CN106075387A - A kind of oral formulations treating chronic leukemia and preparation method thereof - Google Patents
A kind of oral formulations treating chronic leukemia and preparation method thereof Download PDFInfo
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- CN106075387A CN106075387A CN201610479417.XA CN201610479417A CN106075387A CN 106075387 A CN106075387 A CN 106075387A CN 201610479417 A CN201610479417 A CN 201610479417A CN 106075387 A CN106075387 A CN 106075387A
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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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
- A61K31/01—Hydrocarbons
- A61K31/015—Hydrocarbons carbocyclic
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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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
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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
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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
- A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
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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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/02—Peptides of undefined number of amino acids; Derivatives thereof
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
Abstract
The invention discloses a kind of oral formulations treating chronic leukemia and preparation method thereof, described oral formulations includes following component: gefitinib, maytanprine, tanshinone IIA, phycocyanobilin, zaluzanin C, ursolic acid, P-coumaric acid, oleanolic acid, succinic acid, α carotene, protein peptide, caffeic acid, stachyose, disintegrating agent, binding agent, lubricant, surfactant, cosurfactant.The present invention is by multi-medicament effective ingredient reasonable combination, the water solublity having had in human body fluid, there is good anti-tumor activity simultaneously, people's chronic leukemia granulocyte is had the strongest inhibitory action, the fever and headache that chronic leukemia is caused, limbs are weak, inappetence, difference of sleeping cardiopalmus, resistance is poor, and the symptom such as easily catch a cold has good therapeutic effect.
Description
Technical field
The present invention relates to hematologic disease practical technique field, be specifically related to a kind of oral formulations treating chronic leukemia and
Its preparation method.
Background technology
Leukemia is commonly called as leukemia, is a class hematopoietic stem cell malignant clone disease.Clonal leukaemia is because increasing
Grow out of control, dysdifferentiation, apoptosis are obstructed etc., and mechanism breeds accumulation in bone marrow and other hemopoietic tissue in a large number, and infiltrates other groups
Knitting and organ, normal hematopoiesis function is suppressed simultaneously.Leukemic pathogenesis is fully apparent from by the mankind not yet so far, can
Can infect with virus, ionizing radiation, chemical factor, inherited genetic factors etc. relevant, common chronic leukemia is broadly divided into chronic marrow
Cell leukemia and chronic lymphocytic leukemia, be called for short slow grain, be clinically a kind of onset and develop relatively slow in vain
Disorders of blood, primary pathogenic event is owing to the malignant proliferation of bone marrow pluripotential hemopoietic stem cell causes, and shows as Meloid progenitor pond and expands
Exhibition, myelocytic series and CFU-GM undue growth thereof, patient clinical symptom shows as more can be had fatigue and weakness in early days, engender head
Dizzy, shortness of breath and palpitation, to become thin, low grade fever, night sweat, skin purpura, skin pruritus, skeletal pain, normal easy infection, about 10% patient can be concurrent
Autoimmune hemolytic anemia.Vital sign shows themselves in that lymphadenectasis is most common with cervical lymph node enlargement, next to that axil
Nest, groin and coaster lymphadenectasis, be typically medium hardness, smooth surface, and without tenderness, epidermis is without redness, without adhesion, as
Mediastinal lymph node enlargement, compressing bronchus causes cough, hoarseness or breathing because of difficulty；Liver silght enlargement, splenomegaly accounts for
72%, typically under rib 3～4crn, few patients can flat umbilicus, enlargement is obvious not as good as chronic myelocytic leukemia in degree；May occur in which
Pachyderma, tuberosity, so that general erythroderma etc.；Simultaneously with fever and headache, limbs are weak, inappetence, difference of the sleeping heart
Throbbing with fear, resistance is poor, easily catches a cold.
This sick sickness rate is in rising trend at present, severely compromises the healthy of people until life, and common controls
Treatment method has Chinese traditional treatment, chemotherapy, radiotherapy, operation and bone marrow depression etc., wherein chemotherapy, radiotherapy, operation and bone marrow
Suppression, injures patient greatly, and side effect is big, costly.Therefore considering Drug therapy is a kind of actual treatment side
Method, not only has the effect of anti-cancer and detumescence, anti-inflammation, moreover it is possible to can also promote that patient is fast while improving human body immunocompetence
Quick-recovery, is suitable for long-term taking and side effect is little.
