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1.
J Psychopharmacol ; 31(10): 1374-1376, 2017 10.
Article in English | MEDLINE | ID: mdl-28879792

ABSTRACT

Nonsteroidal anti-inflammatory drugs work by non-selectively inhibiting cyclooxygenase enzymes. Evidence indicates that metabolites of the cyclooxygenase pathway play a critical role in the process of learning and memory. We evaluated whether acute naproxen treatment impairs short-term working memory, episodic memory, or semantic memory in a young, healthy adult population. Participants received a single dose of placebo or naproxen (750 mg) in random order separated by 7-10 days. Two hours following administration, participants completed five memory tasks. The administration of acute high-dose naproxen had no effect on memory in healthy young adults.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Memory/drug effects , Naproxen/administration & dosage , Naproxen/adverse effects , Adolescent , Adult , Cyclooxygenase Inhibitors/administration & dosage , Cyclooxygenase Inhibitors/adverse effects , Double-Blind Method , Female , Humans , Male , Prostaglandin-Endoperoxide Synthases/metabolism , Young Adult
2.
J Ethnopharmacol ; 207: 42-46, 2017 Jul 31.
Article in English | MEDLINE | ID: mdl-28602866

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: SKI306X (Joins®) is an anti-inflammatory analgesic herbal medicine extract that was clinically approved for treatment of osteoarthritis in the previous trials and shown to be effective on follow-up studies. However, its potential cardiovascular risk has yet to be investigated. AIM OF THE STUDY: This retrospective cohort study investigated the cardiovascular safety of SKI306X, celecoxib and naproxen. MATERIALS AND METHODS: We used the National Health Insurance Service-National Sample Cohort (NHIS-NSC) to investigate patients over 20 years old with osteoarthritis and rheumatoid arthritis who received a single prescription of SKI306X, celecoxib or naproxen at least once from January 1, 2011 through December 31, 2012. Patients who received SKI306X, celecoxib or naproxen from January 1, 2009 to December 31, 2010 were excluded. Data pertaining to the included patients were investigated to determine the risk of major cardiovascular events associated with the aforementioned prescription using the Cox proportional hazards model after being adjusted for sex, age and comorbidity. RESULTS: A total of 27,253 patients were selected, among which 10,983 were prescribed SKI306X, 12,311 celecoxib and 3959 naproxen. The incidence of major cardiovascular events was highest for celecoxib (15.4%), followed by SKI306X (8.6%) and naproxen (8.0%). Celecoxib had a higher cardiovascular risk than naproxen, while SKI306X did not have a higher risk of cardiovascular events than naproxen. Upon sensitivity analysis, SKI306X was associated with 1.36 times (95%CI: 1.08-1.72) more cardiovascular events than naproxen during 15-60 days of prescription, but not at less than 14 days or more than 61 days. CONCLUSIONS: Evaluation of the cardiovascular safety of the anti-inflammatory analgesic herbal medicine SKI306X revealed that it did not differ from that of naproxen, which is known to have low cardiovascular risk.


Subject(s)
Arthritis, Rheumatoid/drug therapy , Cardiovascular Diseases/chemically induced , Drugs, Chinese Herbal/administration & dosage , Osteoarthritis/drug therapy , Adult , Aged , Anti-Inflammatory Agents/administration & dosage , Antirheumatic Agents/administration & dosage , Antirheumatic Agents/adverse effects , Cardiovascular Diseases/epidemiology , Celecoxib/administration & dosage , Celecoxib/adverse effects , Cohort Studies , Drugs, Chinese Herbal/adverse effects , Female , Humans , Incidence , Male , Middle Aged , Naproxen/administration & dosage , Naproxen/adverse effects , Retrospective Studies , Risk Factors , Time Factors , Young Adult
3.
Recent Pat Drug Deliv Formul ; 11(1): 28-35, 2017.
Article in English | MEDLINE | ID: mdl-28056749

