CN106038537A - Oral medicine composition for treating albinism - Google Patents
Oral medicine composition for treating albinism Download PDFInfo
- Publication number
- CN106038537A CN106038537A CN201610412398.9A CN201610412398A CN106038537A CN 106038537 A CN106038537 A CN 106038537A CN 201610412398 A CN201610412398 A CN 201610412398A CN 106038537 A CN106038537 A CN 106038537A
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- China
- Prior art keywords
- wedelolactone
- metformin hydrochloride
- treating
- albinism
- albinic
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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
- A61K31/366—Lactones having six-membered rings, e.g. delta-lactones
- A61K31/37—Coumarins, e.g. psoralen
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention relates to the field of medicines, in particular to an oral medicine composition for treating albinism. The oral medicine composition comprises medically acceptable excipients and raw materials. The raw materials include, by weight, 5-9 parts of wedelolactone and 1 part of metformin hydrochloride. The oral medicine composition has the advantages that obvious albinism treatment effects cannot be realized by the metformin hydrochloride, but albinism improving effects of the wedelolactone can be obviously improved if the metformin hydrochloride and the wedelolactone are jointly orally administered.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind of for treating albinic combination of oral medication.
Background technology
Albinism is that tryrosinase lacks or a kind of skin of causing of hypofunction and accessory organ's short of melanin cause
Heritability leukoderma.Patient is usually expressed as retina non-pigment, iris and pupil and presents pale pink, keeps in dark place.Skin, eyebrow
Hair, hair and other chaetas are white or yellow-white.This disease belongs to Familial Occurrence disease, it is considered that this disease is autosome
Recessive genetic disorder, often betides in the crowd of consanguineous marriage.But also having two albino's marriages, its filial generation is the most normal
Situation, illustrate that albinism at least exists two kinds of different hereditary form.
Current albinic treatment, mainly by physical method, reduces ultraviolet as far as possible and radiates eyes and the infringement of skin.
Photosensitizer, hormone etc. can also be used to treat, but still lack of albinic effective medicine.
Domestic painting rosy clouds etc. (it is coated with rosy clouds, Zhang Rongxin, Ma Jingxin, Liu Yaling, Liu Ying, Li Hong. Herba Ecliptae ethanol extraction
Animal coloring element effect and impact melanogenic on murine melanoma cells B16. China's combination of Chinese and Western medicine skin cypridology is miscellaneous
Will. 2006,5(1): 1-4) report, Herba Ecliptae ethanol extraction also has promotion melanin and generates, raises tyrosinase activity
Effect, but fail to find out Herba Ecliptae ethanol extraction and promote that melanin generates, raise the activated monomer of tyrosinase activity
Compound.
Summary of the invention
For above-mentioned prior art, it is an object of the invention to provide a kind of for treating albinic oral pharmaceutical compositions
Thing.
For realizing above-mentioned purpose, the technical solution used in the present invention is:
One is used for treating albinic combination of oral medication, former by pharmaceutically acceptable adjuvant and following weight ratio
Material is made: wedelolactone 5 ~ 9 weight portion, metformin hydrochloride 1 weight portion.
As a preferred version of the present invention, the weight ratio of described raw material is: wedelolactone 6 weight portion, hydrochloric acid two
First biguanide 1 weight portion.
As another preferred version of the present invention, the weight ratio of described raw material is: wedelolactone 7 weight portion, hydrochloric acid
Metformin 1 weight portion.
As another preferred version of the present invention, the weight ratio of described raw material is: wedelolactone 8 weight portion, hydrochloric acid
Metformin 1 weight portion.
As another preferred version of the present invention, above-mentioned pharmaceutically acceptable adjuvant includes titanium dioxide.
Metformin hydrochloride described in technical scheme CAS is 1115-70-4, belongs to conventional antidiabetic drug
Thing, reports that its topical administration is to dermatosis such as hirsutism, acne, reverse property acne, acanthosis nigricans, psoriasis and skin in recent years
Tumors etc. have therapeutical effect, and this is known in those skilled in the art.
