CN105434389A - Topiroxostat controlled-release tablet and preparation method thereof - Google Patents
Topiroxostat controlled-release tablet and preparation method thereof Download PDFInfo
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- CN105434389A CN105434389A CN201510886865.7A CN201510886865A CN105434389A CN 105434389 A CN105434389 A CN 105434389A CN 201510886865 A CN201510886865 A CN 201510886865A CN 105434389 A CN105434389 A CN 105434389A
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- controlled
- holder
- controlled release
- release
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
- A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses a topiroxostat controlled-release tablet and a preparation method thereof. The topiroxostat controlled-release tablet is composed of a drug-containing tablet core and a coating membrane layer covering the drug-containing tablet core, the drug-containing tablet core comprises topiroxostat, a filling agent and sodium chloride, and the coating membrane layer comprises a controlled-release material, plasticizer and a pore-foaming agent. During preparation, the drug-containing tablet core is wrapped with the coating membrane layer, and the topiroxostat controlled-release tablet is obtained. The topiroxostat controlled-release tablet and the preparation method thereof are characterized in that the topiroxostat controlled-release tablet is composed of a quick-release part and a controlled-release part; after the topiroxostat controlled-release tablet enters a human body, the quick-release part is released rapidly, a certain plasma concentration is achieved, the controlled-release part is released slowly, the certain plasma concentration is maintained, good drug efficacy can be achieved, and the side effect of the drug can be effectively avoided. The topiroxostat controlled-release tablet has the advantages of being rapid to dissolve, rapid to absorb, high in bioavailability, good in stability, convenient to take and the like, and therefore the side effect brought by taking the drug to a patient is reduced. The preparation technology is simple, the obtained product is stable in quality, and the preparation method is suitable for large-scale production.
Description
Technical field
The present invention relates to a kind of technical field of chemical medicine controlled release tablet, particularly relate to a kind of holder and take charge of his controlled release tablet, the invention still further relates to the preparation method of this controlled release tablet.
Background technology
Uric acid is the normal products of metabolism of purine nucleotide, when uricopoiesis too much and underexcretion time, in blood, uric acid increases to over and namely forms hyperuricemia normal range; Uric acid major sedimentary too much in blood in joint, cartilage, sub-dermal soft tissue and kidney, cause the complex clinical such as arthritis and nephropathy to show, be namely referred to as gout, thus hyperuricemia and uric acid to deposit in organ-tissue be the basic pathogenesis of gout.And the cause of disease causing uric acid to raise is comparatively complicated, constitutional and the large class of Secondary cases two can be divided into.
Along with the raising of people's living standard, the improvement of nutritional condition, take in animal proteinum, the increase of fat and the change (drink, smoking etc.) of life-form structure, the sickness rate of hyperuricemia and gout rises gradually, age of onset in advance, hyperuricemia can cause the formation of gouty acute arthritis recurrent exerbation, tophus, tophaceous arthritis and joint deformity, involving kidney causes chronic interstitial nephritis and uric acid kidney stones to be formed, normal increase patient suffering, and have a strong impact on patients ' life quality.
At present, China's patient with gout still constantly increases, and present the trend spread to becoming younger, therefore gout class medicine is very large in China market potentiality, but gout class medicine mostly in the market is old medicine, though cheap but side effect is obvious, if there is new medicine to release in good time, market prospect is by considerable.
Holder takes charge of him all has significant inhibitory action to the xanthine oxidase of oxidized form and reduced form, and thus its effect reducing uric acid is more powerful, lasting, and therefore this product can be used for the chronic hyperuricemia for the treatment of gout.Two advantages are had: 1) allopurinol only has inhibitory action to the xanthine oxidase of reduced form compared with allopurinol, and he all has significant inhibitory action to the xanthine oxidase of oxidized form and reduced form to hold in the palm a department, thus its effect reducing uric acid is more powerful, lasting; 2) because allopurinol is purine analogue, inevitably cause the impact relating to purine and other enzymatic activitys of pyridine metabolism, therefore in allopurinol treatment, need to repeat heavy dose of administration to maintain higher levels of drugs, also bring the serious even fatal untoward reaction caused by drug accumulation thus.And he is non-purines xanthine oxidase inhibitor to hold in the palm a department, therefore there is better safety.
