CN1768743A - Telmisartan soft capsule and preparation method thereof - Google Patents
Telmisartan soft capsule and preparation method thereof Download PDFInfo
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- CN1768743A CN1768743A CN 200510117562 CN200510117562A CN1768743A CN 1768743 A CN1768743 A CN 1768743A CN 200510117562 CN200510117562 CN 200510117562 CN 200510117562 A CN200510117562 A CN 200510117562A CN 1768743 A CN1768743 A CN 1768743A
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- soft capsule
- telmisartan
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Abstract
The invention relates to a Telmisartan soft capsule and method of preparation, wherein the soft capsule comprises Telmisartan and contents of the mixture of diluent, auxiliary solvent, solubilizing agent, suspension auxiliary agent and surface active agent.
Description
Technical field
The present invention relates to telmisartan soft capsule and preparation method thereof.
Background technology
Telmisartan is that a benzimidazole is long-acting, efficient, the angiotensin-ii receptor inhibitor of low toxicity, belong to non-peptide class, be the novel depressor of a class, but the nervous plain AT1 receptor of highly selective vasoactive, to the action intensity of AT1 receptor than strong about 20000 times of AT2,, medicine is fat-soluble higher simultaneously, thereby has stronger tissue penetration and effect specificity.It optionally blocks the affinity interaction of the interior synthetic Angiotensin II of body to AT1, antagonism activates arteries contraction, sympathetic activation and the physiological effecies such as the increase of pressure receptor sensitivity, increased blood pressure that the back is produced by AT1, bring high blood pressure down, weaken myocardial cell and shrink, and retardance AT1 acts on the water retention that produces behind the kidney.Telmisartan also can reverse cardiac muscle and proliferation of smooth muscle of arterial blood tube wall and the plumpness by the AT1 mediation, delays the process of myocardial hypertrophy and kidney interstitial fibrosis.Reduce the sickness rate and the case fatality rate of heart failure.To blood glucose, a few nothing influences of blood fat.Efficacy of antihypertensive treatment is reliable, better tolerance.Carrying out at present the III phase clinical research that relevant this product is used for the diabetic nephropathy treatment.The present commercially available telmisartan sheet that has.
Summary of the invention
The present invention is intended to improve telmisartan solid orally ingestible stripping quantity, improves curative effect of medication, reduces dust from flying simultaneously with the healthy and environment of protection operator, has proposed telmisartan soft capsule.
Another object of the present invention provides the preparation method of telmisartan soft capsule.
Telmisartan soft capsule of the present invention can prepare by the various appropriate method of soft capsule preparation, and its preferred for preparation method is as follows: with a plurality of mixed the content in telmisartan and diluent, cosolvent, solubilizing agent, suspending agent, the surfactant; Get gelatin, water, sorbitol and/or glycerol routinely the abundant mixing of ratio get glue, make the adhesive tape of suitable depth; Adopt die pressing to prepare soft capsule, soft capsule cleans soft capsule, drying through solidifying by cooling in wind, drying with appropriate solvent, promptly gets product.
Described telmisartan soft capsule, the medicine acceptable carrier that it is characterized in that containing telmisartan He be fit to make soft capsule.
Described telmisartan soft capsule is characterized in that its content a plurality of mixed by in telmisartan and diluent, cosolvent, solubilizing agent, suspending agent, the surfactant.
Described telmisartan soft capsule, wherein said diluent comprise Polyethylene Glycol, soybean oil, safflower oil, hydrogenated palm oil, olive oil, Oleum Vitis viniferae, Semen Maydis oil or the Oleum Cocois of PEG400 or PEG600 liquid state, preferred PEG400 or olive oil; The addition 10%--90% of diluent.
Described telmisartan soft capsule, wherein said cosolvent comprise the lower aliphatic alcohols of C3-C8 or its mixture, hydroxypropyl, preferred hydroxypropyl; The addition of cosolvent is 1%--20%.
Described telmisartan soft capsule, wherein said solubilizing agent comprise meglumine, triethanolamine, diethanolamine, monoethanolamine, ethylenediamine, diethylamine or its mixture, preferred triethanolamine; The addition of solubilizing agent is 1%--20%.
