Hypromellose hollow capsule introduction


Brief Introduction of Hypromellose 1. Hollow Capsules

Hypromellose hollow capsule is a hollow hard capsule made of hypromellose plus excipients. Hypromellose is2-Hydroxypropyl ether methyl cellulose with a relative molecular weight86000It is made of cotton wool or wood pulp fiber treated with caustic soda, and then etherified with propylene oxide, chlorinated alkane and alkali cellulose. According to the addition of gelling agents, hydroxypropyl methylcellulose hollow capsules can be divided into two categories: with gelling agents and without gelling agents. Hypromellose does not have gel properties, and most manufacturers of hypromellose hollow capsules adopt the method of adding gelling agents (such as carrageenan, gellan gum, sodium alginate, etc.) to hypromellose solution to prepare hollow capsule products. However, the gelling agent is susceptible to the dissolution of the medium.PHOr the influence of metal ions, in the simulated in vitro dissolution test, the dissolution rate of capsules in different dissolution media will slow down, affecting the dissolution rate of the contents. Hypromellose hollow capsules without gelling agent can dissolve quickly and release drugs in different dissolution media. Currently on the market in the absence of gelling agent of hydroxypropyl cellulose hollow capsule products onlyCapsugelofVcaps®MoreHelifan CapsuleLefancaps®ofH-caps®-Pure.

2. hydroxypropyl cellulose hollow capsule advantage

Hypromellose hollow capsules have the following advantages: (1) The capsule has low moisture content, and the moisture content reaches1%It will not become brittle, and regional environmental differences have little effect on hydroxypropyl methylcellulose hollow capsules, which is more suitable for filling hygroscopic and moisture-sensitive drugs or functional foods. (2) The dissolution rate of the capsule without gelling agent is affected by temperature and dissolution medium.pHLess impact. (3) Hypromellose is a partial methyl and partial polyhydroxypropyl ether of cellulose. It has stable chemical properties, no risk of cross-linking reaction or Maillard reaction, no interaction with the contents, and will not cause hypromellose hollow capsules. Delayed disintegration, relatively stable drug release rate, can be widely used. (4) Capsule electrostatic effect is small or no electrostatic effect, the contents of electrostatic adsorption is small, more conducive to the filling of drugs. (5) Hypromellose has good affinity with most polymer materials. The coating material is easy to adhere to the capsule and has good uniformity. It can be coated with water and organic solvents such as ethanol. It is especially suitable for the preparation of slow-release coated capsules. (6) Hypromellose hollow capsules have a low incidence of fragments, strong moisture resistance and good stability. From a safety point of view, they are more suitable for inhalation than gelatin hollow capsules. (7) Hypromellose hollow capsule has less adhesion to esophagus than gelatin hollow capsule. When patients take Hypromellose hollow capsule, foreign body sensation and other adverse reactions are less, and the patient's medication compliance is improved. (8) Low storage conditions, low humidity environment is almost not brittle, good stability at high temperature, not easy to stick. (9) Plant origin, no risk of animal-derived diseases, can meet the needs of people with special religious beliefs and vegetarians.

Dissolution Test of Hypromellose Hollow Capsule of 3. Lifan Capsule

Lifan capsules are currently available.H-caps ®(with gelling agent) andH-caps ®-Pure(no gelling agent) two kinds of hydroxypropyl methylcellulose hollow capsule products, the dissolution of the above two products were measured, the results showed that,H-caps ®Dissolution rate of Hollow Capsules of HypromellosepHand metal salt ions have a greater impact;H-caps ®-PureDissolution rate of hypromellose hollow capsules was not affectedpHand metal salt ions.

1.Test Method

Take0.25gCefradine is filled into gelatin hollow capsules, respectively,H-caps ®Hollow capsules of hypromellose andH-caps ®-PureHypromellose in hollow capsules. According to the Pharmacopoeia of the People's Republic of China2020The requirements under the annual version of the two cefradine capsules, respectively, test the above-mentioned finished drug capsules in purified water,pH 1.2Hydrochloric acid solution,pH 4.5potassium dihydrogen phosphate solution andpH 6.0Dissolution data in potassium dihydrogen phosphate solution.