Wedelolactone described in technical scheme, English name Wedelolactone, No. CAS is 524-12-9,
Being the composition all contained in Chinese crude drug Herbia Wedeliae, Herba Ecliptae, this is known in those skilled in the art.
The present inventor shows through substantial amounts of research, and wedelolactone has promotion melanin and generates, and raises cheese
The activity of propylhomoserin enzymatic activity, whitening disease has certain therapeutical effect, but required dosage is higher.When wedelolactone and hydrochloric acid
When metformin Combined with Oral is administered, metformin hydrochloride is remarkably improved wedelolactone and promotes melanin to generate and raise cheese
The activity of propylhomoserin enzyme.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is further explained.It should be appreciated that following example are only used for solving
Release the present invention rather than limit the scope of the invention.
Embodiment 1 is used for treating albinic oral tablet and preparation thereof
As follows for treating albinic oral tablet prescription:
As follows for treating albinic oral tablet preparation method:
1) take recipe quantity wedelolactone, metformin hydrochloride is pulverized respectively, crosses 80 mesh sieves, mixes to obtain material powder；
2) take recipe quantity starch to add water and be prepared as the starch slurry that concentration is 5%；
3) step 1) gained material powder is added step 2) gained starch slurry, then will remove hydroxypropyl methyl fiber in prescription
Adjuvant outside element, titanium dioxide adds mix homogeneously, the compressed tablet heart；
4) hydroxypropyl methyl cellulose, titanium dioxide are added ethanol dissolving dispersion and carries out the sheet heart of step 3) as coating solution
Coating and get final product.
Embodiment 2 anti-albinism pharmacodynamic study and safety research
Male albino disease rat 144,28 week old, body weight 320～350g, it is randomly divided into 8 groups, often group 18.In experimentation
Freely ingesting water, within 12 hours, light and shade circulation light shines.
A group gavage gives normal saline；
B group gavage gives metformin hydrochloride aqueous solution, and metformin hydrochloride dosage is 10mg/kg；
C group gavage gives wedelolactone aqueous suspension, and wedelolactone dosage is 90 mg/kg；
D group gavage gives metformin hydrochloride, wedelolactone aqueous suspension, and metformin hydrochloride, wedelolactone dosage divide
Wei 10mg/kg, 50mg/kg；
E group gavage gives metformin hydrochloride, wedelolactone aqueous suspension, and metformin hydrochloride, wedelolactone dosage divide
Wei 10mg/kg, 60mg/kg；
F group gavage gives metformin hydrochloride, wedelolactone aqueous suspension, and metformin hydrochloride, wedelolactone dosage divide
Wei 10mg/kg, 70mg/kg；
G group gavage gives metformin hydrochloride, wedelolactone aqueous suspension, and metformin hydrochloride, wedelolactone dosage divide
Wei 10mg/kg, 80mg/kg；
H group gavage gives metformin hydrochloride, wedelolactone aqueous suspension, and metformin hydrochloride, wedelolactone dosage divide
Wei 10mg/kg, 90mg/kg；
Each treated animal is every 3 days and is administered once, and is administered 15 times altogether.
(1) medicine impact on animal pattern skin tryrosinase
After last is administered, each group Rat Fast 24h, often group puts to death 6 rats, takes every rat dorsum skin (3 cm
X3cm), making the frozen section of 4～5 μ m thick under-30 degrees Celsius, fix 45min with the paraformaldehyde of 45% under room temperature, 37 take the photograph
Under family name's degree, the slide being loaded with section is placed in 30min in the methanol solution containing 0.5% hydrogen peroxide, with answering of 3% citric acid dilution
Closing Digestive system (Wuhan Boster Biological Technology Co., Ltd.) digestion, the probe in-situ with 10 μ g/ μ L digoxigenin labellings is miscellaneous
Hand over liquid (Wuhan Boster Biological Technology Co., Ltd.) 30 μ L to drip in tested slice surface, hatch 90 min.Ground control is used
The phosphate buffer of 0.5mol/L replaces probe.Sodium citrate buffer (Sen Beijia bio tech ltd, Nanjing) is washed
Wash twice, hatch 20 min with hybrid stability liquid and confining liquid (Wuhan Boster Biological Technology Co., Ltd.) the most respectively, with
Rabbit anti digoxin antibody hatches 60min(Beijing Zhong Shan Bioisystech Co., Ltd), with biotin goat-anti rabbit anti-igg (in Beijing
Mountain Bioisystech Co., Ltd), confining liquid (Wuhan Boster Biological Technology Co., Ltd.) and horseradish peroxidase-labeled
Streptavidin (Beijing Zhong Shan Bioisystech Co., Ltd) hatch respectively 20min, DAB dyeing, HE redye after at optical microphotograph
Microscopic observation.