ABSTRACT

BACKGROUND: The absorption of drug through skin avoids many side effects of oral route like gastric irritation, nausea, systemic toxicity etc and thus improves patient compliance. Naproxen sodium (NPRS) is one of the potent NSAID agents. OBJECTIVE: The present study was aimed to develop and evaluate the gel formulation containing NPRS for transdermal drug delivery reducing the side effects and improving patient compliance. The patents on topical delivery of NSAIDS (US 9012402 B1, US 9072659 B2, US 20150258196 A1) and patents indicating use of herbal penetration enhancers (US 20100273746A1, WO 2005009510 A2, US 6004969 A) helped in selecting the drug, excipients. METHOD: Current protocol employs various extracts of Piper cubeba fruit to evaluate its role in absorption of NPRS. Various batches containing 1% NPRS and varying concentrations of synthetic permeation enhancers or the extracts were formulated in carbopol gel. Gel was evaluated for parameters like organoleptic parameters, pH, viscosity and spreadability. An ex-vivo percutaneous absorption of NPRS from gel was investigated and compared with best performing synthetic enhancer, transcutol P (TP). RESULT: The batch containing 2% n-hexane extract (NHE) of Piper cubeba showed higher permeation than TP and Chloroform (CE), Methanolic (ME) and aqueous (AE) extracts as well. It showed improved % cumulative release (85.09%) and flux (278.61µg/cm2.h), as compared to TP and other extracts. Histopathology indicated the formulation safer as compared to that with synthetic enhancer. CONCLUSION: It suggests P. cubeba as effective and safer tool for transdermal delivery and acts as therapeutic facilitator for naproxen. GC-MS analysis indicates lignans & terpenes in NHE to which this permeation enhancement activity may be attributed.


Subject(s)
Drug Delivery Systems , Gels/chemistry , Naproxen/administration & dosage , Piper/chemistry , Plant Extracts/chemistry , Administration, Cutaneous , Humans , Patents as Topic
4.
Cephalalgia ; 37(10): 965-978, 2017 Sep.
Article in English | MEDLINE | ID: mdl-27521843

ABSTRACT

Introduction Migraine headache is a neurological disorder whose attacks are associated with nausea, vomiting, photophobia and phonophobia. Treatments for migraine aim to either prevent attacks before they have started or relieve attacks (abort) after onset of symptoms and range from complementary therapies to pharmacological interventions. A number of treatment-related adverse events such as somnolence, fatigue, and chest discomfort have previously been reported in association with triptans. The comparative tolerability of available agents for the abortive treatment of migraine attacks has not yet been systematically reviewed and quantified. Methods We performed a systematic literature review and Bayesian network meta-analysis for comparative tolerability of treatments for migraine. The literature search targeted all randomized controlled trials evaluating oral abortive treatments for acute migraine over a range of available doses in adults. The primary outcomes of interest were any adverse event, treatment-related adverse events, and serious adverse events. Secondary outcomes were fatigue, dizziness, chest discomfort, somnolence, nausea, and vomiting. Results Our search yielded 141 trials covering 15 distinct treatments. Of the triptans, sumatriptan, eletriptan, rizatriptan, zolmitriptan, and the combination treatment of sumatriptan and naproxen were associated with a statistically significant increase in odds of any adverse event or a treatment-related adverse event occurring compared with placebo. Of the non-triptans, only acetaminophen was associated with a statistically significant increase in odds of an adverse event occurring when compared with placebo. Overall, triptans were not associated with increased odds of serious adverse events occurring and the same was the case for non-triptans. For the secondary outcomes, with the exception of vomiting, all triptans except for almotriptan and frovatriptan were significantly associated with increased risk for all outcomes. Almotriptan was significantly associated with an increased risk of vomiting, whereas all other triptans yielded non-significant lower odds compared with placebo. Generally, the non-triptans were not associated with decreased tolerability for the secondary outcomes. Discussion In summary, triptans were associated with higher odds of any adverse event or a treatment-related adverse event occurring when compared to placebo and non-triptans. Non-significant results for non-triptans indicate that these treatments are comparable with one another and placebo regarding tolerability outcomes.


Subject(s)
Migraine Disorders/diagnosis , Migraine Disorders/drug therapy , Tryptamines/administration & dosage , Acute Disease , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Clinical Trials as Topic/methods , Drug Therapy, Combination , Humans , Migraine Disorders/epidemiology , Naproxen/administration & dosage , Sumatriptan/administration & dosage , Treatment Outcome
5.
J Ethnopharmacol ; 195: 214-221, 2017 Jan 04.
Article in English | MEDLINE | ID: mdl-27847337

