CN102198111A - Preparation method of antifungal tablet - Google Patents
Preparation method of antifungal tablet Download PDFInfo
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- CN102198111A CN102198111A CN 201110163850 CN201110163850A CN102198111A CN 102198111 A CN102198111 A CN 102198111A CN 201110163850 CN201110163850 CN 201110163850 CN 201110163850 A CN201110163850 A CN 201110163850A CN 102198111 A CN102198111 A CN 102198111A
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Abstract
The invention discloses a preparation method of an antifungal tablet and solves the problems of complex process, high cost and high quality control difficulty in the preparation of traditional Terbinafine hydrochloride tablets. The method comprises the steps of: 1, weighing Terbinafine hydrochloride, adhesive, carboxyrnethyl starch sodium, starch and magnesium stearate; and 2, putting and mixing the Terbinafine hydrochloride, the starch and a part of carboxyrnethyl starch sodium in a mixing tank, then adding and mixing the adhesive with the mixture, pelletizing, drying and finishing, adding the magnesium stearate and the rest carboxyrnethyl starch sodium, mixing and tabletting. In the preparation method of the antifungal tablet provided by the invention, by the use of the composite adhesive, the compressibility of drug particles and promote drug disintegration can be enhanced, tight tabletting and good adhesive force are obtained, the obtained tablets are bright and free from sticking, the degree of disintegration is remarkably reduced, the drug solubility is improved, the preparation process is simple in implementation, the cost of raw materials and accessories for every tablet is less than 1 Yuan, therefore, the price is low, and the product quality can be easily controlled.
Description
Technical field
The present invention relates to a kind of preparation method of antifungal drug.
Background technology
Terbinafine HCl can disturb the metabolism of fungus.It can suppress the Squalene Cycloxygenase of fungus specifically, finally makes membranolysis to reach the effect of killing fungus.Oral absorption is good, and mainly be distributed in keratodermatitis with high concentration, it is stronger to the mycotic infection of superficial part effect, external or short-term are oral can cure most dermatomycosiss, to the not influence of mammiferous normal cell, this is terbinafine HCl and the exclusive sterilization mode of other allylamine class antifungal agent simultaneously.
Terbinafine HCl is a lipophilic parent cutin chemical compound, so it diffuses to skin and first easily.Terbinafine is promoted in the world widely as first medicine that can effectively treat tinea unguium.Terbinafine has the antimycotic of belonging to medicine, characteristics such as better tolerance, short treating period, good effect, also be a unique up to now active drug that can effect a radical cure tinea unguium simultaneously, therefore terbinafine HCl has set up the golden standard of treatment skin, hair and fungal infection of nail for the whole world.Dermopathic sickness rate is very high, and according to interrelated data statistics, national total prevalence rate is 1.23%, promptly has 1.6 hundred million people to suffer from various degree dermatosis approximately.So far existing patient above 1,000 ten thousand has accepted the treatment of terbinafine HCl tablet, has nearly 5,000 ten thousand people to treat the dermatophytosis that it is suffered from by using terbinafine HCl simultaneously.
Terbinafine HCl has now been developed and has been made ointment, solution, gel and tablets and other formulations, is widely used in the treatment of dermatomycosis.At present, this kind exists that choice of drug dosage form preparation process complexity, the higher manufacturer of cost are less, adjuvant adds the improper problem that disintegration time prolongs, the stripping limit is low that causes.Domestic production producer is few, and drug price is higher, and dissolution is wayward, the marketing difficulty.
Summary of the invention
The objective of the invention is to exist complex process, cost height, quality wayward for the preparation that solves existing terbinafine HCl tablet, the adjuvant interpolation is improper to cause the problem that disintegration time prolongs, the stripping limit is low, and a kind of preparation method of antifungal drug tablet is provided.
The preparation method of antifungal drug tablet is carried out according to the following steps: one, take by weighing 100～150 parts terbinafine HCl, 4～8 parts adhesive, 8～15 parts carboxymethylstach sodium, 50～60 parts starch and 0.5～3 part magnesium stearate by ratio of weight and the number of copies; Two, the carboxymethylstach sodium of the terbinafine HCl that takes by weighing, starch and 6～10 parts is placed mix 20min in the mixing channel, add the mixed soft material of adhesive then, granulate after 14 mesh sieves, 14 mesh sieve granulate are crossed in dry back, the magnesium stearate that adding takes by weighing and the carboxymethylstach sodium of surplus, mix the back compacting in flakes, promptly finish the preparation of antifungal drug tablet; Wherein adhesive is that 1%～10% hypromellose solution and mass concentration are that 4%～10% starch slurry mixes according to volume ratio at 3: 10 by mass concentration in the step 1.
