scholarly journals Lipid bound extended release buprenorphine (high and low doses) and sustained release buprenorphine effectively attenuate post‐operative hypersensitivity in an incisional pain model in mice ( Mus musculus )

2021 ◽  
Author(s):  
Kaela Navarro ◽  
Katechan Jampachaisri ◽  
Monika Huss ◽  
Cholawat Pacharinsak
Keyword(s):  
Sustained Release ◽  
Mus Musculus ◽  
Extended Release ◽  
Low Doses ◽  
Pain Model ◽  
Incisional Pain

Extended-release Buprenorphine, an FDAindexed Analgesic, Attenuates Mechanical Hypersensitivity in Rats (Rattus norvegicus)

2021 ◽  
Author(s):  
Eden D Alamaw ◽  
Benjamin D Franco ◽  
Katechan Jampachaisri ◽  
Monika K Huss ◽  
Cholawat Pacharinsak
Keyword(s):  
Extended Release ◽  
Low Dose ◽  
Clinical Signs ◽  
High Dose ◽  
Male Adult ◽  
Pain Model ◽  
Mechanical Hypersensitivity ◽  
Treatment Groups ◽  
Incisional Pain ◽  
Thermal Hypersensitivity

A new extended-release buprenorphine (XR), an FDA-indexed analgesic, has recently become available to the laboratoryanimal community. However, the effectiveness and dosing of XR has not been extensively evaluated for rats. We investigatedXR’s effectiveness in attenuating postoperative hypersensitivity in a rat incisional pain model. We hypothesized that highdose of XR would attenuate mechanical and thermal hypersensitivity more effectively than the low dose of XR in this model. We performed 2 experiments. In experiment 1, male adult Sprague–Dawley rats (n = 31) were randomly assigned to 1 of the 4 treatment groups: 1) saline (saline, 0.9% NaCl, 5 mL/kg, SC, once); 2) sustained-release buprenorphine (Bup-SR; 1.2 mg/kg, SC, once), 3) low-dose extended-release buprenorphine (XR-Lo; 0.65 mg/kg, SC, once), and 4) high-dose extended-releasebuprenorphine (XR-Hi; 1.3 mg/kg, SC, once). After drug administration, a 1 cm skin incision was made on the plantar hind paw under anesthesia. Mechanical and thermal hypersensitivity were evaluated 1 d before surgery (D-1), 4 h after surgery (D0), and for 3 d after surgery (D1, D2, and D3). In experiment 2, plasma buprenorphine concentration (n = 39) was measured at D0, D1, D2, and D3. Clinical observations were recorded daily, and a gross necropsy was performed on D3. Mechanical and thermal hypersensitivity were measured for 3 d (D0-D3) in the saline group. Bup-SR, XR-Lo, and XR-Hi effectively attenuated mechanical hypersensitivity for D0-D3. Plasma buprenorphine concentrations remained above 1 ng/mL on D0 and D1 in all treatment groups. No abnormal clinical signs were noted, but injection site reactions were evident in the Bup-SR (71%), XR-Lo (75%), and XR-Hi (87%) groups. This study indicates that XR-Hi did not attenuate hypersensitivity more effectivelythan did XR-Lo in this model. XR 0.65 mg/kg is recommended to attenuate postoperative mechanical hypersensitivity for upto 72 h in rats in an incisional pain model.

scholarly journals Preparation and scale up of extended-release tablets of bromopride

2014 ◽  
Vol 50 (2) ◽  
pp. 291-300 ◽  
Author(s):  
Guilherme Neves Ferreira ◽  
Marcos Giovani Rodrigues Silva ◽  
Aline Guerra Manssour Fraga ◽  
Luiz Cláudio Rodrigues Pereira da Silva ◽  
Luiz Marcelo Lira ◽  
...  
Keyword(s):  
Sustained Release ◽  
Mathematical Models ◽  
Extended Release ◽  
Scale Up ◽  
Study Data ◽  
Matrix Tablets ◽  
Tableting Machine ◽  
Compaction Behavior ◽  
Mathematical Equations ◽  
And Control