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Andrographis paniculata Nees (Acanthacae) have broad range of pharmacological effects such as hepatoprotective, antifertility, antimalarial, antidiabetic, suppression of various cancer cells and anti-inflammatory properties and is widely used medicinal plant in the traditional Unani and Ayurvedic medicinal systems. Andrographolide (AN) is one of the active constituent of the A. paniculata Nees extract (APE). They have been found in many traditional herbal formulations in India and proven to be effective as anti-inflammatory drug. AIM OF THE STUDY: To evaluate the pharmacokinetic and pharmacodynamic (anti arthritic) herb-drug interactions of A. paniculata Nees extract (APE) and pure andrographolide (AN) with naproxen (NP) after oral co-administration in wistar rats. MATERIALS AND METHODS: After oral co-administration of APE (200mg/Kg) and AN (60mg/kg) with NP (7.5mg/kg) in rats, drug concentrations in plasma were determined using HPLC method. The main pharmacokinetic parameters of Cmax, tmax, t1/2, MRT, Vd, CL, and AUC were calculated by non-compartment model. Change in paw volume, mechanical nociceptive threshold, mechanical hyperalgesia, histopathology and hematological parameters were evaluated to study antiarthritic activity. RESULTS: Co-administration of NP with APE and pure AN decreased systemic exposure level of NP in vivo. The Cmax, tmax, AUC0-t of NP was decreased. In pharmacodynamic study, NP (10mg/kg) alone and NP+AN (10+60mg/kg) groups exhibited significant synergistic anti-arthritic activity as compared to groups NP+APE, APE and AN alone. CONCLUSION: The results obtained from this study suggested that NP, APE and pure AN existed pharmacokinetic herb-drug interactions in rat which is correlated with anti-arthritic study. The knowledge regarding possible herb-drug interaction of NP might be helpful for physicians as well as patients using AP. So further studies should be done to understand the effect of other herbal ingredients of APE on NP as well as to predict the herb-drug interaction in humans.


Subject(s)
Andrographis/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Arthritis, Experimental/drug therapy , Diterpenes/administration & dosage , Herb-Drug Interactions , Naproxen/pharmacokinetics , Plant Extracts/administration & dosage , Administration, Oral , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/blood , Area Under Curve , Arthritis, Experimental/blood , Arthritis, Experimental/chemically induced , Arthritis, Experimental/physiopathology , Chromatography, High Pressure Liquid , Diterpenes/isolation & purification , Edema/chemically induced , Edema/prevention & control , Female , Freund's Adjuvant , Half-Life , Hyperalgesia/chemically induced , Hyperalgesia/physiopathology , Hyperalgesia/prevention & control , Metabolic Clearance Rate , Naproxen/administration & dosage , Naproxen/blood , Nociception/drug effects , Nociceptive Pain/chemically induced , Nociceptive Pain/physiopathology , Nociceptive Pain/prevention & control , Pain Threshold/drug effects , Phytotherapy , Plant Extracts/isolation & purification , Plants, Medicinal , Rats, Wistar
6.
Cancer Prev Res (Phila) ; 7(2): 246-54, 2014 Feb.
Article in English | MEDLINE | ID: mdl-24346344

ABSTRACT

Urinary bladder cancer prevention studies were performed with the nonsteroidal anti-inflammatory drugs (NSAID) naproxen (a standard NSAID with a good cardiovascular profile), sulindac, and their nitric oxide (NO) derivatives. In addition, the effects of the ornithine decarboxylase inhibitor, difluoromethylornithine (DFMO), alone or combined with a suboptimal dose of naproxen or sulindac was examined. Agents were evaluated at their human equivalent doses (HED), as well as at lower doses. In the hydroxybutyl(butyl)nitrosamine (OH-BBN) model of urinary bladder cancer, naproxen (400 or 75 ppm) and sulindac (400 ppm) reduced the incidence of large bladder cancers by 82%, 68%, and 44%, respectively, when the agents were initially given 3 months after the final dose of the carcinogen; microscopic cancers already existed. NO-naproxen was highly effective, whereas NO-sulindac was inactive. To further compare naproxen and NO-naproxen, we examined their effects on gene expression in rat livers following a 7-day exposure. Limited, but similar, gene expression changes in the liver were induced by both agents, implying that the primary effects of both are mediated by the parent NSAID. When agents were initiated 2 weeks after the last administration of OH-BBN, DFMO at 1,000 ppm had limited activity, a low dose of naproxen (75 ppm) and sulindac (150 ppm) were highly and marginally effective. Combining DFMO with suboptimal doses of naproxen had minimal effects, whereas the combination of DMFO and sulindac was more active than either agent alone. Thus, naproxen and NO-naproxen were highly effective, whereas sulindac was moderately effective in the OH-BBN model at their HEDs.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Antineoplastic Combined Chemotherapy Protocols/therapeutic use , Eflornithine/administration & dosage , Neoplasms, Experimental/prevention & control , Nitric Oxide/administration & dosage , Urinary Bladder Neoplasms/prevention & control , Animals , Chemoprevention/methods , Drug Evaluation, Preclinical , Female , Naproxen/administration & dosage , Naproxen/analogs & derivatives , Neoplasms, Experimental/chemically induced , Rats , Rats, Inbred F344 , Sulindac/administration & dosage , Urinary Bladder Neoplasms/chemically induced
7.
Int J Pharm ; 451(1-2): 34-40, 2013 Jul 15.
Article in English | MEDLINE | ID: mdl-23624087