The antifungal drug tablet of the present invention's preparation, its main feature is the composite adhesive of selecting for use, can improve the compressibility of drug particles and the disintegrate of promotion medicine, tabletting is tight, bonding force is good again, the sheet light of extrusion, no sticking, and disintegration declines to a great extent, improve drug dissolution, can guarantee the terbinafine HCl sheet, have mouldability and quality stability preferably as the oral tablet dosage form, be beneficial at regular time and quantity and take, be beneficial to and improve the compliance that clinical patients is used.The preparation method of a kind of antifungal drug tablet of the present invention has that preparation process thereof is simple, and needed raw material, adjuvant are common, and legal source is all arranged, and 1 yuan of every flake products supplementary material cost less than is cheap; Product quality is easy to control, taking convenience, the advantage that expense is cheap.Oral absorption is good, and mainly is distributed in keratodermatitis with high concentration, and it is stronger to the mycotic infection of superficial part effect, and short-term is oral can cure most dermatomycosiss, and this variety production producer is less, and the market competitiveness is strong, and market prospect is wide.
The present invention is directed to terbinafine HCl is crystalline powder, its mobile relatively poor characteristics, adopt the technology of the back tabletting of granulating, what the present invention granulated employing is to add starch slurry and the blended adhesive granulation of hypromellose solution in drug powder, after mixing, starch slurry and hypromellose solution can produce bridging action, liquid exists with the strap shape in granule (suitably increases amount of liquid 0.3＜S＜0.8 o'clock, liquid bridge links to each other, liquid becomes continuous phase, the space diminishes, the composition of air phase of loosing, claim the strap shape), the bridge formation liquid that produces when wet granulation solidifies after drying, forms the granule of certain intensity, solvent evaporation when dry in the binder solution is removed, and the fixed solid that becomes of residual binding agent is built bridge.The cementation that the bridging action of binding agent can be worked in coordination with starch slurry and hypromellose coalesces together powder and is convenient to prepare granule, the present invention does not more add binding agent and only depends on Van der Waals force or only add the method that a kind of binding agent only depends on cementation that powder is coalesced together and be more conducive to prepare granule, cooperate the fluidizer magnesium stearate, the granule of making has good flowability and compressibility.Product good looking appearance, good fluidity, wearability are strong, compression molding is good.Selecting carboxymethylstach sodium for use is disintegrating agent, carboxymethyl starch sodium imbibition effect highly significant, and function admirable, price is lower, and the bioavailability height has been avoided the influence of binding agent to dissolution.
Description of drawings
Fig. 1 is a dissolution curve chart in the specific embodiment eight, wherein realizes the dissolution curve of the antifungal drug of "---" expression present embodiment preparation, the dissolution curve of dotted line "---" expression market existing goods.
The specific embodiment
Technical solution of the present invention is not limited to the following cited specific embodiment, also comprises the combination in any between each specific embodiment.
The specific embodiment one: the preparation method of present embodiment antifungal drug tablet is carried out according to the following steps: one, take by weighing 100～150 parts terbinafine HCl, 4～8 parts adhesive, 8～15 parts carboxymethylstach sodium, 50～60 parts starch and 0.5～3 part magnesium stearate by ratio of weight and the number of copies; Two, the carboxymethylstach sodium of the terbinafine HCl that takes by weighing, starch and 6～10 parts is placed mix 20min in the mixing channel, add the mixed soft material of adhesive then, granulate after 14 mesh sieves, 14 mesh sieve granulate are crossed in dry back, the magnesium stearate that adding takes by weighing and the carboxymethylstach sodium of surplus, mix the back compacting in flakes, promptly finish the preparation of antifungal drug tablet; Wherein adhesive is that 1%～10% hypromellose solution and mass concentration are that 4%～10% starch slurry mixes according to volume ratio at 3: 10 by mass concentration in the step 1.
Carboxymethylstach sodium uses as disintegrating agent in the present embodiment.
The tablet specification of present embodiment preparation is 0.125g (in a terbinafine HCl).
