CN103893170B - A kind ofly prevent and treat pharmaceutical composition and the application thereof that postoperative complication is cut in palace - Google Patents
A kind ofly prevent and treat pharmaceutical composition and the application thereof that postoperative complication is cut in palace Download PDFInfo
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- CN103893170B CN103893170B CN201410143010.0A CN201410143010A CN103893170B CN 103893170 B CN103893170 B CN 103893170B CN 201410143010 A CN201410143010 A CN 201410143010A CN 103893170 B CN103893170 B CN 103893170B
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Abstract
The invention discloses and a kind ofly prevent and treat pharmaceutical composition and the application thereof that postoperative complication is cut in palace, said composition is prepared from by active component and adjuvant, and described active component comprises α-allocryptopine or its officinal salt.Pharmaceutical composition of the present invention can reduce the follicule-stimulating hormone (FSH) level of hysterectomy postoperative patient person, improves estradiol and testosterone water, thus alleviates the generation of hysterectomy post-operative complication, prevent and treat Anxiety And Depression Symptoms simultaneously, thus improves the quality of life of women.
Description
Technical field
The invention belongs to medical art, specifically, particularly relate to and a kind ofly prevent and treat pharmaceutical composition and the application thereof that postoperative complication is cut in palace.
Background technology
Hysterectomy is one of the most frequently used and the most basic operation of department of obstetrics and gynecology.The treatment of a lot of obstetrical and gynecological disease must adopt uterectomy.In the U.S., there are hundreds thousand of women's row uterectomys every year.China is nearly 1,000,000 cases with uterine excisions every year.
But hysterectomy is postoperative causes some complication, comprising: (1) spirit depressing.The endocrine adjustment of uterus and ovary and central nervous system form a feedback system.After hysterectomizing, this feedback element is destroyed, particularly can disturb normal secretions and the metabolism of central neurotransmitter during decrease in estrogen, Anxiety And Depression Symptoms in various degree can be caused, there is depressed, mood anxiety, lack the performances such as interest, insomnia and dreamful sleep, hypomnesis, thus reduce the quality of life of women.(2) urinary system symptom increases.Female urinary system and reproductive system have homology, are all estrogen-dependent organ.Decrease in estrogen after hysterectomizing, can make Periurethral elastic tissue thinning, occur urinary incontinence, mucous membrane of urethra atrophy, and resistance declines, and easily brings out urinary tract infection, occurs a series of urinary tract infection symptoms such as frequent micturition, urgent micturition, dysurea.(3) femal sexual function goes down.Estrogen is the most important adjustment hormone of femal sexual function, and ovary is Major Secretory organ, after hysterectomizing, the blood fortune of ovary and function affect by it, most women's federations experience sexual function change in various degree, and as hyposexuality or shortage, sexual activity frequency reduces, property reactivity reduces, orgasm is difficult and genitals feels to go down.(4) hypo-ovaria.Endocrine between the front uterus of menopause and ovary remains accurate and trickle dynamic equilibrium, must destroy this balance after hysterectomizing, and can impel ovarian function generation decay, and menopause syndrome in advance and comparatively obvious.After hysterectomy there is deterioration in ovary, shows as low estrogen and High gonadotropic hormone state,
Hormone Replacement Therapy cuts the clinical conventional therapeutic scheme of post-operative complication as palace, and it has the restriction of contraindication and the potential danger of cardiovascular and cerebrovascular vessel and woman's cancer, thus causes use limited.Seek for the effective clinical solution of this situation, there is important clinical and social benefit.
α-allocryptopine (α-Allocryptopine), molecular formula C
21h
23nO
5, molecular weight 369.41 is from bloodroot Herba Macleayae Cordatae, extract the isoquinoline alkaloid obtained, and has antibacterial, parasite killing and kills the pharmacologically actives such as maggot, arrhythmia, anti-infarction.CN102234282A discloses a kind of preparation method of allocryptopine, and it is undertaken by following processing step: A. acid extraction: to be rich in the bloodroot of allocryptopine for raw material, seepage pressure effects after sour water soaks; B. macroporous resin enrichment: extracting solution adjusts pH to 7.5-8.5, crosses macroporous adsorptive resins, concentrate eluant; C. solvent extraction: adopt organic solvent extraction eluting concentrated solution; D. column chromatography: with aluminium oxide or silica gel as column packing, acetate-methanol gradient elution, Fractional Collections flow point; E. crystallization: with mixed solvent crystallization, obtain the allocryptopine product that purity reaches more than 95%.