ABSTRACT

Intra-articular injection of oil solutions of lipophilic prodrugs that rapidly degrade to their parent compound in synovial fluid may constitute a feasible approach to increase the joint residence time of non-steroidal anti-inflammatory drugs. In this in vivo study, oil solutions of the N,N-diethyl glycolamide ester prodrug of naproxen (16 mg/ml) were injected into the rat knee joint by dosing 6 µl formulation per 100g body weight. The sustained release properties were compared to those of intra-articularly injected aqueous and oil solutions of naproxen by monitoring the naproxen serum concentrations over time. Two oils, medium-chain triglycerides and castor oil, differing with respect to viscosity were tested. After intra-articular administration of oil prodrug solutions, a significant increase in the time to maximum naproxen serum concentration from around 40 to 245 min, an increase in the MRT(j) from around 0.11 to 3.3h and a 30% reduction in the maximum serum concentration were observed compared to that of the parent naproxen. The similar serum profiles obtained using the two oils indicate that the release was not affected by the oil viscosity. A prolonged naproxen joint residence time in rats was shown by intra-articular injection of an oil prodrug solution.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Glycolates/chemistry , Naproxen/administration & dosage , Oils/chemistry , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Castor Oil/chemistry , Delayed-Action Preparations , Esters , Injections, Intra-Articular , Knee Joint , Male , Naproxen/chemistry , Naproxen/pharmacokinetics , Prodrugs , Rats , Rats, Sprague-Dawley , Time Factors , Triglycerides/chemistry , Viscosity
8.
Int J Pharm ; 416(1): 136-44, 2011 Sep 15.
Article in English | MEDLINE | ID: mdl-21723930

ABSTRACT

The aim of this study was to evaluate the potential application of microemulsions as a transdermal drug delivery for naproxen (Np). The pseudo-ternary phase diagrams were developed for microemulsions composed of isopropyl myristate, Span 80, Labrafil M, Labrasol, and Cremophor EL, ethanol and isopropyl alcohol and 0.5N sodium hydroxide. The final concentration of Np in microemulsion systems was 10% (w/w). The microemulsions were characterised by conductivity, droplet size, viscosity and pH. Moreover, in vitro permeability studies were performed using diffusion cells from rat skin. The permeation rates of Np from microemulsions (M1(Np) and M2(Np)) were higher than the commercial (C) gel formulation. The paw oedema test was performed in rats to evaluate the anti-inflammatory activity of Np. The volume increase in paw oedema after 6hr was 0.71±0.46% with M2(Np), whereas M1(Np) and C exhibited 6.48±2.71% and 14.97±3.15% increases in oedema, respectively. Additionally, a significant analgesic effect was detected in the hot plate and tail-flick tests for all test microemulsion and C formulations when compared with the control. Histopathological examination of the treated skin was performed to investigate changes in skin morphology. In conclusion, the microemulsion formulations, especially the M2(Np) formulation, may be used as an effective alternative for the transdermal delivery of Np.


Subject(s)
Chemistry, Pharmaceutical/methods , Emulsions/chemistry , Emulsions/chemical synthesis , Naproxen/pharmacology , Naproxen/pharmacokinetics , Skin Absorption/drug effects , Administration, Cutaneous , Analgesics/administration & dosage , Analgesics/chemistry , Analgesics/pharmacology , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Diffusion Chambers, Culture , Drug Evaluation, Preclinical/methods , Drug Stability , Emulsions/administration & dosage , Hydrogen-Ion Concentration , Male , Naproxen/administration & dosage , Naproxen/chemistry , Particle Size , Rats , Rats, Wistar , Skin/anatomy & histology , Skin/drug effects , Solubility , Viscosity
9.
AAPS PharmSciTech ; 11(3): 1138-46, 2010 Sep.
Article in English | MEDLINE | ID: mdl-20652458

ABSTRACT

In view of the good skin tolerability, glycofurol was used as a vehicle-based gel, and its effect in the topical penetration of Naproxen (NAP) was investigated. The aims of this study were to develop a suitable gel with bioadhesive property, spreadability, and viscosity for topical anti-inflammatory effect. Three gelling and adhesive agents were examined: Carbopol 974P, Gantrez AN 119, and polyvinylpyrollidone K30. Skin permeation rates and lag times of NAP were evaluated using the Franz-type diffusion cell in order to optimize the gel formulation. The permeation rate of NAP-based gel across the excised rat skin was investigated. A significant increase in permeability parameters such as steady-state flux (J(ss)), permeability coefficient (K(p)), and penetration index (PI) was observed in optimized formulation containing 2% Transcutol as an permeation enhancer. From skin irritation test, it was concluded that the optimized novel glycofurol-based gel formulation was safe to be used for topical drug delivery. The developed glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most of the problems associated with drug therapy.


