CN102846607A - Solid preparation comprising cevimeline hydrochloride as active component and application thereof - Google Patents
Solid preparation comprising cevimeline hydrochloride as active component and application thereof Download PDFInfo
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- CN102846607A CN102846607A CN2012101017689A CN201210101768A CN102846607A CN 102846607 A CN102846607 A CN 102846607A CN 2012101017689 A CN2012101017689 A CN 2012101017689A CN 201210101768 A CN201210101768 A CN 201210101768A CN 102846607 A CN102846607 A CN 102846607A
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- solid preparation
- cevimeline hydrochloride
- cevimeline
- calcium
- sodium
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Abstract
The invention relates to a solid preparation comprising cevimeline hydrochloride as an active component and application thereof. The solid preparation is an oral solid preparation prepared by carrying out pharmaceutical technology on cevimeline hydrochloride and pharmaceutically acceptable auxiliary materials. The solid preparation disclosed herein has the advantages of stable and controllable quality, safety and effectiveness, and is mainly clinically used as a medicine for treating dry mouth symptom for sicca syndrome paitients.
Description
Technical field
The present invention relates to a kind of oral solid formulation of cevimeline hydrochloride.It is oral ordinary tablet, freeze-dried instant sheet, Film coated tablets, enteric coatel tablets, hard capsule and the granule that cevimeline hydrochloride and pharmaceutically acceptable adjuvant are made by preparation technique.Cevimeline hydrochloride solid preparation of the present invention and application quality thereof are stable, controlled, safe and effective, belong to medical technical field.
Background technology
Sjogren syndrome can individualism, also can appear in other autoimmune diseases, the individualism person is primary Sjogren's syndrome (1SS), is secondary Sjogren syndrome (2SS) and be secondary to other autoimmune such as rheumatoid arthritis, systemic sclerosis, systemic lupus erythematosus (sle) patient.The primary disease sickness rate is high, is a global disease, is mainly in women more than 40 years old.Its pathomechanism mainly is because autoimmune excessive responsing reaction causes the large amount lymphocyte of exocrine gland, plasmocyte infiltrating, and gland cell is destroyed, afunction, thus a series of clinical symptoms and performance appear.
Sjogren syndrome approximately 80% patient has the xerostomia performance, although other patient's salivary flows reduce no conscious sympton.Serious xerostomia person carries water tumbler, needs again and again drinking-water during speech, and advancing the food difficulty needs water to send down, and the drinking-water of waking up midnight quenches one's thirst or does from sleep soundly and wake up.Pathological changes is often involved lung, liver, kidney, gastrointestinal, skin, joint and lymph etc., Chang Jifa rheumatoid arthritis, lupus erythematosus, polymyositis, arteritis nodosa etc. simultaneously can concurrent chronic active hepatitis, malignant lymphoma and the allergic vasculitis such as skein cell tumor.
At present both at home and abroad modern medicine is without effective medicine, can only anti symptom treatment, and as using artificial saliva, often gargle with saliva stimulating glandular secretion function with citric acid soln and replace part saliva, smear before the meal the oral cavity with 2% methylcellulose and can improve symptom etc. by chance.The primary disease course of disease is slow, depend on pathological changes involve scope and with other diseases, the case of pseudolymphoma is needed close observation, and it lapses to, and malignant lymphoma person's poor prognosis occurs.
Adopt the technology of the present invention that cevimeline hydrochloride is prepared into solid preparation, not only expanded the dosage form range of application of cevimeline hydrochloride, particularly through the selection to the present invention's prescription, obtained the sense of taste good, taking convenience, disintegrate rapidly, absorb soon, rapid-action, bioavailability is high, can improve the curative effect for the treatment of sjogren syndrome patient xerostomia symptom, taking convenience, and preparation method is simple, is fit to large-scale production.
Summary of the invention
The purpose of this invention is to provide a kind of disintegrate fast, absorb rapidly, bioavailability and blood drug level that can the Effective Raise medicine improve the cevimeline hydrochloride solid preparation of taste, taking convenience, few side effects simultaneously.