Reproducibility of the tablet manufacturing process and control of its pharmaceutics properties depends on the optimization of formulation aspects and process parameters. Computer simulation such as Design of Experiments (DOE) can be used to scale up the production of this formulation, in particular for obtaining sustained-release tablets. Bromopride formulations are marketed in the form of extended-release pellets, which makes the product more expensive and difficult to manufacture. The aim of this study was to formulate new bromopride sustained release formulations as tablets, and to develop mathematical models to standardize the scale up of this formulation, controlling weight and hardness of the tablets during manufacture according to the USP 34th edition. DOE studies were conducted using Minitab(tm) software. Different excipient combinations were evaluated in order to produce bromopride sustained-release matrix tablets. In the scale-up study, data were collected and variations in tableting machine parameters were measured. Data were processed by Minitab(tm) software, generating mathematical equations used for prediction of powder compaction behavior, according to the settings of the tableting machine suitable for scale-up purposes. Bromopride matrix tablets with appropriate characteristics for sustained release were developed. The scale-up of the formulation with the most suitable sustained release profile was established by using mathematical models, indicating that the formulation can be a substitute for the pellets currently marketed.

scholarly journals Equivalent intraperitoneal doses of ibuprofen supplemented in drinking water or in diet: a behavioral and biochemical assay using antinociceptive and thromboxane inhibitory dose–response curves in mice

PeerJ ◽  
2016 ◽  
Vol 4 ◽  
pp. e2239 ◽  
Author(s):  
Raghda A.M. Salama ◽  
Nesreen H. El Gayar ◽  
Sonia S. Georgy ◽  
May Hamza
Keyword(s):  
Drinking Water ◽  
Dose Response ◽  
Formalin Test ◽  
Response Curves ◽  
Time Curve ◽  
Pain Model ◽  
Threshold Time ◽  
Dose Response Curves ◽  
Inhibitory Agents ◽  
Incisional Pain

Background.Ibuprofen is used chronically in different animal models of inflammation by administration in drinking water or in diet due to its short half-life. Though this practice has been used for years, ibuprofen doses were never assayed against parenteral dose–response curves. This study aims at identifying the equivalent intraperitoneal (i.p.) doses of ibuprofen, when it is administered in drinking water or in diet.Methods.Bioassays were performed using formalin test and incisional pain model for antinociceptive efficacy and serum TXB2for eicosanoid inhibitory activity. The dose–response curve of i.p. administered ibuprofen was constructed for each test using 50, 75, 100 and 200 mg/kg body weight (b.w.). The dose–response curves were constructed of phase 2a of the formalin test (the most sensitive phase to COX inhibitory agents), the area under the ‘change in mechanical threshold’-time curve in the incisional pain model and serum TXB2levels. The assayed ibuprofen concentrations administered in drinking water were 0.2, 0.35, 0.6 mg/ml and those administered in diet were 82, 263, 375 mg/kg diet.Results.The 3 concentrations applied in drinking water lay between 73.6 and 85.5 mg/kg b.w., i.p., in case of the formalin test; between 58.9 and 77.8 mg/kg b.w., i.p., in case of the incisional pain model; and between 71.8 and 125.8 mg/kg b.w., i.p., in case of serum TXB2levels. The 3 concentrations administered in diet lay between 67.6 and 83.8 mg/kg b.w., i.p., in case of the formalin test; between 52.7 and 68.6 mg/kg b.w., i.p., in case of the incisional pain model; and between 63.6 and 92.5 mg/kg b.w., i.p., in case of serum TXB2levels.Discussion.The increment in pharmacological effects of different doses of continuously administered ibuprofen in drinking water or diet do not parallel those of i.p. administered ibuprofen. It is therefore difficult to assume the equivalent parenteral daily doses based on mathematical calculations.

scholarly journals In Vitro and In Vivo Evaluation of pH-Sensitive Hydrogels of Carboxymethyl Chitosan for Intestinal Delivery of Theophylline

2012 ◽  
Vol 2012 ◽  
pp. 1-9 ◽  
Author(s):  
Hemant Kumar Singh Yadav ◽  
H. G. Shivakumar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Extended Release ◽  
Carboxymethyl Chitosan ◽  
Ph Sensitive ◽  
Acidic Ph ◽  
Release Formulation ◽  
Nocturnal Asthma