Subject(s)
Bandages , Naproxen/chemistry , Pharmaceutical Vehicles/chemical synthesis , Polyethylene Glycols/chemistry , Skin/chemistry , Absorption , Administration, Topical , Animals , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Diffusion , Drug Evaluation, Preclinical , Gels/chemistry , Male , Naproxen/administration & dosage , Rats , Rats, Sprague-Dawley
10.
Anticancer Res ; 29(9): 3605-10, 2009 Sep.
Article in English | MEDLINE | ID: mdl-19667155

ABSTRACT

BACKGROUND: Androgen-deprivation therapy is commonly used in patients with progressive prostate cancer (PCa), but can be associated with unpleasant side-effects. The objective of the study was to determine whether treatment with calcitriol and naproxen is effective in safely delaying the growth and progression of PCa in men with early recurrent disease. MATERIALS AND METHODS: Patients with biochemical relapse after local therapy for prostate cancer were treated with high dose calcitriol (DN101, Novacea) (45 microg once per week) and naproxen (375 mg twice daily) for one year and followed with serum PSA levels as well as imaging studies. RESULTS: Twenty-one patients were enrolled in the trial. Four patients met criteria for progression, with a PSA doubling time (PSADT) that decreased while on therapy. Fourteen patients had a prolongation of PSADT compared to baseline. CONCLUSION: Combination therapy with weekly calcitriol and daily naproxen is well tolerated by most patients and prolongation of PSADT was achieved in 75% of patients.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Calcitriol/therapeutic use , Naproxen/therapeutic use , Prostatic Neoplasms/drug therapy , Aged , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Calcitriol/administration & dosage , Humans , Male , Middle Aged , Naproxen/administration & dosage , Recurrence
11.
Drug Deliv ; 16(6): 348-56, 2009 Aug.
Article in English | MEDLINE | ID: mdl-19606949

ABSTRACT

A series of bone-targeting prodrugs, dendritic L-Asp and L-Glu peptides Naproxen conjugates have been synthesized in a convergent approach and well characterized by NMR and MS techniques. Their solubility in water and hydroxyapatite affinity were evaluated in in vitro conditions. All the prodrugs were water soluble and exhibited high affinity to HAP. Compound NAP-G(2)-Asp was found more potent in HAP binding. The efficient release of the active drug moiety (naproxen) occurred by the cleavage of an amide bond in physiological conditions. These results indicated that the dendritic peptides might become a delivery system for bone tissues and provided an effective entry to the development of new bone-targeting molecules.


Subject(s)
Dendrimers/chemical synthesis , Naproxen/chemical synthesis , Peptides/chemical synthesis , Dendrimers/administration & dosage , Drug Delivery Systems/methods , Drug Evaluation, Preclinical/methods , Naproxen/administration & dosage , Peptides/administration & dosage
12.
Inflammopharmacology ; 17(1): 1-5, 2009 Feb.
Article in English | MEDLINE | ID: mdl-19139828