Summary of the invention
Current China market mainly contains holder department his oral tablet, tablet, and injection, although oral tablet and tablet taking convenience, but be subject to the impact of the factor such as disintegrate, drug release, assimilation effect is undesirable, although and injection curative effect is fast, carry, use all inconveniences, and he is also unstable in aqueous to hold in the palm a department.
In recent years, the research and development of controlled release tablet come into one's own gradually, and controlled release tablet is that release by time effects constant release, can not obtain more stable blood drug level by the release of zero-order rule, and " peak valley " fluctuation is less, until basic absorption is complete.Controlled release tablet can make patient reduce medicining times, administration frequency reduces half than ordinary preparation, facilitate patient's Long-term taking medicine, significantly improve the compliance of patient consumes, by the control of drug release rate, medicine slowly absorbs with suitable speed, make blood drug level steady, avoid or reduce peak valley phenomenon, contribute to the toxic and side effects and the raising curative effect that reduce medicine, reduce medicine at gastrointestinal local concentration, reduce zest.
In order to overcome the deficiencies in the prior art, the present invention is by lot of experiments to adjuvant screening and process optimization, and provide a kind of holder to take charge of his controlled release tablet, this controlled release tablet steady quality, drug release is even, and preparation technology is simple.
For achieving the above object, the technical scheme taked of the present invention:
(1) his controlled release tablet of a kind of holder department, by pastille label be wrapped in its outer coatings rete and form, described pastille label comprises a holder department he, filler and osmotic pressure active substance, and described coating rete comprises controlled-release material, plasticizer and porogen.
(2) according to his controlled release tablet of holder according to claim 1 department, it is characterized in that controlled release portion is made up of rapid release and controlled release two parts, wherein immediate release section is containing his 2 ~ 5mg of a holder department, and controlled release portion is containing his 10 ~ 15mg of a holder department.
(3) according to the controlled release tablet of claim 2, wherein immediate release section is containing holder his 5mg of department, and controlled release portion is containing his 15mg of a holder department.
(4) take charge of his controlled release tablet according to holder according to claim 1, it is characterized in that: described filler is lactose; Described osmotic pressure active substance is sodium chloride; Described controlled-release material is at least one in ethyl cellulose, methylcellulose and polyvinyl alcohol; Described plasticizer is triethyl citrate; Described porogen is dextrin.
(5) take charge of his controlled release tablet according to holder according to claim 4, it is characterized in that: described controlled-release material is ethyl cellulose and methylcellulose.
(6) take charge of his controlled release tablet according to holder according to claim 4, it is characterized in that: the weight ratio of described ethyl cellulose and described methylcellulose is 2:1.
Holder of the present invention his controlled release tablet of department can be prepared as follows:
(1) get holder department he, a filler to mix homogeneously with osmotic pressure active substance, with 85% ethanol for binding agent, make soft material, 18 ~ 24 mesh sieves are granulated, and tabletting after dry, obtains pastille label;
(2) with 80% dissolve with ethanol controlled-release material, plasticizer and porogen, make controlled release coat liquid;
(3) the controlled release coat liquid prepared evenly is sprayed at the pastille wicking surface that step (1) prepares, obtains holder after drying and take charge of his controlled release tablet.
Holder of the present invention his controlled release tablet of department has following beneficial effect:
(1) after controlled release tablet of the present invention enters human body, immediate release section discharges rapidly, reaches certain blood drug level, and controlled release portion slow releasing maintains certain blood drug level, not only can play good drug effect and effectively can avoid drug side effect again.
(2) the present invention has the advantages such as stripping is rapid, absorption is fast, bioavailability is high, good stability, taking convenience, thus the side effect that minimizing drug administration brings to patient, and preparation technology is simple, products obtained therefrom steady quality, applicable large-scale production.