The specific embodiment two: the different of present embodiment and the specific embodiment one are to take by weighing 100 parts terbinafine HCl, 4 parts adhesive, 8 parts carboxymethylstach sodium, 50 parts starch and 0.5 part magnesium stearate in the step 1 by ratio of weight and the number of copies.Other step and parameter are identical with the specific embodiment one.
The specific embodiment three: the different of present embodiment and the specific embodiment one are to take by weighing 150 parts terbinafine HCl, 8 parts adhesive, 15 parts carboxymethylstach sodium, 60 parts starch and 3 parts magnesium stearate in the step 1 by ratio of weight and the number of copies.Other step and parameter are identical with the specific embodiment one.
The specific embodiment four: the different of present embodiment and the specific embodiment one are to take by weighing 110～140 parts terbinafine HCl, 5～7 parts adhesive, 9～13 parts carboxymethylstach sodium, 52～58 parts starch and 1～2 part magnesium stearate in the step 1 by ratio of weight and the number of copies.Other step and parameter are identical with the specific embodiment one.
The specific embodiment five: the different of present embodiment and the specific embodiment one are to take by weighing 120 parts terbinafine HCl, 6 parts adhesive, 11 parts carboxymethylstach sodium, 53 parts starch and 1.5 parts magnesium stearate in the step 1 by ratio of weight and the number of copies.Other step and parameter are identical with the specific embodiment one.
The specific embodiment six: the different of present embodiment and the specific embodiment one are to take by weighing 125 parts terbinafine HCl, 6.5 parts adhesive, 12 parts carboxymethylstach sodium, 55 parts starch and 1.5 parts magnesium stearate in the step 1 by ratio of weight and the number of copies.Other step and parameter are identical with the specific embodiment one.
The specific embodiment seven: the different of present embodiment and one of specific embodiment one to six are that drying is to place drying baker dry down in 70 ℃ in the step 2.Other step and parameter are identical with one of specific embodiment one to six.
The specific embodiment eight: the preparation method of present embodiment antifungal drug tablet is carried out according to the following steps: one, take by weighing 125 parts terbinafine HCl, 6.5 parts adhesive, 12 parts carboxymethylstach sodium, 55 parts starch and 1.5 parts magnesium stearate by ratio of weight and the number of copies; Two, the carboxymethylstach sodium of the terbinafine HCl that takes by weighing, starch and 8 parts is placed mix 20min in the mixing channel, add the mixed soft material of adhesive then, granulate after 14 mesh sieves, 14 mesh sieve granulate are crossed in dry back, the magnesium stearate that adding takes by weighing and the carboxymethylstach sodium of surplus, mix the back compacting in flakes, promptly finish the preparation of antifungal drug tablet; Wherein adhesive is that 5% hypromellose solution and mass concentration are that 8% starch slurry mixes according to volume ratio at 3: 10 by mass concentration in the step 1.
The antifungal drug tablet of present embodiment preparation, by research, checking and the Study on Stability of technology preparation, quality research is the result show, state quality standard can be controlled the inherent quality of product, every detection index conformance with standard regulation of product; Stripping curve shows that the stripping behavior of product meets statutory standards (seeing Table 1 and Fig. 1, the dissolution curve chart), and stripping curve compares and studies show that, in 15min, stripping is 90% (greater than 85%), and bioavailability meets statutory standards in provable its body; In production and storage, related substance does not obviously increase; Present embodiment preparation process prescription is feasible, and drug quality has good stability.
The antifungal drug tablet usage and dosage of present embodiment preparation is: oral, each 0.25 gram of being grown up once a day, about 2～6 weeks of the course of treatment, is cured several weeks in mycology, just can see the normal fully and infection symptoms disappearance of skin appearance; Be 6 week～3 month the course of treatment that is used for the most patients of tinea unguium; The patient that some patient, particularly those thumbs (toe) first infect may need 6 months or longer time; Cure and stop to treat the back some months in mycology, it is normal fully to see that the state of an illness continues to go to the deck outward appearance; As the oral tablet dosage form, make terbinafine HCl have mouldability and quality stability preferably, be beneficial to quantitatively and take, the specification that is prepared into 0.125g is more conducive to the compliance that clinical patients is used.