ABSTRACT

UNLABELLED: We have been developing a family of phosphatidylcholine (PC)-associated NSAIDs, which appear to have improved GI safety and therapeutic efficacy in both rodent model systems and pilot clinical trials. As naproxen has been demonstrated to be associated with the lowest cardiovascular adverse events in comparison with both COX-2 selective inhibitors and conventional NSAIDs, we have been developing a Naproxen-PC formulation for evaluation in animal models and clinical trials. We have determined that an oil-based formulation of naproxen and triple strength soy lecithin provides excellent GI protection in both: 1) an acute NSAID-induced intestinal bleeding model in rats pretreated with L-NAME that are intragastrically administered a single dose of naproxen (at a dose of 50 mg/kg) vs the equivalent dose of Naproxen-PC; and 2) a more chronic model (at a naproxen dose of 25 mg/kg BID) in rats that have pre-existing hindpaw inflammation (induced with a intradermal injection of Complete Freund's Adjuvant/CFA). Both models demonstrate the superior GI safety of Naproxen-PC vs naproxen while this novel formulation had significant anti-inflammatory efficacy to reduce hindpaw edema and the generation of PGE(2) in the collected joint synovial fluid. CONCLUSION: Naproxen-PC appears to induce significantly less GI injury and bleeding in two rodent model systems while maintaining anti-inflammatory and COX-inhibitory activity.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Inflammation/drug therapy , Lecithins/chemistry , Naproxen/administration & dosage , Animals , Anti-Inflammatory Agents, Non-Steroidal/toxicity , Cyclooxygenase Inhibitors/administration & dosage , Cyclooxygenase Inhibitors/toxicity , Dinoprostone/metabolism , Disease Models, Animal , Dose-Response Relationship, Drug , Drug Administration Schedule , Edema/drug therapy , Edema/physiopathology , Gastrointestinal Hemorrhage/chemically induced , Gastrointestinal Hemorrhage/prevention & control , Inflammation/physiopathology , Naproxen/toxicity , Rats , Glycine max/chemistry , Synovial Fluid/metabolism
13.
AAPS PharmSciTech ; 9(1): 54-9, 2008.
Article in English | MEDLINE | ID: mdl-18446461

ABSTRACT

The purpose of this research was to obtain directly compressible agglomerates of naproxen containing disintegrant by spherical crystallization technique. Acetone-water containing hydroxypropyl celloluse (HPC) and disintegrant was used as the crystallization system. In this study croscarmellose sodium (Ac-Di-Sol) was employed as disintegrant. The agglomerates were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (XRPD), and scanning electron microscopy and were evaluated for flow, packing and tableting properties and drug release. The growth of particle size and the spherical form of the agglomerates resulted in formation of products with good flow and packing properties. The improved compaction properties of the agglomerated crystals were due to their fragmentation occurred during compression. DSC and XRPD studies showed that naproxen particles, crystallized in the presence of HPC and Ac-Di-Sol did not undergo structural modifications. The dissolution rate of naproxen from tablets made of naproxen-(Ac-Di-Sol) agglomerates was enhanced significantly because of including the disintegrant in to the particles. This was attributed to an increase in the surface area of the practically water insoluble drug is exposed to the dissolution medium. In conclusion the spherical crystallization technique developed in this study is suitable for obtaining agglomerates of drug with disintegrant.


Subject(s)
Cellulose/chemistry , Crystallization/methods , Drug Carriers/chemistry , Drug Compounding/methods , Excipients/chemistry , Naproxen/chemistry , Tablets/chemical synthesis , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Drug Evaluation, Preclinical , Microspheres , Naproxen/administration & dosage , Particle Size
15.
Farm. hosp ; 31(3): 169-172, mayo-jun. 2007. tab
Article in Es | IBECS | ID: ibc-056688

ABSTRACT

Objetivo: Evaluar la prescripción de medicamentos en una clínica odontológica de una universidad mexicana. Método: Mediante un estudio observacional y descriptivo, se analizaron 698 prescripciones odontológicas en 14 servicios clínicos que conforman la clínica en estudio, enfocados a la conservación y restauración de la salud bucal en enero-junio 2005. Se registraron criterios como: medicamento prescrito, indicación, dosis, intervalo de dosificación, individualización de la terapia, duración de tratamiento y presencia de interacciones farmacológicas potenciales. Para determinar la inadecuación en los criterios de prescripción se comparó la información obtenida en recetas y expedientes clínicos, con la de la literatura especializada. Resultados: Los medicamentos más prescritos fueron paracetamol, naproxeno, ampicilina y dicloxacilina en 43,26, 15,38, 7,45 y 7,02%. La indicación, dosis e intervalo de dosificación fueron los criterios con mayor inadecuación en la prescripción. Las principales interacciones potenciales fueron entre los antiinflamatorios no esteroideos con el captopril y la amoxicilina. Conclusiones: Con lo anterior, se determinó que el 37,25% de las prescripciones fueron inadecuadas. A través de este estudio se establecieron estrategias que permitirán en un futuro tener una política de uso racional de los medicamentos empleados


Objective: To assess the drug prescription service in a dental clinic of a Mexican university hospital. Method: An observational, descriptive study was carried out which analysed 698 drugs prescribed for dental problems in 14 dental health care departments in our clinic between the period of January-June 2005. The following criteria were established: prescribed drug, indication, dosage, dosage interval, individualised treatment, treatment duration and potential drug interactions. Information taken from prescriptions and clinical records was compared with information from literature on the subject in order to determine the adequacy of prescription criteria. Results: The most frequently prescribed drugs were paracetamol, naproxen, ampicillin and dicloxacillin (43.26, 15.38, 7.45 and 7.02%). The prescription criteria which showed the least adequacy were as follows: indication, dosage and dosage interval. The main potential drug interactions occurred between non-steroidal anti-inflammatory drugs and captopril/amoxicillin. Conclusions: Taking the above into consideration, it was determined that 37.25% of prescriptions were inadequate. This study has helped to establish strategies which will facilitate the appropriate use of drugs in the future


