CN101015519B - Loratadine oral compound medication composition - Google Patents
Loratadine oral compound medication composition Download PDFInfo
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- CN101015519B CN101015519B CN 200710078245 CN200710078245A CN101015519B CN 101015519 B CN101015519 B CN 101015519B CN 200710078245 CN200710078245 CN 200710078245 CN 200710078245 A CN200710078245 A CN 200710078245A CN 101015519 B CN101015519 B CN 101015519B
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Abstract
This invention relates to an orally adminstered compound Chinese medicinal composition of loratadine for treating cough. The composition comprises quick-release part containing loratadine and slow-release part containing centrum antitussive drug, wherein the centrum antitussive drug is preferably dextromethorphan. The invention maintains the quick and long lasting action of loratadine or desloratadine, overcomes the quick releasing and short action on relieving cough of dextromethorphan, slow releases dextromethorphan, and maintains the drug effect to arrive the purpose of relieving cough for a long time.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, be specifically related to a kind of pharmaceutical composition for oral administration of treating cough, contain the loratadine or the Desloratadine immediate release section of effective dose and contain the slow-released part of the maincenter cough medicine of effective dose, and pharmaceutic adjuvant.Said composition drug treatment cough once a day, and long-acting.
Background technology
Cough be respiratory tract disease symptom often arranged.In recent years, because the earth atmosphere pollution is serious day by day, environment for human survival worsens, and the immunologic function of human body is destroyed, and the respiratory system disease sickness rate is ascendant trend year by year, and the popular of atypical pneumonia is exactly evidence.Statistics shows, in the U.S., into Respiratory Clinic prescription on individual diagnosis patient number second coughs.According to national health department's statistics, annual nearly 300,000,000 people of China infect respiratory system disease, and the patient that wherein coughs reaches more than 5,000 ten thousand.Ministry of Public Health points out that in " national health service research " China urban and rural residents cough prevalence is 15.36%.The area that economy is flourishing, the sickness rate of respiratory system disease is high more.And the chronic cough patient also causes complication such as hypertension, cerebral anoxia, pulmonary heart disease easily.
The India Ordain Health Care product P edicof-D syrup that lists a company; Belong to the new compound of treatment cough, every 10ml contains loratadine 5mg and dextromethorphan 10mg, once a day; Be applicable to the caused dry cough of a variety of causes, anaphylaxis or respiratory tract infectious cough and smoker's cough.Wherein, dextromethorphan is a central antitussive, and antitussive is mainly used in dry cough through suppressing bulbar center, and its antitussive effect is better than codeine, but does not suppress respiratory center, no addiction property, and no analgesic activity, toxicity is low, has the characteristics of quick-acting, strong effect, safety.Loratadine is the second filial generation antihistaminic of oral quick-acting, long-acting and strong effect.The periphery histamine H1-receptor is had high selectivity, and the caused allergic symptom of competitive inhibition histamine does not have drowsiness effect and anticholinergic effect, has auxiliary treatment inflammatory and allergic cough's effect simultaneously concurrently.The mechanism of action of two kinds of compositions is complementary, treating both the principal and secondary aspects of a disease, and both the various inflammation and the anaphylaxis that cause cough simultaneously can alleviated or cure to control cough effectively again, played synergistic therapeutic action.Therefore, this prescription constitutes rationally, and is safe and effective.
However, but there is significant difference in the medicine of loratadine and the dextromethorphan moving characteristic of learning of generation.Absorb rapidly from gastrointestinal tract behind the oral dextromethorphan, approximately onset in half an hour, the blood plasma peak time is about 2.5 hours, and eliminating the half-life is 1.2-3.9 hour, continuous action to 6 hour.Absorb rapidly from gastrointestinal tract behind the oral loratadine; About 1-3 hour onset; Loratadine and major metabolite decarboxylation ethoxy loratadine blood plasma peak time thereof are about 1.3 and 2.5 hours respectively, on average eliminate the half-life to be respectively 8.4 and 28 hours, and continuous action reached more than 24 hours.It is thus clear that dextromethorphan is rapid-action, action time is short, can only respite cough symptom; The loratadine onset is relatively slow, but long action time can continue to alleviate or cure various inflammation and the anaphylaxis that causes cough.Therefore, the two is processed conventional formulation unite and take, can not guarantee simultaneously that two components can both keep effective blood drug level and common performance therapeutical effect in official hour.That is to say; Took once above-mentioned conventional formulation in one day; Possibility is enough for the patient of only performance cough in short-term, and it is not enough frequently needing the patient of lasting antitussive for those coughs, and perhaps they can only rely on extra other antitussive medicines of taking to treat.