Chitosan is a natural polymer which has limited solubility. Chitosan gets solubilized at acidic pH but is insoluble at basic pH. In the present study, carboxymethyl chitosan (CMC) was prepared which shows high swelling in basic pH and thus can delay the drug release and can act as matrix for extended release formulation. CMC was characterized by FTIR and NMR. pH-sensitive hydrogels of theophylline were formulated using CMC and carbopol 934. Hydrogels were evaluated for swelling, drug content in vitro drug release studies, and in vivo studies on rabbit. The swelling studies have shown little swelling in acidic pH 432% at the end of two hours and 1631% in basic pH at the end of 12 hours. The release profile of the formulation I containing CMC and carbopol in 1 : 1 ratio showed sustained release. In vivo studies showed that the release of theophylline from the prepared hydrogel formulation (Test) exhibit better prolonged action when compared to (standard) marketed sustained release formulation. The studies showed that the pH-sensitive hydrogel of CMC can be used for extended release of theophylline in intestine and can be highly useful in treating symptoms of nocturnal asthma.

Analgesic Efficacy of Low Doses of Dexketoprofen in the Dental Pain Model

1996 ◽  
Vol 11 (6) ◽  
pp. 320-330 ◽  
Author(s):  
C. Gay ◽  
E. Planas ◽  
M. Donado ◽  
J.M. Martínez ◽  
R. Artigas ◽  
...  
Keyword(s):  
Analgesic Efficacy ◽  
Dental Pain ◽  
Low Doses ◽  
Pain Model

scholarly journals Venlafaxine-Induced Orthostatic Hypotension in a Geriatric Patient

2013 ◽  
Vol 2013 ◽  
pp. 1-3
Author(s):  
Vidyashree Chikkaramanjegowda ◽  
Jose de Leon
Keyword(s):  
Adverse Drug Reaction ◽  
Drug Reaction ◽  
Orthostatic Hypotension ◽  
Extended Release ◽  
Geriatric Patients ◽  
Standing Position ◽  
Low Doses ◽  
History Of ◽  
Clinically Significant ◽  
Caucasian Female

Venlafaxine is not usually associated with risk of orthostatic hypotension. A 65-year-old US Caucasian female taking 225 mg/day of venlafaxine extended-release developed symptomatic orthostatic hypotension. The systolic and diastolic blood pressure dropped by 25 and 18 mm Hg, respectively, from supine position to standing position within 3 minutes. The patient was otherwise healthy and the orthostatic hypotension resolved with venlafaxine discontinuation. This was a probable venlafaxine adverse drug reaction according to the Naranjo scale. This case contributes to the scarce literature that indicates that clinicians need to be aware that occasionally venlafaxine can induce clinically significant orthostatic hypotension, particularly in geriatric patients. Our patient did not have orthostatic hypotension when she was taking venlafaxine at 60 years of age in higher venlafaxine doses (300 mg/day) but developed this adverse drug reaction when venlafaxine was restarted at the geriatric age. This case indicates that a history of prior tolerance to venlafaxine does not guarantee tolerance after 65 years of age. If a clinician decides to use venlafaxine in geriatric patients, the clinician should warn the patient about the risk of orthostatic hypotension and consider very slow titration and low doses.

scholarly journals Formulation, Optimization and Evaluation of Bilayer Tablet of Antihypertensive Drug

2019 ◽  
Vol 9 (4) ◽  
pp. 704-708 ◽  
Author(s):  
, Swetanshu ◽  
Vijay Sharma
Keyword(s):  
Sustained Release ◽  
Initial Dose ◽  
Maintenance Dose ◽  
Extended Release ◽  
Immediate Release ◽  
Sustained Release Tablet ◽  
Bilayer Tablet ◽  
Release Drug ◽  
Sequential Release ◽  
Release Tablet

Hypertension or high blood pressure occurs when the high cardiac output exerts pressure on the arterial wall as the blood flow increases. Bi-layer tablets are prepared with one layer of drug for immediate release while second layer designed to release drug later, either as second dose or in an extended release manner. Bi-layered tablet is suitable for sequential release of two drugs in combination, separate two incompatible substances, and also for sustained release tablet in which one layer is immediate release as initial dose and second layer is maintenance dose. Bilayer tablet is suitable for sequential release of two drugs in combination, separate two incompatible substances and also for sustained release tablet in which one Layer is immediate release as initial dose and second layer is maintenance dose. The preparation of tablets in the form of multi layers is used to provide systems for the administration of drugs. Keywords: Hypertension, Bi-layered tablet, Enalapril, Immediate release and Sustained release.

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