarding solubility. Drugexcipient compatibility studies the pharma innovation journal. Drugexcipientshell interactions using thermoplastic. Excipients and drugs may have certain incompatibilities which lead to drug excipient interaction. This guidance is intended to assist applicants in complying with the content and format requirements of labeling for human prescription drug and biological products under 21 cfr 201. Ananta chaudhary, department of pharmacy, assoiate professor, adtu, guwahati.

Isothermal stress testing method was used to assess the compatibility of drug drug drug excipient. Hence, the present study was aimed to assess the interaction of curcumin with excipients used in nanoformulations. Drug excipient interaction in pharmaceutical dosage forms the active pharmaceutical ingredients are in intimate contact with the excipient which are greater quantity excipient and drugs may have certain incompatibility which lead to drug excipient interaction. However, to date, research on the interaction between hydration status and drugs excipients has been scarce. Each chapter is contributed by chosen experts in their respective. Aldehydes, alcohols, phenols, alkaloids and unsaturated fats and oils are all susceptible to oxidation. Fung mh1, devault m2, kuwata kt2, suryanarayanan r1. Pdf drugexcipient compatibility studies by physico. Labeling for human prescription drug and biological.

The discovery of a new chemical entity with promising efficacy and toxicity is. It is important to assess the risk whether such interactions would reduce oral bioavailability of a drug from its dosage form. Guidance for industry food and drug administration. Towards an improved understanding of drug excipient interactions to enable rapid optimization of nanosuspension formulations.

This book presents a concise summary of relevant scientific and mechanistic information that can aid the use of excipients in formulation design and drug delivery applications. Pharmaceutical dosage form is a combination of active pharmaceutical ingredients api and excipients. Most basic amine drugs that are substantially ionized and soluble at the same ph as an insoluble excipient of opposite charge are likely to undergo such interactions. Drug excipient interactions between 6aminocaproic acid and the excipients citric acid were found in highly concentrated solutions at ph 4. The ftir and dsc study were performed to determine the drug excipient compatibility of diltiazem hydrochloride. Celecoxib, drug excipient interaction, permeability, caco2 cells 423. Pdf interactions and incompatibilities of pharmaceutical. Interactions and incompatibilities of pharmaceutical excipients with. Excipient interactions and best practice guide for use of excipients. This improves patient compliance, especially in children. Drug oa molecular complexes were formed upon addition of oleic acid oa in the. Drugexcipient interaction and its importance in dosage.