CN106667938A - Lomerizine hydrochloride tablets and preparation method thereof - Google Patents
Lomerizine hydrochloride tablets and preparation method thereof Download PDFInfo
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- CN106667938A CN106667938A CN201710064537.8A CN201710064537A CN106667938A CN 106667938 A CN106667938 A CN 106667938A CN 201710064537 A CN201710064537 A CN 201710064537A CN 106667938 A CN106667938 A CN 106667938A
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- Prior art keywords
- preparation
- lomerizine hydrochloride
- lomerizine
- adhesive
- recipe quantity
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- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
-
- 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
- A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
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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)
- Medicinal Preparation (AREA)
Abstract
The invention relates to lomerizine hydrochloride tablets and preparation method thereof. The preparation method comprises the following specific steps: weighing lomerizine hydrochloride and adhesive, adding in a solvent to stir and dissolve for later user; weighing filling agent and disintegrating agent, adding in a wet mixing granulator to uniformly mix, adding a solution containing the lomerizine hydrochloride and the adhesive to prepare a soft material, pelletizing by use of a 20-mesh screen, drying on a fluid bed at 60 DEG C until the moisture is less than 5%, integrating the dry particles through the 20-mesh screen, adding the lubricant with the prescription amount to uniformly mix, detecting the lomerizine content in the particle, computing tablet weight, tableting, packaging by use of aluminum plastic to obtain the lomerizine hydrochloride tablet. Compared with the prior art, the raw material and the adhesive are dissolved in the ethanol at the same time, and then added in other mixed powder in a solution status, thereby greatly improving the content uniformity; furthermore, the raw material and the adhesive are existent in the preparation in a coexisting status, the raw material is prevented from being directly exposed, and the stability of the related substance of the product is greatly increased.
Description
Technical field
The invention belongs to field of medicine preparing technology, it particularly relates to arrive a kind of lomerizine hydrochloride piece and its preparation
Method.
Background technology
Lomerizine hydrochloride piece is clinical common medicine, for treating the prophylactic treatment of antimigraine.This product is hexichol piperazine
Class calcium channel blocker, selective cerebral vasodilation effect.With the quickening pace of modern life with the increase of operating pressure,
The incidence of disease more and more higher of the antimigraine that I crosses, has become the common disease of puzzlement people.Lomerizine is calcium ion of new generation
Antagonist, it is increasing cerebral blood flow (CBF), while suppressing cerebral vasoconstriction, may also suppress the generation for propagating neurogenic inflammation,
So as to prevent the generation of migraine.The side effect for being outside the centrum that it causes seldom occurs, thus it than other calcium from
Sub- antagonist such as nicardipine and flunarizine is more selective, and duration of efficacy is longer, and side effect is smaller.
It is to add adhesive wet granulation after supplementary material is well mixed that lomerizine hydrochloride piece is typically prepared technique, is used
Conventional tablet production technology is prepared.Because preparation specification is small, it is difficult to mix；Obtained tablet is in the relevant material of storage period
Can raise, dissolution rate can continue to reduce.
The content of the invention
In order to solve the above technical problems, a kind of hydrochloric acid Lome of, dissolution rate stabilization good the invention provides uniformity of dosage units
Sharp piperazine piece and preparation method thereof.
A kind of preparation method of lomerizine hydrochloride piece of the present invention, the preparation method is comprised the following steps that：Claim
The lomerizine hydrochloride and adhesive of recipe quantity are taken, stirring and dissolving in the solvent of recipe quantity is added to, it is standby；Weigh recipe quantity
Filler and disintegrant, are added in wet mixing pelletizer and are well mixed, by containing lomerizine hydrochloride and with adhesive
Solution is added, softwood processed, is pelletized with 20 mesh sieves, 60 DEG C of dryings of fluid bed to moisture less than 5%, dry particl through 20 mesh sieve whole grains,
Add the mix lubricant of recipe quantity uniform, the content of lomerizine hydrochloride, calculates piece weight, compressing tablet, plastic-aluminum bag in detection particle
Dress, obtains final product.