Described telmisartan soft capsule, wherein said suspending agent PEG4000 or PEG6000 solid polyethylene glycol, aerosil, liquid paraffin, sucrose ester, lanoline, lecithin, Cera Flava, glyceryl monostearate, C8-C22 high fatty alcohol or its mixture, preferred aerosil; The suspending agent addition is 1%--30%.
Described telmisartan soft capsule, wherein said surfactant comprise sorbester p17, sorbester p18, Tween 80, polysorbate60, sodium lauryl sulphate, neutral liquid ester, preferably sodium dodecyl sulfate; The addition of surfactant is 1%～20%.
Described telmisartan soft capsule, the content of wherein said telmisartan are 1%～50%.
The preparation method of described telmisartan soft capsule, with a plurality of mixed the content in telmisartan and diluent, cosolvent, solubilizing agent, suspending agent, the surfactant, with gelatin, water, sorbitol and/or glycerol is the capsule material, adopt die pressing to prepare soft capsule, soft capsule is through solidifying by cooling in wind, drying, wash, do eventually, promptly with appropriate solvent.
The specific embodiment:
Telmisartan soft capsule of the present invention can prepare by the various appropriate method of soft capsule preparation, preferably makes by being prepared as follows method:
The preparation of content: get telmisartan, diluent (the Polyethylene Glycol that comprises PEG400 or PEG600 liquid state, soybean oil, safflower oil, hydrogenated palm oil, olive oil, Oleum Vitis viniferae, Semen Maydis oil or Oleum Cocois), cosolvent (comprises hydroxypropyl, the lower aliphatic alcohols of C3-C8 or its mixture), solubilizing agent (comprises meglumine, triethanolamine, diethanolamine, monoethanolamine, ethylenediamine, diethylamine or its mixture), suspending agent (comprises PEG4000, the Polyethylene Glycol that PEG6000 is solid-state, aerosil, liquid paraffin, sucrose ester, lanoline, lecithin, Cera Flava, glyceryl monostearate, C8-C22 high fatty alcohol or its mixture), surfactant (comprises sorbester p17, sorbester p18, Tween 80, polysorbate60, sodium lauryl sulphate, neutral liquid ester) a plurality of mixed content that gets in, standby.
Soft capsule molding preparation: get the abundant mixing of gelatin, water, sorbitol and/or glycerol and get glue, it is standby to regulate the adhesive tape that is compressed to suitable depth by press; Adopt die pressing to prepare soft capsule,, clean soft capsule, drying with appropriate solvent, promptly through solidifying by cooling in wind, drying.
Beneficial effect of the present invention is embodied in following aspect:
1, dispersion of medicine, stripping is more complete, and dissolution rate is stable; In human body, absorb steadily, improved bioavailability, stable curative effect.
2, loading amount is accurately more easy to control, and active constituent content is even, and dosage is accurate, and blood drug level is more stable, stable curative effect, and side effect is less.
3, because the preparation characteristic (with soft capsule shell sealing, secluding air, shading packing content thing) of soft capsule determines it can effectively keep the stable of medicine, improved safety, the effectiveness of medicine.
4, reduce flying upward of dust in the production process, protected the healthy and environment of operator.
Enumerate several embodiment and be used to further specify the present invention, but the present invention does not mean and only is confined to following examples.
The soft capsule of following examples preparations, all be with gelatin, water, sorbitol and/or glycerol routinely ratio be the capsule material.
Appearance character, disintegration, the content of investigating soft capsule by influence factor's test respectively wait the feasibility that further specifies soft capsule preparation method of the present invention.
Embodiment 1)
PEG400 280g
Telmisartan 40g
Sodium lauryl sulphate 50g
Triethanolamine 30g
Granulate 1000
The soft capsule content that adopts above prescription to make adopts die pressing to prepare soft capsule, and through study of pharmacy influence factor test, it is as follows to investigate the result:
| The investigation factor | Appearance character | Disintegration (min) | Content (%) |
| 0 day | Oval soft capsule | 13 | 99.1 |
| |
Oval soft capsule | 15 | 98.8 |
| |
Oval soft capsule | 13 | 98.9 |
| |
Oval soft capsule | 14 | 99.0 |
Conclusion: investigate through high temperature, high humidity, high light condition effect factor, this product visual examination no change, disintegration time and content are all stable, show that this preparation method is feasible.
