CN105853456A - Enteric capsule for treating prostate cancer and preparation method thereof - Google Patents
Enteric capsule for treating prostate cancer and preparation method thereof Download PDFInfo
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- CN105853456A CN105853456A CN201610256938.9A CN201610256938A CN105853456A CN 105853456 A CN105853456 A CN 105853456A CN 201610256938 A CN201610256938 A CN 201610256938A CN 105853456 A CN105853456 A CN 105853456A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
- A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/275—Nitriles; Isonitriles
- A61K31/277—Nitriles; Isonitriles having a ring, e.g. verapamil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/423—Oxazoles condensed with carbocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/74—Synthetic polymeric materials
- A61K31/785—Polymers containing nitrogen
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5073—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
Abstract
The invention discloses an enteric capsule for treating prostate cancer and a preparation method thereof. The enteric capsule is mainly prepared from the following components in parts by weight: hemslecin, anemonin, tanshinone, quercetin, bicalutamide, soy isoflavone, solasodine, eoixol, homo-orientin, uridine, tricin, flammukinan, phycocyanobilin, liquiritin and rheum emodin; the enteric capsule also comprises a diluent, a PH value modifier, a sub-coat, an enteric-coated coat, povidone K30 and hydroxypropyl methyl cellulose. The enteric capsule for treating prostate cancer prepared by the method has better anti-inflammation, analgesic and anticarcinogenic functions, a significant effect on prostate cancer through clinical verification, reliable quality, and very good clinical significance.
Description
Technical field
The present invention relates to urinary disorders practical technique field, be specifically related to a kind of enteric glue treating carcinoma of prostate
Capsule and preparation method thereof.
Background technology
Carcinoma of prostate refers to occur at prostatic epithelial malignancy, is that prostatic acini cell is abnormal unordered
The result of growth.Adenocarcinoma, duct adenocarcinoma, bladder transitional cell carcinoma, squamous cell carcinoma, glandular scale is included in histological type
Cancer.Wherein adenocarcinoma of prostate accounts for more than 95%, and therefore, generally our described carcinoma of prostate refers to prostate
Adenocarcinoma.The sickness rate of carcinoma of prostate has the most geographical and race difference.At developed countries and regions such as America and Europes,
It is the modal malignant tumor of male, and its mortality rate occupies the second of various cancer；In Asia, its sickness rate
Less than western countries, but in recent years in rapid ascendant trend.The cause of disease of carcinoma of prostate is not yet found out, may be with something lost
The many factors such as biography, environment, gonadal hormone are relevant.Prostatic secretions function is regulated by androgen testis nine ketone, rush property
The lutropin of glandular hormone plays indirect action.Carcinoma of prostate common sympton mainly has a dysuria, waist,
Pain, lymph node or the hematogenous metastasis symptoms such as sacrum portion, sciatic nerve, and day by day weak, become thin weak, enter
The General Symptoms of row, cachexia or renal failure.The morbidity of carcinoma of prostate has with sexual activity, dietary habit
Closing, the risk that the more person of sexual activity suffers from carcinoma of prostate increases, and high fat diet also has certain relation with morbidity.This
Outward, the morbidity of carcinoma of prostate is with race, regional, religions belief possibility is relevant.
Prevent and treat carcinoma of prostate clinically at present, have treatment by Chinese herbs, endocrine therapy Bisphosphonates treatment and
The methods such as immunization therapy, but utilize antitumor drug to treat carcinoma of prostate, the most just come into one's own,
This carcinoma of prostate being primarily due to about 20%～30% is independent of androgen.Chemotherapy is mainly suitable for advanced metastatic
Prostate cancer patient, after endocrine therapy or radiotherapy failure, can use chemotherapy.As auxiliary therapy
Often can play endocrine therapy and the irreplaceable effect of radiotherapy.Therefore the treatment of medicine seems the heaviest
, not only wanting can be the strongest to the inhibitory activity of prostate gland cancer cell, moreover it is possible to untoward reaction that may be present is dropped
To minimum, the misery of rapid recovery patient, the most just the medical treatment to carcinoma of prostate has significantly to enter
Step.
Summary of the invention
Present invention solves the technical problem that and be to provide a kind of enteric coated capsule treating carcinoma of prostate and preparation side thereof
Method.
