CN1311825C - Pioglitazone soft capsule and its preparing method - Google Patents
Pioglitazone soft capsule and its preparing method Download PDFInfo
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- CN1311825C CN1311825C CNB2005100803627A CN200510080362A CN1311825C CN 1311825 C CN1311825 C CN 1311825C CN B2005100803627 A CNB2005100803627 A CN B2005100803627A CN 200510080362 A CN200510080362 A CN 200510080362A CN 1311825 C CN1311825 C CN 1311825C
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- soft capsule
- pioglitazone
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Abstract
The present invention relates to a pioglitazone soft capsule and a preparation method thereof. The content of the soft capsule is prepared into a solution or a mixed suspension by mixing and dissolving the pioglitazone and one and/or several kinds of a dissolving agent, a latent solvent, a suspending agent, a solubilizing agent and a surface active agent, and the soft capsule is prepared.
Description
Technical field
The present invention relates to pioglitazone soft capsule and preparation method thereof,, make the soft capsule that content is solution-type or suspension type by selection to its composition.
Background technology
Pioglitazone is a kind of thiazolidinediones euglycemic agent that is used for the treatment of type 2 diabetes mellitus.Mechanism of action is relevant with the existence of insulin, can reduce the insulin resistant of peripheral tissues and liver, increases the processing of the glucose that relies on insulin, and reduces the output of glycogen.It is by peroxide activator enzyme paraphyte activated receptor Y (PPAI-x), regulate transcribing of the multiple protein relevant with lipid metabolism with sugar, thereby amplified the Role in Plant Signal Transduction behind the Insulin receptor INSR in liver and the peripheral tissues, improved Blood glucose control, and do not stimulate secretion of insulin.Present good hypoglycemic activity, equally also can reduce the level of insulin, but do not destroy the negative feedback balance between blood glucose-insulin, be difficult for producing the hypoglycemia phenomenon.
At present existing pioglitazone peroral dosage form is tablet, capsule, and the disintegrate of solid orally ingestibles such as tablet, capsule is slow, absorption difference in the body, bioavailability are low.Soft capsule dosage form has been accelerated the process of disintegrate in the body, decomposition, stripping with respect to tablet, hard capsule, makes the easier absorption of active ingredient.
Summary of the invention
The present invention is intended to overcome problems such as the poor stability, the bioavailability that have the pioglitazone solid orally ingestible are low, has changed the dissolution and the low shortcoming of bioavailability of pioglitazone oral formulations, has improved curative effect.
Pioglitazone soft capsule of the present invention can prepare by the various appropriate method of soft capsule preparation, the preparation method of preferred pioglitazone soft capsule is as follows: one in pioglitazone and lytic agent, cosolvent, suspending agent, solubilizing agent, the surfactant and/or a plurality of mixed dissolution are made solution-type or suspension type content, adopt pressed film method to prepare soft capsule, soft capsule is through solidifying by cooling in wind, drying, wash ball, do eventually with appropriate solvent, promptly get product.
Pioglitazone soft capsule content described in the preparation method of the present invention composed as follows: form by pioglitazone and adjuvant.Wherein said adjuvant comprises in lytic agent, cosolvent, suspending agent, solubilizing agent, the surfactant one and/or a plurality of.Wherein lytic agent is Polyethylene Glycol, fish oil, soybean oil, refining Oleum Arachidis hypogaeae semen, Radix Oenotherae erythrosepalae oil, Herba Silybi mariani oil, Oleum Vitis viniferae, Oleum Helianthi, safflower oil, the Fructus Hippophae wet goods vegetable and animals oils of PEG400 or PEG600 liquid state, preferred PEG400 or soybean oil, the addition 10%-90% of lytic agent, preferably: 20-80%, more preferably: 30-70%; Cosolvent is mixture, pluronic F-68, zein, hydrogenated palm oil, soybean lecithin, lecithin, polyglycerol ester, sucrose fat of lower alcohols such as propylene glycol, glycerol, isopropyl alcohol and/or several alcohol etc., preferred propylene glycol or hydrogenated palm oil, the addition of cosolvent is 1%-50%, preferably: 5-45%, more preferably: 10-40%; Solubilizing agent is ethanol or hydroxypropyl, preferred hydroxypropyl, and the solubilizing agent addition is 0.1%-20%, and is preferred: 0.5%-15%, more preferably: 1%-10%; Suspending agent is the solid-state Polyethylene Glycol of PEG4000, PEG6000, liquid paraffin, lanoline, Cera Flava, glyceryl monostearate, high fatty alcohol, preferred PEG6000 or Cera Flava, addition is 1%～10%, and is preferred: 1.5%-8%, more preferably: 2%-6%; Surfactant is sorbester p17, sorbester p18, Tween 80, polysorbate60, sodium lauryl sulphate, neutral liquid fat, preferred neutral liquid fat, and the addition of surfactant is 1%～30% preferred: 3%-25%, more preferably: 5-20%; Wherein the content of pioglitazone is 1%～20%, and is preferred: 2-15%, more preferably: 3-10%; Each component sum of content is 100%.It is primary raw material that softgel shell adopts gelatin, glycerol and/or sorbitol etc., can add 0.2～0.8% titanium dioxide and make as opacifier.