Embodiment 2)
PEG600 300g
Telmisartan 60g
Propylene glycol 30g
Hydroxypropyl 60g
Granulate 1000
The soft capsule content that adopts above prescription to make adopts die pressing to prepare soft capsule, and through study of pharmacy influence factor test, it is as follows to investigate the result:
| The investigation factor | Appearance character | Disintegration (min) | Content (%) |
| 0 day | Oval soft capsule | 14 | 99.2 |
| | Oval soft capsule | 15 | 98.8 |
| | Oval soft capsule | 15 | 98.9 |
| | Oval soft capsule | 13 | 98.7 |
Conclusion: investigate through high temperature, high humidity, high light condition effect factor, this product visual examination no change, disintegration time and content are all stable, show that this preparation method is feasible.
Embodiment 3)
Olive oil 310g
Telmisartan 50g
Lecithin 10g
Cera Flava 30g
Granulate 1000
Adopt above prescription to make soft capsule content, adopt die pressing to prepare soft capsule, through study of pharmacy influence factor test, it is as follows to investigate the result:
| The investigation factor | Appearance character | Disintegration (min) | Content (%) |
| 0 day | Oval soft capsule | 14 | 99.1 |
| | Oval soft capsule | 15 | 98.7 |
| | Oval soft capsule | 16 | 99.0 |
| | Oval soft capsule | 13 | 99.2 |
Conclusion: investigate through high temperature, high humidity, high light condition effect factor, this product visual examination no change, disintegration time and content are all stable, show that this preparation method is feasible.
Embodiment 4)
Semen Maydis oil 310g
Telmisartan 50g
Glyceryl monostearate 10g
Cera Flava 30g
Granulate 1000
Adopt above prescription to make soft capsule content, adopt die pressing to prepare soft capsule, through study of pharmacy influence factor test, it is as follows to investigate the result:
| The investigation factor | Appearance character | Disintegration (min) | Content (%) |
| 0 day | Oval soft capsule | 14 | 98.9 |
| | Oval soft capsule | 15 | 98.8 |
| | Oval soft capsule | 14 | 99.1 |
| | Oval soft capsule | 13 | 98.5 |
Conclusion: investigate through high temperature, high humidity, high light condition effect factor, this product visual examination no change, disintegration time and content are all stable, show that this preparation method is feasible.
Embodiment 5)
Soybean oil 315g
Telmisartan 50g
Lecithin 15g
Aerosil 20g
Granulate 1000
Adopt above prescription to make soft capsule content, adopt die pressing to prepare soft capsule, through study of pharmacy influence factor test, it is as follows to investigate the result:
| The investigation factor | Appearance character | Disintegration (min) | Content (%) |
| 0 day | Oval soft capsule | 15 | 99.0 |
| | Oval soft capsule | 16 | 98.9 |
| | Oval soft capsule | 14 | 98.9 |
| High light 10 days | Oval soft capsule | 15 | 98.3 |
Conclusion: investigate through high temperature, high humidity, high light condition effect factor, this product visual examination no change, disintegration time and content are all stable, show that this preparation method is feasible.
