CN104435312B - A kind of Bai Ai capsules as intestinal transport body inhibitor application - Google Patents
A kind of Bai Ai capsules as intestinal transport body inhibitor application Download PDFInfo
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- CN104435312B CN104435312B CN201410645232.2A CN201410645232A CN104435312B CN 104435312 B CN104435312 B CN 104435312B CN 201410645232 A CN201410645232 A CN 201410645232A CN 104435312 B CN104435312 B CN 104435312B
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/13—Coniferophyta (gymnosperms)
- A61K36/14—Cupressaceae (Cypress family), e.g. juniper or cypress
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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
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- A61K36/185—Magnoliopsida (dicotyledons)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
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- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/80—Scrophulariaceae (Figwort family)
- A61K36/804—Rehmannia
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- 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
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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
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Abstract
The invention discloses a kind of application of Bai Ai capsules as intestinal transport body inhibitor.This intestinal transport body inhibitor is inhibited to intestines transporter, especially P glycoprotein (P gp), and therefore, Bai Ai capsules can serve as intestinal transport body inhibitor, especially P gp inhibitor.This intestinal transport body inhibitor --- Bai Ai capsules can serve as the adjuvant drug of Western medicine, especially Irbesartan, so that with Western medicine drug combination to prevent or disease preventing and treating.
Description
Technical field
The present invention relates to a kind of application of Bai Ai capsules as intestinal transport body inhibitor.
Background technology
Clinically Chinese and Western medicine drug combination is increasingly universal at present, and its effect has obtained the generally accreditation of medical field.Chinese and Western medicine
Joint can reduce toxic side effect with Synergistic, reduce dosage, reduce medication taboo, expand accommodation.But due in
The chemical composition of medicine and pharmacological action are sufficiently complex, and it is improper that Chinese and Western medicine is used in combination, and can also lessen the curative effect, and increase side effect or draw
Play drug induced disease, serious even threat to life, so to evade and prophylactic agent incompatibility simultaneously.
The content of the invention
The technical problems to be solved by the invention are to provide a kind of Bai Ai capsules as intestinal transport body for the state of the art
The application of inhibitor.
The present invention solve the technical scheme that is used of above-mentioned technical problem for：A kind of Bai Ai capsules press down as intestinal transport body
The application of preparation.
Wherein, the Bai Ai capsules include the component of following parts by weight：
Wherein, the intestinal transport body is P- glycoprotein.
Wherein, the effective dosage ranges of the intestinal transport body inhibitor are 1.5~6g/ days.
Wherein, the effective dose of the intestinal transport body inhibitor is 1.5g/ days, 3g/ days or 6g/ days.
Wherein, the effective dose of the intestinal transport body inhibitor is 3g/ days.
A kind of Bai Ai capsules are used as intestinal transport body inhibitor and application of the Irbesartan on hypertension is prevented and treated.
Wherein, the effective dosage ranges of the intestinal transport body inhibitor are 1.5~6g/ days, the Irbesartan
Effective dose be 120mg/ days.
Compared with prior art, the advantage of the invention is that：The main component of Bai Ai capsules is cacumen biotae, glutinous rehmannia, folium artemisiae argyi
And lotus leaf, it is inhibited to intestines transporter, especially P- glycoprotein (P-gp), and therefore, Bai Ai capsules can serve as intestines
Road transporter inhibitors, especially P-gp inhibitor.Bai Ai capsules be as intestinal transport body inhibitor present invention firstly discovers that
Application, i.e. basing on practicality invention of the Bai Ai capsules on as intestinal transport body inhibitor be pioneering, and Bai Ai is not found before
Capsule is applied with this.
Yin Baiai capsules are intestinal transport body inhibitor, therefore the adjuvant drug of Western medicine can be served as with it, and it can be reduced
The administration dose of Western medicine, and strengthen the drug effect of Western medicine, while substantially reducing the toxic side effect of Western medicine.For example, Ruo Baiai capsules fill
When the adjuvant drug of Irbesartan is used to prevent and treat hypertension, especially essential hypertension, Bai Ai capsules can strengthen shellfish in distress
Husky smooth drug effect, combines and takes after a period of time, it is possible to decrease the dosage of Irbesartan even cuts out Irbesartan, so
The toxic side effect of Irbesartan can be substantially reduced on the basis of curative effect is stablized.