Cevimeline hydrochloride solid preparation provided by the invention contains cevimeline hydrochloride active ingredient and the excipient substance that is fit to make solid preparation, and wherein the percentage by weight of cevimeline hydrochloride is 10-70%, and the percentage by weight of adjuvant is 30-90%.Every of described cevimeline hydrochloride solid preparation preferably contains cevimeline hydrochloride 10-100mg.
Described oral administration solid preparation is oral ordinary tablet, freeze-dried instant sheet, Film coated tablets, enteric coatel tablets, hard capsule, granule, oral cavity disintegration tablet, the effervescent tablet of making by preparation technique with cevimeline hydrochloride and pharmaceutically acceptable adjuvant.
The specification of cevimeline hydrochloride is per unit dosage 10-100mg; Pharmaceutically acceptable adjuvant can be filler, binding agent, disintegrating agent, lubricant, correctives (necessity) and coating materials.Wherein filler includes but not limited to lactose, sucrose, glucose, mannitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium phosphate, calcium carbonate, calcium bicarbonate, starch, carboxymethyl starch, pregelatinized Starch or microcrystalline Cellulose; Binding agent includes but not limited to starch, gelatin dextrin, maltodextrin, sucrose, arabic gum, polyvinylpyrrolidone, various viscosity methylcellulose, low viscosity carboxymethyl cellulose, various viscosity ethyl cellulose, various viscosity polyvinyl alcohol, polyethylene glycol 6000 or the following hyprolose of 50mpaS; Disintegrating agent includes but not limited to pregelatinized Starch, microcrystalline Cellulose, alginic acid, pure wood fiber element, carboxymethyl starch sodium, guar gum, crospolyvinylpyrrolidone, methylcellulose or cross-linking sodium carboxymethyl cellulose; Lubricant includes but not limited to magnesium stearate, calcium stearate, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, PEG 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, sodium chloride, sodium laurylsulfate or magnesium laurylsulfate; Correctives includes but not limited to steviosin, sorbitol, maltose alcohol, glycyrrhizin, stem tea element, Sodium Cyclamate, flavoring banana essence, flavoring pineapple essence, Mint Essence, Fructus Foeniculi, vanillin, Fructus Citri Limoniae essence, cherry essence or rose essence.
Pharmaceutical preparation of the present invention also comprises wetting agent, is purified water or ethanol etc.The used coating material of the present invention includes but not limited to cellulose and derivant thereof, crylic acid resin, ethene polymers etc.
The specific embodiment:
Following case study on implementation is used for explaining the present invention, but is not limited to this.
Embodiment 1
Make 1000 cevimeline hydrochloride sheets with the raw material of following weight proportion.
Preparation technology:
1. the cevimeline hydrochloride crude drug was pulverized 80 mesh sieves, and was for subsequent use.
2. lactose is crossed 60 mesh sieves, and is for subsequent use.
3. get cevimeline hydrochloride, add lactose, hyprolose, fully mix homogeneously.
4. with purified water soft material processed, 20 mesh sieves are granulated, 60 ℃ of dryings, 24 mesh sieve granulate.
5. add the abundant mix homogeneously of magnesium stearate, tabletting, and get final product.
Embodiment 2
1. prepare 6% Opadry enteric coating agents alcoholic solution;
2. get embodiment 1 gained element sheet, pour in the coating pan, start coating pan, and blowing hot-air, at 30-40 ℃ of preheating 10min, and blow plain sheet off adhere on the label medicated powder, evenly spray into coating solution, medicinal liquid is evenly coated on the label, namely get the cevimeline hydrochloride enteric coatel tablets.
Embodiment 3:
Make 1000 cevimeline hydrochloride sheets with the raw material of following weight ratio.
Preparation method:
1. the cevimeline crude drug was pulverized 80 mesh sieves, for subsequent use.
2. lactose is crossed 60 mesh sieves, and is for subsequent use.