The technical scheme is that a kind of enteric coated capsule treating carcinoma of prostate, described enteric coated capsule be by
Mainly it is composed of the following components in parts by weight: hemsleyadin 1-1.6 part, Anemonin 0.8-1.2 part, TANSHINONES
0.03-0.0.09 part, Quercetin 0.2-0.5 part, bicalutamide 0.01-0.03 part, soybean isoflavone 0.8-1.4 part,
Solasodine 0.08-0.12 part, Coixol 0.6-0.8 part, isorientin 0.5-0.8 part, uridine
0.04-0.06 part, tricin 0.9-1.5 part, Flammukinan 1-3 part, phycocyanobilin 0.3-0.6 part, liquiritin
0.06-0.1 part, rheum emodin 0.08-0.12 part；Described enteric coated capsule also includes: diluent 5-8 part, PH
Value regulator 0.8-2.4 part, sub-coat 3.8-5.2 part, enteric layers 2.6-4.8 part, PVP K30 2-3 part,
Hydroxypropyl methyl cellulose 0.8-1.2 part.
Further, described diluent is lactose and pregelatinized Starch mixes according to the mass ratio of 3:2:
Lactose can give human body heat supply, the synthesis enhance metabolism, organized, the microorganism of life in large intestine
Lactose can be utilized to generate organic acid, make intestinal pH value decline, these organic acid can stimulate intestinal peristalsis promoting, promotes
Effective ingredient absorbs；Pregelatinized Starch can increase mobility and compressibility, also carries lubrication.
Further, described pH value regulator refers to sodium carbonate.
Further, described sub-coat comprises mannitol, Pulvis Talci, and its weight ratio is 3:5, mannitol without
Hygroscopicity, fast drying, chemical stability is good, has good pelletize, prepares for anticarcinogen, antimicrobial drug
Filler；Talcum have lubricity, anti-glutinous, fluidizer, acid-resisting, stable chemical nature, covering power good,
The excellent Wuli-Shili-Renli system approach such as absorption affinity is strong, owing to the crystal structure of Talcum is stratiform, so having
Easily split into tending to and special slip of scale.
Further, described enteric layers is acrylic resin II, 95% ethanol, phthalic acid diethyl
Ester, polyoxyethylene sorbitan monoleate are mixed to prepare according to 50:150:2:1, and its enteric layers being mixed can be with packaging medicine
Effective ingredient so that enteric coated capsule will not be dissolved in the stomach of aobvious acidity, it is to avoid stomach is damaged by medicine,
Only in intestinal, chance akaline liquid medicine just can dissolve thus absorb performance drug effect.
The preparation method of a kind of enteric coated capsule treating carcinoma of prostate is:
(1) by the hemsleyadin of described composition by weight, Anemonin, TANSHINONES, Quercetin, bicalutamide,
Soybean isoflavone, solasodine, Coixol, isorientin, uridine, tricin, Flammukinan,
Phycocyanobilin, liquiritin, rheum emodin mechanical mixture, mixing speed 240-300r/min, stirs 30-45min, so
Rear use super micron mill is pulverized, and crosses 300-400 mesh sieve, then presses equal increments method addition diluent, sodium carbonate
Mixing, obtains hybrid medicine fine powder, standby；
(2) mass concentration 95% ethanol solution of the PVP K30 and its 3-5 times amount that take 2-3 part is prepared as
Binding agent, then the hybrid medicine fine powder (1) prepared carries out the general pill heart for powder speed 30 revs/min,
To hybrid medicine fine powder be finished time, by the prepared ball heart in drying equipment be dried, after 20 mesh sieves, obtain
Drug particles, standby；
(3) drug particles that (2) prepare is placed in coating granulator, by the hydroxypropyl first of 0.8-1.2 part
The insulating liquid that mass concentration 95% ethanol of base cellulose and its 4-6 times amount is mixed to prepare is coated, and is dried
After, it is placed in coating granulator pot, the sub-coat that the mannitol of described composition by weight, Pulvis Talci are mixed to prepare,
Being added to for, in powder machine, being coated by granulation solution, described granulation solution is by the dodecane of 1.5-2.5 part
Base sodium sulfate is slowly added to the deionized water of 3-5 times amount, agitation to forming whirlpool, continue stirring 15 minutes with
On, dispersion, until granulation solution stable chemical nature that to be all dissolved to solution limpid prepared, described, is also
A kind of well surfactant, obtains medicine coarse granule, standby；
(4) medicine coarse granule prepared by (3) is placed in coating granulator pot, regulates spray gun, carry out enteric
Layer coating, carries out vacuum drying treatment, took out 10 mesh sieves and remove bulky grain above sieve after coating, after
20 mesh sieves remove the little granule below sieve, package storage, i.e. prepare the enteric coated capsule for the treatment of carcinoma of prostate.