Summary of the invention
Present invention solves the technical problem that and be to provide a kind of oral formulations treating chronic leukemia and preparation method thereof.
For solving above-mentioned technical problem, the technical solution adopted in the present invention is as follows:
A kind of oral formulations treating chronic leukemia, described oral formulations mainly includes the composition of following weight portion:
Gefitinib 6～12 parts, maytanprine 5～10 parts, tanshinone IIA 5～8 parts, phycocyanobilin 3～6 parts, zaluzanin C 3～5
Part, ursolic acid 8～15 parts, P-coumaric acid 10～14 parts, oleanolic acid 6～10 parts, succinic acid 3～8 parts, alpha-carotene 2～5
Part, vitamin D2 1～3 parts, protein peptide 30～50 parts, caffeic acid 3～5 parts, stachyose 6～8 parts, disintegrating agent 6.5～9.5 parts,
Binding agent 80～120 parts, lubricant 5～8 parts, surfactant 1～2 parts, cosurfactant 0.5～0.8 part.
Further, described disintegrating agent is crospolyvinylpyrrolidone, is that a kind of white has hygroscopicity and easily flows
Powder, there is the strongest expansion character and the complexing power with multiclass material, be primarily due to it and there is high capillary activity,
Thus can promptly water be absorbed in tablet, when swelling pressure has exceeded the intensity of medicine, compile and make medicine moment disintegrate, and
And the most swelling in water do not have full-bodied gel layer, thus its disintegrating property is the most superior, and medicine can be made at stomach
Intestinal juice splits rapidly the material being broken into fine particle, so that the rapid solution absorption of functional component, plays a role.
Further, described binding agent is the ethyl cellulose of pharmaceutical grade, and its Heat stability is good has excellent alkali resistance
With weak acid resistant, long term storage is never degenerated, and has good compatibility with all of plasticizer, is a kind of well medicine bonding
Agent.
Further, described lubricant is gel aluminum hydroxide, the most good lubricant effect, also have antiacid and
The protective effects on gastric mucosa, can effectively reduce the dripping of irritant drugs damage to gastric mucosa.
Further, described surfactant is levan, and it has the best amphipathic property, is the best
Surfactant, be transfructosylase catalysis the water solublity being formed by connecting with one or more fructose molecules by sucrose and
The macromolecule polysaccharide of stickiness, has different physiological roles and biological activity.
Further, described cosurfactant is sorbitol, can change the surface activity of surfactant and hydrophilic
Lipophile balanced, participate in forming micelle, adjust water and the polarity of oil, thus preferably strengthen the surface activity of compound.
Further, described protein peptide refers to a kind of full-natural nutritive material extracted from Semen sojae atricolor, is also that human body is thin
The important component part of born of the same parents, comprises the aminoacid of multiple needed by human body, and vital movement plays extremely important effect, human body
There is a protein peptide operating system in digestive system, small-molecular peptides directly can be absorbed by intestinal, is rapidly introduced in blood, quilt
Being transported to the position that needed by human body is wanted, peptide molecule can continue to keep biological activity after entering human body, directly participates in and regulation human body
Important vital movement, therefore soybean protein peptide is when human-body fatigue, weakness, immune system are destroyed, and effect is especially apparent.
At antithrombus formation, elimination human-body fatigue, the liver protecting, prevent arteriosclerosis, enhancing human body physical agility and muscle strength, enhancing people
The aspects such as body immunity all have obvious action, can strengthen the combination effect between ingredient.
The preparation method of a kind of oral formulations treating chronic leukemia is:
Step one: by the binding agent of described composition by weight and mass concentration be 55～75% ethanol according to the weight of 1:3～5
Amount than mix homogeneously and is fully dissolved, and binding agent ethyl cellulose is slowly added into the container filling solvent under stirring
In, until complete wetting is dissolved, make binder solution, standby,；
Step 2: by the gefitinib of described composition by weight, maytanprine, tanshinone IIA, phycocyanobilin, zaluzanin C,
Ursolic acid, P-coumaric acid, oleanolic acid, succinic acid, alpha-carotene, vitamin D2, protein peptide, caffeic acid, several amino acids,
Stachyose mechanical mixture uniformly after, multi-angle rolling while stirring, make can not the medicine densification distribution of composition, ground system
Become fine powder, cross 300 mesh sieves, prepare hybrid medicine fine powder, standby；
Step 3: first binder solution prepared by step one is placed on blender and at the uniform velocity stirs, mixing speed
180r/min, then hybrid medicine fine powder step 2 prepared is slowly added to, and prepares hybrid medicine, then it is dense to be reduced pressure by hybrid medicine
Retract and receive ethanol, prepare hybrid medicine extractum, add the disintegrating agent of described composition by weight, lubricant, surfactant, help table
Face activating agent, seals up for safekeeping after low temperature sterilization, i.e. prepares a kind of oral formulations treating chronic leukemia of the present invention.
