CN1698619A - Oleanolic acid preparation, its formula and preparing method thereof - Google Patents
Oleanolic acid preparation, its formula and preparing method thereof Download PDFInfo
- Publication number
- CN1698619A CN1698619A CN 200510073072 CN200510073072A CN1698619A CN 1698619 A CN1698619 A CN 1698619A CN 200510073072 CN200510073072 CN 200510073072 CN 200510073072 A CN200510073072 A CN 200510073072A CN 1698619 A CN1698619 A CN 1698619A
- Authority
- CN
- China
- Prior art keywords
- oleanolic acid
- agent
- sodium
- prescription
- preparation
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Landscapes
- Medicinal Preparation (AREA)
Abstract
The invention relates to an oleanolic acid preparation, its formula and preparing process, wherein the new dosages types include soft capsule, dispersible tablet and oral liquid. In the prescription, each item of the soft capsule, dispersible tablet and each 10ml of the oral liquid contains oleanolic acid 5-100mg, preferably 10-80mg, the invention can increase the dissolution rate and bioavailability of the oleanolic acid, thus improves the curative effect.
Description
Technical field the present invention relates to pharmaceutical new oleanolic acid preparation and prescription and preparation method.
Background technology oleanolic acid (Oleanolic Acid) is a pentacyclic triterpenoid, chemical name is 3-hydroxyl-3 β-olive-12-alkene-28-acid, it is the active drug composition that is distributed widely in the multiple natural plants such as Herba Swertiae Mileensis, Fructus Ligustri Lucidi, Cortex araliae chinensis, has multiple pharmacological effect, enzyme, blood sugar lowering, blood fat reducing, antiplatelet aggregation, arteriosclerosis, antiinflammatory, antiviral, raise immunity, anti-peroxidation, mutation, effect such as anticancer are fallen as hepatoprotective, diseases such as treatment acute, chronic hepatitis now have been widely used in, good effect, side effect is low.
The preparation of the present oleanolic acid that gone on the market has tablet and capsule.Because oleanolic acid is difficult for being dissolved in water, the medicine dissolution rate is slow, absorbs badly in the body, tablet and capsule bioavailability are low, weak curative effect (Wang Lixin etc. the chemistry of oleanolic acid and pharmacological research. pharmacy practice magazine, 2001,19 (2): 104; Tian Liting etc. the pharmacological research overview of oleanolic acid. CHINA JOURNAL OF CHINESE MATERIA MEDICA, 2002,27 (12): 884), domestic for this reason Experimental Development once Olea acid dropping balls and solid dispersion, to improve bioavailability and curative effect.
Summary of the invention the present invention is intended to overcome the existing low problem of oleanolic acid preparation bioavailability, prepared new oleanolic acid preparation, dosage form comprises soft capsule, dispersible tablet and oral administration solution, these new oleanolic acid preparations have improved the dissolution and the bioavailability of oleanolic acid, thereby have improved curative effect.
Each dosage form prescription of oleanolic acid preparation that the present invention is new, every of soft capsule, every of dispersible tablet, oral administration solution every (10ml) contain oleanolic acid 5mg～100mg, best 10mg～80mg in the prescription.
The oleanolic acid soft capsule that the present invention is new, also contain lytic agent, emulsifying solubilizing agent, antioxidative stabilizer in the prescription, specifically can be Herba Silybi mariani oil, Oleum Hippophae, refined soybean oil, refining Oleum Arachidis hypogaeae semen, Radix Oenotherae erythrosepalae oil, Oleum Vitis viniferae, sunflower seed wet goods vegetable oil, emulsifying solubilizing agents such as soybean phospholipid, lecithin, polyglycerin ester, sucrose ester, antioxidative stabilizers such as vitamin E, ascorbyl palmitate.These adjuvants can be multiple mix in varing proportions and use, total addition be recipe quantity 40～90%, be preferably 75～85%.Adding these adjuvants can increase the dissolubility of oleanolic acid in vegetable oil, improves the dissolution and the bioavailability of oleanolic acid, and then improves the therapeutic effect of oleanolic acid, also can improve the stability of oleanolic acid simultaneously.The soft capsule shell adopts gelatin, glycerol, sorbitol etc. to make, and the titanium dioxide of adding gelatin weight 0.2～1.2%, best 0.5～0.7% is made opacifier.During preparation oleanolic acid is added in the mixed liquor of vegetable oil, emulsifying solubilizing agent and antioxidative stabilizer, stirs, heating makes material dissolution or mix homogeneously, and pelleting in pellet processing machine is finalized the design after drying promptly then.
