CN100553645C - Solid pipefish dispersion and preparation method thereof and application - Google Patents
Solid pipefish dispersion and preparation method thereof and application Download PDFInfo
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- CN100553645C CN100553645C CNB2007100270640A CN200710027064A CN100553645C CN 100553645 C CN100553645 C CN 100553645C CN B2007100270640 A CNB2007100270640 A CN B2007100270640A CN 200710027064 A CN200710027064 A CN 200710027064A CN 100553645 C CN100553645 C CN 100553645C
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Abstract
The invention discloses a kind of solid pipefish dispersion and its production and application, the preparation method of solid pipefish dispersion, comprise the steps: Solenognathus earlier through complex enzyme hydrolysis, carrying out the antioxidation eliminating sargassum smell then handles, to add polyvinylpyrrolidone through the Solenognathus complex enzyme hydrolysis product of eliminating sargassum smell again, the mass ratio of Solenognathus complex enzyme hydrolysis product and polyvinylpyrrolidone is 1: 1～1: 14, and spray drying can obtain solid pipefish dispersion.The present invention is through lot of experiments, make a kind of solid pipefish dispersion, this solid pipefish dispersion has good curative effect to prostatic hyperplasia and hyperplasia of mammary glands, can reach the therapeutic effect of positive control drug, evident in efficacy than without the same crude drug amount Solenognathus of PROCESS FOR TREATMENT has the low advantage of toxicity simultaneously.Therefore, can be used for preparing the medicine and the health food of treatment benign prostatic hyperplasia, hyperplasia of mammary glands.
Description
Technical field
The present invention relates to the Chinese crude drug Solenognathus, specifically, relate to a kind of solid pipefish dispersion and its production and application.
Background technology
(Benign Prostatic Hyperplasia BPH) is prostate-urethra peripheral cell hypertrophy to benign prostate hyperplasia, and the enlargement of carrying out property of body of gland makes prostate ankylo-urethria, causes that the bladder urine flows out infraction.Clinical manifestation is symptoms such as frequent micturition, dysuria, urine retention and hematuria.This is a kind of common male's senile disease.The people of male about 30%～50% more than 50 years old has prostatic hyperplasia in various degree, and sickness rate increased and increases along with the age.It is reported that male's sickness rate of 70 years old～79 years old is that male more than 70%, 80 years old is then up to 90%.BPH is the dysuric common cause of elderly men, and Chang Bingfa urinary system infection even hydronephrosis and uremia, has influenced patient's quality of life, so cause clinical showing great attention to.But the medicine of existing this disease of treatment is common to exist the problem that curative effect is desirable not to the utmost, toxic and side effects is big.Therefore, research and develop a kind of treatment medicine that prostatoplasia diseases is effective, toxic and side effects is little, this is to guaranteeing that the senior health and fitness will have crucial meaning.
Drug therapy becomes important Therapeutic Method day by day in recent years.The medicine of treatment prostatic hyperplasia mainly contains alpha-2-adrenoceptor blocker, 5 inhibitor, galenical and Chinese patent medicine etc.
The alpha-2-adrenoceptor blocker has Phenoxybenzamine, prazosin, terazosin (hytrin), Alfuzosin (Sang Ta) and Tamsulosin (breathing out happy), and the common side effect of these medicines is a postural hypotension.The 5 inhibitor has finasteride (proscar) and epristeride, and outgrowth prostate is dwindled, and reduces serum DHT.But must long-term prescription, and certain side effect is arranged, descend and ejaculate volume reduces as sexual impotence, libido, Chinese patent medicine has QIANLIETONG, prostatitis to relax etc., and it is clinical that galenical such as Permixon also are applied to, but the clinical trial certificate curative effect of some medicine is similar to placebo.As seen these medicines all respectively have shortcoming.Develop new efficiently, low cytotoxic drug is necessary.