A kind of preparation method of lomerizine hydrochloride piece of the present invention, the filler includes microcrystalline cellulose, breast
One or more in sugar, mannitol, pregelatinized starch.
A kind of preparation method of lomerizine hydrochloride piece of the present invention, the disintegrant includes cross-linked carboxymethyl fiber
One or more composition in plain sodium, sodium carboxymethyl starch, PVPP.
A kind of preparation method of lomerizine hydrochloride piece of the present invention, described adhesive includes PVP K30, hydroxypropyl
One or more in methylcellulose, hydroxypropylcellulose.
A kind of preparation method of lomerizine hydrochloride piece of the present invention, the solvent is water or 95% ethanol.
A kind of preparation method of lomerizine hydrochloride piece of the present invention, the lubricant includes magnesium stearate, micro mist
One or more compositions in silica gel, stearic acid, Compritol 888 ATO.
Compared with prior art, the preparation method of lomerizine hydrochloride piece of the present invention is simultaneously molten by raw material and adhesive
Solution in ethanol, then again with solution state add other mix powder in, uniformity of dosage units can be greatly improved；Other raw material
The state for coexisting a kind of with adhesive is present in preparation, it is to avoid raw material directly exposes, and also greatly increases the relevant material of this product
Stabilization.
Specific embodiment
Lomerizine hydrochloride piece of the present invention and preparation method thereof is described further with reference to specific embodiment,
But protection scope of the present invention is not limited to this.
Embodiment 1：Lomerizine hydrochloride piece (10000)
Preparation method：The lomerizine hydrochloride and hydroxypropylcellulose EXF of recipe quantity are weighed, is added in 95% ethanol of recipe quantity
Stirring and dissolving, it is standby；Mannitol, MCC and the carboxyrnethyl starch sodium of recipe quantity are weighed, wet-mixing granulation is added to
It is well mixed in machine, the ethanol solution containing lomerizine hydrochloride and hydroxypropylcellulose EXF is added, softwood processed uses 20 mesh sieves
Granulation, 60 DEG C of dryings of fluid bed to moisture are less than 5%, and dry particl adds the magnesium stearate mixing of recipe quantity through 20 mesh sieve whole grains
Uniformly,.The content of lomerizine hydrochloride, calculates piece weight, compressing tablet in detection particle.It is aluminum-plastic packaged, obtain final product.
Embodiment 2：Lomerizine hydrochloride piece (10000)
Preparation method：The lomerizine hydrochloride and hydroxypropylcellulose EXF of recipe quantity are weighed, is added in 95% ethanol of recipe quantity
Stirring and dissolving, it is standby；Lactose, MCC and the carboxyrnethyl starch sodium of recipe quantity are weighed, wet mixing pelletizer is added to
In be well mixed, by containing lomerizine hydrochloride and hydroxypropylcellulose EXF ethanol solution add, softwood processed, with 20 mesh sieve series
Grain, 60 DEG C of dryings of fluid bed to moisture are less than 5%, and dry particl adds the magnesium stearate mixing of recipe quantity equal through 20 mesh sieve whole grains
It is even,.The content of lomerizine hydrochloride, calculates piece weight, compressing tablet in detection particle.It is aluminum-plastic packaged, obtain final product.
Embodiment 3：Lomerizine hydrochloride piece (10000)
Preparation method：The lomerizine hydrochloride and hydroxypropylcellulose EXF of recipe quantity are weighed, is added in 95% ethanol of recipe quantity
Stirring and dissolving, it is standby；The new glycosides P1 of pregelatinized starch, MCC, carboxyrnethyl starch sodium and periploca spium of recipe quantity is weighed, plus
Enter in wet mixing pelletizer and be well mixed, the ethanol solution containing lomerizine hydrochloride and hydroxypropylcellulose EXF is added,
Softwood processed, is pelletized with 20 mesh sieves, and 60 DEG C of dryings of fluid bed to moisture are less than 5%, and dry particl adds recipe quantity through 20 mesh sieve whole grains
Magnesium stearate be well mixed,.The content of lomerizine hydrochloride, calculates piece weight, compressing tablet in detection particle.It is aluminum-plastic packaged, obtain final product.
