CN104983717A - Sodium prasterone sulfate sustained-release capsule and preparation method thereof - Google Patents
Sodium prasterone sulfate sustained-release capsule and preparation method thereof Download PDFInfo
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- CN104983717A CN104983717A CN201510305048.8A CN201510305048A CN104983717A CN 104983717 A CN104983717 A CN 104983717A CN 201510305048 A CN201510305048 A CN 201510305048A CN 104983717 A CN104983717 A CN 104983717A
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Abstract
The invention provides a sodium prasterone sulfate sustained-release capsule and a preparation method thereof. The sodium prasterone sulfate sustained-release capsule comprises sodium prasterone sulfate and auxiliary materials acceptable on pharmacy. The sodium prasterone sulfate sustained-release capsule can achieve 12-hour sustained release, and is stable in quality, high in bioavailability and good in medication compliance.
Description
Technical field
The present invention relates to technical field of medicine, particularly, relate to sodium prasterone sulfate slow releasing capsule and preparation method thereof.
Background technology
Sodium prasterone sulfate dosage form of going on the market at present is injection and injection powder pin, and it makes cervix maturation before being mainly used in full-term pregnancy induced labor clinically.
CN1509719 discloses sodium prasterone sulfate and is used for the treatment of climacteric syndrome, especially the novelty teabag of senile, the atrophic vaginitis of women.CN102429912 discloses medical composition and its use prepared by a kind of micronization prasterone or sodium prasterone sulfate.
But the research at present about sodium prasterone sulfate preparation still needs deeply.
Summary of the invention
The present invention is intended to solve one of technical problem in correlation technique at least to a certain extent.For this reason, one object of the present invention is to propose a kind ofly can to realize long-time slow releasing function, improves Drug safety, reduces toxic and side effects, facilitates administration or the sodium prasterone sulfate slow releasing capsule improving curative effect and preparation method thereof.
The present invention proposes based on the following discovery of inventor: because the indication of this medicine is chronic disease, need Long-term taking medicine, and every day multiple dosing, trouble of not only taking medicine, and easily occur situation about missing, causes patient's poor compliance; And drug plasma concentration fluctuation is comparatively large, causes to lead and may occur " peak valley " phenomenon, during blood drug level height, larger toxic and side effects may be produced; May occur time low that drug level is below treatment concentration, affects the treatment.Given this, inventor proposes a kind of sodium prasterone sulfate slow releasing capsule, can realize 12 hours long-time slow releasing functions, improve Drug safety, reduce toxic and side effects, facilitate administration and improve curative effect.
In one aspect of the invention, the invention provides a kind of sodium prasterone sulfate slow releasing capsule.According to embodiments of the invention, this sodium prasterone sulfate slow releasing capsule comprises: sodium prasterone sulfate 100 weight portion; Celphere 137 weight portion; Plasticizer 0.3 ~ 5.1 weight portion; Slow-release material 2.4 ~ 88 weight portion; Antiplastering aid 0.1 ~ 12 weight portion; And binding agent 1.0 ~ 45 weight portion.Inventor finds, 12 hours long-time slow releasing functions can be realized according to the sodium prasterone sulfate slow releasing capsule of the embodiment of the present invention, improve Drug safety, reduce toxic and side effects, facilitate administration and improve curative effect, effectively can reduce administration number of times simultaneously, improve the compliance of patient, and drug plasma concentration is stablized, there will not be " " peak valley " phenomenon ", be conducive to reducing toxic and side effects, improve curative effect.
According to embodiments of the invention, slow-release material can for being selected from least one in ethyl cellulose, cellulose acetate, Aquacoat, Eudragit RL 100, Eudragit RL PO, Eudragit RL 30D, Eudragit RS 100, Eudragit RS30D, Eudragit NE 30D and Eudragit RD 100.