Cyclomastopathy is that the women is common, one of frequently-occurring disease, is more common in 25～45 years old women, is the disorder of the mammary gland normal configuration that causes of a kind of physiology hypertrophy and subinvolution.In China, capsule sexually revises rarely, how based on glandular hyperplasia, so claim " cyclomastopathy " more.The World Health Organization's general designation " optimum mammary dysplasia ".Pathogenic factor is still not fully aware of, and present most scholars think, may lack of proper care relevant with the endocrine function of ovary.Prevalence is 36%, and outstanding performance has lump in distending pain of the breast and the breast.(1) distending pain of the breast: common is one-sided or bilateral distending pain of the breast or tenderness.The course of disease is not wait to the several years in 2 months, and Most patients has the periodically characteristics of pain, and premenstrua takes place or increases the weight of, and alleviates after the menstruation or disappears.(2) lump in breast: often be multiple, one-sided or bilateral; And size, quality also often are cyclically-varying with menstruation, and the premenstrua lump increases, and quality is harder, and lump dwindles after the menstruation, and matter is tough and not hard.Lay one's hand on and can touch lump when looking into and be the joint structure, not of uniform size, unclear with the surrounding tissue boundary, tenderness is arranged more, there is not adhesion with skin and deep tissue, can be pushed not enlargement of axillary gland.(3) menoxenia: this patient can doublely see before and after the menstruation irregularly, amount less or color light, can accompany dysmenorrhea.(4) feelings will changes: the normal emotion will of patient smooth or susceptible to lose temper due to restlessness, anger, psychentonia or tired postemphasis whenever.The treatment Western medicine has methyl testosterone, and the pain severe patient can be tried out.Because of methyl testosterone can cause that female patients is manlike, general edema and liver function injury.Prolonged application also can be brought out malignant tumor, and the patient is difficult for accepting.Chinese traditional treatment has ease pill, little gold plaque, nodules of the breast ball, Xi Huan Wan etc., but has slow curative effect, shortcoming such as not obvious.
Solenognathus is China's rare Chinese medicine.Theory of Chinese medical science thinks that Solenognathus has effects such as warming the kidney to invigorate YANG, dispersing swelling and dissipating binds and tranquillizing and allaying excitement.The patent report (ZL98103137.4, ZL 00113882.0) of reporting 30-40 kind treatment by Chinese herbs prostatic hyperplasia such as using Solenognathus, cyclomastopathy is arranged, the effect of main multiple crude drug, and single Chinese medicine prepares owing to un-extracted, curative effect is not remarkable.This patent adopts the national inventing patent technology of single Solenognathus by having, and the effective ingredient that extracts Solenognathus cooperates medical dressing polyvinylpyrrolidone (PVP-K30) preparation solid dispersion to improve the curative effect of Solenognathus in treatment prostatic hyperplasia, cyclomastopathy.
Summary of the invention
The purpose of this invention is to provide a kind of solid pipefish dispersion.
Another object of the present invention provides the preparation method of above-mentioned solid pipefish dispersion.
Further purpose of the present invention provides above-mentioned solid pipefish dispersion and is used for the treatment of the medicine of benign prostatic hyperplasia or hyperplasia of mammary glands or the application in the health food in preparation.
A kind of preparation method of solid pipefish dispersion, comprise the steps: Solenognathus earlier through complex enzyme hydrolysis, carrying out the antioxidation eliminating sargassum smell then handles, to add polyvinylpyrrolidone through the Solenognathus complex enzyme hydrolysis product of eliminating sargassum smell again, the mass ratio of Solenognathus complex enzyme hydrolysis product and polyvinylpyrrolidone is 1: 1～1: 14, and spray drying can obtain solid pipefish dispersion.
In above-mentioned preparation method, the preferred patent No. of the method for described antioxidation eliminating sargassum smell is 95107286.2, and name is called the method that the patent of invention of " the antioxidation fishy-removing-method of marine product extracting solution " is protected.
In above-mentioned preparation method, preferred 1: 2～1: 9 of the mass ratio of described Solenognathus complex enzyme hydrolysis product and polyvinylpyrrolidone.
In above-mentioned preparation method, described complex enzyme hydrolysis is to adopt Novozymes Company to provide compound enzyme product (Protamex) to carry out enzymolysis.
The resulting solid pipefish dispersion of above-mentioned preparation method can be used to prepare the medicine or the health product of treatment benign prostatic hyperplasia, cyclomastopathy.Can make suitable dosage form as required, tablet, powder, granule, capsule, syrup or suppository etc. also can prepare oral liquid, health promoting wine (medicated wine), use with oral way usually, can certainly adopt other administering mode; Use its every day solid pipefish dispersion dosage to be generally about 10～100000 milligrams, adult's usual amounts is 20～80000 milligrams of every days, and the most frequently used dosage is 30～40000 milligrams; Once a day or divide for several times and use.
Compared with prior art, the present invention has following beneficial effect: the present invention is through lot of experiments, make a kind of solid pipefish dispersion, this solid pipefish dispersion has good curative effect to prostatic hyperplasia and hyperplasia of mammary glands, can reach the therapeutic effect of positive control drug, evident in efficacy than without the same crude drug amount Solenognathus of PROCESS FOR TREATMENT has the low advantage of toxicity simultaneously.Therefore, can be used for preparing the medicine and the health food of treatment benign prostatic hyperplasia, hyperplasia of mammary glands.
