CN105832686A - Hydrochloride lorcaserin dispersible tablet and preparation method thereof - Google Patents
Hydrochloride lorcaserin dispersible tablet and preparation method thereof Download PDFInfo
- Publication number
- CN105832686A CN105832686A CN201610406047.7A CN201610406047A CN105832686A CN 105832686 A CN105832686 A CN 105832686A CN 201610406047 A CN201610406047 A CN 201610406047A CN 105832686 A CN105832686 A CN 105832686A
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- Prior art keywords
- hydrochloric acid
- dispersible tablet
- lorcaserin
- acid lorcaserin
- mixture
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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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
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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 discloses a hydrochloride lorcaserin dispersible tablet, which is used for treating obesity. Hydrochloride lorcaserin is used as raw materials; auxiliary materials are added; the hydrochloride lorcaserin dispersible tablet is prepared. The disintegration speed is high; the absorption speed is high; the bioavailability is high; the taking is convenient; the intestinal tract residue is little; the side effect is low; the taste is sweet; fragrance is realized. Particularly, the medicine taking compliance can be easily improved; the mouthfeel of the preparation is improved; a sticking phenomenon cannot be caused in the granulation and tabletting process; the industrial production can be favorably realized.
Description
Technical field
The present invention relates to a kind of hydrochloric acid lorcaserin novel form, particularly to be hydrochloric acid lorcaserin dispersible tablet and preparation method thereof.
Background technology
Obesity refers to a certain degree of the most overweight blocked up with fat deposit, is body fat, a kind of state that especially triglyceride accumulation too much causes.It does not refer to that simple body weight increases, but the state that body fat tissue savings is superfluous.Due to food intake too much or the change of organism metabolism and cause body fat accumulation too much to cause excess weight increase and cause human pathology, physiological change or hide.
Constitutional and family, the relevant and bad dietary habit motion of the personal lifestyle custom environment such as socio-economic development culture background is not enough.
Men and women's body fat occupies goes here and there more or less difference, but substantially about 20%.Body fat has how many, say, that body fat occupation rate=fat weight/body weight.General adolescence (12 years old) boy and girl's body fat generally 20%, drops to 15% to 18 years old male, and women rises to more than 20%.Within more than 18 years old, men and women is the most in rising trend.Regular fat percentage male is 15% one 20%, and women is 20% one 25%.As from 20% increase to 25% one 30% time, then be exactly fat
Simple Obesity is modal one in all kinds of obesity, accounts for about the 95% of obese people.This kind of systemic Fat Distribution ratio is more uniform, does not has endocrine regulation phenomenon, and also without dysbolismus disease, often there is fat medical history in its family.This obesity mainly caused by inherited genetic factors and overnutrition, referred to as Simple Obesity.
Simple Obesity refers to that the heat that human body is taken in exceedes its heat consumed, and causes fat constituent to accumulate the too much obesity formed in vivo.Due to food intake too much or the change of organism metabolism and cause body fat accumulation too much to cause excess weight increase and cause human pathology, physiological change or hide.Evaluation criteria: bluntness=(ABW-standard body weight) ÷ standard body weight × ± 100%.Interior because natural endowment is insufficiency of the spleen, outer because of surfeit delicious food, few labor drowsiness, cause deficiency of the spleen causing weakness of QI, raw in phlegm-damp；Or older deficiency of the kidney, imbalance of YIN and YANG, expectorant stasis of blood inner product, raw in all can making turbid pathogen, stop up long-pending internal, and it is fat to cause fat.The obesity that fat cellular mast causes is referred to as acquired obesity.
Dispersible tablet is a kind of quick-effective preparation that development in recent years is got up, and due to its distinctive advantage, is the most increasingly paid close attention to by people.Solubilizing agent can be added；The dissolution of hydrochloric acid lorcaserin insoluble drug can be improved, be suitable for taking.Sheet is made for the medicine that disintegrate is difficult can beneficially absorb.The feature of sheet: 1. disintegrate is fast, it is fast to absorb, bioavailability is high；2. taking convenience 3. intestinal residual is few, few side effects.
Summary of the invention
It is an object of the invention to provide a kind of hydrochloric acid lorcaserin dispersible tablet and preparation method thereof.
Objects of the present invention are achieved through the following technical solutions.
Hydrochloric acid lorcaserin dispersible tablet of the present invention is become to be grouped into (percentage by weight) by following:
| Hydrochloric acid lorcaserin | 10-45% |
| Filler | 10-30% |
| Disintegrating agent | 10-25% |
| Binding agent | 0.1-6% |
| Solubilizing agent | 0.1-6% |
| Lubricant | 0.5-5%。 |
It is more than the basic prescription of the present invention, can the most suitably regulate and delete.