Desloratadine is the long-acting tricyclic antidepressants antihistaminic of the strong effect of non-sedating; It is the active metabolite of loratadine; Can record its PC in oral back 30 minutes; Can and reach the highest blood drug level by good absorption after about 3 hours, its elimination half-life is about 27 hours, and acting duration reaches 24 hours.Codeine and dextromethorphan belong to the maincenter cough medicine together, through direct inhibition medulla oblongata coughing centre performance antitussive effect, and oral back onset in 30-45 minute, blood drug level peaking about 1 hour, about 2.5-4 of half-life hour, antitussive effect was kept about 4-6 hour.It is thus clear that, Desloratadine and loratadine, codeine and dextromethorphan drug effect, medicine generation with all have similar characteristics aspect medicine is moving.Therefore, can predict the compound recipe of being made up of the antihistaminic (Desloratadine or loratadine) and the maincenter cough medicine (codeine or dextromethorphan) of no sedation, its therapeutic effect and characteristics also should present proximate characteristic.That is to say,, on the mechanism of action, can play the effect of Synergistic treatment cough, yet the significant difference of pharmacokinetics characteristic has brought the deficiency in the treatment equally, promptly can not satisfy the frequent patient's of cough needs with the similar compound recipe of Pedicof-D.
The folk prescription ordinary preparation product of domestic and international loratadine that has gone on the market and dextromethorphan is numerous, dosage form is comprehensive, the product P edicof-D syrup but the rarely seen India of both compound recipes Ordain Health Care lists a company.
U.S. Pat 5980882 discloses the pharmaceutical composition of a kind of chelating agent and drug-resin complex formation; Comprising a kind of dextromethorphan slow-release suspension, the listing product has
the Dextromethorphan Polistirex of Novartis Consumer Health and the little eyebrow-dextromethorphan slow-release suspension of Shanghai Hyundai Pharmacy stock Co., Ltd.
U.S. Pat 5314697 discloses the related indication slow releasing tablet of a kind of alleviation allergic rhinitis; Wherein comprise effective dose loratadine and pseudoephedrine or their officinal salt; This patent is applied for by SCHERING PLOUGH; The listing product is CLARITIN-D 24HOUR, and domestic import is called Clarinase.
Chinese patent CN1823770 discloses a kind of compound Dextromethorphan oral cavity disintegration tablet of treating cough; Wherein comprise effective dose loratadine and dextromethorphan or their officinal salt; And the adjuvant on the pharmaceutics; It is characterized in that need not water promptly can disintegrate in the oral cavity, and disintegration time was less than 1 minute.
In sum, prior art has been described loratadine or dextromethorphan folk prescription ordinary preparation, dextromethorphan folk prescription slow releasing preparation, loratadine and pseudoephedrine compound slow release preparation and loratadine and dextromethorphan compound recipe ordinary preparation.Therefore, need that exploitation is a kind of to be used to treat cough and the loratadine that can long-acting antitussive and the pharmaceutical composition of dextromethorphan.
Summary of the invention
The objective of the invention is to overcome the deficiency of existing kind, provide a kind of and can prolong the dextromethorphan antitussive time, make itself and loratadine possess long-acting simultaneously; And can give full play to that the two is quick-acting, imitate by force and the loratadine of safety feature and the pharmaceutical composition of dextromethorphan; Further strengthened the effect and prolongation synergism time of two kinds of medicine Synergistic treatment coughs in this compound recipe,, reduced toxic and side effects in the hope of obtaining to reduce the dose number of times; Shorten the course of treatment, improve the effect of compliance.
