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Discovery and preclinical development of ⅢM-160, a Bergenia ciliatabased anti-inflammatory and anti-arthritic botanical drug candidate

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Journal of Integrative Medicine 2019年第3期17卷 192-204页

作者： Sandip B.Bharate Vikas Kumar Sonali S.Bharate Bikarma Singh Gurdarshan Singh Amarinder Singh Mehak Gupta Deepika Singh Ajay Kumar Surjeet Singh Ram A.Vishwakarma Medicinal Chemistry Division Indian Institute of Integrative Medicine Council of Scientific and Industrial Research PK-PD Toxicology & Formulation Division Indian Institute of Integrative Medicine Council of Scientific and Industrial Research Biodiversity and Applied Botany Division Indian Institute of Integrative Medicine Council of Scientific and Industrial Research Quality Control and Quality Assurance Division Indian Institute of Integrative Medicine Council of Scientific and Industrial Research

Objective: Bergenia ciliata(Haw.) Sternb. is used in the Indian traditional system of medicine to treat various ailments including rheumatism and to heal wounds. The objective of the present study was to perform a preclinical characterization of the B. ciliata-based botanical extract ***: ⅢM-160 was chemically standardized and analyzed for heavy metal content, aflatoxins,pesticides and microbial load. The in vitro and in vivo efficacies were determined in suitable models of inflammation, arthritis and nociception. An acute oral toxicity study was performed in Swiss albino mice.A suitable oral formulation was developed and ***: Bergenin was found to be the major component(9.1% w/w) of ⅢM-160. The botanical lead displayed inhibition of lipopolysaccharide-induced production of proinflammatory cytokines in THP-1 cells, with selectivity toward interleukin-6(IL-6) and had an excellent safety-window. It showed anti-inflammatory, anti-arthritic and antinociceptive activity in animal models and was not toxic at oral doses up to 2 g/kg in Swiss-albino mice. The gastroretentive, sustained-release capsule formulation showed sustained-release of the bergenin over the period of 24 h, resulting in improved plasma-exposure of bergenin in Sprague–Dawley ***: The dual-activity of IL-6 inhibition and antinociception marks the suitability of ⅢM-160 for treating rheumatoid arthritis. This study will serve as the benchmark for further research on this botanical formulation.

关键词： Botanical preclinical candidate UIM-160 Bergenia ciliata Arthritis gastroretentive sustained release formulation Bergenin

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Development and characterization of amoxicillin loaded floating microballoons for the treatment of Helicobacter pylori induced gastric ulcer

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Asian Journal of Pharmaceutical Sciences 2013年第3期8卷 174-180页

作者： Rajendra Awasthi Giriraj T.Kulkarni Department of Pharmaceutical Science Jawaharlal Nehru Technological UniversityKukatpally 500085India Laureate Institute of Pharmacy Tehsil e DehraDistt.KangraKathog 177101Himachal PradeshIndia

The current communication reports in vitro characterization of the optimized hollow floating microballoons of amoxicillin on the basis of micromeritic properties and in vitro minimum inhibitory concentration(MIC).Amoxicillin loaded hollow microballoons were prepared by emulsion solvent diffusion *** morphological characterization was done on the basis of scanning electron microscopy(SEM).Fourier Transformed Infrared Spectroscopy(FTIR)was used to investigate drugepolymer *** correlation between the in vitro buoyancy of microballoons and their physical properties,*** and porosity were *** results of FTIR spectroscopy revealed the absence of any drugepolymer *** porosity values of more than 69%and diameter to thickness ratio greater than 2.90,proved a high cavity volume within the microballoons in all size *** spherical shape of microballoons with hollow internal cavity was confirmed from SEM *** in vitro MIC results showed a sustained drug effect from the *** conclusion,it can be said that the developed microballoons can be used for the effective treatment of Helicobacter pylori induced gastric ulcer.

关键词： Floating Gastric ulcer gastroretentive H.pylori Micromeritic Microballoons

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