Delving into the Latest Updates on Lornoxicam with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Bevonium Metilsulfate, Bosporon, Chlortenoxicam

+ [20]

Target

COXs

Action

inhibitors

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Immune System DiseasesNervous System DiseasesSkin and Musculoskeletal Diseases

Active Indication

BursitisCervicobrachial syndromeLow Back Pain+ [7]

Inactive Indication

HeadacheMigraine Disorders

Originator Organization

F. Hoffmann-La Roche Ltd.

Active Organization

Taisho Pharmaceutical Co., Ltd.Takeda Pharmaceuticals International AG

Taisho Pharmaceutical Holdings Co., Ltd.

Inactive Organization

POZEN, Inc.

Drug Highest PhaseApproved

First Approval Date

Denmark (01 Jan 1997),

Cervicobrachial syndromeLow Back PainNeuralgia+ [6]

Regulation-

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Structure/Sequence

Molecular FormulaC13H10ClN3O4S2

InChIKeyWLHQHAUOOXYABV-UHFFFAOYSA-N

CAS Registry70374-39-9

Aim:This study aimed to develop and evaluate lornoxicam (LXM) and thiocolchicoside (TCS) transferosomal transdermal patches.Background:Oral administration of LXM and TCS can lead to gastric irritation, necessitating alternative delivery methods for pain and inflammation relief. Incorporating LXM & TCS into transferosomes within a transdermal patch offers a potential solution.Objective:The objective of this study is to develop and evaluate transferosomal transdermal patches containing LXM and TCS, incorporating Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers. The aim is to enhance the skin permeation of these drugs while mitigating gastric irritation associated with their oral administration.Method:Transferosomes were made by the thin film hydration tactic, with nine formulations based on three independent variables: phosphatidylcholine, span 80, and sonication time. Entrapment efficiency and drug release at 6th h were assessed as dependent variables. The optimized combination was then formulated into transdermal patches via central composite design, evaluating the impact of AVLM and LO on lornoxicam discharge and other physicochemical properties.Results:The average weight and thickness of the patches ranged from 7.52±0.75 to 8.07±0.11g and from 1.69±0.01 to 1.82±0.02mm, respectively, representing minimal variance. The LXM/TCS content homogeneity ranged from 92.84±3.55 to 94.07±4.61% for LXM and from 90.17±1.98 to 93.18±2.98% for TCS, demonstrating robust uniformity. Higher proportions of phosphatidylcholine and span 80, along with lesser sonication time, led to improved entrapment of lornoxicam. In vitro, discharge studies demonstrated optimal discharge with a higher proportion of phosphatidylcholine, a medium proportion of span 80, and a longer sonication time. The transferosomal patches exhibited zero-order discharge kinetics, with LXM & TCS discharge % at 24, 48, and 72 h.Conclusion:The study concludes that formulation TDP-8, which incorporates 3g of Aloe vera leaf mucilage (AVLM) and lime oil (LO) as permeability enhancers, demonstrated favorable discharge characteristics. This indicates its potential as an effective transdermal delivery system for LXM and TCS, offering a promising substitute for pain and inflammation relief while minimizing gastric irritation. The study succeeded in developing and evaluating transferosomal transdermal patches for LXM and TCS, providing an alternative delivery method that minimizes gastric irritation.

02 Jan 2025·Drug Development and Industrial Pharmacy

Development of immediate release tablet formulations of lornoxicam with hot melt extrusion-based three-dimensional printing technology

Article

Author: Yilmaz, Aysel ; Mutlu-Agardan, N. Basaran ; Takka, Sevgi

INTRODUCTIONThis study aims to develop immediate release tablet formulations of lornoxicam (LRX) using hot melt extrusion (HME)-based fused deposition modeling (FDM) focusing on the adjustment of drug release by arranging infill densities and evaluating microcrystalline cellulose II (MCC II) as a disintegrating agent for HME-FDM purposes. LRX is a poorly soluble drug that exhibits pH-dependent solubility with a high thermal degradation temperature. These characteristics make it an ideal model drug for the HME-based FDM technique.METHODSVarious filament formulations were extruded using an extruder, and suitable filaments were used to produce 3D-printed tablets. Filaments and tablets were characterized. Dissolution studies were performed on tablets with different infill densities. DSC, FTIR, XRD, and SEM analyses were conducted.RESULTSAlthough the solubility of LRX increases with pH, disintegrating agents such as MCC II had a more significant effect on the dissolution of LRX than sodium bicarbonate, which was used as the alkalinizing pore-forming agent. Dissolution studies revealed that the dissolution of LRX was enhanced by tablet erosion. Tablet erosion increased as the infill density decreased, and an immediate release profile was reached with tablets having 25% infill density. Despite the availability of conventional immediate release LRX tablets, this newly developed formulation offers the potential to be modulated for personalized therapy via the 3D printing technique.CONCLUSIONThis study demonstrates the feasibility of HME-based FDM printing technology for producing immediate-release LRX tablets with consistent quality, highlighting the utilization of MCC II as a disintegrating agent that enhances LRX dissolution in this process.