The object of the invention is realized through following scheme:
The present invention provides a kind of Orally administered medicinal composition, it is characterized in that, said composition comprises: contain the immediate release section of loratadine or the Desloratadine or their officinal salt of effective dose, contain the slow-released part of the maincenter cough medicine of effective dose, and pharmaceutical carrier.
Orally administered medicinal composition of the present invention, its described maincenter cough medicine is dextromethorphan and codeine, preferred dextromethorphan.Here said dextromethorphan comprises dextromethorphan base and officinal salt thereof, preferred dextromethorphan hydrobromide.
Orally administered medicinal composition of the present invention, the content of wherein said principal agent loratadine or Desloratadine is 1-50mg, dextromethorphan is 1-200mg, preferred loratadine or Desloratadine 5-20mg, dextromethorphan 5-100mg.
Orally administered medicinal composition of the present invention, said slow-released part also comprises slow-release material, and the percentage by weight of its slow-release material is 5-85%, and preferred 15-75% is for accounting for the weight ratio of slow-released part.
The mixture of any one or a few in optional, the hydrogenated vegetable oil cured of above-mentioned said slow-release material, stearyl alcohol, stearic acid, glyceryl monostearate, methylcellulose, sodium carboxymethyl cellulose, hypromellose, polyvidone, card wave spectrum, sodium alginate, chitosan, ethyl cellulose, polymethacrylates, non-toxic polyvinyl chloride, polyethylene, ethylene-vinyl acetate copolymer, cellacefate, acrylic resin, hypromellose phthalate ester, Hydroxypropyl Methyl Cellulose Phthalate, gelatin, carboxymethyl cellulose, polyvinyl alcohol and the dextran from animal fat, Cera Flava, babassu, the mixture of any one or a few in preferred stearyl alcohol, stearic acid, hypromellose, sodium alginate, ethyl cellulose and the acrylic resin.
Orally administered medicinal composition of the present invention is a slow releasing preparation, can be slow releasing tablet, slow releasing pill, sustained-release granular formulation, slow releasing capsule, slow release solution and slow-release suspension, preferred slow releasing tablet and slow releasing capsule.
Above-mentioned said slow releasing tablet can be double-layer tablet or multilayer tablet, and immediate release section is a release layer, and slow-released part is a slow release layer.Said double-layer tablet can be a levels, also can be inside and outside two layers, and wherein internal layer is slow-released part (for nuclear), and skin is an immediate release section, and middle in case of necessity can have the coating sealing coat.
Pharmaceutical composition of the present invention, above-mentioned said pharmaceutical carrier (adjuvant) comprise any one or a few the mixture in filler, binding agent, disintegrating agent and the lubricant.Wherein, described filler is any one or a few the mixture in mannitol, microcrystalline Cellulose, starch, pregelatinized Starch, calcium hydrogen phosphate, sucrose, lactose, red bright alcohol, sorbitol and the xylitol; Described binding agent is any one or a few the mixture in starch, cellulose derivative, polyvidone, gelatin and the Polyethylene Glycol; Described disintegrating agent is starch, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone; Described lubricant is any one or a few the mixture in micropowder silica gel, Pulvis Talci, magnesium stearate, Stepanol MG, hydrogenated vegetable oil, hydrated silica gel sodium and the Semen Tritici aestivi starch.
The Orally administered medicinal composition of treatment cough of the present invention comprises two kinds of principal agents, and wherein dextromethorphan is a cough medicine, and for slow release discharges, loratadine or Desloratadine are antihistaminic, for rapid release discharges.Said principal agent composition is respectively its original shape form or other pharmaceutically acceptable salts.In the said slow releasing preparation, each dosage unit contains loratadine or Desloratadine 1-50mg, preferred 1-20mg, and dextromethorphan is 1-200mg, preferred 5-100mg.
