CN105878238A - Pharmaceutical composition for increasing blood platelets, and preparation method and application thereof - Google Patents
Pharmaceutical composition for increasing blood platelets, and preparation method and application thereof Download PDFInfo
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- CN105878238A CN105878238A CN201610248855.5A CN201610248855A CN105878238A CN 105878238 A CN105878238 A CN 105878238A CN 201610248855 A CN201610248855 A CN 201610248855A CN 105878238 A CN105878238 A CN 105878238A
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- 0 C[n]1c(*C(C(N2*)=O)=NC2=O)nc(CC2=CC=C(*)CC2)c1Cc(cc1)ccc1OC Chemical compound C[n]1c(*C(C(N2*)=O)=NC2=O)nc(CC2=CC=C(*)CC2)c1Cc(cc1)ccc1OC 0.000 description 1
Classifications
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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
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention provides a pharmaceutical composition for increasing blood platelets. The pharmaceutical composition for increasing the blood platelets is characterized in that an active ingredient of the composition consists of a compound I and a compound II, the mass percentages of the compound I and the compound II in the composition are 70% and 30% respectively, the compound I is Clathridine A, and the compound II is Naamidine G. The invention discloses an application of the composition in preparation of drug for increasing blood platelets, and the development and application prospect is good. The application of the composition in preparation of the drug for increasing the blood platelets is disclosed for the first time, the blood platelet increasing activity of the pharmaceutical composition is high, and the progress is remarkable.
Description
Technical field
The present invention relates to the new application of compound, particularly relate to a kind of increased platelets counts medicine and its preparation method and application.
Background technology
The compound Clathridine A that the present invention relates to and Naamidine G be within 2012, deliver (Jayanta Das, et al.,
Total Syntheses of Kealiinines A-C.Org Lett., 14 (24) 6,210 6213.) noval chemical compound,
Both compounds have brand-new framework types, and the compositions of the both compounds that the present invention relates to is in preparation increased platelets counts
Purposes in medicine belongs to first public.
Summary of the invention
Do not find that it has rising blood in it is an object of the invention to study according to existing Clathridine A and Naamidine G
The present situation of the report of platelet activity, it is provided that Clathridine A and Naamidine G compositions are at preparation increased platelets counts medicine
Application in thing.
A kind of increased platelets counts pharmaceutical composition, the active component of said composition is made up of compound I and compound II, this combination
In thing, the mass percent of compound I and compound II is respectively 70% and 30%, and described compound I is Clathridine A,
Structure is as shown in formula I, and described compound II is Naamidine G, shown in structure such as formula (II),
Described increased platelets counts pharmaceutical composition, preparation method is according to matter by the powder of compound I and the powder of compound II
Amount percent respectively 70% and 30% is sufficiently mixed, and adds adjuvant, makes preparation.
The application in preparing antiplatelet drug of the described increased platelets counts pharmaceutical composition.
The Clathridine A that the present invention relates to and Naamidine G compositions use in preparation treatment thrombocytopenia medicine
Way belongs to first public, and owing to framework types belongs to brand-new framework types, and its treatment thrombocytopenia activity is strong, possesses
Prominent substantive distinguishing features, the preventing and treating being simultaneously used for thrombocytopenia obviously has the most progressive.
Detailed description of the invention
The preparation method of compound Clathridine A and Naamidine G involved in the present invention sees document (Jayanta
Das, et al., Total Syntheses of Kealiinines A-C.Org Lett.2012,14 (24) 6,210 6213.).
The present invention is further detailed explanation by the following examples, but protection scope of the present invention is not by specific embodiment
Any restriction, but be defined in the claims.
Embodiment 1: the preparation of compound composition tablet involved in the present invention:
Taking 7 grams of Clathridine A and 3 grams of Naamidine G, add 190 grams of dextrin, mixing, Conventional compression is made
1000.
Embodiment 2: the preparation of compound composition capsule involved in the present invention:
Take 7 grams of Clathridine A and 3 grams of Naamidine G, add starch 190 grams, mixing, encapsulated make 1000
Grain.
Its pharmaceutically active is further illustrated below by pharmacodynamic experiment.