According to embodiments of the invention, plasticizer for being selected from least one in glycerol, propylene glycol, PEG-4000, PEG-4000, PEG-8 000, Oleum Ricini and dimethyl phthalate, can preferably be selected from least one in PEG-8 000 and glycerol.
According to embodiments of the invention, antiplastering aid is be selected from least one in magnesium stearate, Pulvis Talci, micropowder silica gel and sodium lauryl sulphate, is preferably Pulvis Talci.
According to embodiments of the invention, described binding agent is be selected from least one in PVP-k30, PVP-k90, HPMC, HPC, starch, is preferably PVP-k30.
According to embodiments of the invention, described celphere is be selected from least one in sucrose ball core, starch ball core, microcrystalline Cellulose ball core, lactose ball core, silicon dioxide ball core, hypromellose ball core, citric acid ball core and tartaric acid ball core, is preferably sucrose ball core.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, cellulose acetate 3.6 ~ 24 weight portion, PEG-8 000 0.6 ~ 4.2 weight portion, Pulvis Talci 0.3 ~ 11.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RL 30D 3.5 ~ 47.9 weight portion, PEG-8 0001.0 ~ 4.5 weight portion, Pulvis Talci 0.9 ~ 10.5 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RD 100 2.7 ~ 69.5 weight portion, glycerol 0.3 ~ 0.9 weight portion, Pulvis Talci 1.2 ~ 9.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RS 100 4.7 ~ 39.9 weight portion, PEG-8 0000.8 ~ 4.2 weight portion, Pulvis Talci 1.2 ~ 11.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.
In another aspect of this invention, the invention provides a kind of method preparing foregoing sodium prasterone sulfate slow releasing capsule.According to embodiments of the invention, the method can comprise: (1) utilizes binding agent, is attached on celphere by sodium prasterone sulfate, carries pill core to obtain; (2) described year pill core is carried out sustained release film coat, to obtain pastille slow-release micropill; (3) by described pastille slow-release micropill fill capsule, to obtain described sodium prasterone sulfate slow releasing capsule.Inventor finds, utilize the method fast and effeciently can prepare foregoing sodium prasterone sulfate slow releasing capsule, and step is simple, easy to operate, be applicable to suitability for industrialized production, and the sodium prasterone sulfate slow releasing capsule prepared can realize 12 hours long-time slow releasing functions, improve Drug safety, reduce toxic and side effects, facilitate administration, and raising curative effect, effectively can reduce administration number of times simultaneously, improve the compliance of patient, and drug plasma concentration is stablized, there will not be " " peak valley " phenomenon ", be conducive to reducing toxic and side effects, improve curative effect.
According to embodiments of the invention, step (1) may further include: sodium prasterone sulfate is crossed 80 mesh sieves, the sodium prasterone sulfate after sieving and described celphere is added in centrifugal granulator and carries out pelletize; obtain described year pill core; wherein, aspiration pressure is 0.7bar, and atomizing pressure is 2bar; thimble pressure is 1bar; blanking velocity is 3rpm, and peristaltic pump efficiency is 10%, and rotary speed is 135rpm; spray 8%PVP-k30 solution, baking temperature is 55 DEG C.
According to embodiments of the invention, step (2) may further include: by described year pill core, add in fluid bed and carry out described sustained release film coat, obtain described pastille slow-release micropill, wherein, inlet temperature is 55 DEG C, and temperature of charge is 38 ~ 47 DEG C, atomizing pressure is 1.0bar, hydrojet speed 10ml/min.
The invention provides the slow releasing preparation technology of sodium prasterone sulfate.At least there is following beneficial effect:
1, within one day, only need to take twice medicine, patient complies with;
2, the blood drug level of stable state is provided, maintains Finite Concentration for a long time, thus reduce the toxic and side effects of medicine, improve the safety of medicine and the curative effect of medicine.
