Pharmacological preparation device with bakuchiol and O-acetyl-bakuchiol for use against arthritis

Abstract

A pharmacological composition consisting of bakuchiol and O-acetyl-bakuchiol as active ingredients, formulated in a pharmaceutically acceptable carrier, configured to provide anti-inflammatory, analgesic and anti-rheumatic effects.

Description

AREA OF INVENTION

[0001] The invention relates to pharmaceutical and biomedical compositions for the treatment and management of inflammatory and autoimmune diseases. More specifically, it relates to a bioactive pharmacological composition containing bakuchiol and O-acetyl-bakuchiol as the main active ingredients for the relief of symptoms in rheumatoid arthritis and other chronic inflammatory diseases. The invention integrates computer-generated data on molecular interactions with pharmacologically active dosage forms for a targeted antirheumatic effect. BACKGROUND OF THE INVENTION

[0002] Rheumatoid arthritis (RA) is a chronic, systemic autoimmune disease that primarily affects the joints, leading to inflammation, swelling, and ultimately cartilage and bone loss. Current drug therapies are mainly based on nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, and disease-modifying antirheumatic drugs (DMARDs). Although effective, these often cause severe side effects such as gastrointestinal problems, liver damage, and immunosuppression, making long-term therapy difficult.

[0003] Natural bioactive compounds from medicinal plants have proven to be safer and more sustainable alternatives for treating inflammatory diseases. Bakuchiol, a meroterpene isolated from Psoralea corylifolia, has shown potent anti-inflammatory and antioxidant properties in previous studies. However, its specific pharmacodynamic role and molecular interaction with key inflammatory mediators such as tumor necrosis factor-alpha (TNF-α) have remained largely unexplored. Its derivative, O-acetyl-bakuchiol (BAc), exhibits altered pharmacokinetic properties with potentially improved bioavailability and target affinity.

[0004] The present invention addresses this unmet need with a scientifically validated pharmacological composition system that integrates bakuchiol and O-acetyl-bakuchiol for a targeted antirheumatic effect. This system demonstrates effective suppression of inflammatory mediators and the restoration of normal physiological parameters, thus offering a safe and natural therapeutic alternative for rheumatoid arthritis. SUMMARY OF THE INVENTION

[0005] The invention relates to a device for the production of a pharmacological composition designed as a biotherapeutic formulation system with bakuchiol and O-acetyl-bakuchiol as the primary active ingredients. The composition has anti-inflammatory, analgesic, and antirheumatic effects and is suitable for oral or injectable administration. The device integrates computer-optimized molecular binding data with pharmacological in vivo validations to establish a therapeutic model with a dual mechanism of action.

[0006] The composition exhibits a strong molecular affinity for TNF-α receptors, as confirmed by docking simulations with binding energies of -7.29 kcal / mol for bakuchiol and -7.19 kcal / mol for O-acetylbakuchiol. In vivo studies using experimental arthritis models confirm the system's ability to significantly reduce paw inflammation, normalize hematological parameters, and restore joint mobility. The pharmacological system thus provides a stable, biocompatible, and efficient platform for administering natural antirheumatic agents and represents a safer alternative to conventional chemical therapies. DETAILED DESCRIPTION

[0007] The invention relates to a pharmacological formulation device containing a biologically active composition of bakuchiol and O-acetyl-bakuchiol in pharmaceutically compatible carrier substances. Depending on the intended clinical application, the composition can be formulated as capsules, tablets, an injectable solution, or a topical gel.

[0008] The system contains bakuchiol derived from Psoralea. Seeds of Corylifolia and its acetylated analogue O-acetyl-bakuchiol are blended in a defined ratio to achieve optimal anti-inflammatory and analgesic effects. The active ingredients are dissolved or encapsulated in a biocompatible carrier matrix composed of inert excipients such as microcrystalline cellulose, polyethylene glycol, or plant polysaccharides to ensure stability and controlled release.

[0009] The composition exhibits a strong affinity for inflammatory mediators, particularly TNF-α, as determined by computer-aided docking simulations. The molecular binding of bakuchiol and O-acetyl-bakuchiol to the receptor proteins TNF-α, COX-2, and IL-6 suggests a high inhibitory potential against pro-inflammatory signaling pathways.

[0010] In vivo tests of the pharmacological device in animal models of arthritis showed a significant reduction in paw edema, joint inflammation, and pain sensitivity. The device also normalized hematological parameters such as red blood cell count, hemoglobin level, and erythrocyte sedimentation rate, while simultaneously lowering the white blood cell count, which is often elevated in rheumatoid arthritis. Serum markers of inflammation, including C-reactive protein and rheumatoid factor, were significantly reduced in the test groups treated with the bakuchiol-based formulation.

[0011] Histopathological examination showed restoration of normal joint architecture, a reduction in synovial inflammation, and a decrease in cartilage erosion. The anti-inflammatory efficacy of O-acetyl-bakuchiol (66.5%) and its analgesic effect (47.4%) were comparable to standard antirheumatic drugs, confirming the pharmacological potential of the system.

[0012] The composition can be administered orally, topically, or parenterally. For oral administration, encapsulated bakuchiol and O-acetyl-bakuchiol powders are suspended in a pharmaceutically safe solvent. For topical application, the composition can be incorporated into a hydrogel base with natural stabilizers and penetration enhancers.

[0013] The device offers numerous advantages, including natural origin, high biocompatibility, lack of toxicity, and efficient treatment of inflammatory symptoms. The integration of computer modeling and in vivo validation ensures mechanistic accuracy and predictable therapeutic outcomes.

Claims

[1] A pharmacological composition consisting of bakuchiol and O-acetyl-bakuchiol as active ingredients, formulated in a pharmaceutically acceptable carrier, configured to provide anti-inflammatory, analgesic and anti-rheumatic effects. [2] Composition according to claim 1, wherein the active components exhibit a high binding affinity to tumor necrosis factor -alpha (TNF-α) receptors, which was confirmed by computer-aided docking simulations which yielded binding energies of about -7.29 and -7.19 kcal / mol respectively. [3] Composition according to claim 1, wherein the composition further comprises inert excipients, stabilizers or encapsulation materials selected from microcrystalline cellulose, polyethylene glycol or natural polysaccharides to improve bioavailability and delayed release. [4] Composition according to any of the preceding claims, wherein the composition device causes a reduction in arthritic inflammation, a normalization of hematological parameters and an improvement in joint histopathology, and thus represents a natural and biocompatible alternative to conventional synthetic antirheumatic drugs.