The specific embodiment:
Pioglitazone soft capsule of the present invention can prepare by the various appropriate method of soft capsule preparation, preferably make: get pioglitazone by being prepared as follows method, lytic agent (the Polyethylene Glycol of PEG400 or PEG600 liquid state, fish oil, soybean oil, refining Oleum Arachidis hypogaeae semen, Radix Oenotherae erythrosepalae oil, Herba Silybi mariani oil, Oleum Vitis viniferae, Oleum Helianthi, safflower oil, Fructus Hippophae wet goods vegetable and animals oils, preferred PEG400 or soybean oil), cosolvent (propylene glycol, glycerol, the mixture of lower alcohols such as isopropyl alcohol and/or several alcohol, pluronic F-68, zein, hydrogenated palm oil, soybean lecithin, lecithin, polyglycerol ester, sucrose fat etc., preferred propylene glycol or hydrogenated palm oil), solubilizing agent (ethanol or hydroxypropyl, preferred hydroxypropyl), suspending agent (PEG4000, the Polyethylene Glycol that PEG6000 is solid-state, liquid paraffin, lanoline, Cera Flava, glyceryl monostearate, high fatty alcohol, preferred PEG6000 or Cera Flava), surfactant (sorbester p17, sorbester p18, Tween 80, polysorbate60, sodium lauryl sulphate, neutral liquid fat, preferred neutral liquid fat) in one and/or a plurality of mixed dissolution make solution-type or suspension type content; Get gelatin, purified water, the abundant mixing of glycerol and get glue, it is standby to regulate the adhesive tape that is compressed to 0.5-2.0mm thickness by press; Adopt pressed film method to prepare soft capsule,, wash ball, do eventually, promptly with appropriate solvent through solidifying by cooling in wind, drying.Enumerate several embodiment that are used to that the invention process process is described rather than are used for limiting protection domain, as follows:
Embodiment 1)
| Soybean oil | ?390g |
| Pioglitazone zein Tween 80 | ?10g ?35g ?15g |
Granulate 1000
Softgel shell glue prescription:
Gelatin: glycerol: water=1: 0.6: 0.7
The soft capsule that adopts above prescription to adopt preparation method to make, 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 | ?98.3 |
| High temperature 10 days | Oval soft capsule | ?12 | ?99.1 |
| High humidity 10 days | Oval soft capsule | ?13 | ?99.2 |
| High light 10 days | Oval soft capsule | ?15 | ?98.9 |
Conclusion: through high temperature, high humidity, high light condition effect factor are investigated, and this product visual examination no change, disintegration time and content are all stable.
Embodiment 2)
| ?PEG400 | ?342g |
| Pioglitazone isopropyl alcohol ethanol | ?12g ?31g ?15g |
Granulate 1000
Softgel shell glue prescription:
Gelatin: sorbitol: water :=1: 0.6: 0.7
The soft capsule that adopts above prescription to adopt preparation method to make, 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 | ?98.9 |
| High temperature 10 days | Oval soft capsule | ?13 | ?99.1 |
| High humidity 10 days | Oval soft capsule | ?14 | ?98.7 |
| High light 10 days | Oval soft capsule | ?15 | ?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.
Embodiment 3)
| ?PEG600 | ?327g |
| Pioglitazone propylene glycol hydroxypropyl | ?15g ?30g ?28g |
Granulate 1000
Softgel shell glue prescription:
Gelatin: sorbitol: water=1: 0.5: 0.8
The soft capsule that adopts above prescription to adopt preparation method to make, 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 |
| High temperature 10 days | Oval soft capsule | ?15 | ?98.9 |
| High humidity 10 days | Oval soft capsule | ?13 | ?98.7 |
| High light 10 days | Oval soft capsule | ?14 | ?98.8 |
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.
Embodiment 4)
| Refining Oleum Arachidis hypogaeae semen | ?380g |
| The neutral liquid fat of pioglitazone hydrogenated palm oil liquid paraffin | ?25g ?26g ?19g ?30g |
Granulate 1000
Softgel shell glue prescription:
Gelatin: glycerol: water=1: 0.4: 0.9
The soft capsule that adopts above prescription to adopt preparation method to make, 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 |
| High temperature 10 days | Oval soft capsule | ?13 | ?98.7 |
| High humidity 10 days | Oval soft capsule | ?14 | ?98.8 |
| High light 10 days | 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.