Further, described oral formulations makes granule, tablet, capsule according to common process, according to different
Preparation process adds corresponding adjuvant.
Compared with prior art, beneficial effects of the present invention is embodied in: by multi-medicament effective ingredient rational proportion, Ji Fei
For Buddhist nun, maytanprine, tanshinone IIA, phycocyanobilin, zaluzanin C synergy opposing tumor promotion, reduce blood viscosity, anticoagulant
And thrombolytic, reduce capillary permeability, reduce inflammatory exudation, prevent inflammatory from spreading, improve blood circulation and Weaving Cycle, right
People's chronic leukemia granulocyte has the strongest inhibitory action；Ursolic acid, P-coumaric acid, oleanolic acid, succinic acid, α-Radix Dauci Sativae
Element, protein peptide, caffeic acid, stachyose synergy supplement the material needed for human body, improve the various lifes caused due to cancerous cell
Reason exponential anomaly, strengthens humoral immunization and cellular immune function, inducement interferon and endocrinal environment is had good harmony,
Reducing the dripping of irritant drugs toxic and side effects to human body, the fever and headache causing chronic leukemia, limbs are weak, inappetence,
Difference of sleeping cardiopalmus, resistance is poor, and the symptom such as easily catch a cold has good therapeutic effect.
Detailed description of the invention
Embodiment 1: a kind of oral formulations treating chronic leukemia, described oral formulations mainly includes following weight portion
Composition: gefitinib 6 parts, maytanprine 5 parts, tanshinone IIA 5 parts, phycocyanobilin 3 parts, zaluzanin C 3 parts, ursolic acid 8
Part, P-coumaric acid 10 parts, oleanolic acid 6 parts, succinic acid 3 parts, alpha-carotene 2 parts, vitamin D2 1 part, protein peptide 30 parts, coffee
Coffee acid 3 parts, 6 parts of stachyose, disintegrating agent 6.5 parts, binding agent 80 parts, lubricant 5 parts, 1 part of surfactant, cosurfactant
0.5 part.
Wherein, described disintegrating agent is crospolyvinylpyrrolidone, is that a kind of white has the runny powder of hygroscopicity
End, has the strongest expansion character and the complexing power with multiclass material, is primarily due to it and has high capillary activity, thus
Can promptly water be absorbed in tablet, when swelling pressure has exceeded the intensity of medicine, compile and make medicine moment disintegrate, and
The most swelling in water do not have full-bodied gel layer, thus its disintegrating property is the most superior, and medicine can be made at gastro-intestinal Fluid
In split rapidly the material being broken into fine particle so that the rapid solution absorption of functional component, play a role.Described binding agent is
The ethyl cellulose of pharmaceutical grade, its Heat stability is good, there are excellent alkali resistance and weak acid resistant, long term storage is never degenerated, with institute
Some plasticizers have good compatibility, are a kind of well medicine binding agents.Described lubricant is gel aluminum hydroxide, no
Only have good lubricant effect, also there is antiacid and the protective effects on gastric mucosa, can effectively reduce dripping of irritant drugs and stomach is glued
The damage of film.Described surfactant is levan, and it has the best amphipathic property, is to live in extraordinary surface
Property agent, be transfructosylase catalysis the water solublity being formed by connecting with one or more fructose molecules by sucrose and the height of stickiness
Molecular polysaccharide, has different physiological roles and biological activity.Described cosurfactant is sorbitol, can change surface activity
The surface activity of agent and hydrophile-lipophile balance, participate in forming micelle, adjusts water and the polarity of oil, thus preferably strengthens chemical combination
The surface activity of thing.Described protein peptide refers to a kind of full-natural nutritive material extracted from Semen sojae atricolor, is also human body cell
Important component part, comprises the aminoacid of multiple needed by human body, and vital movement plays extremely important effect, human consumption
There is a protein peptide operating system in system, small-molecular peptides directly can be absorbed by intestinal, is rapidly introduced in blood, is carried
The position wanted to needed by human body, peptide molecule can continue to keep biological activity after entering human body, directly participate in and regulation body weight for humans is wanted
Vital movement, therefore soybean protein peptide is when human-body fatigue, weakness, immune system are destroyed, and effect is especially apparent.Anti-
Thrombosis, eliminate human-body fatigue, the liver protecting, prevent arteriosclerosis, strengthen human body physical agility and muscle strength, enhancing human body and exempt from
The aspects such as epidemic disease power all have obvious action, can strengthen the combination effect between ingredient.