In order to make dextromethorphan slowly discharge, keep drug effect reposefully, and don't influence loratadine or Desloratadine rapid release; Pharmaceutical composition of the present invention can be distributed to dextromethorphan in the slow-release material, obtains slow-released part, and loratadine or Desloratadine are distributed in the rapid release material; Obtain immediate release section; Adopt the conventional method of suitable formulation preparation to process slow releasing preparation then, like tablet, capsule etc., following like concrete method for preparing:
Method 1
A. dextromethorphan is distributed in the slow-release material, obtains slow-released part;
B. loratadine or Desloratadine are distributed in the rapid release material, obtain immediate release section;
C. the slow-released part of step a and the immediate release section of step b are pressed into bilayer or multilamellar slow releasing tablet;
Or the slow-released part of step a and the immediate release section of step b be mixed and made into sustained-release granular formulation;
Or the immediate release section of the slow-released part of step a and step b incapsulated process slow releasing capsule.
A. dextromethorphan is distributed in the slow-release material, obtains the slow release core, like granule, micropill, ball core or label etc.;
B. loratadine or Desloratadine are distributed in the rapid release material, obtain the rapid release coating;
C. the rapid release coating of step b is coated on the slow release core surfaces of step a, processed slow releasing preparation, like sustained-release granular formulation, slow releasing capsule, slow releasing pill or slow releasing tablet etc.
The slow releasing preparation of method for preparing had both kept loratadine or quick-acting, the long lasting antihistamine effects of Desloratadine; Overcome the problem of dextromethorphan rapid release, of short duration antitussive simultaneously, can further strengthen the effects of two kinds of medicine Synergistic treatment coughs in this compound recipe.
Above-mentioned method for preparing is equally applicable to prepare similar slow releasing preparation, the slow-released part that it is characterized in that containing the loratadine or the Desloratadine immediate release section of effective dose and contain the maincenter cough medicine of effective dose, and pharmaceutical carrier.And expection can reach similar therapeutic effect.
Slow releasing preparation of the present invention is used to treat the caused dry cough of a variety of causes, and anaphylaxis or respiratory tract infectious cough and smoker's cough is particularly useful for the frequent patient that coughs.Day obeys once.
Figure of description
Fig. 1 dextromethorphan hydrobromide release profiles relatively
Fig. 2 codeine phosphate release profiles relatively
Fig. 3 dextromethorphan slow-release suspension release profiles relatively
The specific embodiment
Following embodiment is used for further setting forth the present invention, but the present invention is not constituted restriction.
In the specific implementation, according to the difference of method for preparing, in the component in the above various uses adjuvant of optional usefulness partly or entirely.
Embodiment 1
Method for preparing
1. dextromethorphan hydrobromide, microcrystalline Cellulose, stearic acid and ethyl cellulose being crossed that 80 mesh sieves are pulverized and mix homogeneously, is that binding agent prepares soft material with 75% ethanol liquid of polyvidone, and 20 orders are granulated; 60 ℃ of dryings; 40 order granulate add the magnesium stearate mixing, and are subsequent use;
2. loratadine, lactose, starch and carboxymethyl starch sodium are crossed 80 mesh sieves and pulverize and mix homogeneously, prepare soft material with water-wet, 20 orders are granulated, 60 ℃ of dryings, and 40 order granulate add magnesium stearate and micropowder silica gel mixing, and are subsequent use;
3. the slow-releasing granules of step 1 and the immediate-release granules of step 2 are pressed into double-layer tablet.
Method for preparing
1. dextromethorphan hydrobromide, sucrose, stearyl alcohol, sodium alginate and Pulvis Talci are crossed pulverizing of 80 mesh sieves and mix homogeneously, place fluid bed, adopting side spray mode is that binding agent carries out the pill operation with the starch slurry, gets slow-release micro-pill, subsequent use;
2. Desloratadine, sucrose, low-substituted hydroxypropyl cellulose, polyvinylpolypyrrolidone and Pulvis Talci are crossed pulverizing of 80 mesh sieves and mix homogeneously, place fluid bed, adopting side spray mode is that binding agent carries out the pill operation with water, gets fast release micropill, subsequent use;
3. the fast release micropill of the slow-release micro-pill of step 1 and step 2 is packed into simultaneously and process slow releasing capsule in the Capsules.