Embodiment 6)
Compare with external stripping characteristics according to embodiment of the invention method 5 batches of (numbering corresponding) telmisartan soft capsules of preparation and existing preparation telmisartan tablet, select 0.05kgL for use with reference to national standard with embodiment number
-1Hydrochloric acid solution (the 0.1molL of SDS
-1) as dissolution medium, dissolving-out method adopts the oar method to operate, and the results are shown in following table and accompanying drawing:
| Sample time (min) | 5 | 10 | 15 | 20 | 30 | 40 | 50 | 60 |
| The telmisartan sheet | 6.18 | 25.98 | 42.87 | 50.69 | 60.19 | 66.92 | 72.41 | 80.06 |
| Telmisartan soft capsule 1 | 0 | 26.98 | 56.75 | 69.21 | 79.88 | 87.02 | 89.87 | 92.98 |
| Telmisartan soft capsule 2 | 0 | 25.34 | 55.86 | 70.27 | 81.68 | 85.96 | 89.03 | 93.43 |
| Telmisartan soft capsule 3 | 0 | 23.12 | 51.37 | 66.98 | 76.03 | 84.47 | 85.91 | 90.87 |
| Telmisartan soft capsule 4 | 0 | 24.57 | 50.39 | 65.98 | 76.47 | 83.97 | 87.81 | 91.07 |
| Telmisartan soft capsule 5 | 0 | 23.52 | 53.05 | 66.49 | 79.62 | 84.51 | 86.78 | 91.29 |
Conclusion: the stripping situation of telmisartan soft capsule agent is better than tablet, and stripping is more complete, and dissolution rate is stable.
Claims (9)
1. telmisartan soft capsule, the medicine acceptable carrier that it is characterized in that containing telmisartan He be fit to make soft capsule.
2. the described telmisartan soft capsule of claim 1 is characterized in that its content a plurality of mixed by in telmisartan and diluent, cosolvent, solubilizing agent, suspending agent, the surfactant.
3. the described telmisartan soft capsule of claim 1-2, wherein said diluent comprises Polyethylene Glycol, soybean oil, safflower oil, hydrogenated palm oil, olive oil, Oleum Vitis viniferae, Semen Maydis oil or the Oleum Cocois of PEG400 or PEG600 liquid state; The addition 10%--90% of diluent.
4. the described telmisartan soft capsule of claim 1-2, wherein said cosolvent comprise the lower aliphatic alcohols of C3--C8 or its mixture, hydroxypropyl; The addition of cosolvent is 1%--20%.
5. the described telmisartan soft capsule of claim 1-2, wherein said solubilizing agent comprises meglumine, triethanolamine, diethanolamine, monoethanolamine, ethylenediamine, diethylamine or its mixture; The addition of solubilizing agent is 1%--20%.
6. the described telmisartan soft capsule of claim 1-2, wherein said suspending agent PEG4000 or PEG6000 solid polyethylene glycol, aerosil, liquid paraffin, sucrose ester, lanoline, lecithin, Cera Flava, glyceryl monostearate, C8-C22 high fatty alcohol or its mixture; The suspending agent addition is 1%--30%.
7. the described telmisartan soft capsule of claim 1-2, wherein said surfactant comprises sorbester p17, sorbester p18, Tween 80, polysorbate60, sodium lauryl sulphate, neutral liquid ester; The addition of surfactant is 1%～20%.
8. aforesaid right requires each described telmisartan soft capsule, and the content of wherein said telmisartan is 1%～50%.
9. the preparation method of each described telmisartan soft capsule of claim 1-8, it is characterized in that a plurality of mixed the content in telmisartan and diluent, cosolvent, solubilizing agent, suspending agent, the surfactant, with gelatin, water, sorbitol and/or glycerol is the capsule material, adopt die pressing to prepare soft capsule, soft capsule is through solidifying by cooling in wind, drying, wash, do eventually, promptly with appropriate solvent.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510117562 CN1768743A (en) | 2005-11-08 | 2005-11-08 | Telmisartan soft capsule and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510117562 CN1768743A (en) | 2005-11-08 | 2005-11-08 | Telmisartan soft capsule and preparation method thereof |
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| CN1768743A true CN1768743A (en) | 2006-05-10 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101897676A (en) * | 2010-07-27 | 2010-12-01 | 北京京丰制药有限公司 | Telmisartan tablet composition |
-
2005
- 2005-11-08 CN CN 200510117562 patent/CN1768743A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101897676A (en) * | 2010-07-27 | 2010-12-01 | 北京京丰制药有限公司 | Telmisartan tablet composition |
| CN101897676B (en) * | 2010-07-27 | 2011-12-14 | 北京京丰制药有限公司 | Telmisartan tablet composition |
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Open date: 20060510 |