CN107913260A - A kind of loperamide hydrochloride soft capsule and preparation method thereof - Google Patents
A kind of loperamide hydrochloride soft capsule and preparation method thereof Download PDFInfo
- Publication number
- CN107913260A CN107913260A CN201711202575.1A CN201711202575A CN107913260A CN 107913260 A CN107913260 A CN 107913260A CN 201711202575 A CN201711202575 A CN 201711202575A CN 107913260 A CN107913260 A CN 107913260A
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- China
- Prior art keywords
- loperamide hydrochloride
- soft capsule
- sorbierite
- weight
- preparation
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- 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.)
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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
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
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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 present invention relates to technical field of medicine, more particularly to a kind of loperamide hydrochloride soft capsule and preparation method thereof：Loperamide hydrochloride, polyethylene glycol 400, sorbierite, the citric acid filling liquid as made from certain compounding method, pressing loads gelatin glycerine, sorbierite and purified water and conventional rubber is made, and grain is made and weighs the yellowish soft capsule loperamide hydrochloride soft capsule of 0.3~0.5g active constituent contents 2mg/.On the premise of loperamide hydrochloride stability is not changed, loperamide hydrochloride formulation is changed, there is the characteristics of convenient to take, active ingredient rate of release is fast, works rapid, and compliance is good.
Description
Technical field
The present invention relates to technical field of medicine, more particularly to a kind of loperamide hydrochloride soft capsule and its preparation side
Method.
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 haloperidol and pethidine, but therapeutic dose Central nervous system is without any effect.Loperamide hydrochloride be Ah
Piece receptor stimulating agent, its mechanism of action are:Released by the opiate receptor and retardance acetylcholine and prostaglandin that suppress intestinal wall
Put, the contraction of antagonism smooth muscle, reach and reduce enterocinesia and secretion, extend the holdup time of intestinal contents, so as to play antidiarrheal
Effect.
Loperamide hydrochloride be white or off-white color crystalline powder, almost odorless, bitter.In ethanol or glacial acetic acid
It is readily soluble, 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 medicament is used clinically for the symptomatic treatment of non-infectious acute and chronic diarrhea caused by a variety of causes.
But the patent medicine preparation also has its certain shortcoming.For example, common loperamide hydrochloride preparation is mostly on the market
Capsule or tablet, and in paediatrics and old medicine, there are about 50% people and have any problem to swallowing tablet and capsule, hydrochloric acid Lip river
Piperazine butylamine capsule or Tabules have impact on the compliance of drug therapy.It is understood that in order to solve drawbacks described above, this hair
It is bright to propose a kind of loperamide hydrochloride soft capsule and preparation method thereof.
The content of the invention
The present invention provides a kind of loperamide hydrochloride soft capsule and preparation method thereof, and not changing, loperamide hydrochloride is steady
Under the premise of qualitatively, change formulation, have convenient to take, active ingredient rate of release is fast, works rapid, the good spy of compliance
Point.
The present invention provides a kind of loperamide hydrochloride soft capsule and preparation method thereof, it is characterised in that the method is by as follows
Step carries out：
1) preparation of filling liquid：Take 1 parts by weight loperamide hydrochloride to add Purified Water q. s, add the poly- second of 20~30 parts by weight
Glycol -400, stirring add 0.1~0.3 parts by weight sorbierite and stir to dissolving, add 0.1~0.5 parts by weight of lemon to dissolving
Acid adjusts acidity 4.5~7.0, the solution clarified；
2) preparation of rubber：Select 0.8~1.2 parts by weight gelatin, 0.3~1 glycerine, 0.3~1 sorbierite and 0.8~1.2
Conventional rubber is made in purified water；
3) soft capsule die pressing：Filling liquid made from step 1), pressing load rubber, are pressed into a kind of hydrochloric acid Lip river piperazine fourth
Amine soft capsule.
As preferred means, plasticizer is made in step 2) glycerine and sorbierite mixing, and plasticizer and gelatin weight ratio are (0.4
~0.8):1.0；Gelatin is 1 with purified water weight ratio:1.