Embodiment 3
Method for preparing
1. dextromethorphan hydrobromide, calcium hydrogen phosphate and hypromellose being crossed that 80 mesh sieves are pulverized and mix homogeneously, is that binding agent prepares soft material with 50% ethanol liquid of sodium carboxymethyl cellulose, and 20 orders are granulated; 60 ℃ of dryings, 40 order granulate add Semen Tritici aestivi starch mixing; Be pressed into the slow release label, subsequent use;
2. the slow release label with step 1 places coating pan, and the zein ethanol liquid with 10% carries out isolation coat;
3. loratadine, dimethicone, Polyethylene Glycol and acrylic resin are dissolved in an amount of 40% ethanol liquid, add Pulvis Talci and keep stirring the uniform suspension of formation, carry out the rapid release coating with this slow release label to step 2;
4. an amount of acrylic resin, Polyethylene Glycol and tween are dissolved in an amount of 85% ethanol liquid, add Pulvis Talci and lemon yellow and keep stirring the uniform suspension of formation, carry out film coating, get the film coating slow releasing tablet with this slow release label to step 3.
Method for preparing
1. 80 mesh sieves being crossed in codeine phosphate, mannitol, sucrose, hypromellose, ethyl cellulose and micropowder silica gel pulverizes and mix homogeneously; Place fluid bed; Adopting side spray mode is that binding agent carries out the pill operation with the methylated cellulose aqueous solution, gets slow-release micro-pill, subsequent use;
2. adopt side spray mode the slow-release micro-pill of step 1 to be carried out isolation coat with 10% zein ethanol liquid;
3. loratadine, polyvidone, Polyethylene Glycol and acetyl monoglyceride are dissolved in an amount of 70% ethanol liquid, add Pulvis Talci and keep stirring the uniform suspension of formation, carry out the rapid release coating with this slow-release micro-pill to step 2;
4. prepare 6% hypromellose ethanol liquid with 50% ethanol liquid, tween and propylene glycol are dissolved in wherein, add Pulvis Talci and carmine and keep stirring the uniform suspension of formation, carry out film coating with this slow-release micro-pill to step 3.
5. the slow-release micro-pill of step 4 is packed into and process slow releasing capsule in the Capsules.
Embodiment 5
Method for preparing
1. codeine phosphate, starch and hypromellose being crossed 80 mesh sieves and pulverize and mix homogeneously, is that binding agent prepares soft material with 75% ethanol, and 20 orders are granulated, 60 ℃ of dryings, and 40 order granulate add the Pulvis Talci mixing, and are subsequent use;
2. Desloratadine, mannitol and cross-linking sodium carboxymethyl cellulose being crossed that 80 mesh sieves are pulverized and mix homogeneously, is that binding agent prepares soft material with 50% ethanol liquid of low-substituted hydroxypropyl cellulose, and 20 orders are granulated; 60 ℃ of dryings; 40 order granulate add the magnesium stearate mixing, and are subsequent use;
3. the slow-releasing granules of step 1 and the immediate-release granules of step 2 are pressed into double-layer tablet.