Embodiment 4：Lomerizine hydrochloride piece (10000)
Preparation method：The lomerizine hydrochloride and hydroxypropylcellulose EXF of recipe quantity are weighed, is added in 95% ethanol of recipe quantity
Stirring and dissolving, it is standby；The new glycosides P2 of pregelatinized starch, MCC, carboxyrnethyl starch sodium and periploca spium of recipe quantity is weighed, plus
Enter in wet mixing pelletizer and be well mixed, the ethanol solution containing lomerizine hydrochloride and hydroxypropylcellulose EXF is added,
Softwood processed, is pelletized with 20 mesh sieves, and 60 DEG C of dryings of fluid bed to moisture are less than 5%, and dry particl adds recipe quantity through 20 mesh sieve whole grains
Magnesium stearate be well mixed,.The content of lomerizine hydrochloride, calculates piece weight, compressing tablet in detection particle.It is aluminum-plastic packaged, obtain final product.
Comparative example：Lomerizine hydrochloride piece (10000)
Preparation method：The PVP K30 for weighing recipe quantity is added to stirring and dissolving in 95% ethanol of recipe quantity, standby；Weigh
The lomerizine hydrochloride of recipe quantity, pregelatinized starch, MCC and carboxyrnethyl starch sodium, are added to wet-mixing granulation
It is well mixed in machine, PVP K30 ethanol solution is added, softwood processed, is pelletized with 20 mesh sieves, 60 DEG C of dryings of fluid bed to moisture
Less than 5%, dry particl adds the magnesium stearate of recipe quantity to be well mixed through 20 mesh sieve whole grains,.Hydrochloric acid Lome profit in detection particle
The content of piperazine, calculates piece weight, compressing tablet.It is aluminum-plastic packaged, obtain final product.
Compliance test result (each detection refers to pharmacopeia to be carried out)
1. the uniformity of dosage units of the sample of embodiment and comparative example is detected, concrete outcome is shown in Table 1.
The uniform testing result of embodiment sample content of table 1
| Sample | Uniformity of dosage units (A+2.2S) |
| Embodiment 1 | 6.9 |
| Embodiment 2 | 7.4 |
| Embodiment 3 | 7.8 |
| Embodiment 4 | 7.6 |
| Comparative example | 12.5 |
2. the relevant material of the sample of embodiment and comparative example is detected, concrete outcome is shown in Table 2.
The relevant material testing result of the embodiment sample of table 2 (single miscellaneous/total miscellaneous) (%)
| When 0 | Accelerate January | Accelerate 2 months | Accelerate March | Accelerate June | |
| Embodiment 1 | 0.27/0.58 | 0.25/0.55 | 0.31/0.62 | 0.33/0.68 | 0.35/0.72 |
| Embodiment 2 | 0.31/0.60 | 0.33/0.59 | 0.32/0.60 | 0.32/0.66 | 0.34/0.75 |
| Embodiment 3 | 0.28/0.60 | 0.30/0.61 | 0.33/0.63 | 0.31/0.65 | 0.36/0.77 |
| Embodiment 4 | 0.27/0.61 | 0.28/0.61 | 0.29/0.62 | 0.30/0.62 | 0.30/0.67 |
| Comparative example | 0.30/0.59 | 0.34/0.68 | 0.40/0.86 | 0.47/1.02 | 0.66/1.45 |
3. the dissolution rate of the sample of embodiment and comparative example is detected, concrete outcome is shown in Table 3.
