scispace - formally typeset
Search or ask a question
Patent

Pharmaceutical compositions of rhein or diacerein

TL;DR: Compositions by invention are bioequivalent to preparative form of diacerein in dosage 50 mg, sold under the trade name Art 50®, and considerable reduction of side effects, such as pulpy stool, in comparison with Art 50®,.
Abstract: FIELD: medicine. SUBSTANCE: claimed invention relates to granulated from liquid pharmaceutical compositions, which contain rhein or diacerein, or their salts, and pharmaceutically acceptable carrier. Compositions contain from 20 to 45 mg of rhein or diacerein. Invention also relates to methods of producing claimed compositions. Compositions by invention are bioequivalent to preparative form of diacerein in dosage 50 mg, sold under the trade name Art 50®. Compositions do not demonstrate variability in after meal condition and on an empty stomach. EFFECT: considerable reduction of side effects, such as pulpy stool, in comparison with Art 50®. 13 cl, 37 tbl, 17 ex
Citations
More filters
Journal ArticleDOI
TL;DR: The SEDDS offers the benefit of a protective effect against the hostile environment in the gut, and the unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
Abstract: Introduction: Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arises from poor aqueous solubility of drug. Aqueous solubility of lipophilic drugs can be improved by various techniques like salt formation, complexation, addition of co-solvent etc. but self-emulsifying drug-delivery system (SEDDS) is getting more attention for increasing the solubility of such drugs. The SEDDS is an isotropic mixture of drug, lipids, and emulsifiers, usually with one or more hydrophilic co-solvents/co-emulsifiers. This system is having ability to generate oil-in-water (o/w) emulsions or microemulsions upon gentle agitation followed by dilution with aqueous phase. The SEDDSs are relatively newer, lipid-based technological innovations possessing unparalleled potential in improving oral bioavailability of poorly water-soluble drugs.Areas covered: This review provides updated information regarding the types of SEDDS, their preparation techniques, drug delivery and related recent patents along with marketed formulations.Expert opinion: The SEDDS has been explored for improving bioavailability, rising intra-subject heterogeneity, and increasing solubility. SEDDS offers the benefit of a protective effect against the hostile environment in the gut. The unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.

29 citations


Cites background from "Pharmaceutical compositions of rhei..."

  • ...Nahat et al 2015 disclosed the pharmaceutical composition incorporating rhein or diacerein and other excipients....

    [...]

Journal ArticleDOI
TL;DR: It has been reviewed that apart from the risk of diarrhea on long-term administration of DCN, various clinical studies has also shown its modest benefits in treatment of various pathological conditions and DCN is emerging as a new and potentially safe derivative with maximum therapeutic efficacies and minimum side effects which can results in improving the living status of patients suffering from various inflammatory diseases.
Abstract: Diacerein (DCN) was obtained by diacetylation of an anthraquinone derivative rhein and was approved by FDA in 2008, in the treatment of osteoarthritis due to its inhibitory effect on proinflammatory cytokines, including IL-6 and IL-1β. It was synthesized in 1980s and marketed as a tablet in some European Union and Asian countries from 1994. Along with its great potential in the treatment of osteoarthritis, its other applications are also being explored day by day, such as in the treatment of psoriasis, epidermolysis bullosa, breast cancer, type 2 diabetes and periodontitis. The main aim of this review is to explore mechanism of action, various applications and side effects associated with DCN. This has been reviewed that apart from the risk of diarrhea on long-term administration of DCN, various clinical studies has also shown its modest benefits in treatment of various pathological conditions. Hence, DCN is emerging as a new and potentially safe derivative with maximum therapeutic efficacies and minimum side effects which can results in improving the living status of patients suffering from various inflammatory diseases.

12 citations


Cites background from "Pharmaceutical compositions of rhei..."

  • ...When rhein reaches the colonic site, it gets converted into the rhein-9-anthrone which is particularly responsible for the soft stools (Nakhat et al., 2015)....

    [...]