Accompanying drawing explanation
Fig. 1 shows according to embodiments of the invention 2, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared;
Fig. 2 shows according to embodiments of the invention 3, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared;
Fig. 3 shows according to embodiments of the invention 4, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared;
Fig. 4 shows according to embodiments of the invention 5, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared;
Fig. 5 shows according to embodiments of the invention 6, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared;
Fig. 6 shows according to embodiments of the invention 7, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared;
Fig. 7 shows according to embodiments of the invention 8, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared;
Fig. 8 shows according to embodiments of the invention 9, the vitro release curve of the sodium prasterone sulfate slow releasing capsule prepared.
Detailed description of the invention
Embodiments of the invention are described below in detail.Embodiment described below is exemplary, only for explaining the present invention, and can not be interpreted as limitation of the present invention.Unreceipted concrete technology or condition in embodiment, according to the technology described by the document in this area or condition or carry out according to product description.Agents useful for same or the unreceipted production firm person of instrument, being can by the conventional products of commercial acquisition.
In one aspect of the invention, the invention provides a kind of sodium prasterone sulfate slow releasing capsule.According to embodiments of the invention, this sodium prasterone sulfate slow releasing capsule comprises: sodium prasterone sulfate 100 weight portion; Celphere 137 weight portion; Plasticizer 0.3 ~ 5.1 weight portion; Slow-release material 2.4 ~ 88 weight portion; Antiplastering aid 0.1 ~ 12 weight portion; And binding agent 1.0 ~ 45 weight portion.Inventor finds, 12 hours long-time slow releasing functions can be realized according to the sodium prasterone sulfate slow releasing capsule of the embodiment of the present invention, improve Drug safety, reduce toxic and side effects, facilitate administration and improve curative effect, effectively can reduce administration number of times simultaneously, improve the compliance of patient, and drug plasma concentration is stablized, there will not be " peak valley " phenomenon ", be conducive to reducing toxic and side effects, improve curative effect.
According to embodiments of the invention, slow-release material can for being selected from least one in ethyl cellulose, cellulose acetate, Aquacoat, Eudragit RL 100, Eudragit RL PO, Eudragit RL 30D, Eudragit RS 100, Eudragit RS30D, Eudragit NE 30D and Eudragit RD 100.Thereby, it is possible to effectively realize the effect of long-time stable slow release, thus effectively avoid occurring " peak valley " phenomenon ", maintain the drug plasma concentration of stable state, and then effectively can reduce toxic and side effects, improve curative effect of medication.
According to embodiments of the invention, plasticizer can for being selected from least one in glycerol, propylene glycol, PEG-4000, PEG-4000, PEG-8 000, Oleum Ricini and dimethyl phthalate.In preferred embodiments more of the present invention, plasticizer can for being selected from least one in PEG-8 000 and glycerol.Thus, the slow release effect improving capsule is conducive to.
According to embodiments of the invention, antiplastering aid is be selected from least one in magnesium stearate, Pulvis Talci, micropowder silica gel and sodium lauryl sulphate.In preferred embodiments more of the present invention, antiplastering aid is Pulvis Talci.Thereby, it is possible to effectively avoid sticking phenomenon.
According to embodiments of the invention, described binding agent is be selected from least one in PVP-k30, PVP-k90, HPMC, HPC, starch.In preferred embodiments more of the present invention, binding agent is PVP-k30.Thereby, it is possible to be conducive to the mouldability improving crude drug.
According to embodiments of the invention, described celphere is be selected from least one in sucrose ball core, starch ball core, microcrystalline Cellulose ball core, lactose ball core, silicon dioxide ball core, hypromellose ball core, citric acid ball core and tartaric acid ball core.Thus, the slow release effect improving sodium prasterone sulfate slow releasing capsule is conducive to.According to a preferred embodiment of the present invention, described celphere is sucrose ball core.Thereby, it is possible to improve the slow release effect of sodium prasterone sulfate slow releasing capsule further.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, cellulose acetate 3.6 ~ 24 weight portion, PEG-8 000 0.6 ~ 4.2 weight portion, Pulvis Talci 0.3 ~ 11.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.Thus, slow release effect is better, can be to realize long-acting release in 12 hours.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RL 30D 3.5 ~ 47.9 weight portion, PEG-8 0001.0 ~ 4.5 weight portion, Pulvis Talci 0.9 ~ 10.5 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.Thus, slow release effect is better, can be to realize long-acting release in 12 hours.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RD 100 2.7 ~ 69.5 weight portion, glycerol 0.3 ~ 0.9 weight portion, Pulvis Talci 1.2 ~ 9.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.Thus, slow release effect is better, can be to realize long-acting release in 12 hours.