The oleanolic acid dispersible tablet agent that the present invention is new, also contain diluent in the prescription, disintegrating agent, surfactant, adhesive, correctives and lubricant, specifically can be starch, dextrin, pregelatinized Starch, carboxymethylstach sodium, microcrystalline Cellulose, hyprolose, hypromellose, carmethose, polyethylene glycol 6000, basic amino acid such as lysine and arginine, potassium carbonate, potassium bicarbonate, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate, sucrose, glycyrrhetate, aspartame, Folium Stevlae Rebaudianae, spice, 30 POVIDONE K 30 BP/USP 30, silica sol, Pulvis Talci, magnesium stearate etc., these adjuvants can multiplely mix use in varing proportions.Diluent, adhesive, disintegrating agent, the total addition of surfactant be recipe quantity 20～90%, best 40～70) %; The total addition of correctives is 1～10%, best 2～9% of a recipe quantity; The total addition of lubricant is 0.5～5%, best 1～4.5% of a recipe quantity.With the fine powder mix homogeneously of oleanolic acid and diluent, disintegrating agent, surfactant, produce wet granular during preparation with an amount of adhesive, in 60 ℃ of aeration-dryings, granulate, it is even to add correctives and mix lubricant, and tabletting is promptly.
The oleanolic acid oral administration solution that the present invention is new also contains lytic agent, cosolvent, stabilizing agent, sweeting agent and fragrant correctives in the prescription.Lytic agent can be purified water, PEG400 etc.; Cosolvent can be basic amino acid such as lysine and arginine, sodium hydroxide, potassium carbonate, potassium bicarbonate, sodium carbonate, sodium bicarbonate etc.; Stabilizing agent can be sodium benzoate, sodium citrate, potassium citrate, sodium sorbate, potassium sorbate, disodium edetate etc.; Sweeting agent can be sucrose, glucose, xylitol, sorbitol, mannitol, lactose, glycyrrhetate, steviosin, saccharin sodium etc.; The fragrance correctives can be natural and synthetic spice, as fragrant perfumes such as Fructus Musae, Herba Menthae, Fructus Mali pumilae, Fructus Citri tangerinae, Fructus Fragariae Ananssae, chocolate, Rhizoma et radix valerianae, Fructus Vitis viniferae, Fructus Pruni pseudocerasis.These adjuvants can multiplely mix use in varing proportions, and except that purified water, other lytic agent, stabilizing agent, sweeting agent and the total addition of fragrant correctives are 5～75%, best 10～70% of recipe quantity.During preparation oleanolic acid is added in the lytic agent, the dissolving of adding cosolvent adds other adjuvant mixed dissolution again, filters the back and adds purified water to prescribed volume, and fill is in oral liquid bottle, and gland is sterilized, and packing promptly.
Specific embodiment the present invention can be illustrated with the following examples.
Embodiment 1, the oleanolic acid soft capsule:
Prescription: oleanolic acid 20g
Vitamin E 20g
Soybean phospholipid 100g
Herba Silybi mariani oil 600g
Oleum Hippophae 600g
Refined plant oil 660g
Make 1000
Preparation method: 1. soft capsule content preparation: oleanolic acid is added in the mixed liquor of Oleum Hippophae, Herba Silybi mariani oil, refined plant oil, vitamin E and soybean phospholipid, stirring, heating make material dissolution or mix homogeneously, put and are chilled to room temperature.2. soft capsule shell preparation: get a certain proportion of gelatin, glycerol, purified water and prepare according to a conventional method, and add the titanium dioxide of gelatin weight 0.2～1.2%, mix homogeneously, and in 60 ℃ of insulations.3. soft capsule preparation: in pellet processing machine, finalize the design in the rearmounted cylinder of pelleting, be placed in the hothouse of 30～40 ℃ of temperature aeration-drying promptly.
Embodiment 2, oleanolic acid dispersible tablet:
Prescription: oleanolic acid 20g
Arginine 15g
Microcrystalline Cellulose 10g
Carboxymethylstach sodium 8g
Hyprolose 6g
Silica sol 3g
Starch 20g
Glycyrrhetate 10g
80% ethanol liquid of 10% 30 POVIDONE K 30 BP/USP 30 is an amount of
Spice is an amount of
Sodium lauryl sulphate 0.5g
Polyethylene glycol 6000 4g
Make 1000
Preparation method: the fine powder mix homogeneously that takes by weighing oleanolic acid, arginine, microcrystalline Cellulose, carboxymethylstach sodium, hyprolose, silica sol, starch and glycyrrhetate, the 80% ethanol liquid that adds 10% 30 POVIDONE K 30 BP/USP 30, granulate with 14 order nylon wires, wet granular is dry down in 60 ℃, in dried granule, add spice, sodium lauryl sulphate and polyethylene glycol 6000, mixing is with 12 order nylon wire granulate, controlled pressure 4～5kg/cm behind the mixing
2Tabletting promptly.