The specific embodiment
Preparation of embodiment 1 solid pipefish dispersion and acute toxicity testing
One, material
Laboratory sample: freezing Solenognathus (syngnathus acus Linnaeus, habit Solenognathus, syngnathoides biaculeatus weight respectively accounts for 30%) is provided by life sciences institute of Zhongshan University.
Laboratory animal: NIH is a mice, is provided by medical experiment center, Guangdong Province
Two, method and result
Solenognathus capsule preparation: freezing Solenognathus (syngnathus acus Linnaeus, solenognathus hardwickii, syngnathoides biaculeatus, each 10 kilograms of weight), add 40 kilograms of deionized water homogenizer homogenizing, separate into hydrolyzed solution through 50 ℃ of temperature insulation compound enzymes (Protamex), eliminating sargassum smell, intensification enzyme denaturing activity adds 3 times of amount PVPK30, instantaneous spray drying, granulate, incapsulate, make the Solenognathus capsule.
Irritate stomach and give the animal subject acute toxicity testing: selecting healthy NIH is mice, body weight 20 ± 2g, 20, male and female half and half, the Solenognathus capsule powder is made into the 80mg/ml suspension with 0.5% normal saline, mice is once irritated stomach tried thing suspension 0.8ml/20g body weight, observed continuously seven days, mice is movable quick, fur is smooth, do not cause death or abnormal response, being limited to administration concentration and volume can not increase again, can not measure its LD
50So carry out mtd test.Select 20 of healthy mices, male and female half and half divided to gavage Solenognathus capsule powder suspension (80mg/ml) 8 times in 24 hours, each 0.5ml/20g body weight was observed 7 days, allowed mice ad lib and drinking-water during this, mice is movable quick, and fur is smooth, does not cause death or abnormal response.
Three, conclusion
Mice is irritated stomach every day and gives Solenognathus capsule powder maximum tolerated dose and should be not less than 0.5 * 8 * 80 * 50=16g/kg, belongs to actual nontoxic level.
Embodiment 2 treatment prostatic hyperplasia effects
One, material
1.1 laboratory animal: the healthy SD rat, male 4 ages in week, 70, about 200 grams of body weight, 8 age in week 70 of female unpregnancy Wistar rats, body constitution amount 200 ± 20g provides by Guangdong Medical Lab Animal Center.
1.2 experimental drug and reagent: testosterone propionate injection, Mingxing Pharmaceutical Factory, Guangzhou; Positive control drug: proscar, Mo Shadong (Britain) company, branch of Merck company, packing producer, Hangzhou Mo Shadong pharmaceutical Co. Ltd; Solenognathus capsule (preparation method such as experimental example 1) is provided by life sciences institute of Zhongshan University; Soybean oil (injection stage) is produced by Guangzhou Central Ye Pharmaceutical Co., Ltd; Estradiol benzoate injection, Shanghai General Pharmaceutical Co., ltd. produces; Progesterone injection, Shanghai General Pharmaceutical Co., ltd. produces.
Two, method and result
Health male SD rat in 4 age in week, 70 are selected in experiment for use.Get 60 at random, after the ether inhalation anesthesia under aseptic condition the excision bilateral testes, remain 10 rats as sham operated rats, animal is cut scrotum but is not cut testis, rested for 1 week, during injection penicillin 50,000 units/only.The animal of excision bilateral testes is divided 6 groups at random, and 10 every group, promptly model group, the positive are organized (proscar), the basic, normal, high dosage group of Solenognathus capsule, Hippocampus crude drug group.Except that the sham operated rats animal, all the other each treated animal intramuscular injection every day are dissolved in the testosterone propionate (0.5mg/0.1ml/ only) of soybean oil, and the sham operated rats animal gives not contain the medicine soybean oil; Sham operated rats and model group rat oral gavage give normal saline, positive group rat oral gavage gives proscar 0.0446mg/100g body weight, and basic, normal, high each group of Solenognathus capsule gives the crude drug content that Solenognathus capsule 40mg/100g, 80mg/100g, 160mg/100g body weight, Hippocampus crude drug group are equivalent to dosage in the Hippocampus Capsule respectively.Successive administration 40 days was weighed on the 41st day, got prostate, seminal vesicle, calculated the internal organs index (internal organs weight/body weight) of each internal organs.The T inspection statistics is analyzed, and the result is as shown in table 1.By experimental result as can be known, testosterone propionate is induced in the BPH rat models, and the prostate index (weight in wet base) of model control group all is significantly increased than normal control group, and prompting BPH model prepares successfully.The Solenognathus capsule has certain reduction effect to the prostate index: the seminal vesicle index of middle and high dosage group rat, compare with model control group, has significant difference (p＜0.05), compare with positive controls, there was no significant difference (p＞0.05), illustrate that the Solenognathus capsule can reach the therapeutic effect of positive drug proscar, illustrate that thus the Solenognathus capsule has the pharmacological action of treatment BPH, has the low advantage of toxicity simultaneously.
