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Pharmaceutical compositions for calanolides, their derivatives and analogues, and process for producing the same

A composition, calanolide technology, applied in the directions of drug combination, pharmaceutical formulation, drug delivery, etc., can solve the problem of no report and overcome calanolide, low bioavailability, no disclosure or identification, etc.

Inactive Publication Date: 2013-08-14
CRAUN RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the present invention is different from the formulations of existing studies, because the existing studies do not report and overcome the problem of low bioavailability of calatonin
[0009] Second, none of the formulations of the above studies disclosed or identified any pharmaceutical composition comprising calanolides, solubility enhancers, and surfactants that improve the water solubility and bioavailability of calatonin. It is not obvious

Method used

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  • Pharmaceutical compositions for calanolides, their derivatives and analogues, and process for producing the same
  • Pharmaceutical compositions for calanolides, their derivatives and analogues, and process for producing the same
  • Pharmaceutical compositions for calanolides, their derivatives and analogues, and process for producing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0242] Preparation of calanoline A solution

[0243] The following formulation provides a solution of calanoline A suitable for filling soft gels with enhanced water solubility and bioavailability as shown in Examples 9 and 10.

[0244]

[0245] 5.6 kg medium chain triglyceride oil was heated to about 50°C-60°C, then 1.0 kg calanoline A was added and dissolved in the oil. Then PEG-40 hydrogenated castor oil (Cremophor RH 40) was added, the mixture was cooled to room temperature and then 825 mg of the mixture was filled in each soft capsule, each soft capsule contained 100 mg calanoline A for oral administration.

Embodiment 2

[0247] Preparation of calanoline A solution

[0248] The following formulation provides a solution of calanoline A suitable for filling soft gels with enhanced water solubility and bioavailability as shown in Examples 9 and 10. .

[0249]

[0250] 1.0 kg of medium chain triglyceride oil and 2.0 kg of polyethylene glycol 200 were heated to about 50°C-60°C, then 1.0 kg of calatonin A was added and dissolved in the mixture. Then 3.8 kg polysorbate 80 and 0.2 kg sorbitan monolaurate were added and the mixture was cooled to room temperature. Then fill 800mg mixture in each soft capsule, then contain 100mg calanoline A in each soft capsule for oral administration.

Embodiment 3

[0252] Preparation of calanoline A solution

[0253] The following formulation provides a solution of calanoline A suitable for aseptic filling for injection (intramuscular or subcutaneous) with enhanced water solubility and bioavailability as shown in Examples 9 and 11.

[0254]

[0255]

[0256] At 20°C-30°C, 1.0 kg calanolide A was dissolved in 6.32 kg N-methylpyrrolidone. Then 0.4 kg polysorbate 20 and 0.28 kg PEG-40 hydrogenated castor oil were added with stirring until a homogeneous solution was formed and 800 mg of the solution was aseptically filled in each vial for injection.

[0257] Each vial contains 100 mg calanoline A for intramuscular or subcutaneous administration.

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Abstract

The present invention relates to pharmaceutical compositions of calanolides, their derivatives and analogues, and process for producing the same having enhanced solubility and bioavailability for oral or parenteral administration. The invention further provides for a method of using the disclosed compositions for the treatment and prevention of retroviral diseases such as human immunodeficiency, specifically HTV-1 and mycobacterial diseases especially tuberculosis infections in mammals, particularly humans.

Description

technical field [0001] The present application relates to a pharmaceutical composition of calanolide and calanolide derivatives and analogs, and a preparation method thereof, the pharmaceutical composition has enhanced solubility and bioavailability. [0002] In particular, it relates to pharmaceutical compositions of calanolide and calanolide derivatives and analogs for oral or injectable use. [0003] The present invention further discloses a method of treating and preventing retroviral diseases and mycobacterial infections in mammals, particularly humans, using the disclosed compositions. Background technique [0004] Due to the increase in cases of infectious diseases, there is a need for continuous efforts to develop new drugs to treat and prevent these diseases. Among these infectious diseases, human immunodeficiency virus (HIV) and tuberculosis (TB) are the major lethal diseases. [0005] In US Patents 5,591,770, 5,859,049 and 6,268,393, incorporated herein by refer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/08A61K9/107A61K31/352A61K9/20
CPCA61K9/0019A61K9/2054A61K9/08A61K9/205A61K9/4858A61K47/22A61K9/2018A61K9/1075A61K47/26A61K47/44A61K31/352A61K47/14A61K47/10A61K45/00A61K45/06A61P31/04A61P31/06A61P31/12A61P31/14A61P31/18A61P43/00
Inventor 彭宜零扎利赫·克里斯廷·阿卜杜拉
Owner CRAUN RES
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