3. get cevimeline hydrochloride and pregelatinized Starch, lactose, the abundant mix homogeneously of microcrystalline Cellulose.
4. with water soft material processed, 20 orders are granulated, 60 ℃ of oven dry, 24 order granulate.
5. add cross-linking sodium carboxymethyl cellulose, the abundant mix homogeneously of magnesium stearate, tabletting, and get final product.
Embodiment 4:
1. prepare the common gastric solubleness coating solution of Opadry
2. get embodiment 3 gained element sheet, pour in the coating pan, start coating pan, and blowing hot-air, at 30-40 ℃ of preheating 10min, and blow plain sheet off adhere on the label medicated powder, evenly spray into coating solution, medicinal liquid is evenly coated on the label, namely get cevimeline hydrochloride general thin garment piece.
Embodiment 5:
Make 1000 cevimeline hydrochloride capsules with the raw material of following weight proportion.
Preparation technology:
1. cevimeline hydrochloride raw material and adjuvant are pulverized respectively, crossed 80 mesh sieves.
2. get cevimeline hydrochloride with 5% starch slurry soft material processed, 24 orders are granulated, dry after granulate.
3. add carboxymethyl starch sodium, the abundant mix homogeneously of magnesium stearate, be packed in the capsulae vacuus and get final product.
Embodiment 6:
Make 1000 cevimeline hydrochloride capsules with the raw material of following weight proportion.
Preparation technology:
1. the cevimeline hydrochloride crude drug was pulverized 80 mesh sieves, and was for subsequent use.
2. lactose is crossed 60 mesh sieves, and is for subsequent use.
3. get cevimeline hydrochloride, add lactose, hyprolose, fully mix homogeneously.
4. with purified water soft material processed, 20 mesh sieves are granulated, 60 ℃ of dryings, 24 mesh sieve granulate.
5. add the abundant mix homogeneously of magnesium stearate, be packed in the capsulae vacuus and get final product.
Embodiment 7
Make 1000 bags of cevimeline hydrochloride granules with the raw material of following weight proportion,
Preparation technology:
Get cevimeline hydrochloride and other each adjuvant, pulverize respectively, cross 80 mesh sieves, abundant mixing, with purified water soft material processed, 14 mesh sieves are granulated, drying, granulate, packing, and get final product.
Embodiment 8
Make 1000 cevimeline hydrochloride freeze-dried instant sheets with the raw material of following weight proportion
Preparation technology:
Get the 500ml purified water, add the recipe quantity cevimeline hydrochloride, adding mannitol, essence, trichlorine sugarcane stir and make dissolving, transfer pH value to 5.0-7.5 with sodium citrate solution, and quantitative separating is put lyophilizing in the freezer dryer in mould, get the freeze-dried instant sheet.
The lyophilization condition is :-40 ℃ of pre-freezes 4 hours, and the phase I is warming up to-10 ℃, time 2 h, vacuum drying 12 hours, second stage heats up in 1 hour from-10 ℃～30 ℃, and is incubated 4 hours.
Embodiment 9
Make 1000 cevimeline hydrochloride oral cavity disintegration tablets with the raw material of following weight proportion
Preparation technology:
1. cevimeline hydrochloride raw material and adjuvant are pulverized respectively, crossed 80 mesh sieves.
2. get cevimeline hydrochloride and pregelatinized Starch, microcrystalline Cellulose, the abundant mix homogeneously of carboxymethyl starch sodium, with
Water is binding agent soft material processed, and 20 mesh sieves are granulated, after the drying, and 24 mesh sieve granulate.
3. add cross-linking sodium carboxymethyl cellulose, sucralose, Fructus Citri Limoniae essence and the abundant mix homogeneously of magnesium stearate, press
Sheet, and get final product.