The preparation method of a kind of oral formulations treating chronic leukemia is:
Step one: the binding agent of described composition by weight is mixed according to the weight ratio of 1:3 with the ethanol that mass concentration is 55%
Closing and uniformly and fully dissolve, binding agent ethyl cellulose is slowly added into the container filling solvent under stirring, until
Till complete wetting is dissolved, make binder solution, standby,；
Step 2: by the gefitinib of described composition by weight, maytanprine, tanshinone IIA, phycocyanobilin, zaluzanin C,
Ursolic acid, P-coumaric acid, oleanolic acid, succinic acid, alpha-carotene, vitamin D2, protein peptide, caffeic acid, several amino acids,
Stachyose mechanical mixture uniformly after, multi-angle rolling while stirring, make can not the medicine densification distribution of composition, ground system
Become fine powder, cross 300 mesh sieves, prepare hybrid medicine fine powder, standby；
Step 3: first binder solution prepared by step one is placed on blender and at the uniform velocity stirs, mixing speed
180r/min, then hybrid medicine fine powder step 2 prepared is slowly added to, and prepares hybrid medicine, then it is dense to be reduced pressure by hybrid medicine
Retract and receive ethanol, prepare hybrid medicine extractum, add the disintegrating agent of described composition by weight, lubricant, surfactant, help table
Face activating agent, seals up for safekeeping after low temperature sterilization, i.e. prepares a kind of oral formulations treating chronic leukemia of the present invention；
Step 4: add sweeting agent 18 parts in the oral formulations for the treatment of chronic leukemia step 3 prepared, according still further to
Pelletize, be dried, oral granular formulation is made in granulate, sterilizing, the technological process such as subpackage.
Embodiment 2: a kind of oral formulations treating chronic leukemia, described oral formulations mainly includes following weight portion
Composition: gefitinib 9 parts, maytanprine 7.5 parts, tanshinone IIA 6.5 parts, phycocyanobilin 4.5 parts, zaluzanin C 4 parts, Bears
Fruit acid 11.5 parts, P-coumaric acid 12 parts, oleanolic acid 8 parts, succinic acid 5.5 parts, alpha-carotene 3.5 parts, vitamin D2 2 parts,
Protein peptide 40 parts, caffeic acid 4 parts, 7 parts of stachyose, disintegrating agent 8 parts, binding agent 100 parts, lubricant 6.5 parts, surfactant
1.5 parts, cosurfactant 0.65 part.
Wherein, described disintegrating agent is crospolyvinylpyrrolidone, is that a kind of white has the runny powder of hygroscopicity
End, has the strongest expansion character and the complexing power with multiclass material, is primarily due to it and has high capillary activity, thus
Can promptly water be absorbed in tablet, when swelling pressure has exceeded the intensity of medicine, compile and make medicine moment disintegrate, and
The most swelling in water do not have full-bodied gel layer, thus its disintegrating property is the most superior, and medicine can be made at gastro-intestinal Fluid
In split rapidly the material being broken into fine particle so that the rapid solution absorption of functional component, play a role.Described binding agent is
The ethyl cellulose of pharmaceutical grade, its Heat stability is good, there are excellent alkali resistance and weak acid resistant, long term storage is never degenerated, with institute
Some plasticizers have good compatibility, are a kind of well medicine binding agents.Described lubricant is gel aluminum hydroxide, no
Only have good lubricant effect, also there is antiacid and the protective effects on gastric mucosa, can effectively reduce dripping of irritant drugs and stomach is glued
The damage of film.Described surfactant is levan, and it has the best amphipathic property, is to live in extraordinary surface
Property agent, be transfructosylase catalysis the water solublity being formed by connecting with one or more fructose molecules by sucrose and the height of stickiness
Molecular polysaccharide, has different physiological roles and biological activity.Described cosurfactant is sorbitol, can change surface activity
The surface activity of agent and hydrophile-lipophile balance, participate in forming micelle, adjusts water and the polarity of oil, thus preferably strengthens chemical combination
The surface activity of thing.Described protein peptide refers to a kind of full-natural nutritive material extracted from Semen sojae atricolor, is also human body cell
Important component part, comprises the aminoacid of multiple needed by human body, and vital movement plays extremely important effect, human consumption
There is a protein peptide operating system in system, small-molecular peptides directly can be absorbed by intestinal, is rapidly introduced in blood, is carried
The position wanted to needed by human body, peptide molecule can continue to keep biological activity after entering human body, directly participate in and regulation body weight for humans is wanted
Vital movement, therefore soybean protein peptide is when human-body fatigue, weakness, immune system are destroyed, and effect is especially apparent.Anti-
Thrombosis, eliminate human-body fatigue, the liver protecting, prevent arteriosclerosis, strengthen human body physical agility and muscle strength, enhancing human body and exempt from
The aspects such as epidemic disease power all have obvious action, can strengthen the combination effect between ingredient.