By retrieval domestic and foreign literature, bibliographical information α-allocryptopine is not still had to have the biological activity of control hysterectomy post-operative complication at present.
Summary of the invention
In view of gonadal hormone alternative medicine has the restriction of contraindication and the potential danger of cardiovascular and cerebrovascular vessel and woman's cancer, therefore the present inventor is by studying natural drug, provides a kind of plant-derived control palace to cut the medicine of postoperative complication.
In order to realize object of the present invention, inventor is studied by lot of experiments, finally obtains following technical scheme:
Prevent and treat the pharmaceutical composition that postoperative complication is cut in palace, be prepared from by active component and adjuvant, described active component comprises α-allocryptopine or its officinal salt.
Preferably, the pharmaceutical composition of postoperative complication is cut in control palace as mentioned above, and wherein said active component is made up of α-allocryptopine or its officinal salt.
α-allocryptopine cuts postoperative complication to control palace obvious biological activity, but this compound dissolubility in water is very low, and easily changes.α-allocryptopine exists in the form of salts can improve its water solublity, can keep its stability again, be conducive to bioactive performance.Therefore, further preferably, as mentioned above the pharmaceutical composition of postoperative complication is cut in control palace, and wherein said α-allocryptopine officinal salt is the hydrochlorate of α-allocryptopine, tartrate and citrate.
Again further preferably, the pharmaceutical composition of postoperative complication is cut in control palace as mentioned above, and wherein said pharmaceutical composition is oral formulations, and described oral formulations comprises tablet, capsule, granule.
The present invention is proved by animal experiment research, α-allocryptopine is gavaged after 6 weeks to the female rats after uterectomy, compare its follicule-stimulating hormone (FSH) level of model control group significantly to decline, estradiol and testosterone levels significantly raise, this shows that α-allocryptopine can alleviate the generation of hysterectomy post-operative complication, especially can prevent and treat the postoperative premature ovarian failure caused of hysterectomy.Therefore, the present invention also provides a kind of pharmaceutical applications, that is: α-allocryptopine or its officinal salt cut the application in the medicine of postoperative complication in preparation control palace.Preferably, it is premature ovarian failure that postoperative complication is cut in described palace.
Compared with prior art, the pharmaceutical composition tool that the present invention relates to has the following advantages and marked improvement:
(1) α-allocryptopine can reduce the follicule-stimulating hormone (FSH) level of the postoperative rat of hysterectomy, improves estradiol and testosterone water, thus alleviates the generation of hysterectomy post-operative complication.
(2) α-allocryptopine can prevent and treat the postoperative Anxiety And Depression Symptoms caused of hysterectomy, thus improves the quality of life of women.
Detailed description of the invention
Further illustrate α-allocryptopine below by animal experiment example and there is the biological activity that postoperative complication is cut in stronger control palace.
Healthy SPF level female sd inbred rats, body weight 180 ~ 220g, raising temperature (20 ± 2) DEG C, illumination every day 12h, feedstuff, water, bedding and padding are added in time by special messenger change every days.All rats are cooked vagina epithelium exfoliative cyte picture for 1 time, continuous 10d every day.Select the rat having 2 normal oestrous cycles continuously, be divided into following three groups at random: Normal group, model control group, α-allocryptopine intervention group, often organize 10.
Except Normal group, all the other two groups of rats hysterectomize as follows: the urethane solution intraperitoneal injection of anesthesia (1g/kg body weight) with 25%, dorsal position is fixed, wipe out and become mildewed, after skin routine disinfection, in ventrimeson pubic symphysis 0.5cm place, longitudinal incision skin is about 1.5cm, blunt separation abdominal muscle and peritoneum, expose uterus, neat cervix uteri lower edge clamp is from disconnected, the ligation of broken ends of fractured bone silk thread, upwards seek the liparitosis of seeing that milky is shinny, fractionation of fatty group, just the ovary of pink or yellowish red color can be seen, the other ligament of below fallopian tube and palace and fascia in first silk thread ligation ovary, again from disconnected taking-up uterus, two-layered suture surgical wound.