Journal ArticleDOI
TL;DR: The approach of enhancing solubility and wet-ability in accompany with optimized asymmetric osmotic pump system could serve as a promising delivery system and a way to improve the bioavailability of poorly aqueous soluble drugs.
Abstract: In an attempt to improve the low oral bioavailability of Diacerein (DCN), the combination of a ternary solid dispersion and an asymmetric osmotic pump system had been designed to enhance solubility...

10 citations

Journal ArticleDOI
TL;DR: Aspirin-entrapped SLM showed good sustained-release properties, enhanced anti-inflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.
Abstract: BACKGROUND Aspirin is a nonsteroidal anti-inflammatory drug that is very effective in the treatment of inflammation and other health conditions, however, it causes gastric irritation. Recently, researchers have developed patents (US9757529, 2019) of inhalable aspirin for rapid absorption and circumvention of gastric irritation. OBJECTIVE The aim of this work was to formulate aspirin-loaded lipid based formulation in order to enhance oral bioavailability and inhibit gastric irritation. METHODS This solid lipid microparticles loaded with aspirin (SLM) was formulated by a modified cold homogenization-solvent evaporation method. In vitro studies such as in vitro drug release, particle size, Encapsulation Efficiency (EE), micromeritic properties and loading capacity were carried out. Pharmacodynamics studies such as anti-inflammatory and ulcerative properties of the SLM were also carried out in Wistar rats. RESULTS The results showed that aspirin entrapped SLM exhibited the highest EE of 72% and particle size range of 7.60 + 0.141µm to 20.25 + 0.070µm. Formulations had about 55% drug release at 6h in simulated intestinal fluid pH 6.8. The formulations had good flowability that could facilitate filling into hard gelatin capsule shells. The SLM exhibited 100% gastroprotection against aspirin-induced ulcers (p < 0.05). The percentage of anti-inflammatory activities also showed that aspirin-entrapped SLM had 78% oedema inhibition at 7h, while the reference had 68% inhibition at 7h. CONCLUSION Aspirin-entrapped SLM showed good sustained-release properties, enhanced antiinflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.

9 citations


Cites methods from "Pharmaceutical compositions of rhei..."

  • ...Self-Emulsifying Drug Delivery Systems (SEDDS) [54-58], their constituents, methods of development and applications were also described....

    [...]

  • ...Self-Emulsifying Drug Delivery Systems (SEDDS) [54-58], their constituents, methods of development and applications were also described....

    [...]

  • ...SLM = Solid Lipid Microparticles SGF = Simulated Gastric Fluid SIF = Simulated Intestinal Fluid SEDDS = Self-Emulsifying Drug Delivery System LC = Loading Capacity LMC = Lipid Matrix Carrier EE = Encapsulation/Entrapment Efficiency SA = Stearic Acid P90H = Phospholipon ® 90H (soy lecithin hydrogenated) S154 = Softisan ® 154 (completely hydrogenated palm oil) SLN = Solid Lipid Nanoparticles HGH = Human Growth Hormones LBF = Lipid Based Formulations COX = Cyclooxygenase Enzyme...

    [...]

References
More filters
Journal ArticleDOI
TL;DR: The SEDDS offers the benefit of a protective effect against the hostile environment in the gut, and the unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.
Abstract: Introduction: Oral administration of a drug is the most common, ideal and preferred route of administration. The main problem of oral drug formulations is their low bioavailability arises from poor aqueous solubility of drug. Aqueous solubility of lipophilic drugs can be improved by various techniques like salt formation, complexation, addition of co-solvent etc. but self-emulsifying drug-delivery system (SEDDS) is getting more attention for increasing the solubility of such drugs. The SEDDS is an isotropic mixture of drug, lipids, and emulsifiers, usually with one or more hydrophilic co-solvents/co-emulsifiers. This system is having ability to generate oil-in-water (o/w) emulsions or microemulsions upon gentle agitation followed by dilution with aqueous phase. The SEDDSs are relatively newer, lipid-based technological innovations possessing unparalleled potential in improving oral bioavailability of poorly water-soluble drugs.Areas covered: This review provides updated information regarding the types of SEDDS, their preparation techniques, drug delivery and related recent patents along with marketed formulations.Expert opinion: The SEDDS has been explored for improving bioavailability, rising intra-subject heterogeneity, and increasing solubility. SEDDS offers the benefit of a protective effect against the hostile environment in the gut. The unique fabrication techniques provide specific strategy to overcome the low bioavailability and poor solubility problems.

