CN107744513A - A kind of Loperamide hydrochloride capsules and preparation method thereof - Google Patents
A kind of Loperamide hydrochloride capsules and preparation method thereof Download PDFInfo
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- CN107744513A CN107744513A CN201711182585.3A CN201711182585A CN107744513A CN 107744513 A CN107744513 A CN 107744513A CN 201711182585 A CN201711182585 A CN 201711182585A CN 107744513 A CN107744513 A CN 107744513A
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- capsules
- loperamide hydrochloride
- drug particles
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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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/451—Non condensed piperidines, e.g. piperocaine having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
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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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7004—Monosaccharides having only carbon, hydrogen and oxygen atoms
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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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
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- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention provides a kind of Loperamide hydrochloride capsules and preparation method thereof, and the Loperamide hydrochloride capsules include drug particles and Capsules, and wherein drug particles not only have the effect of very high to treating non-infectious acute and chronic diarrhoea.Glucose can guarantee that the needs that heat is metabolized when patient's constitution is extremely weak, can be completely dissolved in pregelatinized starch cold water, there is self-lubricating function, adds magnesium stearate and does lubricant, nontoxic, nonirritant.The Loperamide hydrochloride capsules have the characteristics of supplementary material is simple, and bioavilability is high, and active component is stable, and active ingredient rate of release is fast.
Description
Technical field
The present invention relates to technical field of medicine, more particularly to a kind of Loperamide hydrochloride capsules and preparation method thereof.
Background technology
The chemical name of loperamide hydrochloride is N, N- dimethyl-α, α-diphenyl -4- (rubigan) -4- hydroxyls -1-
Loperamide hydrochloride (be raw material by 2,2- diphenyl -4- bromo-butyric acids, through superchlorination, amination, condensation, into obtaining after salt), change
Structure is learned similar to haloperole and pethidine, but therapeutic dose Central nervous system is without any effect.With prevention acetylcholine
With the release of prostaglandin, so as to suppress enterocinesia, extend the pharmacological action of the holdup time of intestinal contents.
Loperamide hydrochloride be white or off-white color crystalline powder, almost odorless, bitter.In ethanol or glacial acetic acid
It is readily soluble, the slightly soluble in water.With the high-affinity of intestinal wall and obvious " first-pass metabolism ", it is set hardly to be followed into systemic blood
Ring.Loperamide hydrochloride is used clinically for the symptomatic treatment of non-infectious acute and chronic diarrhoea caused by a variety of causes.
It is existing complicated using loperamide hydrochloride as the formulation ingredients of main component, loperamide hydrochloride dissolution rate is influenceed,
Making loperamide hydrochloride, availability is relatively low in vivo, does not play due drug effect.Due to above mentioned problem, clinically for suffering from
During the treatment of person's diarrhoea, therapeutic effect will be influenceed by certain.The present invention proposes a kind of Loperamide hydrochloride capsules, has original
The characteristics of auxiliary material is simple, and bioavilability is high, and active component is stable, and rate of release is fast.
The content of the invention
The invention provides above-mentioned a kind of Loperamide hydrochloride capsules and preparation method thereof, comprise the following steps：
A) it is loperamide hydrochloride, glucose, pregelatinized starch, anhydrous silica gel, Magnesium Stearate is standby；Using pectin
Hollow glue is made in powder, hydroxypropyl methyl cellulose, neck diethyl phthalate, gelatin, lauryl sodium sulfate, silica
Capsule；
B) loperamide hydrochloride and pregelatinized starch that step a) is obtained are weighed, in Mixers with Multi-direction Movement mix 10~
20min, glucose is added, mix 10~20min, add anhydrous silica gel, magnesium stearate, mixed 4~8min, obtain medicine
Grain；
C) the step b) drug particles made are filled into Capsules made from step a), obtain loperamide hydrochloride glue
Capsule；
Preferably, the sour Loperamide, glucose, pregelatinized starch cross 80 mesh sieves；The anhydrous silica gel, magnesium stearate
Cross 30 mesh sieves；
The present invention proposes a kind of Loperamide hydrochloride capsules and preparation method thereof, including drug particles and Capsules：
The mass ratio of the drug particles and the Capsules is (4~6):1；
The drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Preferably, affiliated drug particles include the raw material of following parts by weight：
Preferably, the Capsules includes the raw material of following parts by weight：
The present invention provides a kind of Loperamide hydrochloride capsules and preparation method thereof, and the Loperamide hydrochloride capsules include medicine
Particle and Capsules, wherein drug particles not only have the effect of very high to treating non-infectious acute and chronic diarrhoea.Glucose
The needs that heat is metabolized when patient's constitution is extremely weak are can guarantee that, can be completely dissolved in pregelatinized starch cold water, there is self-lubricating
Effect, add magnesium stearate and do lubricant, it is nontoxic, nonirritant.The Loperamide hydrochloride capsules have that supplementary material is simple, biology
The characteristics of availability is high, and active component is stable, and active ingredient rate of release is fast.
Embodiment
Below by embodiment, the present invention is described in further detail, but should not be understood as protecting the present invention
The limitation of scope, it is all to be based on above-mentioned technical thought, it is used in modification that ordinary skill knowledge and customary means made, replaces
Change, change and belong to the scope of the present invention.