The preparation method of a kind of oral formulations treating chronic leukemia is:
Step one: the binding agent of described composition by weight is mixed according to the weight ratio of 1:4 with the ethanol that mass concentration is 65%
Closing and uniformly and fully dissolve, binding agent ethyl cellulose is slowly added into the container filling solvent under stirring, until
Till complete wetting is dissolved, make binder solution, standby,；
Step 2: by the gefitinib of described composition by weight, maytanprine, tanshinone IIA, phycocyanobilin, zaluzanin C,
Ursolic acid, P-coumaric acid, oleanolic acid, succinic acid, alpha-carotene, vitamin D2, protein peptide, caffeic acid, several amino acids,
Stachyose mechanical mixture uniformly after, multi-angle rolling while stirring, make can not the medicine densification distribution of composition, ground system
Become fine powder, cross 300 mesh sieves, prepare hybrid medicine fine powder, standby；
Step 3: first binder solution prepared by step one is placed on blender and at the uniform velocity stirs, mixing speed
180r/min, then hybrid medicine fine powder step 2 prepared is slowly added to, and prepares hybrid medicine, then it is dense to be reduced pressure by hybrid medicine
Retract and receive ethanol, prepare hybrid medicine extractum, add the disintegrating agent of described composition by weight, lubricant, surfactant, help table
Face activating agent, seals up for safekeeping after low temperature sterilization, i.e. prepares a kind of oral formulations treating chronic leukemia of the present invention；
Step 4: add diluent 120 parts in the oral formulations for the treatment of chronic leukemia step 3 prepared, by system
Grain, it is dried, granulate, sieves, fill, polish, pack and make capsule.
Embodiment 3: a kind of oral formulations treating chronic leukemia, described oral formulations mainly includes following weight portion
Composition: gefitinib 12 parts, maytanprine 10 parts, tanshinone IIA 8 parts, phycocyanobilin 6 parts, zaluzanin C 5 parts, ursolic acid
15 parts, P-coumaric acid 14 parts, oleanolic acid 10 parts, succinic acid 8 parts, alpha-carotene 5 parts, vitamin D2 3 parts, protein peptide 50
Part, caffeic acid 5 parts, 8 parts of stachyose, disintegrating agent 9.5 parts, binding agent 120 parts, lubricant 8 parts, 2 parts of surfactant, help surface
Activating agent 0.8 part.