Embodiment 10
Make 1000 cevimeline hydrochloride effervescent tablets with the raw material of following weight proportion
Claims (8)
1. the present invention is a kind of solid preparation take cevimeline hydrochloride as active component, it is the solid preparation of making by preparation technique with single dose cevimeline hydrochloride and pharmaceutically acceptable adjuvant, includes but not limited to following dosage form ordinary tablet, freeze-dried instant sheet, Film coated tablets, enteric coatel tablets, effervescent tablet, oral cavity disintegration tablet, hard capsule, granule.
2. cevimeline hydrochloride solid preparation as claimed in claim 1 is characterized in that, the specification of the cevimeline hydrochloride in described each prescription is per unit dosage 10-100mg.
3. cevimeline hydrochloride solid preparation as claimed in claim 1 is characterized in that, its pharmaceutically acceptable adjuvant can be filler, binding agent, disintegrating agent, lubricant, correctives (necessity) and coating materials.
4. cevimeline hydrochloride solid preparation as claimed in claim 3, it is characterized in that, filler includes but not limited to lactose, sucrose, glucose, mannitol, sorbitol, calcium sulfate, calcium gluconate, calcium hydrogen phosphate, calcium phosphate, calcium carbonate, calcium bicarbonate, starch, carboxymethyl starch, pregelatinized Starch, microcrystalline Cellulose, hydroxypropyl cellulose.
5. cevimeline hydrochloride solid preparation as claimed in claim 3, it is characterized in that, binding agent includes but not limited to hyprolose, gelatin, dextrin, maltodextrin, sucrose, arabic gum, polyvinylpyrrolidone, methylcellulose, carboxymethyl cellulose, ethyl cellulose, polyvinyl alcohol, polyethylene glycols or starch.
6. cevimeline hydrochloride solid preparation as claimed in claim 3, it is characterized in that, disintegrating agent includes but not limited to pregelatinized Starch, microcrystalline Cellulose, alginic acid, pure wood fiber element, carboxymethyl starch sodium, guar gum, crospolyvinylpyrrolidone, methylcellulose, cross-linking sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose or gas-producing disintegrant.
7. cevimeline hydrochloride solid preparation as claimed in claim 3, it is characterized in that, lubricant includes but not limited to magnesium stearate, calcium stearate, zinc stearate, colloidal silica, sodium stearyl fumarate, Pulvis Talci, glyceryl monostearate, Macrogol 4000, polyethylene glycol 6000, PEG 8000, sodium benzoate, adipic acid, fumaric acid, boric acid, leucine, sodium chloride, sodium laurylsulfate or magnesium laurylsulfate.
8. preparation according to claim 1 can be used for the treatment of sjogren syndrome patient's xerostomia symptom.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012101017689A CN102846607A (en) | 2012-04-09 | 2012-04-09 | Solid preparation comprising cevimeline hydrochloride as active component and application thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012101017689A CN102846607A (en) | 2012-04-09 | 2012-04-09 | Solid preparation comprising cevimeline hydrochloride as active component and application thereof |
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| Publication Number | Publication Date |
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| CN102846607A true CN102846607A (en) | 2013-01-02 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012101017689A Pending CN102846607A (en) | 2012-04-09 | 2012-04-09 | Solid preparation comprising cevimeline hydrochloride as active component and application thereof |
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5340821A (en) * | 1992-07-10 | 1994-08-23 | Snow Brand Milk Products Co., Ltd. | Composition and method for treating Sjoegren syndrome disease |
| CN1819846A (en) * | 2004-05-21 | 2006-08-16 | 千寿制药株式会社 | Ophthalmic percutaneously absorbed preparation containing muscarinic receptor agonist |
-
2012
- 2012-04-09 CN CN2012101017689A patent/CN102846607A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5340821A (en) * | 1992-07-10 | 1994-08-23 | Snow Brand Milk Products Co., Ltd. | Composition and method for treating Sjoegren syndrome disease |
| CN1819846A (en) * | 2004-05-21 | 2006-08-16 | 千寿制药株式会社 | Ophthalmic percutaneously absorbed preparation containing muscarinic receptor agonist |
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Application publication date: 20130102 |