According to a particular embodiment of the invention, sodium prasterone sulfate slow releasing capsule can comprise: sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RS 100 4.7 ~ 39.9 weight portion, PEG-8 0000.8 ~ 4.2 weight portion, Pulvis Talci 1.2 ~ 11.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.Thus, slow release effect is better, can be to realize long-acting release in 12 hours.
In another aspect of this invention, the invention provides a kind of method preparing foregoing sodium prasterone sulfate slow releasing capsule.According to embodiments of the invention, the method can comprise the following steps:
(1) utilize binding agent, sodium prasterone sulfate is attached on celphere, carry pill core to obtain.
According to embodiments of the invention, step (1) may further include: sodium prasterone sulfate is crossed 80 mesh sieves, the sodium prasterone sulfate after sieving and described celphere is added in centrifugal granulator and carries out pelletize; obtain described year pill core; wherein, aspiration pressure is 0.7bar, and atomizing pressure is 2bar; thimble pressure is 1bar; blanking velocity is 3rpm, and peristaltic pump efficiency is 10%, and rotary speed is 135rpm; spray 8%PVP-k30 solution, baking temperature is 55 DEG C.
(2) described year pill core is carried out sustained release film coat, to obtain pastille slow-release micropill.
According to embodiments of the invention, step (2) may further include: by described year pill core, add in fluid bed and carry out described sustained release film coat, obtain described pastille slow-release micropill, wherein, inlet temperature is 55 DEG C, and temperature of charge is 38 ~ 47 DEG C, atomizing pressure is 1.0bar, hydrojet speed 10ml/min.
(3) by described pastille slow-release micropill fill capsule, to obtain described sodium prasterone sulfate slow releasing capsule.In this step, any method known in the art can be utilized to carry out capsule fill.
Inventor finds, utilize the method fast and effeciently can prepare foregoing sodium prasterone sulfate slow releasing capsule, and step is simple, easy to operate, be applicable to suitability for industrialized production, and the sodium prasterone sulfate slow releasing capsule prepared can realize 12 hours long-time slow releasing functions, improve Drug safety, reduce toxic and side effects, facilitate administration, and raising curative effect, effectively can reduce administration number of times simultaneously, improve the compliance of patient, and drug plasma concentration is stablized, there will not be " " peak valley " phenomenon ", be conducive to reducing toxic and side effects, improve curative effect.
Embodiment
Following examples feed intake according to 2000 tablet recipe amounts, and specification is 100mg.Following examples are just described, and do not limit invention scope.
Embodiment 1:
In the present embodiment, year pill core has been prepared according to the prescription shown in following table 1 and operating procedure described below:
Preparation method:
Sodium prasterone sulfate is crossed 80 mesh sieves, weigh the sodium prasterone sulfate after sieving and celphere according to the recipe quantity shown in table 1 respectively, utilize centrifugal granulator and fluid bed to carry out pelletize respectively.After pelletize terminates, obtain carrying pill core.
Table 1
Carry pill core preparation technology to investigate:
Investigation fluid bed and centrifugal granulator prepare a year pill core respectively, compare year pill core uniformity of dosage units that two kinds of methods are prepared, the results are shown in Table 2.