Wherein, described disintegrating agent is crospolyvinylpyrrolidone, is that a kind of white has the runny powder of hygroscopicity
End, has the strongest expansion character and the complexing power with multiclass material, is primarily due to it and has high capillary activity, thus
Can promptly water be absorbed in tablet, when swelling pressure has exceeded the intensity of medicine, compile and make medicine moment disintegrate, and
The most swelling in water do not have full-bodied gel layer, thus its disintegrating property is the most superior, and medicine can be made at gastro-intestinal Fluid
In split rapidly the material being broken into fine particle so that the rapid solution absorption of functional component, play a role.Described binding agent is
The ethyl cellulose of pharmaceutical grade, its Heat stability is good, there are excellent alkali resistance and weak acid resistant, long term storage is never degenerated, with institute
Some plasticizers have good compatibility, are a kind of well medicine binding agents.Described lubricant is gel aluminum hydroxide, no
Only have good lubricant effect, also there is antiacid and the protective effects on gastric mucosa, can effectively reduce dripping of irritant drugs and stomach is glued
The damage of film.Described surfactant is levan, and it has the best amphipathic property, is to live in extraordinary surface
Property agent, be transfructosylase catalysis the water solublity being formed by connecting with one or more fructose molecules by sucrose and the height of stickiness
Molecular polysaccharide, has different physiological roles and biological activity.Described cosurfactant is sorbitol, can change surface activity
The surface activity of agent and hydrophile-lipophile balance, participate in forming micelle, adjusts water and the polarity of oil, thus preferably strengthens chemical combination
The surface activity of thing.Described protein peptide refers to a kind of full-natural nutritive material extracted from Semen sojae atricolor, is also human body cell
Important component part, comprises the aminoacid of multiple needed by human body, and vital movement plays extremely important effect, human consumption
There is a protein peptide operating system in system, small-molecular peptides directly can be absorbed by intestinal, is rapidly introduced in blood, is carried
The position wanted to needed by human body, peptide molecule can continue to keep biological activity after entering human body, directly participate in and regulation body weight for humans is wanted
Vital movement, therefore soybean protein peptide is when human-body fatigue, weakness, immune system are destroyed, and effect is especially apparent.Anti-
Thrombosis, eliminate human-body fatigue, the liver protecting, prevent arteriosclerosis, strengthen human body physical agility and muscle strength, enhancing human body and exempt from
The aspects such as epidemic disease power all have obvious action, can strengthen the combination effect between ingredient.
The preparation method of a kind of oral formulations treating chronic leukemia is:
Step one: the binding agent of described composition by weight is mixed according to the weight ratio of 1:5 with the ethanol that mass concentration is 75%
Closing and uniformly and fully dissolve, binding agent ethyl cellulose is slowly added into the container filling solvent under stirring, until
Till complete wetting is dissolved, make binder solution, standby,；
Step 2: by the gefitinib of described composition by weight, maytanprine, tanshinone IIA, phycocyanobilin, zaluzanin C,
Ursolic acid, P-coumaric acid, oleanolic acid, succinic acid, alpha-carotene, vitamin D2, protein peptide, caffeic acid, several amino acids,
Stachyose mechanical mixture uniformly after, multi-angle rolling while stirring, make can not the medicine densification distribution of composition, ground system
Become fine powder, cross 300 mesh sieves, prepare hybrid medicine fine powder, standby；
Step 3: first binder solution prepared by step one is placed on blender and at the uniform velocity stirs, mixing speed
180r/min, then hybrid medicine fine powder step 2 prepared is slowly added to, and prepares hybrid medicine, then it is dense to be reduced pressure by hybrid medicine
Retract and receive ethanol, prepare hybrid medicine extractum, add the disintegrating agent of described composition by weight, lubricant, surfactant, help table
Face activating agent, seals up for safekeeping after low temperature sterilization, i.e. prepares a kind of oral formulations treating chronic leukemia of the present invention；
Step 4: add filler 180 parts in the oral formulations for the treatment of chronic leukemia step 3 prepared, by system
Grain, be dried, granulate, mixing, tabletting, packaging make tablet.
Clinical verification:
1. case is collected
Collect 60 example chronic leukemia cases, meet relevant standard, institute in " diagnosis of hematological diseases and criterion of therapeutical effect " after diagnosing
Have patient all to check through peripheral hemogram, bone marrow smear inspection and pathological biopsy etc. to make a definite diagnosis.In 60 example patients, chronic myelocytic leukemia
38 examples, wherein male 22 example, women 16 example, age 15～68 years old；Chronic lymphocytic leukemia 22 example, wherein male 13 example,
Women 9 example, age 36～76 years old.
2. Therapeutic Method
A. the 60 example chronic leukemia patients collected are divided into three groups, test group 1, test group 2, test group 3, often organize 20
Example, chronic myelocytic leukemia and chronic lymphocytic leukemia do not illustrate when packet, three groups of every physiology of case
Feature and state of an illness no significant difference, have comparability；
Take the granule of embodiment 1 preparation, embodiment 2 to the most respectively test group 1, test group 2, the patient of test group 3
The tablet of the capsule of preparation, embodiment 3 preparation, according to proportionate relationship 30mg/kg of oral formulations Yu body weight, each takes two
Secondary, within 30th, it is a course for the treatment of, the cycle of taking is 6 courses for the treatment of；
C. during treating, the specially clinical condition such as card record anemia, hemorrhage, infection, osteodynia, liver, spleen, lymphadenectasis
Shape, sign and the change of tongue arteries and veins, the physiological parameter such as periodic detection hemoglobin, leukocyte, juvenile cell, observe patient and persistently delay
Solution time and life span.