Subject(s)
Humans , Drug Prescriptions , Dental Clinics/statistics & numerical data , Student Health Services/statistics & numerical data , Mexico , Drug Interactions , Epidemiology, Descriptive , Homeopathic Dosage , Acetaminophen/administration & dosage , Naproxen/administration & dosage , Ampicillin/administration & dosage , Dicloxacillin/administration & dosage , Captopril/administration & dosage , Amoxicillin/administration & dosage
16.
Eur J Pharmacol ; 514(1): 53-9, 2005 May 02.
Article in English | MEDLINE | ID: mdl-15878324

ABSTRACT

Frequently used for humans as non-steroidal anti-inflammatory drug, naproxen has been known to induce ulcerative gastric lesion. The present study investigated the in vivo protective effect of astaxanthin isolated from Xanthophyllomyces dendrorhous against naproxen-induced gastric antral ulceration in rats. The oral administration of astaxanthin (1, 5, and 25 mg/kg of body weight) showed a significant protection against naproxen (80 mg/kg of body weight)-induced gastric antral ulcer and inhibited elevation of the lipid peroxide level in gastric mucosa. In addition, pretreatment of astaxanthin resulted in a significant increase in the activities of radical scavenging enzymes such as superoxide dismutase, catalase, and glutathione peroxidase. A histologic examination clearly proved that the acute gastric mucosal lesion induced by naproxen nearly disappeared after the pretreatment of astaxanthin. These results suggest that astaxanthin removes the lipid peroxides and free radicals induced by naproxen, and it may offer potential remedy of gastric ulceration.


Subject(s)
Pyloric Antrum/drug effects , Stomach Ulcer/prevention & control , beta Carotene/analogs & derivatives , Adjuvants, Immunologic/pharmacology , Animals , Disease Models, Animal , Dose-Response Relationship, Drug , Glutathione Peroxidase/metabolism , Male , Malondialdehyde/metabolism , Naproxen/administration & dosage , Naproxen/toxicity , Pyloric Antrum/metabolism , Pyloric Antrum/pathology , Rats , Rats, Sprague-Dawley , Stomach Ulcer/chemically induced , Stomach Ulcer/metabolism , Superoxide Dismutase/metabolism , Time Factors , Xanthophylls , beta Carotene/pharmacology
17.
Mult Scler ; 10(6): 636-42, 2004 Dec.
Article in English | MEDLINE | ID: mdl-15584488

ABSTRACT

Multiple sclerosis (MS) patients initiating IFN beta-1a, Avonex, therapy (Group 1, n = 30) or experiencing side effects after 6 months on therapy (Group 2, n = 30) were randomized for 5 weeks open label adjunct therapy to naproxen (Aleve), acetaminophen (Tylenol) or ibuprofen (Advil). Our hypothesis was that non-prescription pain medications are effective in decreasing or alleviating the side effects associated with IFN beta-1a therapy. Contrary to the hypothesis, most patients in both groups continued to report side effects on all pain medications. After 5 weeks, headache, fever, chills and injection site pain were low in < or = 50% of patients. Moderate to significant fatigue, muscle or joint pain continued in most patients. As a quality of life measure, the Modified Fatigue Impact Scale (mFIS) improved for Group 1 on naproxen or ibuprofen with greatest improvement in physical subset (P = 0.002 for naproxen and P<0.01 for ibuprofen). Total mFIS for Group 1 on acetaminophen improved (P = 0.04) due to improved cognitive subset rather than physical subset. Group 2, with side effects initially, reported less significant fatigue (severity 5-10) but more moderate fatigue (severity 2-4) at study end for all three medications. All medications improved cognitive subset (P = 0.05). Physical mFIS subset did not improve for Group 2 on acetaminophen, but did with naproxen (P = 0.05) or ibuprofen (P = 0.03). Naproxen and ibuprofen were more effective than acetaminophen in minimizing physical side effects of IFN beta-1a. None of the three pain medications tested were as effective as hypothesized for minimizing fatigue or muscle and joint pain.