Based on the effect of above-mentioned Bai Ai capsules, Bai Ai capsules can be applied on the drug combination with Western medicine, to prevent and treat
Or prevention disease.
Brief description of the drawings
Fig. 1 is the suppression of outer row of Bai Ai of the embodiment of the present invention capsules to the digoxin mediated by P-gp on Caco-2 cells
Make and use；
Fig. 2 is suppression of Bai Ai of the embodiment of the present invention capsules to the Irbesartan mediated by P-gp outer row on Caco-2 cells
Make and use；
Fig. 3 is the pharmacokinetics that the embodiment of the present invention combines the Oral Administration in Rats absorption for taking Bai Ai capsules and Irbesartan
Influence.
Embodiment
The present invention is described in further detail below in conjunction with accompanying drawing embodiment.
The intestinal transport body inhibitor of the present embodiment is specially Bai Ai capsules, and the main component of Bai Ai capsules includes following weight
Measure the component of number：
The present embodiment specifically uses the cypress that the batch produced by Yangzijiang Pharmaceutical Group Co., Ltd is 13080642
End capsule, and the proportioning of the Bai Ai capsule each components is within the above range.
The effective dosage ranges of intestinal transport body inhibitor are 1.5~6g/ days, such as 1.5g/ days, 3g/ days or 6g/ days,
Optimum effective dose is 3g/ days.
The intestinal transport body inhibitor of the present embodiment specifically can be applicable on the adjuvant drug of Western medicine.For example with Irbesartan
Intestinal transport when drug combination is to prevent and treat hypertension (especially essential hypertension), Bai Ai capsules and Irbesartan drug combination
The effective dosage ranges of body inhibitor are 1.5~6g/ days, and the effective dose of Irbesartan is 120mg/ days.Bai Ai capsules and strategic point
Bei Shatan can be administered respectively, and both can also be prepared into the combination medicine for preventing and treating hypertension.
Bai Ai capsules (the manufacturer of the present embodiment can be specifically verified from following several respects：Yangzijiang Pharmaceutical Group is limited
Company, production batch：13080642) intestinal transport body inhibitor can be served as：
1st, Caco-2 cells judge that Bai Ai capsules are P-gp inhibitor
It is specific to prove that Bai Ai capsules are P-gp using Caco-2 cell models and classical P-gp substrate drugs digoxin
Inhibitor.Prove result as shown in figure 1, from figure 1 it appears that Bai Ai capsules can effectively suppress the outer row (IC of digoxin50
=0.42mg/mL).
2nd, Caco-2 cell models and Western medicine --- Irbesartan are utilized, it was demonstrated that Bai Ai capsules can suppress as P-gp substrates
Irbesartan outer row so that improve its absorption.
Table 1 shows that Irbesartan is P-gp substrate (Yi Kelida be known P-gp specific inhibitors), this with
Document report is consistent.And Fig. 2 then shows that Bai Ai capsules can suppress the outer row of Irbesartan, so as to improve its intestinal absorption.
The experimental verification Irbesartan of table 1. is P-gp substrate
The aspect of the above two is all theoretically to demonstrate Bai Ai capsules to serve as intestinal transport body inhibitor, in order to enter one
Step verifies that Bai Ai capsules serve as intestinal transport body inhibitor by testing, and the present embodiment is tested with SD rats as subjects
Card Bai Ai capsules can serve as Western medicine --- the adjuvant drug of Irbesartan.