The invention has the beneficial effects as follows: by multiple Western medicine combination of active principles, solasodine, hemsleyadin, Semen Coicis
Element, TANSHINONES, Anemonin synergy have antiinflammatory, opposing infection, promote cellular metabolism, inhibition of pain
Effect；Soybean isoflavone, bicalutamide, Quercetin, tricin, isorientin, uridine, gold
Pin mushroom polysaccharide, phycocyanobilin, liquiritin, rheum emodin synergy can effective antioxidation, anticancer, suppress intestinal
Road shrinks, and can effectively suppress the growth of tumor, promotes protein, the synthesis of nucleic acid, it is possible to increase lymphocyte
Activity, can strengthen the immunocompetence of human body, the most comprehensively suppress the growth of prostate gland cancer cell.The present invention
The enteric coated capsule for the treatment of carcinoma of prostate has fine anti-inflammation detumescence, antitumaous effect, according to clinical verification to carcinoma of prostate
Evident in efficacy, preparation technology is simple, easy to use, it is adaptable to the popularization of clinical treatment.
Detailed description of the invention
Embodiment 1:
A kind of enteric coated capsule treating carcinoma of prostate, described enteric coated capsule is by the one-tenth of following weight portion by main
It is grouped into: hemsleyadin 1 part, Anemonin 0.8 part, TANSHINONES 0.03 part, Quercetin 0.2 part, ratio card Shandong
Amine 0.01 part, soybean isoflavone 0.8 part, solasodine 0.08 part, Coixol 0.6 part, isorientin 0.5
Part, uridine 0.04 part, tricin 0.9 part, Flammukinan 1 part, phycocyanobilin 0.3 part, Radix Glycyrrhizae
Glycoside 0.06 part, rheum emodin 0.08 part；Described enteric coated capsule also includes: diluent 5 parts, pH value regulator
0.8 part, sub-coat 3.8 parts, enteric layers 2.6 parts, PVP K30 2 parts, hydroxypropyl methyl cellulose 0.8
Part.
Wherein, described diluent is lactose and pregelatinized Starch mixes according to the mass ratio of 3:2: breast
Sugar can give human body heat supply, the synthesis enhance metabolism, organized, the microbes of life in large intestine
Utilizing lactose to generate organic acid, make intestinal pH value decline, these organic acid can stimulate intestinal peristalsis promoting, promotes medicine
Thing effective ingredient absorbs；Pregelatinized Starch can increase mobility and compressibility, also carries lubrication.Described
PH value regulator refers to sodium carbonate.Described sub-coat comprises mannitol, Pulvis Talci, and its weight ratio is 3:5,
Mannitol no hygroscopicity, fast drying, chemical stability is good, has good pelletize, for anticarcinogen, resists
Filler prepared by bacterium medicine；Talcum has lubricity, anti-glutinous, fluidizer, acid-resisting, stable chemical nature, screening
The excellent Wuli-Shili-Renli system approach such as lid power is good, absorption affinity is strong, owing to the crystal structure of Talcum is stratiform,
Tending to and special slip of scale is easily split into so having.Described enteric layers is acrylic resin II
Number, 95% ethanol, diethyl phthalate, polyoxyethylene sorbitan monoleate be mixed to prepare according to 50:150:2:1, its
The enteric layers being mixed can be with the effective ingredient of packaging medicine so that enteric coated capsule will not be in the stomach of aobvious acidity
Being dissolved, it is to avoid stomach is damaged by medicine, only in intestinal, chance akaline liquid medicine just can dissolve thus inhale
Drug effect is waved in transmitting-receiving.