The loratadine dissolution determination
Measure the dissolution of loratadine component among the embodiment 1,3 and 4 with reference to loratadine tablet quality standard (WS-120 (X-105)-97), and with the parallel comparison of listing product clarityne (loratadine tablet, Shanghai Schering Plough pharmaceutical Co. Ltd).Leaching condition: " Chinese pharmacopoeia version in 2005 two appendix XC dissolution determination second method (oar method), 900ml is a dissolution medium with hydrochloric acid solution (0.1mol/L), and temperature is set at 37.5 ℃ ± 0.5 ℃, and rotating speed is that per minute 50 changes sampling and measuring in the time of 30 minutes.The result sees table 1:
Table 1 loratadine dissolution relatively
The Desloratadine dissolution determination
Measure the dissolution of Desloratadine component among the embodiment 2 and 5 with reference to Desloratadine tablet quality standard (WS-097 (X-084)-2002), and believe the parallel comparison in quick spit of fland (Desloratadine sheet, Salubris Parmaceuticals) with the product that goes on the market.Leaching condition: " Chinese pharmacopoeia version in 2005 two appendix XC dissolution determination three therapeutic methods of traditional Chinese medicine (little agar diffusion method); 250ml is a dissolution medium with hydrochloric acid solution (0.1mol/L); Temperature is set at 37.5 ℃ ± 0.5 ℃, and rotating speed is that per minute 50 changes sampling and measuring in the time of 30 minutes.The result sees table 2:
Table 2 Desloratadine dissolution relatively
Shown in table 1 and table 2, clarityne or believe that loratadine or Desloratadine dissolution among quick spit of fland and each embodiment have all reached required standard (>=80%).That is to say, among each embodiment more than at least 80% loratadine or Desloratadine pro-from immediate release section, be dissolved out apace in 30 minutes, its external stripping demonstrates and the similar basically characteristic of listing product.
Embodiment 7 dextromethorphan hydrobromides and codeine phosphate drug release determination
The dextromethorphan hydrobromide drug release determination
Measure the release degree of dextromethorphan hydrobromide component among the embodiment 1,2 and 3 with reference to dextromethorphan hydrobromide sustained-release tablets quality standard (WS-500 (X-430)-95); And with listing product times Ke Er (dextromethorphan hydrobromide sustained-release tablets, Hangzhou Minsheng Pharmaceutical Group Co) parallel comparison.Release conditions: " two appendix XD of Chinese pharmacopoeia version in 2005 drug release determination, first method (adopting dissolution determination second subtraction unit); With water 900ml is dissolution medium; Temperature is set at 37.5 ℃ ± 0.5 ℃; Rotating speed was that per minute 50 changes, in the 1st, 2,4,8,10 and 12 hour sampling and measuring.The result sees table 3 and Fig. 1:
Table 3 dextromethorphan hydrobromide release degree relatively
The codeine phosphate drug release determination
Measure the release degree of codeine phosphate component among the embodiment 4 and 5 with reference to codeine phosphate slow releasing tablet quality standard (WS-375 (X-321)-97), and with the parallel comparison of product Ni Kekang (codeine phosphate slow releasing tablet, Xinan Pharmaceutical Co., Ltd.) of going on the market.Release conditions: " two appendix XD of Chinese pharmacopoeia version in 2005 drug release determination, first method (adopting dissolution determination second subtraction unit); With water 900ml is dissolution medium; Temperature is set at 37.5 ℃ ± 0.5 ℃; Rotating speed was that per minute 75 changes, in the 1st, 2,4,8,10 and 12 hour sampling and measuring.The result sees table 4 and Fig. 2:
Table 4 codeine phosphate release degree relatively
Shown in table 3 and table 4, dextromethorphan hydrobromide or codeine phosphate release degree among times Ke Er or Ni Kekang and each embodiment have all reached required standard (8 hours more than 70% for 2 hours 30-60%, 4 hours 45-80%).As depicted in figs. 1 and 2, each embodiment and listing product release in vitro curve basically identical, wherein embodiment 2 is the most approximate with Bei Keer, embodiment 4 and Ni Kekang.Can know that from The above results the dextromethorphan hydrobromide of all dosage or codeine phosphate will could slowly discharge fully through 12 hours corrosion, dissolving and flooding mechanism effect at least in the slow-released part.
