CN101084916A - Application of hyaluronate in preparing oral products used for preventing or improving ocular vitreous degeneration disease - Google Patents
Application of hyaluronate in preparing oral products used for preventing or improving ocular vitreous degeneration disease Download PDFInfo
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- CN101084916A CN101084916A CN 200710122971 CN200710122971A CN101084916A CN 101084916 A CN101084916 A CN 101084916A CN 200710122971 CN200710122971 CN 200710122971 CN 200710122971 A CN200710122971 A CN 200710122971A CN 101084916 A CN101084916 A CN 101084916A
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Abstract
The invention relates to the application of hyaluronic acid in preparing product for oral administration for preventing or improving degenerative disease of vitreous body. The invention by using hyaluronic acid for preventing or improving degenerative disease of vitreous body through oral administration has the following advantages: hyaluronic acid can be absorbed through oral administration and reach ocular region organ to resist synchysis and relevant pathological changes caused by molecular weight reduction and/or quantitative reductionof hyaluronic acid in degenerative disease of vitreous body, thereby preventing or improving degenerative disease of vitreous body; and has the advantages of good biocompatibility, and no adverse side effect for oral administration; effectively protect ocular mucous membrane from stimulation and damage, thereby avoiding ocular mucous membrane damage caused by degenerative disease of vitreous body.
Description
Technical field
The present invention relates to glass acid and be used for preventing or improving the application of the Orally taken product of vitreum degenerative disease, belong to health food and medical technical field in preparation.
Background technology
The background technology of glass acid
Glass acid (hyaluonic acid claims hyaluronic acid again), the natural human body that is present in, the macromolecule straight chain mucopolysaccharide of forming for disaccharidase unit by glucuronic acid and N-n acetylglucosamine n.Glass acid is many to be existed and application with its salt form (for example hyaluronic acid sodium).Glass acid has the unique viscoelasticity and the characteristic of non-Newtonian fluid, and has important pharmacological action and physiological function.Water retention is one of topmost physiological function of glass acid, and the long strand of glass acid is woven into netted, in addition with or water formation hydrogen bond, water retention value can reach 1000ml/g, the glass acid that is per 1 gram can be caught the moisture that is equivalent to 1000 times of own vols, moisture is not run off, and give viscoelasticity.Glass acid at present has been widely used in the treatment of ophthalmology, department of dermatologry, surgical diseases or has used as adjuvant, and for example: as the indispensable adjuvant of ophthalmologic operation, supported anterior chamber when being used for ophthalmologic operation reduces damage; Be used for eye drop to improve bioavailability of medicament as media; The replacement therapy treatment of arthritis; Oral beauty treatment etc.
The background technology of vitreous degeneration disease
Vitreum is a kind of special mucus gelatinous tissue, under normal condition, be transparent gel state, constitute by collagen fine fiber webs support that forms and the glass acid molecule that interweaves therein, it 99% is a water, at the vitreous body base portion, the concentration maximum of glass acid and collagen, both make vitreous body have rigidity, viscoelasticity and resistance to compression.Disturb both interactional any factors, all can make the vitreous gel degeneration is liquid, causes degenerative diseases such as liquefaction of vitreous, muscae volitantes, vitreous opacity, vitreous body atrophy, posterior detachment of vitreous.This shows that the destruction of vitreous gel state is the fundamental cause of vitreous degeneration.In vitreous body, glass acid plays a part the most key to keeping Vitrea viscoelasticity and resistance to compression, in case the glass acid number amount in the vitreous body reduces or depolymerization takes place, and all can cause vitreous gel to become liquid, thereby cause the generation of vitreous degeneration disease.
The people who suffers from the vitreous degeneration disease at present is more and more, be more common in old people and high myopia patient in the past, but recent findings, incidence rate light in child and the teenager, medium myopia patient vitreous degeneration is also quite high, and the age is big more, the course of disease is long more, refractive diopter is high more, and its degree also increases the weight of thereupon.The vitreous degeneration disease is a progressive process, as can not get correct treatment in time, may produce serious consequence.Current, the vitreous degeneration treatment of diseases is adopted Drug therapy and operative treatment more, Drug therapy mainly reaches the purpose of improvement by the absorption that promotes liquefaction, and curative effect is limited, can not Vitrea liquefaction of facedown and relevant diseases.
According to the above-mentioned reason that causes the vitreous degeneration disease, if can effectively replenish macromole glass acid in the eye vitreous body, the minimizing that resists the degraded of glass acid molecule amount in the vitreous body and quantity is reasonably prevention and improvement means.But because the effect of eye barrier, by external for example the mode of eye drip can't arrive vitreum and play a role, still need and will seek new approach.
Summary of the invention
The purpose of this invention is to provide glass acid and be used for preventing or improving the application of the Orally taken product of vitreum degenerative disease, promptly be used for prevention or improve the vitreum degenerative disease by oral glass acid product in preparation.
The inventor is by discovering for many years, and glass acid can be by oral absorption, and can be assigned to eye organ, and the degraded of macromole glass acid or the minimizing of quantity in the acid of facedown eye glass are used for prevention or improve the vitreum degenerative disease.