The preparation method of a kind of enteric coated capsule treating carcinoma of prostate is:
(1) by the hemsleyadin of described composition by weight, Anemonin, TANSHINONES, Quercetin, bicalutamide,
Soybean isoflavone, solasodine, Coixol, isorientin, uridine, tricin, Flammukinan,
Phycocyanobilin, liquiritin, rheum emodin mechanical mixture, mixing speed 240r/min, stirs 30min, then uses
Super micron mill is pulverized, and crosses 300 mesh sieves, then presses equal increments method addition diluent, sodium carbonate mixing, obtains
Hybrid medicine fine powder, standby；
(2) take the PVP K30 of 2 parts and be prepared as bonding with mass concentration 95% ethanol solution of its 3 times amount
Agent, then the hybrid medicine fine powder (1) prepared carries out the general pill heart for powder speed 30 revs/min, to mixed
When composite medicine fine powder is finished, the prepared ball heart is dried in drying equipment, after 20 mesh sieves, obtains medicine
Granule, standby；
(3) drug particles that (2) prepare is placed in coating granulator, fine with the hydroxypropyl methyl of 0.8 part
The insulating liquid that plain mass concentration 95% ethanol with its 4 times amount of dimension is mixed to prepare is coated, and after drying, puts
In coating granulator pot, the sub-coat that the mannitol of described composition by weight, Pulvis Talci are mixed to prepare, it is added to
For, in powder machine, being coated by granulation solution, described granulation solution is by the sodium lauryl sulphate of 1.5 parts
Being slowly added to the deionized water of 3 times amount, agitation, to forming whirlpool, continues stirring more than 15 minutes, and dispersion is straight
Limpid prepared to being all dissolved to solution, described granulation solution stable chemical nature, is also a kind of good
Surfactant, obtains medicine coarse granule, standby；
(4) medicine coarse granule prepared by (3) is placed in coating granulator pot, regulates spray gun, carry out enteric
Layer coating, carries out vacuum drying treatment, took out 10 mesh sieves and remove bulky grain above sieve after coating, after
20 mesh sieves remove the little granule below sieve, package storage, i.e. prepare the enteric coated capsule for the treatment of carcinoma of prostate.
Embodiment 2:
A kind of enteric coated capsule treating carcinoma of prostate, described enteric coated capsule is by the one-tenth of following weight portion by main
It is grouped into: hemsleyadin 1.3 parts, Anemonin 1 part, TANSHINONES 0.06 part, Quercetin 0.35 part, ratio card
Shandong amine 0.02 part, soybean isoflavone 1.1 parts, solasodine 0.1 part, Coixol 0.7 part, isorientin 0.65
Part, uridine 0.05 part, tricin 1.2 parts, Flammukinan 2 parts, phycocyanobilin 0.45 part, sweet
Grass glycoside 0.08 part, rheum emodin 0.1 part；Described enteric coated capsule also includes: diluent 6.5 parts, pH value are adjusted
Joint agent 1.6 parts, sub-coat 4.5 parts, enteric layers 3.7 parts, PVP K30 2.5 parts, hydroxypropyl methyl fiber
Element 1 part.
Wherein, described diluent is lactose and pregelatinized Starch mixes according to the mass ratio of 3:2: breast
Sugar can give human body heat supply, the synthesis enhance metabolism, organized, the microbes of life in large intestine
Utilizing lactose to generate organic acid, make intestinal pH value decline, these organic acid can stimulate intestinal peristalsis promoting, promotes medicine
Thing effective ingredient absorbs；Pregelatinized Starch can increase mobility and compressibility, also carries lubrication.Described
PH value regulator refers to sodium carbonate.Described sub-coat comprises mannitol, Pulvis Talci, and its weight ratio is 3:5,
Mannitol no hygroscopicity, fast drying, chemical stability is good, has good pelletize, for anticarcinogen, resists
Filler prepared by bacterium medicine；Talcum has lubricity, anti-glutinous, fluidizer, acid-resisting, stable chemical nature, screening
The excellent Wuli-Shili-Renli system approach such as lid power is good, absorption affinity is strong, owing to the crystal structure of Talcum is stratiform,
Tending to and special slip of scale is easily split into so having.Described enteric layers is acrylic resin II
Number, 95% ethanol, diethyl phthalate, polyoxyethylene sorbitan monoleate be mixed to prepare according to 50:150:2:1, its
The enteric layers being mixed can be with the effective ingredient of packaging medicine so that enteric coated capsule will not be in the stomach of aobvious acidity
Being dissolved, it is to avoid stomach is damaged by medicine, only in intestinal, chance akaline liquid medicine just can dissolve thus inhale
Drug effect is waved in transmitting-receiving.