Embodiment sample dissolution rate testing result (%) of table 3
| When 0 | Accelerate January | Accelerate 2 months | Accelerate March | Accelerate June | |
| Embodiment 1 | 102.4 | 100.6 | 101.3 | 99.3 | 100.8 |
| Embodiment 2 | 99.6 | 97.4 | 97.8 | 96.6 | 97.7 |
| Embodiment 3 | 98.3 | 98.9 | 96.2 | 97.5 | 96.9 |
| Embodiment 4 | 99.7 | 99.8 | 101.1 | 101.2 | 101.1 |
| Comparative example | 99.7 | 96.2 | 90.5 | 84.6 | 77.2 |
4. the dissolution rate of the sample of embodiment and comparative example is detected, concrete outcome is shown in Table 4.
The embodiment sample of table 4 accelerates dissolution rate testing result (%)
Result shows, control group is substantially better than using the tablet content uniformity obtained in this patent method, about material and
Dissolution rate is also more stablized.
Claims (7)
1. a kind of preparation method of lomerizine hydrochloride piece, it is characterised in that the preparation method is comprised the following steps that：Weigh place
The lomerizine hydrochloride and adhesive of side's amount, are added to stirring and dissolving in the solvent of recipe quantity, standby；Weigh the filling of recipe quantity
Agent and disintegrant, are added in wet mixing pelletizer and are well mixed, by the solution containing lomerizine hydrochloride and with adhesive
Add, softwood processed, pelletized with 20 mesh sieves, 60 DEG C of dryings of fluid bed to moisture are less than 5%, dry particl is added through 20 mesh sieve whole grains
The mix lubricant of recipe quantity is uniform, and the content of lomerizine hydrochloride, calculates piece weight in detection particle, and compressing tablet is aluminum-plastic packaged, i.e.,
.
2. the preparation method of lomerizine hydrochloride piece according to claim 1, it is characterised in that the filler includes micro-
One or more in crystalline cellulose, lactose, mannitol, pregelatinized starch.
3. the preparation method of lomerizine hydrochloride piece according to claim 1, it is characterised in that the disintegrant includes handing over
One or more in connection sodium carboxymethylcellulose, sodium carboxymethyl starch, PVPP.
4. the preparation method of lomerizine hydrochloride piece according to claim 1, it is characterised in that described adhesive includes poly-
One or more in dimension ketone K30, Hydroxypropyl methylcellulose, hydroxypropylcellulose.
5. the preparation method of lomerizine hydrochloride piece according to claim 1, it is characterised in that the solvent be water or
95% ethanol.
6. the preparation method of lomerizine hydrochloride piece according to claim 1, it is characterised in that the lubricant includes hard
One or more in fatty acid magnesium, superfine silica gel powder, stearic acid, Compritol 888 ATO.
7. the lomerizine hydrochloride piece according to obtained in claim 1-7 any preparation methods.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710064537.8A CN106667938A (en) | 2017-02-04 | 2017-02-04 | Lomerizine hydrochloride tablets and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710064537.8A CN106667938A (en) | 2017-02-04 | 2017-02-04 | Lomerizine hydrochloride tablets and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN106667938A true CN106667938A (en) | 2017-05-17 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710064537.8A Pending CN106667938A (en) | 2017-02-04 | 2017-02-04 | Lomerizine hydrochloride tablets and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1628668A (en) * | 2003-12-15 | 2005-06-22 | 南京金鹰医药科技开发有限公司 | Lomerizine hydrochloride orally disintegrating tablet and preparation method thereof |
| CN103462919A (en) * | 2013-09-22 | 2013-12-25 | 南京正亮医药科技有限公司 | Lomerizine hydrochloride tablet and preparation method thereof |
-
2017
- 2017-02-04 CN CN201710064537.8A patent/CN106667938A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1628668A (en) * | 2003-12-15 | 2005-06-22 | 南京金鹰医药科技开发有限公司 | Lomerizine hydrochloride orally disintegrating tablet and preparation method thereof |
| CN103462919A (en) * | 2013-09-22 | 2013-12-25 | 南京正亮医药科技有限公司 | Lomerizine hydrochloride tablet and preparation method thereof |
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| PB01 | Publication | ||
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Application publication date: 20170517 |