Rat is sub-cage rearing under the same conditions, 5, every cage, and routine feeding standard particle feedstuff, freely drinks sterilized water.Post operation starts on the 9th day, each group gavages following corresponding tested material by 1mL/200g body weight: Normal group and model control group gavage equal-volume purified water, α-allocryptopine intervention group presses rat weight gavage α-allocryptopine 50mg/kg, every day 1 time, continuous 6 weeks.α-allocryptopine is purchased from Mei He bio tech ltd of Shenzhen.Experimental session observes body weight, wound healing, expression, the situation such as chaeta and activity of each treated animal.Fasting 12h before blood sampling in latter second day is terminated in administration, the urethane solution intraperitoneal injection of anesthesia of 25%, heart extracting blood puts common biochemical tube, room temperature leaves standstill, centrifugal in 8h (3000r/min) separation of serum afterwards,-20 DEG C of preservations, adopt the content of kit measurement estradiol, lutropin, follicule-stimulating hormone (FSH), testosterone.
Experimental session is observed and is found, each group rat wound all heals well, and have no hyperemia, ulcer, ooze out and the situation such as infection suppurates, all rats are showed no activity extremely.From modeling in the 1st day latter about the 42nd day, model group had 6 rats to show spirit gradually to show slightly tired, and happiness is rolled up, and voluntary activity reduces.In addition, after off-test, the change of each group Serum Sex Hormones is as shown in table 1.
After table 1 off-test, each group Levels of Serum Sex Hormones in Rats compares
Compare with Normal group,
★ p< 0.05,
★ ★ p< 0.01;
Compare with model control group,
▼ p< 0.05,
▼ ▼ p< 0.01.
Can be found out by the test statistics result of table 1, compared with Normal group, model group rats serum estradiol and testosterone levels obviously reduce (
p< 0.01), follicule-stimulating hormone (FSH) level obviously raises (
p< 0.05); α-allocryptopine intervention group follicule-stimulating hormone (FSH) level compared with model group declines (
p< 0.01), estradiol and testosterone levels raise (
p< 0.05 or
p< 0.01).
Claims (1)
1. α-allocryptopine or its officinal salt cut the application in the medicine of postoperative complication in preparation control palace, and it is premature ovarian failure that postoperative complication is cut in described palace.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410143010.0A CN103893170B (en) | 2014-04-11 | 2014-04-11 | A kind ofly prevent and treat pharmaceutical composition and the application thereof that postoperative complication is cut in palace |
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| CN201410143010.0A CN103893170B (en) | 2014-04-11 | 2014-04-11 | A kind ofly prevent and treat pharmaceutical composition and the application thereof that postoperative complication is cut in palace |
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| CN103893170A CN103893170A (en) | 2014-07-02 |
| CN103893170B true CN103893170B (en) | 2016-01-20 |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105169151A (en) * | 2015-11-03 | 2015-12-23 | 强红枫 | Application of camellia cuspidate-peony flower in preparation of medicine for preventing and treating complications after hysterectomy |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101327211A (en) * | 2008-06-18 | 2008-12-24 | 长沙世唯科技有限公司 | Use of allocryptopine and salt thereof in resisting liver fibrosis |
| CN103083408A (en) * | 2011-10-27 | 2013-05-08 | 中国中医科学院中药研究所 | Composition of traditional Chinese medicine extracts, and preparation method and application thereof |
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2014
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101327211A (en) * | 2008-06-18 | 2008-12-24 | 长沙世唯科技有限公司 | Use of allocryptopine and salt thereof in resisting liver fibrosis |
| CN103083408A (en) * | 2011-10-27 | 2013-05-08 | 中国中医科学院中药研究所 | Composition of traditional Chinese medicine extracts, and preparation method and application thereof |
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Inventor after: Zhang Linghua Inventor after: Yu Peilin Inventor after: Ma Piliang Inventor after: Sun Dongning Inventor before: Zhang Defang |
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Effective date of registration: 20151126 Address after: Shibei District People's road 266000 Shandong city of Qingdao province No. 4 Applicant after: Qingdao Hiser Medical Center Address before: Baoji City, Shaanxi Province Dongfeng Road 721000 District 45 No. Third Hospital of PLA Applicant before: Bai Lingqiang |
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