The preparation method of a kind of enteric coated capsule treating carcinoma of prostate is:
(1) by the hemsleyadin of described composition by weight, Anemonin, TANSHINONES, Quercetin, bicalutamide,
Soybean isoflavone, solasodine, Coixol, isorientin, uridine, tricin, Flammukinan,
Phycocyanobilin, liquiritin, rheum emodin mechanical mixture, mixing speed 270r/min, stirs 37.5min, then makes
Pulverize with super micron mill, cross 350 mesh sieves, then press equal increments method addition diluent, sodium carbonate mixing,
To hybrid medicine fine powder, standby；
(2) take the PVP K30 of 2.5 parts to be prepared as gluing with mass concentration 95% ethanol solution of its 4 times amount
Mixture, then the hybrid medicine fine powder (1) prepared carries out the general pill heart for powder speed 30 revs/min, extremely
When hybrid medicine fine powder is finished, the prepared ball heart is dried in drying equipment, after 20 mesh sieves, obtains medicine
Composition granule, standby；
(3) drug particles that (2) prepare is placed in coating granulator, with the hydroxypropyl methyl fiber of 1 part
The insulating liquid that plain mass concentration 95% ethanol with its 5 times amount is mixed to prepare is coated, and after drying, is placed in
In coating granulator pot, the sub-coat that the mannitol of described composition by weight, Pulvis Talci are mixed to prepare, it is added to supply
In powder machine, being coated by granulation solution, described granulation solution is by slow for the sodium lauryl sulphate of 2 parts
Adding the deionized water of 4 times amount, agitation, to forming whirlpool, continues stirring more than 15 minutes, and dispersion is until complete
It is limpid prepared that portion is dissolved to solution, described granulation solution stable chemical nature, is also a kind of well surface
Activating agent, obtains medicine coarse granule, standby；
(4) medicine coarse granule prepared by (3) is placed in coating granulator pot, regulates spray gun, carry out enteric
Layer coating, carries out vacuum drying treatment, took out 10 mesh sieves and remove bulky grain above sieve after coating, after
20 mesh sieves remove the little granule below sieve, package storage, i.e. prepare the enteric coated capsule for the treatment of carcinoma of prostate.
Embodiment 3:
A kind of enteric coated capsule treating carcinoma of prostate, described enteric coated capsule is by the one-tenth of following weight portion by main
It is grouped into: hemsleyadin 1.6 parts, Anemonin 1.2 parts, TANSHINONES 0.0.09 part, Quercetin 0.5 part, ratio
Card Shandong amine 0.03 part, soybean isoflavone 1.4 parts, solasodine 0.12 part, Coixol 0.8 part, isorientin
0.8 part, uridine 0.06 part, tricin 1.5 parts, Flammukinan 3 parts, phycocyanobilin 0.6 part,
Liquiritin 0.1 part, rheum emodin 0.12 part；Described enteric coated capsule also includes: diluent 8 parts, pH value are adjusted
Joint agent 2.4 parts, sub-coat 5.2 parts, enteric layers 4.8 parts, PVP K30 3 parts, hydroxypropyl methyl fiber
Element 1.2 parts.
Wherein, described diluent is lactose and pregelatinized Starch mixes according to the mass ratio of 3:2: breast
Sugar can give human body heat supply, the synthesis enhance metabolism, organized, the microbes of life in large intestine
Utilizing lactose to generate organic acid, make intestinal pH value decline, these organic acid can stimulate intestinal peristalsis promoting, promotes medicine
Thing effective ingredient absorbs；Pregelatinized Starch can increase mobility and compressibility, also carries lubrication.Described
PH value regulator refers to sodium carbonate.Described sub-coat comprises mannitol, Pulvis Talci, and its weight ratio is 3:5,
Mannitol no hygroscopicity, fast drying, chemical stability is good, has good pelletize, for anticarcinogen, resists
Filler prepared by bacterium medicine；Talcum has lubricity, anti-glutinous, fluidizer, acid-resisting, stable chemical nature, screening
The excellent Wuli-Shili-Renli system approach such as lid power is good, absorption affinity is strong, owing to the crystal structure of Talcum is stratiform,
Tending to and special slip of scale is easily split into so having.Described enteric layers is acrylic resin II
Number, 95% ethanol, diethyl phthalate, polyoxyethylene sorbitan monoleate be mixed to prepare according to 50:150:2:1, its
The enteric layers being mixed can be with the effective ingredient of packaging medicine so that enteric coated capsule will not be in the stomach of aobvious acidity
Being dissolved, it is to avoid stomach is damaged by medicine, only in intestinal, chance akaline liquid medicine just can dissolve thus inhale
Drug effect is waved in transmitting-receiving.
