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1.
North Clin Istanb ; 10(1): 122-126, 2023.
Article in English | MEDLINE | ID: mdl-36910437

ABSTRACT

The work aimed to explore the clinical hypothesis on the possible alternative to Opiorphin and its stable analogues for treating fibromyalgia pain. Fibromyalgia is a condition characterized by chronic pain triggered by an interplay of biological and psychosocial variables, although the exact pathogenesis is still controversial. Standard therapy for low threshold tender point pain includes NSAIDs and opioid analgesics, both of which have serious adverse profiles after long-term exposure, highlighting the need for an intermediate compound capable of bridging the gap between NSAIDs and opioid analgesics. Opiorphin is an anti-nociceptive modulator which inhibits the enzyme responsible for the degradation of natural endogenous opioid neuropeptides. This paper hypothesizes and concludes that Opiorphin and its stable analogues (Sialorphine, STR-324) can be an alternative for the treatment of chronic long-standing low-threshold tender point pain associated with fibromyalgia.

2.
Pak J Pharm Sci ; 34(2): 607-613, 2021 Mar.
Article in English | MEDLINE | ID: mdl-34275836

ABSTRACT

The main intention of the current investigation was to fabricate ocular films of Dexamethasone sodium phosphate (DSP) impregnated in rate controlling membrane and to characterize in vitro and in vivo (iv-iv). DSP release was regulated by HPMC K4M and ethyl cellulose (EC) and dimethyl sulfoxide (DMSO) as a permeability enhancer. DSP suitability with polymers was observed by DSC and FT Infrared spectroscopic readings. The fabricated DSP ocular films were examined for physicochemical tests, in vitro discharge and in vivo infusion in rabbits. The improved formulation (F-8) was proved its stability under stressed storage conditions. The fabricated ocular films process acceptable physical characters with DSP release in a controlled manner. The optimized DSP films were intact even in stressed storage situations. It was concluded that the fabricated films effectively hold the DSP at the programmed site for the desired period of time and exhibit expected pharmacodynamics actions.


Subject(s)
Conjunctivitis/drug therapy , Dexamethasone/analogs & derivatives , Glucocorticoids/administration & dosage , Administration, Ophthalmic , Animals , Cellulose/analogs & derivatives , Delayed-Action Preparations , Dexamethasone/administration & dosage , Dimethyl Sulfoxide , Drug Carriers , Hypromellose Derivatives , In Vitro Techniques , Permeability , Rabbits
3.
Turk J Pharm Sci ; 17(4): 372-380, 2020 Aug.
Article in English | MEDLINE | ID: mdl-32939132

ABSTRACT

OBJECTIVES: The aim of this study of this study was to discover the best poloxamer as a solid dispersion carrier for thiocolchicoside (TCS). MATERIALS AND METHODS: The compatibility of TCS with excipients was studied by differential scanning colorimetry and fourier transform infrared spectroscopy. Different formulations of solid dispersions (SDs) were made with poloxamer carriers, i.e. poloxamer-108, poloxamer-188, poloxamer-237, poloxamer-338, and poloxamer-407 were made by taking TCS:poloxamer in ratios of 1:1, 1:2, 1:4, and 1:6. The SDs were made by a novel microwave fusion method and compressed using an 8-station tablet compression machine. The fabricated SD tablets were characterized by physicochemical constraints and drug release rates. The release of TCS from the prepared SDs was later analyzed by kinetic models. RESULTS: TCS was observed to be compatible with the poloxamer carriers. The SD formulations showed satisfactory physicochemical constraints and TCS release following first-order release. CONCLUSION: Among the poloxamer carriers used, poloxamer-188 was the best for increasing the solubility and release rate of TCS from the SDs.

4.
Pak J Pharm Sci ; 29(3): 945-51, 2016 May.
Article in English | MEDLINE | ID: mdl-27166538

ABSTRACT

The purpose of this investigation was to prepare matrix type transdermal patches of Tramadol HCl using various ratios of Ficus carica fruit mucilage and Povidone. The matrix type transdermal patches were prepared using Tramadol HCl with Ficus carica fruit mucilage and Povidone. The interactions between Tramadol HCl with F. carica fruit mucilage and Povidone were performed by Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared spectroscopy (FTIR). The prepared patches were examined for physicochemical characterization and in vitro drug permeation studies (using a Keshary-Chien diffusion cell across hairless Albino rat skin), skin irritation studies and accelerated stability studies. The drug was found to be free from negligible interactions with the polymers used. The formulated patches possessed satisfactory physicochemical properties, in vitro drug permeation and devoid of serious skin irritation. The selected formulation (F-5) was retains the characteristics even after the accelerated environmental conditions. The study concludes that F. carica fruit mucilage with Povidone is a good combination for preparing transdermal patches.


Subject(s)
Adhesives/chemistry , Analgesics, Opioid/administration & dosage , Drug Carriers , Ficus/chemistry , Povidone/chemistry , Tramadol/administration & dosage , Transdermal Patch , Adhesives/isolation & purification , Administration, Cutaneous , Analgesics, Opioid/chemistry , Analgesics, Opioid/metabolism , Animals , Calorimetry, Differential Scanning , Chemistry, Pharmaceutical , Diffusion , Drug Stability , Fruit , Kinetics , Microscopy, Electron, Scanning , Models, Biological , Permeability , Rabbits , Rats , Rats, Hairless , Skin/metabolism , Skin Absorption , Solubility , Spectroscopy, Fourier Transform Infrared , Technology, Pharmaceutical/methods , Tramadol/chemistry , Tramadol/metabolism
5.
Nat Prod Res ; 26(17): 1649-53, 2012.
Article in English | MEDLINE | ID: mdl-22008064

ABSTRACT

Alangium salviifolium root was screened for phytochemical and anti-inflammatory properties. The percentage inhibition of carrageenan induced paw oedema was studied in rats. Alangium salvifolium gave maximum extractive values with Ethanol and the Loss on Drying value, total ash value and acid-insoluble ash and water soluble ash values were within limits. The extract gave positive tests for phytosterols, triterpenes, flavonoids, carbohydrates and alkaloids. The extract was free from glycosides, saponins, tannins, proteins and amino acids. In acute toxicity studies, Alangium salviifolium root extract was found to be safe up to 3000 mg kg⁻¹, p.o. in the albino rats. The Alangium salviifolium root gave significant per cent inhibition of the maximal paw oedema and very highly significant per cent inhibition of total paw oedema during 6 h. This study revealed that Alangium salviifolium root has good anti-inflammatory actions when compared with Diclofenac sodium.


Subject(s)
Alangiaceae/chemistry , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/therapeutic use , Plant Extracts/chemistry , Plant Extracts/therapeutic use , Plant Roots/chemistry , Animals , Diclofenac/therapeutic use , Edema/drug therapy , Rats
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