Detailed description of the invention
Be further described the specific embodiment of the present invention below in conjunction with embodiment, advantage and disadvantage of the present invention will be more clear along with description.But these embodiments are only exemplary, do not form any restriction to scope of the present invention.It will be understood by those skilled in the art that and can modify to the details of technical solution of the present invention and form or replace down without departing from the spirit and scope of the present invention, but these amendments and replacement all fall within the scope of protection of the present invention.
Embodiment 1
Prescription 1(is by 1000)
His 20g is taken charge of in holder
Lactose 32g
Sodium chloride 40g
Ethyl cellulose 50g
Triethyl citrate 30g
Dextrin 30g
Method for making:
(1) get holder department he, a filler to mix homogeneously with osmotic pressure active substance, with 85% ethanol for binding agent, make soft material, 18 ~ 24 mesh sieves are granulated, and tabletting after dry, obtains pastille label;
(2) with 80% dissolve with ethanol controlled-release material, plasticizer and porogen, make controlled release coat liquid;
(3) the controlled release coat liquid prepared evenly is sprayed at the pastille wicking surface that step (1) prepares, obtains holder after drying and take charge of his controlled release tablet.
Embodiment 2
Prescription 2(is by 1000)
His 20g is taken charge of in holder
Lactose 32g
Sodium chloride 40g
Methylcellulose 50g
Triethyl citrate 30g
Dextrin 30g
Method for making is with embodiment 1.
Embodiment 3
Prescription 3(is by 1000)
His 20g is taken charge of in holder
Lactose 32g
Sodium chloride 40g
Polyvinyl alcohol 50g
Triethyl citrate 30g
Dextrin 30g
Method for making is with embodiment 1.
Embodiment 4
Prescription 4(is by 1000)
His 20g is taken charge of in holder
Lactose 32g
Sodium chloride 40g
Ethyl cellulose 50g
Methylcellulose 25g
Triethyl citrate 30g
Dextrin 30g
Method for making is with embodiment 1.
Embodiment 5
Prescription 5(is by 1000)
His 20g is taken charge of in holder
Lactose 32g
Sodium chloride 40g
Ethyl cellulose 25g
Methylcellulose 25g
Polyvinyl alcohol 25g
Triethyl citrate 30g
Dextrin 30g
Method for making is with embodiment 1.
Test example 1 holds in the palm a preparation for his controlled release tablet of department
The supplementary material of according to the form below, by above-mentioned preparation method, his controlled release tablet is taken charge of in the holder that each embodiment obtains respectively.Wherein, "/" representative does not use.
Test example 2 vitro release is tested
Measure according to dissolution and drug release determination method (" Chinese Pharmacopoeia " 2015 editions four general rule 0931 first methods), analogue body digested road condition, temperature controls at 37 DEG C ± 0.5 DEG C, with degassed fresh purified water for release medium, use the phosphate buffer of pH3 ~ 8, drug release rate test is carried out to holder his controlled release tablet of department, respectively 1,2,4,6,8,12h sampling, according to ultraviolet visible spectrophotometry (" Chinese Pharmacopoeia " 2015 editions four general rules 0401), measure absorbance, calculate accumulative releasing degree according to standard curve.
Can find out, his controlled release tablet of holder obtained by a present invention department can constant speed, evenly discharge, the medicine effective blood drug concentration of long period can be maintained, reduce medicining times; Wherein holder his controlled release tablet of department for embodiment 4 discharged evenly in 12 hours, higher release can be reached at the 12nd hour, illustrate and use ethyl cellulose and the holder of methylcellulose (weight ratio is 2:1) made by controlled-release material to take charge of his controlled release tablet best results, this formula preparation technique is simple, steady quality is reliable, can meet the requirement of industrialized great production.
Claims (7)
1. holder his controlled release tablet of department, by pastille label be wrapped in its outer coatings rete and form, described pastille label comprise a holder department he,
Filler and osmotic pressure active substance, described coating rete comprises controlled-release material, plasticizer and porogen.
2. according to his controlled release tablet of holder according to claim 1 department, it is characterized in that controlled release portion is made up of rapid release and controlled release two parts, wherein immediate release section is containing his 2 ~ 5mg of a holder department, and controlled release portion is containing his 10 ~ 15mg of a holder department.