As preferred means, polyethylene glycol-400, sorbierite, citric acid used in step 1) are food grade materials or medicinal
Level raw material；Gelatin, glycerine, sorbierite, purified water used in step 2) are food grade materials or pharmaceutical grade raw material.
As preferred means, step 1) and step 2) are carried out at 20~30 DEG C under the conditions of RH40%~60%；Step 3) exists
20~30 DEG C, carried out less than under the conditions of RH40%.
As preferred means, a kind of obtained loperamide hydrochloride soft capsule, it is characterised in that loperamide hydrochloride flexible glue
Capsule weighs the yellowish soft capsule of 0.3~0.5g for active ingredient loperamide hydrochloride content 2mg/, grain.
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
Take 2g loperamide hydrochlorides to add Purified Water q. s, add 40g polyethylene glycol-400, stirring adds 0.2g to dissolving
Sorbierite is stirred to dissolving, is added dilute hydrochloric acid and is adjusted acidity to 4.5, adds purified water and be settled to 100ml filling liquids；It is obtained to fill out
Filling liquid pressing loads rubber, suppresses soft capsule 1000, it is dry both a kind of loperamide hydrochloride soft capsule.
Embodiment 2
Take 2g loperamide hydrochlorides to add Purified Water q. s, add 50g polyethylene glycol-400, stirring adds 0.4g to dissolving
Sorbierite is stirred to dissolving, is added dilute hydrochloric acid and is adjusted acidity to 5.0, adds purified water and be settled to 100ml filling liquids；It is obtained to fill out
Filling liquid pressing loads rubber, suppresses soft capsule 1000, it is dry both a kind of loperamide hydrochloride soft capsule.
Embodiment 3
Taking 2g parts by weight loperamide hydrochlorides to add Purified Water q. s, polyethylene glycol-400 is added by 60g, stirring is extremely dissolved,
Add 0.6g sorbierites to stir to dissolving, add dilute hydrochloric acid and adjust acidity to 5.5, add purified water to be settled to 100ml filling liquids；System
Filling liquid pressing load rubber, suppress soft capsule 1000, it is dry both a kind of loperamide hydrochloride soft capsule.
Rubber selects 0.8~1.2 parts by weight gelatin, 0.3~1 glycerine, 0.3~1 sorbierite and 0.8~1.2 purified water system
Into conventional rubber；Glycerine and sorbierite mixing, make plasticizer, plasticizer and gelatin weight ratio are (0.4~0.8):1.0；Gelatin
It is 1 with purified water weight ratio:1.Every loperamide hydrochloride soft capsule weight 0.40g in embodiment.
Loperamide hydrochloride soft capsule recovery test：
Loperamide hydrochloride 10mg is taken, it is accurately weighed, add polyethylene glycol-400, mountain by embodiment 1~3 and preparation process
Filling liquid is made in the auxiliary materials such as pears alcohol, dilute hydrochloric acid, purified water.Take loperamide hydrochloride reference substance appropriate, it is accurately weighed, add methanol
Dissolve and be diluted to solution of the concentration for 20mg/ml as reference substance solution, take 3 bottles of this product, mix, be test solution.
Precision draws reference substance solution and each 10 μ l of test solution, injects liquid chromatograph, the measure and calculation rate of recovery, the results are shown in Table 1.
1 recovery test result (n=3) of table
The result shows that the formula rate of recovery is good.
Loperamide hydrochloride soft capsule is checked according to disintegration time limited inspection technique (two annex XA of Chinese Pharmacopoeia version in 2010), is surveyed
Determine disintegration time limited, as a result such as table 2.
Table 2 disintegration time limited result of the test
The result shows that loperamide hydrochloride soft capsule active ingredient rate of release is fast.Compared with embodiment 1 and embodiment 3,
Wherein embodiment 2 is optimization formula.