Table 2
| Preparation method | Centrifugal granulator | Fluid bed |
| Content | 99.7％ | 98.5％ |
| RSD | 1.2％ | 2.5％ |
The display of above result, due to the difference of specific gravity of raw material and celphere, when adopting fluid bed preparation to carry pill core, the medicament contg uniformity obtained, compared with the difference of centrifugal granulating, therefore selects the method preparation adopting centrifugal granulating to carry a pill core.
Carry pill core prescription screening:
In the present embodiment, investigate mainly for binding agent PVP-k30 consumption, the different differences of carrying the release behavior of pill core when prepared by different amounts PVP-k30 in reference fluid, the results are shown in Table 1.
Result display in table 1, along with the consumption of binding agent increases, the release of carrying pill core 30min in media as well also decreases, but the release of 60min is all close to 100%; Meanwhile, the binder solution of variable concentrations prepare carry pill core also variant on release behavior.What therefore prepared by different binding agent carries the desirable release profile that pill core and different slow release layer coating can obtain wanting.
Embodiment 2:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 150g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity is poured in the hopper of centrifugal granulator after weighing.Celphere is poured in centrifugal granulator and carry out pelletize; aspiration pressure 0.7 is set for bar; atomizing pressure is 2bar; thimble pressure is 1bar; blanking velocity is 3rpm, and peristaltic pump efficiency is 10%, and rotary speed is 135rpm; spray 8%PVP-k30 solution (solvent is 90% ethanol), baking temperature is 55 DEG C.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 1.0bar, hydrojet speed 10ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment as follows: get obtained sodium prasterone sulfate slow releasing capsule according to drug release determination method (Chinese Pharmacopoeia 2010 editions second annex XD first method), with 1% tween pH1.0 hydrochloric acid solution for dissolution medium, rotating speed 100 turns, operation measures in accordance with the law.Sample dilution 10 at 1,4,8 hour respectively and doubly carry out uv measurement, obtained sodium prasterone sulfate slow releasing capsule every is calculated the burst size of 1,2,3,4,6,8,12 hour according to external standard method, draw In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 1.Sodium prasterone sulfate slow releasing capsule every is respectively more than 5% ~ 25%, 50% ~ 70% and 80% of labelled amount for qualified the burst size of 1,4,8 hour.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 3:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 150g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity weighs, and pours in the hopper of centrifugal granulator.Celphere is poured in centrifugal granulator and carry out pelletize, aspiration pressure 0.7bar is set, atomizing pressure 2bar; thimble pressure 1bar, blanking velocity 3rpm, peristaltic pump efficiency 10%; rotary speed 135rpm, spray 8%PVP-k30 solution (solvent is 90% ethanol), 55 DEG C of dryings.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 1.2bar, hydrojet speed 15ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment according to the method for embodiment 1, and draws In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 2.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 4:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 150g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity weighs, and pours in the hopper of centrifugal granulator.Celphere is poured in centrifugal granulator and carry out pelletize, aspiration pressure 0.7bar is set, atomizing pressure 2bar; thimble pressure 1bar, blanking velocity 3rpm, peristaltic pump efficiency 10%; rotary speed 135rpm, spray 8%PVP-k30 solution (solvent is 90% ethanol), 55 DEG C of dryings.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 1.2bar, hydrojet speed 10ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment according to the method for embodiment 1, and draws In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 3.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 5:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 140g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity weighs, and pours in the hopper of centrifugal granulator.Celphere is poured in centrifugal granulator and carry out pelletize, aspiration pressure 0.7bar is set, atomizing pressure 2bar; thimble pressure 1bar, blanking velocity 3rpm, peristaltic pump efficiency 10%; rotary speed 135rpm, spray 7%PVP-k30 solution (solvent is 90% ethanol), 55 DEG C of dryings.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 1.0bar, hydrojet speed 15ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment according to the method for embodiment 1, and draws In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 4.