3. according to his controlled release tablet of holder according to claim 2 department, wherein immediate release section is containing his 5mg of a holder department, and controlled release portion is containing his 15mg of a holder department.
4. take charge of his controlled release tablet according to holder according to claim 1, it is characterized in that: described filler is lactose; Described osmotic pressure active substance is sodium chloride; Described controlled-release material is at least one in ethyl cellulose, methylcellulose and polyvinyl alcohol; Described plasticizer is triethyl citrate; Described porogen is dextrin.
5. take charge of his controlled release tablet according to holder according to claim 4, it is characterized in that: described controlled-release material is ethyl cellulose and methylcellulose.
6. take charge of his controlled release tablet according to holder according to claim 4, it is characterized in that: the weight ratio of described ethyl cellulose and described methylcellulose is 2:1.
7. holder of the present invention his controlled release tablet of department can be prepared as follows:
(1) get holder department he, a filler to mix homogeneously with osmotic pressure active substance, with 85% ethanol for binding agent, make soft material, 18 ~ 24 mesh sieves are granulated, and tabletting after dry, obtains pastille label;
(2) with 80% dissolve with ethanol controlled-release material, plasticizer and porogen, make controlled release coat liquid;
(3) the controlled release coat liquid prepared evenly is sprayed at the pastille wicking surface that step (1) prepares, obtains holder after drying and take charge of his controlled release tablet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510886865.7A CN105434389A (en) | 2015-12-07 | 2015-12-07 | Topiroxostat controlled-release tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510886865.7A CN105434389A (en) | 2015-12-07 | 2015-12-07 | Topiroxostat controlled-release tablet and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105434389A true CN105434389A (en) | 2016-03-30 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201510886865.7A Pending CN105434389A (en) | 2015-12-07 | 2015-12-07 | Topiroxostat controlled-release tablet and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN105434389A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110974796A (en) * | 2019-12-11 | 2020-04-10 | 正大制药（青岛）有限公司 | Clonidine hydrochloride controlled release tablet and preparation method thereof |
Citations (4)
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| CN103142540A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | PGMS (Propylene Glycol Mannate Sulfate) controlled-release tablet and preparation method thereof |
| CN103142539A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Alginic sodium diester controlled-release tablet and preparation method thereof |
| WO2013175494A2 (en) * | 2012-04-10 | 2013-11-28 | Rubicon Research Private Limited | Controlled release pharmaceutical formulations of direct thrombin inhibitors |
| CN104546841A (en) * | 2014-12-22 | 2015-04-29 | 青岛正大海尔制药有限公司 | Compound slow-release preparation containing topiroxostat |
-
2015
- 2015-12-07 CN CN201510886865.7A patent/CN105434389A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013175494A2 (en) * | 2012-04-10 | 2013-11-28 | Rubicon Research Private Limited | Controlled release pharmaceutical formulations of direct thrombin inhibitors |
| CN103142540A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | PGMS (Propylene Glycol Mannate Sulfate) controlled-release tablet and preparation method thereof |
| CN103142539A (en) * | 2013-03-21 | 2013-06-12 | 青岛正大海尔制药有限公司 | Alginic sodium diester controlled-release tablet and preparation method thereof |
| CN104546841A (en) * | 2014-12-22 | 2015-04-29 | 青岛正大海尔制药有限公司 | Compound slow-release preparation containing topiroxostat |
Non-Patent Citations (2)
| Title |
|---|
| 吴涛，等: "药用高分子控释膜的研究进展", 《中国药学杂志》 * |
| 陈慧云，等: "高分子材料纤维素醚类衍生物在缓释制剂辅料中的应用", 《材料导报》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110974796A (en) * | 2019-12-11 | 2020-04-10 | 正大制药（青岛）有限公司 | Clonidine hydrochloride controlled release tablet and preparation method thereof |
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| PB01 | Publication | ||
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| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20160330 |
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| RJ01 | Rejection of invention patent application after publication |