Hydroxycamptothecine cubic liquid crystal precursor composition as well as preparation method and application thereof

A technology of hydroxycamptothecin and liquid crystal precursors, which can be used in liquid delivery, drug combination, and medical preparations of non-active ingredients, etc. It can solve the problems of reducing encapsulation efficiency, drug leakage, and poor targeting of microemulsions. Achieve the effects of avoiding the reduction of drug efficacy, prolonging the action time and protecting the active group

CN104622801AInactive Publication Date: 2015-05-20THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
Publication Date
2015-05-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a hydroxycamptothecine cubic liquid crystal precursor composition as well as a preparation method and an application thereof, and belongs to the technical field of pharmacy. The composition is prepared from the following main raw materials in percentage by weight: 4 to 6% of hydroxycamptothecine, 50 to 78% of liquid crystal material, 2 to 8% of PEG, 1 to 3% of triolein, 2 to 7% of stearin, and 13 to 26% of dispersion medium, wherein the dispersion medium is prepared from the following raw materials in percentage by weight: 8 to 30% of an organic solvent which can be dissolved in water, and 70 to 92% of water. The composition can be continuously released in vitro for more than 30 days, so that the acting time of hydroxycamptothecine is greatly prolonged; and in addition, the local application mode is special, and thus, the effects of slowly releasing and targeting can be achieved synchronously.
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Description

technical field

[0001] The invention relates to the technical field of pharmacy, in particular to a cubic liquid crystal precursor composition of hydroxycamptothecin and its preparation method and application. Background technique

[0002] Hydroxycamptothecin is a tryptophan-terpene alkaloid isolated from Campylodontia involucratae, which inhibits DNA replication, transcription and mitosis by inhibiting DNA topoisomerase Ⅰ, thereby making tumor cells Lethal damage occurs, and it is mainly used clinically for malignant tumors such as gastric cancer, primary liver cancer, leukemia, rectal cancer, and bladder cancer.

[0003] The antitumor activity of hydroxycamptothecin is closely related to its molecular structure. Closing the lactone ring is a necessary form to exert anticancer activity, and opening the lactone ring will greatly reduce or inactivate the activity. Studies have shown that the existing form of the camptothecin drug structure depends on the acidity and alkalini...

Examples

Embodiment 1

[0048] A cubic liquid crystal precursor composition of hydroxycamptothecin, prepared from the following raw materials:

[0049]

[0050] The cubic liquid crystal precursor composition of above-mentioned hydroxycamptothecin is prepared by the following method:

[0051] Weigh hydroxycamptothecin and the dispersion medium absolute ethanol according to the above formula, disperse and dissolve hydroxycamptothecin in absolute ethanol, slowly add water dropwise to the above solution, then add phytantriol, vortex and mix evenly, Then, PEG 400, glyceryl dioleate and Gelucire 33 / 01 were respectively added into the mixture, and the hydroxycamptothecin cubic liquid crystal precursor composition A was obtained after vortex mixing at room temperature.

Embodiment 2

[0053] A cubic liquid crystal precursor composition of hydroxycamptothecin, prepared from the following raw materials:

[0054]

[0055] The cubic liquid crystal precursor composition of above-mentioned hydroxycamptothecin is prepared by the following method:

[0056] Weigh hydroxycamptothecin and propylene glycol as the dispersion medium according to the above formula, disperse and dissolve hydroxycamptothecin in propylene glycol, slowly add water dropwise to the above solution, then add glyceryl monooleate, vortex and mix evenly, and then PEG 400, glyceryl dioleate and Gelucire 43 / 01 were respectively added into the mixture, and the hydroxycamptothecin cubic liquid crystal precursor composition B was obtained after vortex mixing at room temperature.

Embodiment 3

[0058] A cubic liquid crystal precursor composition of hydroxycamptothecin, prepared from the following raw materials:

[0059]

[0060]

[0061] The cubic liquid crystal precursor composition of above-mentioned hydroxycamptothecin is prepared by the following method:

[0062] Weigh hydroxycamptothecin and dispersion medium N-methylpyrrolidone according to the above formula, disperse and dissolve hydroxycamptothecin in N-methylpyrrolidone, slowly add water to the above solution, then add phytantriol, vortex Then, PEG 400, glyceryl dioleate and Gelucire 33 / 01 were added to the mixture, and the hydroxycamptothecin cubic liquid crystal precursor composition C was obtained after vortex mixing at room temperature.