Experimental example 1: the hemoposieis of the present composition:
One, the present composition oral administration impact on mouse peripheral blood platelet counts
Method: Balb/c mice 40,18-22g is female, Nanjing Medical University's Experimental Animal Center, is divided into by body weight
Four groups, the matched group 0.7 that respectively prepared by normal control, present composition 1mg/kg, the compound I of embodiment 1 preparation
Matched group 0.3mg/kg prepared by mg/kg, compound II, is divided into twice oral administration on the 1st, totally 9 times four and half.In giving
Before medicine, be administered latter 1 day, 3 days, 7 days, 14 days cut tail take blood 20ul, F-820 platelet count instrument detection hemogram.
The impact (n=10) on mouse peripheral blood platelet counts of table 1 present composition oral administration
Compare with normal saline group: * p < 0.5**p < 0.01
Result: hematoblastic major function is for participating in hemostasis.Platelet counts and dysfunction may result in bleeding tendency.
Table 1 shows present composition oral administration prepared by embodiment 1 impact on rat peripheral blood platelet counts.Can see
Going out, compared with normal saline group platelet count, administration group platelet counts i.e. has rising upon administration for 3-7 days, within 10-14 days, has
One elevation process become apparent from, and more obvious than individually oriented compound I and compound II effect.These results indicate that certain agent
The present composition oral administration of embodiment 1 preparation of amount can increase rat peripheral blood platelet counts, and this is that the present invention combines
One of thing curative effect playing its hemoposieis.
Two, the present composition of the embodiment 1 preparation therapeutical effect to post hemorrhagic mice
Post hemorrhagic mice affected ICR mice 50, ♀ ♂ half and half, Nanjing Medical University's Experimental Animal Center, is divided into 5
Group (n=10).In addition to normal saline group, other every mice of group, from orbital vein blood-letting 0.5ml, takes blood again and surveys complete after 24h
Portion respectively organizes index, then continuous gastric infusion 1 week, and dosage ibid, after last is administered 1h, takes blood from orbital venous plexus and uses
The full whole bliid platelet analyzer of F-800 surveys These parameters.
Table 2 present composition is to because of caused thrombocytopenic therapeutical effect of losing blood
Type group compares: * p < 0.05**p < 0.01
Result shows, blood-letting mice is after the present composition taking embodiment 1 preparation is treated 7 days, and 2 administration groups are respectively
Comparing in model group, its platelet value is significantly higher than model group, and has exceeded the level of normal saline group mice, and compares
Individually oriented compound I and compound II effect are obvious.
Three, the therapeutical effect that the present composition of embodiment 1 preparation coagulation function caused to radiation reduces
For the research therapeutical effect to acute radiation sickness, observe the present composition pair of embodiment 1 preparation of various dose
6.5Gy irradiates the impact that mouse hemopoietic recovers, and dosage is ibid.
The present composition of table 4 embodiment 1 preparation thrombocytopenic therapeutical effect (10th day) caused to radiation
Compare with modeling group: * p < 0.05**p < 0.01
Result shows, gives after being treated by the present composition according to the preparation of mice embodiment every day 1, and hematoblastic Restoration model adds
Hurry up, effect is obvious, and more obvious than individually oriented compound I and compound II effect.
Conclusion: the present composition can notable increased platelets counts, can be used to prepare the medicine of increased platelets counts.
Claims (3)
1. an increased platelets counts pharmaceutical composition, it is characterised in that the active component of said composition is by compound I and change
Compound II forms, and in said composition, the mass percent of compound I and compound II is respectively 70% and 30%, institute
State shown in the structure such as formula (I) of compound I, shown in the structure such as formula (II) of described compound II:
2. increased platelets counts pharmaceutical composition as claimed in claim 1, it is characterised in that: preparation method is by compound
The powder of I and the powder of compound II are sufficiently mixed according to mass percent respectively 70% and 30%, add adjuvant,
Make preparation.
3. increased platelets counts pharmaceutical composition application in increased platelets counts medicine as claimed in claim 1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610248855.5A CN105878238A (en) | 2016-04-19 | 2016-04-19 | Pharmaceutical composition for increasing blood platelets, and preparation method and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610248855.5A CN105878238A (en) | 2016-04-19 | 2016-04-19 | Pharmaceutical composition for increasing blood platelets, and preparation method and application thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105878238A true CN105878238A (en) | 2016-08-24 |
Family
ID=56705161
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610248855.5A Pending CN105878238A (en) | 2016-04-19 | 2016-04-19 | Pharmaceutical composition for increasing blood platelets, and preparation method and application thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105878238A (en) |
-
2016
- 2016-04-19 CN CN201610248855.5A patent/CN105878238A/en active Pending
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| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160824 |
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| WD01 | Invention patent application deemed withdrawn after publication |