The preparation method of a kind of enteric coated capsule treating carcinoma of prostate is:
(1) by the hemsleyadin of described composition by weight, Anemonin, TANSHINONES, Quercetin, bicalutamide,
Soybean isoflavone, solasodine, Coixol, isorientin, uridine, tricin, Flammukinan,
Phycocyanobilin, liquiritin, rheum emodin mechanical mixture, mixing speed 300r/min, stirs 45min, then uses
Super micron mill is pulverized, and crosses 400 mesh sieves, then presses equal increments method addition diluent, sodium carbonate mixing, obtains
Hybrid medicine fine powder, standby；
(2) take the PVP K30 of 3 parts and be prepared as bonding with mass concentration 95% ethanol solution of its 5 times amount
Agent, then the hybrid medicine fine powder (1) prepared carries out the general pill heart for powder speed 30 revs/min, to mixed
When composite medicine fine powder is finished, the prepared ball heart is dried in drying equipment, after 20 mesh sieves, obtains medicine
Granule, standby；
(3) drug particles that (2) prepare is placed in coating granulator, fine with the hydroxypropyl methyls of 1.2 parts
The insulating liquid that plain mass concentration 95% ethanol with its 6 times amount of dimension is mixed to prepare is coated, and after drying, puts
In coating granulator pot, the sub-coat that the mannitol of described composition by weight, Pulvis Talci are mixed to prepare, it is added to
For, in powder machine, being coated by granulation solution, described granulation solution is by the sodium lauryl sulphate of 2.5 parts
Being slowly added to the deionized water of 5 times amount, agitation, to forming whirlpool, continues stirring more than 15 minutes, and dispersion is straight
Limpid prepared to being all dissolved to solution, described granulation solution stable chemical nature, is also a kind of good
Surfactant, obtains medicine coarse granule, standby；
(4) medicine coarse granule prepared by (3) is placed in coating granulator pot, regulates spray gun, carry out enteric
Layer coating, carries out vacuum drying treatment, took out 10 mesh sieves and remove bulky grain above sieve after coating, after
20 mesh sieves remove the little granule below sieve, package storage, i.e. prepare the enteric coated capsule for the treatment of carcinoma of prostate.
Application in enteric coated capsule of the present invention row adenocarcinoma before the treatment:
One, the interior curative effect research of carcinoma of prostate
1. medicament selection:
Intestinal prepared by enteric coated capsule prepared by the enteric coated capsule embodiment 1 prepared, embodiment 2, embodiment 3
Colloidal sol capsule grinds to form fine powder respectively, mixes with the pure water of 5-8 times amount, standby.
2. test method:
Take male mice 60, body weight 130-150g, to nude mouse subcutaneous vaccination human prostata cancer PC-3,
DU145 or LNCAP cell, after tumor growth to 100-300mm3, is randomly divided into three groups by animal,
Often group 20.Take embodiment 1, embodiment 2, the enteric coated capsule of embodiment 3 preparation respectively to often group mice
Aqueous solution, according to 10ml/kg, takes twice every day, takes continuously 4 weeks, surveys weekly 2-3 tumor volume,
Claim Mus weight, record data.Gross tumor volume (V) computing formula is: V=1/2 × a × b2 wherein a, b table respectively
Show major diameter, wide footpath.