Vitreous degeneration disease among the present invention includes but not limited to liquefaction of vitreous, muscae volitantes, vitreous opacity etc., refers in particular to vitreous opacity.
Except that containing glass acid, also contain adjunct ingredient in the Orally taken product of the present invention.Adjunct ingredient is meant excipient, stabilizing agent, antiseptic, antioxidant, emulsifying agent, correctives, coating materials of medicine and field of health care food routine etc.
Can add other active component in the Orally taken product of the present invention, other active component are meant the material that prevents or improve the vitreum degenerative disease that has except that glass acid, include but not limited to vitamin A, carotene, glucocorticoid and Chinese medicine such as Radix Puerariae, Hai Bu etc.
Glass acid is the acid of macromole glass in the Orally taken product of the present invention, and its molecular weight ranges is 500,000～5,000,000, preferred 1,000,000～3,000,000.
Because the many forms with its salt of glass acid are used, so related glass acid comprises glass acid and physiologically acceptable salt thereof among the present invention, hyaluronic acid sodium etc. for example.
Orally taken product of the present invention can be made various oral formulations by conventional method well known in the art, includes but not limited to tablet, granule, oral liquid, capsule, soft capsule etc.
The content of glass acid is in the Orally taken product of the present invention: in 100 gram Orally taken products, glass acid is 0.05～90 gram, preferred 0.1～50 gram, more preferably 0.3～20 gram, most preferably 0.5～10 gram can be chosen wantonly in the Orally taken product of the present invention and comprises an amount of other active substances and adjuvant.
The present invention takes glass acid through port in prevention or improves the vitreum degenerative disease and has the following advantages: 1) glass acid can be passed through oral absorption, reach each organ of eye, directly replenish the macromole glass acid in the vitreum, the reduction of glass acid molecule amount and/or the caused liquefaction of vitreous of minimizing and the relevant diseases of quantity in the antagonism vitreum degenerative disease, with this purpose that reaches prevention or improve the vitreum degenerative disease, its good biocompatibility, oral having no side effect.2) glass acid has the mucosa protective effect, can effectively protect after oral a mucosa to avoid stimulating and damage, thus the eye mucosa injury of avoiding the degenerated eye disease to cause.
The specific embodiment
Now provide following examples to further specify the present invention, but scope of the present invention never is limited to following examples.
[application example of formulations]
Embodiment 1: the glass acid oral capsule that is used to prevent or improve the vitreum degenerative disease: in 100 grams, wherein hyaluronic acid sodium (molecular weight is 1,200,000) 20 grams, hydroxypropyl emthylcellulose 80 restrain.Insert in the capsulae vacuus, promptly by conventional method.
Embodiment 2: the glass acid oral tablet that is used to prevent or improve the vitreum degenerative disease: in 100 gram oral tablets, wherein hyaluronic acid sodium (molecular weight is 800,000) 3.5 restrains, starch slurry is an amount of, starch is an amount of, magnesium stearate is an amount of, dried starch is an amount of.Make tablet by the conventional method pelletizing press sheet.
Embodiment 3: the glass acid oral liquid that is used to prevent or improve the vitreum degenerative disease: in 100 gram oral liquids, wherein hyaluronic acid sodium (molecular weight 1,800,000) 0.1 restrains, antiseptic is an amount of, water is an amount of.Be prepared into oral liquid by conventional method.
Embodiment 4: the glass acid oral tablet that is used to prevent or improve the vitreum degenerative disease: in 100 gram tablets, wherein hyaluronic acid sodium (molecular weight 2,000,000) 10 restrains, starch slurry is an amount of, starch is an amount of, magnesium stearate is an amount of, dried starch is an amount of.Make tablet by the conventional method pelletizing press sheet.
[experimentation]
Test 1: the confirmation of glass acid oral absorption
Animal and grouping: 20 of rats, divide 2 groups at random, 10 every group.Be respectively normal saline matched group and glass acid group.Fasting (can't help water) is 12 hours before the rat experiment, and lumbar injection pentobarbital sodium 40mg/kg body weight is anaesthetized, and it is the 20mg/kg body weight that glass acid group filling stomach gives glass acid dosage, and glass acid is used normal saline solution before irritating stomach.The dosage that normal saline matched group filling stomach gives normal saline is the 10ml/kg body weight.
The result: peak value does not appear in the concentration of glass acid in the serum of normal saline matched group, oral normal saline is described to not influence of the glass acid concentration in the serum, and it also is rational coming the solution of formulate glass acid to experimentize with it.And glass acid oral after, peak value all appears in the glass acid concentration in the serum, supposition is the absworption peak of HA, and C
MaxAppear at about 7 hours.The results are shown in Table 1.
The content (ng/mL) of glass acid in the serum of oral glass acid of table 1 rat and normal saline (n=10,
)
| Oral back time/hour | The normal saline group | |
| 0 1 2 4 7 10 12 | 100.58±17.33 99.96±6.17 89.48±37.17 93.05±29.47 90.82±32.12 91.06±30.30 95.34±28.87 | 126.57±30.75 114.96±31.06 135.07±23.82 124.82±22.52 372.27±70.73 * 237.93±26.16 * 175.47±33.82 |
Annotate: compare with value before the medicine on the same group,
*There is the utmost point significant difference P＜0.001
As can be seen from Table 1, glass acid can be by oral absorption.