3. curative effect determinate standard
1. complete incidence graph: without anemia, hemorrhage, infection and leukemiacell infiltration performance；Hemoglobin G T.GT.GT 100g/L, the most carefully
Born of the same parents sum ＜ 10 × 109/L, classification is without juvenile cell, platelet 100-400 × 109/L；Juvenile cell ＜ 5% in bone marrow, respectively
It is that hypertrophy is normal；
2. part is alleviated: have 1 or 2 not reach complete incidence graph standard in clinical manifestation, hemogram, bone marrow smear 3；
3. do not alleviate: in clinical manifestation, hemogram, bone marrow smear 3, all not up to part alleviates standard.
4. experimental data statistics
| Group | Case load | Complete incidence graph | Part is alleviated | Do not alleviate | Abnormal response | Effective percentage |
| Test group 1 | 20 | 8 | 11 | 1 | 0 | 95.0% |
| Test group 2 | 20 | 12 | 8 | 0 | 0 | 100.0% |
| Test group 3 | 20 | 7 | 10 | 3 | 0 | 85.0% |
5. efficacy analysis
A. vital sign: equal nothing before and after heart rate, blood pressure, lung, liver, spleen, the rhythm of the heart, routine blood test, routine urinalysis, hepatic and renal function test
Change, 60 example patients have no any untoward reaction during treating；
The most to sum up it is believed that a kind of oral formulations total effective rate treating chronic leukemia of the present invention is 85.0%, improve
Every symptom of chronic leukemia is evident in efficacy, and Clinical practice is safely, effectively.
6. model case
Case one: Korea Spro so-and-so: female, 55 years old, be diagnosed as chronic myelocytic leukemia, patient is with heating, hemorrhage, ecchymosis,
Osteodynia, lusterless complexion, dizziness headache, spiritlessness and weakness, soreness of the waist and knees, the symptom such as dry mouth and throat, use the embodiment of the present invention 1 to prepare
Granule after 5 months, this patient generates heat, hemorrhage, ecchymosis, osteodynia, lusterless complexion, dizziness headache, spiritlessness and weakness, the acid of waist knee joint
Soft, the symptom such as dry mouth and throat alleviates, and after continuing to take 7 months, every hemocyte is the most basic recovers normal, stable disease.
Case two: Lee, female, 35 years old, because weak, splenomegaly do bone marrow examination to hospital January, it is diagnosed as chronic granulocyte
Leukemia, bone marrow smear polar hyperplasia, grain system extremely hypertrophy, shaft-like above ratio increases the most in various degree, and slurry endoparticle is slightly
Having increasing thick, visible addicted to acid basophilic leukocyte, mature erythrocyte slightly differs in size, hemoglobin turgor, lymphocyte ratio
On the low side, use the capsule after three months of the embodiment of the present invention 2 preparation, weak transference cure, splenomegaly after continuing to take three months
Transference cure, the bimester that every physiological parameter recovery normal continuous being taken medicine, stable disease.
Case three: Zhang, man, 63 years old, it is diagnosed as chronic myelocytic leukemia, patients symptomatic is osteodynia, lusterless complexion, head
Dizzy headache, spiritlessness and weakness, the symptom such as soreness of the waist and knees, use the tablet of the embodiment of the present invention 3 preparation after three months, this patient's stasis of blood
Speckle, osteodynia, lusterless complexion, dizziness headache, spiritlessness and weakness, the symptom such as soreness of the waist and knees alleviates, and has substantially recovered normal, consolidates again and controls
After treating five months, leukocyte recovers normal, and transference cure returns to one's perfect health.
Last it is noted that above example is only in order to illustrate technical scheme, it is not intended to limit；Although
With reference to previous embodiment, the present invention is described in detail, it will be understood by those within the art that: it still may be used
So that the technical scheme described in previous embodiment to be modified, or wherein portion of techniques feature is carried out equivalent；And
These amendments or replacement, do not make the essence of appropriate technical solution depart from spirit and the model of embodiment of the present invention technical scheme
Enclose.