3. result of the test:
| Take medicine group | Take medicine pre-neoplastic average external volume | Tumor average volume after taking medicine | Untoward reaction | Death toll |
| Embodiment 1 | 186(mm3) | 36(mm3) | 1 | 0 |
| Embodiment 2 | 223(mm3) | 23(mm3) | 0 | 0 |
| Embodiment 3 | 208(mm3) | 28(mm3) | 0 | 0 |
4. conclusion:
There is vomiting phenomenon in 1 mice of the enteric coated capsule only taking embodiment 1 preparation in process of the test,
Other mices all do not occur that the phenomena of mortality do not occur in any untoward reaction, all mices, by the result of the test in 3
In take medicine before and after gross tumor volume compare the enteric coated capsule of the treatment carcinoma of prostate that can be seen that the present invention to prostatitis
Gland malignant tumor has good inhibition.
Two, the enteric coated capsule of the present invention clinical trial to carcinoma of prostate
1. clinical data: choosing patients with prostate cancer 200 example made a definite diagnosis, in age 38-76 year, all cases is equal
Through imaging diagnosis, and turn out to be carcinoma of prostate through carcinoma of prostate biopsy, while carrying out chemotherapy, make medication
Thing is treated.Be divided into four groups, three groups for the treatment of groups, one group of matched group, often organize 50 examples, often organize patient the state of an illness,
Age, sign show without significant difference, have comparability.
2. experimental drug: use the embodiment of the present invention 1, reality to treatment group 1, treatment group 2, treatment group 3 respectively
Execute example 2, embodiment 3 preparation enteric coated capsule, each 10mg, daily 2 times；To matched group patient
Using capecitabine, by specification is normally taken.
3. criterion:
(1) effective: cardinal symptom (lower urinary tract symptom) and sign major part disappear, lower urinary tract symptom integration
Reduction ratio >=60%；Qmax ＞ 15ml/s, serum PSA value ＜ 4ng/ml；
(2) effective: cardinal symptom (lower urinary tract symptom) and sign major part disappear, lower urinary tract symptom integration
Reduction ratio >=30%；Qmax≤15ml/s and ＞ 10ml, serum PSA value >=4ng/ml and ＜ 10ng/ml；
(3) invalid: cardinal symptom (lower urinary tract symptom) and sign major part disappear, lower urinary tract symptom integration
Reduction ratio ＜ 15%；Qmax and serum PSA value are without improving.
4. experimental result:
| Group | Often organize case load | Effective | Effectively | Invalid | Untoward reaction | Effective percentage |
| Treatment group 1 | 50 | 36 | 11 | 3 | 0 | 94.0% |
| Treatment group 2 | 50 | 42 | 8 | 0 | 0 | 100.0% |
| Treatment group 3 | 50 | 29 | 20 | 1 | 0 | 98.0% |
| Matched group | 50 | 18 | 19 | 9 | 4 | 74.0% |
5. conclusion: as seen from the above table, the enteric coated capsule for the treatment of carcinoma of prostate prepared by the present invention is to carcinoma of prostate
Total effective rate is 94.0%, and has no any untoward reaction, and therapeutic effect is substantially better than current common drug, tool
There is good clinical expansion meaning.
Although the present invention being described and illustrated with reference to its specific embodiments, but those skilled in the art will appreciate that
Arrive, without departing from the spirit and scope of the present invention it can be variously modified, revise and replace.
Such as, due to the change of responding ability of the people of treated particular condition, beyond preferred dose as explained above
Effective dose may be suitable for.Similarly, it was observed that pharmacology respond may basis and rely on selected given activity
Compound or whether there is pharmaceutical carrier and preparation type and mode of administration used and become, according to the mesh of the present invention
And practice be contemplated in result this kind of expection change or difference.Therefore, the invention is intended to only by following patent
The scope required limits and these claim should be explained in rational degree as broadly as possible.
Claims (6)
1. the enteric coated capsule treating carcinoma of prostate, it is characterised in that described enteric coated capsule is by mainly
It is composed of the following components in parts by weight: hemsleyadin 1-1.6 part, Anemonin 0.8-1.2 part, TANSHINONES
0.03-0.0.09 part, Quercetin 0.2-0.5 part, bicalutamide 0.01-0.03 part, soybean isoflavone 0.8-1.4 part,
Solasodine 0.08-0.12 part, Coixol 0.6-0.8 part, isorientin 0.5-0.8 part, uridine
0.04-0.06 part, tricin 0.9-1.5 part, Flammukinan 1-3 part, phycocyanobilin 0.3-0.6 part, liquiritin
0.06-0.1 part, rheum emodin 0.08-0.12 part；Described enteric coated capsule also includes: diluent 5-8 part, PH
Value regulator 0.8-2.4 part, sub-coat 3.8-5.2 part, enteric layers 2.6-4.8 part, PVP K30 2-3 part,
Hydroxypropyl methyl cellulose 0.8-1.2 part.