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 6:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 140g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity weighs, and pours in the hopper of centrifugal granulator.Celphere is poured in centrifugal granulator and carry out pelletize, aspiration pressure 0.7bar is set, atomizing pressure 2bar; thimble pressure 1bar, blanking velocity 3rpm, peristaltic pump efficiency 10%; rotary speed 135rpm, spray 7%PVP-k30 solution (solvent is 90% ethanol), 55 DEG C of dryings.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 1.0bar, hydrojet speed 15ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment according to the method for embodiment 1, and draws In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 5.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 7:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 140g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity weighs, and pours in the hopper of centrifugal granulator.Celphere is poured in centrifugal granulator and carry out pelletize, aspiration pressure 0.7bar, atomizing pressure 2bar; thimble pressure 1bar, blanking velocity 3rpm, peristaltic pump efficiency 10%; rotary speed 135rpm, spray 7%PVP-k30 solution (solvent is 90% ethanol), 55 DEG C of dryings.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 1.2bar, hydrojet speed 20ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment according to the method for embodiment 1, and draws In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 6.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 8:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 170g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity weighs, and pours in the hopper of centrifugal granulator.Celphere is poured in centrifugal granulator and carry out pelletize, aspiration pressure 0.7bar is set, atomizing pressure 2bar; thimble pressure 1bar, blanking velocity 3rpm, peristaltic pump efficiency 10%; rotary speed 135rpm, spray 7%PVP-k30 solution (solvent is 90% ethanol), 55 DEG C of dryings.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 1.0bar, hydrojet speed 15ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment according to the method for embodiment 1, and draws In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 7.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 9:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 170g
Preparation technology:
Sodium prasterone sulfate is crossed 80 mesh sieves, recipe quantity weighs, and pours in the hopper of centrifugal granulator.Celphere is poured in centrifugal granulator and carry out pelletize, aspiration pressure 0.7bar, atomizing pressure 2bar; thimble pressure 1bar, blanking velocity 3rpm, peristaltic pump efficiency 10%; rotary speed 135rpm, spray 7%PVP-k30 solution (solvent is 90% ethanol), 55 DEG C of dryings.After pelletize terminates, obtain carrying pill core and be about 480g.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology:
By year pill core of recipe quantity, add in fluid bed.Open fluid bed, arrange inlet temperature 55 DEG C, temperature of charge 38 ~ 47 DEG C, atomizing pressure 0.8bar, hydrojet speed 15ml/min, coating terminates rear obtained pastille slow-release micropill.Then, get product the pastille slow-release micropill fill capsule prepared preparation, i.e. sodium prasterone sulfate slow releasing capsule.
Above-mentioned obtained sodium prasterone sulfate slow releasing capsule is carried out dissolution in vitro experiment according to the method for embodiment 1, and draws In-vitro release curves, the In-vitro release curves obtained is shown in Fig. 8.From vitro release experimental result, obtained sodium prasterone sulfate slow releasing capsule has stronger slow releasing effect in drug release behavior in vitro.
Embodiment 10:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 150g
Preparation technology: with embodiment 2.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 2.
Embodiment 11:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 150g
Preparation technology: with embodiment 3.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 3.
Embodiment 12:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 150g
Preparation technology: with embodiment 4.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 4.
Embodiment 13:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 140g
Preparation technology: with embodiment 5.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 5.
Embodiment 14:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 140g
Preparation technology: with embodiment 6.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 6.
Embodiment 15:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 140g
Preparation technology: with embodiment 7.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 7.
Embodiment 16:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
8%PVP-k30 solution (solvent is 90% ethanol) 170g
Preparation technology: with embodiment 8.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 8.
Embodiment 17:
1. the preparation of pill core is carried
Prescription:
Sodium prasterone sulfate 200g
Celphere (sucrose ball core) 274g
7%PVP-k30 solution (solvent is 90% ethanol) 170g
Preparation technology: with embodiment 9.
2. pill core slow release layer coating is carried
Prescription:
Preparation technology: with embodiment 9.