Table 1 Solenognathus capsule to testosterone propionate induce the exponential influence of rat prostate model of hyperplasia organ weight in wet base (x ± S.D., n=10)
Annotate: compare with model control group,
*P＜0.05,
*P＜0.01 is compared with positive controls,
Embodiment 3 treatment cyclomastopathy effects
One, material
1.1 laboratory animal: 8 the week age female unpregnancy Wistar rat, body constitution amount 200 ± 20g provides by Guangdong Medical Lab Animal Center.
1.2 experimental drug and reagent: methyl testosterone, pharmaceutical Co. Ltd; Solenognathus capsule (preparation method such as experimental example 1) is provided by life sciences institute of Zhongshan University; Estradiol benzoate injection, Shanghai General Pharmaceutical Co., ltd. produces; Progesterone injection, Shanghai General Pharmaceutical Co., ltd. produces.
Get 8 age in week 70 of female unpregnancy Wistar rats, body constitution amount 200 ± 20g, 26 rats are divided into 7 groups at random, be normal control group, model control group, positive controls, the basic, normal, high dosage group of Solenognathus capsule, Solenognathus crude drug group, every group each 10, except that the normal control group, all the other respectively organize rat muscle injection estradiol benzoate 0.5mg/kg, 1 time/d, 25d uses intramuscular injection Progesterone 4mg/kg subsequently instead continuously, 1 time/d, continuous 5d, the normal control group is not injected hormone and is only only given rat muscle injecting normal saline 0.2ml/, continuously 30d.Positive group rat oral gavage gave methyl testosterone 0.0446mg/100g body weight in 30 days during this time, basic, normal, high each group of Solenognathus capsule gives the crude drug content that Solenognathus capsule 40mg/100g, 80mg/100g, 160mg/100g body weight, Hippocampus crude drug group are equivalent to dosage in the Hippocampus Capsule respectively, and model control group and normal control group give equal-volume physiology and grind water.Successive administration 30 days, the 31st day diameter and height with the 2nd pair and the 3rd pair nipple of vernier caliper measurement, and observe its outward appearance.By experimental result as can be known, estradiol benzoate, Progesterone are induced in the rat mammary gland model of hyperplasia, and height of nipples, the diameter of model control group all are significantly increased than normal control group, and the prompting hyperplasia of mammary gland model prepares successfully.The Solenognathus capsule has certain reduction effect to height of nipples, diameter: height of nipples, the diameter of middle and high dosage group rat, compare with model control group, has significant difference (p＜0.05), compare with positive controls, there was no significant difference (p＞0.05), illustrate that the Solenognathus capsule can reach the therapeutic effect of positive drug, illustrate that thus the Solenognathus capsule has the pharmacological action of treatment cyclomastopathy, has the low advantage of toxicity simultaneously.
Table 2. Solenognathus capsule to testosterone propionate induce the rat mammary gland model of hyperplasia influence (x ± S.D., n=10)
Annotate: compare with model control group,
*P＜0.05,
*P＜0.01 is compared with positive controls,
Claims (4)
1, Solenognathus is used for the treatment of application in the solid dispersion of benign prostatic hyperplasia or cyclomastopathy as unique crude drug in preparation; Described solid pipefish dispersion is to be prepared from by following method: Solenognathus is first through complex enzyme hydrolysis, carrying out the antioxidation eliminating sargassum smell then handles, to add polyvinylpyrrolidone through the Solenognathus complex enzyme hydrolysis product of eliminating sargassum smell again, the mass ratio of Solenognathus complex enzyme hydrolysis product and polyvinylpyrrolidone is 1: 1～1: 14, and spray drying can obtain solid pipefish dispersion.
2, application as claimed in claim 1, the mass ratio that it is characterized in that described Solenognathus complex enzyme hydrolysis product and polyvinylpyrrolidone is 1: 2～1: 9.
3, application as claimed in claim 1 is characterized in that described complex enzyme hydrolysis is to adopt Novozymes Company to provide compound enzyme product P rotamex to carry out enzymolysis.
4, application as claimed in claim 1 is characterized in that described solid pipefish dispersion is a capsule formulation.
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