The Hou Huimin of Shanghai Institute of Pharmaceutical Industry has mentioned dextromethorphan slow-release suspension drug release determination method in " contain the medicated resin microencapsulation and prepare the oral sustained release suspension " literary composition; Measure the release degree (in dextromethorphan) of dextromethorphan hydrobromide component among the embodiment 1-3 with reference to this method at this; And with the listing little eyebrow of product (dextromethorphan slow-release suspension, Shanghai Hyundai Pharmacy stock Co., Ltd) parallel comparison.Release conditions changes dissolution medium into Klorvess Liquid (0.4mol/L) 500ml with reference to embodiment 7, and rotating speed becomes per minute 100 and changes.The result sees table 5 and Fig. 3:
Table 5 dextromethorphan hydrobromide release degree relatively
With shown in Figure 3, although the dextromethorphan release characteristics of little eyebrow and each embodiment all meets the requirement of slow releasing preparation, because the difference of release principle, there is notable difference in release profiles like table 5.The dextromethorphan slow-release suspension relies on ion exchange slowly to discharge medicine, does not have corrosion and course of dissolution, and therefore, discharge very fast relatively early stage, and the later stage is steady; Each embodiment rate of release of matrix type then receives skeleton by the speed of corrosion progressively and the multiple factor affecting such as dissolution velocity of medicine, not limited by exchange capacity and amount of ions, so initial stage release is relatively slow, discharges Du Lvegao at last.In addition, take pastille resin slow-release suspension for a long time and can cause the digestive system ionic environment disorderly, restricted such dosage form and used, and there is not such problem in skeleton type sustained release preparation, for extensively promoting the advantage that won.
Above-mentioned each embodiment shows that the external stripping of pharmaceutical composition of the present invention discharges the characteristic that possesses loratadine quick releasing formulation and dextromethorphan slow releasing preparation simultaneously, therefore; Can keep quick-acting, the long lasting antihistamine effects of loratadine, can overcome the problem of dextromethorphan rapid release, of short duration antitussive again, make dextromethorphan slowly discharge; Keep drug effect reposefully,, further strengthened the effect of two kinds of medicine Synergistic treatment coughs in this compound recipe to reach the purpose of long-acting antitussive; In the hope of obtaining to reduce the dose number of times; Reduce toxic and side effects, shorten the course of treatment, improve the effect of compliance.And above-mentioned method for preparing is equally applicable to contain the similar said loratadine of Desloratadine or codeine and the slow releasing preparation of dextromethorphan compound recipe, and expection can reach similar therapeutic effect.
Though described some preferred embodiments of the present invention, this does not also mean that restriction the present invention, does various variations and modification therein apparently and do not depart from spirit of the present invention to belong to scope of the present invention yet.Scope of the present invention only receives the restriction of incidental claims.
Method for preparing: the method by embodiment 1 prepares, and obtains sustained-release double-layer tablet.
Claims (17)
1. an Orally administered medicinal composition is characterized in that, said pharmaceutical composition comprises: contain loratadine or the Desloratadine or their officinal salt of effective dose immediate release section, contain the slow-released part and the pharmaceutic adjuvant of the maincenter cough medicine of effective dose; Wherein, Said maincenter cough medicine is selected from dextromethorphan, codeine or their officinal salt; Said slow-released part comprises the slow-release material that is selected from stearyl alcohol, stearic acid, hypromellose, sodium alginate, ethyl cellulose and acrylic resin, and it is 5-85% that said slow-release material accounts for the slow-released part percentage by weight.
2. Orally administered medicinal composition as claimed in claim 1, wherein said maincenter cough medicine is a dextromethorphan hydrobromide.
3. Orally administered medicinal composition as claimed in claim 1, the content of wherein said loratadine or Desloratadine are 1-50mg, and the content of said dextromethorphan is 1-200mg.
4. Orally administered medicinal composition as claimed in claim 3, the content of wherein said loratadine or Desloratadine are 5-20mg, and the content of said dextromethorphan is 5-100mg.
5. it is 15-75% that Orally administered medicinal composition as claimed in claim 1, wherein said slow-release material account for the slow-released part percentage by weight.
6. Orally administered medicinal composition as claimed in claim 1, wherein said pharmaceutical composition are tablet, pill, granule or capsule.
7. Orally administered medicinal composition as claimed in claim 6, wherein said tablet are double-layer tablet or multilayer tablet.
8. Orally administered medicinal composition as claimed in claim 7, wherein said double-layer tablet are levels.
9. Orally administered medicinal composition as claimed in claim 7, wherein said double-layer tablet are ectonexine.
10. Orally administered medicinal composition as claimed in claim 9, the internal layer of wherein said double-layer tablet are slow-released part, and skin is an immediate release section.