A kind of enteric coated capsule treating carcinoma of prostate, it is characterised in that described
Diluent be lactose and pregelatinized Starch mixes according to the mass ratio of 3:2.
A kind of enteric coated capsule treating carcinoma of prostate, it is characterised in that described
PH value regulator refer to sodium carbonate.
A kind of enteric coated capsule treating carcinoma of prostate, it is characterised in that described
Sub-coat comprise mannitol, Pulvis Talci, its weight ratio is 3:5.
A kind of enteric coated capsule treating carcinoma of prostate, it is characterised in that described
Enteric layers be acrylic resin II, 95% ethanol, diethyl phthalate, polyoxyethylene sorbitan monoleate according to
50:150:2:1 is mixed to prepare.
A kind of enteric coated capsule treating carcinoma of prostate, it is characterised in that preparation side
Method is:
(1) by the hemsleyadin of described composition by weight, Anemonin, TANSHINONES, Quercetin, bicalutamide,
Soybean isoflavone, solasodine, Coixol, isorientin, uridine, tricin, Flammukinan,
Phycocyanobilin, liquiritin, rheum emodin mechanical mixture, then use super micron mill to pulverize, cross 300-400 mesh sieve,
Press equal increments method again and add diluent, sodium carbonate mixing, obtain hybrid medicine fine powder, standby；
(2) mass concentration 95% ethanol solution of the PVP K30 and its 3-5 times amount that take 2-3 part is prepared as
Binding agent, then the hybrid medicine fine powder (1) prepared carries out the general pill heart for powder speed 30 revs/min,
To hybrid medicine fine powder be finished time, by the prepared ball heart in drying equipment be dried, after 20 mesh sieves, obtain
Drug particles, standby；
(3) drug particles that (2) prepare is placed in coating granulator, by the hydroxypropyl first of 0.8-1.2 part
The insulating liquid that mass concentration 95% ethanol of base cellulose and its 4-6 times amount is mixed to prepare is coated, and is dried
After, it is placed in coating granulator pot, the sub-coat that the mannitol of described composition by weight, Pulvis Talci are mixed to prepare,
It is added to for, in powder machine, being coated by granulation solution, obtain medicine coarse granule, standby；
(4) medicine coarse granule prepared by (3) is placed in coating granulator pot, regulates spray gun, carry out enteric
Layer coating, carries out vacuum drying treatment, took out 10 mesh sieves and remove bulky grain above sieve after coating, after
20 mesh sieves remove the little granule below sieve, package storage, i.e. prepare the enteric coated capsule for the treatment of carcinoma of prostate.
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101559110A (en) * | 2008-04-14 | 2009-10-21 | 张宏桂 | Anti-tumor medicine anemonin as well as preparation method and application of composition thereof |
| CN102040578A (en) * | 2010-12-27 | 2011-05-04 | 国际竹藤网络中心 | Method for preparing high purity tricin from bamboo leaves |
| CN103327994A (en) * | 2010-11-04 | 2013-09-25 | 盖尼奥斯生物医学国际公司 | Combination therapy for prostate cancer using botanical compositions and bicalutamide |
| CN104473949A (en) * | 2014-11-11 | 2015-04-01 | 济南星懿医药技术有限公司 | Pharmaceutical composition used for treating liver cancer |
-
2016
- 2016-04-21 CN CN201610256938.9A patent/CN105853456A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101559110A (en) * | 2008-04-14 | 2009-10-21 | 张宏桂 | Anti-tumor medicine anemonin as well as preparation method and application of composition thereof |
| CN103327994A (en) * | 2010-11-04 | 2013-09-25 | 盖尼奥斯生物医学国际公司 | Combination therapy for prostate cancer using botanical compositions and bicalutamide |
| CN102040578A (en) * | 2010-12-27 | 2011-05-04 | 国际竹藤网络中心 | Method for preparing high purity tricin from bamboo leaves |
| CN104473949A (en) * | 2014-11-11 | 2015-04-01 | 济南星懿医药技术有限公司 | Pharmaceutical composition used for treating liver cancer |
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