Subject(s)
Acetaminophen/administration & dosage , Adjuvants, Immunologic/adverse effects , Analgesics, Non-Narcotic/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Ibuprofen/administration & dosage , Interferon-beta/adverse effects , Multiple Sclerosis, Relapsing-Remitting/drug therapy , Naproxen/administration & dosage , Adult , Drug Therapy, Combination , Fatigue/drug therapy , Female , Humans , Interferon beta-1a , Male , Middle Aged , Pain/drug therapy , Prospective Studies
18.
Clin Rehabil ; 17(1): 96-100, 2003 Feb.
Article in English | MEDLINE | ID: mdl-12617384

ABSTRACT

OBJECTIVE: The aim of this study was to compare the effectiveness of naproxen (10%) applied by topical iontophoresis or by phonophoresis in the treatment of lateral epicondylitis. DESIGN: Randomized controlled trial. SETTING: Dokuz Eylül University School of Physical Therapy and Rehabilitation. SUBJECTS: This study was carried out with 61 patients who had lateral epicondylitis. They were randomized into two groups. INTERVENTIONS: Naproxen was applied to the first group using phonophoresis (29 patients--33 extremities) and to the second group using iontophoresis (32 patients--34 extremities). Patients in both groups were treated by other physiotherapy methods (cold pack, progressive strengthening and stretching exercises). OUTCOMES: Pain scores (at rest, during motion, with pressure, weight lifting), grip strength and Nirschl-Petterone Grading System were evaluated before and after treatment. RESULTS: Pain scores decreased, grip strength and Nirsch-Petterone Grading System statistically significantly increased in both groups after treatment (p < 0.05), but there were no statistical differences between groups before or after treatment (p > 0.05). CONCLUSION: The results suggest that iontophoresis and phonophoresis of naproxen are equally effective electrotherapy methods in the treatment of lateral epicondylitis.


Subject(s)
Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Naproxen/administration & dosage , Naproxen/pharmacology , Tennis Elbow/drug therapy , Administration, Topical , Adult , Aged , Female , Humans , Iontophoresis , Male , Middle Aged , Pain/drug therapy , Pain/etiology , Pain Measurement , Phonophoresis , Treatment Outcome
19.
Chir Organi Mov ; 86(3): 243-7, 2001.
Article in English, Italian | MEDLINE | ID: mdl-12025189

ABSTRACT

The use of magnetic fields in medicine has obtained encouraging results and it has stimulated the research conducted so that the use of this method of treatment may be better and more widespread. A double blind study was conducted to evaluate the effectiveness of the generation of magnetic fields on edema and on pain in patients submitted to surgery for bilateral hallux valgus.


Subject(s)
Hallux Valgus/surgery , Magnetics/therapeutic use , Pain Management , Postoperative Care , Activities of Daily Living , Adult , Aged , Analgesics, Opioid/administration & dosage , Analgesics, Opioid/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Double-Blind Method , Edema/etiology , Edema/therapy , Female , Follow-Up Studies , Hallux Valgus/diagnosis , Humans , Meperidine/administration & dosage , Meperidine/therapeutic use , Middle Aged , Naproxen/administration & dosage , Naproxen/therapeutic use , Pain/drug therapy , Pain, Postoperative/drug therapy , Pain, Postoperative/therapy , Shoes , Surveys and Questionnaires , Time Factors
20.
Säo Paulo; s.n; 2001. 144 p. ilus, tab, graf.
Thesis in Portuguese | LILACS | ID: lil-289845

ABSTRACT

A nimesulida, é um fármaco sintético, pouco solúvel em água (0,01 mg/mL), classificado como antiinflamatório não esteróide, com atividade analgésica e antipirética. No Brasil são comercializadas várias especialidades farmacêuticas orais, contendo nimesulida, na dosagem de 100 e 200 mg. Em termos de saúde pública tais produtos, prescritos pelo médico como similares intercambiáveis, deveriam apresentar, a mesma eficácia clínica, sendo a bioequivalência um requisito fundamental. Um estudo em que se verifique a qualidade biofarmacotécnica de uma amostragem destes produtos torna-se bastante útil para que se possa avaliar a situação atual...


Subject(s)
Humans , Male , Female , Adult , Analgesics/therapeutic use , Anti-Inflammatory Agents, Non-Steroidal/pharmacokinetics , Cytoprotection , Drug Evaluation , Drug Stability , Naproxen/administration & dosage , Piroxicam/administration & dosage , Prostaglandins/chemical synthesis , Quality of Homeopathic Remedies , Similar , Biological Availability , Chromatography, Liquid/methods , Drug Compounding , Efficacy , Liver/metabolism , Data Interpretation, Statistical , Therapeutic Equivalency
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