In like manner, prepare gained sodium prasterone sulfate slow releasing capsule described in embodiment of the present invention 10-embodiment 17, it all has stronger slow releasing effect in drug release behavior in vitro.
In the description of this description, specific features, structure, material or feature that the description of reference term " embodiment ", " some embodiments ", " example ", " concrete example " or " some examples " etc. means to describe in conjunction with this embodiment or example are contained at least one embodiment of the present invention or example.In this manual, to the schematic representation of above-mentioned term not must for be identical embodiment or example.And the specific features of description, structure, material or feature can combine in one or more embodiment in office or example in an appropriate manner.In addition, when not conflicting, the feature of the different embodiment described in this description or example and different embodiment or example can carry out combining and combining by those skilled in the art.
Although illustrate and describe embodiments of the invention above, be understandable that, above-described embodiment is exemplary, can not be interpreted as limitation of the present invention, and those of ordinary skill in the art can change above-described embodiment within the scope of the invention, revises, replace and modification.
Claims (10)
1. a sodium prasterone sulfate slow releasing capsule, is characterized in that, comprising:
Sodium prasterone sulfate 100 weight portion;
Celphere 137 weight portion;
Plasticizer 0.3 ~ 5.1 weight portion;
Slow-release material 2.4 ~ 88 weight portion;
Antiplastering aid 0.1 ~ 12 weight portion; And
Binding agent 1.0 ~ 45 weight portion.
2. sodium prasterone sulfate slow releasing capsule according to claim 1, it is characterized in that, described slow-release material is be selected from least one in ethyl cellulose, cellulose acetate, Aquacoat, Eudragit RL 100, Eudragit RL PO, EudragitRL 30D, Eudragit RS 100, Eudragit RS 30D, Eudragit NE 30D and Eudragit RD 100.
3. sodium prasterone sulfate slow releasing capsule according to claim 1, it is characterized in that, described plasticizer is be selected from least one in glycerol, propylene glycol, PEG-4000, PEG-4000, PEG-8 000, Oleum Ricini and dimethyl phthalate, is preferably selected from least one in PEG-8 000 and glycerol.
4. sodium prasterone sulfate slow releasing capsule according to claim 1, is characterized in that, described antiplastering aid is be selected from least one in magnesium stearate, Pulvis Talci, micropowder silica gel and sodium lauryl sulphate, is preferably Pulvis Talci.
5. sodium prasterone sulfate slow releasing capsule according to claim 1, is characterized in that, described binding agent is be selected from least one in PVP-k30, PVP-k90, HPMC, HPC, starch, is preferably PVP-k30.
6. sodium prasterone sulfate slow releasing capsule according to claim 1, it is characterized in that, described celphere is be selected from least one in sucrose ball core, starch ball core, microcrystalline Cellulose ball core, lactose ball core, silicon dioxide ball core, hypromellose ball core, citric acid ball core and tartaric acid ball core, is preferably sucrose ball core.
7. the sodium prasterone sulfate slow releasing capsule according to any one of claim 1-6, is characterized in that, comprises one of following:
Sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, cellulose acetate 3.6 ~ 24 weight portion, PEG-8 0000.6 ~ 4.2 weight portion, Pulvis Talci 0.3 ~ 11.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion;
Sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RL 30D 3.5 ~ 47.9 weight portion, PEG-8 0001.0 ~ 4.5 weight portion, Pulvis Talci 0.9 ~ 10.5 weight portion, and described binding agent 4.9 ~ 6.8 weight portion;
Sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RD 1002.7 ~ 69.5 weight portion, glycerol 0.3 ~ 0.9 weight portion, Pulvis Talci 1.2 ~ 9.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion;
Sodium prasterone sulfate 100 weight portion, described celphere 137 weight portion, Eudragit RS 1004.7 ~ 39.9 weight portion, PEG-8 0000.8 ~ 4.2 weight portion, Pulvis Talci 1.2 ~ 11.7 weight portion, and described binding agent 4.9 ~ 6.8 weight portion.