Use Bai Ai capsules using 125mg/kg (equivalent to human administration's dosage as 1.5g), 250mg/kg (equivalent to people in advance
Body dosage is 3g), 500mg/kg (being 6g equivalent to human administration's dosage) daily dosage is to SD rat oral gavages 3 days；The
Three days gavage half an hour after, (be about equivalent to human administration's dosage to SD rat oral gavages Irbesartan with 10mg/kg dosage
120mg).Collection whole blood calculates the AUC in 0-72 hours, and using independent samples t test to combining administration group and control group, i.e.,
First group of carry out statistical analysis of alone Irbesartan group, analysis result is as shown in table 2.
The analysis result of the drug combination of table 2. and control group
As shown in Table 2,250mg/kg Bai Ai dosage can cause Irbesartan (Irbesartan) AUC to improve about twice (p
<0.05) no marked difference, but to Cmax is not caused.And blood medicine curve as shown in Figure 3 displays that Bai Ai capsules can increase strategic point
Bei Shatan bioavilability simultaneously extends curative effect.
In summary data, Bai Ai capsules are in vitro in cell experiment and internal P of Rats K experiments all to P-gp substrate drugs
There is effect, raising permeability or bioavilability and the outer row of reduction are embodied in, so as to demonstrate Bai Ai capsules to P-
Gp inhibitory action.It therefore, it can prove, Bai Ai capsules can be used as a kind of new P-gp inhibitor.
Above content is only presently preferred embodiments of the present invention, for one of ordinary skill in the art, according to the present invention's
Thought, will change in specific embodiments and applications, and this specification content should not be construed as to the present invention
Limitation.
Claims (6)
1. a kind of application of Bai Ai capsules in enteron aisle P- glycoprotein transporter inhibitor is prepared, it is characterised in that the Bai Ai
Capsule is made up of the component of following parts by weight：
2. application according to claim 1, it is characterised in that：The effective agent of the enteron aisle P- glycoprotein transporter inhibitor
It is 1.5~6g/ days to measure scope.
3. application according to claim 2, it is characterised in that：The effective agent of the enteron aisle P- glycoprotein transporter inhibitor
Measure as 1.5g/ days, 3g/ days or 6g/ days.
4. application according to claim 3, it is characterised in that：The effective agent of the enteron aisle P- glycoprotein transporter inhibitor
Measure as 3g/ days.
5. a kind of Bai Ai capsules joint Irbesartan is preparing the application in preventing and treating the medicine of hypertension, it is characterised in that described
Bai Ai capsules are made up of the component of following parts by weight：
6. application according to claim 5, it is characterised in that：The effective dosage ranges of the Bai Ai capsules are 1.5~6g/
My god, the effective dose of the Irbesartan is 120mg/ days.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410645232.2A CN104435312B (en) | 2014-11-12 | 2014-11-12 | A kind of Bai Ai capsules as intestinal transport body inhibitor application |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410645232.2A CN104435312B (en) | 2014-11-12 | 2014-11-12 | A kind of Bai Ai capsules as intestinal transport body inhibitor application |
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| Publication Number | Publication Date |
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| CN104435312A CN104435312A (en) | 2015-03-25 |
| CN104435312B true CN104435312B (en) | 2017-08-04 |
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| CN201410645232.2A Active CN104435312B (en) | 2014-11-12 | 2014-11-12 | A kind of Bai Ai capsules as intestinal transport body inhibitor application |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1235611C (en) * | 2003-06-30 | 2006-01-11 | 北京中孚天和医药科技有限公司 | Chinese medicinal composition for treating hypertension |
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| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20170704 Address after: 102200 No. 16, life Garden Road, Beijing, Changping District Applicant after: Beijing Haiyan Pharmaceutical Industry Co., Ltd., Yangzijiang Pharmaceutical Ind Applicant after: GUANGDONG ZHONGXI DAYI DRUG DEVELOPMENT CO., LTD. Applicant after: Yangtze River Pharmaceutical Co., Ltd. Address before: 102200 No. 16, life Garden Road, Beijing, Changping District Applicant before: Beijing Haiyan Pharmaceutical Industry Co., Ltd., Yangzijiang Pharmaceutical Ind Applicant before: GUANGDONG ZHONGXI DAYI DRUG DEVELOPMENT CO., LTD. |
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| GR01 | Patent grant |