Hydrochloric acid lorcaserin is active component, preferred content scope 10-40%, further preferred scope 10-30%.Hydrochloric acid lorcaserin dosage 10-150mg in unit formulation, preferred dose is 10-100mg, preferred dosage is 10,20,100mg.
Due to dispersible tablet require in water can rapidly disintegrate dispersed, have taking convenience, disintegrate rapidly, absorb soon and bioavailability high.Therefore the selection to supplementary product kind and performance thereof is the key preparing sheet.Inventor is through test of many times, it is determined that be suitable for pharmaceutic adjuvant and the consumption thereof of hydrochloric acid lorcaserin dispersible tablet.
Filler selects the weight and volume being used for increasing sheet, in order to the molding of preparation and divided dose.The filler mixture of one or more in lactose, sucrose, microcrystalline Cellulose, pregelatinized Starch, dextrin etc. in the present invention.The preferred 10-30% of amount ranges, particularly preferred 15-25%.
Disintegrating agent is selected from the pharmaceutic adjuvant such as low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone.The preferred 10-25% of consumption, particularly preferred 15-20%.
The kind of solubilizing agent and the selection of consumption are most important for the dissolution of this preparation.One of sodium lauryl sulphate, polyethylene glycol 6000, Macrogol 4000, Tween 80, polysorbate40, sorbester p18, span 40 or the most several mixture are selected in the solubilizing agent of the present invention, mask the bad strange taste of hydrochloric acid lorcaserin further, improve the mouthfeel of sheet.
The lubricant mixture of one or more in micropowder silica gel, magnesium stearate, Pulvis Talci.
Present invention also offers the preparation method of hydrochloric acid lorcaserin dispersible tablet.Hydrochloric acid lorcaserin dispersible tablet of the present invention can be prepared with direct powder compression.Direct powder compression preparation process is: after uniform to hydrochloric acid lorcaserin and filler (such as lactose), disintegrating agent, solubilizing agent, binding agent and mix lubricant, direct powder compression.
Hydrochloric acid lorcaserin dispersible tablet disintegrate of the present invention is fast, it is fast to absorb, bioavailability is high；Taking convenience；Intestinal residual is few, few side effects；Taste is sweet, does not has hydrochloric acid lorcaserin off-odor and has fragrance, is particularly easy to improve patient's drug compliance.
Detailed description of the invention
Embodiment
l
Prescription:
Preparation method:
(1) hydrochloric acid lorcaserin powder (200 mesh) is mixed homogeneously with cane sugar powder (150 mesh) equal increments, obtain mixture A；
(2) after remaining adjuvant being crossed 200 mesh sieves, equal increments mix homogeneously, obtain mixture B；
(3) after mixture A and mixture B being pressed equal increments method mix homogeneously, direct compression.
Embodiment
2
Prescription:
Preparation method:
(1) hydrochloric acid lorcaserin powder (200 mesh) is mixed homogeneously with lactose powder (150 mesh) equal increments, obtain mixture A；
(2) after remaining adjuvant being crossed 200 mesh sieves, equal increments mix homogeneously, obtain mixture B；
(3) after mixture A and mixture B being pressed equal increments method mix homogeneously, direct compression.
Embodiment
3
Prescription:
Preparation method:
(1) hydrochloric acid lorcaserin powder (200 mesh) is mixed homogeneously with lactose powder (150 mesh) equal increments, obtain mixture A；
(2) after remaining adjuvant being crossed 200 mesh sieves, equal increments mix homogeneously, obtain mixture B；
(3) after mixture A and mixture B being pressed equal increments method mix homogeneously, direct compression.
Embodiment
4
Prescription:
Preparation method:
(1) hydrochloric acid lorcaserin powder (200 mesh) is mixed homogeneously with lactose powder (150 mesh) equal increments, obtain mixture A；
(2) after remaining adjuvant being crossed 200 mesh sieves, equal increments mix homogeneously, obtain mixture B；
(3) after mixture A and mixture B being pressed equal increments method mix homogeneously, direct compression.
Invention formulation and technology prepares the study on the stability of sample:
Sample prepared by embodiment 1, embodiment 2, embodiment 3 and embodiment 4 is respectively placed in stability test case, arrange temperature 40 DEG C, carry out under the conditions of relative humidity 75%RH three months accelerating to investigate.
Using disintegration as inspection target, it was demonstrated that the science of the tablet recipe technique invented.