01 Dec 2024·International Journal of Pharmaceutics

A potential cocrystal strategy to tailor in-vitro dissolution and improve Caco-2 permeability and oral bioavailability of berberine

Article

Author: Zhou, Yang ; Zhou, Feng ; Chen, Quanbing ; Yang, Junhui ; Jiang, Lei ; Chen, Hui ; Zhang, Jiantao ; Ma, Jiangpo

Berberine hydrochloride (BER), a promising candidate in treating tumors, diabetes and pain management, has relatively low oral absorption and bioavailability due to its low intestinal permeability. To address these challenges, we developed a BER and lornoxicam cocrystal (BLCC) by a solvent evaporation method and characterized it using X-ray diffraction, differential scanning calorimetry and thermogravimetric analysis. Compared with BER, BLCC exhibited an instant release in pH 1.0 HCl and a sustained release up to 24 h in pH 6.8 buffer solutions and water. The Caco-2 permeability of BLCC has shown a remarkable increase compared to that of BER (i.e., P_app(a→b): 50.30 × 10^-7vs 8.82 × 10^-7 cm/s), which is attributed to the improved lipophilicity of BER (i.e., log P: 1.29 vs -1.83) and the reduced efflux amount of BER (i.e., ER: 1.71 vs 12.11). Furthermore, BLCC demonstrated a relative bioavailability of 410 % in comparison to the original BER, due to notably enhanced intestinal permeability of BLCC and its continuous dissolution in simulated intestinal fluid. BLCC has the potential to tailor the dissolution behavior, improve intestinal permeability, and boost the bioavailability of BER. This indicates that the cocrystal strategy holds promise as an effective approach to improving the oral absorption and bioavailability of active pharmaceutical molecules with low permeability during drug development.

1

News (Medical) associated with Lornoxicam

01 Mar 2020

·acino.swiss

Acino completes acquisition with Takeda for primary care portfolio in key emerging markets

Acino and Takeda Pharmaceuticals announced today the completion of the acquisition for parts of Takeda’s primary care portfolio in selected countries in the Middle East, Africa, and Ukraine. Acino has received anti-trust approvals in Turkey, South Africa, and Ukraine and can now proceed with the integration as planned. As part of the transaction, Acino acquired the rights to selected pain management, gastroenterology, cardiovascular and respiratory products from Takeda’s prescription pharmaceutical and OTC portfolio. Around 270 employees, primarily sales and marketing professionals supporting the portfolio, are also transitioning to Acino. ‘We are excited to welcome our new colleagues to Acino and to expand our offering in our key therapeutic areas and markets’, says Steffen Saltofte, CEO of Acino. ‘The portfolio we have acquired fits very well with our strategy to make high-quality medicines accessible to patients and healthcare professionals in emerging markets.’ The transfer comprises approximately 30 selected prescription pharmaceutical and OTC medicines including Pantoprazole, Dexlansoprazole, Cardiomagnyl, Xefo and Montelukast. The acquisition enables Acino to further reinforce its position in the key markets of the United Arab Emirates, Egypt, Saudi Arabia, Ukraine and South Africa. Additionally, Acino has opened a company in Istanbul, Turkey, to expand its footprint in this country. As previously announced in October 2019, Acino agreed to acquire the assets from Takeda for a total value in excess of $200 million. Additionally, both parties have entered into a multi-year manufacturing and supply agreement, under which Takeda will continue to manufacture the products on behalf of Acino.

Acquisition

100 Deals associated with Lornoxicam

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External Link

KEGG	Wiki	ATC	Drug Bank
D01866	Lornoxicam	M01AC05	DB06725

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Bursitis	Japan	Taisho Pharmaceutical Co., Ltd.	02 Feb 2001
Cervicobrachial syndrome	Denmark	-	01 Jan 1997
Low Back Pain	Denmark	-	01 Jan 1997
Neuralgia	Denmark	-	01 Jan 1997
Osteoarthritis	Denmark	-	01 Jan 1997
Pain	Denmark	-	01 Jan 1997
Pain, Postoperative	Denmark	-	01 Jan 1997
Periarthritis	Denmark	-	01 Jan 1997
Rheumatic Diseases	Denmark	-	01 Jan 1997
Rheumatoid Arthritis	Denmark	-	01 Jan 1997

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Headache	Phase 1	United States	POZEN, Inc.	01 Dec 2005
Migraine Disorders	Phase 1	United States	POZEN, Inc.	01 Dec 2005
Pain, Postoperative	Phase 1	United States	POZEN, Inc.	01 Nov 2005

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01117948 (CTgov)	Phase 2	Alzheimer Disease	219	Lornoxicam (Lornoxicam)	kgzsktfcni(scgdgjaydp) = fuxvzgdlun hwvtsrrayh (iqnlthxwwc, ikbkimwlyg - rlwlafyzmz) View more	-	29 Nov 2012
				Placebo (Placebo)	kgzsktfcni(scgdgjaydp) = bvbuwnhgav hwvtsrrayh (iqnlthxwwc, xggeyylhwe - oqsgmkhcps) View more