Embodiment 1
Affiliated drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Embodiment 2
Affiliated drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Embodiment 3
Affiliated drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Embodiment 4
Affiliated drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Embodiment 5
Affiliated drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Embodiment 6
Affiliated drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Embodiment 7
Affiliated drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
Operating method：
Loperamide hydrochloride, glucose, pregelatinized starch are crossed into 80 mesh sieves, it is standby that anhydrous silica gel, magnesium stearate cross 30 mesh sieves
With；Weigh parts by weight jelly powder, hydroxypropyl methyl cellulose, neck diethyl phthalate, gelatin, lauryl sodium sulfate,
50mg Capsules is made in silica；
Loperamide hydrochloride and pregelatinized starch are weighed, 10~20min is mixed in Mixers with Multi-direction Movement, is added certain
The glucose of amount, 10~20min is mixed, add the anhydrous silica gel weighed and the magnesium stearate weighed, mixed 4~8min, obtain
To drug particles；
Weigh 250mg drug particles to be filled into obtained Capsules, obtain Loperamide hydrochloride capsules；
Stability Determination is carried out to above-described embodiment.
4stability determination：
This product is taken to place 10d under the conditions of 20 DEG C, 40 DEG C, 60 DEG C respectively.Its property is investigated in sampling when 1,3,5,10d
Shape, about material and assay equistability index, and compared with 0d, as a result These parameters have no significant change.
Dissolution determination is carried out to above-described embodiment.
Dissolution determination method：
This product is taken, is shone《Chinese Pharmacopoeia》Dissolution method is to made from embodiment 1~7 in the two annex XC of version in 2010
Loperamide hydrochloride capsules different times dissolution rate is measured, and the results are shown in Table 1.
The dissolution results of the embodiment 1~7 of table 1
| Embodiment 1 | Embodiment 2 | Embodiment 3 | Embodiment 4 | Embodiment 5 | Embodiment 6 | Embodiment 7 | |
| 0 month | 85.1 | 89.3 | 88.3 | 87.8 | 90.2 | 90.2 | 87.7 |
| 2 months | 85.2 | 89.2 | 88.4 | 87.6 | 90.1 | 90.4 | 87.8 |
| April | 85.1 | 89.6 | 89.4 | 87.8 | 90.1 | 90.2 | 87.6 |
| December | 85.1 | 88.1 | 88.3 | 87.7 | 89.8 | 90.1 | 87.5 |
| 24 months | 84.6 | 85.7 | 87.9 | 87.5 | 89.8 | 89.9 | 87.1 |
Claims (4)
1. a kind of Loperamide hydrochloride capsules and preparation method thereof, its method characteristic is, comprises the following steps：
A) it is loperamide hydrochloride, glucose, pregelatinized starch, anhydrous silica gel, Magnesium Stearate is standby；Using jelly powder,
Capsules is made in hydroxypropyl methyl cellulose, neck diethyl phthalate, gelatin, lauryl sodium sulfate, silica；
B) loperamide hydrochloride and pregelatinized starch that step a) is obtained are weighed, in Mixers with Multi-direction Movement mix 10~
20min, glucose is added, mix 10~20min, add anhydrous silica gel, magnesium stearate, mixed 4~8min, obtain medicine
Grain；
C) the step b) drug particles made are filled into Capsules made from step a), obtain Loperamide hydrochloride capsules.
A kind of 2. Loperamide hydrochloride capsules as claimed in claim 1 and preparation method thereof, it is characterised in that the sour Lip river piperazine
Butylamine, glucose, pregelatinized starch cross 80 mesh sieves；The anhydrous silica gel, magnesium stearate cross 30 mesh sieves.
3. a kind of Loperamide hydrochloride capsules as claimed in claim 1 and preparation method thereof, including drug particles and hollow glue
Capsule, it is characterised in that：
The mass ratio of the drug particles and the Capsules is (4~6):1；
The drug particles include the raw material of following parts by weight：
The Capsules includes the raw material of following parts by weight：
A kind of 4. Loperamide hydrochloride capsules as claimed in claim 1 and preparation method thereof, it is characterised in that：
Affiliated drug particles include the raw material of following parts by weight：
Preferably, the Capsules includes the raw material of following parts by weight：
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711182585.3A CN107744513A (en) | 2017-11-23 | 2017-11-23 | A kind of Loperamide hydrochloride capsules and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711182585.3A CN107744513A (en) | 2017-11-23 | 2017-11-23 | A kind of Loperamide hydrochloride capsules and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107744513A true CN107744513A (en) | 2018-03-02 |
Family
ID=61252279
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711182585.3A Withdrawn CN107744513A (en) | 2017-11-23 | 2017-11-23 | A kind of Loperamide hydrochloride capsules and preparation method thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN107744513A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108553435A (en) * | 2018-06-08 | 2018-09-21 | 华益药业科技(安徽)有限公司 | A kind of Valsartan piece and preparation method thereof |
-
2017
- 2017-11-23 CN CN201711182585.3A patent/CN107744513A/en not_active Withdrawn
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108553435A (en) * | 2018-06-08 | 2018-09-21 | 华益药业科技(安徽)有限公司 | A kind of Valsartan piece and preparation method thereof |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| WW01 | Invention patent application withdrawn after publication | ||
| WW01 | Invention patent application withdrawn after publication |
Application publication date: 20180302 |