Controlled-release solid preparation with partial coating
Disclosed is a controlled-release solid preparation, which consists of an internal core and a coating layer, wherein part of the surface of the internal core is not covered with the coating, and is exposed to the surface of the solid preparation. Since the medicament just releases at the exposed part, the aim of controlled release can be achieved by controlling this exposed surface area.
1. A controlled-release solid preparation, being a tablet and consisting of an inner core and a coating layer, said inner core containing an active medicine and an adjuvant, said coating layer containing a sustained release/controlled release material, said coating layer containing or not containing active medicine, characterized in that, a part of the top surface of said inner core is not coated by said coating layer and the bottom and side surfaces of said inner core are coated by said coating layer, and wherein the material of said coating layer is water-insoluble and comprises one or more selected from the group consisting of ethyl cellulose, a cellulose acetate polymer, and an acrylic resin,
the material of coating layer also contains water-soluble pore-forming agent, which is selected from one or several of the groups consisting of povidone, lactose, sodium chloride.
2. The solid preparation according to claim 1 , wherein said inner core is one layer or multi-layers, and said layer is a sustained release layer, or contains both a rapid release layer and a sustained release layer; and wherein when said inner core is two or more layers, components of different layers release in sequence: the outermost layer releases first, then the secondary outer layer releases, then at last the component of the innermost layer of said inner core releases.
3. The solid preparation according to claim 1 , said coating layer is prepared by compression coating method.
4. The solid preparation according to claim 1 , which comprises another coating layer on the outer surface of said coating layer, wherein said another coating layer contains or does not contain active ingredients.
5. The solid preparation according to claim 1 , wherein said inner core is a tablet core consisting of one layer or more than one layer of tablet.
6. The solid preparation according to claim 1 , said inner core has one layer; said layer is sustained release layer; wherein components and contents of said sustained release layer in per 1000 tablets are as follows:
ibuprofen 75 g, hydroxypropyl methyl cellulose K100LV 45-75 g, Methyl cellulose 15 g, lactose 129 g, magnesium stearate 3 g, micro powder silica gel 3 g;
components and contents of said coating layer in per 1000 tablets are as follows:
ethyl cellulose 390-465 g, lactose 250-150 g, magnesium stearate 5 g, micro powder silica gel 5 g.
7. The solid preparation according to claim 1 , said inner core has one layer; said layer is sustained release layer; wherein components and contents of said sustained release layer in per 1000 tablets are as follows:
aripiprazole 15 g, sodium alginate 105 g, hydroxypropyl cellulose 15 g, lactose 159 g, magnesium stearate 3 g, micro powder silica gel 3 g;
components and contents of said coating layer in per 1000 tablets are as follows:
aripiprazole 5 g, hydroxypropyl methyl cellulose K100LV 170 g, lactose 315 g, magnesium stearate 5 g, micro powder silica gel 5 g.
8. The solid preparation according to claim 1 , said inner core has two layers; components of different layers release in sequence: outermost layer releases first, then innermost layer releases; said outermost layer is sustained release layer; innermost layer is rapid release layer; wherein components and contents of said sustained release layer in per 1000 tablets are as follows: prednisolone acetate 20 g, hydroxypropyl methyl cellulose K4M 60 g, lactose 116 g, magnesium stearate 2 g, micro powder silica gel 2 g;
components and contents of said rapid release layer in per 1000 tablets are as follows:
prednisolone acetate 10 g, lactose 40 g, microcrystalline cellulose 44 g, cross-linked sodium carboxymethyl cellulose 5 g, lemon yellow 0.3 g, magnesium stearate 0.7 g;
components and contents of said coating layer in per 1000 tablets are as follows:
ethyl cellulose 390 g, lactose 100 g, magnesium stearate 5 g, micro powder silica gel 5 g.
9. The solid preparation according to claim 1 , said inner core has two layers; components of different layers release in sequence: outermost layer releases first, then innermost layer releases; said outermost layer is sustained release layer 1; innermost layer is sustained release layer 2; wherein components and contents of said sustained release layer 1 in per 1000 tablets are as follows: Lamotrigine 30 g, Hydroxypropyl methyl cellulose K4M 37.5 g, lactose 79.5 g, magnesium stearate 1.5 g, micro powder silica gel 1.5 g;
components and contents of said sustained release layer 2 in per 1000 tablets are as follows: Lamotrigine 30 g, Hydroxypropyl methyl cellulose K100LV 52.5 g, lactose 66 g, natural food color 0.15 g, magnesium stearate 1.05 g;
components and contents of said coating layer in per 1000 tablets are as follows:
ethyl cellulose 390 g, lactose 100 g, magnesium stearate 5 g, micro powder silica gel 5 g.
10. The solid preparation according to claim 2 , which comprises another coating layer on the outer surface of said coating layer, wherein said another coating layer contains or does not contain active ingredients.
11. The solid preparation according to claim 3 , which comprises another coating layer on the outer surface of said coating layer, wherein said another coating layer contains or does not contain active ingredients.
12. The solid preparation according to claim 2 , wherein said inner core contains multiple layers including both a rapid release layer and a sustained release layer.
13. The solid preparation according to claim 2 , wherein said inner core contains multiple layers, and components of different layers release in sequence: the outermost layer releases first, then the secondary outer layer releases, then at last the component of the innermost layer of said inner core releases.
14. The solid preparation according to claim 1 , wherein the tablet is prepared in a tablet press machine by using two punch pins of different sizes, by following steps:
1) mixing all the components for preparing the inner core, and the first pressing is performed by using model number I punch pin to obtain the inner core;
2) putting the inner core in the center of a middle module firstly, then filing the uniformly mixed coating layer components around the inner core and performing the second pressing by using model number II punch pin,
wherein the diameter of the model number I punch pin is less than that of model number II punch pin.
15. The solid preparation according to claim 1 , wherein the coating layer weight is more than that of inner core in the tablet.
16. The solid preparation according to claim 1 , wherein weight ratio between the inner core and coating layer is 3:5.
17. The solid preparation according to claim 1 , said coating layer contains 5-30%, 20-30% or 20% weight ratio water-soluble pore-forming agent.