11. Orally administered medicinal composition as claimed in claim 10 has the coating sealing coat in the middle of the ectonexine of wherein said double-layer tablet.
12. Orally administered medicinal composition as claimed in claim 6, wherein said pharmaceutical composition are capsule.
13. Orally administered medicinal composition as claimed in claim 1, wherein said pharmaceutic adjuvant comprise any one or a few the mixture in filler, binding agent, disintegrating agent and the lubricant.
14. Orally administered medicinal composition as claimed in claim 13, wherein said filler are selected from any one or a few the mixture in mannitol, microcrystalline Cellulose, starch, pregelatinized Starch, calcium hydrogen phosphate, sucrose, lactose, red bright alcohol, sorbitol and the xylitol.
15. the described Orally administered medicinal composition of claim 13, wherein said binding agent are selected from any one or a few the mixture in starch, hydroxypropyl methylcellulose, polyvidone, gelatin and the Polyethylene Glycol.
16. the described Orally administered medicinal composition of claim 13, wherein said disintegrating agent is selected from one or more in starch, carboxymethyl starch sodium, low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose and the polyvinylpolypyrrolidone.
17. the described Orally administered medicinal composition of claim 13, wherein said lubricant are selected from any one or a few the mixture in micropowder silica gel, Pulvis Talci, magnesium stearate, Stepanol MG, hydrogenated vegetable oil, the hydrated silica gel sodium.
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| CN 200710078245 CN101015519B (en) | 2007-02-27 | 2007-02-27 | Loratadine oral compound medication composition |
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| CN 200710078245 CN101015519B (en) | 2007-02-27 | 2007-02-27 | Loratadine oral compound medication composition |
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| EP2486918A4 (en) | 2009-10-09 | 2014-02-26 | Yungjin Pharmaceutical Co Ltd | Pharmaceutical composition with both immediate and extended release characteristics |
| CN102727558A (en) * | 2012-07-04 | 2012-10-17 | 重庆市中药研究院 | Tripterygium Hypoglaucum Hutch root extract, and bi-layer extended release tablet and application thereof |
| CN103948562B (en) * | 2014-03-20 | 2017-10-17 | 广东九明制药有限公司 | A kind of Desloratadine capsule and preparation method thereof |
| CN108524460B (en) * | 2018-05-14 | 2021-01-01 | 佛山市南海东方澳龙制药有限公司 | Nitenpyram double-layer tablet |
| CN114340608B (en) * | 2020-07-20 | 2023-10-31 | 深圳信立泰药业股份有限公司 | Pharmaceutical composition and application thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5314697A (en) * | 1992-10-23 | 1994-05-24 | Schering Corporation | Stable extended release oral dosage composition comprising loratadine and pseudoephedrine |
| CN1535686A (en) * | 2003-04-09 | 2004-10-13 | 北京德众万全药物技术开发有限公司 | Slowly-released preparation containing loratadine and pseudoephedrine sulfate and its preparation method |
| CN1823770A (en) * | 2006-03-27 | 2006-08-30 | 重庆医药工业研究院有限责任公司 | Compound Dextromethorphan oral cavity disintegration tablet |
-
2007
- 2007-02-27 CN CN 200710078245 patent/CN101015519B/en not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5314697A (en) * | 1992-10-23 | 1994-05-24 | Schering Corporation | Stable extended release oral dosage composition comprising loratadine and pseudoephedrine |
| CN1089471A (en) * | 1992-10-23 | 1994-07-20 | 先灵公司 | Stable prolongation release oral dosage composition |
| CN1535686A (en) * | 2003-04-09 | 2004-10-13 | 北京德众万全药物技术开发有限公司 | Slowly-released preparation containing loratadine and pseudoephedrine sulfate and its preparation method |
| CN1823770A (en) * | 2006-03-27 | 2006-08-30 | 重庆医药工业研究院有限责任公司 | Compound Dextromethorphan oral cavity disintegration tablet |
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| CN101015519A (en) | 2007-08-15 |
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