Embodiment 5)
| Herba Silybi mariani oil | ?385g |
| The neutral liquid fat of pioglitazone hydrogenated palm oil | ?12g ?37g ?16g |
Granulate 1000
Softgel shell glue prescription:
Gelatin: sorbitol: water :=1: 0.6: 0.7
The soft capsule that adopts above prescription to adopt preparation method to make, 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 | ?98.9 |
| High temperature 10 days | Oval soft capsule | ?14 | ?99.2 |
| High humidity 10 days | Oval soft capsule | ?13 | ?99.0 |
| High light 10 days | Oval soft capsule | ?15 | ?98.6 |
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.
3, the stripping characteristics according to the pioglitazone soft capsule of this prepared are as follows:
Compare with existing preparation pioglitazone sheet, capsule dissolution:
| Sample time (min) | ?5 | ?10 | ?20 | ?30 | ?45 | ?60 |
| The pioglitazone sheet | ?23.1 | ?59.6 | ?88.3 | ?90.2 | ?96.9 | ?98.9 |
| The pioglitazone capsule | ?39.3 | ?66.8 | ?90.5 | ?91.9 | ?97.3 | ?99.1 |
| Pioglitazone soft capsule | ?45.8 | ?74.9 | ?92.6 | ?96.57 | ?99.7 | ?99.8 |
Conclusion: the dissolution of pioglitazone soft capsule agent is better than sheet, capsule, the dissolution rate height.
Claims (2)
1. pioglitazone soft capsule, it is characterized in that content makes solution-type or suspension type content by 3-10% pioglitazone and other adjuvant mixed dissolutions, the preparation soft capsule, the solution-type content comprises pioglitazone and lytic agent, cosolvent, solubilizing agent, suspension type content comprises pioglitazone and lytic agent, cosolvent, suspending agent, surfactant, wherein adjuvant comprises: the lytic agent of 10-90%, lytic agent are selected from the Polyethylene Glycol of PEG400 or PEG600 liquid state, fish oil, soybean oil, refining Oleum Arachidis hypogaeae semen, Radix Oenotherae erythrosepalae oil, Herba Silybi mariani oil, Oleum Vitis viniferae, Oleum Helianthi, safflower oil, Oleum Hippophae; The cosolvent of 10-40%, cosolvent are selected from propylene glycol, glycerol, isopropyl alcohol, pluronic F-68, zein, hydrogenated palm oil, soybean lecithin, lecithin, polyglycerol ester, sucrose fat; The suspending agent of 1%-10%, suspending agent are selected from the solid-state Polyethylene Glycol of PEG4000, PEG6000, liquid paraffin, lanoline, Cera Flava, glyceryl monostearate; The solubilizing agent of 1%-10%, solubilizing agent are selected from ethanol, hydroxypropyl; 5-20% surfactant, surfactant are selected from sorbester p17, sorbester p18, Tween 80, polysorbate60, sodium lauryl sulphate, neutral liquid fat.
2. the described preparation of soft capsule method of claim 1 is characterized in that the described pioglitazone of claim 1 and other adjuvant mixed dissolutions are made solution-type or suspension type content, the preparation soft capsule.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100803627A CN1311825C (en) | 2005-07-04 | 2005-07-04 | Pioglitazone soft capsule and its preparing method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100803627A CN1311825C (en) | 2005-07-04 | 2005-07-04 | Pioglitazone soft capsule and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1709249A CN1709249A (en) | 2005-12-21 |
| CN1311825C true CN1311825C (en) | 2007-04-25 |
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| CNB2005100803627A Expired - Fee Related CN1311825C (en) | 2005-07-04 | 2005-07-04 | Pioglitazone soft capsule and its preparing method |
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Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102657626B (en) * | 2012-05-23 | 2013-07-17 | 重庆康刻尔制药有限公司 | Medicinal composite tablet of pioglitazone medicine |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1552318A (en) * | 2003-12-18 | 2004-12-08 | 华东中药工程集团有限公司 | Hawthorn leave flavone capsules and their preparing method |
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Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1552318A (en) * | 2003-12-18 | 2004-12-08 | 华东中药工程集团有限公司 | Hawthorn leave flavone capsules and their preparing method |
Non-Patent Citations (2)
| Title |
|---|
| 实用药物制剂技术 庄越等，264.265，人民卫生出版社 1999 * |
| 软胶囊的工艺研究现状 齐惠敏等，天津药学，第9卷第4期 1997 * |
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| CN1709249A (en) | 2005-12-21 |
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Granted publication date: 20070425 |