Embodiment 3, the oleanolic acid oral administration solution:
Prescription: oleanolic acid 3g
Lysine 5g
Sucrose 100g
Glycyrrhetate 3g
Disodium edetate 0.5g
Potassium sorbate 1g
Spice is an amount of
PEG400 50ml
Purified water is an amount of
Make 1000ml
Preparation method: oleanolic acid is added in purified water and the PEG400, add lysine and make dissolving, add sucrose, glycyrrhetate, disodium edetate, potassium sorbate and spice mixed dissolution again, filter, add purified water to prescribed volume, fill in oral liquid bottle, gland, sterilization, packing promptly.
The new oleanolic acid preparation that above embodiment makes meets under the Chinese Pharmacopoeia rules of preparations item prescription to this dosage form.
Claims (7)
1, new oleanolic acid preparation and prescription and preparation method.Characteristics are to have improved the dissolution and the bioavailability of oleanolic acid.
2, the described new oleanolic acid preparation formulation of claim 1 comprises soft capsule, dispersible tablet and oral administration solution.
3, the prescription and the preparation method of described new each dosage form of oleanolic acid preparation of claim 1 and claim 2.
4, claim 1 is to each dosage form prescription of the described new oleanolic acid preparation of claim 3, and every of soft capsule, every of dispersible tablet, oral administration solution every (10ml) contain oleanolic acid 5mg～100mg, best 10mg～80mg in the prescription.
5, claim 1 is to the described new oleanolic acid soft capsule of claim 4, also contain lytic agent, emulsifying solubilizing agent, antioxidative stabilizer in the prescription, specifically can be Herba Silybi mariani oil, Oleum Hippophae, refined soybean oil, refining Oleum Arachidis hypogaeae semen, Radix Oenotherae erythrosepalae oil, Oleum Vitis viniferae, sunflower seed wet goods vegetable oil, emulsifying solubilizing agents such as soybean phospholipid, lecithin, polyglycerin ester, sucrose ester, antioxidative stabilizers such as vitamin E, ascorbyl palmitate.These adjuvants can be multiple mix in varing proportions and use, total addition be recipe quantity 40～90%, be preferably 75～85%.The soft capsule shell adopts gelatin, glycerol, sorbitol etc. to make, and the titanium dioxide of adding gelatin weight 0.2～1.2%, best 0.5～0.7% is made opacifier.During preparation oleanolic acid is added in the mixed liquor of vegetable oil, emulsifying solubilizing agent and antioxidative stabilizer, stirring, heating make material dissolution or mix homogeneously, and pelleting in pellet processing machine is finalized the design after drying promptly then.
6, claim 1 is to the described new oleanolic acid dispersible tablet of claim 4, also contain diluent in the prescription, disintegrating agent, surfactant, adhesive, correctives and lubricant, specifically can be starch, dextrin, pregelatinized Starch, carboxymethylstach sodium, microcrystalline Cellulose, hyprolose, hypromellose, carmethose, polyethylene glycol 6000, basic amino acid such as lysine and arginine, potassium carbonate, potassium bicarbonate, sodium carbonate, sodium bicarbonate, sodium lauryl sulphate, sucrose, glycyrrhetate, aspartame, Folium Stevlae Rebaudianae, spice, 30 POVIDONE K 30 BP/USP 30, silica sol, Pulvis Talci, magnesium stearate etc., these adjuvants can multiplely mix use in varing proportions.Diluent, adhesive, disintegrating agent, the total addition of surfactant are 20～90%, best 40～70% of recipe quantity; The total addition of correctives is 1～10%, best 2～9% of a recipe quantity; The total addition of lubricant is 0.5～5%, best 1～4.5% of a recipe quantity.With the fine powder mix homogeneously of oleanolic acid and diluent, disintegrating agent, surfactant, produce wet granular during preparation with an amount of adhesive, in 60 ℃ of aeration-dryings, granulate, it is even to add correctives and mix lubricant, and tabletting is promptly.