Claims (8)
1. the oral formulations treating chronic leukemia, it is characterised in that described oral formulations mainly includes following weight
The composition of part: gefitinib 6～12 parts, maytanprine 5～10 parts, tanshinone IIA 5～8 parts, phycocyanobilin 3～6 parts, Sino-U.S. chrysanthemum
Element C 3～5 parts, ursolic acid 8～15 parts, P-coumaric acid 10～14 parts, oleanolic acid 6～10 parts, succinic acid 3～8 parts, α-Hu Luo
Bu Su 2～5 parts, vitamin D2 1～3 parts, protein peptide 30～50 parts, caffeic acid 3～5 parts, stachyose 6～8 parts, disintegrating agent 6.5
～9.5 parts, binding agent 80～120 parts, lubricant 5～8 parts, surfactant 1～2 parts, cosurfactant 0.5～0.8 part.
A kind of oral formulations treating chronic leukemia, it is characterised in that described disintegrating agent is
Crospolyvinylpyrrolidone.
A kind of oral formulations treating chronic leukemia, it is characterised in that described binding agent is
Ethyl cellulose.
A kind of oral formulations treating chronic leukemia, it is characterised in that described lubricant is
Gel aluminum hydroxide.
A kind of oral formulations treating chronic leukemia, it is characterised in that described surface activity
Agent is levan.
A kind of oral formulations treating chronic leukemia, it is characterised in that live in the described surface that helps
Property agent is sorbitol.
A kind of oral formulations treating chronic leukemia, it is characterised in that described oral formulations
Preparation method is:
Step one: by the binding agent of described composition by weight and mass concentration be 55～75% ethanol according to the weight ratio of 1:3～5
Mix homogeneously and fully dissolving, makes binder solution, standby；
Step 2: by the gefitinib of described composition by weight, maytanprine, tanshinone IIA, phycocyanobilin, zaluzanin C, Folium Vaccinii vitis-idaeae
Acid, P-coumaric acid, oleanolic acid, succinic acid, alpha-carotene, vitamin D2, protein peptide, caffeic acid, stachyose mechanical mixture are equal
After even, ground fine powder of making, cross 300 mesh sieves, prepare hybrid medicine fine powder, standby；
Step 3: first binder solution prepared by step one is placed on blender and at the uniform velocity stirs, mixing speed 180r/
Min, then hybrid medicine fine powder step 2 prepared is slowly added to, and prepares hybrid medicine, then is returned by hybrid medicine concentrating under reduced pressure
Receive ethanol, prepare hybrid medicine extractum, add the disintegrating agent of described composition by weight, lubricant, surfactant, help surface to live
Property agent, seals up for safekeeping after low temperature sterilization, i.e. prepares a kind of oral formulations treating chronic leukemia of the present invention.
The preparation method of a kind of oral formulations treating chronic leukemia, it is characterised in that described
Oral formulations make granule, tablet and capsule according to common process.
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Cited By (3)
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| CN106038571B (en) * | 2016-07-05 | 2018-08-17 | 福州大学 | A kind of pharmaceutical composition and its application in preparation of anti-tumor drugs of the Gefitinib of targeted drug containing small molecule |
| CN109260188A (en) * | 2018-12-11 | 2019-01-25 | 黄嘉若 | A kind of p-Coumaric Acid treats the purposes of people's acute lymphoblastic leukemia drug in preparation |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105963302A (en) * | 2016-07-05 | 2016-09-28 | 福州大学 | Low-dosage medicine composition containing EGFR (epidermal growth factor receptor) tyrosine kinase and application thereof in preparation of anti-tumor transfer medicines |
| CN106038571B (en) * | 2016-07-05 | 2018-08-17 | 福州大学 | A kind of pharmaceutical composition and its application in preparation of anti-tumor drugs of the Gefitinib of targeted drug containing small molecule |
| CN105963302B (en) * | 2016-07-05 | 2019-08-09 | 福州大学 | A kind of low dose pharmaceutical compositions of the tyrosine kinase containing EGFR and its application in preparation prevention tumor metastasis medicine |
| CN109260188A (en) * | 2018-12-11 | 2019-01-25 | 黄嘉若 | A kind of p-Coumaric Acid treats the purposes of people's acute lymphoblastic leukemia drug in preparation |
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