The antifungal drug tablet of present embodiment preparation, its price (seeing Table 2) compares with the price (seeing Table 3 and 4) of existing terbinafine HCl sheet and emulsifiable paste, as can be known, the each dose of terbinafine HCl sheet (250 milligrams) market price does not wait between 12～20 yuan, the per 50 milligrams of prices of cream preparation do not wait at 4～14 yuan, and price is higher relatively, and 1 yuan of every flake products supplementary material cost deficiency of the used preparation method of present embodiment, cheap, cost has clear superiority.
The antifungal drug of table 1 present embodiment preparation and the dissolution of market existing goods are relatively
The antifungal drug tablet supplementary material price catalog of table 2 present embodiment preparation
The commercially available price catalog of the existing terbinafine HCl sheet of table 3
The commercially available price catalog of the existing Terbinafine hydrochloride emulsifiable paste of table 4
Claims (5)
1. the preparation method of an antifungal drug tablet is characterized in that the preparation method of antifungal drug tablet is carried out according to the following steps: one, take by weighing 100～150 parts terbinafine HCl, 4～8 parts adhesive, 8～15 parts carboxymethylstach sodium, 50～60 parts starch and 0.5～3 part magnesium stearate by ratio of weight and the number of copies; Two, the carboxymethylstach sodium of the terbinafine HCl that takes by weighing, starch and 6～10 parts is placed mix 20min in the mixing channel, add the mixed soft material of adhesive then, granulate after 14 mesh sieves, 14 mesh sieve granulate are crossed in dry back, the magnesium stearate that adding takes by weighing and the carboxymethylstach sodium of surplus, mix the back compacting in flakes, promptly finish the preparation of antifungal drug tablet; Wherein adhesive is that 1%～10% hypromellose solution and mass concentration are that 4%～10% starch slurry mixes according to volume ratio at 3: 10 by mass concentration in the step 1.
2. the preparation method of a kind of antifungal drug tablet according to claim 1 is characterized in that taking by weighing by ratio of weight and the number of copies in the step 1 110～140 parts terbinafine HCl, 5～7 parts adhesive, 9～13 parts carboxymethylstach sodium, 52～58 parts starch and 1～2 part magnesium stearate.
3. the preparation method of a kind of antifungal drug tablet according to claim 1 is characterized in that taking by weighing by ratio of weight and the number of copies in the step 1 120 parts terbinafine HCl, 6 parts adhesive, 11 parts carboxymethylstach sodium, 53 parts starch and 1.5 parts magnesium stearate.
4. the preparation method of a kind of antifungal drug tablet according to claim 1 is characterized in that taking by weighing by ratio of weight and the number of copies in the step 1 125 parts terbinafine HCl, 6.5 parts adhesive, 12 parts carboxymethylstach sodium, 55 parts starch and 1.5 parts magnesium stearate.
5. according to the preparation method of claim 1,2,3 or 4 described a kind of antifungal drug tablets, it is characterized in that drying is to place drying baker dry down in 70 ℃ in the step 2.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 201110163850 CN102198111A (en) | 2011-06-17 | 2011-06-17 | Preparation method of antifungal tablet |
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| CN 201110163850 CN102198111A (en) | 2011-06-17 | 2011-06-17 | Preparation method of antifungal tablet |
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| CN102198111A true CN102198111A (en) | 2011-09-28 |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110200929A (en) * | 2018-12-14 | 2019-09-06 | 悦康药业集团上海制药有限公司 | A kind of oral tablet and preparation method thereof containing terbinafine HCl |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1527706A (en) * | 2001-07-20 | 2004-09-08 | ��˹��ŵ�� | Pharmaceutical compositions containing terbinafin and use thereof |
| CN101548958A (en) * | 2008-04-03 | 2009-10-07 | 北京德众万全药物技术开发有限公司 | Dispersing tablet containing terbinafine hydrochloride |
-
2011
- 2011-06-17 CN CN 201110163850 patent/CN102198111A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1527706A (en) * | 2001-07-20 | 2004-09-08 | ��˹��ŵ�� | Pharmaceutical compositions containing terbinafin and use thereof |
| CN101548958A (en) * | 2008-04-03 | 2009-10-07 | 北京德众万全药物技术开发有限公司 | Dispersing tablet containing terbinafine hydrochloride |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110200929A (en) * | 2018-12-14 | 2019-09-06 | 悦康药业集团上海制药有限公司 | A kind of oral tablet and preparation method thereof containing terbinafine HCl |
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Application publication date: 20110928 |