8. prepare a method for the sodium prasterone sulfate slow releasing capsule in claim 1-7 described in any one, it is characterized in that, comprising:
(1) utilize binding agent, sodium prasterone sulfate is attached on celphere, carry pill core to obtain;
(2) described year pill core is carried out sustained release film coat, to obtain pastille slow-release micropill;
(3) by described pastille slow-release micropill fill capsule, to obtain described sodium prasterone sulfate slow releasing capsule.
9. method according to claim 8, is characterized in that, described step (1) comprises further:
Sodium prasterone sulfate is crossed 80 mesh sieves, the sodium prasterone sulfate after sieving and described celphere is added in centrifugal granulator and carries out pelletize, obtain describedly carrying pill core,
Wherein, aspiration pressure is 0.7bar, and atomizing pressure is 2bar, and thimble pressure is 1bar, and blanking velocity is 3rpm, and peristaltic pump efficiency is 10%, and rotary speed is 135rpm, and spray 7%-8%PVP-k30 solution, baking temperature is 55 DEG C.
10. method according to claim 8, is characterized in that, described step (2) comprises further:
By described year pill core, add in fluid bed and carry out described sustained release film coat, obtain described pastille slow-release micropill,
Wherein, inlet temperature is 55 DEG C, and temperature of charge is 38 ~ 47 DEG C, and atomizing pressure is 0.8-1.2bar, hydrojet speed 10-20ml/min.
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| CN201510305048.8A CN104983717A (en) | 2015-06-04 | 2015-06-04 | Sodium prasterone sulfate sustained-release capsule and preparation method thereof |
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| CN201510305048.8A CN104983717A (en) | 2015-06-04 | 2015-06-04 | Sodium prasterone sulfate sustained-release capsule and preparation method thereof |
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Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1395924A (en) * | 2002-08-26 | 2003-02-12 | 鲁南制药股份有限公司 | Slow-releasing Anixidan capsule |
| CN1509719A (en) * | 2002-12-25 | 2004-07-07 | 庞 飞 | Medicine for treating climacteric syndrome |
| CN1887278A (en) * | 2006-07-25 | 2007-01-03 | 山东省医药工业研究所 | Slow released doxazosin mesilate capsule and its prepn process |
| CN102429912A (en) * | 2011-10-26 | 2012-05-02 | 庞飞 | Pharmaceutical composition prepared with micronized prasterone or sodium prasterone sulfate and use thereof |
| CN102552035A (en) * | 2012-02-04 | 2012-07-11 | 安徽山河药用辅料股份有限公司 | Method for preparing pharmaceutic adjuvant and pellet cores via microcrystalline cellulose and starch by aid of physical mixing method |
-
2015
- 2015-06-04 CN CN201510305048.8A patent/CN104983717A/en active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1395924A (en) * | 2002-08-26 | 2003-02-12 | 鲁南制药股份有限公司 | Slow-releasing Anixidan capsule |
| CN1509719A (en) * | 2002-12-25 | 2004-07-07 | 庞 飞 | Medicine for treating climacteric syndrome |
| CN1887278A (en) * | 2006-07-25 | 2007-01-03 | 山东省医药工业研究所 | Slow released doxazosin mesilate capsule and its prepn process |
| CN102429912A (en) * | 2011-10-26 | 2012-05-02 | 庞飞 | Pharmaceutical composition prepared with micronized prasterone or sodium prasterone sulfate and use thereof |
| CN102552035A (en) * | 2012-02-04 | 2012-07-11 | 安徽山河药用辅料股份有限公司 | Method for preparing pharmaceutic adjuvant and pellet cores via microcrystalline cellulose and starch by aid of physical mixing method |
Non-Patent Citations (1)
| Title |
|---|
| 孟彦 等: "硫酸普拉睾酮钠胶囊处方及工艺的研究", 《齐鲁药事》 * |
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