Observe each group of in situ hybridization section under the high power lens visual field and corresponding ground control is cut into slices, every under counting high power lens
In 100 basal layer cells, endochylema is the cell number of brown color.
Result see table:
aP ＜ 0.01 compared with A group；bP ＜ 0.01 compared with C group.
As seen from the above table, can significantly to heighten albino rats skin tyrosinase mRNA expression (significantly high for wedelolactone
In normal saline and metformin hydrochloride)；Metformin hydrochloride whitening disease rat skin tyrosinase mRNA expression is without significantly
Impact (with normal saline without significant difference)；Albino rats skin cheese after metformin hydrochloride, wedelolactone administering drug combinations
Propylhomoserin enzyme mrna expression is all remarkably higher than wedelolactone (P ＜ 0.01 compared with wedelolactone group).Result shows hydrochloric acid two
Rat skin tyrosinase mRNA expression is not made significant difference by first biguanide, but can remarkably promote wedelolactone whitening disease rat
The rise effect of skin tyrosinase mRNA expression, the most albinic treatment.
(2) medicine coloring element effect to animal pattern skin
After last is administered, each group Rat Fast 24h, often group puts to death 6 rats, takes every rat dorsum skin (3 cm
X3cm), make the frozen section of 4～5 μ m thick under-30 degrees Celsius, under room temperature, fix 45min, paraffin with the paraformaldehyde of 45%
Embedding, graded ethanol is dehydrated.Schmorl staining identification melanin and melanin cellulation, contaminate melanin granule
Color, melanocyte is dyed to pitchy, counts the cell number containing melanin granule in every 100 basal cells under high power lens.
Result see table:
aP ＜ 0.01 compared with A group；bP ＜ 0.01 compared with C group.
As seen from the above table, to be remarkably improved albino rats skin cell number Han melanin granule (significantly high for wedelolactone
In normal saline and metformin hydrochloride)；Metformin hydrochloride whitening disease rat skin contains melanin granule cell number without significantly
Impact (with normal saline without significant difference)；After metformin hydrochloride, wedelolactone administering drug combinations, albino rats skin contains
Melanin granule cell number is all remarkably higher than wedelolactone (P ＜ 0.01 compared with wedelolactone group).Result shows hydrochloric acid two
Rat skin cell number Han melanin granule is not made significant difference by first biguanide, but with albino rats skin during Qi chrysanthemum lactone administering drug combinations
Skin cell number Han melanin granule is significantly higher than the Qi independent medication of chrysanthemum lactone, the most albinic treatment.
(3) medicine safety research to animal pattern
After last is administered, often organizes remaining 6 rats, put to death 3, core, liver, spleen, lung, kidney, intestinal, testis do gross examination of skeletal muscle,
Observe internal organs color and luster and whether there is internal organs enlargement situation；Routine pathology section subsequently, paraffin embedding, HE dyes, optical microphotograph
Whether Microscopic observation each internal organs microstructure exists obvious pathological changes.
Often organizing remaining 3 rat to continue to observe 14 days, observe the active degree of rat every day, skin erythema, nasal cavity divide
Secretion is the most normal, diet/amount of drinking water change；Then put to death each group of rat, core, liver, spleen, lung, kidney, intestinal, testis do substantially
Observe, observe internal organs color and luster and whether there is internal organs enlargement situation；Routine pathology section subsequently, paraffin embedding, HE dyes, optics
Whether basis of microscopic observation each internal organs microstructure exists obvious pathological changes.
