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Compound preparation for treating hyperprolactinemia and preparation method thereof

A technology of hyperprolactinemia and compound preparations, which is applied in the field of compound preparations for the treatment of hyperprolactinemia and its preparation, can solve the problems of clinical application limitations, dependence on imported drugs, and large side effects, so as to improve immunity, Inhibition of physiological lactation, inhibition of secretion and synthesis

Inactive Publication Date: 2016-08-10
刘惠平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The clinical effect is good, but the drug source relies on imports, the price is expensive, the side effects are relatively large, and it is easy to relapse after stopping the drug, so the clinical application is limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1: A compound preparation for the treatment of hyperprolactinemia prepared in this example, including the following ingredients in parts by weight: 13 parts of tamoxifen, 8 parts of letrozole, 7 parts of estradiol valerate, citron 4 parts of clomiphene acid, 2 parts of human chorionic gonadotropin, 1.5 parts of progesterone, 1 part of bromocriptine, 0.7 parts of levodopa, 0.4 parts of octahydrobenzoquinoline, 23 parts of vitamin B6, ginsenoside Rh2 17 parts, 5 parts of fucoidan sulfate, 3 parts of paclitaxel, 0.3 parts of preservative, and 5 parts of emulsifier.

[0016] Wherein, the tamoxifen is prepared from p-bromophenol and acetic acid as starting materials through ether condensation, chlorination, condensation, alkylation, Grivia reaction, dehydration, and salt formation. The method has the advantages of few reaction steps, simple operation, high total yield, low cost, etc., and is more suitable for mass production in the pharmaceutical industry.

[0017] ...

Embodiment 2

[0025] Example 2: A compound preparation prepared in this example for the treatment of hyperprolactinemia, including the following ingredients in parts by weight: 17.5 parts of tamoxifen, 11 parts of letrozole, 9 parts of estradiol valerate, citron 6.5 parts of clomiphene acid, 3.5 parts of human chorionic gonadotropin, 3 parts of progesterone, 2 parts of bromocriptine, 1.1 parts of levodopa, 0.8 parts of octahydrobenzoquinoline, 29 parts of vitamin B6, ginsenoside Rh2 20.5 parts, fucoidan sulfate 8 parts, paclitaxel 4.5 parts, preservative 0.4 parts, emulsifier 7 parts.

[0026] Wherein, the tamoxifen is prepared from p-bromophenol and acetic acid as starting materials through ether condensation, chlorination, condensation, alkylation, Grivia reaction, dehydration, and salt formation. The method has the advantages of few reaction steps, simple operation, high total yield, low cost, etc., and is more suitable for mass production in the pharmaceutical industry.

[0027] Wherei...

Embodiment 3

[0035] Example 3: A compound preparation for the treatment of hyperprolactinemia prepared in this example, including the following ingredients in parts by weight: 24 parts of tamoxifen, 14 parts of letrozole, 11 parts of estradiol valerate, citron 9 parts of clomiphene acid, 5 parts of human chorionic gonadotropin, 4.5 parts of progesterone, 3 parts of bromocriptine, 1.5 parts of levodopa, 1.2 parts of octahydrobenzoquinoline, 35 parts of vitamin B6, ginsenoside Rh2 24 parts, 11 parts of fucoidan sulfate, 6 parts of paclitaxel, 0.5 parts of preservative, and 9 parts of emulsifier.

[0036] Wherein, the tamoxifen is prepared from p-bromophenol and acetic acid as starting materials through ether condensation, chlorination, condensation, alkylation, Grivia reaction, dehydration, and salt formation. The method has the advantages of few reaction steps, simple operation, high total yield, low cost, etc., and is more suitable for mass production in the pharmaceutical industry.

[00...

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Abstract

The invention discloses a compound preparation for treating hyperprolactinemia and a preparation method thereof .The compound preparation is prepared from tamoxifen, letrozole, estradiol valerate, clomifene citrate, human chorionic gonadotropin, progesterone, bromocriptine, levodopa, octahydro benzoquinoline, vitamin B6, ginsenoside Rh2, fucoidan from fucus vesiculosus and paclitaxel .The compound preparation can effectively inhibit the production of pituitary tumor cells and thus inhibit the secretion and synthesis of prolactin of pituitary tumor cells, can effectively reduce the prolactin content in blood of patients with the hyperprolactinemia, the hypothalamus pituitary gonadal axis of the patients can play a good regulating role at all levels, and a feasible method having a wider prospect is provided for effective treatment of the hyperprolactinemia.

Description

technical field [0001] The invention relates to the technical field of oncology drugs, in particular to a compound preparation for treating hyperprolactinemia and a preparation method thereof. Background technique [0002] Hyperprolactinemia is caused by a variety of factors that cause excessive secretion of prolactin (PRL) by eosinophils in the anterior pituitary gland. Elevation of PRL causes dysfunction of the hypothalamus-pituitary-gonadal axis. Clinically, it is manifested as female amenorrhea, Galactorrhea, infertility, thin menstruation, etc.; male sexual dysfunction, impotence, non-ejaculation, breast development, galactorrhea, etc. In the current diagnostic standard, serum PRL>30ng / ml can be diagnosed as hyperprolactinemia. With the continuous improvement of diagnostic technology, the number of patients with hyperprolactinemia is increasing year by year. By the attention of experts at home and abroad. At present, the first choice of chemical drugs is ergotamine...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/24A61P15/00A61P5/08A61K31/737A61K31/704A61K31/57A61K31/565A61K31/48A61K31/473A61K31/4415A61K31/4196A61K31/337A61K31/198A61K31/138
CPCA61K31/138A61K31/198A61K31/337A61K31/4196A61K31/4415A61K31/473A61K31/48A61K31/565A61K31/57A61K31/704A61K31/737A61K38/24A61K2300/00
Inventor 刘惠平李国臣
Owner 刘惠平
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