Excipient–Drug Interactions in Parenteral Formulations

Akers, Michael J.

doi:10.1002/jps.10154

Cited by 180 publications

(68 citation statements)

References 64 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Although reasonable success has been achieved in formulating water-insoluble drugs using liposomes (Schwendener & Schott 1996), emulsions (Floyd 1999;Nakano 2000), microemulsions (Lawrence & Rees 2000), solid dispersion technology (Serajuddin 1999;Leuner & Dressman 2000;Breitenbach 2002) and inclusion complexes employing cyclodextrins (Loftsson & Brewster 1996;Stella & Rajewski 1997;Akers 2002), there is no universal approach applicable to all drugs. Hence, there is a growing need for a unique strategy that can tackle the formulation-related problems associated with the delivery of hydrophobic drugs in order to improve their clinical efficacy and optimize their therapy with respect to pharmacoeconomics.…”

Section: Introductionmentioning

confidence: 99%

Nanosuspensions: a promising drug delivery strategy

Patravale

Date

Kulkarni

2004

Journal of Pharmacy and Pharmacology

758

433

View full text Add to dashboard Cite

Nanosuspensions have emerged as a promising strategy for the efficient delivery of hydrophobic drugs because of their versatile features and unique advantages. Techniques such as media milling and highpressure homogenization have been used commercially for producing nanosuspensions. Recently, the engineering of nanosuspensions employing emulsions and microemulsions as templates has been addressed in the literature. The unique features of nanosuspensions have enabled their use in various dosage forms, including specialized delivery systems such as mucoadhesive hydrogels. Rapid strides have been made in the delivery of nanosuspensions by parenteral, peroral, ocular and pulmonary routes. Currently, efforts are being directed to extending their applications in site-specific drug delivery.

show abstract

Section: Introductionmentioning

confidence: 99%

Nanosuspensions: a promising drug delivery strategy

Patravale

Date

Kulkarni

2004

Journal of Pharmacy and Pharmacology

758

433

View full text Add to dashboard Cite

show abstract

“…Localized tissue damage at the injection site accounts for the pain, redness and sterile inflammation, mostly low grade and readily tolerated, following IM administration of oil vehicle injections [20]. The irritation and inflammatory reactions arise from the intrinsic physicochemical properties of either the drugs, excipients [21] or vehicle [22,23]. Consequently, although post-injection pain is expected after any IM injection, the severity, duration and interference with regular activities may vary between individuals, injections and products, and has been subject to few systematic studies.…”

Section: Introductionmentioning

confidence: 99%

Factors influencing time course of pain after depot oil intramuscular injection of testosterone undecanoate

Sartorius¹,

Fennell²,

Spasevska³

et al. 2010

Asian J Androl

View full text Add to dashboard Cite

Pain following depot intramuscular (IM) injection of oil vehicle-based drugs has been little studied. This study aimed to determine prospectively the prevalence, determinants, severity and functional consequences of pain during the week after IM injection of 1 000 mg testosterone undecanoate (TU) in a 4-mL castor oil vehicle. Androgendeficient men receiving regular T replacement therapy at an academic andrology clinic were recruited to report pain scores using a coloured visual linear analogue scale at seven times over the first day and daily for a week after a deep IM gluteal injection. The time course and covariables influencing pain scores were analysed by mixed model analysis of variance (ANOVA). Following 168 injections in 125 men, pain was reported by 80% of men, peaking immediately after injection, reaching only moderate severity, lasting 1-2 days and returning to baseline by day 4. The pain required little analgesic use and produced minimal interference in daily activities. The time course of pain scores was reproducible in the 43 men who underwent two consecutive injections. Pain was more severe in men who had an earlier painful injection, but less severe in older and more obese men. There were negligible differences in post-injection pain experience between experienced nurses administering injections. Deep IM gluteal injection of depot TU in 4-mL castor oil is well tolerated and post-injection pain is influenced by earlier painful injection experience, as well as age and obesity.

show abstract

“…The presence of such interactions, however, does not necessarily imply an incompatibility, as the pharmacological action of the drug may remain unchanged in the presence of the polymer, and can even be enhanced. The occurrence of drug-excipient close contacts in solid matrices is presently the object of some controversy, and despite evidence of either synergistic or negative effects, [11][12][13] there are no conclusive results to be reported. Thus, further study is needed in order to clarify this matter.…”

Section: Introductionmentioning

confidence: 99%

Drug–excipient interactions in ketoprofen: A vibrational spectroscopy study

2006

View full text Add to dashboard Cite

Ketoprofen (3-benzoyl-a-methylbenzeneacetic acid) is a widely used nonsteroidal antiinflammatory drug (NSAID), always administered in the form of drug-excipient physical mixtures (PMs). The occurrence of possible interactions between ketoprofen and two commonly used excipients-lactose (LAC) and polyvinylpyrrolidone (PVP)-was evaluated, through vibrational spectroscopy techniques [both Raman and Inelastic Neutron Scattering (INS)]. Spectral evidence of drug:excipient close contacts, which were enhanced by aging, was verified for the (1:1) (w:w) (ketoprofen:PVP) and (ketoprofen:LAC) PMs, both by Raman and INS. These interactions were found to involve mainly the central carbonyl and the terminal methyl-carboxylic moieties of the ketoprofen molecule, this being reflected in particular vibrational modes, such as the methyl torsion, the outof-plane CÀ ÀOH bending, and the inter-ring C¼ ¼O stretching. #

show abstract

Excipient–Drug Interactions in Parenteral Formulations

Cited by 180 publications

References 64 publications

Nanosuspensions: a promising drug delivery strategy

Nanosuspensions: a promising drug delivery strategy

Factors influencing time course of pain after depot oil intramuscular injection of testosterone undecanoate

Drug–excipient interactions in ketoprofen: A vibrational spectroscopy study

Contact Info

Product

Resources

About