Test 2: the distribution situation of the oral back of glass acid in tissue
Method: glass is sour to be used [
125I] carry out labelling, investigate its increased radioactivity in vivo.
Animal and grouping: 32 of mices are divided into 4 groups, 8 every group at random.Fasting (can't help water) is 12 hours before the mouse experiment, and the chemical dose that each group filling stomach gives glass acid is that 60mg/kg, radiological dose are 1.06 * 10
5The cpm/g body weight (is min
-1/ g body weight), respectively at one group of mice of execution in 1,4,12 and 24 hour behind the medicine, dissect immediately, the organ of getting has: eyeball, brain, skin, testis, skeletal muscle, fat, liver, spleen, kidney, lung, the heart, small intestinal, glandular stomach, every mice is taken a sample at fixed position respectively.Investigate the distribution situation of glass acid in each tissue, represent that with ID (%)/g promptly every 1g organizes the radioactivity of intake to account for the percentage rate of oral dose.
As shown in Figure 1, [
125I]-glass acid is after oral 1 hour, examined the increased radioactivity that all has in the tissue in various degree 13 of mices.Because [
125I]-glass acid after oral 1 hour the radioactivity in the serum reach absworption peak, prompting [
125I]-glass acid can be rapidly be distributed in each tissue through blood, comprises eyeball.
Description of drawings: Fig. 1 represent mice oral [
125I]-glass acid after, glass acid is in mice body radioactivity distribution situation.
Test 3: the embodiment of the invention 1 is improved the clinical research of vitreum muddiness
Treatment target: 190 of 100 routine vitreous opacity patients suffer from eye, and wherein male 62 examples are suffered from eye for 138, and women 38 examples are suffered from eye for 52. 21～80 years old age, 21～40 years old 26 example wherein, 40～70 years old 69 example, 5 examples more than 70 years old.
Methods for the treatment of: 1 time oral 2 (40 milligrams of about Hyaluronic Acids), 3 times on the 1st, 3 months was 1 course for the treatment of.
Criterion of therapeutical effect: cure-drift disappears at the moment, change without unusual in the funduscopy vitreum; Produce effects-drift obviously reduces at the moment, the minimizing that diminishes of funduscopy vitreum internal haze thing; Take a turn for the better-drift quantity reduces at the moment, and density lowers, and funduscopy vitreum internal haze thing reduces; Unchanged before and after invalid-drift treatment at the moment.
Treatment results: cure 52 eyes, account for 27.4%; 63 eyes of produce effects account for 33.1%; 69 eyes that take a turn for the better account for 36.3%; Invalid 6 eyes account for 3.2%. Total effective rate is 96.8%.
Claims (6)
1, glass acid is used for preventing or improving the application of the Orally taken product of vitreum degenerative disease in preparation.
2, the described application of claim 1, wherein Orally taken product is any dosage form that can be oral.
3, the described application of claim 1, wherein Orally taken product is health food or medicine.
4, the arbitrary described application of claim 1-3, wherein said glass acid comprise glass acid and physiologically acceptable salt thereof, and its molecular weight ranges is 500,000～5,000,000, preferred 1,000,000～3,000,000.
5, the arbitrary described application of claim 1-3 wherein in 100 gram products, contains glass acid 0.05～90 gram, preferred 0.1～50 gram, more preferably 0.3～20 gram, most preferably 0.5～10 gram.
6, the arbitrary described application of claim 1-5 wherein contains an amount of other active component and adjuvant in the Orally taken product.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2007101229713A CN100508987C (en) | 2007-07-06 | 2007-07-06 | Application of hyaluronate in preparing oral products used for preventing or improving ocular vitreous degeneration disease |
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|---|---|---|---|
| CNB2007101229713A CN100508987C (en) | 2007-07-06 | 2007-07-06 | Application of hyaluronate in preparing oral products used for preventing or improving ocular vitreous degeneration disease |
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| CN101084916A true CN101084916A (en) | 2007-12-12 |
| CN100508987C CN100508987C (en) | 2009-07-08 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103316032A (en) * | 2013-05-24 | 2013-09-25 | 凌霄 | A hydroxytyrosol composition and applications thereof |
-
2007
- 2007-07-06 CN CNB2007101229713A patent/CN100508987C/en active Active
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103316032A (en) * | 2013-05-24 | 2013-09-25 | 凌霄 | A hydroxytyrosol composition and applications thereof |
| CN103316032B (en) * | 2013-05-24 | 2016-08-17 | 凌霄 | Compositions containing hydroxytyrosol and application thereof |
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| Publication number | Publication date |
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| CN100508987C (en) | 2009-07-08 |
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Effective date of registration: 20181228 Address after: 250101 989 Xinjie street, Ji'nan high tech Zone, Shandong Patentee after: Pharmaceutical Sciences, Shandong Province Address before: 250014 No. 264 Shanda Road, Lixia District, Jinan City, Shandong Province Patentee before: Ling Peixue |