7, claim 1 also contains lytic agent, cosolvent, stabilizing agent, sweeting agent and fragrant correctives to the described new oleanolic acid oral administration solution of claim 4 in the prescription.Lytic agent can be purified water, PEG400 etc.; Cosolvent can be basic amino acid such as lysine and arginine, sodium hydroxide, potassium carbonate, potassium bicarbonate, sodium carbonate, sodium bicarbonate etc.; Stabilizing agent can be sodium benzoate, sodium citrate, potassium citrate, sodium sorbate, potassium sorbate, disodium edetate etc.; Sweeting agent can be sucrose, glucose, xylitol, sorbitol, mannitol, lactose, glycyrrhetate, steviosin, saccharin sodium etc.; The fragrance correctives can be natural and synthetic spice, as fragrant perfumes such as Fructus Musae, Herba Menthae, Fructus Mali pumilae, Fructus Citri tangerinae, Fructus Fragariae Ananssae, chocolate, Rhizoma et radix valerianae, Fructus Vitis viniferae, Fructus Pruni pseudocerasis.These adjuvants can multiplely mix use in varing proportions, and except that purified water, other lytic agent, stabilizing agent, sweeting agent and the total addition of fragrant correctives are 5～75%, best 10～70% of recipe quantity.During preparation oleanolic acid is added in the lytic agent, the dissolving of adding cosolvent adds other adjuvant mixed dissolution again, filters the back and adds purified water to prescribed volume, and fill is in oral liquid bottle, and gland is sterilized, and packing promptly.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510073072 CN1698619A (en) | 2005-05-31 | 2005-05-31 | Oleanolic acid preparation, its formula and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510073072 CN1698619A (en) | 2005-05-31 | 2005-05-31 | Oleanolic acid preparation, its formula and preparing method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1698619A true CN1698619A (en) | 2005-11-23 |
Family
ID=35474970
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200510073072 Pending CN1698619A (en) | 2005-05-31 | 2005-05-31 | Oleanolic acid preparation, its formula and preparing method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1698619A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103550235A (en) * | 2013-10-26 | 2014-02-05 | 苏州天南星生物科技有限公司 | Preparation for preventing or treating liver injury |
| CN103599108A (en) * | 2013-11-20 | 2014-02-26 | 中山大学 | Application of oleanolic acid in preparing medicament for preventing and treating cholestasis |
| CN109985014A (en) * | 2019-05-17 | 2019-07-09 | 贵州天安药业股份有限公司 | Hydrochloric acid glitazone dispersion piece is used in a kind for the treatment of of diabetes B |
-
2005
- 2005-05-31 CN CN 200510073072 patent/CN1698619A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103550235A (en) * | 2013-10-26 | 2014-02-05 | 苏州天南星生物科技有限公司 | Preparation for preventing or treating liver injury |
| CN103599108A (en) * | 2013-11-20 | 2014-02-26 | 中山大学 | Application of oleanolic acid in preparing medicament for preventing and treating cholestasis |
| CN109985014A (en) * | 2019-05-17 | 2019-07-09 | 贵州天安药业股份有限公司 | Hydrochloric acid glitazone dispersion piece is used in a kind for the treatment of of diabetes B |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2023073349A (en) | Capsule and powder formulations containing lanthanum compounds | |
| KR20070119700A (en) | Formulations containing fenofibrate and surfactant mixture | |
| CN100477991C (en) | Oral formulation of neogambogic acid for treating tumor | |
| CA3152326C (en) | Preparation of transmucosal psychoactive alkaloid composition | |
| WO2008083561A1 (en) | Oral pharmaceutical composition of glycyrrhizin or its salts and the preparation method thereof | |
| US20120029064A1 (en) | formulation of silibinin with high efficacy and prolonged action and the preparation method thereof | |
| CN102470121B (en) | Pharmaceutical compositions comprising dronedarone | |
| CN104922143B (en) | The composition and its preparation method and application of EGCG and chitosan oligosaccharide | |
| JP2013512948A (en) | Solid dispersion comprising 20-O-β-D-glucopyranosyl-20 (S) -protopanaxadiol | |
| CN1698619A (en) | Oleanolic acid preparation, its formula and preparing method thereof | |
| CN112972404A (en) | Sildenafil freeze-dried orally disintegrating tablet and preparation method thereof | |
| CN1762341B (en) | Salvianolic acid compound for treating cardiovascular and cerebrovascular disease and liver disease, and application thereof | |
| CN102085238B (en) | Lipid preparation containing radix gentianae totalglycoside-phospholipid complexes and preparation method thereof | |
| CN1943734A (en) | A Chinese traditional medicine for clearing away heat and toxic material | |
| CN1561992A (en) | Precursor liposome preparation containing silybum marianum extract and its preparing process | |
| CN101081227B (en) | Composition of diammonium glycyrrhizinate | |
| CN102697765B (en) | Ranitidine hydrochloride/bismuth potassium citrate pharmaceutical composition solid lipid nanoparticles preparation | |
| KR20190083770A (en) | Composition for prevention and treatment of liver disease containing milk thistle with improved dissolution rate | |
| CN106943390B (en) | Application of the Strychnos nux-vomica aglycon in preparation prevention or treatment antiarrhythmic medicament | |
| CN1228051C (en) | Medicinal composition for treating cardiovascular disease | |
| CN1850206A (en) | Medicine for treating women's climateric syndrome and preparing method | |
| US20100034887A1 (en) | Bursting Pellets | |
| CN1383817A (en) | oral breviscapine slow release preparation | |
| CN1969861A (en) | Sustained release system of clozapine solid liposome microparticle | |
| CN1820749A (en) | Formula of amoxycillin sodium/ambroxo/ hydrochloride powder injection and its preparing method |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |