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Chemical Modulation of Topical and Transdermal Permeation
Published in Marc B. Brown, Adrian C. Williams, The Art and Science of Dermal Formulation Development, 2019
Marc B. Brown, Adrian C. Williams
Counter ions can directly influence the effective physicochemical properties of the parent drug, such as lipophilicity. Ion-pairing can be simply through the selection of a salt for the active drug, such as the use of the sulphate of terbutaline or lignocaine hydrochloride. Alternatively, counter ions can be selected to possess chemical penetration-enhancing activity. For example, oleic acid was paired with ondansetron, salicylates have been paired with amines and quaternary ammonium ions, and ion-pairs of loxoprofen with organic amines such as trimethylamine have been shown to enhance flux of this non-steroidal anti-inflammatory agent.
Chronic postsurgical pain after total knee arthroplasty: A prospective cohort study in Japanese population
Published in Modern Rheumatology, 2021
Koji Aso, Masahiko Ikeuchi, Shogo Takaya, Natsuki Sugimura, Masashi Izumi, Hiroyuki Wada, Yusuke Okanoue, Jyunpei Dan
All TKAs were performed through a 12–13-cm anterior knee incision and medial parapatellar arthrotomy. The tourniquet was used for a brief period only for the cementation of the implants and wound closure. Posterior-stabilized (PS) or cruciate-retaining (CR) components (ACTIYAS®, Bi-surface®; Kyocera, Kyoto, Japan: Persona®, Vanguard®, NexGen LPS flex®, NexGen MIS Tibial Component®; Zimmer Biomet, Warsaw, IN: PFC Sigma®; Johnson & Johnson, Raynham, MA) were used in 193 and 18 knees, respectively. All surgeries were performed by or under supervision of a senior doctors (M. I. or K. A.) in our hospital. Both general anesthesia and combination of local infiltration of analgesia (LIA) with ultrasound-guided femoral nerve block were used in all patients except compromised host and patients with diabetes mellitus or severe chronic kidney disease. After the bone cut, analgesic drugs consisting of 20 ml of 0.75% ropivacaine, 20 ml saline and 6.6 mg of dexamethasone were injected into the peri-articular tissues when using LIA. Regular postoperative pain management was as follows: fentanyl intravenous patient-controlled analgesia was used during a 24-h post-operative period. Loxoprofen and 2000 mg acetaminophen were used for approximately 1week. For severe postoperative acute pain, additional prescription of weak opioid was allowed as needed, and the opioid use was minimized. All patients in this study were managed using a standard clinical pathway program. The standard rehabilitation schedule was as follows: post-operative day (POD) 1: quadriceps setting exercise, ambulation using a walking frame with weight bearing as tolerated, active-assisted range-of-motion exercise; POD7: staircase climbing; POD14–16: patients were discharged to go home or sent to a rehabilitation center.
Formulation and evaluation of interpenetrating polymeric network for controlled drug delivery
Published in Drug Development and Industrial Pharmacy, 2021
Nighat Batool, Asif Mahmood, Rai Muhammad Sarfraz, Hira Ijaz, Nadiah Zafar, Zahid Hussain
Optimized formulation (FM3) depicted pH-dependent reversible swelling and de-swelling pattern as shown in Figure 6. Khalid et al. [3], developed pH-sensitive hydrogels for controlled delivery of loxoprofen. They also reported similar swelling and de-swelling patterns in their study.
Recent prescription status of oral analgesics in Japan in real-world clinical settings: retrospective study using a large-scale prescription database
Published in Expert Opinion on Pharmacotherapy, 2019
Takahiro Ushida, Daiju Matsui, Teruyoshi Inoue, Mizuka Yokoyama, Hiroshi Takatsuna, Takuyuki Matsumoto, Atsushi Takita, Takao Kurusu, Hiroshi Sakoda, Kaoru Okuizumi
Loxoprofen is an NSAID developed in Japan and is widely used in at least 28 countries worldwide [27]. The high proportions of patients prescribed loxoprofen in this study could be explained by it being a prodrug with a short plasma half-life and having no direct effects on the gastrointestinal tract, thereby reducing gastrointestinal disorders. ADRs of loxoprofen were reported in 409 of 13,486 patients (3.03%), with low incidence rates of gastrointestinal ADRs (total of 2.25%) and cardiac ADRs (0.03% such as palpitation (2 patients), hypertension, and increased blood pressure (each 1 patient) [28]. A COX-2-selective inhibitor, celecoxib, has also been reported to be associated with the development of gastrointestinal disorders, although less frequently [29,30]. The proportions of patients prescribed loxoprofen and celecoxib were 32.5% and 16.0%, respectively, but the mean prescription days were greater for celecoxib (34.6 days) than for loxoprofen (25.7 days). Although clinical study conducted overseas has shown that rofecoxib, a COX-2-selective inhibitor could increase the risk of serious and fatal cardiovascular disorders such as myocardial infarction and stroke [31], a recent large-scale, long-term study in patients with chronic pain (PRECISION trial) showed that the cardiovascular risk associated with celecoxib (2.3%) does not exceed that for ibuprofen (2.7%) and naproxen (2.5%) [32]. Therefore, loxoprofen and celecoxib can continue to be used frequently for pain relief. Acetaminophen reportedly causes gastrointestinal disorders less frequently than NSAIDs [33]. The prescription dose of acetaminophen in Japan was lower than that overseas (maximum daily dose, 4,000 mg) until 2010, which resulted in a weak analgesic effect, and acetaminophen was, therefore, prescribed less frequently than NSAIDs in Japan [3]. In 2011, an increased maximum daily dose of acetaminophen, which was equivalent to that prescribed overseas, was approved in Japan [3], thereby allowing more potent analgesic effects to be achieved. Accordingly, the number of patients prescribed acetaminophen was expected to increase. However, the present study, which was conducted in 2017, shows that acetaminophen was still prescribed less frequently (10.5%) than loxoprofen (32.5%), and its median daily prescription dose (1,200 mg) was lower than that of the approved dose (4,000 mg), although the reasons were not clear.