Except H group rat liver tissue exists slight hepatocyte edema, without other notable untoward reaction, the H put to death after 14 days
In group rat, liver organization is without notable pathological changes, illustrates that above-mentioned hepatocyte pathology is changed to reversible damage, metformin hydrochloride, Sesarmae dehaani
Chrysanthemum lactone composition oral is administered whitening disease model animal without notable toxic action.
Claims (5)
1. one kind is used for treating albinic combination of oral medication, it is characterised in that described combination of oral medication is by medicine
On, the raw material of acceptable adjuvant and following weight ratio is made: wedelolactone 5 ~ 9 weight portion, metformin hydrochloride 1 weight
Part.
The most according to claim 1 for treating albinic combination of oral medication, it is characterised in that described raw material
Weight ratio is: wedelolactone 6 weight portion, metformin hydrochloride 1 weight portion.
The most according to claim 1 for treating albinic combination of oral medication, it is characterised in that described raw material
Weight ratio is: wedelolactone 7 weight portion, metformin hydrochloride 1 weight portion.
The most according to claim 1 for treating albinic combination of oral medication, it is characterised in that described raw material
Weight ratio is: wedelolactone 8 weight portion, metformin hydrochloride 1 weight portion.
5. treat albinic combination of oral medication according to being used for described in Claims 1-4, it is characterised in that described doctor
Pharmaceutically acceptable adjuvant includes titanium dioxide.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610412398.9A CN106038537B (en) | 2016-06-14 | 2016-06-14 | For treating albinic combination of oral medication |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610412398.9A CN106038537B (en) | 2016-06-14 | 2016-06-14 | For treating albinic combination of oral medication |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN106038537A true CN106038537A (en) | 2016-10-26 |
| CN106038537B CN106038537B (en) | 2018-07-27 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610412398.9A Expired - Fee Related CN106038537B (en) | 2016-06-14 | 2016-06-14 | For treating albinic combination of oral medication |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109820849A (en) * | 2019-02-26 | 2019-05-31 | 青岛大学附属医院 | Wedelolactone is preparing the application in the drug for treating fungal keratitis |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008127366A2 (en) * | 2006-10-31 | 2008-10-23 | Warsaw Orthopedic, Inc. | A device and method for treating osteolysis using a drug depot to deliver an anti-inflammatory agent |
| CN103816148A (en) * | 2014-01-28 | 2014-05-28 | 中国药科大学 | Application of wedelolactone in preparation of anti-pulmonary fibrosis drug |
-
2016
- 2016-06-14 CN CN201610412398.9A patent/CN106038537B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008127366A2 (en) * | 2006-10-31 | 2008-10-23 | Warsaw Orthopedic, Inc. | A device and method for treating osteolysis using a drug depot to deliver an anti-inflammatory agent |
| CN103816148A (en) * | 2014-01-28 | 2014-05-28 | 中国药科大学 | Application of wedelolactone in preparation of anti-pulmonary fibrosis drug |
Non-Patent Citations (2)
| Title |
|---|
| HUIMING CHEN ET AL.: "Wedelolactone disrupts the interaction of EZH2-EED complex and inhibits PRC2-dependent cancer", 《ONCOTARGET》 * |
| 梅寒芳等: "蟛蜞菊乙醇提取物促进黑色素生成及其机理的初步研究", 《广东药学院学报》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109820849A (en) * | 2019-02-26 | 2019-05-31 | 青岛大学附属医院 | Wedelolactone is preparing the application in the drug for treating fungal keratitis |
| CN109820849B (en) * | 2019-02-26 | 2022-02-22 | 青岛大学附属医院 | Application of wedelolactone in preparation of medicine for treating fungal keratitis |
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| Publication number | Publication date |
|---|---|
| CN106038537B (en) | 2018-07-27 |
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