29 citations

Journal ArticleDOI
TL;DR: It has been reviewed that apart from the risk of diarrhea on long-term administration of DCN, various clinical studies has also shown its modest benefits in treatment of various pathological conditions and DCN is emerging as a new and potentially safe derivative with maximum therapeutic efficacies and minimum side effects which can results in improving the living status of patients suffering from various inflammatory diseases.
Abstract: Diacerein (DCN) was obtained by diacetylation of an anthraquinone derivative rhein and was approved by FDA in 2008, in the treatment of osteoarthritis due to its inhibitory effect on proinflammatory cytokines, including IL-6 and IL-1β. It was synthesized in 1980s and marketed as a tablet in some European Union and Asian countries from 1994. Along with its great potential in the treatment of osteoarthritis, its other applications are also being explored day by day, such as in the treatment of psoriasis, epidermolysis bullosa, breast cancer, type 2 diabetes and periodontitis. The main aim of this review is to explore mechanism of action, various applications and side effects associated with DCN. This has been reviewed that apart from the risk of diarrhea on long-term administration of DCN, various clinical studies has also shown its modest benefits in treatment of various pathological conditions. Hence, DCN is emerging as a new and potentially safe derivative with maximum therapeutic efficacies and minimum side effects which can results in improving the living status of patients suffering from various inflammatory diseases.

12 citations

Journal ArticleDOI
TL;DR: The approach of enhancing solubility and wet-ability in accompany with optimized asymmetric osmotic pump system could serve as a promising delivery system and a way to improve the bioavailability of poorly aqueous soluble drugs.
Abstract: In an attempt to improve the low oral bioavailability of Diacerein (DCN), the combination of a ternary solid dispersion and an asymmetric osmotic pump system had been designed to enhance solubility...

10 citations

Journal ArticleDOI
TL;DR: Aspirin-entrapped SLM showed good sustained-release properties, enhanced anti-inflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.
Abstract: BACKGROUND Aspirin is a nonsteroidal anti-inflammatory drug that is very effective in the treatment of inflammation and other health conditions, however, it causes gastric irritation. Recently, researchers have developed patents (US9757529, 2019) of inhalable aspirin for rapid absorption and circumvention of gastric irritation. OBJECTIVE The aim of this work was to formulate aspirin-loaded lipid based formulation in order to enhance oral bioavailability and inhibit gastric irritation. METHODS This solid lipid microparticles loaded with aspirin (SLM) was formulated by a modified cold homogenization-solvent evaporation method. In vitro studies such as in vitro drug release, particle size, Encapsulation Efficiency (EE), micromeritic properties and loading capacity were carried out. Pharmacodynamics studies such as anti-inflammatory and ulcerative properties of the SLM were also carried out in Wistar rats. RESULTS The results showed that aspirin entrapped SLM exhibited the highest EE of 72% and particle size range of 7.60 + 0.141µm to 20.25 + 0.070µm. Formulations had about 55% drug release at 6h in simulated intestinal fluid pH 6.8. The formulations had good flowability that could facilitate filling into hard gelatin capsule shells. The SLM exhibited 100% gastroprotection against aspirin-induced ulcers (p < 0.05). The percentage of anti-inflammatory activities also showed that aspirin-entrapped SLM had 78% oedema inhibition at 7h, while the reference had 68% inhibition at 7h. CONCLUSION Aspirin-entrapped SLM showed good sustained-release properties, enhanced antiinflammatory properties and total gastric protection from aspirin-induced ulcers and could be used as once-daily oral aspirin.

9 citations