2.analysis of results

(1) in purified water, gelatin hollow capsules,H-caps ®Hypromellose hollow capsules (type I and type II) andH-caps ®-PureComparison of dissolution curves of hydroxypropyl methylcellulose hollow capsules (type III).

(2)pH 1.2 hydrochloric acid solution, gelatin hollow capsules, H-caps®Hypromellose hollow capsules (type I and type II) and H-caps®-Comparison of dissolution curves of Pure Hallocellulose Hollow Capsules (Type III).

(3)pH 4.5 potassium dihydrogen phosphate solution, gelatin hollow capsules, H-caps®Hypromellose hollow capsules (type I and type II) and H-caps®-Comparison of dissolution curves of Pure Hallocellulose Hollow Capsules (Type III).

(4)pH 6.0 potassium dihydrogen phosphate solution, gelatin hollow capsules, H-caps®Hypromellose hollow capsules (type I and type II) and H-caps®-Comparison of dissolution curves of Pure Hallocellulose Hollow Capsules (Type III).

Dissolution test results show that: H-caps®The dissolution rate of HPMC hollow capsules was greatly affected by pH and metal salt ions. H-caps®-Pure hydroxypropyl methylcellulose hollow capsules do not contain gel, so it has a similar dissolution curve with gelatin hollow capsules, and the dissolution rate is not affected by pH and metal salt ions, and has a faster release rate in different dissolution media.

 

Hollow capsule H-caps of hypromellose without gel®-Pure is consistent under different dissolution conditions and is more suitable for the use of chemicals. Among the varieties that have been listed in the world, there are darafenib capsules, lenvatinib capsules, dabigaturate mesylate capsules, adefovir dipivoxil capsules, etc. that use hollow capsules without gelling agent hypromellose. We are familiar with various prazole products, such as omeprazole, esomeprazole, dexlansoprazole, rabeprazole, pantoprazole products are all proton pump inhibitors. In general, these drugs have two very obvious characteristics:(1) sensitive to moisture;(2) unstable in acidic conditions. So hydroxypropyl methyl cellulose hollow capsule is the best choice for this class of drugs. Merck is currently developing a treatment for the new coronavirus.Monuprovir capsules, which are also hollow capsules of hypromellose using no gelling agent.

 

The future development trend of 4. hypromellose

Although hydroxypropyl methylcellulose hollow capsules without gelling agents have similar solubility, disintegration and bioavailability to gelatin hollow capsules, and have some advantages that gelatin hollow capsules do not have, they are still not widely used at present. One of the main reasons is the high cost of hydroxypropyl methylcellulose raw materials, resulting in high product prices. At the same time, due to technical barriers, the process technology of hydroxypropyl cellulose hollow capsules without gelling agents is difficult, and there are very few manufacturers that can produce at present, which limits the application of hydroxypropyl cellulose hollow capsules in pharmaceutical preparations. Hydroxypropyl cellulose hollow capsules developed by Jiangsu Lifan Capsule Co., Ltd. (H-caps®和H-caps®-Pure) can be customized according to the user's demand for formulation dissolution.

Although the current hypromellose hollow capsule product sales in the international capsule market only accounted for about 10% share, but its development momentum is very strong. With the change of people's life concept and the penetration of pure natural concept, hydroxypropyl methyl cellulose hollow capsule will be more and more concerned by people, and consumers are more inclined to pursue green and healthy capsule products. Hypromellose hollow capsules have the potential to replace gelatin hollow capsules. It is expected that in the next few years, hypromellose hollow capsules will form a new situation of competition with gelatin hollow capsules. Its market growth space is very broad and can better meet people's dietary requirements and market needs. It will have a strong development prospect in the capsule field.

 

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