Hydrochloric acid lorcaserin raw material used by above example is that Pfizer's Pharmaceutical produces；Producer supplied by adjuvant is Ka Lekang pharmacy, Degussa pharmacy, Le Jiawen pharmacy, International Specialty Products pharmaceutical Co. Ltd and the mountains and rivers, Huainan pharmaceutical Co. Ltd.
Claims (8)
1. a hydrochloric acid lorcaserin dispersible tablet, is made up of following weight percent composition:
Hydrochloric acid lorcaserin dispersible tablet according to claim 1, wherein said:
The filler mixture of one or more in microcrystalline Cellulose, lactose, sucrose, pregelatinized Starch, dextrin etc.；
Disintegrating agent is selected from one of low-substituted hydroxypropyl methylcellulose, polyvinylpolypyrrolidone, carboxymethyl starch sodium, cross-linking sodium carboxymethyl cellulose or the most several mixture；
Binding agent is selected from polyvidone, high replacement one of hydroxypropylcellulose, gelatine size, starch slurry, sodium carboxymethyl cellulose or several mixture therein；
The lubricant mixture of one or more in micropowder silica gel, magnesium stearate, Pulvis Talci.
Hydrochloric acid lorcaserin dispersible tablet the most according to claim 1, wherein said hydrochloric acid lorcaserin content range 10-45%.
Hydrochloric acid lorcaserin dispersible tablet the most according to claim 1, wherein said filler loading scope 10-30%.
Hydrochloric acid lorcaserin dispersible tablet the most according to claim 1, wherein said disintegrating agent consumption 15-20%.
Hydrochloric acid lorcaserin dispersible tablet the most according to claim 1, wherein said binder dosage 0.5-2%.
6. according to the hydrochloric acid lorcaserin dispersible tablet described in any claim in claim 2-5, wherein: hydrochloric acid lorcaserin content range 10-40%；Filler loading 10-30%；Disintegrating agent consumption 15-20%；Binder dosage 0.5-2%, solubilizing agent consumption 0.5-2%.
Hydrochloric acid lorcaserin dispersible tablet the most according to claim 1, wherein said hydrochloric acid lorcaserin unit dose 10-100mg.
8. the preparation method of hydrochloric acid lorcaserin dispersible tablet described in claim 1, uses direct powder compression, after uniform to hydrochloric acid lorcaserin and filler, disintegrating agent, solubilizing agent, binding agent and mix lubricant, and direct powder compression.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610406047.7A CN105832686A (en) | 2016-06-12 | 2016-06-12 | Hydrochloride lorcaserin dispersible tablet and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201610406047.7A CN105832686A (en) | 2016-06-12 | 2016-06-12 | Hydrochloride lorcaserin dispersible tablet and preparation method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN105832686A true CN105832686A (en) | 2016-08-10 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201610406047.7A Pending CN105832686A (en) | 2016-06-12 | 2016-06-12 | Hydrochloride lorcaserin dispersible tablet and preparation method thereof |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106166156A (en) * | 2016-08-31 | 2016-11-30 | 安徽省润生医药股份有限公司 | A kind of hydrochloric acid green card color Linkou County cavity disintegrating tablet and preparation method thereof |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104721192A (en) * | 2015-03-24 | 2015-06-24 | 南京昂谷医药科技有限公司 | Pharmaceutical composition containing lorcaserin and medical application of pharmaceutical composition |
| CN105228986A (en) * | 2014-04-21 | 2016-01-06 | 杭州普晒医药科技有限公司 | A kind of chlorine Ka Selin eutectic and preparation method thereof, pharmaceutical composition and purposes |
| CN105456212A (en) * | 2015-12-18 | 2016-04-06 | 北京万全德众医药生物技术有限公司 | Hydrochloric lorcaserin tablets and preparing method thereof |
-
2016
- 2016-06-12 CN CN201610406047.7A patent/CN105832686A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105228986A (en) * | 2014-04-21 | 2016-01-06 | 杭州普晒医药科技有限公司 | A kind of chlorine Ka Selin eutectic and preparation method thereof, pharmaceutical composition and purposes |
| CN104721192A (en) * | 2015-03-24 | 2015-06-24 | 南京昂谷医药科技有限公司 | Pharmaceutical composition containing lorcaserin and medical application of pharmaceutical composition |
| CN105456212A (en) * | 2015-12-18 | 2016-04-06 | 北京万全德众医药生物技术有限公司 | Hydrochloric lorcaserin tablets and preparing method thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106166156A (en) * | 2016-08-31 | 2016-11-30 | 安徽省润生医药股份有限公司 | A kind of hydrochloric acid green card color Linkou County cavity disintegrating tablet and preparation method thereof |
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Application publication date: 20160810 |