Loperamide hydrochloride Stability of Soft Capsules is tested：
2 sample of Example places 10d under the conditions of 20 DEG C, 40 DEG C, 60 DEG C respectively.Sampled when 1,3,5,10d
Investigate its character, in relation to material and assay equistability index, and compared with 0d.As a result These parameters become without obvious
Change.
Result above shows, on the premise of loperamide hydrochloride stability is not changed, changes loperamide hydrochloride agent
Type, has the characteristics of convenient to take, active ingredient rate of release is fast, works rapid, and compliance is good.
The foregoing is merely illustrative of the preferred embodiments of the present invention, is not intended to limit the invention, all essences in the present invention
Any modification made within refreshing and principle, equivalent substitution, improvement etc., are all contained within protection scope of the present invention.
Claims (5)
1. the present invention provides a kind of loperamide hydrochloride soft capsule and preparation method thereof, it is characterised in that the method is by following step
It is rapid to carry out：
1) preparation of filling liquid：Take 1 parts by weight loperamide hydrochloride to add Purified Water q. s, add the poly- second two of 20~30 parts by weight
Alcohol -400, stirring add 0.1~0.3 parts by weight sorbierite and stir to dissolving, add 0.1~0.5 parts by weight of lemon acid to dissolving
Acidity is adjusted 4.5~7.0, the solution clarified；
2) preparation of rubber：Select 0.8~1.2 parts by weight gelatin, 0.3~1 glycerine, 0.3~1 sorbierite and 0.8~1.2 purifying
Conventional rubber is made in water；
3) soft capsule die pressing：Filling liquid made from step 1), pressing load rubber, it is soft to be pressed into a kind of loperamide hydrochloride
Capsule.
2. loperamide hydrochloride soft capsule according to claim 1, it is characterised in that step 2) glycerine and sorbierite mixing,
Plasticizer is made, plasticizer and gelatin weight ratio are (0.4~0.8):1.0；Gelatin is 1 with purified water weight ratio:1.
3. loperamide hydrochloride soft capsule according to claim 1, it is characterised in that polyethylene glycol used in step 1)-
400th, sorbierite, citric acid are food grade materials or pharmaceutical grade raw material；Gelatin, glycerine used in step 2), sorbierite, purified water
For food grade materials or pharmaceutical grade raw material.
4. loperamide hydrochloride soft capsule according to claim 1, it is characterised in that step 1) and step 2) are 20~30
DEG C, carried out under the conditions of RH40%~60%；Step 3) is carried out at 20~30 DEG C less than under the conditions of RH40%.
5. loperamide hydrochloride soft capsule according to claim 1, it is characterised in that：1) active ingredient loperamide hydrochloride
Content 2mg/；2) grain weighs the yellowish soft capsule of 0.3~0.5g.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711202575.1A CN107913260A (en) | 2017-11-27 | 2017-11-27 | A kind of loperamide hydrochloride soft capsule and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201711202575.1A CN107913260A (en) | 2017-11-27 | 2017-11-27 | A kind of loperamide hydrochloride soft capsule and preparation method thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN107913260A true CN107913260A (en) | 2018-04-17 |
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ID=61897029
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201711202575.1A Withdrawn CN107913260A (en) | 2017-11-27 | 2017-11-27 | A kind of loperamide hydrochloride soft capsule and preparation method thereof |
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| CN (1) | CN107913260A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112336700A (en) * | 2019-08-08 | 2021-02-09 | 河北菲尼斯生物技术有限公司 | Stable butylphthalide-containing medicine and preparation method thereof |
-
2017
- 2017-11-27 CN CN201711202575.1A patent/CN107913260A/en not_active Withdrawn
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112336700A (en) * | 2019-08-08 | 2021-02-09 | 河北菲尼斯生物技术有限公司 | Stable butylphthalide-containing medicine and preparation method thereof |
| CN112336700B (en) * | 2019-08-08 | 2023-12-01 | 河北菲尼斯生物技术有限公司 | Stable butylphthalide-containing medicament 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 |
Application publication date: 20180417 |
|
| WW01 | Invention patent application withdrawn after publication |